Professional Documents
Culture Documents
It is Adrenergic Agonist.
It binds to and activates adrenergic receptors in the body.
These receptors include alpha-adrenergic receptors and beta-adrenergic
receptors, which are found on various tissues and organs throughout the
body.
Activation of these receptors leads to physiological responses such
as increased heart rate, dilation of airways, and mobilization of
glucose.
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3. Mechanism of Action
4. Indications :
Tachycardia
Hypertension
Arrhythmias
Severe Headache
Nervousness & Anxiety
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Hyperglycemia
6. Contraindications
8. Pharmacokinetic Profile
9. Special considerations:
Do not administer Adrenaline into the Gluteal region otherwise, it may cause gas
gangrene.
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Don’t use this drug for diabetic patients.
Don’t use adrenaline if you’ve already had cardiac problems.
Use the best possible route with the best possible calculated dose.
Drug # 2: Aminoglycoside
Prototype
Streptomycin
1. Generic name:
Streptomycin
2. Trade name:
Ambistryn-S
3. Mechanism of Action:
Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. Disrupts the
initiation complex formation during translation. It also induces misreading of the mRNA,
leading to the synthesis of incorrect proteins.
4. Indications:
5. Pharmacokinetic Profile:
Distribution: The volume of distribution of streptomycin ranged from 30-35% body weight,
corresponding to the extracellular fluid volume. Penetrates various body tissues, including the
lungs, kidneys, and cerebrospinal fluid.
6. Route of Administration:
7. Contraindications:
Hypersensitivity to streptomycin or other aminoglycosides. Concomitant live bacterial
vaccines.
8. Dosage:
Moderate-Severe Infections
1-2 g/day IM divided every 6-12hr; no more than 2 g/day
Tuberculosis
Daily therapy: 15 mg/kg IM every day; no more than 1 g/day
Twice weekly therapy: 25-30 mg/kg IM 2 times/week; no more than 1.5 g/day
Tularemia
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1-2 g IM in divided doses for 7-10 days or until patient is afebrile for 5-7 days
Plague
15 mg/kg IM every 12hr for minimum 10 days
Streptococcal Endocarditis
1 g IM every 12hr for 7 days, THEN 500 mg q12hr for 7 days, concomitant with penicillin. If
>60 years old, 500 mg every 12hr for the entire 14 days.
9. Dosage Form:
Streptomycin is available as a powder for injection, which is reconstituted before
administration.
10. ADRs
Ototoxicity:
Streptomycin is known for its potential to cause damage to the inner ear, leading to hearing
loss and vestibular (balance) disturbances. Ototoxicity is usually dose-dependent and may be
irreversible.
Nephrotoxicity:
Streptomycin can affect the kidneys, leading to renal damage. Monitoring kidney function is
important during treatment.
Neuromuscular Blockade:
Streptomycin may interfere with neuromuscular transmission, leading to muscle weakness or
paralysis. This effect is particularly important in patients with pre-existing neuromuscular
disorders.
Allergy Screening:
Before administration, inquire about any history of allergies, especially to aminoglycoside
antibiotics, to prevent allergic reactions.
3. Classification:
They belong to the class of anti-epileptic drugs known as “valproic acid derivatives” or
“Valproate derivatives.
4. Mechanism of Action:
• Inhibition of voltage-gated sodium channels: VPA obstructs the entry of sodium ions into
neurons, leading to decreased neuron excitability and firing rate. This prevents generating and
propagating abnormal electrical impulses responsible for triggering seizures.
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• Inhibition of gamma-aminobutyric acid (GABA) transaminase: VPA inhibits the function
of the GABA transaminase enzyme, which is responsible for the degradation of GABA. This
process increases the levels and activity of GABA, thereby enhancing the inhibition of neuronal
function and ultimately diminishing the vulnerability to seizures. In cases of neuropathic pain,
VPA has been demonstrated to impede neurogenic inflammation through GABA-A receptor-
mediated inhibition.
• Enhancement of GABA synthesis: VPA stimulates the synthesis of GABA by increasing
the expression and activity of glutamic acid decarboxylase (GAD), the enzyme responsible for
converting glutamate, which is the primary excitatory neurotransmitter in the brain, into
GABA. This process also contributes to the increase in GABA levels and activity. GABA is
synthesized from α-ketoglutarate via the tricarboxylic acid (TCA) cycle and metabolized into
succinate semialdehyde. This intermediate is further transformed into succinate by GABA
transaminase and succinate semialdehyde dehydrogenase, respectively. Prior research has
indicated that VPA inhibits GABA transaminase and succinate semialdehyde dehydrogenase,
thereby elevating GABA concentration by reducing its degradation.
• Inhibition of HDACs: VPA inhibits the action of HDAC enzymes, notably HDAC1, which
are involved in the regulation of gene expression by modifying the acetylation status of
histones, which are proteins that wrap around DNA. This process leads to changes in chromatin
structure, subsequently influencing the transcription of many genes, including those linked to
neuronal plasticity, synaptic transmission, neurogenesis, neuroprotection, and inflammation.
This phenomenon could potentially elucidate a portion of the enduring effects of VPA on
mood, cognition, neurodevelopment, apoptosis, and its potential antitumor properties.
• Modulation of calcium channels: VPA modulates the activity of various calcium channels,
including T-type, L-type, and N-type calcium channels. These channels are essential in
neuronal signalling, neurotransmitter release, gene expression, and cellular survival. The exact
effects of VPA on calcium channels are complex and depend on several factors, such as channel
subtype, location, state, and co-expression with other proteins. Certain studies indicate that
VPA effectively inhibits T-type calcium channels, which have been implicated in absence
seizures and thalamocortical oscillations. Other studies suggest that VPA enhances L-type
calcium channels, which are involved in neuronal plasticity and neuroprotection. VPA may
also affect N-type calcium channels associated with neuropathic pain and migraine.
5. Indications:
• Use as monotherapy or adjunctive therapy in the management of complex
partial seizures and simple or complex absence seizures
• Adjunctive therapy in the management of multiple seizure types that include
absence seizures.
• Prophylaxis of migraine headaches.
• Acute management of mania associated with bipolar disorder.
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o Emergency treatment of status epilepticus.
6. Pharmacokinetic Profile:
Absorption:
Distribution:
• Volume of distribution is 11L/1.73m2 Or 0.1 - 0.41 l/kg
• Protein binding is linear at low concentrations with a free fraction of
approximately 10% at 40 mcg/mL but becomes non-linear at higher concentrations with
a free fraction of 18.5% at 135 mcg/mL. This may be due to binding at separate high
and low-affinity sites on albumin proteins. Binding is expected to decrease in the elderly
and patients with hepatic dysfunction.
Metabolism:
Sodium valproate undergoes extensive hepatic metabolism, primarily through glucuronidation
and mitochondrial β-oxidation. The major metabolite is 2-n-propyl-4-pentenoic acid (2-ene-
VPA). It is also a substrate for cytochrome P450 enzymes, particularly CYP2C9.
Excretion:
The elimination half-life of sodium valproate is approximately 9 to 18 hours in adults.
It is primarily eliminated renally as metabolites, with a small portion excreted
unchanged in the urine.
The elimination half-life may be shorter in children.
7. ADR's:
Adverse drug reactions associated with sodium valproate include:
Gastrointestinal disturbances (nausea, vomiting, diarrhea)
Sedation and drowsiness
Weight gain
Tremor
Hair loss
Hepatotoxicity (elevated liver enzymes, hepatomegaly)
Pancreatitis
Teratogenic effects (increased risk of congenital malformations)
Hyperammonemia
Thrombocytopenia
Bone marrow suppression
Hyperammonemic encephalopathy (especially in patients with urea cycle disorders)
8. Route of Administration:
Oral
Intravenous
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9. Contraindication:
10. Dosage:
Inj-IV: 500 mg, Syrup 200 mg/5ml, 250 mg/5ml, 500 mg/5ml, Susp: 200 mg/5ml,
Tabs: 125 mg, 200 mg, 250 mg, 500 mg Capsules: 500mg- 1000mg/day
Dosage form:
They are available in the form of:
Tablets
Capsules
Syrups
Suspension
Injectable (IV)
Drug # 4: Isoniazid
1. Generic name: Isoniazid
3. Class
Antimycobacterial antibiotic.
4. Mechanism of action.
Inhibit cell wall synthesis in mycobacterium tuberculosis by interfering with mycolic acid
production.
5. Indications.
Tuberculosis (TB) in combination with other anti TB drugs.
prevention of latent TB infection.
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isoniazid prophylaxis therapy( reduces the risk of TB in HIV
Positive individuals.
6. Pharmacokinetic
Absorption.
Isoniazid easily absorbed from GIT. Absorption is decreased with food(fatty substances and
carbohydrates). So it should be taken before meal, optimally on empty stomach.
Distribution.
Diffuses readily in body tissues, placenta and meningitis.
Metabolism.
Metabolized by the liver by acetylation.
Excretion.
Mainly excreted in urine.
7. Route of administration
Normally taken orally but may be administered IM and IV to critically ill patients.
Hepatotoxicity
deficiency of vitamin B6
peripheral neuropathy (nerve damage) due to deficiency of vitamin B6
anxiety, depression, memory loss, seizures.
9. Contraindications
Severe liver disease
Acute pyridoxine deficiency .
Hypersensitive to isoniazid
Regular liver function monitoring is necessary throughout the treatment. Patient with a
pre existing liver disease or at high risk of hepatotoxicity may require low doses.
pyridoxine supplement may be recommended to prevent neuropathy.
Pregnant and breastfeeding should consult with their health care professional before
taking isoniazid.
Drug # 5: ATROPINE
1. Generic name:
Atropine
2. Brand Names:
Atropine is available under various brand names, including Atropen, Atropisol, and Sal-
Tropine, among others.
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4. Classification:
Atropine is classified as an anticholinergic agent.
5. Indication:
Atropine is used for various medical purposes, including the treatment of bradycardia,
organophosphate poisoning, and as a pre-anesthetic medication to reduce salivation and
respiratory secretions.
6. Pharmacokinetic Profile:
8. Route of Administration:
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Atropine can be administered orally, intravenously, intramuscularly, subcutaneously, or
topically (e.g., ophthalmic solution).
9. Contraindications:
Atropine is contraindicated in individuals with a known hypersensitivity to the drug, glaucoma,
severe tachycardia, and in certain cases of obstructive diseases such as pyloric stenosis and
paralytic ileus.
Drug # 6: BENZODIAZEPINES
DIAZEPAM:
1. Trade Name:
Valium® (first marketed name)
Other names are:
Diastat, Valtoco, Dizac, Calmpose etc
2. Classification:
Diazepam -------> Benzodiazepines
Benzodiazepines --------> depressants known as sedative-hypnotics or anxiolytics
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3. Mechanism of Action:
4. Indications:
Anxiety Disorders: including generalized anxiety disorder (GAD), panic disorder, and
social anxiety disorder. It helps alleviate feelings of tension, restlessness, and excessive
worry.
Muscle Spasms: relieving muscle spasms and involuntary muscle contractions
associated with conditions such as muscle strains, sprains
Seizure Disorders: as an anticonvulsant medication to treat various types of seizures,
including generalized tonic-clonic seizures, absence seizures, and febrile seizures. .
Alcohol Withdrawal: Diazepam is often prescribed to manage symptoms of alcohol
withdrawal syndrome, including agitation, tremors, hallucinations, and seizures.
Preoperative Sedation and Anesthesia Adjunct: Diazepam is sometimes used as a
preoperative medication to reduce anxiety and induce sedation before surgical procedures.
It may also be used as an adjunct to anesthesia to enhance muscle relaxation and reduce the
required dosage of anesthetic agents.
5. Pharmacokinetic Profile:
Bioavailability:
Oral = 90–100% ( 15-60 minutes onset of action )
Rectal = 90% (5-30 minutes onset of action)
Nasal = 75–95%
Intravenous = 97 –100% (1-5 minutes onset of action)
Intramuscular = slow and incomplete absorption (15-30 minutes onset of action)
Diazepam readily crosses the blood-brain barrier and is highly protein-bound
It is highly lipid soluble and widely distributed throughout the body.
Diazepam is metabolized in the liver by CYP450 enzyme system (CYP3A4 – major
route )
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Diazepam is excreted by the kidneys
The half-life of diazepam in general is 30–56 hours.
8. Routes of administration:
Oral, rectal , nasal , intravenous and intramuscular
9. Contraindications:
Hypersensitivity
Myasthenia gravis
Severe respiratory insufficiency
Hepatic and renal insufficiency
Sleep apnea syndrome
Lactating women
Drug # 7: CEPHRADINE
1. Drug generic Name: CEPHRADINE
4. Mechanism of action:
The mechanism of action (MOA) of cephradine involves inhibiting bacterial cell wall synthesis
by binding to penicillin-binding proteins (PBPs). This action weakens the bacterial cell wall,
leading to cell lysis and eventual death of the bacteria.
5. Indications:
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Cephradine is commonly indicated for the treatment of various bacterial infections, including
respiratory tract infections (such as pneumonia, bronchitis, and sinusitis), skin and soft tissue
infections, urinary tract infections, and certain types of bacterial meningitis. It may also be used
for prophylaxis in certain surgical procedures to prevent postoperative infections.
6. Pharmacokinetics(ADME):
The pharmacokinetics (PK) of cephradine involve absorption, distribution, metabolism, and
elimination processes in the body:
Absorption: Cephradine is usually administered orally and is well absorbed from the
gastrointestinal tract.
Distribution: It distributes widely into body tissues and fluids, achieving therapeutic
concentrations in the urine, respiratory secretions, bile, and synovial, pleural, and peritoneal
fluids.
Metabolism: Cephradine is primarily eliminated unchanged by the kidneys via glomerular
filtration and tubular secretion. It undergoes minimal metabolism in the liver.
Elimination: The elimination half-life of cephradine is relatively short, usually around 0.5 to
1 hour in adults with normal renal function. However, this may vary depending on factors such
as renal function and dosing frequency.
8. Route of Administration:
Cephradine can be administered via several routes :
Oral: Cephradine is commonly available in oral dosage forms such as capsules or
tablets, which are taken by mouth.
Intramuscular (IM) injection: Cephradine can be administered via injection into a
muscle, usually done by a healthcare professional.
Intravenous (IV) injection: In certain situations, cephradine may be administered
directly into a vein, typically in a hospital or clinical setting.
The choice of route depends on factors such as the severity of the infection, patient's condition,
and healthcare provider's preference.
Capsules: These are solid oral dosage forms containing cephradine powder enclosed in
a gelatin shell.
Tablets: Similar to capsules, tablets contain cephradine in solid form but are
compressed into a solid dosage form without a gelatin shell.
Powder for oral suspension: This form consists of cephradine powder, which is
reconstituted with water to form a liquid suspension for oral administration, often used
for pediatric patients or those who have difficulty swallowing tablets or capsules.
Injection: Cephradine is available in sterile powder form for reconstitution and
administration via intramuscular or intravenous injection.
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The dosage of cephradine can vary depending on factors such as the type and severity of the
infection, patient age and weight, renal function, and other individual considerations. However,
typical dosages for adults with normal renal function are as follows:
For mild to moderate infections:
Oral: 250 mg to 500 mg every 6 to 12 hours.
For severe infections or those caused by less susceptible organisms:
Oral: 500 mg to 1 gram every 6 to 12 hours.
For intramuscular or intravenous administration:
500 mg to 1 gram every 6 to 12 hours.
Dosage adjustments may be necessary in patients with impaired renal function to avoid
accumulation of the drug and potential toxicity.
10. Contraindications :
Drug # 8: Chlorpheniramine
1. Brand name
Chlor-Trimeton, Demazin, Allerest 12 Hour, Piriton, Chlorphen-12, Tylenol Cold/Allergy.
2. Generic name
Chlorpheniramine maleate
3. Class
Chlorpheniramine is in a class of medications called antihistamines first-generation H1
4. Mechanism of action
The mechanism of action of chlorpheniramine is as a Histamine H1 Receptor Antagonist.
Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous
histamine, which subsequently leads to temporary relief of the negative symptoms brought on
by histamine.
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5. Indication
histamine H1 antagonist used in
allergic reactions
hay fever
rhinitis
urticaria, and
asthma.
6. Pharmacokinetics
Absorption
Well absorbed in the gastrointestinal tract.
Volume of distribution
Not Available
Protein binding
72%
Metabolism
Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Route of elimination
Not Available
Half-life
21-27 hours
Clearance
Not Available
Drowsiness
Dizziness
Constipation
stomach upset
blurred vision or dry mouth/nose/throat may occur.
8. Route of administration
Oral
Injectable
The injection may be given by the subcutaneous, intramuscular or intravenous route.
Interactions
Hypersensitivity to chlorpheniramine or any component of the formulation, narrow-angle
glaucoma, bladder neck obstruction, symptomatic prostate hypertrophy, during acute asthmatic
attacks, stenosing peptic ulcer, pyloroduodenal obstruction. Avoid use in premature and term
new-borns due to possible association with SIDS.
9. Dosage Forms & Strengths
Adult
Tablet
4mg
8mg
12mg
Syrup
2mg/5mL
Allergic Rhinitis
Tablets or syrup: 4 mg PO q4-6hr; not to exceed 24 mg/day
Extended-release tablets: 8 mg PO q8-12hr or 12 mg q12hr; not to exceed 24 mg/day
Extended-release capsules: 12 mg PO qDay; not to exceed 24 mg/day
Sustained-release capsules: 8-12 mg PO q8-12hr, up to 16-24 mg/day
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Pediatric
Tablet
4mg
8mg
12mg
Suspension
2mg/mL
Syrup
2mg/5mL
Allergic Rhinitis
<2 years: Safety & efficacy not established
2-6 years: 1 mg PO q4-6hr; not to exceed 6 mg/day
6-12 years: 2 mg PO q4-6hr; not to exceed 12 mg/day or sustained release HS
>12 years
Tablets or syrup: 4 mg PO q4-6hr; not to exceed 24 mg/day
Extended-release tablets: 8 mg PO q8-12hr or 12 mg q12hr; not to exceed 24 mg/day
Extended-release capsules: 12 mg PO qDay; not to exceed 24 mg/day
Sustained-release capsules: 8-12 mg PO q8-12hr, up to 16-24 mg/day
Drug # 9: Cimetidine
1. Generic Name: cimetidine (HCL)
2. Trade name : Tagamet HB ®
3. Class of drug: Cimetidine belongs to the class of drugs called H2 Blockers
➢ Indications : Cimetidine is indicated to reduce gastric acid secretion and to treat the
following
D. systemic mastocytosis
5. Pharmacokinetics of cimetidine :
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Bioavailability 60 to 70 %
Protein Binding 13 to 25 %
Metabolism: liver
Metabolites: cimetidine sulfoxide, hydroxy cimetidine, Guanyl urea cimetidine
On set of action: 30 minutes
Elimination half-life: 2 hours
Duration of action: 4 to 8 hours
Excretion: urine
Parenterally : IV injection
9. Dosage:
Adult dose : 400mg per 12 hours oral
Neonatal dose : 20 mg / kg oral
Paediatric dose : 20 to 30 mg per kg oral
Tablets Syrups
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11. Special considerations:
Take with food. Food increases bioavailability.
For prophylaxis of gastric symptoms, take cimetidine 30-60minutes prior to food
administration.
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Digoxin is approximately 70-80% absorbed in the first part of the small bowel. The
bioavailability of an oral dose varies from 50-90%, however, oral gelatinized capsules of
digoxin are reported to have a bioavailability of 100%.
Protein binding:
Digoxin protein binding is approximately 25%. It is mainly bound to albumin.
Half life:
Digoxin has a half-life of 1.5-2 days in healthy subjects. The half-life in patients who do
not pass urine, usually due to renal failure, is prolonged to 3.5-5 days.
Clearance:
The clearance of digoxin closely correlates to creatinine clearance, and does not depend on
urinary flow. Individuals with renal impairment or failure may exhibit extensively
prolonged half-lives. It is therefore important to titrate the dose accordingly and regularly
monitor serum digoxin levels. One pharmacokinetic study measured the mean body
clearance of intravenous digoxin to be 88 ± 44ml/min/l.73 m². Another study provided
mean clearance values of 53 ml/min/1.73 m² in men aged 73-81 and 83 ml/min/1.73 m² in
men aged 20-33 years old after an intravenous digoxin dose.
7. Adverse drug reactions:
Digoxin toxicity ; confusion, loss of appetite, nausea, vomiting, diarrhea, change in
vision such as blurry or yellow vision, fatigue, fast or irregular heartbeat.
Slow heartbeat—dizziness, feeling faint or lightheaded, confusion, trouble
breathing, unusual weakness or fatigue.
Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or
throat.
8. Route of administration:
ORAL
IV/IM
9. Contra indications:
Acute myocardial infarction.
Hypersensitivity to the drug.
Ventricular fibrillation.
Myocarditis.
Hypomagnesemia.
Hypokalemia.
Wolf-Parkinson-White syndrome.
10. Dosage:
Oral/Tablet dosage: 0.25 mg
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IV/IM Dosage: 250mcg/ml
4. Mechanism of action:
Dobutamine directly stimulates beta- adrenergic receptors and is generally considered a
selective Beta-1 adrenergic agonist. Dobutamine also has mild beta-2 and alpha-1 adrenergic
receptor agonist effect.
Beta 1 receptor:
It directly bind and stimulates beta-1 adrenergic receptor
Stimulation of adenyl cyclase activity
Conversion of ATP to cAMP
Activation of protein kinase A
Phosphorylation of intracellular proteins
Increased calcium influx
Enhanced myocardial contraction
Increased stroke volume
Alpha-1 receptor:
Stimulation of alpha-1 receptor on smooth muscle cells
Activation of G protein
Activation of PLC enzyme
Cleavage of PIP2 into IP3 and DAG
Release of Calcium
Smooth muscle contraction
Beta-2 receptor:
Stimulation of beta 2 receptor on smooth muscle cell
Activation of adenylate Cyclase
Increased of cAMP
Activation of protein kinase A
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Relaxation of smooth muscle
5. Indication:
Inotropic support
Cardiac failure
Open heart surgery
Cardiac stress testing
6. Contraindication:
Atrial fibrillation
Phaeochromocytoma
Ventricular arrhythmia
Hypersensitivity to dobutamine
7. Pharmacokinetic Parameters:
Onset of action is 2 min
Peak plasma conc of drug is 10 min after initiation of an IV infusion
Methylation and conjugation
Half life: 1-2 min
Excretion mainly through urine
9. Route of administration:
For IV use only
Because of its shorter half life it is administered as continuous IV infusion
10. Dosage :
Initial dose: 0.5 to 1 mcg/kg/min
Maintenance dose: 2 to 20 mcg/kg/min
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11. Dosage form:
4. Mechanism of Action:
At low doses it acts through the sympathetic nervous system to increase heart muscle
contraction force and heart rate, thereby increasing cardiac output and blood pressure. Higher
doses also cause vasoconstriction that further increases blood pressure.
5. Indication/Uses: Dopamine is a peripheral vasostimulant used to treat
low blood pressure,
low heart rate,
and cardiac arrest.
Low infusion rates (0.5 to 2 micrograms/kg per minute) act on the visceral vasculature
to produce vasodilation, including the kidneys, resulting in increased urinary flow.
6. Pharmacokinetic (ADME):
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Distribution: Once in the bloodstream, dopamine is distributed throughout the body, crossing
the blood-brain barrier to reach the central nervous system (CNS). It has a short half-life
meaning it is rapidly metabolized and eliminated from the body. Dopamine does not readily
cross the blood-brain barrier when administered peripherally, so its effects on the CNS are
primarily due to the endogenous dopamine produced by the brain.
Excretion: Dopamine and its metabolites are mainly excreted through the kidneys via urine.
The rate of excretion depends on various factors, including kidney function and urine pH.
8. Route of Administration:
Dopamine HCl Injection is administered (only after dilution) by intravenous infusion.
9. Contraindication:
Dopamine should not be used in patients with pheochromocytoma, in patients with uncorrected
tachyarrhythmias or ventricular fibrillation.
injectable solution
• 40mg/mL
• 80mg/mL
• 160mg/mL
•
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Drug # 13: Floroquinolone
1. Generic name:- Ciprofloxacin
3. Class:-
Fluoroquinolones are a class of antibiotics to which moxifloxacin belongs. They are often used
to treat bacterial infections by inhibiting the bacterial DNA gyrase enzyme.
5. Indications:-
Moxifloxacin, a fluoroquinolone, is commonly indicated for treating various bacterial
infections such as respiratory tract infections, skin and soft tissue infections, and intra-
abdominal infections. It may also be used to treat certain types of eye infections when
formulated as an ophthalmic solution. However, specific indications can vary.
6. Pharmacokinetics:-
Moxifloxacin is well absorbed orally and reaches peak plasma concentrations within a few
hours after administration. It has good tissue penetration, allowing it to distribute effectively
into various body tissues and fluids.
Metabolism of moxifloxacin is primarily hepatic, with a significant portion of the drug excreted
unchanged in the urine. The elimination half-life is approximately 12 hours, contributing to a
once-daily dosing regimen for some indications.
The duration of action can vary depending on the specific condition being treated, but the
sustained levels of moxifloxacin in the body contribute to its efficacy with once-daily dosing
in many cases.
Moxifloxacin, like other Fluoroquinolones, may be associated with various adverse drug
reactions (ADRs). Common ADRs include gastrointestinal symptoms such as nausea and
diarrhea, as well as central nervous system effects like dizziness and headache.
Serious ADRs may include tendonitis or tendon rupture, especially in older adults. There may
also be an increased risk of Clostridium difficile-associated diarrhea.
8. Route of administration:-
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It's typically taken orally in tablet form, but it can also be administered intravenously.
9. Contraindications:-
The dosage of moxifloxacin can vary based on the specific infection being treated, the severity
of the condition, and individual patient factors. Standard dosages often range from 400 mg to
800 mg once daily, either orally or intravenously.
**CNS Effects:** Be vigilant for central nervous system effects such as dizziness or
lightheadedness, especially in elderly patients, as moxifloxacin may cause these
symptoms.
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Trade Name: Lasix, Basix, Duride etc.
3. Classification:
Furosemide belongs to a class of medications known as loop diuretics. Diuretics
are drugs that promote diuresis, which is the increased production of urine. Loop
diuretics specifically act on the loop of Henle, a part of the nephron in the
kidneys, to inhibit the reabsorption of sodium and chloride ions.
5. Indication:
Edema associated with congestive heart failure
cirrhosis of the live
renal disease
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Hypertension, either alone or in combination with other antihypertensive agents.
6. PK Profile (ADME):
Absorption: Furosemide is well-absorbed orally, with peak plasma
concentrations occurring within 1-2 hours.
Distribution: It is distributed throughout the body, including the kidneys.
Metabolism: Furosemide undergoes minimal hepatic metabolism.
Excretion: The majority of the drug is excreted unchanged in the urine.
7. Route of Administration:
Furosemide is commonly administered orally, but it can also be given
intravenously for rapid diuresis.
8. Contraindication:
Hypersensitivity to Furosemide or any component of the formulation.
Anuria (lack of urine production).
Severe electrolyte depletion.
9. Adverse Drug Reactions (ADRs):
Electrolyte imbalances (hypokalemia, hyponatremia)
Dehydration
Hypotension
Dizziness
Ototoxicity (especially with rapid intravenous administration)
10. Dose and Dosage Form:
The dosage of Furosemide depends on the patient's condition and response to
therapy.
Typical doses range from 20 mg to 80 mg orally, once or twice daily.
Dosage forms include tablets and oral solutions for oral administration, and
injectable solutions for intravenous use.
11. Special Instruction Considerations:
Patients taking Furosemide should be monitored regularly for electrolyte levels,
renal function, and blood pressure.
It should be used cautiously in patients with hepatic impairment, as it may
exacerbate hepatic encephalopathy.
Patients should be advised to take the medication early in the day to prevent
nocturia.
In cases of intravenous administration, it should be given slowly to minimize
the risk of ototoxicity and hypotension.
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Drug # 15: Lactulose
1. Generic Name: Lactulose
2. Trade Name: Duphalac, Constilac, Enulose
3. Classification: Laxative, Osmotic laxative
4. Mechanism of Action:
Lactulose is a synthetic disaccharide that is not absorbed in the small intestine. It passes into
the colon where it is broken down by bacteria into organic acids, primarily lactic acid and acetic
acid. This acidification of the colonic contents leads to an increase in osmotic pressure, which
draws water into the colon and softens the stool. Additionally, the acidic environment inhibits
the growth of ammonia-producing bacteria, making lactulose useful in the treatment of hepatic
encephalopathy.
5. Indications:
Lactulose is indicated for the treatment of constipation, particularly in patients with chronic
constipation or opioid-induced constipation. It is also used in the management of hepatic
encephalopathy to reduce serum ammonia levels.
6. Contraindications:
Lactulose is contraindicated in patients with galactosemia, intestinal obstruction, or a history
of hypersensitivity to lactulose.
7. Pharmacokinetic Profile:
Lactulose is minimally absorbed from the gastrointestinal tract, with less than 3% of the dose
being absorbed. It undergoes bacterial fermentation in the colon, leading to its pharmacological
effects.
8. Adverse Reactions:
Common adverse reactions include flatulence, abdominal discomfort, cramps, and diarrhea.
Prolonged use or excessive dosage may lead to electrolyte imbalance and dehydration.
9. Route of Administration:
Lactulose is administered orally.
10. Dosage:
Children: The dosage for children varies depending on age and weight, typically ranging from
2.5 to 15 mL daily, divided into two or three doses.
Adults: The initial dosage for adults is usually 15 to 30 mL daily, adjusted based on individual
response. Maintenance doses may range from 15 to 60 mL daily.
11. Dosage Form:
Lactulose is available as an oral solution and oral powder for reconstitution.
12. Special Instructions:
Patients should be advised to drink plenty of fluids while taking lactulose to prevent
dehydration. It may take up to 48 hours for lactulose to produce a laxative effect, so patients
should not increase the dosage prematurely. Additionally, in patients with hepatic
encephalopathy, serum ammonia levels should be monitored regularly during treatment.
29
Drug # 16: Macrolides
Macrolides constitute a class of antibiotics distinguished by a macrocyclic lactone ring,
exhibiting a diverse spectrum of antimicrobial activity. Renowned for their efficacy,
tolerability, and broad-spectrum coverage against Gram-positive and select Gram-negative
bacteria, macrolides serve as cornerstone agents in the treatment of various bacterial infections.
This comprehensive exposition delves into the pharmacology, mechanism of action, spectrum
of activity, clinical applications, adverse effects, and notable examples of macrolide antibiotics.
30
Hepatotoxicity: Rare cases of reversible hepatotoxicity, with elevated liver enzymes and
hepatitis.
Allergic Reactions: Rash, urticaria, anaphylaxis.
Drug Interactions: Interaction with drugs metabolized by the cytochrome P450 system,
leading to altered drug levels and potential toxicity or decreased efficacy.
7. Route of Administration:
Oral, intravenous, or topical administration depending on the specific macrolide and the
indication.
8. Contraindications:
Hypersensitivity to macrolides or any component of the formulation.
History of QT prolongation or ventricular arrhythmias.
Concomitant use with certain medications metabolized by the cytochrome P450 system.
9. Dosage:
Dosage varies depending on the specific macrolide, the severity of the infection, and patient
factors such as age and renal function.
10. Special Instructions/Considerations:
Monitor liver function tests periodically during therapy.
Use with caution in patients with known QT prolongation or risk factors for arrhythmias.
Assess for potential drug interactions, especially with other medications metabolized by the
cytochrome P450 system.
11. Dosage Form:
Macrolides are available in various dosage forms, including tablets, capsules, oral suspensions,
intravenous solutions, and topical formulations.
Notable Examples of Macrolides:
Erythromycin: Effective against Gram-positive and some Gram-negative bacteria, commonly
used for respiratory tract infections, skin and soft tissue infections, and certain sexually
transmitted infections.
Azithromycin: Broad-spectrum macrolide with a long half-life, used for respiratory tract
infections, including atypical pneumonia, and genital infections caused by Chlamydia
trachomatis.
Clarithromycin: Semi-synthetic macrolide with enhanced activity against Gram-negative
bacteria compared to erythromycin, frequently used for respiratory tract infections,
Helicobacter pylori eradication therapy, and skin and soft tissue infections.
31
Drug # 17: Metoclopramide
Metoclopramide is an antiemetic agent and dopamine D2 antagonist used in the treatment of
gastro esophageal reflux disease, prevention of nausea and vomiting, and to stimulate gastric
emptying.
1. Brand Name:
Maxolon
Clopra syrup
Generic Name:
Metoclopramide
2. Class of Drug:
D2 receptor antagonist; 5-HT3 receptor antagonist; 5-HT4 receptor agonist; Prolactin releaser
3. Mechanism of Action:
metoclopramide causes antiemetic effects by inhibiting dopamine D2 and serotonin 5-HT3
receptors in the chemoreceptor trigger zone (CTZ) located in the area postrema of the brain.
Administration of this drug leads to prokinetic effects via inhibitory actions on presynaptic and
postsynaptic D2 receptors, agonism of serotonin 5-HT4 receptors, and antagonism of
muscarinic receptor inhibition. This action enhances the release of acetylcholine, causing
increased lower esophageal sphincter (LES) and gastric tone, accelerating gastric emptying and
transit through the gut. Metoclopramide antagonizes the dopamine D2 receptors. Dopamine
exerts a relaxant effect on the gastrointestinal tract through binding to muscular D2 receptors.
4. Indications:
The FDA has approved metoclopramide to treat nausea and vomiting in patients with
gastroesophageal reflux disease (in patients who fail to respond to established therapy) and
diabetic gastroparesis by increasing gastric motility. Parenteral metoclopramide is also FDA-
approved to control nausea and vomiting in chemotherapy patients.
Metoclopramide is used off-label prophylactically to prevent nausea and vomiting in
postoperative patients when nasogastric suction is contraindicated or unavailable.
Metoclopramide is also used off-label to treat acute migraine in the emergency department.
5. Pharmacokinetics of Drug:
Absorption
Metoclopramide is rapidly absorbed in the gastrointestinal tract with an absorption rate
of about 84%.
The bioavailability of the oral preparation is reported to be about 40.7%, but can range
from 30-100%.
Nasal metoclopramide is 47% bioavailable. A 15mg dose reaches a Cmax of 41.0
ng/mL, with a Tmax of 1.25 h, and an AUC of 367 ng*h/mL.
Distribution:
Volume of distribution is approx 3.5L/kg. It is 30% bound to the plasma protein, mainly
to alpha 1-acid glycoprotein.
Metabolism
Metoclopramide undergoes first-pass metabolism and its metabolism varies according
to the individual. This drug is metabolized by cytochrome P450 enzymes in the liver.
CYP2D6 and CYP3A4 both contribute to its metabolism, with CYP2D6 being more
heavily involved. CYP1A2 is also a minor contributing enzyme. The process of N-4
sulfate conjugation is a primary metabolic pathway of metoclopramide.
Elimination
About 85% of an orally administered dose was measured in the urine within 72 hours
during a pharmacokinetic study. An average of 18% to 22% of 10-20 mg dose was
recovered as a free drug within 3 days of administration.
6. ADRs:
32
Common adverse drug reactions (ADRs) associated with metoclopramide therapy includes
restlessness (akathisia), and focal dystonia. Infrequent ADRs include hypertension,
hypotension, hyperprolactinemia leading to galactorrhea, headache, and extrapyramidal effects
such as oculogyric crisis.
7. Route of administration:
Oral:
Syrup
Tablets
Injection
IV administration
IM administration
IntrNasal Administration
8. Contraindications:
Metoclopramide is contraindicated in patients with the following:
Known hypersensitivity to metoclopramide or excipients
Gastrointestinal bleeding
Obstruction
Perforation
Other contraindications include the following:
Pheochromocytoma
Seizures
Depression
Parkinson disease
9. Dosage form:
Injectable solution
• 5 mg/mL
Syrup
• 5 mg /5 mL
Tablet
• 5 mg
• 10 mg
Dispersible tablets
• 5 mg
• 10 mg
10. Dosage:
For oral dosage forms (solution or tablets)
For diabetic gastroparesis:
Adults—At first, 10 milligrams (mg) four times a day, taken 30 minutes before each
meal and at bedtime for 2 to 8 weeks. Your doctor may adjust your dose as needed.
However, the dose is usually not more than 40 mg.
Children—Use and dose must be determined by your doctor.
For gastroesophageal reflux disease (GERD):
Adults—At first, 10 to 15 milligrams (mg) four times a day, taken 30 minutes before
symptoms are likely to begin or before each meal and at bedtime, for 4 to 12 weeks.
Your doctor may adjust your dose as needed. However, the dose is usually not more
than 60 mg perday.
Children—Use and dose must be determined by your doctor.
33
Usual Adult Dose for Radiographic Exam:
Adults and pediatric patients greater than or equal to 14 years: 10 mg IV as a single dose
administered over 1 to 2 minutes to facilitate gastric emptying where delayed gastric emptying
interferes with radiological examination of the stomach and/or small intestine.
Usual Adult Dose for Nausea/Vomiting -- Chemotherapy Induced:
IV infusion: 1 to 2 mg/kg/dose (depending on the emetogenic potential of the agent) IV (infused
over a period of not less than 15 minutes) 30 minutes before administration of chemotherapy.
The dose may be repeated twice at 2 hour intervals following the initial dose. If vomiting is
still not suppressed, the same dose may be repeated 3 more times at 3 hour intervals.
For doses higher than 10 mg, the injection should be diluted in 50 mL of a parenteral solution.
Normal saline is the preferred diluent. If acute dystonic reactions occur, 50 mg of
diphenhydramine hydrochloride
may be injected IM.
34
4. Mechanism of action :
5. Pharmacokinetics
Absorption:
Morphine is absorbed in the alkaline environments of the upper intestine and
rectal mucosa.
The bioavailability of morphine is 80-100%. Morphine reaches steady-state
concentrations after 24-48 hours.
Parenteral morphine has a Tmax of 15 minutes and oral morphine has a Tmax
of 90 minutes, with a Cmax of 283nmol/L.
The AUC of morphine is 225-290nmol h/L.
Volume of distribution:
The volume of distribution of morphine is 5.31L/kg.
Protein binding:
Morphine is 35% protein-bound, the metabolite morphine-3-glucuronide is 10%
protein-bound, and morphine-6-glucuronide is 15% protein-bound.
Metabolism:
Morphine is 90% metabolized by glucuronidation by UGT2B7 and sulfation at
positions 3 and 6. Morphine can also be metabolized to codeine, nor-morphine, and
morphine ethereal sulfate.
Route of elimination
70-80% of an administered dose is excreted within 48 hours. Morphine
is predominantly eliminated in the urine with 2-10% of a dose recovered
as the unchanged parent drug. 7-10% of a dose of morphine is eliminated
in the feces.
Half-life
Morphine has a half-life of 2-3 hours.
Clearance
The apparent clearance of intravenous or subcutaneous morphine is 1600
mL/min
Toxicity
The LD50 is 0.78µg/mL in males and 0.98µg/mL in females.
6. Route of Administration
Following are the routes of administration for morphine:
35
Oral Route: Morphine is available in tablet and capsule form, given every 4
to 6 hours. Intermediate release and extended release.
Intramuscular (IM) or Subcutaneous (SC): Given for faster pain relief every
4 to 6 hours.
5 to 15 mg 10 (10) 4 hourly IM
9. Contraindications of Morphine:
36
Morphine is contraindicated in conditions like Respiratory disease, Biliary colic,
Raised intracranial pressure, Coronary perfusion disorder, and Head injury.
Drug should not be given to patients suffering from Kidney dysfunction.
10. Special Considerations for Morphine:
Morphine should be used with caution in patients with central nervous system (CNS)
depression, convulsive disorder, ulcerative colitis, fever, recent gastrointestinal (GI)
surgery, brady arrhythmias, supraventricular tachycardia, and pulmonary diseases.
Patients should exercise caution while driving or performing tasks requiring alertness
because it may produce drowsiness.
37
blood flow more easily and lowers blood pressure. Lower blood pressure reduces the
strain on your heart.
1. Generic Name:
Nifedipine
2. Brand Name: Adalat
3. Classification:
Nifedipine is a Dihydropyridine Calcium Channel Blocker (CCB).
4. Mechanism of Action:
Nifedipine acts as a calcium channel blocker, specifically targeting L-type calcium
channels in vascular smooth muscle cells and cardiac myocytes.
It inhibits calcium influx through these channels, leading to peripheral vasodilation by
preventing smooth muscle contraction, thereby reducing systemic vascular resistance
and lowering blood pressure.
Nifedipine also promotes coronary artery vasodilation, enhancing myocardial oxygen
supply and relieving angina symptoms.
While it exhibits negative chronotropic and inotropic effects to a lesser extent, its
primary action is centered on vasodilation and arterial compliance improvement.
These mechanisms collectively contribute to its efficacy in managing hypertension
and angina pectoris.
5. Indications:
Hypertension: Nifedipine is indicated for the treatment of hypertension, lowering
blood pressure by inducing peripheral vasodilation.
Angina Pectoris: It is used to manage chronic stable angina and variant angina,
relieving angina symptoms and improving exercise tolerance.
Raynaud's Phenomenon: Nifedipine may be prescribed to alleviate symptoms such
as cold fingers and toes associated with Raynaud's phenomenon by promoting
peripheral vasodilation and enhancing blood flow.
38
6. PK Profile
7. ADRs:
8. Route of Administration:
Route of
Administration Description
Immediate-
release Available for specific indications or situations such as hypertensive
Formulations emergencies, although less common due to associated risks.
9. Contraindications:
Contraindication Description
39
Contraindication Description
Pregnancy and Use during pregnancy or lactation only if benefits outweigh risks;
Lactation consult a healthcare provider.
Extended-Release Available for once-daily dosing in various strengths (e.g., 30 mg, 60 mg,
Tablets 90 mg).
40
Drug # 20: NSAIDS
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of medications widely
used to relieve pain, reduce inflammation, and lower fever. They work by inhibiting the
activity of cyclooxygenase enzymes (COX-1 and COX-2), which are involved in the
production of prostaglandins, substances that contribute to pain and inflammation.
NSAIDs are commonly used to manage various conditions such as arthritis, menstrual
cramps, headaches, and musculoskeletal injuries.
1. Brand and Generic Names:
Generic Brand
2. Mechanism of Action:
COX Inhibition: NSAIDs block cyclooxygenase (COX) enzymes, particularly
COX-1 and COX-2.
Prostaglandin Reduction: By inhibiting COX enzymes, NSAIDs decrease
prostaglandin synthesis, which mediates inflammation, pain, and fever.
Analgesia: NSAIDs alleviate pain by reducing prostaglandin levels, thereby
diminishing pain perception.
Anti-inflammatory: NSAIDs curb inflammation by lowering prostaglandin
production, mitigating swelling and discomfort.
Antipyretic: NSAIDs lower fever by inhibiting prostaglandins in the
hypothalamus, regulating body temperature.
3. Route of Administration:
Oral administration is the most common route for NSAIDs, with many available
in tablet, capsule, or liquid form for ease of ingestion.
Some NSAIDs may also be available in topical formulations for localized pain
relief, applied directly to the skin over the affected area.
41
4. Indications:
NSAIDs are primarily indicated for the management of pain, inflammation, and
fever associated with various conditions such as arthritis, musculoskeletal injuries,
and headaches.
They are often used as first-line agents in the treatment of mild to moderate pain,
including acute and chronic pain syndromes.
5. Special Considerations:
Caution should be exercised in patients with a history of gastrointestinal ulcers or
bleeding, as NSAIDs can increase the risk of gastrointestinal adverse effects.
Patients with renal impairment or heart failure require careful monitoring when
using NSAIDs, as these medications can affect renal function and fluid balance.
Long-term use of NSAIDs, especially at high doses, should be approached
cautiously due to the potential for cardiovascular events and renal toxicity.
6. Contraindications:
NSAIDs are contraindicated in patients with a history of hypersensitivity reactions
to these medications or other components of the formulation.
They should be avoided in individuals with a history of gastrointestinal bleeding,
peptic ulcer disease, or inflammatory bowel disease.
Use of NSAIDs is contraindicated in the setting of perioperative coronary artery
bypass graft (CABG) surgery due to the increased risk of cardiovascular events.
7. Pharmacokinetics and Dynamics:
Tmax (Time to Peak Plasma Concentration): Tmax varies among different
NSAIDs and formulations, typically ranging from 1 to 4 hours after oral
administration.
Cmax (Peak Plasma Concentration): Cmax also varies depending on the
specific NSAID and dosage form but generally occurs within a few hours after
administration.
Volume of Distribution (Vd): Vd represents the theoretical volume in which the
total amount of drug would need to be uniformly distributed to produce the
observed plasma concentration. It varies widely among NSAIDs due to differences
in their physicochemical properties.
Area Under the Curve (AUC): AUC reflects the total systemic exposure to the
drug over time and is influenced by factors such as absorption, distribution,
metabolism, and elimination.
Half-Life: The half-life of NSAIDs varies widely, ranging from a few hours to
several days, depending on factors such as drug potency, metabolism, and renal
clearance.
42
8. Dosage form:
Trade: Various commercial brands exist globally, with names like Pedialyte, Rehidrat,
Dioralyte, etc.
2. Class:
Electrolyte and carbohydrate replacement therapy
3. MOA:
Replaces fluids and electrolytes lost through diarrhea, vomiting, or other illnesses.
Sugar promotes water absorption through the intestines.
Electrolytes maintain fluid balance and essential mineral levels.
4-Indications:
Treatment of dehydration caused by diarrhea, vomiting, or other illnesses leading
to fluid loss.
Prevention of dehydration in high-risk groups, especially children under 5.
5. PK (ADME):
Absorption: Rapidly absorbed from the intestines into the bloodstream.
Distribution: Distributed throughout body fluids.
Metabolism: Electrolytes and carbohydrates are used by the body for various functions.
Elimination: Excess fluids and electrolytes are excreted through urine and feces.
6. Route of administration:
Oral administration, given in small, frequent sips.
7. ADR
Generally well-tolerated in most individuals.
Potential for electrolyte imbalance with improper dilution or use.
Mild gastrointestinal discomfort in some cases (e.g., bloating, nausea).
8. Contra indications:
Severe dehydration requiring intravenous fluids.
Known intestinal blockage or perforation.
Severe intolerance to any ingredient in ORS.
9. Dosage form/ Dosage:
Pre-mixed solutions sold in packets, sachets, or bottles.
43
Homemade versions can be prepared using specific recipes and precise
measurements.
Dosage varies depending on age, severity of dehydration, and individual needs.
10. Special considerations:
Follow precise instructions for preparation and administration, especially for
homemade solutions.
Store pre-mixed solutions according to product recommendations.
Seek medical attention if severe dehydration, persistent symptoms, or concerns
arise.
Do not use as a substitute for breastfeeding or formula in infants.
3. Mechanism of action.
Penicillin kills bacteria through binding of the beta-lactam ring to DD-transpeptidase,
inhibiting its cross-linking activity and preventing new cell wall formation
4. Indication
44
Penicillin V potassium is used to treat certain infections caused by bacteria such as
pneumonia and other respiratory tract infections, scarlet fever, and ear, skin, gum, mouth,
and throat infections.
Descriptions. Penicillin G benzathine injection is used to treat bacterial infections (eg,
mild to moderate infections of the upper respiratory tract, syphilis, yaws, bejel, pinta). It
is also used to prevent rheumatic fever, chorea, rheumatic heart disease, or acute
glomerulonephritis. This medicine is an antibiotic.
5. Pharmacokinetic profile:
6. ADR’s
Hypersensitivity Reactions: The commonly encountered adverse drug reaction
with penicillin is hypersensitivity of immediate onset or delayed onset.
Immediate onset: This kind of reaction occurs within 20 minutes post-
administration. It is characterized by urticaria, pruritis, edema, laryngospasm,
bronchospasm, hypotension, vascular collapse, and death.
Delayed onset: This reaction occurs within 1 to 2 weeks of treatment. It is rare
and is characterized by fever, malaise, urticaria, myalgia, arthralgia, abdominal
pain, and skin rashes.
Gastrointestinal System: GI symptoms were the most common and were
reported in over 1% of patients, including nausea, vomiting, stomatitis, which are
commonly observed with oral administration. Pseudomembranous colitis is also
observed during or after the treatment.
Hematologic Reactions: If the dose is exceeded 10 million units/day and if a
patient has received a higher dose previously, then those patients can precipitate
Coombs positive hemolytic anemia and neutropenia, which is resolved when
therapy is stopped.
Metabolic Reactions: The salt form of penicillin G may cause electrolyte
imbalances, i.e., hyperkalemia when given IV in a large dose.
Nervous System: Neurological manifestations include hyperreflexia, myoclonic
twitches, seizures, and coma after IV doses and are more likely in patients with
impaired renal function.
Urogenital System: Urological manifestations with large IV doses include renal
tubular damage. The penicillins can also cause acute interstitial nephritis, a disease
characterized by inflammation of the tubules and interstitium of the kidneys.[15]
Acute interstitial nephritis can also present with hematuria, fever, and rash. The
recommendation is to withdraw the drug as the disease could lead to renal failure
in this situation.
Other: Jarisch- Herxheimer reaction is precipitated when penicillin is administered
in patients with syphilis.
Drug-Drug Interactions
Concurrent sulfonamides, erythromycin, chloramphenicol should be avoided due
to antagonistic effects.
Tubular secretion of penicillin G can be blocked by probenecid- higher and longer
plasma concentrations are achieved. Probenecid also decreases the volume of
distribution of penicillin.
45
Drugs like aspirin, phenylbutazone, sulfonamides, indomethacin, thiazide,
furosemide, and ethacrynic acid increase the half-life of penicillin by competing
with tubular secretion
7. Route of adminstration.
Nearly all antibacterial agents have been linked to Clostridium difficile associated
diarrhea (CDAD), including penicillin, with severity ranging from mild diarrhea to fatal
colitis. This strain produces toxins A and B that contribute to the development of CDAD.
During infections caused by hyper toxin-producing strains of C. Difficile, the rate of
morbidity and mortality can be increased since these infections are often resistant to
antimicrobial treatments and may require colectomy.
Neurosyphilis: 2.4 million units IM qDay x10-14 days; administer with probenecid 500
mg PO QID (penicillin G aqueous preferred)
Anthrax
46
Cutaneous: 600,000-1,000,000 units IM qDay
Inhaled (post-exposure): 1.2 million units IM q12hr for up to 2 weeks, THEN switch to
PO treatment (total treatment 60 days)
Diphtheria
Adjunct with antitoxin: 300,000-600,000 units IM qDay
Carrier state: 300,000 units IM qDay
Vincent’s Infection (fusospirochetosis)
600,000-1,000,000 units IM qDay
Erysipeloid
600,000-1,000,000 units IM qDay
Rat-Bite Fever
Indicated for Streptobacillus moniliformis and Spirillum minus (rat-bite fever)
600,000-1,000,000 units IM qDay
Whipple’s disease
1.2 million units IM qDay for 10-14 days; coadminister with streptomycin, THEN
Trimethoprim/sulfamethoxazole or doxycycline PO for 1 yr
47
Intravenous (IV): For rapid systemic effect, often used in severe cases or
emergencies.
Intramuscular (IM): For long-acting effect, especially when oral administration
is not feasible.
Topical: For localized inflammation, such as in skin conditions or eye problems.
Inhalation: For respiratory conditions like asthma.
48
Syrups: Available in concentrations like 1 mg/mL or 5 mg/mL.
Creams: Strengths may vary depending on the specific condition being treated.
Ointments: Similar to creams, strengths vary based on the intended use.
Eye drops: Typically come in concentrations of 0.1% or 1%.
Inhalers: Metered-dose inhalers deliver specific amounts of medication per puff.
49
4. Mechanism of Action:
The mechanism of action Salbutamol, or albuterol, primarily works by
binding to and activating beta-2 adrenergic receptors in the smooth muscle cells of the
lungs. This activation leads to the relaxation of these muscles, resulting in bronchodilation
and improved airflow. Additionally, salbutamol can inhibit the release of inflammatory
mediators and increase the clearance of mucus from the airways.
5. Indications:
Salbutamol, also known as albuterol, is commonly prescribed for the treatments:
Asthma
Chronic obstructive pulmonary disease (COPD)
Respiratory conditions
It's used to relieve symptoms such as wheezing
Shortness of breath
Chest tightness
Coughing
6. Pharmacokinetics of salbutamol :
The pharmacokinetics of salbutamol involve rapid absorption after inhalation, with peak
plasma concentrations reached within 1 to 2 hours. It has a relatively short duration of
action, typically around 4 to 6 hours. Salbutamol undergoes extensive metabolism in the
liver, primarily via sulfation and glucuronidation, and is excreted mainly in the urine as
inactive metabolites.
7. Adverse Drug reactions :
Common adverse drug reactions (ADRs) associated with salbutamol include:
Tremor: Especially in the hands.
Palpitations: Increased heart rate or awareness of heartbeat.
Headache: Mild to moderate headaches may occur.
Tachycardia: Rapid heart rate.
Nervousness: Feelings of anxiety or restlessness.
8. Route of administration: Salbutamol can be administered:
Inhalar
Orally : Tablets and syrups
Parenterally : IV , IM injections
9. Contraindications:
Hypersensitive
Cardiovascular conditions
Hyperthyroidism
Severe hypertension
Diabetes
Pregnancy and breastfeeding
10. Dosage:
Adult dose
Metered-Dose Inhaler (MDI):
For acute asthma symptoms: 2 inhalations (100-200 mcg per inhalation) every 4-
6 hours as needed. The maximum dose should not exceed 8 inhalations in 24 hours.
50
For prevention of exercise-induced bronchospasm: 2 inhalations 15-30 minutes
before exercise.
Nebulizer Solution:
The usual dose is 2.5 mg to 5 mg (0.083% or 0.5% solution) administered via
nebulization every 4-6 hours as needed. The maximum dose should not exceed 20
mg in 24 hours.
Extended-Release Tablets:
The typical dosage is 4 mg orally every 12 hours. However, dosing may vary based
on individual response and physician recommendations.
Neonatal dose :
Intravenous: 4 micrograms/kg IV over 10 minutes.
Nebulized endotracheal: 400 microgram 2 hrly, maximum 12 doses.
51
2. Trade Name: Vancocin
4. Mechanism of action:
When it reaches the cell wall of an actively dividing susceptible gram-positive bacterium,
vancomycin binds to the acyl-D-ala-D-ala portion of the growing cell wall. After binding,
it prevents the cell wall from forming the cross-linking necessary to keep it strong.
5. Indications:
Vancomycin is indicated in adult and pediatric patients for the treatment of septicemia,
infective endocarditis, skin and skin structure infections, bone infections, and lower
respiratory tract infections.
6. Pharmacokinetics:
Absorption:
Oral vancomycin has a bioavailability of less than 10%.
Onset of action:
Vancomycin has a rapid onset of action with a serum peak concentration immediately
following the completion of the intravenous infusion. The onset of action of oral
vancomycin is currently unknown.
Distribution:
large volume of distribution (0.4 L/kg to 1.0 L/kg) in body tissues and fluids, excluding
cerebrospinal fluid (CSF) with non-inflamed meninges
Protein Binding:
approximately 55%
Half-life: Vancomycin has a bi-phasic elimination half-life, with its initial half-life being
relatively quick and a terminal half-life of 4 to 6 hours in healthy adults with normal renal
function. The elimination half-life is significantly prolonged in patients with renal
dysfunction. Close monitoring is necessary for these patients.
8. Side effect:
Nausea or stomach upset may occur
Dizziness
Hearing problems
Easy bruising/bleeding
signs of kidney problems (such as changes in the amount of urine).
9. Route of administration:
52
Intravenous, oral, rectal administration, since vancomycin hydrochloride is irritating to
tissue and causes drug fever, pain and possibly necrosis it should never be injected
intramuscularly.
10. Contraindication:
vancomycin hydrochloride is contraindicated in patients with known hypersensitivity to
vancomycin, or any other excipients or in patients with previous anaphylaxis or major
allergy with other glycopeptides.
Patients are at a higher risk for developing AKI if they have underlying renal function
impairment.
- 250mg
- 750mg
- 1g
- 5g
- 10g
- 7.5g
- 10.5g
- 15g
- 750mg/150mL
- 1g/200mL
- 1.25g/250mL
- 1.5g/300mL
- 1.75g/350mL
- 2g/400mL
53
3 Standard Clinical cases
1) Hypertension
Mr. JS is a 55-year-old male who presents to the clinic with a chief complaint of frequent
headaches and occasional dizziness. He reports that these symptoms have been bothering
him for the past few months. He describes the headaches as throbbing in nature, primarily
occurring in the mornings and sometimes accompanied-by nausea. He also mentions a
family history of hypertension-and-heart disease.
Medical History
➢ Vital Signs:
➢ Physical Examination:
➢ Obese appearance
➢ Extremities: No edema
➢ Laboratory Findings:
➢ Urinalysis: Normal
Questions:
1.What is the most likely diagnosis based on John Smith's presenting symptoms and
54
medical history?
Considering John Smith's symptoms and medical history, the likely diagnosis is
uncontrolled
hypertension accompanied by symptoms like headaches and occasional dizziness.
2 .What is the significance of John's family history of hypertension and heart disease
John's family history of hypertension and heart disease indicates a genetic
predisposition to cardiovascular conditions, underscoring the importance of
effective management strategies.
3.Evaluate John's current blood pressure reading. Is it within the recommended
target.
range for hypertensive patients, and how would you classify his hypertension
according to guidelines?
John's blood pressure reading of 160/95 mm Hg exceeds the recommended target range
for
hypertensive patients, classifying his hypertension as Stage 2 according to guidelines.
4. Review John's current antihypertensive medication, Losartan 50 mg daily. Is this
an appropriate initial treatment, and should any changes be considered?
Initiation of Losartan 50 mg daily is appropriate, but considering his elevated blood
pressure, dosage adjustment or additional medication may be necessary for better control.
5. What lifestyle modifications would you recommend to John for managing his
hypertension?
Lifestyle modifications for John should include weight loss through regular exercise and
a low sodium diet, reduction of alcohol consumption, and stress management techniques
like meditation or yoga to help lower blood pressure and improve overall cardiovascular
health.
6.Interpret John's laboratory findings, including fasting blood glucose, cholesterol
levels, and serum creatinine. How do these values contribute to his overall
cardiovascular risk?
John's laboratory results show slightly elevated fasting blood glucose, high cholesterol
levels, and normal serum creatinine, indicating increased cardiovascular risk due to
potential metabolic syndrome and dyslipidemia.
7. What additional diagnostic tests or assessments, If any, would you recommend for
Johns' hypertension evaluation?
Additional diagnostic tests such as ambulatory blood pressure monitoring,
echocardiogram, and renal function tests may be warranted to assess for target organ
damage and secondary causes of hypertension.
8. Discuss the potential reasons for John's morning headaches and occasional
dizziness. Could they be related to his hypertension?
These symptoms could be related to John's hypertension, possibly due to increased
intracranial pressure from elevated blood pressure levels exacerbated by poor lifestyle
habits.
9. What are the primary goals of treatment for John's hypertension, and how would
you monitor his progress in achieving these goals?
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The primary goals of treatment involve lowering John's blood pressure to target levels,
reducing cardiovascular risk, and preventing target organ damage. Monitoring progress
includes regular, blood pressure checks, assessing medication adherence, lifestyle
modifications, and evaluating for any adverse effects.
2) Asthma
HT, a 32-year-old woman, 155 cm, 81 kg; presented to hospital casualty with a history of
increased breathlessness and wheezing, over the last 5days. She is known to have had
asthma for 20 years and has smoked 10 cigarettes per day since the age of 15. Her last
hospital admission was one month ago. She works in a small ‘do-it-yourself’ shop, as a
counter assistant. HT lives in a tenth-floor council flat; she is single. On medical
examination, the following is found:
❖ Not able to speak in sentences – stops for breath after Two words
5. List the medicines available for the acute treatment of asthma and describe the
method of administration.
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Medicines like inhalers with short-acting beta-agonists (like salbutamol) are used for
quick relief. Corticosteroids (like prednisolone) are taken by mouth, and ipratropium
bromide is used as an inhaler.
6. Describe the role of the pharmacist in the care of this patient.
Pharmacists help by teaching patients how to use inhalers correctly, making sure they
take their medicines as prescribed, and giving advice on managing asthma triggers.
7. What are the aims of asthma treatment for the patient and the professional?
Patients want relief from symptoms, fewer flare-ups, and a better quality of life.
Professionals aim to help patients control their asthma well by giving personalized
treatment plans and educating them about managing their condition.
8. Explain the social issues this patient will face on discharge.
After leaving the hospital, the patient might face challenges like finding suitable housing,
getting help to quit smoking, and dealing with asthma triggers at work.
9. Critically review the non-pharmacological therapies that are available for people
with asthma. Would these be of benefit to this patient?
Non-medical treatments like avoiding triggers, staying away from smoke, and managing
stress can help some people with asthma. These might be helpful for this patient too.
10. Discuss the role of an asthma management plan for this patient.
An asthma management plan is like a roadmap for patients, showing them how to watch
for symptoms, what medicines to take, and what to do if their asthma gets worse. It helps
patients take charge of their asthma and stay healthy.
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3) Ulcerative colitis
Mrs. D has recently been admitted with an episode of acute severe ulcerative colitis. This
is her third flare this year. This time she has a 5-day history of bloody diarrhea with
abdominal pain. Onaverage, she passed her bowels seven times a day. She is currently
taking mesalazine 800 mg three times daily and prednisolone 20 mg daily. Mrs. also has
an elevated temperature of 38°C and a pulse rate of 92 bpm. She is due to have an
abdominal X-ray and a stool culture.
Biochemistry Findings
6. How should this flare be managed? Several days later you see Mrs. D, who is
distressed as she is not responding to treatment and she desperately wants to avoid
surgery. The consultant has suggested that ciclosporin may be an option, and she
asks to talk to you
about it.
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Flare management may involve adjusting medication doses, using steroids, and
monitoring for complications.
7. Why is surgery likely?
Surgery becomes likely if medical treatments fail or if complications like perforation or
severe bleeding occur.
8. What is the evidence for the use of ciclosporin.
Studies show that ciclosporin can be effective in severe cases of ulcerative colitis,
particularly when surgery is a concern.
9. What should you discuss with her about the use of ciclosporin?
Mrs. D should discuss potential side effects like kidney problems, high blood pressure,
and increased infection risk with her doctor before starting ciclosporin.
10. What dose of ciclosporin should she receive and how should it be given?
Mrs. D's doctor will determine the appropriate dose and how to administer ciclosporin
based on her individual situation.
11. What drugs would you expect her to be discharged on?
After discharge, Mrs. D may receive mesalazine, immunosuppressant like azathioprine,
and possibly a gradual reduction in prednisolone dosage.
12. What monitoring would you do?
Ongoing monitoring will involve checking inflammatory markers, kidney function, and
electrolyte levels to ensure treatment effectiveness and safety.
13. What counselling should she be given?
Mrs. D should be educated about the importance of sticking to her medication regimen,
recognizing signs of worsening symptoms, and understanding potential side effects.
14. What future treatment is she likely to receive?
Future treatment will likely involve long-term maintenance medications and regular
follow-up appointments to manage her condition effectively.
15. Do antibacterial have a role in ulcerative colitis?
Antibiotics are generally not used as the primary treatment for ulcerative colitis since it's
considered an inflammatory condition rather than an infectious one
Summary
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I started my clinical clerkship at Rehman Medical Institute(RMI) on 4th December which
comes to end on 22nd of January During Clinical Clerkship at RMI hospital has
highlighted the critical role pharmacists play in patient care. I have learned how to collect
cases from patients and different Medical departments. Moreover, I've learned about
medication management, including reconciliation and safety protocols, as well as
different drug distribution systems like unit dose and automated dispensing. Clinical
pharmacy services, such as therapy management and antimicrobial stewardship,
underscored the pharmacist's role in optimizing therapy. Pharmaceutical care planning
involves assessing patient needs and developing tailored care plans. Overall, hospital
pharmacy studies have equipped me with essential skills to provide safe and effective
pharmaceutical care in both inpatient and outpatient settings. During Hospital visits I
learned about Professional dealing with patients and other Health Care Professionals.
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1) Hypertension 2) Asthma 3) Ulcerative Colitis
Three cases were studied, each presenting unique challenges in healthcare management.
Hypertension was addressed with pharmacological and non-pharmacological
interventions based on NICE guidelines, focusing on ARBs and lifestyle modifications.
Asthma management involved quick-relief medications and essential tests for assessing
lung function, highlighting the pharmacist's role in patient education. Ulcerative colitis
posed difficulties despite initial treatment, leading to consideration of ciclosporin therapy,
emphasizing the importance of longterm monitoring and patient counseling for effective
disease management.
During classes, students presented topics. e.g. In-patient Flow, De range values and Drug
Dose Calculations. I have come to know that Inpatient pharmacy flow ensures efficient
medication management from admission to discharge, involving settlement, verification,
dispensing, counseling, and monitoring. Clinical assessment relies on reference ranges for
interpreting lab results and identifying health issues, crucial for accurate diagnosis and
treatment monitoring. These Values can be easily related to patent condition for disease
or infection identification, moreover before and after lab values must be keep in
consideration to know about either medication is working or not. Drug dose calculations
is important part of Intensive Care Unit (ICU). Different tasks must be performed in ICU
to ensure patient safety Dose Optimization, Dilutions, Fluid selection, Narcotic drugs,
anesthetic drugs and Sepsis management. I have learned about basic formulas needed for
calculations of High alert medications like Aminophyline, Amiodarone, Dopamine,
Epinephrine, Esmolol, and Bretylium.
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