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AMH Summary: Chapter 1 – Allergy and Anaphylaxis 1

AMH SUMMARY
CHAPTER 1: ALLERGY & ANAPHYLAXIS

A. ANAPHYLACTIC REACTIONS

GENERAL
• Severe reactions which can be life threatening
• Involves symptoms such as urticaria, angioedema, hypotension
• Fatalities often occur from respiratory obstruction due to upper airway oedema or
bronchospasm
• Triggers include foods, drugs, stings, blood products
• Appearance of symptoms can come in minutes to several hours of exposure

TREATMENT
• Adrenaline is used for first suspicion of anaphylaxis, usually injected into the thigh when
anaphylaxis occurs
• IV fluids restore blood pressure in combination with adrenaline
• Bronchodilators such as beta2 agonists may help in relieving bronchospasm
• Glucagon may help in persistent hypotension in patients on beta blockers
• Corticosteroids have a delayed effect and are used to reduce duration of reaction and
prevent relapse

B. MODERATE ALLERGIC REACTIONS

ANTIHISTAMINES
• Sedating (cyproheptadine, dexchlorpeniramine, dimenhydrinate, doxylamine, pheniramine,
promethazine, trimeprazine)
• Non sedating (cetirizine, desloratidine, fexofenadine, loratidine)
• Antagonists of histamine at H1 receptors, reducing vasodilation and capillary permeability
• Patient response to specific antihistamines varies, trialling a few antihistamines may be
required to determine the most effective agent
• Used for chronic urticaria and angioedema
• Also reduces itch, number, size and duration of urticarial lesions
• Adverse effects include drowsiness, more pronounced in sedating antihistamines such as
doxylamine and promethazine
• Other effects include dizziness, tinnitus
• Less sedating antihistamines can cause drowsiness, but not as much as sedating ones
• Cetirizine more likely to cause sedation in comparison to less sedating antihistamines

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AMH Summary: Chapter 1 – Allergy and Anaphylaxis 2

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 3 – Analgesics 1

AMH SUMMARY: CHAPTER 3 – ANALGESICS


PAIN CHRONIC PAIN

Route of administration Neuropathic pain


• Oral: Conventional release, controlled release, soluble or effervescent, • Antidepressants: Nortriptyline is more tolerable than amitriptyline.
transmucosal lozenges SSRIs are less effective than TCAs but have a lower incidence of
• Parenteral: SC administration is used in acute and chronic pain where adverse effects.
as IV administration should only be for acute, severe pain. IM • Antiepileptics: Carbamazepine is the drug of choice for trigeminal
administration is not favoured as it is painful and absorption may be neuralgia. Pregabalin and gabapentin may also be used for
erratic. PCA is also available. neuropathic pain.
• Other: Transdermal patches, epidural, intrathecal or regional nerve • Other: Opioids, lignocaine, ketamine, topical capsaicin.
blockade, rectal, inhaled nitrous oxide. Patches are not recommended
for acute pain due to slow onset of action. They are not suitable for Cancer pain
opioid naïve patients with chronic non-cancer pain due to inflexibility of • Treatment: Opioids, antiepileptics, TCAs, local anaesthetics,
dosage and risk of overdose. ketamine, clonidine
• Metastatic bone pain: Radiotherapy, bisphosphonates, NSAIDs,
ACUTE PAIN dexamethasone, radioactive strontium-89
• Pain due to inflammation and oedema in confined spaces:
Renal and biliary colic Dexamethasone may be used.
• Parenteral NSAIDs and opioids
Breakthrough and incident pain
Acute herpes zoster • For incident pain, use NSAIDs or short acting opioid half an hour prior
• The antiviral agents, aciclovir, famciclovir and valaciclovir, relieve the to exertion of strenuous activity. Nitrous oxide and oxygen may also be
acute pain of herpes zoster. If taken within 3 days of when the rash used during movement.
first appears, it may reduce the duration of post-herpetic neuralgia.
Opioids and amitriptyline may also be used.

NON-OPIOID ANALGESICS

Generic name Brand name Side effects Precautions Other comments


Aspirin Solprin • GI ulceration, • HF, HT • Black stools, difficulty breath, swollen ankles are serious adverse effects.
bleeding time • Asthma Immediately seek medical attention if you notice any of these signs.
• Peptic ulcer • Where possible, temporarily cease aspirin a week prior to surgical and dental
• Gout procedures.
• Surgery • Reye’s syndrome: Avoid use of aspirin in children < 12 years and in those aged 12-
(bleeding risk) 16 years with chicken pox, influenza or fever.
• Enteric coated formulations do not reduce the risk of GI ulceration
+
Paracetamol Panadol • transaminases • Na restriction for • Paracetamol has fewer adverse effects compared to NSAIDS
soluble products • Do not take more than 4g daily

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AMH Summary: Chapter 3 – Analgesics 2

OPIOID ANALGESICS

Common adverse effects • Controlled release preparations should not be crushed because this
• Nausea and vomiting, dizziness, drowsiness, constipation, urinary can lead to more rapid and unpredictable absorption
retention, respiratory depression • Do not cut or divide patches
• Sufentanil, remifentanil, alfentanil are shorter acting derivatives of
Counselling fentanyl used for analgesia during anaesthesia
• L1, L16* • Naloxone is used to reverse opioid sedation

Practice points Comparative information


• Morphine is the preferred opioid analgesic for mod-severe pain. • When changing opioid, start at half of the approximate equianalgesic
• For the treatment of constipation in patients on opioids for a long-term dose; then titrate as required
basis, recommend a stimulant laxative (eg docusate with senna) or an • Ensure you are familiar with how to use the opioid comparative
osmotic laxative (eg sorbitol) information table in Chapter 3 of the AMH

Generic name Brand name and strength Other comments


Dextroproproxyphene Di-gesic (tab) • Dosage: 2 q4h prn max 8
• Avoid use in renal impairment
• Avoid regular use due to accumulation of parent compound and cardiotoxic metabolite

Tramadol Tramal 50 mg (cap) • Used for moderate pain or neuropathic pain


Tramal SR 50, 100, 150, 200 mg • Has lower risk of constipation compared to other opioids
(12 hr controlled release tab) • Naloxone only partially antagonises tramadol. Use with caution in patients with epilepsy due to an
Durotram XR increased risk of seizures in tramadol overdose.
(24 hr controlled release tab)
Codeine Codeine phosphate 30 mg (tab) • Dosage: 30-60mg q4h prn. Max 240mg daily
Codeine linctus 5 mg/mL (liq)

Oxycodone Endone 5 mg (tab) • Controlled release tablets should not be used for initial stabilisation.
Oxycontin 5, 10, 20, 40, 80 mg (tab) • When switching from another opioid to oxycodone, calculate the equianalgesic dose, halve this
OxyNorm 5, 10, 20 mg (cap) number and titrate the dose upwards until an effective daily dose is established. Once this is done,
OxyNorm liquid 1 mg/mL (liq) divide the total daily dose in 2 and give controlled release product every 12 hours.
Proladone (supp) • Suppositories have slower onset and longer effect than conventional tablets.

* L1 stands for ancillary label 1 and L16 stands for ancillary label 16

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AMH Summary: Chapter 3 – Analgesics 3

Generic name Brand name and strength Other comments


Buprenorphine Norspan 5, 10, 15 g/hr (patch) Patch
Temgesic 200 g (tab) • Dosage: 5mcg/hr patch initially and titrate dose.
Temgesic 300 g/mL (inj) • Apply to dry, hairless skin on torso. Note the date and time of application. Remove after a week and
apply a new patch on a different area. Patches must not be cut or divided.
• Ensure the patch does not come into contact with direct sources of heat such as electric blankets,
heat pads, heat lamps, saunas.
• Do not wear >2 patches at any time. Max dose 2 x 20mcg/hr patches.
• Do not dose at intervals of <3 days since it takes 3 days to reach steady state after applying a
patch
• An alternative opioid should not be initiated until 24 hours after last patch has been removed.
• Buprenorphine is a partial agonist. Its effect is not reversed by naloxone in usual doses.

Sublingual
• Dosage: 200-400mcg tds prn
• Place tablet under the tongue and keep in place until dissolved. Do not chew or swallow tablet.

Fentanyl Durogesic 12, 25, 50, 75 , 100 g/hr • Can be used in severe renal impairment since it has no active or toxic metabolites
Actiq 200, 400, 600, 800 g (loz)
Fentanyl 50 g/mL (inj) Patch (for chronic pain)
• Dosage: Use one patch every 3 days
• Do not use in opioid-naïve patients
• Apply to dry, hairless, skin on the upper part of your body. Note the date and time of application.
Remove after 3 days and apply a new patch on a different place.
• Ensure the patch does not come into contact with direct sources of heat such as electric blankets,
heat pads, heat lamps, saunas.
• Do not use patch for postoperative and other acute pain because of risk of life-threatening
respiratory depression
• The maximum effect can be seen within 24-72 hours.
• 40-50% of the fentanyl dose remains in the patch. Dispose used patches appropriately.

Lozenge (for breakthrough pain)


• Dosage: Initially 200mcg, repeat in 30 minutes if required. If >4 breakthrough doses are required
per day, adjust the regular opioid dose
• Place in the mouth against the cheek and move it around the mouth using the applicator. Let it
dissolve for 15 minutes.

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AMH Summary: Chapter 3 – Analgesics 4

Generic name Brand name and strength Other comments


Fentanyl (cont.) Subcutaneous
• Dosage: Calculate equivalent 24-hr fentanyl dose
• SC fentanyl is not recommended for acute pain
• Fentanyl injection should not be used sublingually for breakthrough pain.

1
Morphine MS Contin 5, 10, 15, 30, 60, 100, • For breakthrough pain, use additional doses of morphine liquid. As a rule, /6 of the total daily dose
200 mg (tab) may be given as often as needed. If repeated breakthrough doses are required, adjust regular
Kapanol 10, 20, 50, 100 mg (cap) morphine dose.
MS Mono 30, 60, 90, 120 mg (cap) • For maintenance dosing
Ordine1, 2, 5, 10 mg/mL (liq) - Use MS Contin controlled release tablet or controlled release liquid twice daily. The total daily
MS Contin suspension 20, 30, 60, dose should be determined using the oral liquid first
100, 200 mg (liq) - Use Kapanol controlled release capsule once to twice daily, or MS Mono once daily. The total
Morphine sulfate injections daily dose should be determined using the oral liquid first.
1
Anamorph 30 mg (tab) - For SC infusions, calculate the total daily oral dose of morphine and give /3 by SC infusion over
Sevredol 10, 20 mg (tab) 24 hours
• Controlled release tablets must be swallowed whole. They should not be crushed or chewed.
• Pellets in controlled release capsules may be sprinkled on soft food or mixed with 30mL liquid. Take
within 30 mins for Kapanol or 60 mins for MS Mono. Pellets should not be crushed or chewed.

Pethidine Pethidine (inj) • Not recommended for migraine treatment due to short duration of action
• Do not use naloxone for norpethidine toxicity
1 1
Hydromorphine Dilaudid 2, 4, 8 mg • For breakthrough pain, use a dose equivalent to /12 to /6 the usual total daily dose.
Dilaudid 1 mg/mL (liq)

Methadone Physeptone 10 mg (tab) • Not for acute pain (high bioavailability, long half-life)
Methadone 5mg/mL (liq)

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AMH Summary: Chapter 3 – Analgesics 5

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 4 – Antidotes and Antivenoms 1

AMH SUMMARY
CHAPTER 4: ANTIDOTES & ANTIVENOMS

GI DECONTAMINATION ANTIVENOMS

Mainly indicated if within 2 hours of poisoning Box jellyfish antivenom


• Douse adherent jellyfish tentacles with
Activated charcoal vinegar to minimise further damage from
• Most effective decontaminant venom
• However, it is not effective for poisonings • Apply cold pack to provide pain relief
with alcohols, strong acids or alkalis, KCl,
metals (Au, Li, Fe), button batteries, Funnel web spider antivenom
cyanide, Fl preparations, glycols and • Pressure immobilisation first aid (venom
esters, as it does not bind to these toxins can be inactivated locally)
• Endotracheal intubation may be required
Red back spider antivenom
Repeat-dose activated charcoal • Pressure immobilisation is NOT indicated
• Beneficial for only a few drugs including (it may increase pain and does not
carbamazepine, dextropropoxyphene, reduce systemic features)
aspirin, phenobarbitone, digoxin, quinine,
theophylline, verapamil, controlled Stonefish antivenom
release products, TCAs, phenothiazines • Immerse limb in hot water (50oC) to
provide pain relief
Whole bowel irrigation • DO NOT use pressure immobilisation
• Indicated for some compounds that are bandages for stone fish wounds,
not adsorbed onto activated charcoal otherwise local pain and tissue damage
(e.g. metals) and for poisonings involving may be increased due to venom
controlled release preparations retardation

Gastric lavage Snake antivenoms include:


• Infrequently used • Black snake antivenom
• Brown snake antivenom
Emesis induction (with ipecacuanha) • Death adder antivenom
• Not recommended • Polyvalent snake antivenom
• Ipecac syrup is contraindicated if • Sea snake antivenom
poisoning involves corrosive agents, • Taipan antivenom
hydrocarbons, seizure-causing agents, or • Tiger snake antivenom
if the patient is likely to become
unconscious within 30 min

Cathartics
• No proven benefit

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AMH Summary: Chapter 4 – Antidotes and Antivenoms 2

ANTIDOTES Glucagon
• Acute -blocker overdose
Acetylcysteine • CCB overdose with heart block
• Paracetamol overdose unresponsive to Ca2+

Atropine, pralidoxime Naloxone


• Organophosphate poisoning • Opioid overdose or intoxication

Calcium gluconate Pyridoxine


• Magnesium toxicity • Treatment and prophylaxis of pyridoxine
• Hydrofluoric acid burns deficiency
• Severe hyperkalaemia not due to digoxin
toxicity Thiamine
• Acute CCB poisoning with heart block • Thiamine deficiency
• Prophylaxis of thiamine deficiency in
Deferasirox alcohol misuse, malnutrition, prolonged
• Treatment of chronic iron overload due to fasting, TPN
blood transfusions in adults and children
6 yrs old
• Treatment of chronic iron overload in
children aged 2-5 yrs for whom
desferrioxamine is unsuitable or ineffective

Deferiprone
• Treatment of chronic iron overload in
patients with thalassaemia major, when
desferrioxamine is unsuitable or ineffective

Desferrioxamine
• Acute iron poisoning
• Chronic iron overload

Digoxin-specific antibody
• Potentially life-threatening digoxin
poisoning

Ethanol
• Acute ethylene glycol (antifreeze)
poisoning
• Acute methanol poisoning

Flumazenil
• Benzodiazepine overdose or intoxication

Fuller’s earth
• Alternative to activated charcoal in acute
paraquat poisoning

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AMH Summary: Chapter 4 – Antidotes and Antivenoms 3

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Pharmaceutical Society of Australia. Australian Pharmaceutical Formulary and Handbook 20th


edition; 2006; p 329, 330

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

Disclaimer: While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not
accept any responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this
publication. It is also noteworthy that The Medicine Box is unaffiliated with the Pharmacy Board of Australia, the former Pharmacy
Board of NSW, the Australian Pharmacy Council or the Pharmaceutical Society of Australia. All information in this publication is
provided by past pharmacy graduates and has not been verified by the above organisations.

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AMH Summary: Chapter 5 – Anti-infectives 1

AMH SUMMARY
CHAPTER 5: ANTI-INFECTIVES

A. ANTIBACTERIALS

OVERVIEW OF PRINCIPLES
• Indications listed for monographs are not comprehensive, based on clinical practice and
evidence of appropriate use
• Choice considers likely infecting organism. Ideally use a narrow spectrum agent with few
adverse effects
• Anti-infectives should be used if there is clear evidence that it will not recover without its
use as many common infections can resolve spontaneously
• Never treat viral infections with anti-bacterials
• For prophylaxis, restrict to certain clinical conditions
• Use for surgical prophylaxis in procedures with high risk of infection such as abdominal
surgery, surgery with breach of colon, cardiac surgery
• Combination therapy used in mixed infections to cover whole spectrum, when anti-infective
synergy is needed or to prevent infective resistance to treatment
• Avoid topical use (except in eye) as sensitivity and resistance may occur
• Oral or rectal doses of anti-infectives are adequate, unless they are not available
• Duration of therapy dependent of the severity of infection
• Broader spectrum anti-infectives affect bacterial flora, more likely to cause gastrointestinal
adverse effects and superinfection with resistant organisms
• Resistance: judicious use of anti-infectives may slow emergence of resistant strains
• Probiotics should be avoided in severely ill or immunocompromised patients as they can
cause infections

AMINOGLYCOSIDES
(amikacin, gentamycin, tobramycin)
• Works by inhibiting protein synthesis by binding 30 S ribosome, causing membrane
damage
• Used for Gram negative infections, surgical and non-surgical prophylaxis
• Adverse effects include nephrotoxicity (presents as gradual worsening renal failure),
ototoxicity (nausea and vertigo)
• Counselling: If using for more than 7-10 days, kidneys may not work as well. Stopping
medication will improve its function
• Creatinine clearance and drug monitoring required if using for more than 48 hours.

CARBAPENEMS
(ertapenem, imipenem, meropenem)
• Works by inhibiting bacterial cell wall synthesis, bactericidal
• Specific conditions: allergy to penicillins- possibility of cross reactivity
• Adverse effects include nausea, vomiting, diarrhoea

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AMH Summary: Chapter 5 – Anti-infectives 2

• Broad spectrum antibiotics with good activity against Gram positive, Gram negative
bacteria and anerobes
• Practice points
- Useful when single treatment required for complex mixed infections
- P. aeruginosa may develop resistance quickly
- Monitor renal, hepatic function, complete blood picture during prolonged treatment

CEPHALOSPORINS
(cefaclor, cefepime, cefotaxime, cefoxitin, ceftazidime, ceftriaxone, cefuroxime, cephelexin,
cephalothin, cephazolin)
• Works by interfering with bacterial cell wall peptidoglycan synthesis
• Specific conditions:
• Allergy to penicillins- possibility of cross reactivity
• Impaired vitamin K synthesis- increased risk of bleeding
• Adverse effects include nausea, rash, electrolyte disturbances
• Cephalothin, cephalexin, cephazolin, cefaclor and cefoxitin considered moderate spectrum
cephalosporins
• Cefotaxime, ceftriaxone, ceftazidime are broad spectrum, with less Gram positive activity
• Practice points
- Monitor renal function and complete blood pictures
- Superinfection may occur, especially with broad spectrum cephalosporins

GLYCOPEPTIDES
(teicoplanin, vancomycin)
• Works by inhibiting bacterial cell wall synthesis by preventing formation of peptidoglycan
polymers
• Used in serious infections such as MRSA, surgical prophylaxis for major procedures
• Adverse effects: oral vancomycin- usually GI adverse effects, others include phlebitis,
nephrotoxicity and ototoxicity
• Narrow spectrum of action, mainly working on Gram positive bacteria
• Practice points: monitor renal function, blood picture and hearing during long courses

LINCOSAMIDES
(clindamycin, lincomycin)
• Inhibiting protein synthesis binding to 50S ribosomal subunit
• Alternative for those with severe allergy to penicillins
• Adverse effects include diarrhoea (mild to severe), nausea, vomiting, abdominal pains and
cramps
• Active against staphylococci and streptococci and most anaerobes
• Monitor complete blood count, hepatic and renal function
• Cross resistance of lincosamides and macrolides for staphylococci and streptococci

MACROLIDES
(azithromycin, roxithromycin, erythromycin, clarithromycin
• Works by binding to 50S subunit

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AMH Summary: Chapter 5 – Anti-infectives 3

• Used as an alternative to individuals with penicillin or cephalosporin allergies


• Also has immunomodulatory and anti-inflammatory effects
• Adverse effects include nausea, vomiting, diarrhoea, abdominal pain and cramps
• Oral erythromycin poorly tolerated due to GI effects
• Broad spectrum antibiotics against Gram positive and some Gram negative bacteria
• High degree of cross resistance between erythromycin and newer macrolides

NITROIMIDAZOLES
(metronidazole, tinidazole)
• Works by interfering with DNA synthesis
• Used for anaerobic infections, protozoal, amoebic infections and surgical prophylaxis
• Adverse effects include nausea, anorexia, abdominal pain and metallic taste
• Tinidazole has a longer half life and can be used daily and better tolerated than
metronidazole
• Practice points
- Monitor blood count and neurotoxic reactions for long treatment
- Most active against anaerobes
- No alcohol while on this medication (can cause severe reactions)

PENICILLINS
(amoxycillin and clavulanic acid, ampicillin, amoxycillin, benzathine penicillin, benzylpenicillin,
dicloxacillin, flucloxacillin, phenoxymethylpenicillin, piperacillin, procaine penicillin, ticarcillin)
• Works by affecting peptidoglycan synthesis
• Contraindications: allergic reactions to penicillins
• Adverse effects include diarrhoea, nausea, rash, urticaria, superinfection, broncospasm
(severe)
• Narrow spectrum penicillins act on Gram positive organisms (dicloxacillin, flucloxacillin)
• Moderate spectrum penicillins include amoxycillin and ampicillin
• Clavulanic acid extends the activity of pencillins such as amoxycillin to make it broad
spectrum
• Practice points
- Use frequent doses for maximal antibacterial effect
- Monitor renal and hepatic function

QUINOLONES
(ciprofloxacin, moxifloxacin, norfloxacin, ofloxacin)
• Works by inhibitng DNA gyrase and topoisomerase IV
• Reserved for suspected infections where other antibiotics are ineffective
• Specific conditions
• Can induce seizures
• Combination with steroid use can increase risk of tendon damage
• Adverse effects include rash, itch, nausea, vomiting, severe tendon rupture (rare and
serious)
• Quinolones have excellent activity against haemophilis influenzae, enteric and other Gram
negative bacteria

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AMH Summary: Chapter 5 – Anti-infectives 4

• Counselling
- Medication can cause dizziness
- Stop taking medication if tendon soreness or inflammation occurs

RIFAMYCINS
(rifabutin, rifampicin)
• Works by inhibiting RNA polymerase
• Reserved for MRSA, mycobacterial infection and prophylaxis of meningitis and epiglottitis
• Adverse effects include nausea, vomiting, cramp, discolouration of urine (orange red) and
stained contact lenses
• Counselling: tell doctor if any loss of appetite, tiredness, and jaundice occurs.

TETRACYCLINES
(doxycycline, minocycline)
• Works by inhibiting 30S subunit (bacteriostatic)
• Used for respiratory infections and acne
• Not to be used for children under 8 years and pregnancy
• Adverse effects include nausea, vomiting, teeth discolouration, photosensitivity
• Counselling
- Take with food or milk to reduce stomach upset
- Remain upright for an hour after taking
- Do not take antacids, calcium, iron or zinc supplements within 2 hours of medication.
- Avoid sun exposure by sunscreen or covering up

ANTIMYCOBACTERIALS

• Used for mycolbacterium avium complex infection

Capreomycin
• Used for tubercolosis
• Adverse effects include nephrotoxicity, transient proteinuria, eosinophilia, haemolysis,
hearing loss
• Counselling: tell doctor if you have hearing loss or feel unsteady or dizzy.
• Practice points
- Monitor plasma creatine and potassium before starting
- Check audio and vestibular function

Cycloserine
• Interferes with cell wall synthesis
• Used in tuberculosis
• Contraindicated in epilepsy, severe renal function and frequent alcohol use
• Adverse effects include drowsiness, malaise, confusion, depression
• Counselling
- Medication can cause drowsiness, do not operate machinery while affected
- Can affect feelings, causing depression, excitement or confusion, let doctor know
• Practice points

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AMH Summary: Chapter 5 – Anti-infectives 5

- Monitor renal function, full blood count and liver function


- Monitor CNS toxicity each month and obtain cycloserine blood concentration

Dapsone
• Used for leprosy, pneumonia and for preventing toxoplasmosis
• Adverse effects include dose related asymptomatic haemolytic anaemia
• Dapsone syndrome can occur, starting in the first six weeks with symptoms of rash,
fever and jaundice. Resolves after ceasing
• Counselling
- Take with food
- Stop if troublesome rash occurs
• Practice points
- Full blood count, liver function required
- Stop if serious skin reaction or muscle weakness occurs

Ethambutol
• Used to treat tubercolosis
• Contraindicated in optic neuritis
• Adverse effects include optic neuritis decreasing visual acuity and causing colour
blindness. This is reversible.
• Counselling - may affect the vision, stop taking it and tell doctor if changes to eyesight
occur
• Practice points
- Measure creatinine clearance
- Monitor visual acuity and colour vision

OTHER ANTIBACTERIALS

Aztreonam
• Inhibit cell wall synthesis, binding to protein in Gram negative bacteria
• Used for gram negative aerobes
• Adverse effects include rash, diarrhoea, nausea, abnormal taste
• Practice points - combine with other agents to cover anaerobic and Gram positive
infections

Chloramphenicol
• Inhibit bacterial protein synthesis of 50S subunit
• Contraindicated in bone marrow depression and blood dyscrasias
• Adverse effects include nausea, vomiting and bone marrow suppression, grey
syndrome
• Grey syndrome involves grey skin, low body temperature, lethargy
• Counselling - tell doctor if pale skin, sore throat, fever or bruising occurs after stopping
the medication
• Practice points
- Broad spectrum activity (Gram positive and negative) and anaerobes
- Complete blood picture required before and during treatment
- Stop if haematological changes occur

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AMH Summary: Chapter 5 – Anti-infectives 6

Colistin
• Works by binding to phospholipids in bacterial cell wall
• Used for infections due to multidrug resistant Gram negative bacteria and respiratory
infection
• Adverse effects include nephrotoxicity, neurotoxicity, cough, bronchospasm
• Practice points - monitor renal function during systemic treatment

Hexamine hippurate
• Works by being hydrolysed to ammonia and formaldehyde
• Used in prophylaxis of chronic or recurrent urinary tract infection
• Contraindicated in severe hepatic impairment and dehydration
• Adverse effects include nausea, vomiting, diarrhoea
• Counselling - avoid anything with sodium bicarbonate such as Ural as it reduces the
agent’s effectiveness.

Nitrofurantoin
• Works by inhibiting bacterial protein DNA, RNA, cell wall synthesis
• Used for lower UTI and its prophylaxis
• Contraindicated in severe allergy and moderate to severe renal impairment
• Adverse effects include nausea, vomiting, anorexia, abdominal pain
• Counselling
- Take with food to reduce nausea and improve absorption
- May cause drowsiness, do not operate machinery if affected
- Tell doctor if breathing difficulty, cough, numbness occurs
- Urine discolouration may occur (brown), contact lenses may be stained
- Monitor pulmonary function, liver function, renal function

Quinupristin with dalfopristin


• Binds to bacterial ribosome, inhibit protein synthesis
• Used in severe MRSA or vancomycin resistant enterococcus faecium infection
• Adverse effects include thrombophlebitis, arthralgia, myalgia

Sodium fusidate
• Inhibit protein synthesis
• Used in S aureus infections
• Adverse effects include nausea, epigastric discomfort, lethargy
• Counselling
- Take with food to reduce indigestion
- Practice points - resistance develops rapidly with single use. Medication used in
combination with other antibiotics

Sulfadiazine
• Inhibits bacterial folate production
• Used in toxoplasma gondii infection
• Contraindicated in sulphonamide allergy, late pregnancy, neonates less than 4 weeks,
severe renal and hepatic impairment
• Adverse effect includes fever, nausea, rash
• Counselling

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AMH Summary: Chapter 5 – Anti-infectives 7

- Tell doctor if sore throat, fever, rash occur


- Avoid sun exposure by covering up or using sunscreen
- Drink plenty of fluids while on this medication
• Practice points - monitor renal function

Trimethoprim
• Inhibits bacterial folate production
• Used in UTI, prostatitis, epididymo-orchitis
• Contraindicated in allergy, severe renal impairment and megaloblastic anaemia (folate
deficient)
• Adverse effects include fever, itch, rash, hyperkalaemia
• Practice points
- Monitor blood and folate levels
- Monitor potassium
- Give at night for UTI

Trimethoprim with sulfamethoxazole


• Contraindicated in sulphonamide allergy, late pregnancy, renal and hepatic impairment,
megaloblastic anaemia
• Counselling
- Take with food
- Drink plenty of fluids
- Avoid sun exposure, cover up or use sunscreen
- Tell doctor if sore throat, rash, fever occurs

B. ANTIFUNGALS

AZOLES
(fluconazole, itraconazole, ketoconazole, miconazole, posaconazole, voriconazole)
• Work by impairing ergosterol in fungal cell membranes
• Adverse effects include rash, headache, dizziness, abdominal pain
• Miconazole and ketoconazole have wide spectrum of activity
• Itraconazole has broader spectrum than fluconazole
• Itraconazole capsules and liquid are not interchangeable

OTHERS

Amphotericin
• Binds to ergosterol in cell membranes
• Used in severe systemic fungal infections
• Adverse effects include infusion reactions (IV), thrombophlebitis, nephrotoxicity,
neurological effects such as seizure, tinnitus, hearing loss
• Monitor renal function

Griseofulvin
• Disrupts fungal cell microtubule function

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AMH Summary: Chapter 5 – Anti-infectives 8

• Used in dermal fungal infection


• Contraindicated in lupus and severe hepatic disease
• Adverse effects include headache, nausea, diarrhoea, anorexia
• Counselling
- Take with food
- May cause dizziness, if affected, do not operate machinery
- Minimise sun exposure by sunscreen or covering up
- The contraceptive pill may not be as effective when taking this medication

Nystatin
• Bind to ergosterol in fungi
• Used in oral thrush
• Adverse effects include nausea, vomiting diarrhoea
• Best to take after meals, continue for 2 days after symptoms disappear

Terbinafine
• Works by inhibiting squalene epoxidase in fungi, causing membrane disruption
• Used in onchyomycosis
• Contraindicated in hepatic disease (severe, chronic or active)
• Adverse effects include nausea, vomiting, abdominal pain, rash
• Counselling - tell doctor if you feel tired, nauseous, or have ulcers
• Obtain liver function tests while on this medication

C. ANTIVIRALS

GUANINE ANALOGUES
(acyclovir, famiciclovir, ganciclovir, valiciclovir, valganciclovir)
• Work by inhibitng viral DNA polymerase and DNA synthesis
• Used in herpes simplex infections, shingles and CMV
• Contraindicated in those with severe reactions to the medication
• Adverse effects include nausea, heading and vomiting
• Medication can cause dizziness

NEURAMINIDASE INHIBITORS
(oseltamivir, zanamivir)
• Works by reducining influenza virus by inhibiting neuraminidase and viral load
• Adverse effects include nausea, vomiting, abdominal pain and bronchospasm (zanamivir)
• Take with food with oseltamivir

D. HIV ANTIRETROVIRALS

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)


(abacavir, didanosine, emtricitabine, lamivudine, stavudine, zidovudine)

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AMH Summary: Chapter 5 – Anti-infectives 9

• Converted by cellular enzymes to active phosphorylated metabolites that inhibit viral


reverse transcriptase and viral DNA synthesis
• Used in HIV in adults and children, prophylaxis during pregnancy to prevent vertical
transmission of HIV
• Adverse effects include headache, nausea, myalgia, peripheral lipotrophy
• Counselling - lactic acid in body can build up and cause symptoms, tell doctor if nausea,
vomiting fatigue stomach pain occurs
• Practice points
- Avoid the combinations of stavudine with didanosine or zidovudine, lamuvidine with
emtricitabine, didanosine with tenofovir
- Measure lactate concentration
- Stop if lactic acidosis develops

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)


(delavirdine, efavirenz, nevirapine)
• Works by reversibly inhibiting HIV-1 reverse transcriptase
• Used for HIV infection
• Contraindicated in those with serious adverse reactions to individual NNRTIs
• Adverse effects include rash, malaise, nausea
• Rash occurs but treatment usually continues unless severe
• Practice points
- Stop NNRTI if elevated liver enzymes or severe rash
- When choosing NNRTI consider adverse effects of other drugs used to treat HIV
patients

PROTEASE INHIBITORS
(atazanavir, darunavir, fosamprenavir, indiavir, lopinavir with ritonavir, nelfinavir, ritonavir,
saquinavir, tipranvir)
• Works by inhibiting HIV-1 and HIV-2 protease, preventing maturation and replication
• Used for HIV infection
• Contraindicated in those with serious reactions to protease inhibitors
• Adverse effects include headache, diarrhoea, nausea, vomiting, fat accumulation, weight
gain, hyperglycaemia

E. ANTIPROTOZOALS

DRUGS FOR MALARIA


(e.g. atovaquone with proguanil)
• Inhibits parasite mitochondrial electron transport, reduce pyrimidine biosynthesis
• Proguanil - plasmodial dihydrofolate reductase inhibitor
• Best taken with food. Start 1-2 days before entering and 7 days after leaving area

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AMH Summary: Chapter 5 – Anti-infectives 10

F. ANTHELMINTICS

• For worm infections

BENZIMIDAZOLES
(albendazole, mebendazole)
• Inhibits microtubule polymerisation by binding to beta tubulin in parasite
• Use for roundworm, threadworm, hookworm, tapeworm
• Adverse reactions include headache, nausea, vomiting, diarrhoea
• Counselling - tablets may be crushed, chewed or swallowed

PYRANTEL
• Works by depolarising neuromuscular blocking agent, causing worm detachment of worm
and expulsion
• Used for threadworm, roundworm and hookworm
• Adverse reactions include nausea, vomiting, diarrhoea, cramps, headache

Copyright © The Medicine Box 2012


AMH Summary: Chapter 5 – Anti-infectives 11

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 6 – Cardiovascular 1

AMH SUMMARY: Chapter 6 - Cardiovascular

- HEART FAILURE -
 Encourage patients to weigh themselves daily and to consult their doctor immediately if they have
persistent weight gain (indication of fluid retention)
 Consider non-drug measures including exercise, reducing salt, fluid and alcohol, and stopping
smoking.

DRUGS OF CHOICE FOR HEART FAILURE


a) Loop Diuretics
b) ACE Inhibitors
c) Beta-blockers
d) Angiotensin II antagonists
e) Aldosterone antagonists
f) Digoxin
g) Anti-thrombotics

LOOP DIURETICS
- loop diuretics are the diuretics of choice for heart failure and reduction of fluid retention.
- combine with an ACE inhibitor in heart failure
- if hypotension occurs decrease dose of diuretic before that of the ACE inhibitor
- start with a low dose then adjust according to clinical response; use the lowest effective maintenance
dose
- usually given once daily in the morning although there may be a better clinical response if the drug is
given in divided doses rather than as a single dose
- when twice daily dosing is needed, the second dose is usually given at midday; diuresis may interfere
with sleep if given later than early evening 6pm
- higher doses are necessary in refractory heart failure:
o a trial of IV frusemide may be more effective than increasing oral doses
o increase diuretic effect by adding a thiazide diuretic; use small, intermittent thiazide doses with
careful monitoring, seek specialist advice
- monitor weight and electrolytes
- hypokalaemia is less likely when diuretics are used with ACE inhibitors or angiotensin II receptor
blockers than when used alone
- may feel dizzy on standing when taking this medicine. Get up gradually from sitting or lying to minimize
this effect; sit or lie down if you become dizzy.

 FRUSEMIDE – Lasix, Urex, Uremide


Precautions:
- exacerbates gout (diuretic induced hyperuricaemia);
- hypotension and electrolyte imbalances more likely in elderly.

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AMH Summary: Chapter 6 – Cardiovascular 2

Side Effects: hyponatraemia, hypokalaemia, hypomagnesaemia, dehydration, hyperuricaemia, gout,


dizziness, orthostatic hypotension

Dosage: Initially: 20-40mg d or bd. Maintenance dose: 20-400mg d. Maximum dose: 1g d.

 BUMETANIDE – Burinex
May be used in patients allergic to frusemide (eg rash) but risk of cross-reactivity cannot be excluded.

Precautions & Side Effects: as above

Dosage: 0.5–4 mg d or bd.

 ETHACRYNIC ACID - Edecrin


May be used in patients allergic to both bumetanide and frusemide, but has a greater risk of ototoxicity and
reduced excretion in renal impairment.

Precautions & Side Effects: as above

Dosage: 50–200 mg d or bd.

ACE INHIBITORS
- Start immediately after diagnosis of heart failure; begin at low dose, then gradually increase to
maintenance dose (or maximum tolerated dose); reduce dose of loop diuretic if necessary.
- In trials, the combination of ACE-I and A2-Antagonists worsened renal function and increased risk of
hypotension and hyperkalaemia. It may be an option for people with chronic heart faiure or non-responsive
hypertension (seek specialist).

BETA-BLOCKERS
- May aggravate heart failure and cause hypotension at the initiation of treatment; start treatment at very low
dose and increase dosage slowly over weeks to maintenance dose.
- In particular, metoprolol (Betaloc, Minax), bisoprolol (Bicor) and carvedilol (Dilatrend), reduces mortality in
stabilized heart failure when used together with an ACE inhibitor and a diuretic.

ANGIOTENSIN II ANTAGONISTS
- Can be used instead if patients cannot tolerate ACE inhibitors.
- Even though it can further reduce mortality when used together with an ACE inhibitor, it may also
increase the risk of adverse effects (hypotension and hyperkalaemia). This combination is not usually
used unless under specialist care.

ALDACTONE ANTAGONISTS
- In severe heart failure, both eplerenone and low dose spironolactone is used with an ACE inhibitor, loop
diuretic and, in some cases, digoxin. Monitor potassium each week for the first month, then each month
for 2 months, then every 3 months and when indicated clinically.

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AMH Summary: Chapter 6 – Cardiovascular 3

 EPLERENONE – Inspra
Indication: reduction of risk of CVD in patients with heart failure within 3-14 days of acute MI (in
combination with standard therapy)
Precautions: hyperkalaemia, diabetes and proteinuria
Side Effects: hyperkalaemia, hypotension, dizziness, altered renal function, increased creatinine
concentration
Dosage: initially 25mg d then increase to maintenance dose of 50mg d within 4 weeks
Practice points: check potassium concentration at baseline, first week, one month after starting treatment
and then every 3 months; stop treatment or reduce dose if hyperkalaemia occurs

 SPIRONOLACTONE – Aldactone, Spiractin


Potassium-sparing diuretic

Precautions:
- when used with other drugs that can increase potassium concentrations such as ACE
inhibitors. Avoid combination or monitor potassium concentrations.
- increases risk of hyperkalaemia especially in patients with renal impairment and those taking
ACE inhibitors or angiotensin II antagonists. Avoid use in severe renal impairment.

Side Effects: hyperkalaemia, hyponatraemia, weakness, headache, nausea, vomiting

Dosage:
For oedema – Initially: 100 mg d. Maintenance: 25–200 mg daily.
For severe heart failure – Initially: 25 mg once daily; increase to 50 mg daily after 8 weeks if progression of
heart failure without hyperkalaemia; decrease to 25 mg every other day if hyperkalaemia occurs.

DIGOXIN
- prevents worsening of heart failure in combination with an ACE inhibitor, beta blocker and a loop diuretic.
- therapeutic Range: lower concentrations of 0.5–0.8 micrograms/L for patients with heart failure who are in
sinus rhythm, as higher concentrations may be associated with increased rates of mortality and
hospitalization.
- narrow therapeutic index, hence concentration monitoring is required.
- check renal function and electrolyte concentrations before starting digoxin

Precautions:
- Hypokalaemia, hypomagnesaemia, hypercalcaemia, acidosis, hypoxia—increase risk of
digoxin toxicity; correct abnormality if possible.
- Hypothyroidism—may increase sensitivity to digoxin and require smaller doses.
- Renal impairment – reduce dose in elderly and in moderate-to-severe impairment.
- Acute MI, ischaemic heart disease, myocarditis—increase risk of arrhythmias.

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AMH Summary: Chapter 6 – Cardiovascular 4

Side Effects: anorexia, nausea, vomiting, diarrhoea, blurred vision, visual disturbances, confusion,
drowsiness, dizziness, nightmares, agitation, depression

Dosage:
Loading: oral/IV 250–500 micrograms every 4–6 hours, to a maximum of 1.5 mg.
Maintenance: oral 125–250 micrograms once daily (rarely increased up to 500 micrograms daily).

ANTI-THROMBOTICS
- Patients with heart failure have increased risk of thromboembolism.
- Warfarin or low dose aspirin may be indicated in patients with atrial fibrillation or recent MI;
warfarin usually preferred to aspirin in high risk patients (eg. history of embolism, recent
exacerbation of heart failure)

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AMH Summary: Chapter 6 – Cardiovascular 5

- ANGINA -
DRUGS OF CHOICE FOR ANGINA
a) Beta-blockers
b) Calcium Channel Blockers
c) Nitrates
d) Others: nicorandil, ivabradine, perhexiline

BETA-BLOCKERS
- Recommended as initial therapy.
- Beta-blockers may be used with nitrates, nicorandil, perhexiline and dihydropyridine calcium channel
blockers.
- Combine a beta-blocker with diltiazem cautiously; avoid combining a beta-blocker with verapamil (risk of
severe bradycardia and heart block).
- Abrupt withdrawal of beta-blocker may lead to increased myocardial ischaemia, risk of infarction and
sudden death; if withdrawal is required, reduce dose gradually over 2 weeks (or 4–6 weeks if the patient has
been treated for many years).

CALCIUM CHANNEL BLOCKERS


- Similar efficacy to beta blockers in angina.
- Verapamil is the drug of choice in this class for patients with stable angina. It is contraindicated in
patients with systolic heart failure.
- Diltiazem can be used safely with nitrates and with caution with beta-blockers (monitor for bradycardia).

NITRATES
- Use short acting nitrates (sublingual isosorbide dinitrate or spray glyceryl trinitrate) to treat acute attacks
of angina, or immediately before strenuous activity that may precipitate an attack.
- Use long acting nitrates (isosorbide mononitrate, transdermal glyceryl trinitrate) to prevent angina in
patients with more frequent symptoms.
- Tolerance to nitrates occurs with continuous exposure, so must ensure a nitrate-free period of 10-12
hours each day.

 GLYCERYL TRINITRATE – Anginine, Lycinate sublingual; Nitrolingual spray; Transiderm Nitro,


Nitro-dur patches

Side Effects: dizziness, headache, flushing, palpitations, orthostatic hypotension, fainting, peripheral
oedema

Acute Angina
Sublingual tablet: 300–600 micrograms (half to 1 tablet) repeated every 3–4 minutes until pain is resolved,
to a maximum of 2 or 3 tablets over 15 minutes. (discard unused tablets within 3 months)

Sublingual spray, 400–800 micrograms (1–2 sprays) repeated every 5 minutes until pain is resolved. Call an
ambulance if 2 sprays over 15 minutes do not relieve pain. (longer shelf life until expiry date).

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AMH Summary: Chapter 6 – Cardiovascular 6

Prevention of chronic angina


Patches: 5mg patch for up to 12-14 hours daily. Maximum 15mg patch.

 ISOSORBIDE DINITRATE – Isordil, Sorbidin


Side Effects: same as above

Acute Angina
Sublingual tablet (Isordil 5mg): 5–10 mg. Call an ambulance if 2 sublingual tablets over 15 minutes do not
relieve pain.

Prevention of chronic angina


Oral tablet (Isordil, Sorbidin 10mg): 10–40 mg up to 3 times daily.

 ISOSORBIDE MONONITRATE – Duride, Imdur, Monodur


- take at the time of day when angina is most frequent, eg at night for nocturnal angina or in the morning
for daytime angina
- twice daily dosing with isosorbide mononitrate is not recommended, as there will be no nitrate-free
interval and tolerance will be more likely to develop
- 1 daily (60mg or 120mg)

Dosage: Initially: 30–60 mg once daily, increased up to 120 mg once daily if necessary.

OTHER DRUGS
 IVABRADINE – Coralan
- limited data as it is a new drug
- used in stable angina where beta blockers and other drugs are contraindicated or not
tolerated

Precautions:
- hypotension (contraindicated if bp 90/50)
- low heart rate (contraindicated if <60 beats/min)
- avoid treatment with potent CYP3A4 inhibitors (eg ketoconazole, itraconazole,
clarithromycin). Caution use with other CYP3A4 inhibitors (especially with diltiazem or
verapamil, which also lower heart rate and are moderate inhibitors of CYP3A4.)

Side Effects: enhanced visual brightness (resolves after 2 months), blurred vision, bradycardia, ventricular
extrasystoles, atrioventricular block (first degree), headache, dizziness

Dosage: Initially: 5mg bd; increase after 3-4 weeks to 7.5mg bd if required.

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AMH Summary: Chapter 6 – Cardiovascular 7

 NICORANDIL – Ikorel (10mg, 20mg)


- for prevention and treatment of stable angina
- may be used as an alternative to long acting nitrates

Precautions: reduce dose in severe hepatic impairment


Side Effects: headache (especially on initiation), dizziness, lethargy, nausea, palpitations, flushing, myalgia
Dosage: Initially: 5 mg twice daily, increased after 1 week to 10–20 mg twice daily.

 PERHEXILINE – Pexsig 100mg


- for angina refractory to other medical or surgical treatment
- low therapeutic index, hence requires therapeutic drug monitoring.
- monitor clinically, especially for signs of hepatotoxicity and peripheral neuropathy
- sample collection: Take blood sample after 3–5 days on loading dose to identify slow
metabolisers. (Slow metabolisers have higher perhexiline concentration than normal
metabolisers and no detectable metabolite.) Then take samples each month (half-life 7–
14 days) until treatment is stabilized, then every 3–6 months thereafter.
- Therapeutic Range: 0.15–0.6 mg/L (0.5–2 micromol/L).

Side Effects: dizziness, nausea, headache, weight loss

Dosage:
Initially: 200–300 mg once daily for 5–7 days, then reduce to 100 mg daily.
Maintenance normal metaboliser: 100–200 mg once daily; adjust according to concentration.
Maintenance slow metaboliser: 50–100 mg once a week; adjust according to concentration.

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AMH Summary: Chapter 6 – Cardiovascular 8

- MYOCARDIAL INFARCTION -
DRUGS OF CHOICE FOR MYOCARDIAL INFARCTION
a) Oxygen, morphine & GTN
b) Anti-platelets: aspirin & clopidogrel
c) Thrombolytics
d) Heparin
e) Beta-blockers
f) ACE Inhibitors
g) Aldosterone antagonists

Acute MI Treatment

 treat all MIs with thrombolytics when coronary angioplasty is not available unless there is a specific
contraindication; give thrombolytics as early as possible (within 30 minutes of presentation)
 treat all MIs with beta-blocker, ACE inhibitor, aspirin and clopidogrel unless there is a specific
contraindication

Post MI treatment

 continue clopidogrel (1-12 months), aspirin, beta-blockers, ACE-I (and eplerenone if used)
 use warfarin instead of antiplatelet agents in patients with AF, heart failure or previous emboli.
Warfarin alone (INR around 3)
 warfarin (INR 2–2.5) with low dose aspirin (75 mg daily) may be more beneficial than aspirin alone
but with increased risk of severe haemorrhage. Specialist advice required.
 consider treating all patients with one of the statins regardless of cholesterol concentration

OXYGEN, MORPHINE & GTN


Relieves symptoms of acute MI; use GTN infusion if there is ongoing chest pain or heart failure.

ANTI-PLATELETS: ASPIRIN & CLOPIDOGREL


Aspirin: 300mg daily initially (with clopidogrel) to all patients. Use clopidogrel alone if allergic to aspirin.
Continue with low-dose aspirin (150mg daily) long term. Combine with clopidogrel for at least 1 month and
up to 12 months after thrombolytic treatment and stent placement.

THROMBOLYTICS
- streptokinase, reteplase, alteplase, tenecteplase
- use within 12 hours of onset of chest pain lasting 30 minutes and ECG observation.

HEPARIN
Given routinely with thrombolytics (alteplase, reteplase, tenecteplase) in high risk patients of
thromboembolism. It may be given with streptokinase in selected patients.

BETA-BLOCKERS
Atenolol, metoprolol or propranolol should be started early after MI when patients are stable. Avoid
oxprenolol and pindolol as they do not benefit patients with acute MI due to their sympathomimetic activity.

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AMH Summary: Chapter 6 – Cardiovascular 9

ACE INHIBITORS
Start within the first 24-48 hours in patients who are stable.

ALDOSTERONE ANTAGONISTS
Start eplerenone early post MI in patients with left ventricular systolic dysfunction and symptoms of heart
failure.

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AMH Summary: Chapter 6 – Cardiovascular 10

- HYPERTENSION -

DRUGS OF CHOICE FOR HYPERTENSION


a) ACE Inhibitors
b) Angiotensin II antagonists
c) Calcium Channel Blockers
d) Thiazide Diuretics
e) Beta-blockers
f) Others: vasodilators, centrally acting antihypertensives, alpha-blockers

Treatment
First line:
 ACE-I (or A2A) or
 Dihydropyridine calcium channel blocker (i.e. not diltiazem or verapamil) or
 Low-dose thiazide diuretic (if 65 or older)

If inadequate effect: add a second hypertensive rather than increasing the dose of the first. Preferred
combinations:
 ACE-I (or A2A) + calcium channel blocker or thiazide diuretic
 Calcium channel blocker + thiazide diuretic
 Beta-blocker + ACE-I (or A2A) or dihydropyridine calcium channel blocker
 Beta-blocker + thiazide diuretic (ok but increases risk of diabetes)

Avoid combinations if possible:


 Verapamil + beta-blocker (risk of severe bradycardia and heart block)
 ACE-I (or A2A) + potassium-sparing diuretic (risk of hyperkalaemia)
 ACE-I + A2A (may increase renal complications. Specialist use only)

Table: Drug choice dependent on coexisting conditions

Coexisting conditions Favorable


Diabetes ACE-I (or A2A)
Heart failure ACE-I (or A2A), beta-blockers (carvedilol, controlled
release metoprolol, bisoprolol), thiazides
Post MI beta-blockers (except oxprenolol, pindolol), ACE
inhibitors (or A2A)
Angina beta-blockers (except oxprenolol, pindolol), calcium
channel blockers, ACE-I
AF ACE-I (or A2A), (verapamil, diltiazem, beta-blockers
may help rate control)
Unfavorable
Asthma,COPD beta-blockers (use beta1 cardioselective eg atenolol,

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AMH Summary: Chapter 6 – Cardiovascular 11

metoprolol cautiously in mild-to-moderate)


Bradycardia beta-blockers, diltiazem, verapamil
Heart failure Calcium channel blockers (especially verapamil,
diltiazem)
Gout Thiazide diuretics

ACE INHIBITORS
Precautions:
- Risk of hyperkalaemia in elderly and renal impairment; avoid combinations with potassium, potassium-
sparing diuretics and NSAIDs (including selective COX-2 inhibitors).

Side Effects: hypotension, cough, hyperkalaemia, headache, dizziness, fatigue, nausea, renal impairment

- First-line treatment, especially in patients with diabetes and proteinuria, heart failure or post-MI.
- Most (except captopril) maintain an antihypertensive effect for up to 24 hours and can be given once daily.

Practice Points:
- when initiating ACE inhibitors:
o stop potassium supplements and potassium-sparing diuretics
o stop other diuretics for 24 hours
o start with a low dose
- check renal function and electrolytes before starting ACE inhibitor and review after 1–2 weeks
- onset of ACE inhibitor associated angioedema may not occur for several years

 CAPTOPRIL – Acenorm, Capoten, Topace


Dosage:
Hypertension: Initially 12.5mg bd, increased at intervals of 2-4 weeks to 25-50mg bd.
Heart failure: Initially 6.25mg tds, increased at 2 week intervals to 25-75mg bd. Maximum 150mg daily.
Myocardial infarction: start 3 days post MI at 6.25mg tds, increased up to 25mg tds over several days
to final target dose of 50mg tds.
Renal impairment/taking a diuretic: Initially 6.25mg bd.

 ENALAPRIL – Renitec, Alphapril, Amprace; Renitec Plus (enalapril + HCT), Zan-Extra (enalapril +
lercanidipine)
Dosage:
Hypertension: Initially 5mg daily, increased at intervals of 1-2 weeks up to 10-40mg daily as 1-2
divided doses. 1 daily for combination products.
Heart failure: Initially 2.5mg daily, increased up to 10-20mg daily as 1-2 divided doses.
Renal impairment/taking a diuretic: Initially 2.5mg daily.

 FOSINOPRIL – Monopril; Monoplus (fosinopril + HCT)


Dosage:

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AMH Summary: Chapter 6 – Cardiovascular 12

Hypertension: Initially 10mg daily, increased up to 40mg daily. 1 daily for combination product.
Heart failure: Initially 5-10mg daily, increased up to 10-40mg daily.
Renal impairment/other diuretics: Initially 5-10mg daily.

 LISINOPRIL – Lisodur, Prinivil, Zestril, Fibsol


Dosage:
Hypertension: Initially 5-10mg daily, increased at intervals of 2-4 weeks up to 20mg once daily.
Maximum 40mg daily.
Heart Failure: Initially 2.5mg daily, increased at 4 week intervals up to 20mg daily.
Myocardial infarction: Initially 5mg within 24hours of onset of symptoms, followed by 5mg after 24
hours, then 10mg once daily for 6 weeks. Continue treatment in patients developing heart failure.
Renal impairment/taking a diuretic: Initially 2.5-5mg daily

 PERINDOPRIL – Coversyl; Coversyl Plus (perindopril + indapamide), Perindo


Dosage: (doses are for perindopril arginine – Coversyl; 2.5mg arginine = 2mg erbumine)
Hypertension: 5mg once daily. Maximum 10mg daily. 1 daily for combination product.
Heart Failure: Initially 2.5mg once daily; increased up to 5mg once daily.
Renal impairment: Initially 2.5mg once daily or on alternate days depending on severity.

 QUINAPRIL – Accupril; Accuretic (quinapril + HCT)


Dosage:
Hypertension: Initially 5-10mg once daily, increase at 4 week intervals to 10-40mg daily in 1-2 divided
doses. 1 daily for combination product.
Heart failure: Initially 5mg daily, increase at weekly intervals to 10-20mg daily in 2 divided doses. If
10mg bd is tolerated, then change to 20mg daily after 1 month.
Renal impairment/taking a diuretic: Initially 2.5-5mg daily.

 RAMIPRIL – Ramace, Tritace; Triasyn (ramipril + felodipine)


Dosage:
Hypertension: 2.5mg once daily, increase after 2-3 weeks to 5mg if necessary. Maximum 10mg daily.
1 daily for combination product.
Heart failure: Initially 2.5mg bd, beginning 2-10 days post MI; increase at intervals of 1-3 days to 5-
10mg daily in 2 divided doses.
Renal impairment/taking a diuretic: Initially 1.25mg once daily.

 TRANDOLAPRIL – Gopten, Dolapril, Tranalpha


Dosage:
Hypertension: 1mg daily, increase after 2-4 weeks to 2mg daily if necessary. Maximum 4mg daily.
Myocardial infarction: initiate treatment 3 days post MI with 0.5mg daily, then 1mg daily for 3 days.
Increase to 2mg daily for 4 weeks then to a maximum dose of 4mg daily if tolerated.
Renal impairment/hepatic impairment/taking a diuretic: Initially 0.5mg daily.

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AMH Summary: Chapter 6 – Cardiovascular 13

ANGIOTENSIN II ANTAGONISTS
Indications: Hypertension, heart failure in patients who can't tolerate ACE inhibitors.

Side Effects: dizziness, headache, hyperkalaemia

Practice Points:
- before starting angiotensin II antagonists stop potassium supplements and potassium-sparing
diuretics; check renal function and electrolytes and review regularly
- unlike ACE inhibitors, angiotensin II antagonists do not inhibit the breakdown of bradykinin and may
be useful if unable to tolerate an ACE inhibitor because they:
o cause less cough than ACE inhibitors
o may be used if there is a history of angioedema caused by an ACE inhibitor (with close
monitoring as there is a small risk of recurrence)
- maximum antihypertensive effect occurs about 4–6 weeks after starting treatment

 CANDESARTAN – Atacand; Atacand Plus (+HCT)


Dosage:
Hypertension: 8mg daily, increase up to 16mg if necessary. 1 daily for combination product.
Heart failure: Initially 4mg daily, then double the dose at intervals of at least 2 weeks to highest
tolerated dose. Maximum 32mg daily.
Severe renal impairment: Initially 4mg once daily; may require lower maximum dose.

 EPROSARTAN – Teveten; Teveten Plus (+HCT)


Dosage: Initially 600mg once daily, increase to 800mg once daily if necessary. Start at 400mg once daily
for patients with renal/hepatic impairment, elderly or taking diuretics. 1 daily for combination product.

 IRBESARTAN – Avapro, Karvea; Avapro HCT/Karvezide (+HCT)


Dosage:
Hypertension: 150mg once daily, increase up to 300mg daily if necessary. Start at 75mg if elderly. 1
daily for combination product.

 LOSARTAN – Cozaar
Dosage: 50mg once daily, increase after 3-6 weeks to 100mg once daily if necessary. Start at 25mg
once daily if taking diuretics.

 OLMESARTAN – Olmetec, Olmetec Plus (+ HCT)


Dosage: Initially 20mg once daily, increase to 40mg once daily after 8 weeks if necessary. (makes little
difference so preferably add HCT for better reduction of blood pressure). 1 daily for combination product.

 TELMISARTAN – Micardis; Micardis Plus (+HCT)


Precaution: use with caution in mild-to-moderate hepatic impairment
Dosage: usually 20-40mg once daily; increase if necessary to 80mg once daily.

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AMH Summary: Chapter 6 – Cardiovascular 14

 VALSARTAN – Diovan, Exforge HCT (+amlodipine+HCT), Co-Diovan (+HCT)


Dosage: 80mg daily and increase to 160mg daily. Maximum 320mg daily.

CALCIUM CHANNNEL BLOCKERS


- Dihydropyridines (amlodipine, felodipine, lercanidipine, nifedipine) are suitable as first-line treatment of
hypertension.
- Verampil and diltiazem are contraindicated in heart failure. Less risk with dihydropyridines, but use with
caution.

Indications: Hypertension, angina

Side Effects: peripheral oedema, rash, headache, fatigue, dizziness, flushing, nausea, abdominal pain,
gingival hyperplasia, bradycardia (diltiazem, verapamil), constipation (verapamil)

Dihydropyridine
Dihydropyridines especially cause headache, flushing, peripheral oedema and palpitations.

 AMLODIPINE – Norvasc, Perivasc; Caduet (amlodipine + atorvastatin)


Dosage: Initially 2.5-5mg once daily, increase over 1-2 weeks to a maximum of 10mg once daily. 1 daily for
combination product.

 FELODIPINE- Felodur ER, Plendil ER


- avoid grapefruit juice as it may increase side effects.

Dosage: Initially 5mg once daily. Maintenance dose 5-10mg once daily. Maximum 20mg daily.

 LERCANIDIPINE – Zanidip
Precautions: do not use with cyclosporin, severe renal/hepatic impairment.
Dosage: Initially 10mg once daily; increase after 2 weeks up to a maximum of 20mg once daily.

 NIFEDIPINE – Adalat, Adefin; Adalat Oros/Adefin XL/Addos XR (controlled release)


- normal tablet: bd
- controlled release tablet: daily

Practice Points:
 nifedipine controlled release tablet 60mg is approximately equivalent to nifedipine conventional
tablets 20mg twice daily
 stop nifedipine if marked hypotension or dyspnoea occur
 short acting formulations of nifedipine may be associated with reflex tachycardia, which may
exacerbate ischaemic heart disease

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AMH Summary: Chapter 6 – Cardiovascular 15

Dosage:
Normal tablet: Initially 10-20mg bd, increase to 20-40mg bd.
Controlled release tablet: Initially 20mg or 30mg once daily, increase to a maximum of 90mg once
daily (angina) or 120mg once daily (hypertension).

Benzothiazepine
 DILTIAZEM – Cardizem, Vasocardol, Coras 60mg; Cardizem CD/Vasocardol CD (180,240,360)
Precautions: contraindicated in severe bradycardia

- Normal tablet: 3-4 times a day


- CR tablet: 1 daily

Dosage:
Angina:
- Conventional tablet: initially 30mg 3-4 times daily, increase as required up to 180-240mg daily.
- Controlled release: initially 180mg once daily; increase as required up to 360mg once daily.

Hypertension:
- Controlled release products, initially 180-240mg once daily; increase as required up to 360mg once daily.

Phenylalkylamine
 VERAPAMIL – Anpec, Isoptin (40,80,120,160); Cordilox SR, Isoptin SR, Anpec SR (180,240mg);
Veracaps SR (160,240mg); Tarka (verapamil + trandolapril)

Indications: AF, flutters, hypertension, angina

Precautions:
- treatment with antiarrhythmics increases risk of heart failure, bradycardia and proarrhythmic effect; avoid
combination.
- treatment with drugs which cause bradycardia may further decrease heart rate and cause hypotension
(use with beta blockers not recommended unless under specialist care).

- Normal tabs: 2-3 times a day


- Controlled release: 1 daily

Dosage:
Arrhythmias: Maintenance 120-480mg daily.
Angina & Hypertension:
- normal tablet: Initially 80mg bd to tds. Maintenance 160mg bd to tds
- controlled release: For angina, initially 180-240mg once daily, increase up to 240mg bd if necessary. For
hypertension, initially 120-180mg once daily, increase up to 240mg d or bd if necessary.
- Combination product: once daily.

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AMH Summary: Chapter 6 – Cardiovascular 16

THIAZIDE DIURETICS
- First line treatment in hypertension for >65 years. Due to association of diabetes, they are no longer
recommended first line monotherapy in younger patients.
- Risk of hypokalaemia; monitor potassium concentration.
- May be used together with loop diuretics in severe heart failure to increase diuresis; use small doses
with careful monitoring under specialist advice.
- To minimize diuretic-induced hypokalaemia: use low dose thiazide; or combine with ACE inhibitor/A2A;
or use potassium supplements/potassium-sparing diuretics when potassium <3.5 mmol/L.

Precautions:
- may precipitate gout by increasing uric acid concentrations
- less effective in renal impairment where CrCL <25ml/min
- electrolyte imbalance (eg hypokalaemia) and orthostatic hypotension more likely in elderly.

Side Effects: dizziness, weakness, muscle cramps, polyuria, orthostatic hypotension, hyponatraemia,
hypokalaemia, hyperuricaemia, hypochloraemic alkalosis, hypomagnesaemia. Increases in BSL and plasma
lipids are minimal with low doses.

 HYDROCHLOROTHIAZIDE – Dithiazide + other combined products


Precautions & Side Effects: same as above
Dosage: 12.5-25mg daily mane

 INDAPAMIDE – Natrilix & Dapatabs 2.5mg; Natrilix SR 1.5mg


- same side effects but LESS hypokalaemia with SR formulation when compared to the non-SR.

Dosage: 1.25–2.5 mg once daily in the morning.

 CHLORTHALIDONE – Hygroton 25mg


Dosage: 12.5–25 mg daily mane

Aldosterone antagonists and potassium-sparing diuretics


These drugs are not required routinely in patients on thiazide or loop diuretics; reserve for use if
hypokalaemia occurs (serum potassium <3.5 mmol/L)

 AMILORIDE – Kaluril; Moduretic/Amizide (amiloride + HCT)


- Amiloride is a potassium-sparing diuretic and is not required routinely in patients taking diuretics
- amiloride is preferred to potassium supplements to prevent diuretic-induced hypokalaemia because of
greater convenience and tolerability
- amiloride is available either alone, or in combination with a thiazide diuretic (hydrochlorothiazide 50 mg);
the combination product has an unnecessarily high content of hydrochlorothiazide (not more than 25 mg
is required to treat hypertension): Moduretic & Amizide

Precautions:

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AMH Summary: Chapter 6 – Cardiovascular 17

- increased risk of hyperkalaemia when used with ACE inhibitors, elderly, renal impairment.

Side Effects: hyperkalaemia, hyponatraemia and hypochloraemia (especially when combined with thiazide
diuretics), weakness, headache, nausea, vomiting, constipation, impotence, dizziness, muscle cramps,
reduces magnesium loss

Dosage:
For Amiloride only -
Prevention of diuretic-induced hypokalaemia: 2.5-5mg daily.
Oedema: Initially 5mg daily then reduce dose accordingly.

For Amiloride + hydrochlorothiazide combination –


Hypertension: 0.5 daily
Oedema: Initially 1-2 daily; maximum 4 daily.

 EPLERENONE – Inspra
Indication: Reduction of risk of cardiovascular death in patients with heart failure and left ventricular
impairment within 3–14 days of an acute MI (in combination with standard therapy)

Monitoring: check potassium concentration at baseline, within the first week, 1 month after starting treatment
or dosage adjustment and then every 3 months; stop treatment and/or reduce dose if hyperkalaemia occurs

Contraindications: renal impairment where creatinine clearance <50 mL/min; hyperkalaemia where
potassium >5.5 mmol/L

Precautions: increased risk of hyperkalaemia in diabetes/proteinuria, renal impairment and elderly

Side Effects: hyperkalaemia, hypotension, dizziness, altered renal function, increased creatinine
concentration

Dosage: Initially 25 mg once daily; increase to maintenance dose of 50 mg once daily within 4 weeks.

 SPIRONOLACTONE – Aldactone, Spiractin


- has potassium-sparing and anti-androgenic activity
- reserve use of spironolactone for hirsutism in females for whom other treatments are not suitable
- in severe heart failure, spironolactone is used with an ACE inhibitor, loop diuretic and, in some cases,
digoxin; monitor potassium each week for the first month, then each month for 2 months, then every
3 months and when indicated clinically

Precautions:
- when used with other drugs that can increase potassium concentrations such as ACE
inhibitors. Avoid combination or monitor potassium concentrations.

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AMH Summary: Chapter 6 – Cardiovascular 18

- increases risk of hyperkalaemia especially in patients with renal impairment and those taking
ACE inhibitors or angiotensin II antagonists. Avoid use in severe renal impairment.

Side Effects: hyperkalaemia, hyponatraemia, weakness, headache, nausea, vomiting

Dosage:
For oedema – Initially: 100 mg d. Maintenance: 25–200 mg daily.
For severe heart failure – Initially: 25 mg once daily; increase to 50 mg daily after 8 weeks if
progression of heart failure without hyperkalaemia; decrease to 25 mg every other day if
hyperkalaemia occurs.

 TRIAMTERENE with HYDROCHLOROTHIAZIDE – Hydrene


- Combination product: triamterene 50mg + hydrochlorothiazide 25mg.

Dosage:
Hypertension: 0.5-1 daily after breakfast
Oedema: Initially 1 bd, then adjust accordingly up to a maximum of 4 daily.

BETA-BLOCKERS

- No longer first-line for hypertension. They are associated with reduced protection against stroke and
increased risk of diabetes compared with other classes.
- Beta1-selective beta-blockers (eg atenolol, metoprolol) may produce less bronchospasm, less peripheral
vasoconstriction and less alteration of glucose and lipid metabolism. They may be preferred in peripheral
vascular disease, Raynaud's syndrome, diabetes or mild-to-moderate reversible airways disease.
- Practice points: when stopping treatment reduce dosage gradually (over 2 weeks or 4–6 weeks if the
patient has been treated for many years); abrupt withdrawal may exacerbate angina, or precipitate rebound
hypertension, MI or ventricular arrhythmias.

Precautions:
- Asthma & diabetes as beta blockers can mask signs of hypoglycaemia (tachycardia & tremors). Use
Beta1-selective beta-blockers (eg atenolol, metoprolol).
- Hyperthyroidism: mask clinical signs (tachycardia) . Avoid in combination with verapamil.

Side Effects: nausea, diarrhoea, bronchospasm, dyspnoea, cold extremities, exacerbation of Raynaud's
syndrome, bradycardia, hypotension, orthostatic hypotension (carvedilol, labetalol), heart failure, heart
block, fatigue, dizziness, abnormal vision, decreased concentration, hallucinations, insomnia, nightmares,
depression, alteration of glucose and lipid metabolism, oedema (carvedilol)

Table: Comparative Information between beta blockers

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AMH Summary: Chapter 6 – Cardiovascular 19

Drug Receptors antagonized Elimination Route


Atenolol Beta1 Renal
Bisoprolol Beta1 Renal and hepatic
Carvedilol Alpha1, beta1, beta2 Hepatic
Labetalol Alpha1, beta1, beta2 Hepatic
Metoprolol Beta1 Hepatic
Nebivolol Beta1 Hepatic
Oxprenolol Beta1, beta2 Hepatic
Pindolol Beta1, beta2 Hepatic and renal
Propranolol Beta1, beta2 Hepatic

Beta1 – cardioselective
Beta2 – bronchi, glucose

 ATENOLOL – Tenormin, Noten, Atehexal, Tensig


Dosage:
Hypertension, Angina, Migraine: 25-100mg once daily
Tachyarrhythmias: 50-100mg once daily
Myocardial Infarction: 50mg daily maintenance

 BISOPROLOL – Bicor
- all strengths except for 1.25mg are on authority of ppl with severe heart failure (main indication)

Dosage: Initially: 1.25mg once daily for 1 week; increase dose if tolerated to 2.5mg once daily for 1 week,
then 3.75mg once daily for 1 week, then 5mg once daily for 4 weeks, then 7.5mg once daily for 4 weeks,
then 10mg once daily for maintenance.

 CARVEDILOL – Dilatrend 3.125mg, 6.25mg, 12.5mg, 25mg


Indication: stable mild-to-severe heart failure

Dosage:
Hypertension: Initially 12.5mg once daily for 2 days. Maintenance 25mg once daily, increase if necessary at
intervals of at least 2 weeks up to a maximum of 50mg once daily or in 2 divided doses.

Heart Failure: Initially 3.125 mg twice daily for 2 weeks; increase at intervals of at least 2 weeks to 6.25 mg
twice daily, then 12.5 mg twice daily, then 25 mg twice daily (maximum in patients <85 kg with mild-to-
moderate heart failure and in all patients with severe heart failure) or 50 mg twice daily (maximum in
patients >85 kg); use the highest dose tolerated by the patient.

 ESMOLOL – Brevibloc inj


- very short duration of action and is used IV in for short term treatment of flutters and AF, sinus
tachycardias, perioperative hypertension.
- Steady state 5 min; half-life 9 min; elimination 10-20min after stopping infusion

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AMH Summary: Chapter 6 – Cardiovascular 20

- Infusion may be continued for up to 48 hours if necessary.

Side Effects: hypotension, chest pain, peripheral ischaemia, nausea, vomiting, constipation, dizziness,
somnolence, fatigue, confusion, agitation, headache, sweating, inflammation (injection site)

Dosage:
Loading Dose: IV 500mcg/kg over 1 minute, then infuse 50mcg/kg/min over the next 4 minutes.
Maintenance: IV 50-200 mcg/kg/min

 LABETALOL – Presolol, Trandate (100, 200mg)


Dosage: initially 100 mg twice daily, increased each week; maintenance 200–400 mg twice daily.

 METOPROLOL – Betaloc, Minax, Lopresor; Tropol-XL controlled release


- Controlled release tablets may be broken in half or swallowed whole; do not chew or crush
them.

Dosage:
Hypertension: Initially 50-100mg once daily for 1 week. Maintenance 50-100mg d or bd.
Angina: Initially 25-50mg bd. Maintenance 50-100mg bd or tds.
Tachyarrhythmias: 50-100mg bd or tds
Myocardial Infarction: Initially 25-50mg q6h for 48 hours. Maintenance 50-100mg bd.
Prevention of migraine: 50-75mg bd
Heart Failure: Controlled release tablet: initially 23.75 mg once daily for a minimum of 2 weeks (halve
dose in patients with NYHA III or IV heart failure for first week). Increase dose (if well tolerated) as
follows, remaining at each dose level for a minimum of 2 weeks: 47.5 mg once daily, then 95 mg once
daily, then 190 mg once daily for maintenance.

 NEBIVOLOL – Nebilet
Evidence of benefit is stronger for bisoprolol, carvedilol and metoprolol than for nebivolol.
Dosage: 5mg once daily (hypertension) or 10mg once dialy (heart failure)

 OXPRENOLOL – Corbeton 20,40mg


Dosage:
Hypertension: Initially 40-80mg bd, increased each week. Maintenance 80-160mg bd.
Angina: Initially 20-40mg tds, increased if necessary up to 320mg daily.
Tachyarrhythmias: 20mg bd to tds, up to 80mg daily.

 PINDOLOL – Visken, Barbloc 5mg,15mg


Dosage:
Hypertension: Initially 5mg bd, increased by 10mg daily every 3-4 weeks. Maintenance 10-30mg daily in
2-3 divided doses.
Angina: 7.5-20mg daily in 3 divided doses.
Tachyarrhythmias: 15-30mg daily in 3 divided doses.

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AMH Summary: Chapter 6 – Cardiovascular 21

 PROPRANOLOL – Deralin, Inderal (10,40mg)


Dosage:
Hypertension: Initially 20-40mg bd, increased by the same amount each week. Maintenance 120-320mg
d in 2-3 divided doses.
Angina, tremor: Initially 40mg bd or tds, increased by the same amount each week. Maintenance 120-
320mg daily n 2-3 divided doses.
Tachyarrhythmias (including anxiety): 10-40mg tds or qid.
MI: Initially 40mg qid for 2-3 days. Maintenance 80mg bd.
Prevention of migraine: Initially 40mg bd. Maintenance 80-160mg daily.

VASODILATORS
Indications: Vasodilators are potent anti-hypertensives reserved for refractory hypertension or for acute
treatment of hypertensive emergencies

 HYDRALAZINE – Alphapress
- is given IV in emergencies.
- is given orally in refractory hypertension with other antihypertensives.
- used in heart failure, with a nitrate, when patients can't take ACE inhibitor or A2A.
Side Effects: flushing, headache, dizziness, tachycardia, palpitations, oedema (sodium and water retention)

Practice Points:
- prolonged treatment (>6 months) may induce a lupus-like syndrome; check antinuclear factor before
starting and during prolonged treatment
- beta-blockers and thiazides are often used with hydralazine to prevent tachycardia and fluid
retention
- the combination of hydralazine and isosorbide dinitrate has been shown to reduce mortality in heart
failure, although it is not as effective as an ACE inhibitor; consider this combination in people unable
to tolerate an ACE inhibitor or an angiotensin II antagonist

Dosage:
Hypertension: initially 25mg bd. Maintenance 50-200mg daily. Note that for doses >100mg, there is an
increased risk of lupus-like syndrome and should not be given without prior tests.
Heart failure: gradually increase dose to 300mg daily in 4 divided doses as tolerated; give with isosorbide
dinitrate.

CENTRALLY ACTING ANTIHYPERTENSIVES


Indications: These are not considered first line agents as they are less well tolerated than other
antihypertensives.

 CLONIDINE – Catapres 100, 150mcg

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AMH Summary: Chapter 6 – Cardiovascular 22

Precautions:
- depression may be exacerbated
- increase BSL in diabetics

Side Effects: drowsiness, dry mouth, bradycardia, constipation, headache, fatigue, weakness

Dosage: 50-100 mcg bd, increase by 100-200 mcg every 2-3 days. Maintenance 150-300mcg bd

Practice Points:
- withdraw clonidine over at least 7 days; stopping abruptly may precipitate a severe withdrawal
syndrome. It occurs 18-72 hours after stopping with rebound hypertension (rapid heart rate,
headache, flushing, tremor, sweating, insomnia, agitation.)
- presence of a beta-blocker can worsen the withdrawal syndrome; withdraw clonidine as above, after
having stopped the beta-blocker several days before.
- clonidine is still marketed the treatment of menopausal flushing but evidence for efficacy in this
indication is limited

 METHYLDOPA – Aldomet
- Methyldopa is often used to treat hypertension in pregnancy, but CNS and hepatic adverse effects limit its
use in non-gestational hypertension.

Precaution: exacerbates depression

Side Effects: sedation, dizziness, light-headedness, tiredness, weakness, dry mouth, fever, headache,
nausea, diarrhoea, positive direct Coombs' test

Dosage: Initially 125-250mg bd for 2 days, then adjust by 250-500mg daily at 2 day intervals. Maintenance
125-500mg bd to qid. When used with other antihypertensives, daily dose is usually <500mg

Practice Points:
- the sedating effect of methyldopa is exacerbated by dose increases; increase dosage at night to
minimise inconvenience of increased sedation
- monitor blood count and liver function during first 6–12 weeks of treatment

 MOXONIDINE – Physiotens
- contraindicated in heart failure
- withdraw moxonidine gradually over a few days; if a beta-blocker is given in combination, withdraw beta-
blocker first then moxonidine after a few days

Side Effects: somnolence, weakness, dizziness, dry mouth, bradycardia, rash

Dosage: Initially 200mcg once daily in the morning; may be increased up to 400mcg daily in 1 or 2 divided
doses after 2 weeks; maximum 600mcg daily as 2 divided doses.

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AMH Summary: Chapter 6 – Cardiovascular 23

SELECTIVE ALPHA BLOCKERS


Indications: Hypertension, prostate
Side Effects: orthostatic hypotension, nasal congestion, urinary urgency, dizziness, headache, weakness,
fatigue, drowsiness

- Prazosin has a short duration of action and must be taken 2–3 times daily. Terazosin have a longer
duration of action and can be taken once daily.
- THIRD LINE TREATMENT for hypertension

Practice Points:
- first dose hypotension is common with the selective alpha-blockers; it is most serious in the elderly and
in patients with fluid depletion or who are taking diuretics
- to minimise first dose hypotension, start with a small dose of alpha-blocker given before bedtime, and
titrate dose slowly (at 2-week intervals); in patients taking diuretics, withhold diuretic for a few days
before starting alpha-blocker; introduce additional antihypertensives cautiously in patients already taking
an alpha-blocker

 PRAZOSIN – Minipress, Pressin


Dosage: Initially 0.5mg twice daily, increasing to 1mg bd to tds after 3–7 days. Maintenance, 3–20 mg daily
in 2–3 divided doses.

 TERAZOSIN – Hytrin
Dosage: initially 1mg once daily, increase after 7 days to 2mg once daily. Maintenance: 2-20mg once daily.

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AMH Summary: Chapter 6 – Cardiovascular 24

- ARRHYTHMIAS -

ANTI-ARRHYTHMICS
ALL ANTIARRHYTHMICS have the potential to worsen arrthymias. Avoid if possible.
Do not combine verapamil with beta-blocker (unless under specialist supervision); risk of bradycardia and
reduced cardiac output.

Table: Drugs that prolong QT interval (predispose to a fatal arrhythmia)

Class Drugs
Anti-arrhythmics amiodarone, disopyramide, sotalol

Anti-psychotics amisulpride, droperidol, haloperidol, pimozide

Anti-infectives chloroquine, clarithromycin, erythromycin,


fluconazole, mefloquine, moxifloxacin, pentamidine,
quinine, voriconazole

Others arsenic trioxide, cisapride, cocaine, dasatinib,


dolasetron, lapatinib, methadone, sunitinib,
tacrolimus, TCAs, vardenafil

 AMIODARONE – Aratac, Cordarone X 100, 200mg


Precautions: Electrolyte disturbances (eg hypokalaemia, hyperkalaemia, hypomagnesaemia)—increased
risk of arrhythmias; correct before starting treatment if possible.
Thyroid dysfunction, including goitre or nodules—increased risk of hypo- or hyperthyroidism.

Side Effects: Amiodarone has serious adverse effects including potential to worsen arrhythmia
(proarrhythmic effect); these are slow to resolve after it is stopped (very long half-life).

- nausea and vomiting (especially while loading), constipation, anorexia, taste disturbance (metallic taste,
loss of taste), transient elevation of hepatic transaminases, hyper- or hypothyroidism, fever, photosensitivity,
skin pigmentation (blue-grey), benign corneal microdeposits, headache, dizziness, fatigue, neurotoxicity
(tremor, ataxia, paraesthesia, peripheral neuropathy, limb weakness), sleep disturbances (vivid dreams or
nightmares), pulmonary toxicity, bradycardia, hypotension (IV infusion)

Dosage:
- Adult dose: 200–400 mg 3 times daily for 1 week, followed by 200–400 mg twice daily for 1 week.
Maintenance, 100–400 mg once daily.

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AMH Summary: Chapter 6 – Cardiovascular 25

- Concentration monitoring
Therapeutic range, 1–2.5 mg/L.
Concentration monitoring is rarely necessary in practice. Adverse effects may occur within the therapeutic
range.
The maximum effect of dosage change is not seen for 1–3 months or more because half-life is 27–
107 days.

- Counselling:
While taking amiodarone avoid sun exposure, wear protective clothing whenever outdoors, use sunscreen
(broad spectrum, factor 30+ sunscreen containing titanium dioxide is recommended).
Amiodarone interacts with grapefruit juice and many other drugs; avoid grapefruit and tell your doctor or
pharmacist that you are taking amiodarone before starting any new medication.
You will need regular blood tests, ECGs and chest x-rays while taking amiodarone.
Tell your doctor if you develop shortness of breath or a dry cough, problems with your vision, weight loss,
muscle weakness or worsening of your heart symptoms.

Monitoring:
- before starting amiodarone, check baseline clinical status, serum potassium, thyroid and liver function,
lung function (including chest x-ray), and ECG; repeat 6 monthly during treatment
- check ECG for significant QT prolongation (>500 milliseconds)
- amiodarone contains 75 mg iodine in each 200 mg tablet and affects thyroxine metabolism; it complicates
the diagnosis of thyroid dysfunction; when requesting thyroid function tests, notify laboratory that the patient
is taking amiodarone; seek specialist advice
- thyroid function abnormalities and the risk of developing hyper- or hypothyroidism persist for at least
3 months after stopping treatment; liver damage may develop up to a year after stopping treatment
- if dyspnoea or nonproductive cough develop, perform chest x-ray and pulmonary function tests as soon as
possible and monitor closely
- perform eye examination annually; essential for those who develop visual symptoms

 DIGOXIN – Lanoxin PG/Sigmaxin PG 62.5mcg; Lanoxin/Sigmaxin 250mcg


Digoxin has a narrow therapeutic index; adverse effects are related to its plasma concentration and very few
occur at <0.8 micrograms/L. It interacts with many drugs

Precautions:
Hyperthyroidism, fever—increase sympathetic tone; digoxin relatively ineffective; treat underlying cause
and use larger doses or combine with another agent.
Hypothyroidism—may increase sensitivity to digoxin and require smaller doses.
Hypokalaemia, hypomagnesaemia, hypercalcaemia, acidosis, hypoxia—increase risk of digoxin toxicity;
correct abnormality if possible.
Acute MI, ischaemic heart disease, myocarditis—increase risk of arrhythmias.

Side Effects: anorexia, nausea, vomiting, diarrhoea, blurred vision, visual disturbances, confusion,
drowsiness, dizziness, nightmares, agitation, depression

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AMH Summary: Chapter 6 – Cardiovascular 26

- Concentration monitoring:
Take blood sample immediately before dose (trough), or at least 6 hours after dose to allow
for redistribution.
Steady state is reached after about 5 days if renal function is normal (half-life is 36 hours).
The manufacturers recommend a therapeutic range of 0.5–2 micrograms/L (0.5–
2 nanograms/mL).

Practice Points:
- check renal function and electrolyte concentrations before starting digoxin
- onset of effect occurs 4–6 hours after initial dose
- regularly assess patients for evidence of digoxin toxicity (including resting heart rate); routine
measurement of pulse rate before giving next dose of digoxin is not necessary

 DISOPYRAMIDE – Rythmodan 100,150mg


Therapeutic range 2–4 mg/L (6–12 micromol/L).

Precautions:
Impaired ventricular function - disopyramide may precipitate heart failure.
Electrolyte disturbances (eg hypokalaemia, hyperkalaemia, hypomagnesaemia) - increase risk of
arrhythmias; correct before starting treatment if possible.
Diabetes - hypoglycaemia may occur with disopyramide

Side Effects: dry mouth, constipation, nausea, vomiting, blurred vision, dizziness, urinary retention,
dyspnoea, palpitations

Dosage: Initially 200–300 mg. Maintenance, 100–150 mg every 6 hours. Maximum 800mg daily.

 FLECAINIDE – Tambocor
Contraindicated in heart block, or history of MI.

Side Effects: nausea, vomiting, diarrhoea, constipation, headache, dizziness, tinnitus, visual disturbances,
fatigue, tremor, nervousness, paraesthesia, ataxia, heart block (first degree), angina, arrhythmias (new or
worsened), worsening heart failure, dyspnoea, flushing, increased sweating, rash

Dosage: 50-100mg bd

 SOTALOL – Sotacor, Cardol, Solavert, Sotahexal


- avoid abrupt withdrawal in patients with ischaemic heart disease; reduce dose over 8–14 days to avoid
exacerbation of angina and precipitation of MI and ventricular arrhythmias

Indication: Arrhythmias

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AMH Summary: Chapter 6 – Cardiovascular 27

Precautions:
Heart failure – sotalol may precipitate or worsen heart failure
Pulmonary hypertension – exacerbate symptoms
Electrolyte disturbances (eg. hypokalaemia, hyperkalaemia, hypomagnesaemia) – increases risk of
arrhythmias; correct before starting treatment if possible.
Obstructive airways disease – may worsen due to bronchospasm induced by sotalol.
Risk factors for prolonged QT interval
Diabetes – mask signs of hypoglycaemia.

Side Effects: Sotalol has serious adverse effects including the potential to worsen arrhythmia (proarrhythmic
effect). palpitations, hypotension, bradycardia, exacerbation of heart failure, exacerbation of Raynaud's
syndrome, dyspnoea, fatigue, drowsiness, dizziness, headache, disturbances of vision, taste and hearing,
dyspepsia, nausea, vomiting, diarrhoea, impotence, reduced libido, rash

Dosage: Initially 40-80mg bd, increase up to 160mg bd. Maximum dose 640mg daily.

 VERAPAMIL – Isoptin, Anpec, Cordilox


See calcium channel blockers

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AMH Summary: Chapter 6 – Cardiovascular 28

- CHOLESTEROL -
- measure lipids every 4–6 weeks during dose titration (maximum effect of a given dose of lipid regulating
agent is achieved after at least 4 weeks, longer for gemfibrozil); then measure lipids every 6–12 months
during maintenance
- if response to a single agent is inadequate, first question compliance and then consider using an
alternative agent or an additional drug

DRUGS OF CHOICE FOR CHOLESTEROL


a) Statins
b) Bile acid binding resins
c) Fibrates
d) Others: ezetimibe, nicotinic acid

STATINS (HMG-CoA reductase inhibitors)


Precautions: Increases risk of myopathy and rhabdomyolysis; start at low dose and monitor renal function
and creatine kinase regularly.

Side Effects: myalgia, mild transient GI symptoms, elevated transaminase concentrations, headache,
insomnia, dizziness

Counselling: Take once daily, preferably in the evening, because morning doses are slightly less effective.
(Atorvastatin and rosuvastatin can be taken at any time, as it is not affected like this.)
Seek medical advice promptly if you have any muscle pain, tenderness or weakness.

Practice Points: more than 80% of the LDL lowering effect of a statin is achieved with 50% of maximum
dose (eg simvastatin 40 mg); adding a bile acid binding resin (in low dosage), ezetimibe or a sterol
margarine at this point can be much more effective in reducing LDL than increasing the dose of statin
(although effect on clinical outcomes of such combinations, compared to high dose statin alone, are
unknown). In mixed hyperlipidaemia, a statin can be used with a more potent triglyceride lowering drug,
eg fish oil or gemfibrozil if necessary

Monitoring:
- monitor transaminase and creatine kinase (CK) at baseline, repeat during treatment if
indicated clinically; monitoring every 6–12 months is recommended for children taking
pravastatin
- stop statin if:
o transaminase concentrations are persistently elevated to >3 times the upper limit of
normal
o CK concentration is >10 times the upper limit of normal
o there is persistent unexplained muscle pain (even if CK is normal)
- treatment may be resumed after at least 4 weeks if myopathy/myositis was mild and CK
concentration, if raised, has returned to normal. Consider:

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AMH Summary: Chapter 6 – Cardiovascular 29

o whether a precipitant (eg trauma, surgery) or a drug interaction contributed to this


adverse effect (see Statins)
o using a lower dose (as these adverse effects are dose-related)
o using an alternative statin (although there are no data comparing risk between
agents)
- if the problem recurs on rechallenge, stop statins permanently

 ATORVASTATIN – Lipitor
Dosage: 10-80mg once daily. Increase every 4 weeks if necessary.

Avoid grapefruit juice as it may increase the amount of atorvastatin in your bloodstream and could increase
the chances of side effects occurring.

 FLUVASTATIN – Vastin 20,40mg; Lescol XL 80mg


Abdominal pain and dyspepsia are more common with the maximum dose
Dosage:
Conventional capsule, 40 mg once daily; increase after 4 weeks if necessary; maximum 40 mg twice a day.
Range, 20–80 mg daily.
Controlled release tablet, 80 mg once daily, swallowed whole.

 PRAVASTATIN – Pravachol, Lipostat, Cholstat


Dosage: Usual range 20–80 mg daily (in 1 or 2 doses).

 ROSUVASTATIN – Crestor
Dosage: Initially 5 or 10 mg once daily. Usual range, 5–20 mg once daily. Maximum 40 mg once daily
(specialist supervision). Asian start 5mg daily.
Treatment with gemfibrozil, maximum 10 mg once daily.

 SIMVASTATIN – Lipex, Zocor, Zimstat, Simvar; Vytorin 10/20, 10/40, 10/80 (simvastatin +
ezetimibe)
- measure baseline ALT and AST when starting simvastatin and ezetimibe combination
- avoid grapefruit juice as it may increase the amount of simvastatin in your bloodstream and could increase
the chances of side effects occurring.
- myopathy is common with maximum dose.

Dosage: Range 10–80 mg once daily.

BILE ACID BINDING RESINS


- This medicine can reduce the effect of a number of other medicines. The best way to avoid a problem is to
take other medicines at least 1 hour before, or 4–6 hours after, this medicine.
- consider supplements of fat-soluble vitamins (A, D, E and K) for patients taking high doses of resins over a
long period of time

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AMH Summary: Chapter 6 – Cardiovascular 30

Side Effects: constipation, abdominal pain, dyspepsia, flatulence, nausea, vomiting, diarrhoea, anorexia

 CHOLESTYRAMINE – Questran Lite

Dosage: Initially 4 g twice a day, increasing to maintenance dose over 2–4 weeks. Usual range, 12–16 g
daily in 2–3 divided doses. Maximum 36 g daily. Combination treatment with another agent for
dyslipidaemia, 4 g once or twice a day.

Mix with water, juice or highly fluid foods such as soup. Reduce the gritty texture by mixing dose and
standing it in the refrigerator for at least 4 hours or overnight

 COLESTIPOL – Colestid Granules


Dosage: Initially 5-10 g daily in 1–2 doses, increasing gradually every 1-2 months. Usual range, 10-30 g
daily in 2-4 doses. Combination treatment with other lipid regulating agent, 5 g once or twice a day

FIBRATES
Side Effects: GI disturbances (eg dyspepsia, abdominal pain)
Practice Points: measure full blood count and liver function before starting and during treatment

 FENOFIBRATE – Lipidil
Side Effects: increased transaminase concentrations, urticaria, rash
Dosage: 145 mg once daily.

- Avoid exposure of skin to sun, wear protective clothing and use sunscreen.
- Practice Points: monitor hepatic transaminases every 3 months during the first year; stop treatment if
elevated >3 times the upper limit of normal

 GEMFIBROZIL – Jezil, Lopid


Side Effects: dry mouth, headache, myalgia
Dosage: 600 mg twice a day before food.
- Practice Points: consider gemfibrozil for isolated hypercholesterolaemia only if more potent agents
(eg statin, ezetimibe, resin or nicotinic acid) are not tolerated

OTHERS
 EZETIMIBE – Ezetrol
Precautions: Treatment with fenofibrate - ezetimibe may further increase risk of gall bladder disease.
Side Effects: headache, diarrhea
Dosage: 10mg daily

 NICOTINIC ACID

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AMH Summary: Chapter 6 – Cardiovascular 31

- Flushing and stomach upsets usually stop after 2-6 weeks. Can minimize SE but taking with antacids or
food or taking aspirin 150mg half an hour before nicotinic acid
- Monitor liver function and BGL especially at the start

Precautions: Peptic Ulcer disease, Gout, Diabetes, Arrthymias (exacerbations occur)


Side Effects: vasodilation (see Practice points), face and neck flushing, hypotension, dyspepsia, diarrhoea,
nausea, vomiting, hyperpigmentation
Dosage: Initially 250 mg 3 times daily; increase by 250 mg every 4 days to maintenance of 500 mg – 1 g
3 times daily. Take with food.

 OMEGA-3 esters
Indication: Hypertriglyceridaemia
Dosage: 4g daily cc

- PULMONARY HYPERTENSION –

 AMBRISENTAN – Volibris
Side effects: palpitations, constipation
Dosage: 5mg once daily
Practice points:
o Measure ALT/AST concentrations at baseline, each month and 2 weeks after increase in
dosage.

 BOSENTAN – Tracleer
Side effects: increased liver proteins, fatigue, itch, hypotension, muscle cramps, palpitations, decrease
in sperm count.
Dosage: 62.5mg bd for 4 weeks. Maintenance dose 125mg bd
Practice points:
o Measure ALT/AST concentrations at baseline, each month and 2 weeks after increase in
dosage.

 SILDENAFIL – Ravatio
Contraindication: nitrates, ritonavir, ketoconazole or itraconazole
Side effects: nosebleeds
Dosage: 20mg tds
Practice point: reduce dose gradually when drug is stopped

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AMH Summary: Chapter 6 – Cardiovascular 32

- PERIPHERAL VASCULAR DISEASE –

 CILOSTAZOL – Pletal
Side effects: diarrhea, nausea, vomiting, dyspepsia, headache, dizziness, bruising, rash, itch, rhinitis,
peripheral oedema, palpitations, tachycardia, arrhythmia, angina
Dosage: 100mg bd before food

 HYDROXYETHYLRUTOSIDES – Paroven
Side effects: nausea, chronic diarrhea, headache, dizziness, rash, flushing, yellow discoloration of skin
Dosage: 250mg tid to qid for 4 weeks then decrease to 250mg once daily or bd cc

 OXPENTIFYLLINE – Trental
Side effects: nausea, vomiting, dizziness, headache, flushing
Dosage: 400mg bd or tid cc
Practice points: improves healing of venous leg ulcers and is most effective when used with compression

- ORTHOSTATIC HYPOTENSION –
Non-drug therapy: sleeping with head tilted up, salt supplements
Drug treatments: low dose fludrocortisone, caffeine, NSAIDs, pyridostigmine, phenylephrine,
pseudoephedrine, dihydroergotamine

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AMH Summary: Chapter 6 – Cardiovascular 33

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Recommended text
National Heart Foundation. Guide to management of hypertension. Updated December 2010.

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be reproduced or
stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any responsibility for
any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 7 – Blood and Electrolytes 1

AMH SUMMARY: Chapter 7 – Blood & Electrolytes

- ANTICOAGULANTS -

HEPARINS
- Dalteparin and Enoxaparin are Low Molecular Weight Heparins (LMWHs)
- LMWHs have a longer half life (3-6 hours) than heparin (60min), so only require once daily
dosing but costs more.
- HIT (heparin-induced thrombocytopenia) is lower with LMWHs than heparin. Do not use
LMWH as an alternative (danaparoid is ok) in HIT as cross reactivity occurs in 90% of cases.

Side Effects:
bruising and pain at injection site, hyperkalaemia, mild reversible thrombocytopenia (does not
necessarily indicate increased risk for severe thrombocytopenia). Severe thrombocytopenia may occur
in <1% of patients in short term use. This will result in bleeding, stroke, death. Withhold heparins if
platelet count drops 30-50% below baseline. If heparin-induced thrombocytopenia (HIT) occurs, future
use may be contraindicated. Typically occurs within 5-10 days of treatment.

Precautions:
Renal impairment: Use LMWHs (dalteparin, enoxaparin) with caution, monitor clinical condition and
antifactor Xa levels; consider dosage reduction when creatinine clearance is <30 mL/minute

Monitoring:
Monitor platelet count on days 0, 3 and 5, then on alternate days if treatment is continued.
+ Monitor APTT; reference range varies with APTT reagent and is usually about 1.5–2.5 times the
control value. (HEPARIN)
+ Monitor antifactor Xa in patients at high risk of bleeding (eg multiple trauma, renal impairment, thin
or obese patients, pregnant women) or if overdose is suggested by bleeding.(LMWH & Danaparoid)

 DALTEPARIN – Fragmin

Dosage:
Prevention of VTE: SC 2500u d for 5-10days or until mobilized, starting 1-2 hours before surgery
(for moderate risk); SC 5000u d for 5-10 days, starting in evening before surgery (for high risk).

Treatment of VTE: SC 100 unit/kg bd for 5-10 days

Treatment of unstable angina: SC 120 units/kg (max 10000 units) bd for 5-7 days or until stable
with aspirin 150-300mg daily for acute conditions.

 DANAPAROID – Orgaran
Dosage:
Prevention of VTE: SC 750 units bd for 7-10 days or until mobilized, starting 1-4 hours before
surgery.

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AMH Summary: Chapter 7 – Blood and Electrolytes 2

 ENOXAPARIN – Clexane
- marketed for prevention of VTE in patients bedridden due to acute illness; reserve for high risk
patients for VTE (elderly people, acute infection, acute heart failure, respiratory insufficiency) and
at low risk of bleeding.

Dosage:
Prevention of VTE: Surgical patients, moderate risk, SC 20 mg daily for 7–10 days or until
mobilised, starting 2 hours before surgery.
Surgical patients, high risk, SC 40 mg daily for 7–10 days or until mobilised, starting 12 hours
before surgery. May be continued up to 30 days after total hip replacement surgery.
Medical patients, SC 40 mg daily for 6–14 days or until mobilised.

Treatment of VTE: SC 1 mg/kg twice daily, or 1.5 mg/kg once daily, for 5–10 days.

Treatment of unstable angina: SC 1 mg/kg twice daily for up to 8 days with aspirin.

Renal impairment: Dose according to antifactor Xa or creatinine concentration.


1mg = 100 units of antifactor Xa activity.

 HEPARIN
Dosage:
Prevention of VTE: General surgery, SC 5000 units 2 hours before procedure, then 5000 units 2–
3 times daily for 7–10 days or until mobilised.
High risk patients, SC 5000 units 2–3 times daily for 7–10 days or until mobilised.

Treatment of venous and arterial thromboembolism:


IV bolus 5000 units, followed by either IV infusion 1000–2000 units/hour or SC 15 000–
20 000 units every 12 hours. Adjust doses according to APTT.

Acute MI: IV bolus 60 units/kg (4000 units maximum), then IV infusion 12 units/kg/hour
(1000 units/hour maximum), adjusted according to APTT, for 48 hours.

VITAMIN K ANTAGONISTS
 PHENINDIONE – Dindevan
- contraindicated in pregnancy and breastfeeding (CAT D)
- used less frequently than warfarin due to higher incidence of side effects

Dosage: 100mg bd on first day, 50mg bd on second day, then adjust according to INR (2-3). Usual
maintenance 20-80mg bd.

 WARFARIN – Coumadin, Marevan

Dosage: usually 5mg d for 2 days then adjust according to INR 2-3.

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AMH Summary: Chapter 7 – Blood and Electrolytes 3

Counselling:
-Take tablets at about the same time every day; use a calendar or 'anticoagulant book' to keep a
record of your dose and to mark off the date immediately after taking a dose.
-Always take the same brand of tablets.
-This medicine is affected by vitamin K which is found in certain foods (green vegetables). Eat a
normal, balanced diet without varying it too much, to keep your intake stable.
-Avoid excessive alcohol consumption; 1–2 standard drinks per day maximum
-Avoid drinking large amounts of cranberry juice as this may increase the effects of warfarin.
-Tell your doctor and pharmacist that you are taking this medicine before starting or stopping any other
medication or taking vitamin supplements, herbal or OTC products.
- Regular blood tests are required; obtain result within 24 hours of the test and before the next dose, in
case it needs adjusting. Extra blood tests may be needed while you have any other serious illness.
-Tell your doctor immediately if you have any bruising, bleeding, pink, red or dark brown urine, or red
or black stools.

Monitoring: Monitor INR before starting treatment and then everyday until INR stabilizes. In the long
term, monitor at intervals no more than 4 weeks. May have to monitor more frequent if there are
changes in patient’s condition or other illnesses (eg. infections, heart failure, thyroid, changes in
medicines, diet etc)

Over-anticoagulation with warfarin:


 use vitamin k to treat overdose of warfarin (injection is commonly used orally for the small
doses required)
 the anticoagulant effect of warfarin may be difficult to re-establish for several days/weeks after
large doses of vitamin K; if intending to restart warfarin, use the lowest possible dose of
vitamin K
 if over-anticoagulated:
o unexpected bleeding at therapeutic INR, investigate for underlying cause
o INR <5 (no significant bleeding), lower the dose or omit next warfarin dose; resume
warfarin at lower dose when INR is therapeutic
o INR 5–9, stop warfarin; give vitamin K (1–2.5 mg oral or 0.5–1 mg IV); measure INR
within 24 hours and resume warfarin at lower dose when INR is therapeutic
o INR >9, stop warfarin and give vitamin K (2.5–5 mg oral or 1 mg IV); measure INR after
6–12 hours and resume warfarin at lower dose when INR is therapeutic; if bleeding risk
is high consider giving prothrombin complex (factors II, IX & X), with factor VII, or fresh
frozen plasma
o serious bleeding, stop warfarin; give IV vitamin K (5–10 mg) and prothrombin complex
(factors II, IX & X), with factor VII if available, or fresh frozen plasma; monitor patient
continually until INR <5 and bleeding stops

OTHER ANTICOAGULANTS
 BIVALIRUDIN – Angiomax inj

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AMH Summary: Chapter 7 – Blood and Electrolytes 4

- use with aspirin 300 mg daily

Indication: Percutaneous coronary intervention, with aspirin

Dosage: IV bolus 0.75 mg/kg followed by IV infusion 1.75 mg/kg/hour for the duration of the
procedure and for up to 4 hours afterwards; begin treatment just before the procedure.

 FONDAPARINUX – Arixtra

Dosage:
Prevention of VTE: SC 2.5 mg once daily for 5–9 days; give first dose 6 hours after surgical
closure once haemostasis has been established; may be continued up to 31 days after
orthopaedic surgery.

Treatment of VTE: <50kg SC 5mg once daily. 50-100kg SC 7.5mg once daily. >100kg SC 10mg
once daily.

 LEPIRUDIN – Refludan
Indication: Acute heparin-induced thrombocytopenia type 2 with thrombocytopenia or
thromboembolic complications

Side Effects: bleeding (in particular from puncture sites and wounds), abnormal liver function,
cough, bronchospasm, stridor, dyspnoea

Dosage:
Initial IV bolus 0.4 mg/kg (maximum 44 mg) over 15–20 seconds followed by IV infusion
0.15 mg/kg/hour (maximum 16.5 mg/hour) for 2–10 days or longer if necessary.
Adjust dosage according to APTT ratio (target range 1.5–2.5)

Monitoring: monitor APTT ratio 4 hours after starting treatment and then at least once daily (more
often in patients with renal impairment)

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AMH Summary: Chapter 7 – Blood and Electrolytes 5

- ANTIPLATELET -
- used in management of arterial thrombosis not VTE (fibrin clots)
- low dose aspirin is recommended for the prevention of CVD: MI, stroke, high risk patients (eg. acute
and post MI, angina).
- dipyridamole is used with warfarin for prevention of thromoembolism in patients with prosthetic heart
valves; secondary prevention of stroke in combination with aspirin.
- clopidogrel is rarely used in combination with aspirin due to lack of additional benefit (increases risk
of bleeding though)
- avoid ticlopidine due to severe neutropenia side effects.
- Glycoprotein receptor inhibitors are used with heparin and low dose aspirin to prevent ischaemic
cardiac complications following percutaneous coronary intervention (abciximab, eptifibatide) and in
patients with unstable angina (eptifibatide, tirofiban).

Table: Preferred Antiplatelet

Indication Treatment
Primary prevention of CVD Low dose aspirin 75-150mg daily
Stable Angina Aspirin – use clopidogrel if allergic to aspirin

Acute MI Aspirin and clopidogrel with percutaneous coronary


intervention or fibrinolysis
Post MI Aspirin – use clopidogrel if allergic to aspirin. May use
clopidogrel with aspirin together for at least 1 month after
fibrinolytic therapy and up to 12 months after stent placement.

Warfarin may be preferred to aspirin if complications exist


(AF, thromboembolism, aneurysm). Warfarin + aspirin is
effective but increases risk of bleeding.
Coronary artery bypass graft Aspirin
Percutaneous coronary intervention Aspirin and clopidogrel with low dose heparin and
glycoprotein IIb/IIIa inhibitor
Post-intracoronary stenting Aspirin with clopidogrel for at least 1 month and up to
12 months, then aspirin alone
Valve prosthesis Warfarin - add aspirin with warfarin in patients with
mechanical valve prosthesis and embolic risk factors
Acute treatment of stroke Aspirin
Primary prevention of stroke in AF Aspirin – use warfarin for high risk patients
Secondary prevention of stroke Aspirin or aspirin with dipyridamole. Use clopidogrel if allergic
to aspirin. In AF, use warfarin instead.
Peripheral arterial disease Aspirin – use clopidogrel if allergic to aspirin.

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AMH Summary: Chapter 7 – Blood and Electrolytes 6

Glycoprotein IIb/IIIa receptor inhibitors


Indications:
Unstable angina and non–ST-segment elevation MI in high risk patients (tirofiban, eptifibatide)
Percutaneous coronary intervention (abciximab)
Percutaneous coronary intervention with stenting (eptifibatide)
Unstable angina refractory to conventional treatment where percutaneous coronary intervention is
planned (abciximab)

- Stop treatment immediately if emergency coronary artery bypass graft surgery is required.
- Abciximab has a longer duration of action than tirofiban and eptifibatide and is less suitable for
patients likely to need coronary artery bypass graft surgery.
- glycoprotein IIb/IIIa receptor inhibitors are used with heparin, LMWHs or bivalirudin and low
dose aspirin
- stop heparin, aspirin and glycoprotein IIb/IIIa receptor inhibitor if platelet count <100x109/L or
drops 25% below baseline platelet count

 ABCIXIMAB – Reopro
- give low dose aspirin and heparin infusion with abciximab
- monitor PT, APTT, creatinine clearance, platelet count, haemoglobin and haematocrit before
treatment; after starting monitor haemoglobin and haematocrit at 12 hours and 24 hours, and
platelet count at 2 hours and 24 hours

Side Effects: increased risk of thrombocytopenia due to development of antibodies.

Precaution: abciximab infusion within 30 days increases risk of thrombocytopenia.

Dosage:
Percutaneous coronary intervention: IV bolus 250 micrograms/kg before procedure, then infuse
0.125 micrograms/kg/minute for 12 hours.

 EPTIFIBATIDE – Integrilin
Dosage:
Percutaneous coronary intervention: IV bolus 180 micrograms/kg just before intervention, followed by
second bolus of 180 micrograms/kg 10 minutes later. Start IV infusion, 2 micrograms/kg/minute,
simultaneously with first bolus until hospital discharge or up to a maximum of 18–24 hours post
intervention.

Unstable angina: IV bolus 180 micrograms/kg followed by 2 micrograms/kg/minute IV infusion for up to


72 hours until initiation of coronary artery bypass graft surgery or discharge from hospital. If
percutaneous coronary intervention is performed during that time, continue infusion for 20–24 hours
after intervention for a maximum duration of 96 hours in total.

 TIROFIBAN – Aggrastat

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AMH Summary: Chapter 7 – Blood and Electrolytes 7

Dosage: IV 0.4 microgram/kg/minute for 30 minutes, followed by 0.1 microgram/kg/minute for 48–
108 hours.

OTHERS
 ASPIRIN – DBL Aspirin 100mg; Solprin dispersible 300mg; Cartia 100mg enteric coated
- in patients with a history of aspirin-induced ulcer bleeding clopidogrel causes more recurrent ulcer
bleeding than aspirin combined with a PPI

Side Effects: GI irritation, asymptomatic blood loss, increased bleeding time

Dosage: 75–150 mg daily; dose of 150–300 mg daily may be required in acute conditions (MI, acute
ischaemic stroke, unstable angina, placement of intracoronary stent).
1 bd for Asasantin SR (aspirin 25mg + dipyridamole 200mg)

 CLOPIDOGREL – Iscover, Plavix

Side Effects: bleeding, may be severe (includes GI bleeding), diarrhoea, rash

Dosage: 75 mg daily.
Placement of a stent: Loading dose 300–600 mg at least 6 hours before the procedure, then 75 mg
once daily with aspirin; continue for at least 1 month and up to 12 months.

 DIPYRIDAMOLE – Persantin 25,100mg; Persantin SR capsules 200mg


- take on an empty stomach.

Side Effects: headache, diarrhoea, nausea, vomiting, hot flushes, hypotension, tachycardia

Dosage:
Prevention of thromboembolism: 300-600mg daily in 3-4 doses.
Secondary prevention of stroke and TIA: 200mg CR bd

 TICLOPIDINE – Ticlid, Tilodene


- use clopidogrel instead of ticlopidine if possible due to lower risk of severe adverse effects
- risk of neutropenia is greatest in the first 12 weeks of treatment; obtain full blood count at
baseline, then every 2 weeks for 4 months
- stop ticlopidine if neutrophil count is <1.2x109/L or platelet count is <80x109/L; neutropenia is
usually reversible on stopping ticlopidine

Side Effects: diarrhoea, nausea, anorexia, vomiting, upper abdominal pain (tolerance may
develop), minor bleeding, mild-to-severe neutropenia, rash

Dosage: 250 mg twice daily.


Placement of coronary stent, give with aspirin; begin treatment on day of procedure and continue
for 2–4 weeks.

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AMH Summary: Chapter 7 – Blood and Electrolytes 8

- THROMBOLYTICS -
Indications:
Acute MI
Acute massive VTE in patients who are haemodynamically unstable
Peripheral arterial thromboembolism
Thrombosed IV cannulae, central venous catheters
Acute ischaemic stroke within 3 hours of onset of symptoms (alteplase)

Side Effects: bleeding, including bleeding at injection sites, intracerebral bleeding, internal bleeding
(eg GI, genitourinary)

- Streptokinase, alteplase, reteplase and tenecteplase are used in the management of acute MI
within 6–12 hours of onset of chest pain.
- Weight-adjusted heparin is given routinely with alteplase, reteplase and tenecteplase and may
be given with streptokinase in patients at high risk of systemic or venous thromboembolism.
- Streptokinase should be avoided in Aboriginal people and Torres Strait Islanders because of
their frequent high levels of anti-streptococcal antibodies.
- Streptokinase is approved for treatment of deep venous thrombosis and pulmonary embolism;
alteplase is approved for treatment of massive pulmonary embolism.
- Alteplase may be used for the treatment of acute ischaemic stroke in selected patients within
3 hours of symptom onset.

 ALTEPLASE – Actilyse
Dosage:
Acute MI: Give with weight-adjusted heparin. 3-hour IV infusion, 10 mg bolus, then 50 mg over the
first hour and 40 mg over the following 2 hours (if <65 kg adjust so total dose is <1.5 mg/kg).

Pulmonary Embolism: IV, bolus of 10 mg, then 90 mg infused over 2 hours (if <65 kg adjust so
total dose is <1.5 mg/kg).

Acute Ischaemic Stroke: IV, bolus of 0.1 mg/kg, then 0.8 mg/kg infused over 60 minutes
(maximum total dose 90 mg).

 RETEPLASE – Rapilysin
Dosage: Give with weight adjusted heparin. IV, 2 injections of 10 units, 30 minutes apart; give
each bolus injection slowly over no more than 2 minutes.

 STREPTOKINASE – Streptase
- stop heparin before giving streptokinase; check APTT (which should be less than twice the
normal control value before beginning thrombolytic treatment and before reinstituting heparin)

Precaution: Streptokinase treatment or severe streptococcal infection (eg acute rheumatic fever,
glomerulonephritis) in previous 12 months or more—anti-streptokinase antibodies are likely to be
present; efficacy of streptokinase is likely to be reduced.

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AMH Summary: Chapter 7 – Blood and Electrolytes 9

Dosage:
Acute MI: IV infusion, 1 500 000 units over 30–60 minutes.
Deep venous thrombosis, pulmonary or peripheral arterial thromboembolism: IV, 250 000 units
infused over 30 minutes, then 100 000 units/hour for 24–72 hours.

 TENECTEPLASE - Metalyse
- give with weight adjusted heparin

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AMH Summary: Chapter 7 – Blood and Electrolytes 10

- HAEMOSTATIS -
 TRANEXAMIC ACID – Cyklokapron
Indications:
Prevention of hereditary angioedema
Prevention of haemorrhage in patients with mild-to-moderate coagulopathies undergoing minor
surgery
Menorrhagia
Hyphaema

Side Effects: nausea, vomiting, diarrhea

Dosage:
Hereditary angioedema: 1–1.5 g 2–3 times daily either continuously or intermittently
Menorrhagia: 1–1.5 g 3–4 times daily for 3–5 days.

 VITAMIN K/Phytomenadione – Konakion tabs/injection


Indication:
Haemorrhage or threatened haemorrhage due to severe hypoprothrombinaemia, eg excessive
oral anticoagulation, hypovitaminosis K
Prevention and treatment of haemorrhagic disease of the newborn

Side Effects: pain, tenderness and erythema (IM injection)

Dosage:
Reversal of oral anticoagulant effect: 0.5–10 mg, depending on INR and presence of minor or
major bleeding.

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AMH Summary: Chapter 7 – Blood and Electrolytes 11

- ANAEMIA -
ERYTHOPOIETIN AGONISTS
Indications:
Anaemia of chronic renal failure
Chemotherapy-induced anaemia in non-myeloid malignancy
Elective surgery with expected moderate blood loss in patients with mild-to-moderate anaemia
Blood collection before major elective surgery in patients with anaemia
Prevention of anaemia of prematurity

Side Effects: hypertension (especially with rapid haemoglobin rise), headache, flu-like symptoms,
bone pain, myalgia, fever, rash, hypotension, peripheral oedema, nausea, vomiting, diarrhoea,
dyspnoea, increase in platelets, thrombosis of vascular access (patients on dialysis), local pain (SC
route)

- Darbepoetin alfa, epoetin alfa and epoetin beta seem to have similar efficacy and safety. Pain
at injection site seems more frequent with darbepoetin alfa.
- Darbepoetin alfa has a longer duration of action than epoetin which may allow less frequent
dosing.

 DARBEPOTIN ALFA – Aranesp


 EPOETIN ALFA - Eprex
 EPOETIN BETA – NeoRecormon

OTHER DRUGS FOR ANAEMIA


 FOLIC ACID
- folic acid decreases risk of elevated liver enzymes, and mucosal and GI adverse effects in
patients receiving methotrexate for treatment of rheumatoid arthritis and psoriasis

Dosage:
Treatment of folate deficiency: 5mg d for at least 4 months
Prevention of folate deficiency: 0.5mg d before conception and for first 12 weeks of pregnancy in
low risk women. 5mg daily for high risk women.
With MTX 1-5mg once daily.

 IRON – Ferrogradumet, Ferro-liquid, Ferrosig, Ferrum H


Side Effects: abdominal pain, nausea, vomiting, constipation, diarrhoea (all dose-related), black
discolouration of faeces

Dosage:
Treatment of iron deficiency: 100–200 mg daily.

 VITAMIN B12 - Neo B12


Dosage:
Initial treatment: IM 1000 micrograms on alternate days for 1–2 weeks or until improvement occurs.

Copyright © The Medicine Box 2009


AMH Summary: Chapter 7 – Blood and Electrolytes 12

Prevention and maintenance: IM 1000 micrograms every 2–3 months.

- ELECTROLYTE IMBALANCE -
 POLYSTYRENE SULFONATE RESINS– Resonium A
Indication: Hyperkalaemia

Side Effects: gastric irritation, constipation, faecal impaction, diarrhoea, nausea, vomiting, anorexia,
hypokalaemia, sodium retention (sodium resin), hypocalcaemia (sodium resin), hypercalcaemia
(calcium resin)

Dosage: oral 15 g as a suspension or paste, 3–4 times daily. Rectal 30g as an enema.

 ALUMINIUM HYDROXIDE – Alu-Tab


Indication: Hyperphosphataemia in chronic renal failure
Dosage: 600–1200 mg with food, up to 4 times a day.

 CALCIUM CARBONATE – Caltrate


Indication: Hyperphosphataemia in chronic renal failure
Dosage: 168–1200 mg elemental calcium (given as 420–3000 mg calcium carbonate) with each
meal according to clinical response.

 LANTHANUM – Fosrenol
Indication: Hyperphosphataemia in chronic renal failure requiring dialysis
Side Effects: nausea, vomiting, diarrhoea, constipation, abdominal pain, hypocalcaemia
Dosage: Initially 250–750 mg 3 times daily (with each main meal). Maintenance 500 mg–1 g
3 times daily (with each main meal).

 SEVELAMER – Renagel
Indication: Hyperphosphataemia in chronic renal failure
Side Effects: nausea, vomiting, diarrhoea, constipation, flatulence, dyspepsia, abdominal pain, itch,
rash, hypertension, cough, dyspnoea, headache
Dosage: 800–1600 mg 3 times a day with each main meal, then adjust dose according to serum
phosphate concentration

- sevelamer has the potential to bind fat-soluble vitamins A, D, E and K; monitor and give
supplements if necessary (give them 1 hour before or 3 hours after sevelamer)

Copyright © The Medicine Box 2009


AMH Summary: Chapter 7 – Blood and Electrolytes 13

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2009

Copyright © The Medicine Box 2009

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2009


AMH Summary: Chapter 8 – Dermatological 1

AMH SUMMARY: CHAPTER 8 – DERMATOLOGICAL


GENERAL PRINCIPLES • Topical immunomodulators
• Tar and ichthammol
Photosensitivity • Antihistamines (sedating antihistamines are useful at night in patients
• Systemic photosensitisers: amiodarone, griseofulvin, NSAIDs, having trouble getting to sleep)
phenothiazines, methoxsalen, quinolones, retinoids, St John’s wort, • Systemic immunomodulators including corticosteroids, cyclosporin and
tetracyclines, thiazides azathioprine
• Topical photosensitisers: triclosan, coal tar derivatives, methoxsalen, • Phototherapy: UVB phototherapy, photochemotherapy using
retinoids, sulfonamides methoxsalen, PUVA are effective in unresponsive eczema
• No evidence for evening primrose oil
DRUGS FOR ECZEMA
Special cases
Treatment • Atopic dermatitis
• Hydration using tepid water, bath oil or colloidal oatmeal • Nappy dermatitis
• Wet compresses for acute infected eczema (with exudative or crusting • Eyelid dermatitis (moisturisers, pimecrolimus, topical corticosteroids
lesions) using aluminium acetate (Burow’s solution) or potassium may be used)
permanganate (Condy’s crystals). Hydrate area, apply emollient and/or • Secondary infection (bacterial, viral or fungal)
topical corticosteroid then apply wet compresses for 15-60 mins. • Seborrhoeic dermatitis in adults (treat with ketoconazole, miconazole,
• Moisturisers selenium sulfide, pyrithione zinc, ciclopirox, coal tar)
• Topical corticosteroids
Class Generic name Brand name Counselling and practice points
Betamethasone Diprosone Potency
• Mild: hydrocortisone, hydrocortisone acetate
Clobetasone Becoderm-C Flareup • Moderate: betamethasone valerate (0.02-0.05%), clobetasone, desonide, triamcinolone
• Potent: betamethasone diproprionate, betamethasone valerate (0.1%), mometasone, methylprednisolone
Desonide Desowen • Very potent: betamethasone diproprionate in an optimised vehicle

Hydrocortisone Sigmacort Pregnancy


Corticosteroids

• Pregnancy. Desonide, mometasone are ADEC category B3. The others are ADEC category A.
Methylprednisolone Advantan
Site of application
Momethasone Elocon • Use hydrocortisone on face and on skin folds. If unresponsive, use methylprednisolone for 2-3 days (max 7
days). Take caution if applying topical corticosteroids onto eyelids. Avoid potent corticosteroids on these
Triamcinolone Aristocort areas.

Other
• Use for shortest period possible. Avoid contact with broken skin, eyes, mouth and mucosal membranes
• Wet wrap treatment may used for acute eczema
• Protection with polythene films may be used on the palms and soles; use gloves for hands

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 2

Class Generic name Brand name Counselling and practice points


Tar Coal tar Ionil T Plus General
• Antipruritic and mildly antiseptic
Ichthammol Egoderm • Longer lasting anti-inflammatory properties and fewer adverse effects than topical corticosteroids but less
potent and messier to use
Wood tars Pinetarsol
Coal tar
•Avoid contact with eyes
•Coal tar may stain skin, hair, clothes, pillow, bath tub.
•L8 *. Remove coal tar preparations before sunlight exposure.
•Combined with salicylic acid, sulfur, allantoin (keratolytic properties), zinc oxide (astringent properties), or
pyrithione zinc (bacteriostatic and fungistatic properties)

Other Moisturisers Sorbolene • Humectants attract transdermal water to the stratum corneum and so moisture levels are preserved
• Emollients smooth the skin surface by filling oil droplets into spaces between dry skin flakes

Pimecrolimus Elidel • Topical immunomodulators are as effective as potent corticosteroids but are expensive
(anti-inflammatory, • Suitable for patients > 2 years of age
calcineurin • Apply thin film twice a day to affected areas
inhibitor) • Avoid contact with eyes, mouth and inside your nose
• L8 * - Wear protective clothing and use sunscreen
• Facial flushing or skin irritation may occur after drinking alcohol
• Treatment period is usually no more than 6 weeks.

* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 3

DRUGS FOR ACNE

Treatment Counselling
• Topical: Retinoids, benzoyl peroxide, azelaic acid, antibacterials • Wash affected areas gently. Do not scrub skin using abrasive
(clindamycin and erythromycin) cleansers as this may cause more inflammation and worsen acne
• Oral: Antibacterials (doxycycline, minocycline, erythromycin), hormonal • Avoid using toners and oil-based moisturisers
treatments (oestrogens in COCs, cyproterone, spironolactone), • Avoid squeezing or picking acne lesions to minimise scarring
isotretinoin • Eat a healthy balanced diet. No relationship exists between particular
• Other: Effectiveness of preparations containing aluminium oxide, foods and acne.
triclosan, sulphur, salicylic acid, resorcinol, or allantoin is questionable

Class Generic name Brand name Dose Side effects Other comments
Adapalene Differin n • Erythema, peeling, • Wash with warm water, rinse and gently pat dry before applying retinoid cream
irritation, dry skin • Avoid contact with eyes, lips, sunburnt areas
Isotretinoin Isotrex n • Do not use during • L8 * - Protect treated areas from sunlight with protective clothing or sunscreen
Retinoids (skin)

pregnancy (Cat X) • Use a moisturiser to prevent the skin from becoming dry and irritated
Tazarotene Zorac n • Cosmetics may be used minimally but wash them off before applying
medication
Tretinoin Stieva-A n • Avoid waxing treated areas as it may cause irritation
• Acne may temporarily worsen in the first few weeks of treatment. Do not be
discouraged. Do not stop treatment as a result of this.
• Tretinoin is also indicated for photoageing & tazarotene for plaque psoriasis
Acitretin Neotigason 25-50mg d • Dryness of skin, • Isotretinoin is indicated for acne where as acitretin is for severe psoriasis and
lips and mucous keratinisation disorders.
Isotretinoin Roaccutane 0.5mg/kg d membranes • Take with food to maximise absorption
(treatment • Hair thinning • If lips become dry, use Vaseline. For dry eyes, use lubricant eye drops.
course • Myalgia • L8 * - Protect skin from sunlight with protective clothing or sunscreen
Raised liver • Avoid taking vitamin A supplements
Retinoids (oral)


enzymes • Avoid waxing and dermabrasion for half a year after stopping treatment to
(C/I in severe liver minimise scarring and skin irritation
impairment) • Avoid using topical anti-acne preparations as local irritation may increase
• Hyperlipidaemia • Report promptly if you notice mood swings, nausea, headaches or visual
(C/I in those with changes
existing hyper- • The treatment course is usually 3 months for acitretin and 4-6 months for
lipidaemia) isotretinoin.
• Do not use during • Do not donate blood during treatment and after treatment for at least 8 weeks
pregnancy (Cat X) (for isotretioin) and 2 years (for acitretin)
or with tetracycline • Use adequate contraception before, during and after treatment for 1 month (for
(risk of intracranial isotretinoin) and for 2-3 years (for acitretin). The POP is considered unsuitable.
hypertension) • Avoid alcohol during, and for 2 months after treatment.
* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 4

Class Generic name Brand name Dose Side effects Other comments
Oral retinoids (cont.) Monitoring
• Complete blood count, biochemical profile, liver function and fasting blood
lipids should be measured at baseline and during treatment
• Blood glucose should be monitored throughout treatment in patients who have
type 1 diabetes
• Radiological evaluation for skeletal hyperostosis is recommended in patients
receiving long term treatment (> 1 year)

Azelaic acid Finacea bd • Scaling, itch • Before applying, wash affected areas with mild soap or soap substitute and
warm water; gently pat dry
• Wash hands after application
Other

• Avoid contact with eyes


Benzoyl Benzac d-bd • Skin dryness • Azelaic acid should be used cautiously in patients with dark complexions since
peroxide it may cause hypopigmentation
• Benzoyl peroxide may bleach coloured fabrics

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 5

DRUGS FOR SKIN INFECTIONS

Class Generic name Brand name Dose Other comments


Bifonazole Mycospor d Treatment for tinea
• Topical: Azoles are the treatment of choice (fungistatic). Terbinafine produces a more rapid response
Clotrimazole Canesten 2-3 times d than azoles (fungicidal) but is more expensive. Tolnaftate is less effective than both these agents.
• Systemic: Griseofulvin (mainly targets dermatophytes), itraconazole, terbinafine
Econazole Pevaryl 2-3 times d • Other: Condy’s crystals or Burow’s solution for interdigitalis infections, saline compresses or drying
Azoles

agents for acute vesicular tinea pedis


Ketoconazole Nizoral 1-2 times d
Treatment for cutaneous candidiasis (umbilicus, groin, beneath breasts, between skin folds)
Miconazole Daktarin d • Topical: Azoles, nystatin, terbinafine
• Systemic: Fluconazole, itraconazole, ketoconazole
• Other: topical corticosteroids to reduce inflammation
Anifungals

Treatment for nail infections


Amorolfine Loceryl 1-2 weekly
• Systemic: Terbinafine, itraconazole, fluconazole, griseofulvin
• Topical: Amorolfine (mainly for superficial infection of distal end of nail)
Ciclopirox Stieprox twice weekly
Counselling
Nystatin Mycostatin 2-3 times d
• Continue using the treatment for 2 weeks after symptoms have gone (except terbinafine)
Other

• Creams are generally preferred. Sprays may be applied to areas difficult to reach. Lotions may be
Terbinafine Lamisil d
applied to hairy areas. Powders may be used on feet, groin and inside socks and shoes
• Counsel on personal hygiene eg. dry between toes, use a separate towel for infected area, wear
Tolnaftate Mycil bd
thongs in public areas, change socks daily, avoid sharing towels. Discard old shoes.
• Nystatin: Avoid occlusive dressings which promote growth of yeast and release of endotoxins.
• Amorolfine: File down the affected nail, clean with alcohol swab, and apply nail lacquer once or twice
weekly (6 months for finger nails and 12 months for toe nails). Do not use cosmetic lacquers or
artificial nails during treatment. Wear impermeable gloves if using organic solvents.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 6

Class Generic name Brand name Dose Other comments


Clindamycin Clindatech bd Clindamycin and erythromycin
• Wash affected areas with warm water, rinse and pat dry before applying cream.
Erythromycin Eryacne bd • Avoid contact with eyes, lips and inside of your mouth or nose
• Maximum benefit seen after 8-12 weeks.
Antibacterials

Metronidazole Rozex bd
Metronidazole
Mupirocin Bactroban tds •Indicated for rosacea
•Condition should improve after 3 weeks
Silver sulfadazine Flamazine d
Mupirocin
Sodium fusidate Fucidin 2-3 times d •Children with impetigo should remain at home until treatment is started and improvements can be
seen. Sores on exposed surfaces must be covered with a watertight dressing when the child returns
to school.

Silver sulfadiazine
• Indicated for prevention and treatment of infection in severe burns, leg ulcers and pressure sores
• Contraindicated in patients with sulphonamide allergy
• A thick layer (3-5 mm) can be applied daily or more frequently

Sodium fusidate
• Topical sodium fusidate may promote bacterial resistance

Aciclovir Zovirax 5 times d • Wash hands before and after use


Avoid contact with eyes and inside of mouth
Antivirals


Idoxuridine with Virasolve q4h • Do not rub eyes after touching a cold sore
lignocaine • Do not share eating utensils
• Avoid kissing
Penciclovir Vectavir 6 times d • Treat as early as possible in course of infection

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 7

SCABICIDES AND PEDICULICIDES

Generic name Brand name Other comments


Benzoyl benzoate Ascabiol Scabies
• Drug choice: Permethrin 5%, benzyl benzoate, crotamiton, maldison. Perimethrin 5% is the treatment of choice.
Crotamiton Eurax • Benzyl benzoate: Apply to clean, dry skin from chin down and wash off 24 hours later. Repeat after 5 days (reduces
possibility of treatment failure). Dilution is required for children.
Ivermectin Stromectol (oral) • Permethrin 5%: Apply to clean, dry skin from chin down. Leave on skin for 12 hours. Wash with warm soapy water and
rinse thoroughly. Repeat after 7 days (reduces possibility of treatment failure).
Maldison KP 24 • Apply on every inch of the body – between fingers and toes, under nails, in skin folds, to belly button, between the
buttocks and to groin area. In children > 2 years, elderly or immunocompromised people, also apply to the scalp, neck,
Permethrin Lyclear Pyrifoam face and ears.
Lice Breaker • If you wash your hands during the treatment period, reapply the lotion to the washed area.
• Soft toys, bed linen and clothing that have come in contact with the patient should be washed and dried on hot machine
Pyrethrins with Banlice settings the morning after each treatment. These should then be stored in sealed plastic bags for at least 3 days.
piperonyl butoxide • The itch may last for 2-3 weeks. This is not a sign of ongoing infestation. Treat with moisturiser, topical corticosteroids,
crotamiton or an antihistamine.
• Review one month after initiation of treatment. This is the time it takes for lesions to heal and for any eggs and mites to
mature if treatment is unsuccessful.
• The affected person and all household contacts should be treated at the same time to avoid re-infection.

Head lice
• Drug choice:
- Neurotoxic insecticides: permethrin 1%, maldison, pyrethrins with piperonyl butoxide. Pemethrin 1% is the treatment of
choice in pregnancy and breastfeeding, and has a short application time (10 minutes). Maldison is safe for children > 1
year old and requires a long application time (12 hours).
- Physical insecticides: benzyl alcohol, dimeticone 4%, isopropyl myristate
• Maldison: Apply lotion to dry hair and leave in hair for 8-12 hours. Use a lice comb to remove dead lice. Repeat
treatment after 7-10 days to kill any newly hatched lice. The lotion is preferred over the shampoo as the contact time is
longer. Wear gloves while applying and wash hands afterwards.
• Permethrin 1%: Apply to damp hair after washing with usual shampoo. Leave on hair for 10 minutes before rinsing with
warm water. Use lice comb to remove dead lice. Repeat after 7 days.
• Only treat if live louse is found
• Avoid contact with eyes, mouth and inside nose.
nd
• Treatment requires 2 applications 1 wk apart. The 2 treatment kills the lice that have hatched since the first application.
• Avoid using a hair dryer during treatment as heat can destroy the active ingredient.
• Avoid using conditioner for at least 1 day before and after treatment.
• Send children back to school after the first treatment.
o
• Wash pillow cases and towels in hot water. Soak combs and hairbrushes in hot water (> 60 C) for 30 seconds.
• Ensure hats and hairbrushes are not shared.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 8

DRUGS FOR PSORIASIS

Drugs which could exacerbate psoriasis: lithium, hydroxychloroquine, ACEIs, NSAIDs, -blockers

Drug choice
• Topical: moisturisers, salicylic acid, coal tar, dithranol, topical corticosteroids, calcipotriol, tazarotene
• Phototherapy: UVB light, PUVA
• Systemic: acitretin, immunosuppressants (methotrexate, cyclosporin, ustekinumab, hydroxyurea), TNF- antagonists

Class Generic name Brand name Formulation Side effects Other comments
Immuno- Cyclosporin Cicloral Oral • Infection • L8, L18 *
modulators • Renal insufficiency (C/I in renal • Clean your teeth and gums thoroughly
impairment; use with caution in those • Seek medical attention if you notice signs of infection
+
treated with K , ACEIs, angiotensin II • Also indicated for severe psoriasis and prevention of
antagonists and nephrotoxic agents organ transplant rejection
including NSAIDs, aminoglycosides) • Monitoring: blood (FBE), renal (CR, urea), liver (AST,
+
• Anaemia ALT), BP, K , urinalysis
+
• K , BP, cholesterol
• Gingival hyperplasia
Methotrexate Methoblastin Oral • Myelosuppression • Take on the same day each wk
Injection • Pulmonary toxicity • L8 **
• Hepatotoxicity • Seek medical attention if you notice cough, difficulty
• Photosensitivity breathing, bleeding, or signs of infection
• Lymphoma • Give folic acid or folinic acid supplement to reduce GI
• Severe skin reactions (rare) effects (nausea, diarrhoea). Usual dose is 1-5mg daily.
• Also indicated for treatment of solid tumours, severe
disabling psoriasis
• Avoid conception until 3 months after stopping treatment
for either partner
• Monitoring: blood (FBE), renal (Cr), liver (AST, ALT),
lung (PFT), chest x-ray
Ustekinumab Stelara Injection • Infection • Check patient for infection, active/latent TB
TNF- Adalimumab Humira All injections • Infection • Seek medical attention if you notice signs of infection
antagonists Etanercept Enbrel • Worsening HF • Some vaccines should not be given to people receiving
• Blood dyscrasias TNF- antagonists
Infliximab Remicade • Monitoring: blood (FBE), renal (Cr), liver (AST, ALT),
skin cancer

* L8 stands for ancillary label 8, L18 stands for ancillary label 18

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 9

Class Generic name Brand name Formulation Side effects Other comments
Other Calcipotriol Daivonex Cream • Skin irritation •Avoid use on skin folds and face to minimise potential irritation
Ointment •Wash hands after use.
Liquid •L8 *
•Do not mix with other preparations. Calcipotriol is unstable in the presence of
salicylic acid or UVA.

Dithranol Micanol Cream • Skin irritation • Dithanol stains the skin brown. Pigmentation clears about 2 weeks after
Ointment stopping treatment.
Paste • Wear plastic gloves to prevent staining of hands and wash hands after use.
• Avoid using dithranol on face, skin folds, genitals and blistered areas of skin.
• Wash bathtub or shower with hot water immediately after use and use a
household cleaner if further cleaning is required.
• Dithranol will stain clothing and linen permanently.
• Keep in a dark place and combine with salicylic acid to minimise oxidation of
dithranol into an ineffective brown/purple powder.
Methoxsalen Available Oral • Itch, nausea • L8 *
(for photo- through SAS Solution (oral) • Do not sunbathe for 24 hours before and 48 hours after PUVA therapy.
sensitisation Serious burning may occur of there is overexposure to sunlight or artificial UV
before UVA emission after taking methoxsalen
phototherapy) • Wear wrap-around sunglasses with 100% UVA-absorbing properties for at
least 24 hours after oral treatment otherwise cataracts may occur.
• Avoid foods containing natural photosensitisers (limes, figs, parsley, parsnips,
mustard, carrots and celery)
• Baseline and annual monitoring of eye function, liver function, antinuclear
antibodies
Salicylic acid Ionil Cream • Skin irritation • Avoid contact with eyes, lips and inside your mouth or nose
Lotion • Wash hands immediately after applying medication
Gel • Keratolytic activity of salicylic acid potentiates effects of topical corticosteroids,
Liquid dithranol and tar by increasing their penetration into skin.
Paint
Coal tar Linotar Gel Cream • Skin irritation • Stains clothing, skin, hair
Lotion • Unpleasant smell
Gel • L8 *
Ointment
Shampoo
Paste
Paint
* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 10

DRUGS FOR WARTS

Treatment choices Practice points


• Cutaneous warts: salicylic acid, glutaraldehyde, podophyllum resin. • Minimise the risk of cross-infection by using individual towels and
Salicylic acid is an irritant and should not be applied onto the face or avoiding skin maceration
broken skin. It should be used with caution in those with diabetes and • In patients with diabetes, lesions may be best left untreated since poor
PVD. circulation may result in infection.
• Anogenital warts: podophyllotoxin, imiquimod

Generic name Brand name Other comments


Glutaraldehyde Diswart • Soak skin to soften area, dry surface completely, abrade wart surface with pumice stone and protect surrounding skin with
(antimicrobial) white soft paraffin before application.
• Apply twice daily. Treatment may be continued for 3 months.
• Avoid contact with eyes, face, broken skin and other sensitive areas
• This medicine is highly inflammable. Keep away from flames at all times.
• Stains brown.

Imiquimod Aldara • Apply at night.


• Do not bathe and shower after application
• Prior to application, wash affected area with mild soap and water and allow to dry
• Wash hands before and after use
• Wash off with mild soap and water about 6-10 hours later.
• Apply to the affected area 3 times a week (M, W, F). If you decide to have sex, apply the cream afterwards or wash it off if
you have already applied the cream. Continue treatment for maximum of 16 weeks.

Podophyllotoxin Wartec • 7-day treatment cycle: apply twice a day for 3 days followed by no treatment for 4 days; treatment cycle may be repeated as
(antimitotic) necessary for up to 4 cycles. See CMI for detailed instructions and further precautions.
• Wash hands before and after use.
• Avoid contact with eyes.
• Wash affected area with mild soap and allow to dry prior to application.
• Do not bathe or shower after application.

* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 11

DRUGS FOR ACTINIC KERATOSES

Generic name Brand name Dose Other comments


Diclofenac Solareze bd for 60-90 days • Avoid contact with eyes and mouth
• L8 *

Fluorouracil Efudix d-bd • L8 *


• Avoid contact with eyes and mouth.
• Your skin will redden, blister, peel or crack where you apply this cream, this is expected.

Methyl Metvix See AMH • Avoid sun exposure on treated areas for a couple of days after treatment.
aminolevulinate • Pain during and after treatment may require oral analgesics.

Imiquimod Aldara See comments • Basal cell carcinoma: Apply to the affected area 5 times a week. Apply to the lesion and about 1cm of
the surrounding skin. L8 *. Do not apply cream near the hairline, eyes, ears, nose or lips. Treat for 6
weeks.
• Actinic keratoses: Apply to entire treatment area 3 times a week. L8 *. Avoid contact with eyes, lips,
nostrils. Treat for 16 weeks.

DRUGS FOR ALOPECIA

Generic name Brand name Dose Other comments


Finasteride Propecia 1d • Used to reduce unwanted facial hair
• Continuous treatment is needed to maintain response. Not all hair is recovered.

Minoxidil Rogaine 1mL bd where hair • Wash hands after use


regrowth is needed • Continuous treatment is required to maintain response. At least four months of treatment is needed
before hair regrowth is obvious.
• Do not wear a wig, scarf or hat for at least 1 hour after application. This may caused undesirable adverse
effects due to an increased amount of minoxidil being absorbed

* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 12

OTHER

Generic name Brand name Dose Other comments


Eflornithine Vaniqa bd • Apply a thin layer to the affected areas of face and chin twice daily
(ornithine • Do not wash treated areas for at least 4 hours after applying the cream
decarboxylase • This cream only reduces the rate of hair growth. Other forms of hair removal may still be needed. Do not
inhibitor to apply the cream until at least 5 minutes after waxing or shaving.
unwanted facial • If irritation, apply once daily. Stop treatment if irritation continues
hair) • Continued use is required to maintain an effect.

Sunscreens Sunsense As directed • Chemical agents: Only benzophenones absorb both UVA and UVB radiation. Physical barriers (titanium
dioxide, zinc oxide) reflect most UV radiation, providing protection against UVA and UVB
• The SPF is the ratio of minimum UV energy required to produce minimal erythema on skin protected by
sunscreen to energy required to produce the same erythema on unprotected skin. Doubling the SPF
does not equate to doubling the safe exposure time.
• If sunscreen and insect repellent are to be applied at the same time, a combination product containing
low concentration DEET may be more suitable.

* L8 stands for ancillary label 8

Copyright © The Medicine Box 2013


AMH Summary: Chapter 8 – Dermatological 13

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 9 – Ear, Nose and Throat 1

AMH SUMMARY: CHAPTER 9 – EAR, NOSE AND THROAT

A. EAR INFECTIONS

Acute Otitis Media (AOM)


1. Definition: infection of the middle ear cavity
2. Prevalence: children
3. Symptoms: pain, fever and irritability (in infants)
4. Cause: viruses or bacteria (S.pneumonia, H.influenza or M. catarrhalis)
5. Treatment (symptomatic):
Age Treatment
6-24 months Reassessed if symptoms persist after 24 hrs Symptomatic treatment
>2 years Antibacterial only indicated if symptoms for pain and fever
persist after 48 hrs

6. Drug choice (symptomatic):


a. Analgesics
• Paracetamol/ NSAIDs

b. Antibacterial
• Indicated in patients with
- Persisting systemic features (fever & vomiting)
- Aboriginal and Torres Strait Islander children
- Immunocompromised patients

• Choice of antibacterial:
- Amoxycillin
- Cefaclor
- Cefuroxime
- If poor response to amoxicillin, then amoxycillin with clavulanic acid

N.B. NOT INDICATED – topical antihistamine, decongestant or antibacterial ear drops

Summary of characteristics and treatment for different forms of otitis media


Acute Suppurative Recurrent acute Glue ear
• Pain, fever and • Perforated • > 3 episodes of • Fluid behind an
irritability (in eardrum & AOM in 6 months/ intact eardrum in
infants) mucopurulent > 4 episodes in 12 the absence of
• Effusion often discharge months signs and
persists for • Risk factor for symptoms of
Characteristic

several weeks chronic acute infection


after AOM; suppurative otitis • Lasting > 3
resolved media & otitis months
spontaneously media with
effusion (Glue ear)
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AMH Summary: Chapter 9 – Ear, Nose and Throat 2

Acute Suppurative Recurrent acute Glue ear


5 days 10 days • Referral to ENT • Resolution may be
Length of treatment specialist – enhanced with
suspected oral antibacterial
complications/ treatment for 10-
antibacterial 14 days
resistance

Chronic suppurative otitis media


1. Prevalence: remote communities
2. Treatment:
a. Non-pharmacological:
• Debris & discharge removed QID by ear toilet (rolled tissue); continue until dry
• Ear toilet may sometimes be followed by 1% acetic acid.

b. Pharmacological:
• Ciprofloxacin ear drops
• Chloramphenicol ear drops
• Aminoglycoside-containing ear drops

WARNING FOR AMINOGLYCOSIDE


Avoid in perforated eardrum/ tympanostomy tube (grommets)
Stop medication if ringing in ears, hearing loss/ gait develops

REFER TO ENT SPECIALIST IF TREATMENT RESISTANT/


DISCHARGE PERSIST FOR >1 MONTH

Otitis Externa

1. Definition: inflammation of the external ear canal


2. Symptoms: white ‘blotting paper’ debris/ black spores on auroscopy – fungi
3. Cause:
• Bacteria
• Fungi
• Dermatitis
• Foreign objects
• Local trauma
• Water in ear canal – swimming

4. Treatment:
a. Non-pharmacological
• Meticulous gentle cleansing and drying with ear toilet (rolled tissue paper)
• Repeat at least daily in severe infection

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AMH Summary: Chapter 9 – Ear, Nose and Throat 3

b. Pharmacological
• Topical agents can be used in addition to ear toilet
• Inflammation – avoid products with alcohol or acetic acid; may cause irritation &
pain
• Absence of fungal infection – use topical corticosteroid/ antibacterial combination
• Fungal / no improvements after 48 hours – use topical antifungal

Drug Class Generic Came Important Points


antibacterial framycetin Not to be used for > 7 days due to risk of fungal infection
neomycin Consider antiseptics as an alternative
chloramphenicol
combined framycetin Not to be used for > 7 days due to risk of fungal infection
antibacterial gramicidin Use when cause of infection is unidentified
dexamethasone
antifungal nystatin Only present in combination products
clioquinol Consider topical antifungal agent as an alternative
eg nystatin, clotrimazole, miconazole
antiseptic/ acetic acid May be instilled regularly as a preventative measure
drying agent ethanol eg after swimming and showering

5. Prevention:
• Keep ears dry
• Avoid local trauma
• Avoid swimming
• During treatment, use cotton balls with petroleum jelly while showering/ bathing
• Following treatment, use ear plugs while swimming, showering/ bathing; alcohol
after exposure to water.

Administration of ear medication

1. Ear drops:
• Warm container in cup of warm water.
• Clean and dry ear.
• Gentle massage/ pressure ear tragus.
• Lie with the affected ear uppermost
• Instillation:
- Minimal swelling – instil drops directly into ear canal; remain in position for few
minutes
- Swelling – saturate sponge wick or ribbon gauze with drops; insert into ear
canal; review daily until swelling subsides
2. Ear ointment:
• Small amount squeezed into ear canal/ around ear.

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AMH Summary: Chapter 9 – Ear, Nose and Throat 4

B. EAR WAX

Ear wax
1. Prevalence: Older people
2. Symptom: deafness, pain
3. Cause: wax build up associated with hearing aids and cotton bud use
4. Treatment:
• Gentle syringing with warm water (37° C)/ sodium chloride 0.9 % solution
• Wax (impacted/ hard) – cerumenolytic drops before syringing
a. Carbamide peroxide: 5-10 drops BD for up to 4 days
b. Docusate: Fill ear canal with drops for 2 consecutive nights before syringing
c. Sodium bicarbonate: 5 drops BD for 3-4 days
d. Dichlorobenzene + Chlorobutol: 5 drops - BD for few days or
- 10-30 min before syringing
5. AVOID SYRINGING
• History of otic surgery
• Perforated eardrum
• Otitis media/ externa

C. VESTIBULAR DISORDERS

Tinnitus
1. May be:
• Idiopathic
• Associated with hearing loss
• Prominent feature of Ménière’s disease
2. Caused by:
• Ear wax
• Otitis media
• Drugs
- Aspartame
- Salicylates
- NSAIDs
- Aminoglycoside
- Loop diuretics

3. Possible treatment:
• Hearing aids – increase awareness of surrounding ambient noise
• TCA – limited use because of adverse effects

Vertigo
1. Characteristics:
• Mild
• Self-limiting
• Idiopathic

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AMH Summary: Chapter 9 – Ear, Nose and Throat 5

2. Benign paroxysmal positional vertigo


• Symptoms: severe, short-lasting vertigo induced by certain head position
• Treatment
- Non-pharmacological: Postural retraining – Epley manoeuvre
- Pharmacological: Severe persistent symptoms – surgery

3. Vestibular neuronitis (labyrinthitis)


• Definition: inflammation of vestibular nerve
• Symptom: nausea, vomiting, nystagmus
• Caused: virus
• Treatment:
- Usually self-limiting
- Acute attack – prochloperazine, antihistamine (cyclizine, dimenhydrinate,
promethazine, pheniramine)

4. Ménière’s disease
• Symptoms: recurrent vertigo, tinnitus, hearing loss
• Treatment:
a. Non-pharmacological
- Salt restriction
- Avoid – alcohol, caffeine, CNS stimulants, cigarette
b. Pharmacological
- Acute attack - Prochloperazine, antihistamine (cyclizine, dimenhydrinate,
promethazine, pheniramine)
- Long term control – betahistine ± diuretics (N.B. DOES NOT IMPROVE
HEARING)
- Surgery

D. RHINITIS AND SINUSITIS

Rhinitis:
1. Definition: Inflammation of the lining of the nose

2. Symptoms
• Congestion
• Rhinorrhoea
• Sneezing
• Itching

3. Causes:
• Acute (infectious): viral (common cold)
• Allergic (hay fever):
- Seasonal
- Hypersensitive reaction - perennial symptoms

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AMH Summary: Chapter 9 – Ear, Nose and Throat 6

• Other:
- Irritant (heat, cold, smoke, dust)
- Hormonal (pregnancy)
- Drugs (ß-blocker, NSAIDs, ACE-I, oral contraceptives)
4. Treatment:
Acute Allergic Other
Steam inhalation Intranasal corticosteroid • Treatment variable∗
Sodium chloride 0.9 % Intranasal antihistamine + • Identify and avoid
drops/ sprays decongestant precipitating factors
Decongestant (Oral/ Intranasal mast cell stabiliser • Ensure symptoms not due
intranasal) Intranasal anticholinergic to excessive use of
Oral corticosteroids – intranasal decongestant -
disabling symptoms/ polyps rebound congestion

* Variable treatment: Use oral decongestant/ intranasal corticosteroid


or anticholinergic for unresponsive treatment.

Sinusitis
1. Definition: Inflammation of the sinuses

2. Symptoms
• Fever
• Weakness
• Fatigue
• Cough
• Congestion

3. Cause:
• Viral
• Allergic

4. Treatment:
• Acute
Symptom Treatment
Pain/ Fever Paracetamol
NSAIDs
Exudate Steam inhalation
Sodium chloride 0.9 % drops/ sprays
Decongestant (Oral/ intranasal)
Steam inhalation
Sodium chloride 0.9 % drops/ sprays

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AMH Summary: Chapter 9 – Ear, Nose and Throat 7

Antibacterial is indicated if:


• Poor response to decongestant/ intranasal corticosteroid
• Maxillary toothache
• Tenderness over sinuses
• Headache
• Mucopurulent discharge for > 1 week
• Prolonged fever

Uncomplicated cases – (amoxycillin, cefuroxime, cefaclor, doxycycline)


Unresponsive treatment – (amoxycillin + clavulanic acid -7-14 days)

• Chronic:
a. Analgesic
b. Corticosteroid (intranasal/ systemic)
c. Nasal lavage
d. Decongestant (Oral/ intranasal) – temporary relief
e. Antibacterial
f. Surgery

E. MOUTH AND THROAT CONDITIONS

Angular cheilitis
1. Cause:
• Oral candidiasis
• Ill-fitting dentures
• Dermatitis
• Vitamin B/ iron deficiency
• Crusting – infection (Staphylococcus aureus)

2. Symptoms: redness and maceration of skin at angle of the mouth with oral candidiasis
3. Treatment:
• Topical miconazole/ nyastatin

Dental abscess
1. Treatment:
• Abscesses drainage
• May required antibacterial

Dry mouth
1. Causes:
• Disease of salivary glands
• Radiation therapy
• Medication (drugs with anticholinergic activity)

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AMH Summary: Chapter 9 – Ear, Nose and Throat 8

2. Treatment:
a. Non-pharmacological
• Regular drinks (non-acidic, sugarless)
• Ice sucking
• Lozenges sucking
• Sugarless chewing gums
• Regular dental checks – monitor dental and gingival health

b. Pharmacological
• Artificial saliva preparation: Aquae, Biotène Oralbalance, Oralube

Gingivitis
1. Cause: plaque and calculus deposition on teeth
2. Treatment:
a. Non-pharmacological
• Removal by dentist
• Effective brushing
• Flossing

b. Pharmacological
• Non-alcoholic chlorhexidine mouthwash
• Antibacterial treatment (acute ulcerative gingivitis)
5. Amoxycillin with clavulanic acid/ clindamycin - 5 days

Herpes stomatitis
1. Treatment
a. Non-pharmacological
• Adequate fluid intake
• Soft diet
• Analgesic

b. Pharmacological
• Non-alcoholic chlorhexidine mouthwash – tooth brushing is too painful
• Antiviral- severe herpes stomatitis

Oral candidiasis
1. Prevalence:
• Elderly
• Treatment with broad spectrum antibacterials/ inhaled corticosteroids
• Immunosuppressant
• Diabetes

2. Treatment
• Immunocompetent: Topical miconazole, amphotericin, nyastatin – 1-2 weeks
• Severe unresponsive/ immunnocompromised: oral antifungal – fluconazole
• Denture associated candida stomatitis: Brush surface of dentures with oral
miconazole after cleaning teeth

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AMH Summary: Chapter 9 – Ear, Nose and Throat 9

Oral ulceration
1. Cause:
• Trauma
• Nutritional deficiency
• Immunosuppression
• Dermatological disease
• Medication
• Infection – herpes simplex, coxsackie viruses, candida, syphilis

2. Treatment
• Treat cause when possible; many cases are self-limiting (usually 10-14 days)
• Pharmacological
- Local corticosteroid: triamcinolone paste – reduce inflammation
- Local anaesthetics: lignocaine, benzocaine; benzydamine – reduce pain
Orabase paste, Bonjela, SM33, Ora-Sed gel – protect ulcerated area

Sore throat
1. Prevalence: Group A beta-haemolytic Streptococci- children
2. Cause:
• Virus
• Occassionally bacterial- Streptococcal i.e. Group A beta-haemolytic Streptococci

3. Treatment:
• Symptomatic relief – combine anaesthetic + antiseptic lozenge, gargle/ spray
• Antibacterial treatment: phenoxymethylpenicillin / roxithromycin – 10 days
- Reduce rheumatic fever risk in ATSI
- In non-indigenous with fever, tonsillar exudates, cervical lymphadenopathy,
absence of cough: Group A streptococcal pharyngitis

Tooth decay
1. Treatment:
• Regular brushing + flossing
• Avoid sugary foods, smoking (↓ saliva)
• Flouride mouthwash – encourage tooth enamel to repair itself

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AMH Summary: Chapter 9 – Ear, Nose and Throat 10

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2009

Copyright © The Medicine Box 2009

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2010


AMH Summary: Chapter 10 – Endocrine and Metabolic 1

AMH SUMMARY
CHAPTER 10: ENDOCRINOLOGY

DIABETES: TYPE 2 DIABETES

Pathophysiology
• Symptoms: polyuria, polydipsia
• Long term complications: retinopathy, nephropathy, neuropathy

Treatment
• Non-pharmacological: includes healthy diet (consisting of high fibre carbohydrates with
low GI), regular exercise (e.g. jogging, resistance training)
• Pharmacological: to be initiated if BGL > 15 mmol/L and symptoms persistent after 3
months of non-drug treatment
• Treatment targets
- Fasting blood glucose: < 6 mmol/L
- Random blood glucose: 4-8 mmol/L
- Glycated haemoglobin concentration (HbA1C): 7%

• Treatment regimen
1. First line treatment • Metformin: all patients
• Sulphonylurea: patients who are not overweight
2. Add another agent • Sulfonylurea + metformin
• Bedtime basal insulin + oral treatment
• (metformin, sulfonylurea or both)
3. Replace oral • Acute illness/trauma (infection, MI, stroke, coma)
antidiabetic drugs • Pregnancy
with insulin • Surgery

Practice points and counselling


• Monitor BGL and urine ketones
• Eat something when consuming alcohol because alcohol may mask hypoglycaemia
• Monitor renal function, eye function and wound healing on a regular basis

Cardiovascular risk reduction


• Non-pharmacological: reduce weight, cease smoking
• Pharmacological: low dose aspirin, ACEI/angiotensin II antagonist, hyperlipidaemic

INSULIN

Adverse effects: hypoglycaemia (sweating, hunger, faintness, palpitation, tremor, headache,


visual disturbance, altered mood), weight gain, local injection reactions

Dose: may reduce by 20% when switching from BD human isophane insulin to D insulin
glargine
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AMH Summary: Chapter 10 – Endocrine and Metabolic 2

Type 1 diabetes Type 2 diabetes


• Basal bolus regimen: short/ultra-short • Combined with oral antidiabetic:
acting insulin before each meal; long- long acting insulin usually given D
acting insulin D or BD (before bedtime • Monotherapy: split-mixed insulins are
and/or breakfast) commonly given D or BD before
• Continuous SC infusion: continuous breakfast or dinner.
infusion of short/ultra-short acting
insulin with bolus doses given before
meals
• Split-mixed regimens: 2/3 of total daily
dose given before breakfast; rest
before dinner.

Counselling
• Insulin is injected subcutaneously under the skin usually in the abdomen:
- Gently rotate vial/cartridge of cloudy insulin before use.
- When mixing insulin, draw up short-acting insulin into syringe to avoid
contaminating the vial with long acting insulin.
- Pinch skin to prevent injecting into blood vessel.
- Rotate injection sites to prevent lipodystrophy.
- Short-acting insulin is used 30 minutes before meals.
- Ultra-short acting insulin is used immediately before meals/soon after meals prn.

Important:
Do not mix insulin glargine with other insulin.
Sulfonylureas are often reduced or stopped once insulin therapy is established;
glitazone or metformin may be continued while insulin dose is titrated.

METFORMIN
(Diabex, Diaformin, Glucophage)

General
• No risk of hypoglycaemia, weight gain
• Also used with clomiphene for polycystic ovary syndrome

Adverse effects: vitamin B12 malabsorption, nausea, vomiting, anorexia, diarrhoea

Lactic Acidosis
• Symptoms include loss of appetite, weight loss, abdominal pain, cramps,
diarrhoea, nausea, vomiting, fatigue
• Increased risk of lactic acidosis exists in renal impairment, hepatic
impairment, and moderate-severe heart failure
• Monitor plasma creatinine before starting treatment and every 4-6 months
• Do not use metformin if CrCl < 30 mL/min; replace with insulin

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AMH Summary: Chapter 10 – Endocrine and Metabolic 3

• Temporarily cease metformin if illness affects renal function (dehydration,


shock, sepsis) or increases tissue hypoxia/acidosis risk (MI, pulmonary
embolism)

Dose
• Conventional vs controlled release
- Conventional: initially 500 mg 1-3 times daily, max 3 g daily
- Controlled release: initially 500 mg daily with evening meal; max 2 g daily.
- Transfer from conventional to CR: Start CR with equivalent daily dose. If >
2 g/day is required, use conventional tablets

• Renal impairment
- CrCl 60-90 mL/min: 2 g daily
- CrCl 30-60 mL/min: 1 g daily with food

• Combination with glibenclamide (Glucovance)


- Initially 1 tab Glucovance 500/2.5 d cc (breakfast); max 1 Glucovance 500/5 TDS
- Elderly: commence with Glucovance 250/1.25 with breakfast
- Do not use previous doses of metformin and glibenclamide to start fixed
dose combination therapy tablets are not bioequivalent.

• Surgery: Stop metformin 2 days, before, during and after surgery.

Counselling
• Metformin has a slow onset of effect and may take up to 2 weeks to establish control
• Inform doctor if symptoms of lactic acidosis (loss of appetite, weight loss, abdominal
pain, cramps, diarrhoea, nausea, vomiting, fatigue) present

SULPHONYLUREA
(glibenclamide, gliclazide, glimeperide, glipizide)

Adverse effects: weight gain, hypoglycaemia (esp in elderly, renal or hepatic impairment)

Precaution: may reduce dose in severe renal impairment due to hypoglycaemia risk

Comparative information:

Important:
Avoid glibenclamide (possibly glimeperide) in elderly, renal or hepatic impairment

Sulphonylurea Brand name Dose frequency Hypoglycaemia risk


Glibenclamide Daonil, Glimel D/ BD High
Gliclazide Diamicron D/ BD Intermediate
Glimepiride Amaryl, Dimirel D High/ intermediate
Glipizide Minidiab, Melizide D/ BD Low/ intermediate

Counselling: take with food to minimise risk of hypoglycaemia


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AMH Summary: Chapter 10 – Endocrine and Metabolic 4

REPAGLINIDE
(NovoNorm)

General:
• May be used as monotherapy; no improvement shown in patients inadequately
controlled with sulphonylurea
• Hypoglycaemia risk similar to sulphonylurea

Adverse effects: hypoglycaemia, N & V, GI upset

Dose: initially 0.5 mg TDS before meals; max 16 mg daily

Counselling: do not take dosage if skipped meals

THIAZOLIDINEDIONES/GLITAZONES

General: rosiglitazone and pioglitazone are reserved for those unable to tolerate
metformin/sulfonylurea. Use with caution.

Contraindications: ketoacidosis, type 1 diabetes, treatment with insulin (increased risk of


heart failure; combination with rosiglitazone is contraindicated)

Glitazones and CV disease


• Rosiglitazone is contraindicated in heart failure and acute coronary syndrome
(risk of heart failure development and cardiac ischaemic events)
• Rosiglitazone is not recommended in patients with peripheral arterial disease,
IHD and in those taking nitrates
• Glitazones should not be combined with insulin due to heart failure risk
• Combination of rosiglitazone with insulin is contraindicated: may increase the
risk of heart failure and myocardial ischaemia

Precautions: osteoporosis (or risk factors), diabetic macular oedema

Adverse effects: weight gain, peripheral oedema, heart failure, headache, dizziness,
arthralgia, decrease in haemoglobin and haematocrit, increases in HDL and LDL cholesterol
(rosiglitazone only)

Dose
• Pioglitazone (Actos)
- Initially 15-30 mg D; max 45 mg D
- Treatment with insulin: commence with 15 mg once daily + monitor carefully.
- Mild heart failure: start with a low dose; wait several months before increasing
dose.

• Rosiglitazone (Avandia)
- 4 mg once daily; may be increased to 8 mg daily
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AMH Summary: Chapter 10 – Endocrine and Metabolic 5

• Rosiglitazone with metformin (Avandamet)


- Give as 2 divided doses with food; max rosiglitazone 8 mg with metformin 2 g
- Conversion to combination product: patients stabilised on each drug separately
may commence with the current daily doses of rosiglitazone + metformin
- Adding rosiglitazone: initially 4 mg rosiglitazone daily + current metformin dose
- Adding metformin: initially 1 g metformin daily + current rosiglitazone dose

Counselling:
• Inform doctor of symptoms if you notice swollen feet or ankles, breathlessness, nausea,
vomiting, abdominal pain, fatigue, loss of appetite, dark urine

Practice points:
• Combination with metformin: useful in patient stabilised on same doses of each drug

ACARBOSE
(Glucobay)

Contraindications: partial intestinal obstruction, inflammatory bowel disease, major hernia, GI


disorders with malabsorption

Adverse effects: GI upset (can be reduced by gradual dose titration, unlikely to be alleviated
by antacids)

Dose: initially 50 mg daily, max 600 mg daily

Practice points: if hypoglycaemia occurs, give glucose, NOT SUCROSE (cane sugar) due to
delayed sucrose absorption

SITAGLIPTIN
(Januvia)

Mechanism of action: dipeptyl peptidase 4 inhibitor

Precautions: renal impairment (reduce dose if CrCL < 50mL/ min); treatment with sulfonylurea
increases hypoglycaemia risk

Adverse effects: hypoglycaemia (mainly when used with a sulfonylurea), headache, nausea,
infections (e.g. nasopharyngitis, URTI, UTI)

Dose:
• 100 mg daily
• Renal impairment
CrCl 30-50 mL/minute: 50 mg once daily
CrCl < 30 mL/minute: 25 mg once daily
Important: Sitagliptin appears to have no significant effect on weight.

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AMH Summary: Chapter 10 – Endocrine and Metabolic 6

HYPOGLYCAEMIA

Hypoglycaemia can occur in diabetic patient receiving insulin, sulfonylureas or repaglinide.


Mild hypoglycaemia will respond to oral administration of glucose or sucrose (glucose is preferred
to sucrose due to the delayed sucrose absorption).

TREATMENT

Adults
• Severe hypoglycaemia: unable to take solids or fluids: SC/IM glucagon / 20 mL of
glucose 50% injection (into a secure IV cannula in an antecubital vein because of risk of
superficial thrombophlebitis)

Children
• Give glucagon / IV glucose 10% injection (2–5 mL/kg over 3 minutes, followed by
0.1 mL/kg/minute until recovery)
• Continue monitoring blood glucose to prevent hyperosmolarity, with the risk of cerebral
oedema.

Note:
• Response should occur within 6 minutes for glucagon and within 4–5
minutes for glucose.
• When the person has responded, give longer acting carbohydrates (eg a
sandwich) to prevent recurrent hypoglycaemia.
• Prolonged treatment with glucose infusion may be required for
hypoglycaemia due to a long acting sulfonylurea.
• Octreotide (SC 50 micrograms) may be used in patients with persisting
hypoglycaemia despite glucose infusion.

GLUCAGON
(GlucaGen Hypokit)
Also used as adjunct treatment for -blocker or calcium channel blocker overdose.

Contraindications:
• Insulinoma, glucagonoma, phaeochromocytoma

Precautions:
• Chronic hypoglycaemia, adrenal insufficiency, starvation—glucagon is ineffective

Adverse effects:
• Nausea and vomiting, hypokalaemia (large doses)

Doses:
• Hypoglycaemia
• Adult, child > 5 years: SC, IM or IV, 1 mg.
• Child < 5 years: SC, IM or IV, 0.5 mg.

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AMH Summary: Chapter 10 – Endocrine and Metabolic 7

Diagnostic aid:
• IV/IM, 0.2–2 mg depending on radiological technique and route

Counselling:
• Ensure symptoms of low blood glucose (hypoglycaemia) + appropriate glucagon
injection administration are made aware to friends and families.

Practice points:
• Person should respond to glucagon within 10–15 minutes; if there is no response,
administer IV glucose
• Give complex carbohydrates orally when person has responded to prevent recurrent
hypoglycaemia

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AMH Summary: Chapter 10 – Endocrine and Metabolic 8

THYROID DISORDERS

HYPOTHYROIDISM

Pathophysiology

• Lab reading: Low T4 level


• Classified as primary or secondary hypothyroidism
• Primary hypothyroidism
- Causes: Hashimoto’s thyroiditis, radioactive iodine treatment, thyroid surgery
- Diagnosis: Elevated thyroid stimulating hormone (TSH) with low or low-to-normal T4
• Secondary hypothyroidism
- Causes: Pituitary or hypothalamic disease
- Diagnosis: Normal to low TSH with low T4

Treatment

• Thyroxine T4 (Oroxine, Eutroxsig) and liothyronine T3 (Tretroxin)

Indication:
- Thyroxine
Longer t1/2, longer duration of action
Used for 1° and 2° hypothyroidism, drug of choice for pregnant women

- Liothyronine
More rapid onset of action, shorter duration of action
More suitable for severe hypothyroidism in emergency (e.g. myxoedema coma), also
used for thyroid cancer

Precautions:
- Hypopituitarism, adrenal insufficiency, cardiovascular disorder, diabetes

Adverse effects:
- Hyperthyroidism, tachycardia, arrhythmia, excitability, insomnia, flushing, sweating,
diarrhoea, excessive weight loss, decreased bone density

Dose:
- Thyroxine: 100-200 mcg daily on an empty stomach usually before breakfast. May
disperse tablet in small amount of milk/water for infants.
- Liothyronine: 20-60 mcg daily in 2-3 divided dose

Practice and counselling

• Consider drug precipitants such as lithium and amiodarone.


• Use lower doses of drugs such as hypnotics, digoxin, anaesthetic agents and analgesics
until the person is euthyroid.

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AMH Summary: Chapter 10 – Endocrine and Metabolic 9

• Thyroxine
- Replacement is lifelong except following subacute or postpartum thyroiditis, radioactive
iodine treatment or partial thyroidectomy
- Monitor TSH and T4 levels every 6-8 weeks and adjust the thyroxine dose accordingly
(low-to-mid normal range for 1° hypothyroidism, mid-to-upper normal range for 2°
hypothyroidism). Check annually.
- Allow at least 6 weeks after changing thyroxine dosage before checking TSH as
thyroxine has a long half life

HYPERTHYROIDISM (also called thyrotoxicosis)

Pathophysiology

• Common causes include Graves' disease, toxic multinodular goitre, toxic adenoma,
sub-acute thyroiditis
• Specific precipitants include iodine-containing products such as amiodarone, IV contrast
media, kelp
• Lab reading: suppressed TSH with high free T4 and/or high free T3

Treatment regimens to maintain euthyroidism

• Adjusted regimen
- Initiate high-dose carbimazole or propylthiouracil for 3–4 weeks
- Adjust dose based on T4/T3 concentrations (not TSH)
- Review every 4–6 weeks, titrate to lowest effective maintenance dose
- Graves' disease: treat for 12–18 months

• Block-replace regimen
- Start long-term treatment with high-dose antithyroid medication
- Add thyroxine after normalisation of T4/T3 concentrations (about 6 weeks) to maintain
euthyroid state
- Confirm biochemical euthyroidism every 3 months
- No longer indicated in Graves' disease
- Contraindicated in pregnancy

• With radioactive iodine for radioactive treatment


- Stop antithyroid medications 4 days before treatment and restart 3 days afterwards
- Assess therapeutic effect by tapering off antithyroid medications 2-4 months after
radioactive iodine treatment

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AMH Summary: Chapter 10 – Endocrine and Metabolic 10

Drug choice

• Carbimazole (Neo-mercazole) and propylthiouracil (PTU)

Use:
- Grave’s disease, thyroid storm, preparation for thyroid surgery or radioactive iodine
treatment
- Ineffective in sub-acute thyroiditis (since recovery is spontaneous and definitive
treatment is usually not necessary)

Precautions in pregnancy:
- Propylthiuracil is the preferred medication in pregnancy according to the AMH (despite
its ADEC Category C status). Use the lowest effective dose.
- The block-replace regimen is contraindicated in pregnancy.

Adverse effects:
- Itching, mild leucopenia, nausea, vomiting, headache, GI upset, arthralgia

Agranulocytosis (rare but serious adverse effect)


Both drugs may cause agranulocytosis. See doctor immediately if fever, mouth
ulcer, sore throat or rash develop, especially within 3 months of treatment.

Dose:
- Carbimazole (Neo-mercazole)
Initially: 20–40 mg daily in divided doses for 3–4 weeks; max 60 mg daily
Adjusted regime, DM: 5–15 mg daily in single or divided doses according to response
Block-replace regimen, continue initial dose + add 100–150 mcg thyroxine when T4 in
normal range
Thyroid storm: 60–80 mg daily in divided doses, gradually reduced

- Propylthiouracil (PTU)
Initially: 200–400 mg daily in 2–4 divided doses for 3–4 weeks.
Adjusted regimen, DM: 25–300 mg daily according to response
Block-replace regimen, continue initial dosage + add 100–150 mcg thyroxine when T4 in
normal range
Thyroid storm: Adult, 600–800 mg daily, in divided doses, gradually reduced

- Switching between drugs


The 2 drugs can be interchanged without recurrence of adverse effects.
50 mg propylthiouracil 5 mg carbimazole

• Iodine (Aqueous Iodine Solution)


Iodine works by transiently inhibiting thyroid hormone release and reducing thyroid
vascularity in Graves’ disease. This product is indicated for short term use before surgery
for Graves’ disease. It is contraindicated in pregnancy and breastfeeding.

Copyright © The Medicine Box 2011


AMH Summary: Chapter 10 – Endocrine and Metabolic 11

OESTEOPOROSIS

PATHOPHYSIOLOGY

Diagnosis
• Consider treatment in people with presence or history of osteoporotic fracture or when bone
density is > 2.5 SD below young mean value, especially if they have other risk factors for
fracture.

Risk factors
• Diseases that may contribute to bone fragility include metastatic cancer, multiple myeloma,
osteomalacia, hypogonadism, hyperthyroidism, hyperparathyroidism, liver disease,
malabsorption syndromes and Cushing's disease.

Lifestyle Medications Innate


Calcium intake Thyroxine Age
Physical activity Corticosteroids Gender
Smoking Antiepileptic drugs Menstrual history (early menarche)
Alcohol intake Heparin Weight
Family history of low trauma-fracture
History of low trauma-fracture

Corticosteroid-induced osteoporosis
• To minimise risks:
- Use lowest effective dose of corticosteroids
- Use topical or inhaled preparations
- Maintain adequate calcium intake with calcium and vitamin D
- Measure BMD regularly in people on long-term corticosteroid treatment
- Monitor for hypogonadism in men
• For prevention and treatment, consider alendronate, etidronate, risedronate and zoledronic
acid, teriparatide, calcitriol

Osteoporosis in men
• Most likely due to 2° causes of osteoporosis such as hypogonadism and excessive alcohol
• Management:
- Non-pharmacological management (fall prevention)
- Calcium and Vitamin D supplementation
• Consider alendronate and risedronate as 1st line treatment. May use zoledronic acid or
teriparatide. No evidence of benefit for calcitriol in men

Non-pharmacological management (fall prevention)


• Regular weight-bearing physical activity
• Balance training
• Walking (may lower hip fracture risk in postmenopausal women)
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AMH Summary: Chapter 10 – Endocrine and Metabolic 12

• Reduce use of sedatives


• Improve poor vision
• Home and environment modification

TREATMENT OPTIONS

1st line treatment • Bisphosphonate (established postmenopausal osteoporosis)


2nd line treatment • Raloxifene
Other drugs • Strontium
• Teriperatide
Supplements • Calcium and vitamin D

Bisphosphonates

Bisphosphonate Indication
Alendronate • Paget’s disease of bone
• Prevention and treatment of osteoporosis
Clodronate • Hypercalcaemia of malignancy
• Osteolytic bone metastases from breast cacner or multiple
myeloma
Etidronate • Paget’s disease of bone
• Treatment of postmenopausal osteoporosis
• Prevention of corticosteroid-induced osteoporosis
• Prevention and treatment of heterotopic ossification due
Ibandronic Acid • Treatment of postmenopausal osteoporosis
Pamidronate • Paget’s disease of bone
• Hypercalcaemia of malignancy
• Osteolytic bone metastases from breast cancer or advanced
multiple myeloma
Risedronate • Paget’s disease of bone
• Treatment of postmenopausal osteoporosis
• Treatment and prevention of corticosteroid induced
osteoporosis
Tiludronate • Paget’s disease of bone
Zoledronic Acid • Hypercalcaemia of malignancy
• Prevention of skeletal related events (e.g. pathological fracture,
spinal cord compression) with advanced bone malignancies

Precautions:
• Hypocalcaemia – contraindicated
• Osteonecrosis of the jaw
• Renal impairment

Adverse effects:
• Oesophageal adverse effects, osteonecrosis of the jaw (consider dental assessment
before using a bisphosphonate), bone pain, hypocalcaemia
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AMH Summary: Chapter 10 – Endocrine and Metabolic 13

Dose:
• Most oral formulations are taken once a week, swallow whole with a full glass of plain
water in the morning before breakfast and remain upright for at least 30 mins.

Counselling:
• Ensure adequate intake of calcium and vitamin D. They need to be taken at a different
time of day.
• Consider full dental assessment and complete any dental procedures before starting
treatment to minimise risk of osteonecrosis of the jaw
• Concomitant use of NSAIDs should be avoided as the combination may increase risk of
oesophageal adverse effects
• Do not take antacids, calcium, iron or mineral supplements within 30 minutes of
alendronate as they may interfere with its absorption.
• See doctor immediately if patient experiences pain on swallowing, or new/worsening
heartburn

Calcium
Precautions:
• Hypercalcaemia, hypercalciuria – contraindicated
• Treatment with digoxin – contraindicated in digoxin toxicity (risk of arrhythmia)
• Treatment with calcitriol – risk of hypercalcaemia (avoid combination)

Adverse effects:
• Belching, flatulence, abdominal distension, constipation

Dose:
• Adults: 800mg
• Pregnancy and breastfeeding: 1100-1200mg
• Postmenopausal women: 1200-1500mg

Important:
Calcium carbonate requires acidity for optimal dissociation and should be taken
with food; clinical effect may be reduced in achlorhydria or by drugs which
increase gastric pH, e.g. PPIs, H2 antagonists

Products

Active Proprietary Names


ingredients
Ca carbonate Titralac Cal-Sup CAL-600 Caltrate
(Chewable) (Chewable)
Ca citrate Citracal
Ca carbonate, Ca Sandocal (Dispersible)
lactate gluconate
Combination Caltrate with Ostelin vitamin Citracal + D Bio Calcium
products Vitamin D D and Calcium
(Ca + Vit D3) MaxCal-D

Copyright © The Medicine Box 2011


AMH Summary: Chapter 10 – Endocrine and Metabolic 14

Vitamin D
Include:
• Colecalciferol (Vitamin D3 – OsteVit-D, Blackmores Vitamin D3, Ostelin Vitamin D)
• Ergocalciferol (Vitamin D2 – Available only in OTC Vitamin and mineral preparations)

Precautions:
• Avoid in severe renal impairment due to inability to convert colecalciferol/ergocalciferol
into active form
• Hypercalcaemia - contraindicated

Adverse effects:
• Nausea, vomiting, anorexia, apathy, constipation, headache, thirst, sweating, polyuria
(i.e. symptoms of hypercalcaemia)

Dose:
• Treatment of moderate-to-severe vitamin D deficiency:
75–125 micrograms (3000–5000 IU) daily for 6–12 weeks then 25 micrograms (1000
IU) daily
• Prevention of vitamin D deficiency:
Recommended adequate intake, assuming no, or minimal, sunlight exposure:
< 50 years: 5 mcg (200 international units) daily
51–70 years: 10 mcg (400 international units) daily
> 70 years: 15 mcg (600 international units) daily
Doses up to 25 mcg daily may be appropriate in institutionalised/ bedbound patients

Practice points:
• Slow onset of action (4-8 weeks) and prolonged duration of action (8-16 weeks)
• Ergocalciferol is only available in OTC vitamin and mineral preparations
• No risk of hypercalcaemia at physiological doses (e.g. < 2000 units daily)
• Halibut/cod liver oil capsules contain colecalciferol and vitamin A which can be toxic at
high doses
• 1 mcg 40 IU

Cinacalcet (Sensipar)
Indications:
• Hypercalcaemia in parathyroid carcinoma
• Primary hyperparathyroidism when parathyroidectomy is not an option
• Secondary hyperparathyroidism in patients with end stage renal disease receiving
dialysis (adjunctive treatment)

See AMH for more information

Copyright © The Medicine Box 2011


AMH Summary: Chapter 10 – Endocrine and Metabolic 15

Denosumab (Prolia)
Drug class:
• RANK ligand monoclonal antibody

Indication:
• Postmenopausal osteoporosis

Contraindications, precautions:
• Predisposition to low Ca levels (e.g. hypoparathyroidism, thyroid, parathyroid surgery,
renal impairment)
• Risk factors for osteonecrosis of the jaw (e.g. chemotherapy, dental disease, poor oral
hygiene, cancer with bone lesions)
• Immunosuppression

Adverse effects:
• Hypercholesterolaemia, hypocalcaemia, skin infection, pancreatitis

Dose:
• SC injection once every 6 months

Monitoring and counselling:


• Monitor Ca levels (due to risk of hypocalcaemia)
• Ensure adequate calcium and vitamin D intake

Raloxifene (Evista)
Indication:
• Prevention and treatment of postmenopausal osteoporosis

Contraindication:
• History of VTE

Precautions:
• Prolonged immobilisation
• Unexplained uterine bleeding (risk of endometrium proliferation)
• History of hypertriglyceridaemia induced by oestrogens

Adverse effects:
• Common: hot flushes, sweating, leg cramps, peripheral oedema, sleep disorders
• Infrequent: DVT, pulmonary embolism, retinal vein thrombosis

Dose:
• 60mg once daily

Practice point:
• Ensure adequate intake of calcium and vitamin D; prescribe supplements if necessary

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AMH Summary: Chapter 10 – Endocrine and Metabolic 16

Salcatonin (Miacalcic)
Indications:
• Paget’s disease of bone
• Hypercalcaemia

Adverse effects:
• Common: Flushing, nausea, vomiting, dizziness
• Rare: Tingling of hands, increased urinary frequency, allergic reactions including rash
and anaphylaxis

Dose:
• Paget’s disease: SC/MI 50-100 units daily for 3-6 months
• Hypercalcaemia: 5-10 units/kg daily by slow IV infusion over at least 6 hours, or by slow
IV injection in 2-4 divided doses

See AMH for further information

Strontium (Protos)
Indication:
• Treatment of postmenopausal osteoporosis

Precautions:
• Increases risk of VTE
• Not recommended if creatinine clearance < 30 mL/minute (lack of data)

Adverse effects:
• Common: Nausea, diarrhoea, headache, dermatitis, increased creatine kinase
concentration
• Rare: DVT, Pulmonary embolism, CNS effects (disturbed consciousness, memory loss,
seizures)
Dose:
• 2 g once daily at bedtime at least 2 hours after meal

Practice point:
• Medication taken at bedtime, at least 2 hours after eating, because food and drink can
reduce its absorption. Mix the granules in water and drink immediately

Teriparatide (Forteo)
Indications:
• Postmenopausal osteoporosis when other agents are unsuitable and there is a high risk
of fractures
• Primary osteoporosis in men when other agents are unsuitable and there is a high risk
of fractures

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AMH Summary: Chapter 10 – Endocrine and Metabolic 17

Contraindications:
• Paget’s disease of bone
• Hyperparathyroidism

Practice point:
• Max duration of 18 months treatment due to potential risk of osteosarcoma
• Ensure adequate intake of calcium and vitamin D

See AMH for further information

Copyright © The Medicine Box 2011


AMH Summary: Chapter 10 – Endocrine and Metabolic 18

References

1. E-MIMS. 5.0. Sydney: MediMedia Australia Pty Ltd; 2006


2. AMH. Adelaide: Australian Medicines Handbook Pty Ltd; 2006
3. eTG Complete. North Melbourne: Therapeutic Guidelines Ltd; 2008
4. Australian Pharmaceutical Formulary and Handbook (APF) ACT: PSA; 2006

Copyright © The Medicine Box 2011

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

Disclaimer: While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not
accept any responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this
publication. It is also noteworthy that The Medicine Box is unaffiliated with the Pharmacy Board of Australia, the former Pharmacy Board
of NSW, the Australian Pharmacy Council or the Pharmaceutical Society of Australia. All information in this publication is provided by
past pharmacy graduates and has not been verified by the above organisations.

Copyright © The Medicine Box 2011


AMH Summary: Chapter 11 – Eye Drugs 1

AMH SUMMARY: Chapter 11 – EYE DRUGS

- Eye Infections -
 Bacterial conjunctivitis (rapid onset, mucus discharge): use antibacterials. Usually self-limited
and lasts for 2-3 days.
 Viral infections (watery discharge, recent URTI): infectious; use artificial tears and cool
compresses
 Allergic conjunctivitis (water discharge, itching)
 Seborrhoeic blepharitis (greasy scales on lid margin): apply warm compresses. scrub lids with
a damp cotton bud soaked in mild soap (eg. 1:10 diluted baby shampoo or Lidcare) or dilute
sodium bicarbonate (1 teaspoon per 250ml hot tap water) twice daily.
 Staphylococcal blepharitis (crusts and ulceration of eyelash base): scrub lids as above,
followed by an antibacterial eye ointment, massaged with a clean finger into base of eyelashes
bd for 10-14 days.
 Stye (infection of eyelash follicle – swelling and pain): hot water compresses 3-4 times daily.
 Herpetic eye infection/keratitis (ulceration of cornea – foreign body sensation, photophobia,
tearing): antiviral
 Cellulitis (acute bacterial inflammation/infection): systemic antibacterials

AMINOGLYCOSIDES
 FRAMYCETIN (eye) – Soframycin
Dosage: 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop 4 times daily for
5 days.

 GENTAMICIN (eye) – Genoptic; Minims


- gentamicin should be reserved for use by ophthalmologists and for serious infections not
responding to treatment with other topical antibacterials (after taking sample for microbiological
culture)
- can be used as prophylaxis after surgery.

Dosage: 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop 4 times daily for
5 days.
For prophylaxis: 1 drop 4 times daily until epithelium healed (rarely >4 days).

 TOBRAMYCIN (eye)- Tobrex


- tobramycin should be reserved for use by ophthalmologists and for serious infections not
responding to treatment with other topical antibacterials (after taking sample for microbiological
culture)
- can be use as prophylaxis after surgery

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AMH Summary: Chapter 11 – Eye Drugs 2

Dosage: 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop 4 times daily for
5 days. Ointment may be used as an adjunct to drops at night, or as a single agent 3 times daily,
eg in children.
Prophylaxis: 1 drop 4 times daily until epithelium healed (rarely >4 days).

QUINOLONES
Side Effects: mild transient ocular irritation, lid margin crusting and scaling, unpleasant taste

- Ofloxacin and ciprofloxacin have similar efficacy to tobramycin


- Quinolones should be reserved for specialist treatment of bacterial keratitis and other
antibacterials are preferred for conjunctivitis, to slow emerging resistance.
- Marketed for severe conjunctivitis or keratitis.

 CIPROFLOXACIN (eye) – Ciloxan


Dosage: Conjunctivitis - 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop
4 times daily for 5 days. Keratitis - 1 drop every 5 minutes for the first hour, then once every hour
until there is improvement; decrease frequency according to clinical response (only under
supervision of ophthalmologist).

 OFLOXACIN (eye) – Ocuflox


Dosage: as above.

OTHER ANTIBACTERIALS
 CHLORAMPHENICOL (eye) – Chlorsig, Chloromycetin
Dosage:
Blepharitis - Massage ointment into lid margin 2–3 times daily.
Conjunctivitis - 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop 4 times
daily for 5 days. Ointment may be used at night as an adjunct to drops, or as a single agent
3 times daily, e.g. in children.

 PROPAMIDINE – Brolene
Side Effects: stinging and burning after instillation
Dosage: Keratitis - 1 drop every hour until there is improvement, then gradually reduce frequency
according to clinical response (treatment duration is usually months). It can also be used for acute
conjunctivitis.

 SULFACETAMIDE – Bleph-10
- use is not recommended as it is an irritant.

Dosage:
Blepharitis - Massage 2 drops into lid margin 2–3 times daily.

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AMH Summary: Chapter 11 – Eye Drugs 3

Conjunctivitis - 1 drop every 2–4 hours for 2 days; then if there is improvement, 1 drop 4 times
daily for 5 days.

ANTIVIRALS
 ACICLOVIR (eye) – Zovirax
Indications: Herpes Simplex Keratitis
Side Effects: transient mild stinging after instillation
Dosage: Apply about 1 cm of ointment into the lower conjunctival sac 5 times daily for 14 days, or
for 3 days after corneal epithelium healed, whichever is shorter.

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AMH Summary: Chapter 11 – Eye Drugs 4

- Glaucoma-
- Prostaglandin analogues (bimatoprost, latanoprost, travoprost) are first line agents over beta
blockers.
- Brimonidine or carbonic anhydrase inhibitors (brinzolamide, dorzolamide) are third line.
- Pilocarpine tend to be useful as an adjunct.
- Separate eye drops by at least 5 minutes.

BETA-BLOCKERS
- timolol is nonselective; betaxolol are selective beta1 blockers.

Contraindications: Asthma (cardioselective agents i.e. betaxolol may be used); Bradyarrhythmia.


Avoid combination with verapamil as bradycardia may occur.

Side Effects (systemic): stinging on instillation (especially betaxolol solution), bradycardia

 BETAXOLOL – Betoptic
Dosage: 1 bd

 TIMOLOL – Tenopt, Timoptol; Timoptol-XE; (+brimonidine = Combigan); (+dorzolamide =


Cosopt); (+latanoprost = Xalacom); (+travoprost = DuoTrav)
Dosage: 1 daily (Timoptol-XE, Xalacom, DuoTrav) or 1 bd (Timoptol, Combigan, Cosopt)

PROSTAGLANDIN ANALOGUES
Side Effects: gradual (over months to years), usually irreversible increase in iris pigmentation in
treated eyes, especially those of mixed colour, eg blue/brown; darkening, lengthening and thickening
of the eyelashes, conjunctival hyperaemia (usually transient)

Dosage: 1 drop at night

 BIMATOPROST – Lumigan
Side Effects: ocular itch, superficial punctate keratitis, blepharitis, conjunctival oedema, dry eyes,
headache

 LATANOPROST – Xalatan
Side Effects: ocular irritation (preservative benzalkonium chloride), blepharitis, punctate corneal
epithelial erosions, bitter taste, rash

 TRAVOPROST – Travatan
Side Effects: itch, keratitis, headache

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 5

ALPHA2 AGONISTS

 APRACLONIDINE – Iopidine
- The effect of apraclonidine usually declines after a month; it is indicated for short term use (up
to 3 months).

Side Effects: ocular irritation, especially allergic blepharoconjunctivitis (with >3 months use), dry
mouth and nose, altered taste perception

Dosage: 1 drop 2–3 times daily.

 BRIMONIDINE – Alphagan
Side Effects: ocular irritation, ocular allergic reaction, conjunctival blanching, lid retraction,
blepharitis, dry mouth and nose, taste disturbance, fatigue, headache, drowsiness, dizziness

Dosage: 1 drop 2–3 times daily.

CARBONIC ANHYDRASE INHIBITORS


Side Effects: ocular irritation, foreign body sensation, bitter taste

 BRINZOLAMIDE – Azopt
Side Effects: blurred vision
Dosage: 1 bd

 DORZOLAMIDE – Trusopt
Side Effects: conjunctivitis and lid reactions
Dosage: 1 drop 3 times daily.

OTHER DRUGS FOR GLAUCOMA


 ACETAZOLAMIDE – Diamox
- systemic carbonic anhydrase inhibitor (reduces aqueous humour secretion); also acts as a
diuretic by alkalinizing the urine.

Indications: glaucoma, epilepsy (absence seizures)

Precautions: gout, sulfur allergy.

Side Effects: paraesthesia (of hands, face, feet or mucocutaneous junctions), fatigue, drowsiness,
depression, decreased libido, bitter or metallic taste, nausea, vomiting, abdominal cramps,
diarrhoea, black faeces, polyuria, renal stones, metabolic acidosis, electrolyte changes
(hypokalaemia, hyponatraemia)

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 6

Dosage: 125 mg twice daily, increase to a maximum of 250 mg 4 times daily. Take with food.
 MANNITOL – Osmitrol inj
Indications: acute closed angle glaucoma

Side Effects: nausea, vomiting, local pain, skin necrosis and thrombophlebitis (injection site), chills,
dizziness, urticaria, hypotension, tachycardia, fever, angina-like chest pains. Fluid and/or
electrolyte shift can produce pulmonary congestion, acidosis, electrolyte loss, dry mouth, thirst,
oedema, headache, blurred vision, seizures and heart failure.

Dosage: IV 1–2 g/kg (5–10 mL/kg of 20% solution) over 30 minutes.

 PILOCARPINE – Pilopt, PV Carpine


Indications: acute and chronic glaucoma

Side Effects: fluctuating blurred vision, accommodative spasm and frontal headache in people
<40 years (usually decreasing after 2–4 weeks; simple analgesics may reduce pain), miosis,
ocular irritation, follicular conjunctivitis.

Dosage: Chronic open angle glaucoma – 1 drops of 2% qid.

- if using more than one eyedrop, instill pilocarpine last.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 7

- Allergic and Inflammatory Eye Conditions -


Allergic conjunctivitis: itchy, red, watery eyes with oedema.
Treatment:
- Mild symptoms: irrigate with saline bd & use artificial tears 4-8 times daily and cold water
compresses.
- Moderate symptoms: use topical drugs (ketorolac, levocabastine, ketotifen, olopatadine). Long
term use of topical vasoconstrictor-antihistamine combinations are not recommended due to
rebound conjunctivitis.
-Severe symptoms: seek specialist advice; topical corticosteroids may be required.
-Recurrent disease: use cromoglycate as a preventative.

VASOCONSTRICTORS
Indications: mild ocular congestion

Side Effects: rebound hyperaemia, stinging on instillation


Note: Do not use regularly for more than 5 days. Although advertised as being useful for relieving eye
redness due to minor irritations such as dust, smoke and contact lens wear, a cool compress is as
beneficial and is safer. Using drops like this for too long can cause symptoms similar to red eyes.
 NAPHAZOLINE – Murine Clear Eyes, Albalon, Naphcon Forte; (+antazoline = Antistine-
Privine); (+phenramine = Naphcon-A or Visine Allergy)

Dosage: 1 drop every 6–12 hours as required.

 PHENYLEPHRINE (eye) – Albalon Relief; Prefrin


Dosage: 1 drop every 3–4 hours as required.

 TETRAHYDROZOLINE – Murine Sore Eyes; Visine Advanced Relief


Dosage: 1 drop every 6–12 hours as required.

ANTIHISTAMINES
 AZELASTINE (eye) – EyeZep
Dosage: 1 bd then increase to 1 qid

 LEVOCABASTINE (eye) – Livostin


Side Effects: Drowsiness
Dosage: 1 drop twice daily, increasing to 3–4 times daily if necessary.

 KETOTIFEN – Zaditen
Dosage: 1 bd

 OLOPATADINE – Patanol
Side Effects: hyperaemia, keratitis, dry eye
Dosage: 1 bd

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 8

NSAIDS
 DICLOFENAC (eye) – Voltaren Optha
Indications: inhibition of miosis during cataract surgery & prevention of inflammation after.
Side Effects: delayed epithelial growth and wound healing, persistent epithelial defects following
keratoplasty.
Dosage: 1 drop 3-5 times daily.

 FLURBIPROFEN – Ocufen
Indication: inhibition of miosis during cataract surgery
Dosage: as above.

 KETOROLAC (eye) – Acular


Indication: short term (2-4 weeks) treatment of seasonal allergic conjunctivitis; prevention and
reduction of inflammation after cataract surgery.
Side Effects: local allergic reactions, superficial keratitis
Dosage: 1 drop qid. May start 24 hours before cataract surgery.

CORTICOSTEROIDS
Side Effects: ocular hypertension (usually reversible) proportional to dose, potency, penetration and
duration of treatment; retarded corneal healing, rebound inflammation

 DEXAMETHASONE (eye) – Maxidex


Dosage: 1 drop 2-4 times daily

 FLUOROMETHOLONE – Flucon, FML; Flarex


Dosage: as above

 HYDROCORTISONE (eye) – Hycor ointment


Dosage: Apply 2–4 times daily.

 PREDNISOLONE (eye) - Minims; (+phenylephrine = Prednefrin Forte)


Dosage: 1 drop 2-4 times daily

OTHER DRUGS FOR ALLERGIC EYE CONDITONS


 CROMOGLYCATE (eye) – Opticrom
- delayed onset of action; may take 3-6 weeks to see effect.

Indications: seasonal allergic conjunctivitis


Side Effects: transient stinging on instillation
Dosage: 1 drop 4–6 times daily.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 9

- Dry Eyes -
Use Artificial Tears to provide symptomatic relief.

Eye drops
Preservative: Refresh Tears, Visine, Genteal, Tears Naturale, Systane, Liquifilm, Viscotears
Use these if eye drops are used infrequently. Polytears and Genteal contain a less irritant preservative
so use it in more frequent users.

Preservative-free: Theratears, Cellufresh, Celluvisc, Lacri-lube


Non-irritant but more expensive and packaged in single dose containers. Most useful if patients use
drops 4-6 times per day, wears contacts or has an allergy to a preservative. Single use vials can be
used more than once if refrigerated up to 24hours.

Eye Ointments: use before bedtime if symptoms interrupt sleep or occur on awakening.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 10

- Eye Examinations& Procedures -


ANTICHOLINERGICS
Indications: Mydriasis (pupil dilation) for the examination of peripheral lens and retina; Cycloplegia
(paralysis of accommodation).

Side Effects: intolerance to bright light (glare), stinging on instillation (especially 1% cyclopentolate),
blurred vision (especially near vision), transient intraocular pressure elevation (especially in pre-
existing ocular hypertension)

 ATROPINE (eye) – Atropt


Dosage: Diagnostic Use – 1 drop every 5 minutes prn; Uveitis – 1 drop tds to qid.

 CYCLOPENTOLATE – Cyclogyl
Dosage: 1 drop repeated after 5 minutes if necessary. Examine after 20 minutes.

 HOMATROPINE – Isopto Homatropine


Dosage: Diagnostic – 1 drop every 5 minutes; Uveitis (inflammation of inner eye) – 1 drop q4h

 TROPICAMIDE – Mydriacyl
Dosage: 1 drop every 5 minutes prn. Examine after 20 minutes.

OTHER DRUGS FOR MYDRIASIS


 PHENYLEPHRINE (eye)
Indications: pupil dilator with duration of action of 5-7 hours. Maximal mydriasis occurs after 60-90
minutes.
Diagnostic mydriasis, relief of ocular congestion.

Precautions: recent MI, angina, insulin-dependent diabetes – BP elevation

Side Effects: rebound miosis, hyperaemia, stinging on instillation

Dosage: generally as an adjunct


Mydriasis – 1 drop once; Uveitis – 10% 1 drop tds.

LOCAL ANAESTHETICS
 AMETHOCAINE (eye)
 OXYBUPROCAINE
 PROXYMETACAINE

Copyright © The Medicine Box 2012


AMH Summary: Chapter 11 – Eye Drugs 11

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 12 – Gastrointestinal 1

AMH SUMMARY: CHAPTER 12 – GASTROINTESTINAL


DRUGS FOR DYSPEPSIA, REFLUX AND PEPTIC ULCERS
H. Pylori-related ulcers
Dyspepsia • The preferred regimen is PPI standard dose twice daily, clarithromycin
• Dyspepsia: PPIs are more effective than antacids or H2 antagonists 500mg twice daily, amoxycillin 1g twice daily for 7 days
• Functional dyspepsia: PPIs and H2 antagonists are equally effective • If amoxycillin unsuitable, use metronidazole instead (PPI standard
but H2 antagonists are less expensive dose twice daily, clarithromycin 500mg twice daily, metronidazole
• Antacids prn 400mg twice daily for 7 days)
• H.pylori eradication • If clarithromycin unsuitable, replace with amoxycillin (PPI standard
dose twice daily, amoxycillin 500mg three times daily, metronidazole
400mg twice daily for 14 days)
GORD
NSAID-related ulcer
Treatment options • Replace NSAID with paracetamol and non-drug treatment.
• Mild, intermittent symptoms • Treatment: PPI, H2 antagonist, or misoprostol
• Lifestyle measures, antacids and short intermittent courses of H2 • Prevention: PPI, double dose H2 antagonist, misoprostol
antagonists
• More severe symptoms
− Full dose PPI (or H.pylori test for uninvestigated reflux
symptoms)
− Double dose PPI
− Standard dose H2 antagonist
− Metoclopramide or domperidone

Practice points
• Intermittent PPI use is more cost-effective than continuous H2
antagonist use
• Combination treatment is less effective than increasing the dose of PPI
• Doubling dose of H2 antagonist does not increase efficacy and is not
recommended
• NSAIDs, CCBs, nitrates, theophylline can worsen reflux. Avoid use if
reflux occurs.

Infant GORD
• If severe, thickened oral fluids may reduce symptoms
• Drug treatment should be avoid if possible. However, if GORD
persists, H2 antagonists and PPIs may be used.

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 2

Class Generic name Brand name Dose Side effects and precautions Other comments
3+ 2+
Aluminium hydroxide Alu-tab As directed • Constipation (for Al and Ca ) • Liquid preparations are more effective than solid
2+
• Diarrhoea (for Mg ) preparations.
Antacids

Calcium carbonate Titralac As directed • Use with caution in severe renal • Tablets should be chewed or sucked before
impairment: antacids containing swallowing to maximise effect
Combination antacids Mylanta As directed Al3+ and Na+ should be avoided

Bismuth subcitrate (SAS) 120mg qid for • Blackening of faeces • Take on an empty stomach (bismuth is less effective
10-14 days • Darkening of teeth and tongue if taken with food or milk)
Cytoprotective

• Chew tablets before swallowing


• Bismuth toxicity can occur if it is taken for >2 months
agents

Sucralfate Carafate 1g bd • Constipation • Tablets can be dispersed in water


(maintenance) • Contraindicated in severe renal
impairment

Cimetidine Magicul 400mg bd • Cimetidine has also been • Avoid cimetidine if possible
associated with anti-androgenic • Cimetidine interacts with carbamazepine, phenytoin,
Famotidine Pepcidine 20mg bd effects such as gynaecomastia, TCAs, SSRIs, theophylline, warfarin
H2 antagonists

impotence
Nizatidine Tazac 150-300mg bd

Ranitidine Zantac 300mg d

All listed doses


are for GORD.

Esomeprazole Nexium 20mg d • Headache • Swallow whole; do not crush or chew.


• Abdominal pain • Esomeprazole, lansoprazole, omeprazole: tablets
Lansoprazole Zoton 30mg d may be dispersed in water and taken within 30
minutes. Capsules may be opened and the contents
PPIs

Omeprazole Losec 20mg d dispersed water or juice and taken immediately.

Pantoprazole Somac 40mg d

Rabeprazole Pariet 20mg d

Misoprostol Cytotec 400mg bd • Diarrhoea • Take with meals to reduce the risk of diarrhoea
Other

• Abdominal pain • Seek medical attention if you notice black stools or


coffee-coloured vomit

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 3

DRUGS AFFECTING GASTROINTESTINAL MOTILITY

Generic name Brand name Indication Dose Side effects Other comments
Cisapride (SAS) Gastroparesis 15-40mg d in 2-4 doses • Diarrhoea •L18 *
15 minutes before meals • Abdominal cramps •Seek medical attention if you feel
• QT prolongation dizzy, vomit or have diarrhoea

Hyoscine butylbromide Buscopan IBS 10-20mg 3-4 daily


(smooth muscle relaxant) GI, renal, biliary spasm

Mebeverine Colofac IBS 135mg daily cc • Dyspepsia


(smooth muscle relaxant)

Peppermint oil Mintec IBS 1 tds • Heartburn • Take half an hour before meals
(smooth muscle relaxant) • Do not break or chew capsules as
peppermint oil can irritate the oral
cavity and throat

* L18 stands for ancillary label 18

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 4

DRUGS FOR NAUSEA AND VOMITING

Drug choice: Dopamine antagonists, sedating antihistamines, anticholinergics, 5HT3 antagonists, substance P antagonists, dexmethasone, lorazepam
Pregnancy: Ginger (up to 1g daily), pyroxidine (up to 50mg bd), metoclopramide, prochlorperazine

Class Generic name Brand name Indication Dose Other comments


Domperidone Motilium Nausea and vomiting 10-20mg 3-4 times d • Domperidone does not readily cross the BBB therefore CNS
Gastroparesis effects are less likely to occur. All other dopamine antagonists
Stimulation of lactation have central dopamine antagonist activity and may cause
extrapyramidal side effects. Domperidone is the antiemetic of
Dopamine antagonists

choice in patients taking treatment for Parkinson’s disease.

Droperidol Droleptan Prevention of post-op Injection as directed • L1 *


N&V • The risk of sedation and EPSE limit its use

Haloperidol Serenace N & V associated with 1-2mg tds prn • L1, L16 *
chemotherapy • Haloperidol is used to treat N&V following chemotherapy
when other agents are ineffective due to risk of CNS effects

Metoclopramide Maxolon N&V 5-10mg 2-3 times d • L12 *


Gastric stasis • Metoclopramide is safe in pregnancy (category A)
Aid in GI radiology

Prochlorperazine Stemetil N&V 10mg tds • L1 *


Vertigo • This medicine may increase the effect of alcohol.

Dimenhydrinate Dramamine N & V due to motion 50-100mg 4-6 times d • L1 *


st
sickness, labyrinthitis, • For motion sickness, take 1 dose 30 mins before travel.
Meniere’s disease
Antihistamines

Pheniramine Avil Allergic conditions 22.65mg 2-3 times daily


Pruritis
Motion sickness
N&V
Vertigo due to Meniere’s

Promethazine Phenergan N&V 25mg 4-6 times d


Motion sickness

* L1 stands for ancillary label 1, L12 stands for ancillary label 12 and L16 stands for ancillary label 16

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 5

Class Generic name Brand name Indication Dose Other comments


Dolasetron Anzemet Post-operative, See AMH for details. • Dolasetron, ganisetron and tropisetron are given once daily;
5HT3 antagonists
chemotherapy-induced, ondansetron is given 2-3 times daily
Granisetron Kytril radiotherapy-induced
N&V Tropisetron counselling points
Ondansetron Zofran • C - Take medication at least one hour before food
• L1 * - This medicine may cause dizziness
Tropisetron Navoban

Aprepitant Emend Used in combination with 125mg on day 1, an • Decreases effectiveness of pill; use additional contraception
Substance P
antagonists

5HT3 antagonists and hour before chemo, during the 3-day course and for 1 month after your last dose
Fosaprepitant Emend IV dexmethasone to prevent then 80mg on days 2 of aprepitant
N&V associated with and 3 (aprepitant)
chemotherapy

Hyoscine Kwells Motion sickness 0.3mg every 4-6 hrs prn Take the first dose 30 mins before travel
Other


hydrobromide • Use limited by anticholinergic side effects

* L1 stands for ancillary label 1

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 6

LAXATIVES

Lines of therapy • Children: (Liquid paraffin emulsion or lactulose) + stimulant (senna or


• Lifestyle and dietary measures ( fluid intake, fibre intake, exercise) bisacodyl)
• Bulking agent or osmotic laxative • Pregnancy: Use docusate, lactulose, sorbitol, bulking agent. Avoid
• Stimulant stimulant laxatives and polyethylene glycol
• IBS: Antispasmodics (eg. mebeverine, hyoscine butylbromide,
Special cases peppermint oil), TCAs, laxatives, increased fibre intake
• Opioid-induced: Use Coloxyl with Senna or an osmotic laxative
(sorbitol or lactulose); do not use bulking-agent; avoid high fibre diet Other
• Terminal care: Use Coloxyl with Senna • Avoid suppositories and enemas if haemorrhoids or anal fissure are
present

Class Generic name Brand name Dose Other comments


Docusate Coloxyl 100-150mg d or bd • Onset of action is 1-3 days with oral administration and 5-20 mins following rectal
Stool softeners

administration
Liquid paraffin Parachoc 40mL d • Drink plenty of fluid throughout the day
• Liquid paraffin: Do not take a dose immediately before lying down. May reduce
Poloxamer Coloxyl drops 10 drops tds absorption of fat-soluble vitamins (A, D, E, K)
(infant < 6 months) • Poloxamer is preferred in children < 3 years old.

Bisacodyl Bisalax 5-15mg n (oral) • May be used long term for constipation in people taking opioids, spinal damage and
Stimulants

in chronic neuromuscular disease


Senna Senokot 7.5-30mg n (oral) • Insufficient evidence exists to confirm chronic use of stimulant laxatives as being
harmful to the colon
Sodium picosulfate Durolax SP Drops 5mg n (oral) • Onset of action is 6-12 hours(oral); 15-60mins (supp); 5-15 mins (enema)

Glycerol Glycerol Supp 1 d prn • Onset of action for glycerol, lactulose, sorbitol: 1-3 days (oral) and 5-30 mins (rectal)
• Onset of action for polyethylene glycol or saline laxatives: 0.5-3 hrs (oral), 2-30 mins
Osmotic laxatives

Lactulose Actilax 10-25mL d (rectal)


• Saline laxatives: adequate hydration is important
Polyethylene glycol Movicol As directed

Saline laxatives Picoprep As directed

Sorbitol Sorbilax 20mL d

Bulking agents Metamucil As directed • Drink plenty of fluid throughout the day
Bulking
agents

• Do not take immediately before going to bed


• Full effect may take several days

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 7

ANTIDIARRHOEALS

Special cases Practice points


• Diarrhoea-predominant IBS: Use antidiarrhoeal agents. If abdominal • Breastfeeding should be continued.
pain exists, use antispasmodics (eg mebeverine, hyoscine
butylbromide, peppermint oil) or TCAs.
• Diverticular disease: Use bulking agent. Add short term opioid
antidiarrhoeal if necessary.
• Inflammatory bowel disease: Antidiarrhoeal agents are of limited use
and may be dangerous.
• Bile acid-related diarrhoea: Cholestyramine is the treatment of
choice.

Class Generic name Brand name Dose Other comments


Codeine Codeine phosphate 30-60mg 3-4 times daily prn • Loperamide is least likely to produce CNS effects at usual dosage
antidiarrhoeals

• Both codeine and diphenoxylate cause drowsiness


Diphenoxylate Lomotil 5mg 3-4 times daily • Avoid long term use of codeine due to potential addiction
Opioid

• Atropine is added to diphenoxylate to discourage misuse


Loperamide Immodium 4mg stat, then 2mg after every • Avoid use in children
loose stool

Absorbent antidiarrhoeals Donnagel 30mLl stat, then 15mL after • Not recommended
(kaolin and pectin) each loose bowel action
Other

Oral rehydration salts Gastrolyte Add 2 tabs to each 200mL of


drinking water

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 8

DRUGS FOR INFLAMMATORY BOWEL DISEASES

Crohn’s disease Ulcerative colitis


• 5-aminosalicylates: Induce remission in mild-to-moderate disease • 5-aminosalicylates: Induce remission in mild-to-moderate disease, but
• Corticosteroids: Induce remission in acute disease. Rectal main role is maintenance of remission
corticosteroids are effective for distal colonic inflammation. • Corticosteroids: induce remission in acute disease. Rectal
• Azathioprine and mercaptopurine: Maintain remission corticosteroids are effective for distal colonic inflammation.
• Methotrexate: Induces remission or prevents relapse; mainly used in • Azathioprine and mercaptopurine: Maintain remission
patients intolerant to azathioprine and mercaptopurine • Cyclosporin: IV cyclosporine for corticosteroid-refractory disease
• TNF- antagonists: For moderate-to-severe disease unresponsive to • Infliximab: For moderate-to-severe disease unresponsive to
conventional therapy conventional therapy
• Antibacterials: Include metronidazole and ciprofloxacin • Other: Anti-diarrhoeals, antispasmodics
• Other: Anti-diarrhoeals, cholestyramine, diet

Class Generic name Brand name Dose Other comments


Budesonide Entocort 9mg d cc • Possible side effects: adrenal suppression, increased susceptibility to infection,
Corticosteroids

sodium and water retention, oedema, hypertension, hypokalaemia,


Hydrocortisone Colifoam 1 d or bd for 2-3 wks, then every hyperglycaemia, dyslipidaemia, osteoporosis, muscle wasting
nd
2 day until remission • L9 *
• Seek medical attention if you notice signs of infection
• Tell all healthcare professionals treating you that you are taking corticosteroids
Prednisolone Predsol 1 enema n until remission
• Budesonide: L18 *

Balsalazide Colazide Acute UC: 3 tds until remission • All 5-aminosalicylates are contraindicated in people allergic to salicylates;
Maintenance 2 bd until remission sulfazsalazine is contraindicated in those allergic to sulfonamides
• Common adverse effects: rash, headache, diarrhoea
5-aminosalicylates

Mesalazine Salofalk See AMH for details • Balsalazide is a pro-drug of mesalazine


• Mesasal: Take tablets at least half an hour before food
Olsalazine Dipentum Acute UC: 1g bd • Salofalk: Take tablets at least one hour before food
Maintenance UC: 500mg bd • Pentasa: Absorption not affected by food. The tablets may be dispersed in
50mL cold water, stirred and taken immediately.
Sulfazalazine Salazopyrin Acute UC: 2-4g d in 3-4 doses • Olsalazine: Take with food to avoid diarrhoea
Maintenance: 500mg qid • Sulfasalazine: Take with food to avoid gastrointestinal upset; monitor complete
Crohn’s colitis: 3-6g daily in blood profile liver function and urine; disposable lenses may still be used since
divided doses sulfasalazine tends to stain soft lenses
Adalimumab Humira Injection as directed • See RA notes in summary for Chapter 15
antagonists
TNF-

Infliximab Remicade Injection as directed • See RA notes in summary for Chapter 15

* L9 stands for ancillary label 9, L18 stands for ancillary label 18

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 9

DRUGS FOR OBESITY

Indication: Obesity in adults (BMI>30 pr >27 with other risk factors eg HT, diabetes, hyperlipidaemia)

Drug choice: Orlistat, sibutramine, phentermine, fluoxetine and other SSRIs, meal replacement

Generic name Brand name Dose Side effects Precautions Other comments
Orlistat Xenical 120mg tds • Oily stools • Cholestasis • Take with your main meals. Do not take your dose if you
(GI lipase inhibitor) miss a meal or if it does not contain fat.
• This medication may cause oily stools, especially if your
diet is high in fat.
• Apply caloric restriction, increased physical activity and
eating behaviour modification
• Blood glucose, BP and lipid control may improve so
changes to other medications may be necessary
• Orlistat may absorption of fat-soluble vitamins (ADEK)

Phentermine Duromine 15mg d • Overstimulation • Contraindicated in • L12 *


(sympathomimetic, of CNS CVD, hyperthyroidism, • Tell your doctor is you get short of breath
increases (eg insomnia, glaucoma, peptic ulcer, • Recommended for short term use only
metabolism) agitation, sibutramine, MAOI
tachycardia) • Use with caution for
drugs that contribute to
serotonin toxicity

Sibutramine Reductil 10mg m • HR, BP • Contraindicated in • Monitor BP and HR


(NAd and serotonin • Palpitations, CVD, bipolar disorder, • Increased physical activity and eating behaviour
reuptake inhibitor, haemorrhoids modification should be applied in conjunction with
induces satiety) • Use with caution for treatment
drugs that contribute to
serotonin toxicity

* L12 stands for ancillary label 12

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 10

DRUGS FOR PERIANAL DISORDERS AND OTHER GASTROINTESTINAL DRUGS

Pruritus ani Anal fissure


• Keep area clean and dry; avoid irritants • Avoid straining
• Apply sorbolene cream after cleansing; hydrocortisone may relieve • Increase fibre and fluid intake
inflammation • Take a warm bath
• Bulking agent or stool softener
Haemorrhoids • Topical anaesthetic (relieves pain only)
• Avoid straining • Rectal GTN (mainly relieves pain)
• Increase fibre and fluid intake
• Anorectal medications

Generic name Brand name Indications Other comments


Anorectal products Proctosedyl Haemorrhoids • Limit use to no more than a week because local anaesthetics may sensitise perianal skin
Anal fissure and topical corticosteroids may exacerbate local infection
Pruritis
Glyceryl trinitrate Rectogesic Anal fissure • Use tds for up to 8 weeks
• May cause headaches

Pancreatic enzymes Creon 5000 Cystic fibrosis • Take this medicine with food
Chronic pancreatitis • Do not crush or chew. Sprinkle the granules onto a small amount of soft food.
After gastrectomy or • Avoid taking this medicine with hot liquid or food as heat can damage enzymes
pancreatic surgery

Ursodeocycholic acid Ursofalk Chronic cholestatic liver


disease

Copyright © The Medicine Box 2009


AMH Summary: Chapter 12 – Gastrointestinal 11

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2009

Copyright © The Medicine Box 2009

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2009


AMH Summary: Chapter 13 – Genitourinary 1

AMH SUMMARY
CHAPTER 13: GENITOURINARY

A. URINARY INCONTINENCE

TYPES OF URINARY INCONTINENCE


• Urge incontinence - failure to uninhibited contraction of bladder
• Stress incontinence - impaired urethral support preventing urine loss due to pressure such
as coughing
• Overflow incontinence - bladder emptying failure, unable to contract detrusor muscles

TREATMENT

Anticholinergics
(darifenacin, oxybutynin, propanthelene, solifenacin, tolterodine)
• Relaxes bladder and increases capacity for urge incontinence
• Adverse effects include dry mouth, blurred vision, constipation, confusion
• Avoid in patients with dementia

Alpha blockers
(prazosin, tamsulosin, terazosin)
• Reduces overflow incontinence by relaxing muscle in bladder
• Adverse effects include dizziness, particularly with the first dose and drowsiness

Practice points with incontinence


• Pelvic floor exercise, bladder training and behavioural techniques are effective first line
treatment for stress and urge incontinence

B. NOCTURAL ENURESIS IN CHILDREN

• Involuntary loss of urine, possibly from maturational delay and usually resolves
spontaneously
• Non drug treatment is preferred such as motivational therapy and alarm systems

TREATMENT

Desmopressin
• Antidiruretic hormone
• Adverse effects includea headache (tablet), nosebleed, rhinitits, nausea, abdominal
pain (intranasal)
• Not to be used if child has vomiting or diarrhoea
• Ensure that child has enough fluid to quench thirst from 1 hour before dose or 8 hours
after

Copyright © The Medicine Box 2009


AMH Summary: Chapter 13 – Genitourinary 2

C. BENIGN PROSTATIC HYPERPLASIA

• Prostate disorder causing urinary obstruction


• Drug therapy used for symptom relief by reducing outflow resistance
• Drug choice dependent on prostate size

TREATMENT

Alpha blockers
(prazosin, tamsulosin, terazosin)
• Increase urinary flow by relaxing bladder neck and prostatic smooth muscle
• May be effective regardless of prostate size
• Full effect in 4-6 weeks

5-alpha-reductase inhibitors
(finasteride)
• Reduces prostate size, appears effective if prostate is very large, equivalent to 40cm3 or
larger
• Can cause sexual dysnfunction
• Contraindicated in women and children
• A clinical response may take 6 months or more

D. PROSTATITIS

• Inflammation of prostate gland

ACUTE BACTERIAL PROSTATITIS


• Associated with UTI
• Treat with trimethoprim, norfloxacin
• Ensure adequate fluids, rest, stool softener and pain relief

CHRONIC BACTERIAL PROSTATITIS


• Associated with chronic or relapse UTI, pain associated
• Trimethoprim, norfloxacin, ciprofloxacin for at least 4 weeks
• General measures include adequate fluid intake, rest, pain relief, similar to acute prostatitis

CHRONIC NON-BACTERIAL PROSTATITIS


• Similar symptoms to chronic prostatitis
• No proven benefit with any treatment
• Pain relief and relief of constipation may help

Copyright © The Medicine Box 2009


AMH Summary: Chapter 13 – Genitourinary 3

E. ERECTILE DYSFUNCTION

• Therapy aims to achieve penile erection adequate for sexual intercourse


• Erectile dysfunction can be caused by physical (e.g neurological, vascular, endocrine)
problems and psychological problems

Phosphodiesterase 5 inhibitors
(sildenafil, tadafil, vardenafil)
• Works by breaking down cGMP, increasing blood flow to penis during sexual
stimulation
• Contraindicated in nitrate use
• Adverse effects include headache, dizziness, nasal congestion, risk of priapism
• Can also cause visual disturbances
• Counselling - stop taking medication if you experience loss of vision
- nitrate use may cause a drop in blood pressure

Alprostadil
• Dilates cavernosal arteries, relaxes smooth muscle of corpus cavernosum
• Contraindicated in conditions leading to priapism and penile implants
• Adverse effects include penile pain and erection lasting 4-6 hours
• Counselling - tell doctor if increased or new pain in penis occurs or bending of penile
shaft

Papaverine
• Relaxes vascular components of penile system
• Adverse effects include pain upon injection, priapism and dizziness
• Counselling- tell doctor of increased pain in penis
• Take care when getting up from sitting position as medication can cause dizziness

Copyright © The Medicine Box 2009


AMH Summary: Chapter 13 – Genitourinary 4

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2009

Copyright © The Medicine Box 2009

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2009


AMH Summary: Chapter 15 – Musculoskeletal 1

AMH SUMMARY: CHAPTER 15 – MUSCULOSKELETAL


DRUGS FOR OSTEOARTHRITIS

Drug choice: Paracetamol, topical NSAIDs, capsaicin and rubefacients, Hylans may be used if other treatment options (intra-articular corticosteroids
NSAIDs, intra-articular corticosteroids, intra-articular hylans, glucosamine NSAIDs, joint replacement surgery) are contraindicated

NSAIDs may not necessarily trigger a better response than paracetamol even Glucosamine should not be taken by people allergic to shellfish
if clinical signs of inflammation are evident.

Class Generic name Brand name Dose Side effects Precautions Other comments
Aspirin Astrix 300mg cc prn • GI ulceration • Asthma Comparative information
• Salt and fluid retention • Bruising • All NSAIDs worsen CVD
Diclofenac Voltaren 75-100mg d cc prn, max 200mg • Hypertension • Coagulation disorder • COX-2 inhibitors have a
• CVD lower risk of GI upset than
Ibuprofen Brufen 200-400mg tid-qid cc prn • Gastrointestinal non-selective agents
• Renal impairment • Enteric coated and rectal
Indomethacin Indocid 25-50mg bd-qid cc prn • Surgery formulations do not reduce
Non-selective NSAIDs

the risk of GI ulceration


Ketoprofen Orudis 200mg d cc prn
Practice points
Ketorolac Toradol 10mg every 4-6 hrs cc prn • Complete blood count,
creatinine, liver function
Mefenamic acid Ponstan 500mg tds cc prn should be monitored at
baseline and annually
Naproxen Naprosyn 250-500mg bd cc prn (conv) thereafter. Monitor BP for
etoricoxib.
Piroxicam Feldene 10-20mg d cc prn • Consider ceasing NSAID
2-3 days before surgery
Sulindac Aclin 200-400mg d cc prn due to increased risk of
bleeding assoc with
Tiaprofenic acid Surgam 300mg d or bd cc prn non-selective agents and
increased risk of thrombotic
events assoc with COX-2
inhibitors. A 7-day interval
may be necessary for
aspirin.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 2

Class Generic name Brand name Dose Side effects Precautions Other comments
Celecoxib Celebrex 200mg d cc prn Counselling
• Tell the doctor if you
inhibitors
COX-2

Etoricoxib Arcoxia 30-60 mg d cc prn develop swollen ankles,


difficulty breathing, black
Meloxicam Mobic 7.5-15mg d cc prn stools, coffee-coloured
vomit
Parecoxib Dynastat inj.
Drug-specific
• Aspirin: avoid use in
children < 12 years and in
12-16 year olds
recovering from chicken
pox, influenza or fever,
due to increased risk of
Reye’s syndrome
• Celecoxib: do not use in
patients allergic to
sulphonamides

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 3

DRUGS FOR RHEUMATOID ARTHRITIS

Drug treatment
• Drug choice is determined by disease severity, relative efficacy and toxicity profile of drugs
• Combinations of antirheumatics may be used
• Early RA: antirheumatic agents, analgesics, corticosteroids, NSAIDs
• Mild disease: sulfasalazine, hydroxychloroquine
• Moderate-severe disease: methotrexate, IM gold, penicillamine, cytokine modulators, leflunomide

Practice points
• Pneumococcal and annual influenza vaccinations are recommended for all patients with RA
• If possible, limit use of more toxic agents during remission.
• Omega-3-fatty acids (2.6g daily) or gamma-linolenic acid (1.4-2.8g daily) may reduce severity of symptoms according to evidence

Class Generic name Brand name Dose Side effects Monitoring Other comments
Abatacept Orencia IV every 4 weeks • Infections • Blood (FBE) • Avoid using > 1 cytokine
• HT • Renal (Cr) modulator together as this
• Liver (AST, ALT) increases susceptibility to
infection
Rituximab Mabthera IV 2-dose course, Infections Blood (FBE)
Cytokine modulators

• • • Seek medical attention if you


repeat after > 6 months • Renal (Cr) notice signs of infection
• Liver (AST, ALT) • Some vaccines should not be
given to people receiving
Tocilizumab Actemra IV every 4 weeks • Infections • Blood (FBE) cytokine modulators
• Hyperlipidaemia • Liver (AST, ALT) • Rituximab: may give
• Neutropenia • Lipids paracetamol, antihistamine,
• Thrombocytopenia methyl-prednisolone 30 mins
pre-infusion to reduce infusion
Anakinra Kineret SC daily • Infections • Blood (FBE) reaction
• Neutropenia
Adalimumab Humira SC every 2 weeks • Infections • Blood (FBE) • Seek medical attention if you
• Worsening HF • Renal (Cr) notice signs of infection
Certolizumab Cimzia SC every 2 weeks • Blood dyscrasias • Liver (AST, ALT) • Some vaccines should not be
antagonists

• Skin cancer given to people receiving TNF-


Etanercept Enbrel SC once or twice a wk antagonists
TNF-

Golimumab Simponi SC every 4 weeks

Infliximab Remicade IV every 8 weeks

* L8 stands for ancillary label 8

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 4

Class Generic name Brand name Dose Side effects Monitoring Other comments
Methotrexate Methotrexate Oral/IM/SC weekly • Myelosuppression • Blood (FBE) • Take on the same day each wk
(folic acid • Pulmonary toxicity • Renal (Cr) • L8 **
antagonist) If GI effects occur, • Hepatotoxicity • Liver (AST, ALT) • Seek medical attention if you
divide oral dose into • Photosensitivity • Lung (PFT) notice cough, difficulty
3 and take at 0, 12 • Lymphoma • Chest x-ray breathing, bleeding, or signs of
and 24 hours. • Severe skin reactions (rare) infection
• Give folic acid or folinic acid
supplement to reduce GI effects
(nausea, diarrhoea). Usual
dose is 1-5mg daily.
• Also indicated for treatment of
solid tumours, severe disabling
psoriasis
• Avoid conception until 3 months
after stopping treatment for
either partner
Immunosuppressants

Azathioprine Imuran 50-150mg daily in • Infections • Blood (FBE) • L8 **


divided doses • Myelosuppression • Renal (Cr, urea) • Interaction: allopurinol reduces
• Hepatotoxicity • Liver (AST, ALT) metabolism of azathioprine and
• Alopecia increases the risk of bone
• Mouth ulceration marrow toxicity
• Tell your doctor if you notice
bleeding or signs of infection
• Also indicated for prevention of
organ transplant rejection

Leflunomide Arava 20mg daily • Infections • Blood (FBE) • L2 (risk of liver damage), L8 **
• Diarrhoea • Renal (Cr) • Seek medical attention if you
• Alopecia • Liver (AST, ALT) notice yellowing of the skin
• liver enzymes (use with • BP (jaundice) or signs of infection
methotrexate can risk of • Some vaccines should not be
hepatic reaction) given to people receiving TNF-
• Paraesthesia antagonists

** L2 stands for ancillary label 2 and L8 stands for ancillary label 8

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 5

Class Generic name Brand name Dose Side effects Monitoring Other comments
Cyclosporin Cicloral 3mg/kg daily in 2 • Infection • Blood (FBE) • L8, L18 **
(calcineurin divided doses • Renal insufficiency • Renal (CR, urea) • Clean your teeth and gums
Immunosuppressants

inhibitor) (cyclosporin is C/I in renal • Liver (AST, ALT) thoroughly


+
impairment and must be • BP, K • Seek medical attention if you notice
used with caution in those • Urinalysis signs of infection
+
treated with K , ACEIs, • Also indicated for severe psoriasis
angiotensin II antagonists and prevention of organ transplant
and nephrotoxic agents rejection
including NSAIDs and
aminoglycosides)
• Anaemia
+
• K , BP, cholesterol
• Gingival hyperplasia

Auranofin Riduara 3-9mg daily cc • Diarrhoea, dyspepsia • Blood (FBE) • Seek medical attention if you notice
• Taste disturbance • Urinalysis signs of infection, rash, diarrhoea
Gold-induced dermatitis • Gold-induced dermatitis may
Gold salts


Aurothiomalate Myocrisin inj. • Nephrotoxicity worsen with exposure to sunlight
• liver enzymes
• Blood dyscrasias
• Myelosuppression
• Proteinuria
Hydroxychloroquine Plaquenil 200-400mg daily cc • Rash • Blood (FBE) • Seek medical attention if you have
• Retinal damage • Renal (Cr) trouble seeing things. Wear
• GI adverse effects • Liver (AST, ALT) sunglasses in bright light.
• Eye • Also indicated for lupus and malaria

Penicillamine D-Penamine 250-1000mg daily in • Myelosuppression • Blood (FBE) • L4 ***


2-3 divided doses ac Stomatitis Urinalysis Seek medical attention if you notice
Other

• • •
• Proteinura signs of infection
• C/I in patients with penicillin • Do not take within 1 hr of food, milk,
allergy antacids and other drugs
Sulfasalazine Salazopyrin 2-3g daily in divided • Myelosuppression • Blood (FBE) • Also indicated for ulcerative colitis,
(5-aminosalicylate) doses cc • Renal (Cr) and Crohn’s disease
• Liver (AST, ALT) • May stain soft lenses; consider
disposable lenses
• Sulfasalazine impairs absorption of
folic acid, consider supplementation

*** L4 stands for ancillary label 4, L8 stands for ancillary label 8 and L18 stands for ancillary label 18

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 6

DRUGS FOR GOUT

Drug choice
• Acute gout: NSAIDs, corticosteroids, colchicine
• Long term treatment: Allopurinol and probenecid (for urate-lowering treatment), colchicine and NSAIDs (for prophylaxis)
• In renal impairment, corticosteroids are preferred for acute gout.
• In patients on warfarin, systemic corticosteroids are the treatment of choice for acute gout.

Generic name Brand name Dose Side effects Precautions Other comments
Colchicine Colgout Acute attack: initially • Diarrhoea, nausea, • Renal impairment • Consider for acute gout only when NSAIDs and
1mg, then 500mcg abdominal discomfort • Clarithromycin corticosteroids are contraindicated
1 hr later (max 1.5mg • Agranulocytosis, can inhibit • Colchicine may be used instead of NSAIDs in HF
per course, min 3-day thrombocytopenia, metabolism of as it does not cause oedema
interval btwn courses) leucopenia, aplastic colchicine • Colchicine has a delayed onset of effect. May use
anaemia (rare) other analgesics (paracetamol) first.
Prophylaxis: 500mcg • Avoid grapefruit juice ( risk of side effects)
once/twice daily • Tell the doctor if you develop severe diarrhoea,
muscle pains, unusual bleeding
• Monitor complete blood count

Allopurinol Zyloprim 100-300mg daily pc • Itchy rash • Renal impairment • Start allopurinol after an acute attack has settled
(xanthine oxidase (maintenance) • Azathioprine and (otherwise it may worsen the attack)
inhibitor, reduces mercaptopurine • Once treatment is established, continue
uric acid production) (allopurinol allopurinol at the current dose, even during
reduces attacks of gout
metabolism of • This medicine may make you feel dizzy.
azathioprine and • Drink ample fluids during treatment to prevent
mercaptopurine, kidney stones
increasing the • Contact the doctor if you develop a rash, swollen
risk of bone lips, fever or sore throat
marrow toxicity) • Monitor uric acid every 4 weeks

Probenecid Pro-cid 500mg bd cc • Rash, nausea, • Renal impairment • Wait until attack has settled before starting
(increases renal (maintenance) vomiting • Avoid aspirin treatment with probenecid; may worsen acute
excretion of uric • Uric acid kidney ( effect of attack
acid) stones probenecid) • Continue probenecid if acute attack occurs
• Thrombocytopenia • Drink ample fluid during treatment to prevent
(rare) kidney stones
• Monitor renal function and blood count
• Prohibited in elite sports due to potential as
masking agent

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 7

DRUGS FOR OTHER MUSCULOSKELETAL CONDITIONS

Acute soft tissue injuries Back pain


• Bursitis and tendonitis: • Acute: Continue ordinary activity. Paracetamol, NSAIDs or opioids
- Avoid painful activities, use passive motion exercises, and apply may be used. Evidence for muscle relaxants is conflicting.
heat or ice packs • Chronic: Stay active, massage, and use short-term paracetamol and
- Use analgesics (NSAIDs and paracetamol) to reduce pain and aid NSAIDs if necessary. TCAs or opioids may be used. Insufficient
mobilisation evidence for muscle relaxants.
- Topical NSAIDs and rubefacients may be considered.

• Strains and sprains:


- RICE (rest, ice, compression, elevation)
- Topical NSAIDs and rubefacients may be considered.

Class Brand name Formulation Side effects Precautions Other comments


Hylans Synvisc Injection • Pain and swelling • Contraindicated in •Synvisc is derived from chickens.
Fermathron infected or inflamed Elimination of infective agents may not
joints be complete

Topical Voltaren Emulgel Topical • Capsaicin may cause • Pregnancy and • Apply for up to 14 days, then review
musculoskeletal Deep Heat stinging or burning breastfeeding need for further treatment
agents • Salicylates may have
systemic effects

Copyright © The Medicine Box 2012


AMH Summary: Chapter 15 – Musculoskeletal 8

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 16 – Neurological 1

AMH SUMMARY
CHAPTER 16: NEUROLOGICAL

A. EPILEPSY

PARTIAL SEIZURES

First-line treatment: Carbamazepine

Carbamazepine
• Works by blocking sodium channels
• Adverse effects include drowsiness, ataxia, dizziness diplopia, headache
• Requires concentration monitoring (4-12mg/L)
• Take with food
• May cause drowsiness or dizziness, do not operate machinery if affected
• Tell doctor if rash, sore throat, ulcers occur

Other medications
• Gabapentin, lamotrigine, levetiracetam, oxycarbazepine, phenobarbitone, phenytoin,
pregabalin, tiagabine, topiramate, valproate

GENERALISED TONIC-CLONIC

First-line treatment: Carbamazepine, valproate

Valproate
• Works by blocking sodium channels
• Contraindicated in severe hepatic dysfunction and pancreatic dysfunction
• Adverse effects include nausea, vomiting, increased appetite, weight gain, drowsiness
• Counselling
- Take with food, do not crush or chew tablets
- May make you drowsy, do not operate machinery if affected
- Appetite may increase
- Tell doctor if fever, rash, jaundice, bleeding develop

Other medications
• Lamotrigine, levetiracetam, oxcarbazepine, phenobarbitone, phenytoin, topiramate

Copyright © The Medicine Box 2012


AMH Summary: Chapter 16 – Neurological 2

ABSENCE SEIZURES

First-line treatment: Valproate, ethosuximide

Ethosuximide
• Reduces threshold calcium conductance in thalamic neurones
• Adverse effects include anorexia, nausea, weight loss
• Concentration monitoring required, 40-100mg/L
• Counselling
- May cause drowsiness and dizziness
- Contact doctor if fever, sore throat, ulcers or bruising develop

Other medications
• Clobazam, clonazepam, lamotrigine

MYOCLONIC SEIZURES

First-line treatment: Valproate

Other medications
• Clobazam, clonazepam, phenobarbitone, levetiracetam

INFANTILE SPASMS

First-line treatment: Tetracosactrin (ACTH analogue), prednisolone

Other medications
• Clonazepam, nitrazepam, valproate, vigabatrin

OTHER IMPORTANT POINTS


• Lamotrigine - risk of severe skin reactions (Steven Johnson’s syndrome)
• Phenytoin interacts with multiple medication and can cause gingival hypertrophy
• Topiramate - risk of causing acute myopia with secondary acute closed angle glaucoma

B. PARKINSONISM

• Drug treatment aims to redress balance of dopamine deficiency and cholinergic excess
• The decision to begin treatment dependent on whether condition has become physically or
socially debilitating
• All medications are not shown to slow progression of disease

Carbidopa/ levadopa with benserazide


• Converts to dopamine in brain, benserazide (dopamine decarboxylase inhibitor)
reduces peripheral dopamine production

Copyright © The Medicine Box 2012


AMH Summary: Chapter 16 – Neurological 3

• Levodopa improves bradykinesia, rigidity and tremor (to a certain degree)


• Contraindicated in closed angle glaucoma
• Adverse effects include anorexia, nausea, vomiting, sudden unpredictable loss of
mobility (off effect)
• Counselling
- Take at same time each day and same way
- May cause drowsiness, if affected, do not operate machinery
- May cause dizziness of standing up too quickly

Bromocriptine, cabergoline, pergolide


• Acts as dopamine agonists
• Improves bradykinesia and rigidity
• Not as effective as levodopa with bradykinesia and rigidity
• May be used in combination with levodopa to lower its overall dose

Apomorphine
• Used in those severely disabled by motor fluctuations refractory to conventional
treatment
• Contraindicated in hypotonia and neuropsychiatric disorders such as Alzheimer’s
disease

Pramipexole
• Non-ergot derived dopamine agonist
• Dose reduction may be required in those with renal impairment

Rotigotine
• Patch formulation dopamine agonist
• Patch to be applied the same time each day to hairless, clean area around the hip,
abdomen, thigh, upper arm or shoulder
• Rotate site of application daily

Selegiline
• MAOB inhibitor with dopamine inhibition
• Adverse effects include insomnia, headache, dizziness

Anticholinergics
(beznhexol, benztropine, biperiden, orphenadrine)
• Used to reduce tremor, little effect on rigidity and bradykinesia
• Adverse effects include dry mouth, blurred vision, constipation

Entacapone
• Inhibits catechol-O-methytransferase (COMT), increasing levodopa available to brain,
prolonging clinical response to levodopa
• Used as an adjunct in levodopa, experiencing fluctuation in motor function due to end of
dose effect

Copyright © The Medicine Box 2012


AMH Summary: Chapter 16 – Neurological 4

C. MIGRAINE

• Analgesics and antiemetics for symptomatic relief

Ergot alkaloids
(dihydroergotamine)
• 5HT1b/1d agonist
• Adverse effects
• Dependence may occur with overuse, resulting in rebound headaches
• Nausea, vomiting, abdominal pain

Triptans
(naratriptan, sumatriptan, zolmitriptan, eletriptan)
• 5HT1 agonists
• Contraindicated in MI history, heart disease, uncontrolled hypertension
• Adverse effects include sensation of tingling, heat, pain and tightness in body
• Counselling
- Most effective when headache is beginning to develop
- Medication may cause drowsiness or dizziness
- If no improvement after first dose, do not repeat dose

Methysergide
• 5HT2 antagonist
• Contraindications include vascular diseases, valvular heart disease, uncontrolled
hypertension
• Adverse effects include nausea, vomiting, drowsiness, dizziness, myocardial infarction
• Counselling
- May cause drowsiness and dizziness
- Stop treatment if tingling, numbness or chest pains occur

PizotIfen
• 5HT2 antagonist
• Adverse effects include sedation, fatigue, weight gain, increased appetite
• Counselling
- May cause drowsiness
- Appetite may increase, pay attention to diet to avoid weight gain

D. ALZHIEMER’S DISEASE

• Degeneration in brain of cholinergic neurones and fall in Ach concentrations


• Treatment involves antipsychotics, mood stabilisers (carbamazepine, valproate) and
anticholinesterases.

Anticholinesterases
(donepezil, galantamine, rivastigmine)
• Decreases breakdown of Ach, reducing deficiency of cholinergic activity in Alzheimer’s
• Contraindicated in active peptic ulcer and GI or ureteric obstruction

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AMH Summary: Chapter 16 – Neurological 5

• Adverse effects include nausea, vomiting and drowsiness


• Counselling
• May cause dizziness or drowsiness
• Omit 1 or more doses if adverse effects occur

Memantine
• NMDA antagonist, reducing glutamate induced neuronal degradation
• Contraindications include history of seizures
• Adverse effects include confusion, dizziness, drowsiness, headache
• Counselling- drowsiness and dizziness may occur, do not operate machinery if affected

E. MULTIPLE SCLEROSIS

Glatiramer
• Used to reduce frequency of relapses in patients with relapsing-remitting MS
• Adverse effects include pain in injection site, post injection reaction
• Rotate injection site to reduce irritation and pain

Interferon beta
• Acts through antagonising immunoregulatory actions including gamma interferon,
reduction of cytokine release and augmentation of suppressor T-cell function
• Adverse effects include pain and inflammation of injection site, rash, flu-like symptoms,
suicidal thoughts
• Counselling
- Tell doctor if felling depressed or sad
- Take paracetamol beforehand and inject at bedtime
- Rotate injection site to prevent irritation
• Practice point - complete blood count and liver function tests at 1, 3, 6 months

F. MYASTHENIA GRAVIS

Neostigmine and pyridostigmine


• Adverse effects include increased salivation, nausea, vomiting, abdominal cramps

G. OTHER NEUROLOGICAL DRUGS

• Baclofen - structural analogue of GABA for chronic spasticity


• Dantrolene - muscle relaxant for chronic spasticity
• Modafanil - non amphetamine psychostimulant for sleeplessness
• Riluzole - may act by inhibiting glutamate neurotransmission used in amyotrophic lateral
sclerosis
• Ropinirole - dopamine against used in restless leg syndrome

Copyright © The Medicine Box 2012


AMH Summary: Chapter 16 – Neurological 6

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 17 – Obstetric and Gynaecological 1

AMH SUMMARY: Chapter 17 – Obstetric & Gynaecological

- CONTRACEPTION -

DRUGS OF CHOICE FOR CONTRACEPTION


a) Combined oral contraceptives
b) Progestogens
c) Intrauterine devices IUD
d) Others

Emergency Contraception:
 LEVONORGESTREL – Postinor, Norlevo
- prevent or delay ovulation and induce transient changes in endometrium. It can’t disrupt an
implanted fertilized egg.
- repeat dose if vomiting occurs within 2 hours
- no limit in recurrent use
- take within 72 hours of unprotected sex (24 hours most effective but still has a contraceptive effect
when taken up to 120 hours afterwards).
- 1.5mg immediately or 750mcg q12h
- safe during breastfeeding

COMBINED ORAL CONTRACEPTIVES (pill)


Indications: Contraception, Moderate Acne (Loette), Androgenisation (hirsutism and acne) in women
(cyproterone – Brenda-35, Diane-35, Juliet-35, Estelle-35), menstrual disorders, period pain, endometriosis,
PMS

Contraindications: history of breast, endometrial cancer, migraines, pregnancy, viral hepatitis

Precautions: diabetes, hypertension (monitor), depression, epilepsy, migraine, cholestatic jaundice, smoking
(increases risk of thromboembolism), hyperlipidaemia

Side Effects: breakthrough bleeding, nausea, vomiting, changes in weight, breast enlargement and
tenderness, headache, mood changes (eg depression), changes in libido, fluid retention, acne, thrush

Dosage: start in the first week of active tablets on day 1-5 of menses to be protected immediately. If start
active pills after this time, use additional contraception or avoid intercourse until 7 active pills have been
taken.
- Missing pills: <24 hours – take it asap and take the next pill at usual time
- Missing pills: >24 hours – take it asap and next pill at usual time (i.e. 2 pills at one time) but need to
wait 7 days for protection. But if the 7 days extend into inactive pills, then you need to skip the
inactive pills and go straight to a new pack of active pills (so no periods for this month)

Copyright © The Medicine Box 2012


AMH Summary: Chapter 17 – Obstetric and Gynaecological 2

* If you missed active pills and need to take emergency contraceptive tablets, you should start taking your
pill again within 12 hours of taking the emergency contraceptive tablets. You will need to use additional
contraception, eg condoms, or avoid intercourse until you have taken active pills for 7 days.

Breakthrough Bleeding:
If breakthrough bleeding persists for >3 months and another cause cannot be identified (eg missed pills,
drug interaction), try the following (in order):
 change to a monophasic COC if taking a triphasic COC
 change the progestogen or increase dose (especially if bleeding occurs late in cycle)
 take active tablets for 9 weeks in a row
 change to a standard dose COC (with 30–35 micrograms ethinyloestradiol or 50 micrograms of
mestranol) if taking a low dose COC (with 20 micrograms ethinyloestradiol)
 change the progestogen again
 change to a high dose COC (with 50 micrograms ethinyloestradiol).

Drug Choice (Progesterone):


 Levonorgestrel, norethisterone: lower risk of venous thromboembolism (VTE).
 Gestodene, desogestrel: less androgenic activity than levonorgestrel but twice the risk of VTE.
Generally not first choice for new users.
 Dienogest: one-third anti-androgenic activity to that of cyproterone. Benefits acne.
 Drospirenone: anti-mineralocorticoid (mild diuretic and potassium retention) and anti-androgenic
activity.
 Cyproterone: progestogenic and anti-androgenic. Used with an oestrogen to treat women with
androgenisation (severe acne, hirsutism). Higher risk of VTE and is not indicated in the absence of
androgenisation.

Table: Monophasic and Triphasic COCs


Monophasic = fixed dose of estrogen and progesterone in each active pill
Triphasic = both estrogen and progesterone content varies – more complex and high risk of fluid retention
and PMS

Monophasic Low Dose Monophasic Standard Dose Monophasic High Dose

Loette, Microgynon 20 Levlen, Microgynon 30, Microgynon 50 (ethinyloestradiol


(ethinyloestradiol Monofeme, Nordette 50 mcg/levonorgestrel 125 mcg)
20 mcg/levonorgestrel 100 mcg) (ethinyloestradiol
30 mcg/levonorgestrel 150 mcg)
Yaz (ethinyloestradiol Brevinor, Norimin
20mcg/drospirenone 3mg) (ethinyloestradiol
35 mcg/norethisterone 0.5 mg)
Brevinor-1, Norimin-1 Triphasic
(ethinyloestradiol
35 mcg/norethisterone 1 mg)

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 3

Marvelon (ethinyloestradiol Logynon, Trifeme, Triphasil, Triquilar


30 mcg/desogestrel 150 mcg) (ethinyloestradiol
30 mcg/40 mcg/30 mcg levonorgestrel
50 mcg/75 mcg/125 mcg)
Valette (ethinyloestradiol Improvil, Synphasic (ethinyloestradiol
30 mcg/dienogest 2 mg) 35 mcg/35 mcg/35 mcg/norethisterone
0.5 mg/1 mg/0.5 mg)
Yasmin (ethinyloestradiol Qlaira (oestradiol 3mg/2mg/2mg/1mg
30 mcg/drospirenone 3 mg) dienogest nil/2mg/3mg/nil)
Femoden, Minulet
(ethinyloestradiol
30 mcg/gestodene 75 mcg)
Norinyl-1 (mestranol
50 mcg/norethisterone 1 mg)
Brenda-35, Diane-35, Estelle-
35, Juliet-35 (ethinyloestradiol
35 mcg/cyproterone 2 mg)

 CYPROTERONE with ETHINYLOESTRADIOL – Brenda, Diane, Juliet, Estelle


 DESOGESTREL with ETHINYLOESTRADIOL – Marvelon
 DIENOGEST with ETHINYLOESTRADIOL - Valette
 DIENOGEST with OESTRADIOL - Qlaira
 DROSPIRENONE with ETHINYLOESTRADIOL – Yasmin, Yaz
 GESTODENE with ETHINYLOESTRADIOL – Femoden, Minulet
 LEVONORGESTREL with ETHINYLOESTRADIOL – Loette, Microgynon 20ED; Microgynon 30ED,
Levlen; Monofeme, Nordette; Logynon, Triquilar ED; Trifeme, Triphasil
 NORETHISTERONE with ETHINYLOESTRADIOL – Brevinor, Normin, Improvil
 NORETHISTERONE with MESTRANOL – Norinyl

PROGESTOGENS (minipill)
Indications: contraception when can’t use oestrogen (breastfeeding, history of thromboembolism, smokers),
menstrual disorders

Contraindications: breast cancer, hepatitis

Side Effects: menstrual irregularity, prolonged bleeding, spotting, amenorrhoea, depression, weight gain

 ETONOGESTREL – Implanon implant


- protection occurs within 1st day of insertion if inserted on day 1-5 of cycle; if inserted another time,
then additional contraception is required for 7 days after insertion.
- insert every 3 years

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 4

 LEVONORGESTREL – Microlut, Norlevo-2, Levonelle-1, Postinor-1; Mirena IUD


- Side Effects: Emergency contraception, nausea, vomiting, breast tenderness, vaginal bleeding,
headache
Levonorgestrel IUD, irregular bleeding, reduced menstrual flow, amenorrhoea, expulsion of device
(particularly in the first year), reversible ovarian cysts
- Use additional contraception for 48 hours if not starting within 1-5 day of menstruation. There are no
inactive pills like the COC so must be taken continuously. If you miss a pill and its over 3 hours, you
are not protected. Take it as soon as you remember but use additional contraceptive methods for the
next 48 hours.
- The minipill is less effective than COCs.
- Mirena IUD: Insert within first 7 days after start of menstrual cycle or 6 weeks after delivery; may be
replaced by new IUD at any time in cycle; replace every 5 years. Contraceptive effect is immediate if
inserted on day 1–7 of cycle otherwise use extra protection for the next 7 days.

 MEDROXYPROGESTERONE – Depo-Provera inj, Depo-Ralovera inj, Provera


- Indications: Contraception (IM depot), dysfunctional uterine bleeding, endometeriosis, HRT
- SE: IM, 50% become amenorrhoeic within 12 months, delayed return of menstrual periods after
stopping (may take >6 months), decreased bone mineral density, depression, weight gain
- Practice points: delayed return of fertility
- Dose: 10mg tds (endometriosis); 5-10mg d for 10-14 days of cycle (dysfunctional bleeding)
- Dose: 150mg IM every 3 months. Give first dose within 5 days after start of menstrual cycle. Delay
until 21 days after delivery if not breastfeeding and until 6 weeks if breastfeeding. Contraceptive
effect immediate if injected within first 5 days of cycle. It has a delayed return of fertility up to one
year.

 NORETHISTERONE – Micronor, Noriday-28, Locilan-28; Primolut N


- Indication: delay menstruation, HRT, endometriosis, uterine bleeding.
- Dose:
Contraception: 350mcg d start first day of cycle;
Delay of menstruation: 5mg tds for up to 14 days starting 3-5 days before expected menstruation
(bleeding starts 2-3 days after stopping tablets);
Dysfunctional uterine bleeding: 5mg tds for 10 days to stop bleeding OR 5mg d-bd for days 16-25 of
cycle.
Endometriosis: 5-10mg daily; continue treatment for at least 4-6 months.
HRT: 1.25mg d for 10-14 days of each month with continuous estrogen.

IUD
 COPPER IUD – Multiload IUD
- SE: period pain, increased menstrual flow with possible menorrhagia, expulsion of device
(particularly in the first year)
- Replace every 5 years
- The copper IUD can be used as an emergency contraceptive (not the Mirena IUD).

Copyright © The Medicine Box 2012


AMH Summary: Chapter 17 – Obstetric and Gynaecological 5

VAGINAL RING
 ETONOGESTREL with ETHINYLOESTRADIOL – NuvaRing
- Side Effects: vaginitis, vaginal discharge, irregular bleeding, headache, nausea, weight gain, breast
tenderness, mood changes, device-related problems (eg foreign body sensation, expulsion of ring)
- Insert ring into vagina during first 5 days of cycle and leave for 3 weeks; remove for a 1 week break,
then insert a new ring. Periods should start 2-3 days after ring is removed, insert a new one 1 week
after regardless of period or not.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 6

- MENOPAUSE: HRT -
Indications: Short term relief of menopausal symptoms eg. hot flushes, night sweats (up to 5 years)
Oestrogen relieves symptoms (hot flushes, night sweats, urogenital atrophy). Progestogen reduces risk of
endometrial cancer associated with unopposed oestrogen.

Contraindications: thromboembolism, uterine bleeding, severe liver disease, breast cancer, coronary artery
disease

Side Effects: breast enlargement and tenderness, abnormal mammogram, headache, depression, change in
libido, weight change, irregular or breakthrough bleeding, spotting, endometrial hyperplasia (oestrogen-only
HRT), leg cramps, dry eye syndrome (oestrogen-only HRT)

Types of Treatment
- Oestrogen-only HRT: for women post-hysterectomy with no history of endometriosis.
- Vaginal oestrogen: first choice for urogenital symptoms. Stop treatment annually to see if its still
required.
- Combined HRT: for women with intact uterus, use combined HRT as oestrogen-only HRT increases
risk of endometrial cancer. But combined HRT has increased risk of breast cancer.

Practice Points
- tell doctor if there’s blood clots (swollen leg, difficulty breathing, chest pain), breast changes,
changes in vaginal bleeding
- use HRT at lowest effective dose for the shortest time possible. (2-3 years is sufficient in most
women)
- Review at least annually.
- Choose vaginal preparations for women who only have urogenital symptoms

Oestrogens
 CONJUGATED EQUINE OESTROGENS – Premarin, Premia Continuous
 OESTRADIOL – Estrofem, Progynova, Aerodiol spray, Vagifem pessary, Sandrena gel, Climara patches,
Femtran patches, Menorest patches, Trisequens tab, Estalis patches
 OESTRIOL – Ovestin tab, pessaries, cream
- Indications: menopausal symptoms, adjunct to vaginal surgery
 PIPERAZINE OESTRONE SULFATE – Ogen

Oestrogen/progestogen
 TIBOLONE – Livial
- Do not start tibolone until at least 12 months after last period to avoid increased irregular bleeding.

Side Effects: abdominal pain, bloating, weight increase, vaginal bleeding or spotting, vaginal discharge and
itching, vaginitis, breast pain, hypertrichosis

Dosage: 2.5mg daily

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 7

Progestogens
 MEDROXYPROGESTERONE – Provera, Depo-Provera etc
Indications: contraception (IM depot); uterine bleeding (oral); secondary amenorrhoea (oral); endometriosis

Precautions:
Adolescents—reduction in BMD with IM depot (during the period when peak bone mass is usually attained)
may be more significant than in adults; only use if other contraceptive methods are considered unsuitable or
unacceptable.

Side Effects: IM, 50% become amenorrhoeic within 12 months, delayed return of menstrual periods after
stopping (may take >6 months), loss of BMD, weight gain

Dosage:
Contraception: IM 150mg very 12 week. Protection immediate if given within 5 days after start of
menstrual cycle. Delay until 21 days after delivey if not breastfeeding or until 6 weeks if
breastfeeding.
Endometriosis: IM 50mg each week, or 100mg every 2 weeks for months; oral 10mg tds
Dysfunctional uterine bleeding: 5-10mg d for 10-14 dys during assumed second half of cycle.
Secondary amenorrhoea: 5-10mg d for 5-10 days during assumed second half of cycle.
HRT: 5-10mg d for 10-14 days of each month with continuous oestrogen, or 1.25-5mg d with
continuous oestrogen.

- delayed return of fertility (1 year)


- the repeat injection can be given up to 2 weeks early or late without the need for additional
contraceptive protection

 NORETHISTERONE – Micronor, Noriday, Locilan, Primolut N


Indication: contraception; HRT as adjunct to oestrogen; endometriosis; delay of menstruation; dysfunction
uterine bleeding

Dosage:
Contraception: 350mcg d beginning first day of menstruation
Delay of menstruation: 5mg bd-tds for up to 14 days, start 3-5 days before expected menstruation.
Dysfunctional uterine bleeding: to stop bleeding – 5mg tds for 10 days. To regulate bleeding – 5mg
d-bd for days 16-25 of cycle.
Endometriosis: 5-10mg d; continue treatment for at least 4-6 months.
HRT: 1.25mg d for 10-14 days of each month with continuous oestrogen.

Practice Points:
- There are no inactive pills so must be taken continuously.
- If forget to take a pill, take it as soon as you remember. If more than 3 hours, you are not protected.
Resume normal pill taking, but use additional contraceptive methods for the next 48 hours.
Emergency pill should be used if unprotected intercourse has occurred.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 8

- Less effective than the COC.


- Effective if started on first day of period; but use additional methods for 48 hours if started any other
time.

- DYSFUNCTIONAL UTERINE BLEEDING –

NSAIDs & Tranexamic acid


- can be used together
- NSAIDs started at onset of bleeding and taken regularly for 3-5 days. Tranexamic acid (Cyklokapron) is
used for 3-5 days during periods.
- dosage: 1-1.5g tds for 3-5 days.

COCs

Progestogens
- Levonorgestrel IUD (Mirena) is effective long term. It may be taken for 6 months before full benefit is seen.
Side effects include spotting and breast tenderness and may take 3-6 months to settle.
- Depot medroxyprogesterone (Depo-Provera): use in amenorrhoea is limited.

Danazol (Azol)
- poorly tolerated due to androgenic side effects. Must be used with effective non-hormonal contraception.

GnRH Agonists
- poorly tolerated due to hypo-oestrogenic side effects and can be costly. Must be used with effective non-
hormonal contraception

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 9

- ENDOMETRIOSIS –
Endometriosis is the presence of endometrial tissue outside the uterus. Patients may be asymptomatic or
have pelvic pain, menstrual changes, bowel symptoms or infertility.

NSAIDs
NSAIDs may be adequate for symptom relief in some women and can be used with other treatments. They
are effective in relieving dysmenorrhoea, however, evidence is inconclusive regarding their effect on pain
due to endometriosis.

Combined oral contraceptives


Combined oral contraceptives can be taken long term and are usually well tolerated. Both cyclical and
continuous regimens are used but there is no evidence that one regimen is more effective than the other.
However, 'tricycling' (having a pill-free interval once every 3 months) may be useful in women with
dysmenorrhoea.

Progestogens
Norethisterone, dydrogesterone and IM or oral medroxyprogesterone can all be used long term. Adverse
effects include irregular bleeding and weight gain. Continuous oral progestogens and IM
medroxyprogesterone also provide contraception if no doses are missed.

Limited evidence suggests the levonorgestrel IUD may also be effective in reducing pain associated with
endometriosis.

Danazol, gestrinone
Danazol and gestrinone both have androgenic adverse effects that limit their use: duration of treatment is 6–
9 months with danazol and 6 months with gestrinone. An effective non-hormonal method of contraception
must be used during treatment.

Gonadotrophin-releasing hormone agonists


The GnRH agonists, goserelin (Zoladex) and nafarelin (Synarel spray), are associated with hypo-
oestrogenic adverse effects such as hot flushes, vaginal dryness and decreased BMD. Duration of
treatment is limited to 6 months due to loss of BMD. Adding combined HRT allows treatment for up to
2 years (reduces these adverse effects and protects against BMD loss while maintaining efficacy). An
effective non-hormonal method of contraception must be used during treatment (to avoid pregnancy in the
event of missed doses).

GOSERELIN: 3.6mg implant every 4 weeks(up to 6 months for endometriosis)

NAFARELIN: 200mcg bd for 6 months (1 spray in one nostril in the morning and 1 spray in the other nostril
at night); may be increased up to 400mcg bd.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 10

- DELAY LABOUR –
Delay delivery for 24-48 hours

 NIFEDIPINE - Adalat
- relaxes uterine smooth muscle
Indication: preterm labour (<34 weeks gestation)

Dosage: initially 20mg. repeat after 30min if uterine contractions persist. If contractions continue after 3
hours, give 20mg every 3-8 hours until contractions cease. Maximum 160mg/day. Maintenance after 72
hours if necessary, give daily dose until 34 weeks gestation.

 SALBUTAMOL – Ventolin inj


- note oral nifedipine is preferred

Side Effects: maternal tachycardia, hypokalaemia, hyperglycaemia, exacerbation of diabetes, dyspnoea,


palpitations, anxiety, oliguria; fetal tachycardia

Dosage: IV 100-250mcg

- PRE-ECLAMPSIA & ECLAMPSIA –


Pre-eclampsia (hypertension with proteinuria or other disorders of the liver, kidneys, clotting system, brain,
placenta usually developing 20 weeks gestation). Eclampsia (pre-eclampsia with 1 or more seizures) is a
serious complication can result in poor intrauterine growth and early delivery.

Treatment: consider delivery of baby depending on gestational age and condition. Magnesium sulfate is the
drug of choice to prevent seizures in women with pre-eclampsia.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 11

- LABOUR -
- Ripen cervix and induce labour: Prostaglandins (mainly dinoprostone PGE2 gel)
- induction of uterine contraction: oxytocin, ergometrine, prostaglandins
- post partum haemorrhage: oxytocin, ergometrine, prostaglandins
- delivery of placenta: oxytocin, misoprostol

OXYTOCIC DRUGS
 CARBETOCIN – Duratocin inj
Indication: prevents postpartum haemorrhage (PPH)
Side Effects: nausea, vomiting, abdominal pain, itch, flushing, feeling of warmth, sweating, dizziness,
hypotension

- has longer duration of action than oxytocin


- give by slow IV injection over 1 minute.

 ERGOMETRINE inj
Indication: PPH; third stage labour (in combination with oxytocin) – not appropriate for labour induction.
Side Effects: nausea and vomiting
Dosage: 200mcg IM following delivery of placenta for prevention; or IV 25-50mcg every 2-3 minutes for
treatment.

 OXYTOCIN – Syntocinon inj


Indication: induction of labour; prevents and treats PPH (in combination with ergometrine)
Side Effects: nausea and vomiting

- note: combination with ergometrine may increase likelihood of side effects and has little advantage
over oxytocin alone.

PROSTAGLANDINS
Side Effects: nausea, vomiting, diarrhoea, back pain, transient hypertension or hypotension,
bronchoconstriction, headache, epigastric pain, vasovagal symptoms, blurred vision, facial flush, fever,
altered fetal heart rate, uterine hypercontractility and hypertonus

Prostaglandin E1 analogue
 GEMEPROST - Cervagem
Indication: Termination of pregnancy in second trimester
Side Effects: vaginal bleeding and uterine pain in the interval between pessary insertion and surgical
intervention (severity increases if interval is >3 hours)
Dosage: insert 1 pessary every 3 hours until effect. Maximum 5 pessaries in 24 hours.

 MISOPROSTOL – Cytotec
Indication: termination of second trimester; medical management of miscarriage; intrauterine fetal death

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 12

Dosage: 400mcg sublingual every 3 hours up to maximum 3 doses.

Prostaglandin E2
 DINOPROSTONE – Prostin E2 Vaginal Gel; Cervidil pessary
Indication: induction of labour
Dosage: 1-2mg of vaginal gel q6h; insert one pessary and remove when contractions begin.

Prostaglandin F2 alpha
 DINOPROST – Prostin F2 alpha inj
Indications: rarely used in termination; severe PPH refractory to other measures.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 13

- LACTATION –
Lactation Suppression
Dopamine agonists: cabergoline & bromocriptine
 CABERGOLINE – Cabaser, Dostinex
- preferred over bromocriptine due to fewer side effects
Dosage: 0.5mg each week in 1-2 doses

 BROMOCRIPTINE – Kripton, Parlodel


Side Effects: erythromelalgia, leg cramps
Dosage: 1.25mg bd-tds

Lactation Stimulation
Dopamine antagonists: metoclopramide & domperidone

 METOCLOPRAMIDE – Maxolon, Pramin


Side Effects: restlessness, drowsiness, dizziness, headache
Dosage: 10mg tds, taper dose over 7-10 days before stopping

 DOMPERIDONE – Motilium
Side Effects: dry mouth, headache
Dosage: 10mg tds, taper dose over 7-10 days before stopping.

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 14

- VAGINAL INFECTIONS –
THRUSH
For acute episodes use clotrimazole, miconazole or nystatin. Single doses are usually effective for first or
infrequent episodes. They may damage contraceptive diaphragms and latex condoms.
Oral antifungals (fluconazole) is effective for acute episodes and should be considered if creams have failed.
Antifungal prophylaxis with weekly oral fluconazole for up to 6 months is indicated in women with recurrent
thrush (4+ episodes in 12 months) or severe symptoms.
Pregnancy – use vaginal antifungals for 1 week (vaginal applicators may be used with care). A single
150mg fluconazole appears safe and may be used if vaginal antifungals have failed.

BACTERIAL VAGINOSIS
Symptoms: vaginal discharge without soreness, itching or irritation.
Treatment with oral metronidazole or clindamycin (vaginal/oral). Aci-Jel may be used to reduced symptoms
and prevent recurrence.

TRICHOMONIASIS
Women may have symptoms of vaginal discharge, itching and irritation and is sexually transmitted. Treat all
individuals with a single dose of metronidazole or tinidazole.

- PMS (Premenstrual Syndrome) –


Symptoms: mood or behavior changes, cognitive disturbances and physical problems during menstruation.
Symptoms may begin up to 14 days before and resolve within 3 days of, the beginning of a period.

TREATMENT
 Increase calcium intake to 1200-1500mg daily.
 Use 50-100mg daily of pyridoxine (vitamin B6)
 Monophasic COCs
 SSRIs (fluoxetine, sertraline)

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AMH Summary: Chapter 17 – Obstetric and Gynaecological 15

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be reproduced or
stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any responsibility for
any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 1

AMH SUMMARY: CHAPTER 18 – PSYCHOTROPICS


ANTIDEPRESSANTS

Drug choice Serotonin toxicity


• First line: TCAs, SSRIs, mirtazapine, moclobemide • Symptoms include hyperreflexia, clonus, tremor, incoordination, mental
• Second line: venlafaxine, desvenlafaxine, duloxetine state changes (confusion, agitation), shivering, sweating, diarrhoea
• Third line: other antidepressant agents and non-selective MAOIs
Drugs that may contribute to serotonin toxicity
Comparative information • Antidepressants
• Weight gain: TCAs, mirtazapine • Opioids (tramadol, pethidine, dextromethorphan)
• Sedation: TCAs, mirtazapine, mianserin • Stimulants (phentermine)
• Need for adjunctive drugs: less likely initially with TCAs, mirtazapine, • Illicit drugs (LSD, amphetamines)
mianserin • Others (selegiline, tryptophan, lithium, linezolid)
• Toxicity: TCAs, MAOIs and venlafaxine are more toxic in overdose
Special cases
Treatment regimens • Pregnancy: may consider TCAs, SSRIs (except paroxetine)
• Improvements seen within 1-3 weeks • Elderly: lower starting dose, more gradual increases
• Full antidepressant effects may take 6-8 weeks
• Continue treatment for 4-12 months after episode of major depression Other treatments
• Withdraw antidepressant over at least 1-2 weeks • Psychotherapy, ECT, St John’s wort
• Consider augmentation with lithium if maximum antidepressant dose
only produces a partial response

Antidepressant changeover guide


• > 10-14 days for fluoxetine, phenelzine, tranylcypromine
• 2-4 days for TCAs, SSRIs (except fluoxetine), mianserin, mirtazapine
• 1-2 days for duloxetine, venlafaxine, desvenlafaxine, moclobemide,
reboxetine
• If switching from fluoxetine to MAO, must wait for 5 weeks

Some antidepressant withdrawal effects


• TCAs: cholinergic rebound (opposite to anticholinergic effects)
• SSRIs, venlafaxine: dizziness, nausea, paraesthesia, anxiety,
agitation, tremor, sweating, confusion, electric shock-like sensations

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 2

Class Generic name Brand name Dose Side effects Precautions Other comments
MAOI Phenelzine Nardil 45-90mg d in 2-3 doses • Anticholinergic (dry • CVD, angina, cerebro- • Best to take last dose before
mouth, constipation) vascular disease 3pm, otherwise may have
Tranylcypromine Parnate 20-40mg d in 2-3 doses • Weight gain • Epilepsy, threshold trouble sleeping
• Headache, drowsiness, • Bipolar, may provoke • Avoid food containing tyramine
fatigue manic episode (cheese, salami, vegemite, tofu)
• Orthostatic hypotension • Treatment with drugs • L1, L16 *
• Sleep disturbance (mainly that cause serotonin • Tell your doctor if you have
insomnia) toxicity severe headaches, palpitations
• Hypertensive crisis • Pseudoephedrine is (hypotensive crisis)
(severe headache, BP, contraindicated • Tell your HCP if you take other
intracranial haemorrhage, OTC medications due to risk of
cardiac failure) interactions
• Interactions persist for 2-3
weeks after stopping treatment

SSRI Citalopram Cipramil 20mg d • Dry mouth • People at high risk of • Other indications:
Celapram • Weight gain bleeding - OCD
• Drowsiness, headache • Epilepsy, threshold - post-traumatic stress
Escitalopram Lexapro 10mg m • Agitation, tremor • Bipolar disorder, may disorder (paroxetine)
Esipram • Insomnia (less provoke manic episode - bulimia (fluoxetine)
anticholinergic effects) • Treatment with drugs - PMDD (fluoxetine, sertraline)
Fluoxetine Prozac 20mg m that may contribute to • L9, L12 *
Lovan serotonin toxicity • Fluvoxamine and paroxetine
may be taken in the evening.
Fluvoxamine Luvox 50mg d cc • Higher daily dose needed for
Movox OCD and bulimia compared to
depression and anxiety
Paroxetine Aropax 20mg d cc disorders
Extine • Fluoxetine has a long ½ life (up
to 16 days). When changing
Sertraline Zoloft 50mg m over from fluoxetine to another
Eleva antidepressant, wait for >10-14
days.
• When stopping SSRI treatment,
reduce daily dose by half on
weekly basis

* L1 stands for ancillary label 1, L9 stands for ancillary label 9, L12 stands for ancillary label 12, and L16 stands for ancillary label 16

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 3

Class Generic name Brand name Dose Side effects Precautions Other comments
TCA Amitriptyline Endep 25-75mg d max 300mg • Anticholinergic (dry • CVD – heart block, QT • Other indications:
mouth, blurred vision, interval prolongation, - nocturnal enuresis, urge
Clomipramine Anafranil 25-75mg d max 300mg decreased lacrimation, coronary heart disease incontinence
constipation, urinary • Orthostatic hypotension (amitriptyline, imipramine,
Dothiepin Prothiaden 25-75mg d max 300mg retention) • Hyperthyroidism nortriptyline)
Dothep • Weight gain • Closed angle glaucoma - adjunct in pain
• Tachycardia, orthostatic • Epilepsy, threshold management
Doxepin Sinequan 25-75mg d max 300mg hypotension • Bipolar, may provoke (amitriptyline)
rd
Deptran • Sedation manic episode - ADHD (3 line treatment)
• Treatment with drugs that (imipramine)
Imipramine Tofranil 25-75mg d max 300mg contribute to serotonin - migraine prophylaxis
toxicity (amitriptyline)
Nortriptyline Allegron 25-75mg d max 150mg • L1, L9, L16 *
• May take medication at night
Trimipramine Surmontil 25-75mg d max 300mg to avoid daytime drowsiness
• Toxicity with overdose.
Dothiepin is more toxic in
overdose than other TCAs.
• Nortriptyline causes the least
sedation, anticholinergic SEs
and orthostatic hypotension
of all the TCAs.
• Check BP pre-treatment,
post-treatment and after dose
changes

Other Velanfaxine Efexor-XR 75mg d cc • BP, dizziness, • HT • L9, L12 *


(serotonin and NAd headache, palpitations • Epilepsy • Monitor BP
reuptake inhibitor) • Bipolar
• Closed angle glaucoma
Desvenlafaxine Pristiq 50mg d • Treatment with drugs that
(serotonin and NAd may contribute to
reuptake inhibitor) serotonin toxicity

* L1 stands for ancillary label 1, L9 stands for ancillary label 9, L12 stands for ancillary label 12, and L16 stands for ancillary label 16

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 4

Class Generic name Brand name Dose Side effects Precautions Other comments
Other Duloxetine Cymbalta 60mg d cc • Anticholinergic (dry • Epilepsy, threshold •L9, L12 *
(serotonin and NAd mouth, constipation) • Bipolar, may provoke manic
reuptake inhibitor) • Decreased appetite episode
• Sweating, tremor • Treatment with drugs that
contribute to serotonin toxicity

Mirtazapine Avanza 30-45mg n max • Weight gain • Epilepsy, threshold • L1, L9, L16 *
(postsynaptic blockade of Mirtazon 60mg • Sedation • Bipolar, may provoke manic
5HT2 and 5HT3, • Peripheral oedema episode
presynaptic blockade of • Treatment with drugs that
central 2-adrenergic contribute to serotonin toxicity
inhibitory autoreceptors)

Agomelatine Valdoxan 25 mg d • Dizziness, headache, • Hepatic impairment • Monitor LFT


(melatonin agonist, fatigue, LFTs (contraindicated)
5HT2C antagonist) • Mania, other psychiatric
disorders
• Ciprofloxacin, fluvoxamine
(contraindicated)

Moclobemide (MAO-A Aurorix 450-600mg d in 1-2 • Anticholinergic (dry • Bipolar, may provoke manic • L12 *
selective inhibitor) doses, max 600mg d mouth, constipation) episode
(with food, no later • Headache, dizziness • Treatment with drugs that may
than the afternoon) • Anxiety, insomnia contribute to serotonin toxicity

Mianserin Tolvon 30-60mg n • Dry mouth • Epilepsy, threshold • L1, L9, L16 *
(tetracyclic Lumin max 120mg • Sedation, dizziness • Bipolar, may provoke manic • Perform full blood
antidepressant) • Blood dyscrasia episode examination and
• Disturbances of liver baseline hepatic
function (jaundice) function tests

Reboxetine Edronax 4mg bd max 12mg d • Anticholingeric (dry • HT • L9, L16 *


(NAd reuptake inhibitor) mouth, constipation, • Hyperthyroidism • Monitor baseline BP
urinary retention) • Closed angle glaucoma and HR
• Headache • Bipolar
• Insomnia • Epilepsy
• BP

* L1 stands for ancillary label 1, L9 stands for ancillary label 9, L12 stands for ancillary label 12, and L16 stands for ancillary label 16

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 5

ANTIPSYCHOTICS

Generic name Brand name Dose Side effects Precautions Other comments
Amisulpride Solian 50-300mg d All • Parkinson’s All
• Sedation • Epilepsy • L1, L9, L16 *
Aripiprazole Abilify 10-15mg d • Anxiety, agitation • Respiratory failure • Avoid using illicit drugs
• Anticholinergic (dry • Hyperthyroidism • A benzodiazepine may be added if necessary
Asenapine Saphris (wafer) 10mg d mouth, blurred vision, • Risk factors for • Withdraw antipsychotics slowly to prevent rapid
constipation, nausea, prolonged QT relapse and withdrawal symptoms
Chlorpromazine Largactil 25-50mg tds urinary retention) interval • Prophylactic treatment is usually continued for 1-2
• EPSE (parkinsonism, • Previous blood years after first psychotic episode to avoid relapse
Droperidol Droleptan inj dystonia, akathisia, dyscrasias • Monitor weight, BGL, lipids, blood count, LFTs
tardive dyskinesia, • Avoid use of >1 antipsychotic except when changing
Flupenthixol Fluanxol Depot inj neuroleptic malignant from one drug to another
syndrome) • Do not initiate antipsychotic therapy using a depot
Fluphenazine Modecate inj • Metabolic effects formulation (titration is impossible)
( blood glucose,
Haloperidol Serenace 1-5mg 2-3 times d lipids, weight gain) Chlorpromazine
• L8 *
Olanzapine Zyprexa 20mg d Drug-specific • Highly irritant. Do not crush tablets due to risk of
• QT prolongation for oral mucosal irritation. Avoid giving IM or SC due to
Paliperidone Invega 3-12mg d haloperidol, risk of necrosis. Oral hygiene is important with
amisulpride, regular use of oral liquid.
Pericyazine Neulactil 15-30mg d pimozide, droperidol
and ziprasidone Olanzapine
• Response should be seen within 1-2 weeks
Pimozide Orap (SAS) 2-12mg d • Photosensitivity for
• Tell your doctor if you stop smoking as this may
chlorpromazine
Quetiapine Seroquel 400-800mg d affect your dose
• Check glucose tolerance if weight gain occurs
• Use wafer if swallowing difficulties exist
Risperidone Risperdal 4-6mg d
Risperidone
Sertindole Serdolect 12-20mg d • Response occurs in 1-2 weeks
• Use quicklet for those who have difficulty swallowing
Thiothixene (SAS) 10-30 mg d
Other
Trifluperazine Stelazine 2-15mg bd • Haloperidol: Often used for elderly due to low
incidence of hypotension and anticholinergic effects
Ziprasidone Zeldox 20mg bd cc (but high incidence of EPSE)
• Paliperidone: Swallow whole. Do not cut or crush.
Zuclopenthixol Clopixol 10-50mg d • Pimozide: Monitor ECG first

* L1 stands for ancillary label 1, L8 stands for ancillary label 8, L9 stands for ancillary label 9, and L16 stands for ancillary label 16

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 6

Generic name Brand name Dose Side effects Precautions Other comments
Clozapine Clopine 200-600mg d • Headache, • As for other • L1, L9, L12, L16 *
drowsiness antipsychotics • Tell your doctor if you vary your caffeine intake or
• Orthostatic • Severe cardiac stop smoking as this may affect your dose
hypotension disease, circulatory • Blood tests required every week for the first 18
• Weight gain collapse, CNS weeks, then monthly; start only if white cell count
• Anticholinergic depression and absolute neutrophil count are normal
(constipation, urinary (contraindicated) • If seizures occur, reduce dose and consider using
retention) valproate (not carbamazepine)
• Tachycardia • If switching from another antipsychotic, decrease
• Neutropenia, the antipsychotic dose over 1 week and stop for 24
agranulocytosis hours before starting clozapine
• If treatment is restarted after >2 days, start at
12.5mg d
• Withdraw over 1-2 weeks
• Monitoring serum clozapine concentrations may aid
determination of suitable dose
• National distribution system for clozapine requires
registration of GPs, pharmacists, patients

* L1 stands for ancillary label 1, L9 stands for ancillary label 9, L12 stands for ancillary label 12, and L16 stands for ancillary label 16

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 7

DRUGS FOR BIPOLAR DISORDER

Drug choice
• Lithium, valproate, carbamazepine, antipsychotics (conventional), ECT D. Maintenance:
• Lithium, valproate, carbamazepine, or antipsychotics (eg.
Treatment regimens olanzapine)
• Continue maintenance treatment for 6-12 months after first episode
A. Acute mania or mixed episode of acute mania due to risk of relapse
• Severe: (Lithium/valproate) ± antipsychotic ± benzodiazepine • Maintain prophylaxis if needed
• Less severe: lithium/valproate
• Lithium onset of action may be delayed for 6-10 days
Practice points
B. Rapid cycling • All antidepressants may provoke mania or rapid cycling pattern
• Treat factors contributing to cycling (eg. hypothyroidism, drug or • Medication which may induce mania include corticosteroids, ACEIs,
alcohol misuse) dopaminergic agents (levodopa, bromocriptine)
• Lithium/valproate • When using valproate or carbamazepine, monitor electrolytes, liver
function and blood picture
C. Depressive episodes
• Lithium ± (antidepressant/valproate/carbamazepine)
• Antidepressant monotherapy is not recommended

Generic name Brand name Dose Side effects Precautions Other comments
Lithium Lithicarb Acute mania: • Metallic taste • Acute • Take with food. Avoid taking with hot drink.
Quilonum 750-1000mg d • Weight gain hyponatraemia, • Maintain normal salt & fluid intake
in divided doses • Fatigue, headache incl dehydration • Avoid sodium bicarbonate (Salvital, Ural, Citralite,
(max 2500mg) • Leucocytosis • Renal impairment Citravescent), effectiveness of lithium
• Psoriasis • Do not cease abruptly
Prophylaxis: • Treatment with drugs • Regular blood tests are important during treatment
250-1000mg in that contribute to • Monitor renal and thyroid function at baseline, then
divided doses for 2 serotonin toxicity every 3-6 months
wks, then adjust • For patients with CVD, obtain an ECG at baseline
dose based on and at follow-up
serum conc • Watch out for symptoms of lithium toxicity (extreme
thirst, frequent urination, nauseas and vomiting)
• Antidepressants may be used with lithium during
depressive episode of bipolar illness

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AMH Summary: Chapter 18 – Psychotropics 8

ANXIOLYTICS AND HYPNOTICS

Class Generic name Brand name Dose Side effects Precautions Other comments
Alprazolam Xanax 0.5-4mg d • Drowsiness • Respiratory • L1*
• Oversedation depression, • Recommended for short term
Bromazepam Lexotan 3-6mg tds max 60mg • Memory loss myasthenia gravis use due to development of
Anxiety

• Slurred speech (contraindicated) tolerance and dependence


Diazepam Valium 1-10mg d max 30mg • Triazolam: L18 *
• Rapid onset of action for:
Lorazepam Ativan 1-10mg d midazolam, triazolam,
alprazolam, temazepam,
Clobazam Frisium 10-30mg d max 80mg diazepam, flunitrazepam
Benzodiazepines
Both

• Diazepam has a rapid onset


Oxazepam Serepax 15mg n of action and a long half-life
so it is less likely to cause
Flunitrazepam Hypnodorm 0.5-2mg n withdrawal symptoms
Insomnia

Nitrazepam Alodorm 5-10mg n

Temazepam Normison 5-20mg n

Trizolam Halcion 0.125-0.5mg n


Buspirone Buspar 20-30mg in 2-3 divided • Dizziness, headache • Treatment with drugs • L1 *
(partial 5HT1A agonist doses, max 60mg daily that contribute to • L18*. Avoid grapefruit as it
for anxiety) serotonin toxicity may risk of side effects

Diphenhydramine Unisom 50mg nocte • Daytime sedation • Hyperthyroidism (may • L1 *


(sedating antihistamine) be worsened by
anticholinergic SEs)
Other

Doxylamine Restavit 25-30mg nocte • Daytime sedation • Hyperthyroidism • L1 *


(sedating antihistamine)

Zolpidem Stilnox 5-12.5mg nocte • Diarrhoea • Pulmonary • L1, L2 *


(potentiation of GABA) insufficiency
(contraindicated)
Zolpiclone Imovane 7.5mg nocte • Taste disturbance • L1, L2 *
(potentiation of GABA) • Dry mouth

* L1 stands for ancillary label 1, L2 stands for ancillary label 2, and L18 stands for ancillary label 18

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 9

Class Generic name Brand name Dose Side effects Precautions Other comments
Other Melatonin Circadin 2mg 1-2 hrs before bed • Asthenia • Autoimmune disease •L1 *
• Drowsiness • Renal, hepatic
• Backpain, arthralgia impairment

* L1 stands for ancillary label 1

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 10

DRUGS FOR ADHD

Drug choice
• Psychostimulants (methylphenidate and dexamphetamine)
• Atomoxetine
• TCAs
• Clonidine (evidence inconclusive)

Generic name Brand name Dose Side effects Precautions Other comments
Atomoxetine Strattera • Max 1.4mg/kg or 100mg • Dyspepsia • HT, tachycardia, •L1 *
(selective presynaptic daily, whichever is less • Dry mouth cerebrovascular disease •Contact your doctor if you
NAd reuptake inhibitor) • BP, irritability • Seizures notice unusual tiredness,
• Loss of appetite • Treatment with MAOI loss of appetite, yellowing
within 14 days of skin or eyes, dark
urine, pale faeces

Dexamphetamine Dexamphetamine • Max 30mg daily • Dry mouth • CVD • Also used for narcolepsy
(dopamine and NAd • Avoid doses later than • BP, anxiety, insomnia • Substance misuse • L12 *
agonist) the afternoon, otherwise • Loss of appetite • Active psychotic disorder
can cause insomnia

Methylphenidate Concerta • Max 40mg daily • Dry mouth • CVD • Also used for narcolepsy
(dopamine and NAd Ritalin LA • Avoid doses later then • BP, anxiety, insomnia • Substance misuse • L12 *
agonist) the afternoon, otherwise • Loss of appetite • Active psychotic disorder
can cause insomnia

* L1 stands for ancillary label 1 and L12 stands for ancillary label 12

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 11

DRUGS FOR ALCOHOL DEPENDENCE


Treatment of alcoholism
Considerations before treatment of alcoholism • Withdrawal symptoms: benzodiazepines (eg. diazepam), antipsychotics
• Vitamin deficiency, electrolyte imbalance, hypoglycaemia (eg. haloperidol), antiepileptics (eg. carbamazepine, phenytoin),
(give IV thiamine 100mg daily for at least 5 days) analgesics (eg. paracetamol), antiemetics (eg. metoclopramide)
• Withdrawal symptoms • Long-term treatment: acamprosate: disulfiram, naltrexone
• Concurrent drugs including benzodiazepines • For patients with severe liver disease, consider lorazepam and
• Alcohol-induced diseases oxazepam over diazepam

Generic name Brand name Dose Side effects Precautions Other comments
Acamprosate Campral 666mg tds • Diarrhoea • Renal impairment • Reduces craving for alcohol but does not alter CNS
(adults >60kg) • Rash effects of drinking alcohol or withdrawal symptoms
• Swallow tablets whole. Do not crush or chew.
• Should be commenced about 1 week after cessation of
drinking
• Preferred when opioids are used for pain

Disulfiram Antabuse Initially 100mg • Drowsiness • IHD, psychosis • Disulfiram has many potential adverse effects. Ensure
(aldehyde d for 1-2 wks, • Nausea (contraindicated) the patient is completely aware of the risks involved and
dehydrogenase then 200mg d, • Headache • Treatment with has not consumed alcohol in the previous 24 hours
inhibitor) max 300mg d • Potentially serious isoniazid or • Ensure someone is available to supervise daily
effects may occur metronidazole administration
if alcohol is • A reaction may be triggered after taking very small
consumed (intense amounts of alcohol or even if it is rubbed into the skin
flushing, sweating, • Do not take alcohol within 7 days of stopping disulfiram
palpitations, • Contact your doctor if you notice yellowing of whites of
dyspnoea, eyes, or dark urine
hyperventilation)

Naltrexone ReVia 50mg daily • Dizziness, nausea, • Hepatotoxicity (rare) Alcohol withdrawal
(opioid antagonist) headache • Contraindicated in • Reduces craving for alcohol but does not alter CNS
• Nausea, dizziness patients with acute effects of drinking alcohol or withdrawal symptoms
hepatitis, liver failure, • L1, L12 *
on opioid analgesics • Contact your doctor if you notice yellowing of whites of
eyes, or dark urine
• Monitor liver function (esp total bilirubin) before starting
treatment, then each month for the first 3 months
• After stopping naltrexone, the effects of opioids are
blocked for at least 3 days. Be careful of overdose.

* L1 stands for ancillary label 1 and L12 stands for ancillary label 12

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 12

DRUGS FOR NICOTINE DEPENDENCE

Withdrawal symptoms of smoking cessation: Cravings, anxiety, irritability, poor concentration, sleep disturbance, aggression, headaches, cramps

Generic name Brand name Dose Side effects Precautions Other comments
Buproprion Zyban SR Start with 150mg mane • Insomnia, nightmares • Epilepsy • Do not crush or chew tablets
(inhibition of for 3 days to minimise • Agitation, anxiety • Bipolar • You can continue smoking for up to a week after
dopamine and sleep disturbance, then • NRT you start this medicine because it takes time for the
NAd reuptake) 150mg bd for 7-9 wks medicine to become effective
• Don’t use nicotine products while taking this
medicine because it may increase your blood
pressure
• If possible, avoid alcohol when taking buproprion as
it may increase the risk of fits
• You may experience dizziness while on this
medicine
• Contact the doctor if you become agitated or
depressed.

Nicotine Nicabate Formulations available • N&V, indigestion • CVD Patches


Nicorette include gum, inhaler, • Vivid dreams (for • Dentures for gum • Apply to a dry, clean part of the chest, arm or thigh
QuitX lozenge, patch, 24-hour patches) • Asthma for inhaler • Use one patch a day (24 hours for Nicabate, 16
sublingual tablets. See • Skin disease for hours for Nicorette)
AMH for further details. patches • Patch slowly releases nicotine through skin into
• Oral inflammation body
Treatment should for gum, lozenge, • Dispose appropriately by folding together
continue for ~12wks. sublingual tablets • Important to rotate site of application to avoid skin
irritation
• Keep patch on while showering
• If patch falls off regularly, clean skin with alcohol
swab before application or try another brand
• If sleep disturbance occurs, use a 16 hour patch
• Consider a lower strength of the patch if you
experience nausea

Lozenges
•Dissolve lozenge in mouth
•Do not chew lozenges (otherwise ingestion of
nicotine can cause stomach upset)

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 13

Generic name Brand name Dose Side effects Precautions Other comments
Nicotine Gum
(cont.) • Nicotine absorbed through oral mucosa
• Chewing technique is important: Chew for 10 times
until you get a tingling sensation, park gum to side
of mouth until tingling goes away, chew again
• Important not to chew too quickly (otherwise more
saliva is created, nicotine is ingested into stomach
rather than absorbed through oral mucosa and
stomach upsets may occur)
• Most people chew ~10 tabs daily; no more than
once per hour
• Can cut if too bulky

Inhaler
• Mouthpiece like a cigarette holder
• Insert capsule which releases nicotine in gas form
• Align marks on mouthpiece and pull apart
• Take one cartridge from blister tray
• Press cartridge firmly into bottom of mouthpiece and
push the top and bottom firmly together to break the
top seal of the cartridge
• Twist to align marks
• Inhale when ready for up to 20 mins, 6-12 cartridges
daily

Sublingual tablet
•Place under tongue and allow to dissolve
•Do not chew or swallow

Varenicline Champix Initially, 0.5mg once • N&V • Psychiatric • You can continue smoking for up to a week after
daily for 3 days, then • Dyspepsia condition you start this medicine because it takes time for the
0.5mg bd for 4 days, • Dizziness • Use with NRT medicine to become effective
then 1mg bd for 11 • Contact your doctor if you are agitated, depressed
weeks. or have suicidal thoughts
• Don’t use nicotine products while on this medicine
because it can worsen side effects

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 14

DRUGS FOR OPIOID DEPENDENCE

Symptomatic treatment during withdrawal Opioid withdrawal management


• Analgesics eg. paracetamol/NSAID • Methadone (opioid agonist)
• Antiemetics eg. metoclopramide • Buprenorphine (partial opioid agonist)
• Antidiarrhoeal eg. loperamide • Naltrexone (opioid antagonist)
• Clonidine to reduce withdrawal symptoms e.g. HT, tachycardia
• Diazepam for anxiety, agitation

Generic name Brand name Dose Side effects Precautions Other comments
Buprenorphine Subutex See AMH. • Constipation • Respiratory disease • L1 *
(partial opioid agonist) • Hypotension • Ongoing alcohol, • Dissolve tablet under tongue
sedative or opioid use • Give the first dose of buprenorphine at least 6 hours
after last heroin use to avoid precipitation of
withdrawal symptoms
• Do not use concurrently with opioids, alcohol or
benzodiazepines to avoid risk of overdose

Methadone Methadone See AMH. • Constipation • Ongoing alcohol, • L1 *


(opioid agonist) Biodone Forte • Hypotension sedative or opioid use • It may take a few days for methadone to reach its full
effect. You may feel uncomfortable but do not take
opioids or other drugs to compensate.
• For pain relief requiring opioids, higher than standard
doses may be needed

Naltrexone ReVia See AMH. • Dizziness, • Hepatotoxicity (rare) • Patient should be opioid free for at least 7 days before
(opioid antagonist) nausea, • Contraindicated in starting naltrexone,
headache patients with acute • Treatment should be for at least 6 months
• Nausea, hepatitis, liver failure, • After stopping treatment, naltrexone continues to
dizziness on opioid analgesics block the effects of opioids for another 3 days. Do not
attempt to overcome the blockade by using higher
doses of heroin.
• Also used to treat alcohol dependence

Combination products Suboxone See AMH. • Constipation • Respiratory disease • L1 *. Dissolve tablet or film under tongue.
(buprenorphine and (sublingual tab • Hypotension • Ongoing alcohol, • Suboxone (buprenorphine + naloxone) is used to
naltrexone) and film have not sedative or opioid use discourage IV administration. Naloxone, when used
been shown to be • Hepatotoxicity (rare) sublingually, has little clinical effect, but if injected, will
bioequivalent) antagonise the effects of other opioids leading to
withdrawal symptoms.
* L1 stands for ancillary label 1

Copyright © The Medicine Box 2012


AMH Summary: Chapter 18 – Psychotropics 15

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2012

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box
team does not accept any responsibility for any loss which the user may suffer as a result of errors or
inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2012


AMH Summary: Chapter 19 – Respiratory 1

AMH SUMMARY: CHAPTER 19 – RESPIRATORY

- BRONCHODILATORS -

Beta2 agonists
Precautions: hypertension, IHD, heart failure, arrthymias, hyperthyroidism, diabetes
Side Effects: tremor, palpitations, headache, serious hypokalaemia (high doses of beta2 agonists)

Short acting beta2 agonists


Indications: acute asthma, symptom relief during maintenance of asthma and COPD, prevention of
exercise-induced asthma
- Rapid onset of action (5-15min); Short duration of action (3-6 hours)
Dosage: 1-2 qid prn

• SALBUTAMOL – Airomir, Asmol, Ventolin


• TERBUTALINE – Bricanyl

Long acting beta2 agonists


Indications: maintenance of asthma and COPD
- Long duration of action (>12 hours)
- Eformoterol has a quicker onset of action than salmeterol and is marketed for acute relief of
symptoms in adults with asthma already receiving inhaled corticosteroids and regular
eformoterol. The Symbicort combination is marketed for symptom relief in patients receiving
maintenance treatment.
Dosage: 1 bd

• EFORMOTEROL – Oxis Turbuhaler; Foradile; Symbicort (Eformoterol + Budesonide)


• SALMETEROL – Serevent; Seretide (Salmeterol + Fluticasone)
• INDACATEROL – Onbrez (1 daily)

Anticholingerics (inhaled)

Indications: maintenance COPD and severe asthma


Side Effects: dry mouth, throat irritation

• IPRATROPIUM – Atrovent, Ipratrin


Dosage: 3-4 times daily

• TIOTROPIUM – Spiriva
Dosage: 1 d

Copyright © The Medicine Box 2013


AMH Summary: Chapter 19 – Respiratory 2

Theophyllines

Indications: severe obstruction, maintenance in severe asthma and COPD


Interactions: many
Precautions: GORD, arrhythmia, heart failure, thyroid, epilepsy, smoking
Side Effects: nausea, vomiting, diarrhoea, gastro-oesophageal reflux, headache, insomnia,
irritability, anxiety, tremor, palpitations. Narrow therapeutic range.

• AMINOPHYLLINE injection
Dosage: do not give aminophylline if previously treated with theophylline. Reserve use in acute
severe asthma is unresponsive to combined treatment with inhaled short acting beta2 agonists,
inhaled ipratropium and systemic corticosteroids.

• THEOPHYLLINE – Nuelin
- Narrow TI
- Dosage: 1 d cc
- Concentration monitoring: Monitor plasma concentration at initiation of treatment, if drug
regimen is altered, if there is prolonged fever, if adverse effects suspected and if patient
stops or starts smoking.

- CORTICOSTEROIDS (INHALED) -

Indications: maintenance of persistent asthma, severe COPD


Side Effects: dysphonia, oropharyngeal candidiasis, bruising, facial skin irritation following
nebulisation
Systemic Adverse Effects (due to high doses or systemic absorption): adrenal suppression, bone
density loss, glaucoma/cataract, skin thinning and bruising, impaired growth
Counselling: rinse mouth with water, gargle and spit

• BECLOMETHASONE (inhaled) – Qvar


Dosage: 1 bd

• BUDESONIDE (inhaled) – Pulmicort


Dosage: 1 bd

• CICLESONIDE – Alvesco
Dosage: 1 d

• FLUTICASONE (inhaled) – Flixotide


Dosage: 1 bd

Copyright © The Medicine Box 2013


AMH Summary: Chapter 19 – Respiratory 3

- CROMONES -

Indications: maintenance persistent asthma, prevention of exercise-induced asthma


Mode of Action: inhibits release of inflammatory mediators from mast cells
Side Effects: cough, throat irritation, bitter taste, transient bronchospasm

• CROMOGLYCATE (inhaled) – Intal


Dosage: 2-4 times daily

• NEDOCROMIL – Tilade
Dosage: 1 qid
Side Effects: headache, nausea, vomiting, abdominal pain

- LEUKOTRIENE-RECEPTOR ANTAGONISTS -

Mode of Action: inhibits smooth muscle contraction caused by leukotrienes


Indications: maintenance treatment in asthma
Side Effects: headache, abdominal pain, diarrhoea

• MONTELUKAST – Singulair
- can be used in kids >2 years
- Dosage: 1 at bedtime

- IgE ANTIBODIES –
Mode of Action: reduces the immune system’s response to allergen exposure
Indications: treatment of moderate-to-severe allergic asthma in patients treated with inhaled
corticosteroids and with raised serum IgE levels
Side Effects: injection site reactions, rash, bleeding, increased risk of malignancies

• OMALIZUMAB – Xolair
- Dosage: Injection every 2-4 weeks
- Monitor for 2 hours after each dose

Copyright © The Medicine Box 2013


AMH Summary: Chapter 19 – Respiratory 4

- DRUGS FOR COUGH -

Cough suppressants
Contraindications: respiratory failure, asthma, COPD
Side Effects: drowsiness, constipation, nausea, vomiting. CNS adverse effects (drowsiness,
respiratory depression) are more likely with codeine. Dependence and withdrawal symptoms have
been described.

• CODEINE – Codeine Linctus, Actadone


Dosage: 3-4 times daily
• DEXTROMETHORPHAN – Bisolvon Dry, Benadryl
• DIHYDROCODEINE – Rikodeine
Dosage: 3-4 times daily
• PHOLCODINE – Tussinol, Durotuss
Dosage: 3-4 times daily

Mucolytics

• ACETYLCYSTEINE – Mucomyst
o Indication: adjunct treatment in respiratory disease with excessive mucus
o Dosage: inhale 3-5ml q6h. Dilute with equal volume of sodium chloride.

• BROMHEXINE – Bisolvon
o Dosage: 8-16mg tid

• DORNASE ALPHA – Pulmozyme


o Indication: prevention of respiratory complications in cystic fibrosis
o Side effects: voice alteration, pharyngitis, laryngitis, rash
o Note: regular administration required and highly costly.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 19 – Respiratory 5

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2011

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


AMH Summary: Chapter 20 – Vaccines 1

AMH SUMMARY
CHAPTER 20: VACCINES

A. VACCINES IN SCHEDULE

OVERVIEW
• Schedule usually begins at birth

Hepatitis B vaccine
• For children, begin at birth, then 3 doses at 2, 4 and 6/12 months of age

Diptheria, tetanus, pertussis


• 2 doses given. Start at 6 months at age then another at 4 years of age
• Adult formulation should be given at 15-17 years and then another at 50 years

H. influenzae B
• Doses occur at 6 months, 12 months for children. For the Hiberix brand, 4 doses are
required while Liquid Pedavax requires 3
• Vaccine should not be given before 6 weeks and not required after 5 years of age

Pneumoccal 7-valent vaccine


• Given at 2, 4, 6 months of age
• It can be given at 12 months if medically at risk

Polio vaccine
• Given at 2, 4, 6 months of age
• Also given at 4 years
• Booster doses not recommended unless individuals are at special risk

Rotavirus
• Given at 2 and 4 months
• Given at 6 months if it is the Rotateq brand

Measles, mumps, rubella


• Given at 12 months, 4 years (or at 18 months)
• Fever may develop when taking vaccine

Meningococcal C
• Given at 12 months

Varicella zoster vaccine


• Given at 18 months and may be given at 10-13 years

HPV vaccine
• Given to girls at 12-13 years
• Protects against HPV type 16 and 18, also types 6 and 11

Copyright © The Medicine Box 2009


AMH Summary: Chapter 20 – Vaccines 2

OTHER ISSUES WITH VACCINATION


• Catch up schedule should be done if missed schedule dose.
• Written evidence of vaccination is important
• For immunosuppressed agents, do not use live attenuated vaccines
• High risk occupations such as health professional staff and students should be vaccinated
against infections including Hepatits A, B, measles, mumps, rubella, influenza, varicella and
tuberculosis
• High risk occupations should also be up to date with diphtheria, tetanus, polio, measles,
mumps and rubella vaccinations

ADVERSE EFFECTS OF VACCINES


• Serious uncommon effects should be notified
• Common types of adverse effects include pain in injection site, swelling, transient fever

STORAGE
• Vaccines should be kept refrigerated in a cold chain system of transport and storing within
a safe temperature range.
• Freezing damages vaccines

B. OTHER VACCINES (NOT IN SCHEDULE)

BCG vaccine (tuberculosis)


• Generally not recommended as tuberculosis incidence is low in the general population

Cholera vaccine
• Used for travellers in high risk areas
• Avoid food and drink 1 hour before and after taking the vaccine

Japanese encephalitis vaccine


• Use for people in outer Torres Strait Islands or workers who work there for 30 days in
wet season
• Preventative measures should be adopted such as insect repellents as mosquitoes are
carriers of the disease

Rabies, Typhoid, Yellow fever vaccines


• Used for those people exposed to high risk areas of the disease

Q fever
• High risk groups include abattoir workers or individuals with high exposure to animals
such as cattle and sheep

Copyright © The Medicine Box 2009


AMH Summary: Chapter 20 – Vaccines 3

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2009

Copyright © The Medicine Box 2009

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not accept any
responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2009


Topic Summary: Gastrointestinal 1

TOPIC SUMMARY: GASTROINTESTINAL


DYSPEPSIA Non-pharmacological treatment
• Reduce alcohol intake
• Dyspepsia: PPIs are more effective than antacids or H2 antagonists • Stop smoking
• Functional dyspepsia: PPIs and H2 antagonists are equally effective • Avoid trigger foods (e.g. chocolate, caffeine, fatty or spicy foods)
but H2 antagonists are less expensive • Eat smaller meals
• Antacids prn • Do not eat for at least 2 hours before bed
• H.pylori eradication • Avoid tight clothing
• Raise bed head (if symptoms occur at bedtime)
• Weight loss in overweight patients
GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD)

GORD
• Drug choice: PPIs > H2 antagonists > antacids
• Full dose PPI for 4 weeks
• If inadequate response, double-dose PPI for 4 weeks, then step down
to lowest effective dose or stop treatment

Infant GORD
• Common but resolves with increasing age
• Symptoms may reduce with thickened oral fluids or modified feeding
patterns
• Specialists may prescribe H2 antagonists and PPIs

NSAID-related ulcer
• Replace NSAID with paracetamol and non-drug treatment.
• Treatment: PPI, H2 antagonist, or misoprostol
• Prevention: PPI, double dose H2 antagonist, misoprostol

H. Pylori-related ulcers
• See ‘Drugs for Gastrointestinal Infections’

Other practice points


• Drugs that may worsen reflux: NSAIDs, CCBs, nitrates

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 2

DRUGS FOR DYSPEPSIA AND GORD

Class Mode of action Generic name Brand name Dose Other comments
• Neutralise gastric acid Aluminium Alu-tab As directed • Aluminium hydroxide (Alu-tab): causes constipation
and provides hydroxide • Magnesium hydroxide, magnesium trisilicate: causes diarrhoea
symptomatic relief Titralac As directed • Sodium bicarbonate: avoid in hypertension, heart failure, renal
Calcium impairment, peripheral oedema
carbonate Mylanta As directed • Alginic acid: forms a raft over the surface of gastric contents and
limits exposure of stomach to gastric acid
Combination • Simethicone: acts as a surfactant to reduce ‘foaming’ and therefore
Antacids

antacids reflux

Other practice points:


• Liquid preparations are more effective than solid preparations
• Take 1-3 hrs after meals for optimal effect
• Tablets should be chewed or sucked before swallowing to maximise
effect
• Use antacids with caution in severe renal impairment

• Blocks histamine H2- Cimetidine Magicul 400mg bd • Cimetidine inhibits liver enzymes; decreases metabolism of warfarin,
H2 antagonists

receptors in gastric phenytoin, carbamazepine, metoprolol, theophylline; may also


mucosa, therefore inhibits Famotidine Pepcidine 20mg bd cause anti-androgenic effects (gynaecomastia, impotence). Avoid
gastric acid secretion cimetidine if possible.
Nizatidine Tazac 150-300mg bd

Ranitidine Zantac 300mg d

• Inhibits gastric enzyme Esomeprazole Nexium 20mg d • Esomeprazole has greater oral bioavailability than omeprazole (less
(proton pump) which is first-pass metabolism), but efficacy are the same.
responsible for acid Lansoprazole Zoton 30mg d
secretion. They have Other practice points
slower onset of action Omeprazole Losec 20mg d • Swallow whole; do not crush or chew.
than H2-receptor • Tablets may be dispersed in water and taken within 30 minutes.
PPIs

antagonists, but inhibition Pantoprazole Somac 40mg d Orally disintegrating tablets may be dispersed water or juice and
of acid secretion is taken immediately. Capsules may be opened and the contents
greater and longer. Rabeprazole Pariet 20mg d dispersed water or juice and taken immediately.
• Take 30 minutes to 1 hour before meals.
• Possible side effects include abdominal pain and headache.
• Tell your doctor if you notice coffee-coloured vomit or bloody stools.

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 3

Class Mode of action Generic name Brand name Dose Other comments
Cytoprotective agent Bismuth (SAS) 120mg qid for • Chew tablets before swallowing. Take on an empty stomach
subcitrate 10-14 days (bismuth is less effective if taken with food or milk).
• Bismuth toxicity can occur if it is taken for >2 months
• Possible side effects include blackening of faeces, darkening of
teeth and tongue
• Avoid in renal impairment (CrCl < 30 mL/min)
Other

Cytoprotective agent Sucralfate Carafate 1g bd • Tablets can be dispersed in water


(maintenance) • May cause constipation
• Avoid in renal impairment

Prostaglandin E1 analogue Misoprostol Cytotec 400mg bd • Take with meals to reduce the risk of diarrhoea
• Possible side effects include diarrhoea and abdominal pain
• Seek medical attention if you notice black stools or coffee-coloured
vomit

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 4

ANTI-SPASMODIC DRUGS

Generic name Brand name Indication Dose Side effects Other comments
Cisapride (SAS) Gastroparesis 15-40mg d in 2-4 doses • Diarrhoea •L18 *
15 minutes before meals • Abdominal cramps •Seek medical attention if you feel
• QT prolongation dizzy, vomit or have diarrhoea

Hyoscine butylbromide Buscopan IBS 10-20mg 3-4 times daily • Dry mouth, • Trial found no difference between
(smooth muscle relaxant, GI, renal, biliary spasm decreased sweating, hyoscine butylbromide and
reduces intestinal motility) blurred vision, paracetamol for relief of recurrent
urinary retention, abdominal cramps
constipation,
tachycardia
Mebeverine Colofac IBS 135mg tds cc • Dyspepsia
(smooth muscle relaxant,
reduces intestinal motility)

Peppermint oil Mintec IBS 1-2 tds 0.5hr ac • Heartburn • Do not break or chew capsules as
(smooth muscle relaxant, peppermint oil can irritate the oral
reduces intestinal motility) cavity and throat

* L18 stands for ancillary label 18

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 5

ANTI-EMETIC DRUGS

Causes of nausea and vomiting: Chemotherapy, radiotherapy (consider Pregnancy: Ginger (up to 1g daily), pyroxidine (up to 50mg bd),
prophylaxis using 5HT3 antagonist/dexamethasone), pregnancy, post-op, metoclopramide, prochlorperazine
motion sickness

Class Generic name Brand name Indication Dose Other comments


Metoclopramide Maxolon N&V 5-10mg 2-3 times d • Stimulates motility of upper GIT, increasing gastric emptying
Gastric stasis rate and reducing small intestinal transit time
Aid in GI radiology • Metoclopramide is safe in pregnancy (category A)
Simulation of lactation • L12 *
• Side effects: restlessness, dizziness, headache, tardive
dyskinesia (involuntary and repetitive movements)

Prochlorperazine Stemetil N&V 10mg tds L1 *


Dopamine antagonists


Vertigo • This medicine may increase the effect of alcohol.
• Side effects: postural hypotension, drowsiness

Domperidone Motilium Nausea and vomiting 10-20mg 3-4 times d • Domperidone does not readily cross the BBB therefore CNS
Gastroparesis effects are less likely to occur. All other dopamine antagonists
Stimulation of lactation have central dopamine antagonist activity and may cause
extrapyramidal side effects. Domperidone is the antiemetic of
choice in patients taking treatment for Parkinson’s disease.
• Side effects: abdominal cramps, dry mouth, galactorrhoea

Droperidol Droleptan Prevention of post-op Injection as directed • L1 *


N&V • The risk of sedation and EPSE limit its use

Haloperidol Serenace N & V associated with 1-2mg tds prn • L1, L16 *
chemotherapy • Due to increased risk of CNS effects, haloperidol is used to
treat post-chemo N&V only when other agents are ineffective

Dimenhydrinate Dramamine N & V due to motion 50-100mg 4-6 times d • L1 *


st
sickness, labyrinthitis, For motion sickness, take 1 dose 30 mins before travel.
Antihistamines


Meniere’s disease
Sedating

Pheniramine Avil Allergic conditions 22.65mg 2-3 times daily


Motion sickness
N&V
Vertigo due to Meniere’s

* L1 stands for ancillary label 1, L12 stands for ancillary label 12 and L16 stands for ancillary label 16

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 6

Class Generic name Brand name Indication Dose Other comments


Promethazine Phenergan N&V 25mg 4-6 times d
Antihistamines
Motion sickness
(cont.)

Dolasetron Anzemet Post-operative, See eMIMS or AMH for • More effective in preventing nausea and vomiting than
chemotherapy-induced, details. treating an existing case.
Granisetron Kytril radiotherapy-induced • Dolasetron, ganisetron, palonosetron and tropisetron are
5HT3 antagonists

N&V given once daily; ondansetron is given 2-3 times daily


Ondansetron Zofran • QT prolongation risk
• Side effects: headaches, constipation
Palonosetron Aloxi

Tropisetron Navoban Tropisetron counselling points


• C - Take medication at least one hour before food
• L1 * - This medicine may cause dizziness

Aprepitant Emend Used in combination with See eMIMS or AMH for • Decreases effectiveness of pill; use additional contraception
Substance P
antagonists

5HT3 antagonists and details. during the 3-day course and for 1 month after your last dose
Fosaprepitant Emend IV dexmethasone to prevent of aprepitant
N&V associated with
chemotherapy

Hyoscine Kwells Motion sickness 0.3mg every 4-6 hrs prn • Take the first dose 30 mins before travel
hydrobromide
Other

Dexamethasone Dexmethsone PONV 4-20mg 30 mins before • Take with food to avoid GI upset
chemo

* L1 stands for ancillary label 1

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 7

LAXATIVES

Lines of therapy • Children: (Liquid paraffin emulsion or lactulose) + stimulant (senna or


• Lifestyle and dietary measures ( fluid intake, fibre intake, exercise) bisacodyl)
• Bulking agent, osmotic laxative, stool softener, stimulant • Pregnancy: If dietary and lifestyle factors are inadequate, use bulking
agents. Other options include docusate, lactulose and sorbitol.
Special cases Polyethylene glycol may be used occasionally. Avoid stimulants.
• Opioid-induced: Use Coloxyl with Senna, lactulose (Actilax),
polyethylene glycol (Movicol); do not use bulking-agent; avoid high Other
fibre diet • Avoid suppositories and enemas if anal fissure are present
• Palliative care: Use Coloxyl with Senna

Class Mode of action Generic name Brand name Dose Side effects Other comments
Absorbs water in the Psyllium Metamucil As directed Flatulence and • Drink plenty of fluid throughout the
Bulking agents

colon to increase faecal Agiolax stomach rumble day


bulk, which stimulates Fybogel • Do not take immediately before going
motion. Must drink lots to bed
of fluid otherwise Sterculia Normafibe • Full effect may take several days
constipation may occur.
Use as prevention

Increases water content Glycerol Glycerol Supp 1 d prn Flatulence and • Glycerol suppositories can be used
in stools abdominal cramps, for rapid relief of constipation
Osmotic laxatives

Lactulose Actilax 15-30mL d diarrhoea, nausea, • Lactulose and sorbitol take several
anorexia, days to work and must be taken
Polyethylene glycol Movicol As directed electrolyte regularly to maintain their
imbalance effectiveness
Saline laxatives Picoprep As directed • Polyethylene glycol laxatives may
take several days to work and may
Sorbitol Sorbilax 20mL d contain electrolytes to minimise
electrolyte and water loss

Stimulates enteric Bisacodyl Bisalax 5-15mg n Abdominal colic, • May be used long term for
nervous system to cramps, constipation in people taking opioids,
Stimulants

increase motility Senna Senokot 7.5-30mg n hypokalaemia spinal damage and in chronic
neuromuscular disease
Sodium picosulfate Durolax SP Drops 5mg n • Insufficient evidence exists to confirm
chronic use of stimulant laxatives as
being harmful to the colon
• Onset of action is 6-12 hours (oral);
15-60mins (supp); 5-15 mins (enema)

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 8

Class Mode of action Generic name Brand name Dose Side effects Other comments
Surfactant properties Docusate Coloxyl 50-150mg d or bd Abdominal • Onset of action is 1-3 days with oral
that stimulant intestinal discomfort, colic, admin and 5-20 mins following rectal
secretions and increase Liquid paraffin Parachoc 40mL d diarrhoea admin
fluid penetration into • Drink plenty of fluid
Stool softeners

faeces to soften stool Poloxamer Coloxyl drops 10 drops tds • Liquid paraffin: Do not take a dose
(infant < 6 mths) immediately before lying down
(aspiration risk).
• May reduce absorption of fat-soluble
vitamins (A, D, E, K)
• Poloxamer is preferred in children < 3
years. Docusate is preferred in
children > 3 years old.

Peripherally acting Methyl naltrexone Relistor SC single dose Flatulence, • Onset of action is about 30 mins
competitive mu opioid diarrhoea
receptor antagonist,
blocks the constipating
effect of opioids in GIT
Other

5HT4 receptor agonist Prucalopride Resotrans 2mg d Nausea, abdominal • L16*


that increases GI pain, diarrhoea
motility.

* L16 stands for ancillary label 16

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 9

ANTIDIARRHOEALS

Drug choice Practice points


• Oral rehydration salts • Breastfeeding should be continued.
• Antidiarrhoeals: opioids (adults), bulking agents • Lactobacillus GG reduces duration of diarrhoea associated with
rotavirus enteritis
Special cases
• Diverticular disease: Use bulking agent. Add short term opioid
antidiarrhoeal if necessary.
• Bile acid-related diarrhoea: Cholestyramine is the treatment of
choice.
• Infections diarrhoea: May require anti-infective

Class Generic name Brand name Dose Other comments


Codeine Codeine phosphate 30-60mg 3-4 times daily, max 240mg • Loperamide is least likely to produce CNS effects at usual
antidiarrhoeals

dosage
Diphenoxylate Lomotil 5mg 3-4 times daily, max 20mg • Both codeine and diphenoxylate cause drowsiness
Opioid

• Avoid long term use of codeine due to potential addiction


Loperamide Immodium 4mg stat, then 2mg after every loose (unless specialist states otherwise)
stool, max 16mg • Atropine is added to diphenoxylate to discourage misuse
• Avoid use in children

Oral rehydration salts Gastrolyte As directed


Other

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 10

INFLAMMATORY BOWEL DISEASES Aminosalicylates


• All 5-aminosalicylates are contraindicated in people allergic to
Ulcerative colitis: inflammation of the inner lining of the colon and rectum salicylates; sulfazsalazine is contraindicated in those allergic to
sulfonamides
Crohn’s disease: inflammation of the full thickness of the bowel wall and may • Monitor renal and hepatic function at baseline and every 3 months
involve any part of the digestive tract from the mouth to the anus • Common adverse effects: rash, headache, diarrhoea
• Sulfasalazine
Available as tablets (Salazopyrin)
DRUGS FOR INFLAMMATORY BOWEL DISEASES Dosage: Acute UC: 2-4g d in 3-4 doses
Maintenance: 500mg qid
Crohn’s disease Crohn’s: 3-6g daily in divided doses
• 5-aminosalicylates: anti-inflammatory, induces remission in mild-to- Take with food to avoid GI upset
moderate disease Monitor complete blood profile, liver and renal function
• Corticosteroids: Induce remission in acute disease. Rectal May impair folic acid absorption, consider supplementation
corticosteroids are effective for distal colonic inflammation. Contact lenses and urine may stain orange
• Azathioprine and mercaptopurine: Maintain remission • Mesalazine
• Methotrexate: Induces remission or prevents relapse; mainly used in Available as granules, tablets (Salofalk, Pentasa, Mesasal.
patients intolerant to azathioprine and mercaptopurine Mezavant); enema, suppositories (Pentasa, Salofalk)
• TNF- antagonists: For moderate-to-severe disease unresponsive to Mesasal: Take tablets at least half an hour before food
conventional therapy Mezavant: Take with food
• Antibacterials: Include metronidazole and ciprofloxacin Salofalk: Take tablets at least one hour before food
• Other: Anti-diarrhoeals, cholestyramine, diet Pentasa: Absorption not affected by food. The tablets may be
• Smoking increases the risk of developing Crohn’s disease by 3-4 times dispersed in 50mL cold water, stirred and taken immediately.
See references for dosage details
Ulcerative colitis • Balsalazide
• 5-aminosalicylates: Induce and maintain remission in mild-to- Pro-drug of mesalazine
moderate disease Available as capsules (Colazide)
• Corticosteroids: Induce remission in acute disease. Dosage: acute UC: 3 tds until remission; maintenance 2 bd
• Azathioprine and mercaptopurine: Maintain remission • Olsalazine
• Cyclosporin: IV cyclosporin for corticosteroid-refractory disease Available as capsules, tablets (Dipentum)
• Infliximab: Induce and maintain remission in moderate-to-severe Dosage: acute UC: 1g bd; maintenance UC: 500mg bd
disease unresponsive to conventional therapy Take with food to avoid diarrhoea

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 11

Corticosteroids Cyclosporin
• Possible side effects: adrenal suppression, increased susceptibility to • Inhibits cytokine release from activated T cells
infection, sodium and water retention, oedema, hypertension, • Used in UC where patient has not responded to other drugs
hypokalaemia, hyperglycaemia, dyslipidaemia, osteoporosis, muscle • Side effects: reversible renal impairment, hypertension, hirsutism,
wasting gastrointestinal disturbances, pancreatitis, weight gain, oedema,
• L9 * hepatic dysfunction, hyperlipidaemia, anaemia, tremor, fatigue,
• Seek medical attention if you notice signs of infection headache, burning sensation in hands and feet, hyperkalaemia,
• Tell all healthcare professionals treating you that you are taking hypomagnesaemia, hyperuricaemia
corticosteroids • Monitor: FBC, renal function, electrolytes, liver fuction, fasting lipids,
• Prednisolone/prednisone (Predsol): 1 enema n until remission blood pressure, skin checks
• Hydrocortisone (Colifoam): 1 d or bd for 2-3 wks, then every 2nd day
until remission
• Budesonide (Entocort): 9mg m cc. L18 *
• Methylprednisolone (Solu-Medrol): inj as directed

Azathioprine and mercaptopurine


• Thiopurine immunomodulatory drugs which act against rapidly dividing
cells
• Azathioprine is converted to mercaptopurine in body
• Side effects: malaise, headache, nausea, vomiting, diarrhoea, fever,
rash, joint pain, hypotension, disturbed liver function, infections, hair
loss, macrocytosis, lymphopenia
• Avoid allopurinol with azathioprine/mercaptopurine as allopurinol can
increase toxicity/effect of the latter.

Methotrexate
• Folic acid antagonist
• Used in Crohn’s disease that is refractory to standard therapy
• Once weekly dosing
• Folic acid supplementation (usually 10mg per week, taken not on the
same day as methotrexate) reduces side effects such as nausea,
mouth ulcers

TNF- antagonists
• Adalimumab and infliximab injections: monoclonal antibodies that act
against tumour necrosis factor (TNF) alpha.
• Used in moderate to severe Crohn’s and severe UC

* L9 stands for ancillary label 9, L18 stands for ancillary label 18

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 12

DRUGS FOR GASTROINTESTINAL INFECTIONS

Anti-bacterials Helicobacter Pylori


• Quinolones • First line therapy (triple therapy)
Levofloxacin: can be used against H.Pylori; avoid antacids
containing magnesium or aluminium Esomeprazole/omeprazole 20mg bd
Norfloxacin: traveller’s diarrhoea + amoxycillin 1000mg bd
Ciprofloxacin: traveller’s diarrhoea + clarithromycin 500mg bd for 7 days

• Nitroimidazoles: treats H.Pylori, gram-negative anaerobes, gram- If amoxycillin unsuitable, use metronidazole instead:
positive anaerobes, anaerobic protozoa. Side effects: nausea, esomeprazole/omeprazole 20mg bd
diarrhoea, metallic taste. Avoid alcohol (will get intestinal cramping, + clarithromycin 500mg twice daily,
flushing, tachycardia, nausea and vomiting) + metronidazole 400mg twice daily for 7 days
Metronidazole: 400mg bd; avoid alcohol during and 24 hours
after treatment If clarithromycin unsuitable, replace with amoxycillin:
Tinidazole: longer half-life than metronidazole; single dose; esomeprazole/omeprazole 20mg bd
avoid alcohol during and 72 hours after treatment + amoxycillin 500mg three times daily,
+ metronidazole 400mg twice daily for 14 days
• Rifamycins: treats gram-positive organisms and mycobacteria. Side
effects: thrombocytopenia, acute renal failure, flu-like symptoms, • Second line therapy (triple therapy)
impaired liver function, discolouration of urine/sweat/tears Esomeprazole/Omeprazole 20mg bd
Rifampicin: MRSA infections + amoxycillin 1000mg bd
Rifabutin: MAC infections + levofloxacin 500mg (or rifabutin 150mg) bd for 10 days
Rifaximin: traveller’s diarrhoea, hepatic encephalopathy
• Third line therapy (quadruple therapy)
• Glycopeptides Esomeprazole/Omeprazole 20mg bd
Vancomycin: Clostridium-associated diarrhoea + bismuth 120mg qid
+ tetracycline 500mg qid
+ metronidazole 400mg tid for 7-14 days

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 13

Anti-elmintics
• Benzimidazoles: treats roundworm, threadworm, pinworm, hookworm,
whipworm. Side effects: gastrointestinal upset, leucopenia. For
intestinal worms, take on empty stomach
Albendazole: avoid in pregnancy and in children less than 6
months
Mebendazole
Triclabendazole: treats liver fluke
• Ivermectin: treats roundworms.
Take with fatty meals.
Not recommended for children 5 years or less
• Praziquantel: treats schistosomiasis.
Side effects: gastrointestinal upset, headache, dizziness and
drowsiness
• Pyrantel: treats roundworm, hookworm, threadworm, pinworm

Anti-protozoal
• Nitazoxanide: treats cryptosporidiosis
• Aminoglycosides
Paromomycin: given to treat asymptomatic carriers or to
eradicate cysts in amoebic colitis

Viral hepatitis
• Interferons
Side effects: flu-like symptoms, weight loss, depression,
anxiety, somnolence, forgetfulness, thyroid dysfunction , bone
marrow suppression
Check thyroid function and full blood counts
• Ribavirin
Side effects: haemolytic anaemia, teratogenic (both men and
women; avoid 6 months after therapy)
• Nucleosides/Nucleotides: used in hepatitis B
Adefovir: less potent and slower onset of action than tenofovir.
Avoid in pregnancy
Entecavir: side effects – headache, fatigue, dizziness, nausea.
Avoid in pregnancy
Lamivudine: not first-line therapy
Tenofovir: can be used for people with lamivudine and
entecavir resistance.

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 14

DRUGS FOR OBESITY

Indication: Obesity in adults (BMI>30 or >27 with other risk factors eg HT,
diabetes, hyperlipidaemia)
BMI = weight (kg)2
height (m)
Drug choice: Orlistat, phentermine, fluoxetine and other SSRIs (for weight
loss in depressed patients), meal replacement, bariatric surgery

Generic name Brand name Dose Side effects Precautions Other comments
Orlistat Xenical 120mg tds • Oily stools • Contraindicated in • Take with your main meals. Do not take your dose if you
(GI lipase inhibitor) cholestasis miss a meal or if it does not contain fat.
• Vitamin deficiency • This medication may cause oily stools, especially if your diet
is high in fat.
• Apply caloric restriction, increased physical activity and
eating behaviour modification
• Blood glucose, BP and lipid control may improve so
changes to other medications may be necessary
• Orlistat may absorption of fat-soluble vitamins (A, D, E, K)

Phentermine Duromine 15mg d • Overstimulation • Contraindicated in • L12 *


(sympathomimetic, of CNS CVD, hyperthyroidism, • Tell your doctor is you get short of breath
increases (eg insomnia, glaucoma, peptic ulcer, • Recommended for short term use only (max 12 wks)
metabolism) agitation, sibutramine, MAOI
tachycardia) • Use with caution for
drugs that contribute to
serotonin toxicity
• Avoid in hypertension
(may increase BP)

* L12 stands for ancillary label 12

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 15

DRUGS FOR PERIANAL DISORDERS AND OTHER GASTROINTESTINAL DRUGS

Pruritus ani Anal fissure


• Keep area clean and dry; avoid irritants • Avoid straining
• Apply sorbolene cream after cleansing; hydrocortisone may relieve • Increase fibre and fluid intake
inflammation • Bulking agent or stool softener
• Topical anaesthetic (relieves pain only)
Haemorrhoids • Rectal GTN (mainly relieves pain)
• Avoid straining
• Increase fibre and fluid intake
• Anorectal medications

Generic name Brand name Indications Other comments


Anorectal products Proctosedyl Haemorrhoids • Limit use to no more than a week because local anaesthetics may sensitise perianal
Anal fissure skin and topical corticosteroids may exacerbate local infection
Pruritis ani

Glyceryl trinitrate Rectogesic Anal fissure • Use tds for 2-4 weeks
• May cause headaches

Pancreatic enzymes Creon 5000 Pancreatic enzyme • Take this medicine with food
insufficiency (e.g. cystic • Do not crush or chew. Sprinkle the granules onto a small amount of soft food.
fibrosis, chronic pancreatitis, • Avoid taking this medicine with hot liquid or food as heat can damage enzymes
post-gastrectomy or
pancreatic surgery)

Ursodeocycholic acid Ursofalk Chronic cholestatic liver


disease

Copyright © The Medicine Box 2013


Topic Summary: Gastrointestinal 16

Reference

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2013

eTG Complete. Melbourne: Therapeutic Guidelines Ltd; 2013

eMIMS 5.0; MIMS Australia Pty Ltd; Sydney; 2013

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 1

TOPIC SUMMARY: RESPIRATORY


ASTHMA AND COPD
• Asthma: trigger factors (dust mite, pollen, animals, smoking, • Long-acting (duration of action: 12hr) :
respiratory tract infections, exercise, allergens, sensitivity to o Eformoterol (Oxis, Foradile) 1 puff bd (onset 1-3min)
foods/chemicals/preservatives, drugs such as NSAIDs, beta blockers, o Salmeterol (Serevent) 1 puff bd (onset 10-20min)
complementary medicines) o Indacaterol (Onbrez) 1 puff d
• Symptoms of asthma: wheezing, difficulty in breathing, chest tightness,
nocturnal coughs Other practice points (long-acting):
• COPD (chronic obstructive pulmonary disease): airway obstruction due • Combination products available
to inflammatory response of lungs that is not always reversible. o Eformoterol + Budesonide (Symbicort) – can be used for acute
• Symptoms of COPD: emphysema, mucus, airway damage and relief in adults with asthma who are using inhaled
narrowing of airways. Combination of asthma + chronic bronchitis + corticosteroilds.
emphysema and airway obstruction. o Salmeterol + Fluticasone (Seretide) 1 puff bd

DRUGS FOR ASTHMA AND COPD Anticholinergic bronchodilators


Beta2 agonist bronchodilators Mode of action: inhibits bronchoconstriction
Mode of action: stimulation of beta2 receptors causes bronchodilation • Short-acting: Ipratropium (Atrovent, Ipratrin) - onset 2hr; duration of
• Short-acting (onset 5min; duration of action 3hr): action 6hr; use QID
o Salbutamol (Ventolin, Asmol, Airomir) 1-2 puffs qid prn • Long-acting: Tiotropium (Spiriva) - onset 30min; duration of action
o Terbutaline (Bricanyl) 1-2 puffs qid prn 24hr; use 1 daily

Other practice points (short-acting): Corticosteroids


• Acute asthma, symptom relief , prevention of exercise-induced asthma Mode of action: reduce bronchial inflammation
• Use with precaution in hypertension, heart failure, arrhythmias, • Inhaled corticosteroids (preventers in asthma):
diabetes o Beclomethasone (Qvar) 1 bd
• Side effects (high doses): tremor, palpitations, headache o Budesonide (Pulmicort) 1 bd

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 2

o Ciclesonide (Alvesco) 1 d Leukotriene receptor antagonists


o Fluticasone (Flixotide) 1 bd Mode of action: relaxation of smooth muscle and reduction of inflammation
Side effects: hoarse voice, oral thrush • Montelukast (Singulair) 1 n
Counselling: rinse mouth with water after inhalation Side effects: headache, abdominal pain, diarrhoea

• Intranasal corticosteroids (allergic rhinitis): Xanthine bronchodilator


o Budesonide (Rhinocort) 1-2 bd Mode of action: relax smooth muscle and increase diaphragm contractility
o Fluticasone furoate (Avamys) 1-2 d • Theophylline (Nuelin) 1 d cc
o Mometasone (Nasonex) 1-2 d Side effects: low therapeutic index monitoring; nausea, vomiting,
o Triamcinolone (Telnase) 2 d diarrhoea, headache, insomnia, anxiety, tremor, palpitations
Side effects: sneezing, nasal irritation, nosebleeds
Other practice points:
• Oral corticosteroids: prednisolone/prednisone • Concentration monitoring at initiation, changes with drug regimen,
o Counselling: once daily in the morning (evening dose can fever or side effects suspected, changes in smoking habits
cause sleep disturbance); short-term treatment (long term
treatment of 2+ weeks can cause adrenal suppression and
rebound withdrawal symptoms if abrupt cessation)

Cromolyns
Mode of action: chloride channel blockers that stabilise mast cells; block
allergen-induced bronchoconstriction
• Inhalation (asthma prevention):
o Nedocromil (Tilade) 1 qid
o Sodium cromoglycate (Intal) 1 bd to qid
Side effects (inhaled): bronchospasm and throat irritation; headache
• Intranasal (allergic rhinitis): sodium cromoglycate (Rynacrom)
• Eye drops (allergic conjunctivitis): sodium cromoglycate (Opticrom,
Cromolux)

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 3

TREATMENT OF ASTHMA ATTACKS

Mild
Short-acting beta2 agonist monitor for 1 to 24 hours after attack

Moderate
Oxygen therapy short-acting beta2 agonist oral corticosteroids AND start
inhaled corticosteroids monitor with chest x-ray

Severe
HOSPITAL admission immediately oxygen therapy short-acting beta2
agonist + ipratropium oral or i.v. corticosteroids AND start inhaled
corticosteroids adrenaline for anaphylaxis or cardiorespiratory arrest
monitor with chest x-ray and hypokalaemia

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 4

TABLE: INHALED MEDICATIONS FOR ASTHMA AND COPD

Class Generic name Brand name Form Dose Other comments

Salbutamol Airomir MDI, Autohaler 1-2 q4h prn • Prime inhalers when using it for the first time and also if it
hasn’t been used for 5 days or more.
Asmol MDI, nebules (severe 1-2 q4h prn • Dilute nebulising solution with sodium chloride 0.9% if using
Ventolin acute asthma) alone.
Relievers

Terbutaline Bricanyl Turbuhaler 1 q4h to q6h prn • Maximum 8 puffs (children) or 12 puffs (adults) in 24 hours

Ipratropium Atrovent MDI, nebules (severe 2 tid to qid prn • Dilute nebulising solution with sodium chloride 0.9% if using
Ipratrin acute asthma) alone.
• Avoid mist to get into the eyes.

Ciclesonide Alvesco MDI 1-2 d or bd • Rinse mouth with water after inhalation with all inhaled
corticosteroid preparations. Failure will result in hoarse voice,
Corticosteroid preventers

oral thrush, sore throats, and infections.


Fluticasone Flixotide MDI, accuhaler, nebules 1-2 bd
propionate

1-2 bd to qid
Budesonide Pulmicort Turbuhaler, respules

1 bd
Beclomethasone Qvar MDI, autohaler

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 5

Class Generic name Brand name Indication Dose Other comments


Combination products

Budesonide + Symbicort Turbuhaler 1-2 bd for maintenance. • Acute relief: may admin 1 additional inhalation to control
Eformoterol symptoms followed by another inhalation if symptoms persist.
• Maximum 8 inhalations per day

Fluticasone + Seretide MDI, accuhaler 1 bd • Rinse mouth with water after inhalation.
Salmeterol
Non-steroid preventers

Sodium Intal MDI, nebules 2 bd to qid (MDI) • Clean mouthpiece daily and air dry for 24 hours to prevent
cromoglycate 1 qid (nebules) blockage of nozzles. Alternate with extra mouthpiece.

Nedocromil Tilade MDI 2 qid then 2 bd

Eformoterol Foradile Aerolizer 1-2 bd


Controllers
Symptom

Oxis Turbuhaler

Salmeterol Serevent Accuhaler 1-2 bd

Indacaterol Onbrez Breezhaler 1d • SE: nasopharyngitis, cough, URTI, headache, muscle


COPD

spasms.

Tiotropium Spiriva Handihaler 1d • Place capsule into device.

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 6

CROUP DECONGESTANTS
• Symptoms: a barking cough and hoarseness of voice due to Mode of action: vasoconstriction in nasal mucosa
inflammatory oedema within the sub-glottis triggered by an acute viral • Intranasal:
infection. o Oxymetazoline (Dimetapp, Drixine, Logicin, Sudafed)
• Treatment: o Phenylephrine (Nyal)
o Prednisolone (Predmix, Panafcortelone) 1mg/kg orally for 2 o Tramazoline (Spray-Tish)
days o Xylometazoline (Flo, Otrivin)
Counselling: to prevent rebound congestion, do not use for more than
PERTUSSIS (WHOOPING COUGH) 5 days.
• Whooping Cough: contagious bacterial infection causing persistent
cough for more than 2 weeks. • Oral: pseudoephedrine (Sudafed), phenylephrine (Sudafed)
• Treatment: Side effects (oral): increased blood pressure, insomnia, agitation,
o Azithromycin (Zithromax) 500mg daily for 4 days OR anxiety
o Clarithromycin (Klacid, Kalixocin) 500mg bd for 7 days OR
o Erythromycin (EES, E-mycin) 400mg qid for 7 days

INFLUENZA (FLU)
• Start treatment early (within 48 hours of symptom onset).
• Treatment:
o Oseltamivir (Tamiflu) 75mg bd for 5 days OR
o Zanamivir (Relenza) 10mg inhalation for 10 days

Copyright © The Medicine Box 2013


Topic Summary: Respiratory 7

References

Australian Medicines Handbook. Adelaide: Australian Medicines Handbook Pty Ltd; 2013

eTG Complete. Melbourne: Therapeutic Guidelines Ltd; 2013

eMIMS 5.0; MIMS Australia Pty Ltd; Sydney; 2013

Useful resource:

Asthma and COPD medications chart


http://www.nationalasthma.org.au/health-professionals/primary-care-resources/asthma-copd-medications-chart

Copyright © The Medicine Box 2013

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in
this publication must not be reproduced or stored in any way without prior written permission of the
publishers.

While every effort has been made to ensure this publication is as accurate as possible, the Medicine
Box team does not accept any responsibility for any loss which the user may suffer as a result of errors
or inaccuracy of information contained in this publication.

Copyright © The Medicine Box 2013


Study Notes: Diabetes Guideline – Insulin 1

DIABETES GUIDELINE: INSULIN

Diabetes and Insulin

Insulin is a hormone produced in the pancreas that facilitates the uptake of glucose into various cells in
the body to be used as energy. It also helps store excess glucose in the liver. When the control of insulin
fails, diabetes will result.

There are 2 main types of diabetes:


Type 1: body fails to produce insulin due to destruction of insulin-producing cells in the pancreas
and requires the person to inject insulin.
Type 2: person has impaired insulin secretion and insulin resistance - i.e. cells fail to use insulin
properly. Some patients may eventually require insulin injections if other oral medications fail to
control blood glucose levels adequately. Causes include: obesity, age, physical inactivity, genetic.

Types of Insulin

Laboratory-created insulin is made by recombinant DNA technology and is similar to insulin produced by
a human pancreas. The main suppliers of medical insulin in Australia include: Eli Lilly, Novo Nordisk and
Sanofi-Aventis.

There are several different types of insulin which can be categorised into their time of action. The medical
practitioner will determine which one is more suitable for certain individuals.

1. Rapid onset-fast acting insulin: NovoRapid, Humalog


2. Short-acting insulin: Actrapid, Humulin R
3. Intermediate-acting insulin: Protaphane, Humulin NPH
4. Pre-mixed Insulin: Novomix 30, Humalog Mix 25, Humalog Mix 50; Mixtard 30/70, Mixtard 50/50,
Humulin 30/70
5. Long-acting insulin: Lantus, Levemir

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 2

Table: Types of Insulin

Insulin Type Examples Onset of Peak Time Duration Notes


action (hr) of action
(hr)
Rapid onset – fast acting NovoRapid (aspart) 15min 1 4 to 5 • Clear liquid
insulin Humalog (lispro) • Inject immediately before eating

Short-acting Actrapid (neutral) 30min 2 to 3 6 to 8 • Clear liquid


Humulin R (neutral) • Inject half an hour before eating

Intermediate-acting Protaphane (isophane) 1 to 3 hr 4 to 12 16 to 24 • Cloudy liquid


Humulin NPH (isophane) • Contains protamine or zinc to delay
action
• Shake well
• Inject once or twice daily

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 3

Long-acting Lantus (glargine) 1 to 2 No peak 24 • Clear liquid


• Inject once daily
• Do not mix with other insulin in a
syringe

Levemir (detemir) 3 to 4 9 12 to 24 • Clear liquid


• Inject once or twice daily

Mixed insulin Novomix 30 15min 1 16 to 18 • Mixed insulin (rapid-acting +


Humalog Mix 25 intermediate acting)
Humalog Mix 50 • Cloudy liquid
• Inject once or twice daily

Mixtard 30/70 30min 2 to 12 16 to 24 • Mixed insulin (short-acting +


Mixtard 50/50 intermediate acting)
Humulin 30/70 • Cloudy liquid
• Inject once or twice daily

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 4

Insulin Delivery Devices

Oral, transdermal and nasal administration have been developed but are not readily available compared to subcutaneous injections.
Subcutaneous injections are the most common form of administration for insulin and are available in the form of different devices such as:
syringes, delivery devices and pumps.

1. Insulin syringes
- Single-use syringe with plunger and needle
- Use syringe to draw insulin from vials (10ml vials containing 100units/ml)
- Syringe sizes: 0.3ml (30 units), 0.5ml (50 units) or 1.0ml (100 units). Size of syringe is dependent on insulin dose (in units).
- Needle sizes (length): 8mm or 13mm

Diagram: syringe and insulin vial

Syringe Products:
Braun Omnican
BD Ultra-fine
CM Safety Syringe
Terumo

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 5

2. Insulin delivery devices


a) Cartridges/Penfills: 3ml cartridges containing 100units/ml insulin fits into a durable insulin pen device. A new cartridge is inserted
once it is finished.
Table: Insulin pen devices and cartridges

Insulin pen devices Insulin cartridge/penfill

NovoPen® NovoRapid®
Actrapid®
Protaphane®
NovoMix®
Mixtard®
Levemir®

*Recommended pen needles: NovoFine


AutoPen® Lantus®

*Recommended pen needles: Unifine Pentips


HumaPen® Luxura Humalog®
Humulin®

*Recommended pen needles: BD Ultra-Fine

*Note: although most pen needles are interchangeable and used for different devices, the above recommendations are based upon the
information provided by the pen/device manufacturer.

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 6

b) Pre-filled devices: disposable devices prefilled with insulin.

Table: Types of Pre-filled insulin devices

FlexPen® NovoLet®

*Recommended pen needles: NovoFine


*Recommended pen needles: NovoFine

InnoLet® KwikPen®

*Recommended pen needles: NovoFine *Recommended pen needles: BD Ultra-Fine

Solostar®

*Recommended pen needles: BD Micro-Fine

*Note: although most pen needles are interchangeable and used for different devices, the above
recommendations are based upon the information provided by the pen/device manufacturer.

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 7

For all types of insulin delivery devices, a pen needle is required:


• Needle is screwed onto the device and used once per injection.
• Needle sizes (length): 5mm, 6mm, 8mm or 12mm
• Needle sizes (thickness/gauge): 28G, 29G, 30G, 31G (The higher the number, the
finer the needle is)

Pen needles:
Braun Omnican Mini Pen Needles 30g x 8mm
BD Microfine + Pen Needles
Novofine Pen Needles
Penfine Universal Click Pen Needle
Unifine Pentips

Choosing needles:
• Longer needles are useful for obese adults
• Deeper penetration places medication deeper than pain nerve endings
• May inject at 45 degree angle with longer needles (90 degree angle for shorter needles)
• Shorter needles are useful for children and thin adults.

Table: Insulin Forms

Insulin (brand) Available forms on market


NovoRapid Vial, Penfill, FlexPen

Actrapid Vial, Penfill

Protaphane Vial, Penfill, InnoLet, NovoLet

NovoMix Penfill, FlexPen

Mixtard 30/70 Penfill, InnoLet

Mixtard 50/50 Penfill

Humulin R Vial, Cartridge


Humulin NPH Vial, Cartridge
Humulin 30/70 Vial, Cartridge

Humalog Vial, Cartridge, KwikPen

Humalog Mix25 & Mix50 Cartridge, KwikPen

Lantus Vial, Cartridge, Solostar

Levemir Penfill, FlexPen

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 8

3. Insulin pump
An insulin pump is a small programmable device that contains insulin. It is worn outside the body – in a pouch or clipped onto a belt. It is
programmed to deliver insulin into the body through a thin plastic tube (infusion) via a fine needle/cannula that is inserted below the skin
(usually on the abdomen area) where it stays in place for two to three days. It is an alternative to multiple daily injections of insulin by
syringe or pen and is only used for rapid or short-acting insulin.

It delivers fast-acting insulin in two ways:


a) A bolus dose is pumped to provide an extra boost of insulin to counteract food being eaten.
b) A basal dose is pumped continuously based on an adjustable basal rate to deliver insulin needed between meals and at night.

Advantages Disadvantages
• Convenient and discreet form of insulin administration • Costly: insulin pumps, cartridges and infusion sets are more
• Accurate record of insulin usage that can be computer- expensive than syringes
analysed • Pump needs to be worn so may limit certain activities that may
• Patient compliance damage the pump such as swimming, extreme sports etc
• Freedom from a structured meal and exercise regimen • Wearing the pump may be uncomfortable
• Better control of blood sugar levels • Possibility of insulin pump malfunction
• Scar tissue building due to the inserted cannula
• Allergic reactions or skin irritation from adhesive of infusion set
• Larger supply of insulin may be required to use the pump to
cater for wastage involved with refilling reservoir or changing
infusion sets.

In Australia, it is mainly marketed for people with Type 1 diabetes. Subsidies exist through Diabetes
Australia and Commonwealth Department of Health and Aging but individuals must meet and be
assessed against a set of criteria first. The assessment must be completed by an endocrinologist,
credential diabetes education or specialist physician.

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 9

How is insulin injected?

Step-by-step

1. Choose an area to inject the alcohol.


2. Clean area with alcohol swab.
3. Pinch skin into a fold and hold. A fatty area is less painful and helps absorb insulin better.
4. Insert needle quickly and accurately at 45-90 degree angle.
5. Insert needle deep enough and inject insulin by pushing the top of the syringe all the way down or
the button of a pen.
6. Hold in that position for 5 seconds and then remove needle by pulling it straight out for minimal
pain.
7. Pull out needle and dispose in a sharps container.

Tips:

• Most common and best area to inject insulin is the abdomen area. It absorbs insulin the best.
Buttocks, thighs, upper arms can also be used.
• Avoid injecting into a muscle as it is painful and will cause insulin to be absorbed into the body
too quickly.
• Avoid injecting insulin directly into a bloodstream.
• Rotate sites of injection to prevent skin irritation.
• Change needle with each injection.
• Gently roll vials back and forth with the palm of your hands to mix the insulin. Do not shake as it
can create bubbles.
• For pen insulin, roll back and forth with palms as well as shake the pen to mix the insulin.

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 10

Counselling Points: Diabetes & Insulin

Hypoglycaemia
• Watch out for signs and symptoms of hypoglycaemia (low blood sugar levels): lethargy,
confusion, sweating, twitching, trembling, dizziness, headache, light headedness, lack of
concentration, pale, loss of consciousness
• Causes of hypoglycaemia: delaying/missing a meal, strenuous exercise, drinking alcohol,
overdose on insulin or tablets.
• In the event of hypoglycaemia, take fast-acting carbohydrates such as: glucose lollies, fruit juice,
soft drink etc. to relieve the symptoms.

Diet
• No special diet required
• Low glycaemic index (GI) foods
• Low in saturated fat
• High fibre carbohydrate foods: wholegrain breads and cereals, vegetables and fruit
• Low in salt content
• Avoid high amounts of sugars such as lollies and soft drinks
• Limit alcohol consumption.
• Artificial sweeteners preferred over sugar
• Limit serving size of your meals and make sure you eat regularly.

Exercise
• Increase general physical activity and a regular exercise program. Take it slow.
• 30min of exercise each day.
• Drink extra fluid before, during and after exercise to avoid dehydration.
• Take extra carbohydrate before and during exercise to prevent hypoglycaemia

Blood Sugar Monitoring


• Testing blood glucose levels at home will help with diabetes control.
• Frequency of testing depends on each individual, type of diabetes and medication. Usually 3-4
times daily for a person using insulin.
• Record results in a diabetes diary for self and physician records.
• When to test: before breakfast, before meals, before bed, before exercise, two hours after a meal
or when feeling unwell.

Storage
• Store unused insulin in a refrigerator. Do not freeze.
• Once opened, insulin may be kept at room temperature (less than 30 degrees Celsius) for one
month and then thrown away.
• Do not use insulin if: clear insulin has turned cloudy, expired, frozen or exposed to high
temperatures.

Copyright © The Medicine Box 2011


Study Notes: Diabetes Guideline – Insulin 11

References / Resources

1. Diabetes Australia
2. Australian Diabetes Council
3. Australian Diabetes Educators Association (ADEA)
4. Eli Lilly
5. Sanofi-Aventis
6. Novo Nordisk
7. BD
8. Accu-Chek
9. Abbott
10. Point of Care Diagnostics (POCD)
11. Australian Medicines Handbook 2010
12. eMIMS 2010
13. myDr.com.au – Diabetes
14. Australian Pharmaceutical Formulary and Handbook 19th Edition

Copyright © The Medicine Box 2011

All rights reserved. Apart from any use permitted under the Copyright Act 1968 of Australia, material in this publication must not be
reproduced or stored in any way without prior written permission of the publishers.

Disclaimer: While every effort has been made to ensure this publication is as accurate as possible, the Medicine Box team does not
accept any responsibility for any loss which the user may suffer as a result of errors or inaccuracy of information contained in this
publication. It is also noteworthy that The Medicine Box is unaffiliated with the Pharmacy Board of Australia, the former Pharmacy
Board of NSW, the Australian Pharmacy Council or the Pharmaceutical Society of Australia. All information in this publication is
provided by past pharmacy graduates and has not been verified by the above organisations.

Copyright © The Medicine Box 2011

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