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PHARMACOKINETICS - a process by which cells carry a drug across

their membrane by engulfing the drug particles


The drug needs to be a solution first to cross the into a vesicle.
biologic membrane of the cell.
TAKE NOTE:
- If drug is administered parentally- subcu,
intramuscular, intrav- no need to make it The mucous membrane of the GI lining is composed of
into a solution. lipids or fats and protein. Lipid-soluble drug can pass
rapidly through the mucous membrane, water-soluble
Pharmacokinetic Phase dug need a carrier (enzyme or protein). Large particles
-the process of drug movement throughout the body that are non-ionized can pass through the mucous
that is necessary to achieve drug action. membrane.

Four process of pharmacokinetics: Drugs in liquid form are more rapidly absorbed than
solid drugs
1. Absorption
 Takes place in the mucosal lining Pain, stress, and foods that are solid, hot or high in fat
makes drugs remain in the stomach longer because
 Tablets are example- not 100% drug it is with
these causes a slow gastric emptying time.
excipient. This is for the drug to take a particular
size and shape and to enhance drug dissolution. Poor circulation to stomach hampers absorption, du to
A. Disintegration- it has to be broken down into shock or diseases.
small particles
B. Dissolution- a process where broken down Drugs given rectally are absorbed slower than drugs
particles combine with liquid administered by mouth.
C. Absorption- happens in the mucosal lining of
Suppository-based drug affects the absorption.
the small intestine. Movement of drug into the
blood stream after administration. Drugs that are administered intramuscularly are
 Drugs are both disintegrated and dissolve faster absorbed faster in muscles that have increase blood
in acidic fluids (ph 1-2) than in alkaline fluids flow like deltoid than those that do not.
 The very young and older adults have less
gastric activity- drug absorption Is slower Subcutaneous have decreased blood flow compared
 Enteric coated drug are meant to be absorbed with muscle, slower absorption.
in the small intestine.
Absorption of Oral Drugs
 NURSING IMPLICAITON-do NOT crush the
medication. It will not be absorbed in the GI tract > intestinal lumen > liver (via the portal vein)
intended site.
 Drugs are absorbed in the mucosal lining of the First pass metabolism or first-pass effect
small intestine through:
- in the liver some drugs are metabolised in
a. Passive transport (diffusion and facilitated
an inductive form and are excreted, thus,
diffusion)
reducing the drug available to exert a
- no energy needed
pharmacologic effect.
 diffusion drug moves across the cell membrane
- Lidocaine and nitroglyceride should not be
from higher to lower concentration
given orally because it will be inactivated by
 facilitated diffusion
the liver.
b. Active transport (needs enzyme or protein)
- energy required Bioavailability
c. Pinocytosis
- Refers to the percentage of adminestered
drug available for activity.  Two drugs are administered together they
- For orally administered drug bioavailability compete for protein bounding sites in which
is affected by absorption and first-pass drug accumulation will occur and drug toxicity
metabolism may result.
- Oral dug less than 100%
- Intravenous is 100% Low plasma protein level, decreases the number of
- FACTORS that alter BioA: available binding sites and can lead in an increase of
amount of free drug available resulting in drug accu and
1. Drug form
2. Route of administration toxicity.
3. Gastric mucosa and motility Drugs taken during pregnancy:
4. Administration with food and other
drugs 1st trimester- spontaneous abortion
5. Changes in liver metabolism
2nd trimester- spontaneous abortion, teratogensis, or
> decreased of liver meta increased of
other subtler effects
bioavailability
2. Distribution 3rd trimester- fetal growth and development
-refers to the movement of drug from the
circulation to the body tissues 3. Metabolism or biotransformation
- drug affinity to protein binding - Is the process in which the body chemically
> highly protein-bound drugs changes drug into a form that can be
-90% bound to protein excreted
>weakly protein-bound drugs - Liver is a primary site of metabolism
-less than 10% bound to protein - Cytochrome P450 system
TAKE NOTE - liver enzyme
The portion of the drug that is bounded to the - metabolized lipid-soluble drugs to water-
protein is inactive because it is not available to soluble drug for renal excretion
interact with tissue receptor, thus, no
Factors that alter drug metabolism
pharmacologic effect.
1. Liver disease (cirrhosis and hepatitis)- inhibits
The portion that remains unbound is free active drug-metabolizing enzymes in the liver
drugs. Free drugs can exit blood vessel and
reach their site of action, thus, with Decreased drug metabolism > excess drug accumulation
pharmacologic response. > toxicity

Factors that may alter protein binding: Drug half-life

1. Lower albumin levels (hypoalbuminemia) - Is the time it takes for the amount of drugs
 With liver and kidney disease into the body to be reduced by half.
 Malnourished - Amount of administered, amount of drug
 Older adults (mas naa hypoalbuminemia) remaining in the body from the previous
2. Lower plasma protein level dose, and elimination can affect half- life.
- Example: 500 mg paracetamol was
Patients with kidney or liver disease may have administered at 0800H. 4 hours half-life.
significantly lower albumin levels. 0800H- 500 mg
1200H- 250 mg
 NURSING IMPLICATION- check patient’s protein
0400H- 125 mg
and albumin level when administering drugs.
ss

Steady state- amount of drugs absorbed is equal to the


amount of drug eliminated.

 Loading Dose
- The administration of a large initial dose
used to ensure quick therapeutic response,
for a lower maintenance dose. Drugs with
LONG half-lives
- Example: Phenytoin, half-life 22 hours
4. Elimination or excretion
- Main route is through the kidneys
- Drugs are also excreted through bile, lungs,
saliva, sweat and breast milk.
- Urine PH influences drug excretion
 Acidic urine- elimination of weak based drug
 Alkaline urine- elimination of weak acidic based
drug
> prerenal
(profusion of blood towards the kidney),
(dehydration and haemorrhage)
-intrarenal
(within the kidneys/ formation of urine)
(glomerulonephritis, chronic kidney dis), and
-postrenal
(outflow of urine form the kidneys)
(prostatic hypertrophy, stones, and urogenic
bladder) affects excretion.

-creatinin and Blood Urea Nitrogen (BUN) are


used to determine renal function. Creatinine
more reliable, not altered by body processes.

 NURSING IMPLICATION:

Check kidney function to ensure correct dosage of


the medication.
- Dose of drug that produces toxic response
in 50% of the population
PHARMACODYNAMIC PHASE

- the study of the effects of the drugs on the


ONSET, PEAK, AND DURATION OF ACTION
body
- has primary (desirable) and secondary Onset- time it takes for a drug to REACH the minimum
(desirable or undesiarbale effects) effective concentration after administration.
- example: Diphenhydramine: primary effect:
antihistamine (allergy), secondary: Peak- drug has achieved the highest concentration in
blood
drowsiness

Dose-response relationship Duration of Action- length of time the drug exerts a


therapeutic effect
- the body’s physiologic response to change
in drug concentration at the site of action. The Four receptor families:

1. Cell membrane embedded enzymes


Potency
- Receptor cites In the cell surface
- amount of drug needed to elicit a specific 2. Ligand-gated ion channels
physiologic response toa drug -cell membrane gihapon
- a drug with high potency produces -sud ang Na and K
significant therapeutic response at low 3. G protein- coupled receptor systems
concentration. -cell membrane gihapon
- Example: 500mg lower potency na kay need - 3 components: receptor, g protein, effector
og higher dosage para maka feel ka sa (enzyme or ion channel)
therapeutic effect 4. Transcription factors
-receptor site inside the nucleus
Maximal Efficacy
- cell membrane> nuclear membrane>
- The point at which increasing =g the drug;s intracellular proteins> transcription factors>
dosage no longer increase the desired protein synthesis
therapeutic effect.
PHARMACOLOGICAL NURSING TERMS
Therapeutic Index
Agonist- drug that activate receptors and
- Describes the relaitons between the
produced a desired response
therapeutic dose of the drug (ED50) and the
Antagonist- drugs that orevent receptor
toxic dose of the drug (TD50).
activation and blocks the response
- If ED50 response and TD50 response are
Nonspecific drug- drugs affect multiple receptor
close, the drug is said to have a narrow
sites. One type of receptor, different sites.
therapeutic index> CLOSE MONITORING
Nonselective drug- affects multiple receptors.
required for patient’s safety
Side effects- secondary effects. (nursing
ED50 implications: health teaching on side effects)
Adverse reaction- unintentional, unexpected
- Dose of drug that produces therapeutic reactions. Maybe severe or mild. Always
response in 50% of the population undrsirable.
Drug toxicity- drug level exceeds the
TD50
therapeutic range
Tolerance- decreased responsiveness - Example: epinephrine
Tachyphylaxis- acute, rapid decrease in 2. Depression
response to drugs - Neurlogic aciivty
Drug interaction- altered action or effect of a - barbiturates
drug as a result on interaction with one or more 3. Irritation
multiple drugs. - Noxious effects
Drug-nutrient interaction- food may increase or - Laxatives (senocot)
decrease 4. Replacement
- Replace essential body compound
Additive drug effects- response is increased - Insulin
beyond what either could produce alone - Diabetes mellitus
Ex: diuretic and antihypertensive 5. Cytoxic action
Synergistic effect or potentiation- the clinical - Kill invading parasites
effect of the 2 drugs given together is - Chemotherapeutic (antineoplastic
substantially greater than that of either drug medications)
alone. Ex: Co-amoxiclav 6. Antimicrobial Actions
Antagonistic drug effects- blocks the effect of - Kill infectious
the other. Ex: antidote - Co-amoxiclove
7. Modified of Immune Status
Pharmacogenetics - Corticosteroids
-study of genetic factors that influence an - Chemotherapeutic drugs
individual’s response to specific drug.
TABLEST AND CAPSULE
Placebo effect- a drug response not attributed 1. Tablets
to the checmical properties of a drug 2. Capsule
3. Spansule or timed-release capsule
Ethnopharmacology- a subdivision of 4. Enteric-coated (don’t crush)
ethnomedicine and focuses on the use of herbs,
powder, teas and animal products as healing -oral, buccal, sublingual,intravaginally, rectally
remedies.
LUQUIDS
Over-the-counter drug 1. Elixir- syrup glycerine or alcohol (taste)
-safe w/o direct supervision of a health care 2. Suspension- w/ particles (shake)
provider 3. Elmusion- 2 or more liquids
- purchase w/o prescription
-example: shadow ephedrine (emergency Routes:
contraception) - Transdermal (patch), topical (cream)
- NURSING IMPLICATIONS: - Installations: eye drops, eye ointment, nasal
- emphasize that many of these drugs are spray, ear drop
potent AND CAN CAUSE MODERATE TO SEVERE - Inhalations: metered-dose inhaler, MDI
SIDE EFFECTS, especially when taken with other with spacer, nebulizer
drugs. - Nasogastric (nose) & gastrostosmy tubes
(stomach)
Mechanism of Drug Action - Suppositories: rectal (coned or spindle
1. Stimulation shape), vaginal (egg shape), Urethra (pencil
- Enhances intrinsic activity shape)
- Parenteral:
- Intradermal: 10-15
- Intravenous- 25 10 RIGHTS
- Subcutaneous- 45 1. right patient
- Intramuscular- 90 2. right drug
3. right dose
4. right time
NURSING PROCESS 5. right route
6. right assessment
Assessment
7. right documentation
Subjective Data 8. right education
9. right evaluation
 Healthy and fam history 10. right to refuse
 Knowledge of patient
 OTC
 Illness verbalize Philippine National Drug Formulary
 Financial barriers
 Tobacco, caffeine, alcohol - aims to provide accessible, effective,
avaiilable, safe and affordable drugs
Objective Data - provides list of FDA approved drugs
 Seeing, hearing, smelling, touching
REPUBLIC ACTS:
 Physical health assessment
 Lab results RA#9711 or Food and Drug Administration Act of 2009
 Measurement of vital signs
 Body language RA#9502 or Universally Accesible Cheaper and Quality
Medicine Art of 2008
Diagnosis RA#665 Generics Act of 1988
 type of care

Planning

 set goals or expected outcomes & interventions


 time frame

Implementation

 patient teaching
- general, side effects, self-administered,
diet, cultural considerations
 other interventions

Evaluation
- documentation
- Antiseptic, antinflammatory,
antipasmodial, anti-cough, anti-spasmodic,
10 MEDICINAL IN THE PHILIPPINES antioxidant hepatoprotective, antidiabetic,
1. Akapulko antigenotoxic in folklore med.
- Tinea infections, insect bites, ringowrms,
eczema, scabies and itchiness.

5. Lagundi
- Used to reat cough, colds, fever
- Relief for asthma & pharyngitis,
rheumatism, dyspepsia, boils, and diarrhea

2. Ampalaya
- Treatment of diabetes (mellitus),
haemorrhoids, coughs, burns, and calds,
neing studied for anti-cancer
6. Niyog-niyogan
- Intestinal parasite

3. Bawang or garlic
- Used to treat infection
- Antibacterial, antiinflamatory, anticancer,
and anti-hypertensive
- Reduce cholesterol level

7. Sambong
- Treat kidney stones, wounds, cuts,
rheumatism, anti-diarrhea, anti spasm,
colds and coughs and hypertension
4. Bayabas or Guava
10 HERBAL PLANTS IN THE PHILIPPINES

1. Astralagus
- used as an adjunct to boost immune
system

8. Tsaang gubat
- Treat skin allergies including eczema,
scabies, and itchiness wounds in childbirth.

2. Chamomile
-for sleeplessness, anxiety, stomach and
intestinal ailments

9. Ulasimang bato
-athritis

3. Cinnamon
- Bronchitis, GI problems, anorexia, and
diabetes

10. Yerba Buena


-an analgesic to relieve body aches and pain
due to rheumatism and gout.
- treat coughs and colds and insetc bites.

4. Echinacea
- For cold, flue, and infection.
8. Ginseng
- Used to boost immune system. Increase a
5. Garlic
person’s sense of well-being and increase
-used to lower cholesterol, blood pressure, and
stamina
reduce heart disease.

9. Hawthorn
6. Ginger - Heart disease
- Nausea, motion sickness and diarrhea

-
10. Licorice root
7. Gingko - Stomach ulcer, bronchitis, sore throat, and
-asthma, bronchitis, fatigue, and tinnitus viral hepatitis.
11. Mil thistle 14. Turmeric
- Cirrhosis, chronic hepatitis, and gall bladder -heartburn, stomach ulcer, gallstone,
disorder. inflammation and caer.

15. Valerian
- Insomnia, anxiety, headache, depression,
irregular heartbeat, and tremors.
12. Peppermint
- Nausea, indigestion, irritable bowel
syndrome, cold, headaches, muscle and
nerve pain.

13. St. John Wort’s


- Mental disorders and nerve pain
NERVOUS SYSTEM
- responsible for sending, receiving, and interpreting information from all parts of the body.
- responds to external stimuli and also monitors and coordinates the functions of the internal
organs

CENTRAL NERVOUS SYSTEM


- composed of the brain and spinal cord both are enclosed in protective layer - meninges

MENINGES
- outer layer - dura mater
- middle layer - arachnoid mater
- inner layer - pia mater

SUBARACHNOID SPACE
- space between the arachnoid and pia mater is filled with cerebrospinal fluid

BRAIN
- located @ the cranium of skull
- has 3 main parts (cerebrum, cerebellum, and medulla oblongata)

CEREBRUM
- largest part of brain
- divided into Left and Right hemispheres
- concerned with learning, memory, interpretation, and personality

LEFT AND RIGHT HEMISPHERES


- composed of frontal, temporal, parietal, and occipital lobe.
- two hemispheres are connected by a nerve tract called Corpus callosum
- the surface of the cerebral hemisphere is folded which increases surface area

CEREBELLUM
- located @ the back of brain below cerebrum
- controls balance, movement, and coordination

BRAIN STEM
- located beneath cerebrum, in front of cerebellum
- connects brain with spinal cord
- composed of Midbrain, Pons, and Medulla oblongata
- controls a number of autonomic functions including respiration and blood pressure

SPINAL CORD
- extends from Medulla oblongata and down the back
- protected by the vertebral column
- a hollow tube containing cerebrospinal fluid
- 31 pairs of spinal nerves arise from spinal cord, these nerves transmit info from body organs to
brain, and from brain to organs
NURSING CARE OF CLIENTS WITH CNS AND PSYCHOTHERAPEUTIC DRUGS

(Care of clients with Drugs affecting the Central and Peripheral System)
PART 1
Nervous System
-Composed of all nerve tissue:
▪ Brain
▪ Spinal cord
▪ Nerves
▪ Ganglia
-receives stimuli and transmits information to nerve centers for an appropriate
response
2 types: CNS and PNS

Central Nervous System (CNS)


- Composed of brain and spinal cord
- Regulates body functions
*Stimulation of the CNS may either increase the neuron activity or block nerve cell
activity

Peripheral Nervous System (PNS)


2 divisions:
1.) Somatic Nervous System (SNS)
o voluntary
o for locomotion and respiration
2.) Autonomic Nervous System (ANS)
o involuntary
o for functioning of the heart, respiratory system, GI system and glands

Group of Medications

STIMULANTS

Indications:
Attention-Deficit/Hyperactivity Disorder
- dysregulation of the transmitter’s serotonin, norepinephrine and dopamine
- may occur before 7yrs of age and may continue through teenage years
Characteristics: inattentiveness, inability to concentrate, restlessness, hyperactivity,
inability to complete tasks and impulsivity
Narcolepsy
- characterized by falling asleep during normal waking activities
*Sleep paralysis usually accompanies narcolepsy and affects the voluntary muscles
Respiratory Distress
- refers to a condition in which the person is having trouble breathing which often
show signs that they are not getting enough O2
- this condition prevents the body organs from getting the O2 they need to fxn

Major groups of Stimulants:


1. Amphetamines
Examples: Amphetamine Sulfate
Dextroamphetamine Sulfate
Lisdexamfetamine dimesylate
(these medications stimulate the release of norepinephrine from the brain and the
sympathetic
- causes euphoria and increased alertness as well as insomnia, restlessness, tremors,
irritability and weight loss
- have a half-life of 9-13hrs
*Excessive use may lead to psychosis
*Amphetamine and amphetamine-like drugs SHOULD NOT be administered in the
EVENING or BEFORE BEDTIME because insomnia may result

2. Amphetamine-like Drugs
- used for ADHD or narcolepsy
Examples: Methylphenidate HCl
Modafinil
Dexmethylphenidate HCl
Armodafinil
- more effective in treating ADHD than Amphetamines
- classified as Controlled Substance Schedule (CSS) II drug.

3. Anorexiants
- suppress appetite
Examples: Benzphetamine
Diethylpropion HCl
Phentermine HCl
Phentermine topiramate
Phendimetrazine
Liraglutide
Naltrexone HCl
Bupropion HCl
(cause a similar effect on the hypothalamic and limbic regions of the brain to
suppress appetite. These medications do not have serious side effects associated w/
amphetamines)
*Long term use of this medication results to nervousness, restlessness, irritability,
insomnia, palpitation and hypertension

4. Analeptics
- stimulate respiration
Examples: Caffeine citrate 2 main drugs
Theophylline
Doxapram
*Large dose of caffeine will stimulate respiration
*Theophyllinen is mostly used to relax the bronchioles and used to increase respiration
in newborn

DEPRESSANTS
*Drugs that are CNS depressants cause varying degree of depression or reduction in the
functional activity within the CNS
*The degree of depression depends primarily on the drug and the amount of drug taken
Classifications:
Sedative-hypnotics
Analgesics (opioid/nonopioid)
General Anesthetics
Anticonvulsants
Antidepressant
Antipsychotic

1. Sedative-hypnotics
Examples:
Secobarbital sodium
Butabarbital sodium
Phenobarbital
Pentobarbital
Mephobarbital
*Hypnotic effect is a form of natural sleep
Hypnotic drug therapy should be short term to prevent drug dependence and drug
tolerance
*Interrupting hypnotic therapy can decrease drug tolerance but abruptly discontinuing a
high dose of hypnotic taken over a long perion can cause withdrawal symptoms
General rule:
The lowest dose should be taken to achieve sleep
Patients w/ severe respiratory disorders should avoid hypnotics which could
cause an increase in respiratory depression
Hypnotics are contraindicated during pregnancy
Ramelteon is the only major sedative-hypnotic approved for long term use. This
drug may be used to treat chronic insomnia

Non-pharmacologic ways to promote sleep:


1. Arise at a specific hour in the morning
2. Take few or no daytime naps
3. Avoid drinks that contain caffeine and alcohol 6hrs before bedtime
4. Avoid heavy meals or strenuous exercise before bedtime
5. Take a warm bath, listen to quiet music or perform other soothing activities
before bedtime
6. Decrease exposure to loud noises
7. Avoid drinking copious amount of fluids before sleep
8. Drink warm milk before bedtime

Types of Sedative-hypnotics:

• Barbiturates - useful as sleep sustainer for maintaining long periods of sleep


*Must be short term use only
Classifications:
1. Long acting: PHENOBARBITAL and MEPHOBARBITAL
2. Intermediate acting: BUTABARBITAL
3. Short acting: SECOBARBITAL
*The onset of action of Pentobarbital is slower when administered IM than when
administered in PO, whereas for Pentobarbital this medication increases hepatic enzyme
action causing an increased metabolism and decreased effect of drugs (such as
anticoagulants, glucocorticoids, tricyclic antidepressants and kinetine)
*Pentobarbital may cause hepatotoxicity if taken with large doses of acetaminophen

• Benzodiazepines – used to induce sleeping


Examples:
Alprazolam
Estazolam
Lorazepan
Temazapam
Triazolam
Quazepam
Diazepam
Antagonist: Flumazenil
*Must not be used for longer than 3-4weeks
Adverse rxn: anterograde amnesia

• Nonbenzodiazepines
• Melatonin Agonist

PART 2
ANASTHETICS
- Substances that induces insensitivity to pain
Classified as: General and Local
*Monitor vital signs following general and local anesthesia because hypotension and
respiratory depression may result

Balanced Anesthesia
- A combination of drugs each with a specific effect frequently used in general
anesthesia
- Used to minimize cardiovascular problems, decreases the amount of general
anesthetic used
- Reduces possible post-anesthesia nausea and vomiting
- Minimizes the disturbance of organ fxn and decreases pain

May include the following:


1. A hypnotic given the night before
2. Premedication with an opioid analgesic/ benzodiazepine plus an anticholinergic
given about 1hr before surgery to decrease secretions
3. A short-acting non barbiturate such as propofol
4. An inhaled gas, often a combination of an inhalation anesthetic, nitrous oxide
and oxygen
5. A muscle relaxant given as needed

Stages of Anesthesia:
1. Analgesia –
• begins with consciousness and ends with loss of consciousness
• speech is difficult
• sensation of smell and pain are lost
• dreams, auditory and visual hallucinations may occur
• “induction stage”

2. Excitement/Delirium
• Produces a loss of consciousness caused by depression of the
cerebral cortex
• Confusion, excitement or delirium occur
• Induction time is short

3. Surgical
• Surgical procedure is performed during this stage
*As anesthesia deepens, respirations become shallower and the respiratory rate is
increased

4. Medullary Paralysis
• “toxic stage of anesthesia” in which respirations are lost and
circulatory collapse occurs, ventilator assistance is necessary

*The patient’s response to anesthesia may differ according to variables related to health
status of the individual. These variables include: Age, A current health disorder,
Pregnancy, History of heavy smoking and Frequent use of Alcohol and Drugs

Anesthetic agents can be administered through:


➢ Inhalation – anesthetic gas/volatile liquids administered as gas are used to
deliver general anesthesia
Example of volatile liquids:
Halothane
Methoxyflurane
Enflurane
Isoflurane
Desflurane
Sevoflurane
Example of Gas: Nitrous oxide
Adverse rxn:
Respiratory depression
Hypotension
Dysrhythmia
Hepatic dysfunction

➢ Local Infiltration – used to block the pain at the site where the drug is
administered by preventing the conduction of nerve impulses
• Dental procedures
• Suturing skin lacerations
• Short term surgery at a localized area
• Block nerve impulses
• Below the insertion of spinal anesthetic
• Diagnostic procedures (such as lumbar puncture and
thoracentesis)

➢ Spinal route
Requires that a local anesthetic be injected into the subarachnoid space:
- Below the first lumbar space (L1) in adults
- The 3rd lumbar space in children (L3)
*A Postdural-puncture headache might result following a spinal anesthesia possibly
because of a decrease of cerebrospinal fluid pressure caused by the leak of fluid at the
needle insertion point.
Nursing Intervention: Increased fluid intake usually decreases the likelihood of leaking
spinal fluid. Encourage the patient to remain flat
• Spinal Block – into the subarachnoid space
• Epidural Block – in the epidural space
• Caudal Block – through the sacral hiatus
• Saddle Block – lower end of spinal column
*Blood pressure should be monitored during administration of these types of anesthesia

➢ Intravenous – may be used for general anesthesia or for the induction stage
of anesthesia
TIVA – Total Intravenous Anesthesia

➢ Topical – used to decrease sensitivity of nerve endings in the affected area


Forms:
Solutions
Liquid sprays
Ointments
Creams
Gels and powders

ANTISEIZURE DRUG
- Used for epileptic seizures, also called as “anticonvulsants/anti-epileptic” drugs
- This medication acts by stabilizing nerve cell membrane and suppress abnormal
electrical impulses in the cerebral cortex
- Prevents seizures but do not eliminate the cause or provide a cure
• Suppresses sodium/calcium influx
• Increases the action of Gamma Aminobutyric Acid (GABA)
1. Hydantoins – act by inhibiting sodium influx, stabilizing cell membranes, reduces
repetitive neuronal firing and limit seizure ; may cause birth defects or congenital
anomalies
• Phenytoin – for the treatment of tonic-clonic seizure, partial
seizures and status epilepticus ; has narrow therapeutic range:
10-20 mcg/mL
(serum level should be monitored)
*Onset of action of PO route is 30mins-2hrs
*Peak of 1.5-6hrs a steady state of serum concentration at 7-10days
*Duration of action dependent on the half-life which could be up to
45hrs
*IV line should always be flushed w/ saline sol’n before and after use to reduce venous
irritation
*This medicatiom may be diluted in saline sol’n and dextrose should be avoided because
of drug precipitation and must not be administered through IM route
*If medication will exceed 20 mcg/mL→ toxic effects
*If medication is below 10 mcg/mL →will not render a desired effect

Assessment Nursing Planning


Diagnoses
- Obtain a - Risk for - Patient’s
health injury seizure
history frequency will
- Risk for diminish
- Check fall
urinary
output - Patient will
(1500mL) adhere to
antiseizure drug
therapy
- Determine
liver &
kidney fxn

Nursing Interventions Evaluation


- Monitor serum drug level - Evaluate
effectivenes
- Encourage compliance w/ s of drugs
medication in
controlling
- Use seizure precautions seizures

- Determine whether the - Monitor


patient is receiving serum
adequate nutrients phenytoin
levels
- Advise patients who are
receiving oral - Monitor
contraceptives to use an patients for
additional contraceptive hydantoin
method overdose
Patient teachings:
➢ Teach patient to
shake suspension
from the
medications
➢ Advise patients
not to
drive/perform
other hazardous
activities
➢ Counsel female
patient
contemplating of
pregnancy to
consult w/ a
health care
provider
➢ Avoid alcohol
and other CNS
depressants
➢ Teach patient
not to stop the
medication
abruptly
➢ Advise patients
w/ Diabetes
Mellitus to
monitor serum
glucose lvl
➢ Take antiseizure
drug w/ food
and milk at the
same time
everyday
➢ Urine may be
harmless pinkish
red/reddish
brown in color
➢ Maintain good
oral hygiene and
use a soft-
bristled
toothbrush

2. Barbiturates
• Phenobarbital – used to treat tonic-clonic, partial and myoclonic
seizures as well as status epileptic
– therapeutic range: 20-40 mcg/mL

3. Succinimides
• Ethosuximide – acts by decreasing calcium influx through the t-
type calcium channel
- used to treat absence seizure
- Therapeutic range: 40-100 mcg/mL

4. Benzodiazepines
Have antiseizure effects: Clonzepam, Clorazepate dipotassium, Lorazepam,
Diazepam

5. Iminostilbenes
• Carbamazepine – used for psychiatric disorders, trigeminal
neuralgia and alcohol withdrawal. - Therapeutic range: 4-12
mcg/mL
6. Valproate – for tonic-clonic absence and mixed type of seizure
- Therapeutic serum range: 50-100mcg/mL
*Liver enzymes should be monitored
*Hepatoxicity is one of the adverse rxn

Antiseizure drugs and Pregnancy

❖ During pregnancy, seizure episodes increase 25% in women w/ epilepsy


❖ Hypoxia may occur during seizure
❖ Phenytoin and Carbamazepine are linked to fetal anomalies
❖ Valproic acid causes major malformations
❖ Antiseizure drugs tend to act as inhibitors of vitamin K
❖ Pregnant women are given oral vitamin K supplement during the last
week/10days of the pregnancy or is administered to the infant soon after birth
❖ Antiseizure drug can also increase the loss of folate in pregnant women

Antiseizure drugs and Febrile seizures

❖ Seizures associated to fever occur in children between 3mos-5yrs of age


❖ Prophylactic antiseizure drug treatment (such as Phenobarbital/diazepam) may be
indicated for high risk patients
❖ Valproic acid should not be given to children younger than 2yrs old

Antiseizure drugs and Status epilepticus

❖ If treatment is not started immediately, death could result


❖ Drug choice: diazepam or lorazepam via IV followed by phenytoin via IV
❖ For continued seizures, midazolam or propofol and then high-dose barbiturates
are used

PART 3
Parkinson’s Disease
- Caused by an imbalance of the neurotransmitters (DA and ACh) and it is marked by
the degeneration of neurons of the extrapyramidal motor tract in the substantia
nigra of the midbrain
- Chronic, progressive neurologic disorder that affects the extrapyramidal motor tract
which controls posture, balance, locomotion.
- Most common form of Parkinsonism – a syndrome, a recombination of similar
symptoms because of its major features like:
Major Features:
❖ Rigidity (abnormal increased muscle tone) –increases with movement
*Postural changes caused by rigidity and bradykinesia include: chest and head
thrust forward with the knees and hips flexed, shuffling gait and the absence of arm
swing
*Other characteristic symptoms include: masked facies - no facial expressions,
involuntary tremors of the head and the neck, and peel rolling motions of the hands
❖ Bradykinesia (slow movement)
❖ Gait disturbances
❖ Tremors – more prevalent at rest

Neurotransmitters:
Dopamine (DA)
- an inhibitory neurotransmitter
- released from/ produced by : dopaminergic neurons
- maintains and controls Acetylcholine and inhibits its excitatory response
- plays a part in controlling the movements a person makes and their emotional
responses/ TAKE NOTE: Dopamine has a control in the locomotion or movement of a
person
*The right balance of DA is vital for both physical and mental well-being, vital brain
functions that affect mood, sleep, memory, learning, concentration and motor control
are influenced by the levels of DA in a person’s body
Acetylcholine (ACh)
- an excitatory neurotransmitter
- essential for muscles to contract, without it muscles cannot contract
- released from cholinergic neurons
- achieved neurotransmitter of the parasympathetic nervous system that contracts
smooth muscles, dilates blood vessels, increases bodily secretions, and slows heart
rate

*These 2 neurotransmitters (DA and Ach) need to work hand in hand in order to create
a balance ; if one is elevated, there will be a chaos in the body system

How Parkinson’s Disease Develops:


- There are approximately 86 billion neurons in the brain, PD is caused by an
imbalance of the neurotransmitters, dopamine and acetylcholine.
- Reason for degeneration of neurons is unknown.
- Degeneration of dopaminergic neurons -> less dopamine produced -> excitatory
response exceeds the inhibitory response of the dopamine because the level of ACh
is beyond what the dopamine could handle or inhibit, why?: only the dopamine
production is affected but the production of the Ach continues thus there is more
ACh than Dopamine.
- More ACh = more excitatory neurotransmitters
- What happens: *Excessive amount of ACh stimulates neurons that produce (GABA)
Gamma-aminobutyric acid →[inhibits the activity of neuron]
- GABA - an inhibitory neurotransmitter
- it blocks or inhibits certain brain signals and decreases activity in nervous system
- when certain brain signals are inhibited in the nervous system, symptomatic
movement disorders of Parkinson’s Disease occurs (recall rigidity, tremors, gait
disturbance, and bradykinesia)
- by the time early symptoms of PD appear, 80% of the striatal dopamine has been
depleted

Non-pharmacologic measure for Parkinson’s Disease


• Patient teaching
• Exercise [can improve mobility and flexibility] - enroll in therapeutic exercise
programs tailored to pt’s disorder
• Nutrition [a balanced diet with fiber and fluids helps prevent constipation and
weight loss]
• Group support [to help cope and understand this disorder]

Drugs for Parkinson’s Disease

1. Anticholinergics
2. Dopamine replacements (dopaminergics)
3. Dopamine Agonists
4. Monoamine Oxidase B (MAO-B) Inhibitors
5. Catechol-O-methyltransferase (COMT) Inhibitors

1.) Anticholinergics
- Can inhibit the release of ACh
*one of the problems in Parkinson’s Disease is the increased number of ACh
Examples:
Benztropine mesylate
Trihexyphenidyl Hydrochloride

!! : Glaucoma is contraindicated – anticholinergics can induce glaucoma, if pt already has


glaucoma, it could worsen

Side Effects:
- Dry mouth
- Dry secretions
- Urinary retention
- Constipation
- Blurred Vision
- Increase in heart rate

Assessment:
▪ Obtain a health history (report any history of glaucoma, GI dysfunction, urinary
retention, angina, or myasthenia gravis)
▪ Obtain a drug history (report any probable drug-to-drug interaction such as with
phenothiazine tricyclic antidepressants and antihistamine – can increase effect of
dry hexafenidyl hydrochloride)
▪ Assess baseline vital signs for future comparison
▪ Assess pt’s knowledge regarding the medication regimen
▪ Assess usual urinary output

Nursing Diagnosis:
▪ Impaired mobility related to muscle rigidity
▪ Impaired urinary elimination related to urinary retention

Planning:
▪ Pt will have decreased involuntary symptoms caused by the disease or drug
induced parkinsonism
Nursing interventions:
▪ monitor vital signs urine output and bowel sounds (increased pulse rate urinary
retention and constipation are side effects of anticholinergics)
▪ observe for involuntary movements

Patient teachings:
▪ avoidance of alcohol cigarette caffeine and aspirin (to decrease gastric acidity)
▪ encourage the patient to relieve dry mouth with hard candy ice chips or sugarless
chewing gum (because anticholinergics can decrease salivation)
▪ suggest that patient uses sunglasses in direct sunlight (because of possible
photophobia)
▪ advise patients to void before taking the drug (to minimize urinary retention)
▪ counsel patients who take an anticholinergic for control of symptoms of
parkinson's disease to have routine eye examination (because anti-cholinergics are
contraindicated in patients with glaucoma)
▪ encourage patients to ingest foods high in fiber and to increase fluid intake (to
prevent constipation)
Evaluation:
▪ evaluate the outcomes of the therapy
▪ evaluate the patient's response to trihexyfenidyl or the benztrophine vesilate to
determine whether parkinson's disease symptoms are controlled
2.) Dopaminergics
Examples of Dopaminergics
✓ Carbidopa and Levodopa

✓ Levodopa
❖ the first dopaminergic drug - introduced in 1961 but is no longer available
in the United States
❖ When it was introduced, levodopa was effective in diminishing symptoms
and increasing mobility (this is because the blood brain barrier admits
levodopa but not dopamine)
❖ NOTE: the enzyme dopa decarboxylase - converts levodopa to dopamine in
the brain but this enzyme is also found in the PNS and 99% of levodopa is
converted into dopamine before it reaches the brain
❖ THEREFORE only about 1% of levodopa taken in is converted to dopamine
once it reaches the brain
❖ large doses are needed to achieve a pharmacologic response
❖ these high doses could cause many side effects
o nausea
o vomiting
o Dyskinesia
o orthostatic hypotension
o cardiac dysrhythmia and
o psychosis
❖ the fact that so much levodopa is metabolized before it reaches the brain
an alternative drug carbidopa was developed

✓ Carbidopa
❖ inhibit the enzyme dopa decarboxylase in the PNS
❖ more levodopa reaches the brain
❖ Carbidopa is combined with Levodopa in a ratio of one part carbidopa to 10
parts levodopa (1:10)
Advantages of combining levodopa with carbidopa:
➢ more dopamine reaches the basal ganglia
➢ smaller doses of levodopa are required to achieve the desired effect
Disadvantages of the carbidopa levodopa combination:
➢ more available levodopa = more side effects may occur
➢ the peripheral side effects of levodopa are not as prevalent however
angioedema palpitations and orthostatic hypotension may occur
➢ GI disturbances are also very common in patients who are taking carbidopa
levodopa (because dopamine stimulates the chemoreceptor trigger zone or
the ctc in the medulla which then stimulates the vomiting center)
*taking the drug with food can decrease nausea and vomiting but foods
lose the absorption rate of the medication
Assessment:
▪ Assess vital signs for future comparison
▪ Assess patients for signs symptoms of PD (including stoop forward posture,
shuffling gait, mask facies and resting tremors)
▪ Assess patient history (that includes glaucoma, heart disease, peptic ulcer, kidney
or liver disease and psychosis because severe cardiac renal or psychiatric health
problems are contraindications for levodopa)
▪ Assess drug history (especially if the patient is taking monoamine oxidase
inhibitor or MAO-I)
NOTE: if a MAO-I and carbidopa levodopa are taken concurrently it may result to
hypertensive crisis - a severe increase in the blood pressure that may lead to
stroke

Nursing diagnosis:
▪ Impaired physical mobility related to dizziness
▪ Risk for fall
*do not forget that our main objective of administering dopaminergic or carbidopa
levodopa to a patient is to decrease the signs and symptoms of parkinson's
disease within one to four weeks of drug therapy

Nursing interventions:
▪ Monitoring vital signs (electrocardiogram or ECG because orthostatic hypotension
may occur during early use of carbidopa-levodopa)
▪ Instruct patients to rise slowly to avoid faintness
▪ Observe for weakness, dizziness or syncope (which are symptoms of orthostatic
hypotension)
▪ Administer carbidopa-levodopa with low protein foods (because high protein diets
interfere with drug transport to the CNS)
▪ Observe for symptoms of Parkinson’s dse.
▪ Urge the patient not to abruptly discontinue the medication (because rebound
Parkinson's disease may occur)
▪ Advise patients to avoid chewing or crushing the extended release tablets
▪ Encourage patients to report side effects and symptoms of dyskinesia
▪ Explain that it may take weeks or months before symptoms are controlled
▪ Suggest to patients that taking carbidopa-levodopa with food may decrease GI
upset (but food will slow the rate of drug absorption)
Evaluation:
▪ Do not forget to evaluate the effectiveness of drug therapy
▪ Determine if there is an absence of side effect
▪ Determine if the patient and family have increased knowledge of the drug
regimen

3.)Dopamine Agonist
- also called dopaminergics
- used to stimulate dopamine receptors
Examples:

▪ Amantadine
▪ Bromocriptine
▪ Pramipexole
▪ Ropinirole Hydrochloride
1.) Amantadine
-an antiviral drug that affects the dopamine receptors
-can be taken alone or in combination with carbidopa levodopa or anticholinergic
-produces improvement in symptoms but drug tolerance develops

-it can also be used for induced parkinsonism


Side effects:
▪ orthostatic hypotension
▪ confusion
▪ urinary retention
▪ constipation

2.) Bromocriptine mesylate


-more effective than amantadine and anticholinergics
-not as effective as carbidopa-levodopa in allegating symptoms

-patients who cannot tolerate carbidopa-levodopa are given with this medication
Side effects:
▪ nausea
▪ orthostatic hypotension
▪ palpitation
▪ chest pain
▪ lower extremity edema
▪ nightmares
▪ delusion and confusion
Assessment, Nursing Diagnosis and Planning:

▪ for a patient who is taking anticholinergic and carbidopa-levodopa are just the same
for a patient who's taking amantadine and bromocriptine
Patient teachings:
▪ Urge patient taking amanti. to report any signs of skin lesions, seizures, or
depression (a history of these health problems should have been previously
reported to a health care provider)
▪ Advise patients taking bromo. to report symptoms of lightheadedness when
changing positions (because this is a symptom of orthostatic hypotension)
▪ Warn patients to avoid alcohol when taking bromocriptine
▪ Teach patients to check their heart rate and report heart rates that changes or
there will be irregularity noted
▪ Counsel patients not to abruptly stop the medication or the drug without first
notifying a healthcare provider
4.)Monoamine oxidase-B inhibitor (MAO-B inhibitor)
Examples:
▪ Selegiline hydrochloride
▪ Rasagline
-inhibit MAO-B -> prolongs the action of levodopa
Note: the enzyme MAO-B causes catabolism or breakdown of dopamine
➢ Selegiline HCl
- can delay the use of carbidopa-levodopa by one year
*Take note that in parkinson's disease dopamine is actually depleted already
because the production is not enough considering that there is degeneration
of the dopaminergic neurons and so the produced dopamine has to be
preserved but unfortunately the enzyme called MAO-B or monoamine oxidase
b causes catabolism of the dopamine thereby these enzymes will further
deplete or decrease the number of dopamine so Selegiline will inhibit the
MAO-B thus the dopamine will be preserved or the dopamine will not be
catabolized
*Monoamine oxidase A or MAO-A is an enzyme that promotes the metabolism of
tyramine in the GI tract if tyramine is not metabolized it can cause
hypertensive crisis - a severe increase in the blood pressure that may lead to
stroke
TAKE NOTE: Selegiline inhibits both MAO-B and MAO-A, so be wary!
Patient teaching:
▪ Urging him or her to avoid foods high in tyramine such as aged cheese,
red wine, cream, yogurt, chocolate, bananas, raisins, etc. to prevent
hypertensive crisis
▪ Inform the patient that severe drug interaction may occur between
Selegiline and various tricyclic antidepressants or TCAs and Selective
Serotonin Reuptake Inhibitors or SSRIS

5.)Catechol-O-methyltransferase or the COMT inhibitor


Examples:
▪ Entacapone
▪ Tolcapone
! Aside from the fact that dopamine level is decreased there is also a possibility that
dopamine will be inactivated because of COMT - this enzyme inactivates the
dopamine
! these medications will inhibit or stop the COMT from inactivating the dopamine
! when taken with levodopa preparations, COMT inhibitors increase the amount of
levodopa concentration in the brain

❖ Tolcapone - the first COMT inhibitor given with levodopa


! this medication can affect liver function
! Nursing action - you need to check for the liver enzymes in order for you to
determine the liver function of the patient
! patients with liver dysfunction should not take this drug
Side effects:
-dark discoloration of urine, and
-perspiration may be dark (these are harmless)

❖ Entacapone - it does not affect liver function


! a combination of carbidopa levodopa and entacapone provides greater dosing
flexibility and individualization
! you need to inform the patient that urine can have brownish-orange color
discoloration
**The use of entacapone and tolcapone

▪ can intensify the actions of levodopa which may lead to intense and controllable
urges like sex, gambling, and spending money
▪ suddenly falling asleep (you need to warn patient to avoid driving and other
potentially dangerous activities)
EPILEPSY
- a group of neurological diseases characterized by recurrent seizures.

SEIZURE
- happen as a result of sudden surge in the brain’s electrical activities.
- depends on what part of the brain is affected its symptoms include:
❖ loss of awareness
❖ unusual behaviors/sensations
❖ uncontrollable movements
❖ loss of consciousness

The brain is a complex network of billions of neurons.


NEURONS - can be exitatory or inhibitory

● EXITATORY NEURONS - stimulates others to fire rxn potentials and transmit electrical
messages
● INHIBITORY NEURONS - suppress this process, preventing excessive firing

❏ A balance between excitation and inhibition is essential for normal brain functions.

❏ In epilepsy, there is an UP regulation of exitation and and/or DOWN-regulation of


inhibition, causing lots of neurons to fire SYNCHRONOUSLY at the same time.

❏ If this abnormal electrical surge happens within a limited area of the brain, it causes
PARTIAL or FOCAL seizures. Partial seizures subdivide further to:

- Simple partial - depending on the affected brain area, patients may have unusual
feelings, strange sensations, or uncontrollable jerky movements, but remain
conscious and aware of the surroundings .

- Complex partial - involve the loss or changes in consciousness, awareness, and


responsiveness.

❏ If the entire brain is involved, GENERALIZED seizures will result. Generalized seizures
subdivide further to:

- Absence seizures - occurs most often in children, characterized by a brief loss


of awareness, commonly manifested as a blank stare, with or without subtle body
movements such as eye blinking or lip smacking. People with this type of seizure
may not be aware that something is wrong for years.
- Tonic seizures - associated with stiffening of muscles and may cause the
person to fall.
- Atonic seizures, drop attacks - characterized by a sudden loss of muscle tone
which may cause the person to collapse or drop down.

- Clonic seizures - associatd with rhythmic, jerky muscle movements, are rare

- Myoclonic seizures - brief jerks or twitches of a muscle or a group of muscles.


There can be one or many non-rhythmic twitches recurring within a couple of seconds.

❏ Tonic-clonic seizures, also known as convulsive seizures - The most common and
also most dramatic, are combinations of muscle stiffening and jerking. This type is what
most people relate to when they think of a seizure. It also involves sudden loss of
consciousness and sometimes loss of bladder control. A tonic-clonic seizure that lasts
longer than 5min requires immediate medical treatment.

Epilepsy may develop as a result of a:


➔ brain injury
➔ tumor
➔ stroke
➔ previous infection
➔ birth defect

❏ Generalized seizures that start in childhood are likely to involve genetic factors.
Epilepsy due to a single gene mutation is rare. More often, an interaction of multiple genes and
environmental factors is responsible. Hundreds genes have been implicated.

❏ Examples include genes encoding for GABA receptors – major components of the
inhibitory circuit, and ion channels.

❏ Many genetic disorders that cause brain abnormalities or metabolic conditions have
epilepsy as a primary symptom.

❏ The cause of epilepsy is unknown in about half of cases.

❏ Diagnosis is based on observation of symptoms, medical history, and an


electroencephalogram, or EEG, to look for abnormal brain waves.

❏ An EEG may also help in differentiating between partial and generalized seizures.

❏ Genetic testing maybe helpful when genetic factors are suspected.


❏ There is no cure for epilepsy but various treatments are available to control seizures.

❏ Medication successfully controls seizures for about 70% of cases.

❏ Many anti-epileptic drugs are available which target sodium channels, GABA
receptors, and other components involved in neuronal transmission. Different
medicines help with different types of seizures. Patients may need to try several drugs to
find the most suitable.

❏ Dietary therapy: ketogenic diet has been shown to reduce or prevent seizures in many
children whose seizures could not be controlled with medication.

❏ Ketogenic diet is a special high-fat, low-carbohydrate diet that must be prescribed and
followed strictly. With this diet, the body uses fat as the major source of energy instead
of carbohydrates. The reason why this helps control epilepsy is unclear.

❏ Nerve stimulation therapies such as vagus nerve stimulation in which a device


placed under the skin is programmed to stimulate the vagus nerve at a certain rate. The
device acts as a pacemaker for the brain. The underlying mechanism is poorly
understood but it has been shown to reduce seizures significantly.

❏ A surgery may be performed to remove part of the brain that causes seizure. This is
usually done when tests show that seizures are originated from a small area that does
not have any vital function.
UNDERSTANDING PARKINSON’S DISEASE (PD)

PATHOLOGY

➢ Patients with PD experience a loss of cells to a region of the brain called SUBSTANTIA
NIGRA
➢ Patients with PD will see a decline in physical, psychological, and neurological funtions.
➢ The disease manifests in a form of slowed movement known as BRADYKINESIA
➢ Resulting in muscle tremors, gait problems, rigidity or stiffness,postural instability, and
cognitive impairment
➢ The disease is both chronic and progressive, patients gradually lose their ability to
perform even the simplest of tasks.
➢ No cure for Parkinsons, a number of treatments are available for the management of
motor and non-motor symptoms to be used in combination of medications.
➢ Currently, the most popular surgical therapy for the treatment of PD is DEEP BRAIN
STIMULATION (DBS)
➢ Targeted exercise that focuses on general mobility and dexterity may slow down the
progression of the disease
➢ Lifestyle modifications, balanced diet, and rest may also slow down symptoms.
➢ An upcoming form of treatment for PD is VIRTUAL REALITY (VR)

SUBSTANTIA NIGRA - produces Dopamine

DOPAMINE
- a chemical messenger responsible for transferring signals within the brain that
allow coordination of movement.
- when dopamine levels decrease it causes abnormal brain activity, leaving patients less
able to direct or control movements

DEEP BRAIN STIMULATION (DBS)


- delivers electrical pulses to brain cells to decrease the symptoms of PD
- typically works best to lessen motor symptoms like stiffness, slowness, and tremors

VIRTUAL REALITY (VR)


- a fun way to practice motor skills, while also combatting depression
- ranges from treadmill therapy, balance and gait exercises, to therapy tools that provide
excitement and prevent boredom.
Patients with MYASTHENIA GRAVIS experience a decreased ability of muscle movement.

NEUROLOGICAL COMPONENT OF THIS DISEASE AND WHAT WE CAN DO ABOUT IT NERVOUS

SYSTEM
- a group of neurons with gaps in between electrical signals pass between these gaps
from one neuron to the next with the help of neurotransmitters

PIC OF NEUROTRANSMITTER ACETYLCHOLINE

- when acetylcholine binds to the receptor, it opens the receptor and allows sodium to
enter

PIC OF SODIUM

- when sodium enter neuron, its ionic charge allows electrical signal to move from last
neuron to the next
- with acetylcholine bound to the receptor the electrical signal fires until it reaches the
muscle
PIC OF ACETYLCHOLINESTERASE

ACETYLCHOLINESTERASE
- enzyme that breaks down acetylcholine
- breaking down acetylcholine will stop it from being able to open the receptor
- if receptor stays closed---then sodium cannot enter---electrical signal cannot be relayed to the next
nerve
- Acetylcholinesterase Inhibitors WILL BIND to acetylcholinesterase and keep them from breaking
down acetylcholine
- since acetylcholine is NOT broken down, it can BIND to the receptor and ALLOW sodium to ENTER
and allows electrical signal to continue to next neuron

With the nerve impluse continuing to its destination,the muscles can contract and relax. Acetylcholinesterase Inhibitors for

Myasthenia Gravis: Pyridostigmine (medication)


NOTABLE SIDE EFFECTS OF PYRIDOSTIGMINE : Retroperitoneal fibrosis/Retropulmonary
fibrosis
Left side cardiac valve dysfunction
Drugs for Alzheimer’s disease

Alzheimer’s Disease

- Is an incurable dementia illness


- Characterized by Chronic,progressive neurodegenerative the onset is usually between 45 to 65 years
of age.

Theories related to changes that cause the Alzheimer’s disease:

• Degenaration of the cholinergic neuron and deficiency in acetycholine


• Neuritic plaques that form mainly outside of the neurons and in the cerebral cortex
• Apolipoprotein E4 that promotes formation of plaques,which binds beta amyloid in the plaques
• Beta-amyloid lipoprotein accumulation in high levels that may contribute to neuronal injury
• Presence of neurofibrillary tangles with twists inside the neurons

Acetylcholinesterase/Cholinesterase Inhibitor
- is a classification of medication that can be administered to a patient with alzheimer’s disease take note
that one of the theories in alzheimer’s disease poses that there is degeneration of the cholinergic
neuron and there is deficiency in acetylcholine.
- An enzyme called acetylcholinesterase breaks down acetylcholine if this will happen the level of
acetylcholine will further deplete to prevent such from happening.
- Administered which will then inhibit the cholinesterase and preserve the acetylcholine
Ex. Of these medications:

• Donepezil
• Memantine
• Galantamine
• Revastigmine
Rivastigmine
- Increases the amount of Ach at the cholinergic synapses
- Give twice a day
- Contradicted to patients with liver disease because hepatotoxicity may occur.

Assessment
• Assess the patient’s mental and physical abilities.
• Obtain a history that includes any liver or renal disease or dysfunction
• Assess for memory and judgement loss
• Observes for signs of behavioral disturbances
• Examine pt. for signs of aphasia
• Note motor function
• Determine family member’s ability to cope with patient’s mental and physical changes.

Nursing Diagnosis:
• Self care Deficit related to memory loss
• Chronic confusion related to memory loss

Planning:
• Patient’s memory will be improved
• Patient will maintain self care of body functions with assistance

Nursing Interventions
• Assist the patient in ambulation and activity
• Monitor for side effects
• Record Vital signs periodically
• Observe any patient behavioral changes
• Patient teaching:
-Teach family members about safety measures
-Patient should rise slowly to avoid dizziness and loss of balance
-Monitor routine liver function tests

Evaluation
• Evaluate effectiveness of drug regimen
Drugs for Myasthenia Gravis
-is a chronic autoimmune neuro muscular disease that affects approximately 20 in every 100 000 people

Antibodies attack the acetylcholine receptor sites then later on these receptor sites will be obstructed and
eventually destroyed so there will be less acetylcholine receptor sites and so the acetylcholine molecucles are
prevented from binding to the receptors and the stimulation of normal neuromuscular transmission is inhibited
thereby there is ineffective muscular contraction and weakness because take note your acetylcholine is very
important neurotransmitter in order for your muscles to contract so if theres a problem with the transmission so
later on there will be also a problem in relation to muscle contraction.

Manifestations:
• Ptosis
• Diplopia
• Dysphagia
• Dysarthia
• Respiratory muscle weakness
Acetylcholine may also be depleted because of the enzyme Acetylcholine or cholinesterase take note
that this enzyme is responsible for the breakdown of acetylcholine and so to stop that
acetylcholinesterase will be administered in order to inhibit the action of the acetylcholinesterase
and it will prevent the breakdown of acetylcholine thus preserving acetylcholine and this means
that there is more acetylcholine available to activate the cholinergic receptors and promote
muscle contraction.
Ex medications:
Neostigmine
Pyridostigmine

Neostigmine
• Short-acting, with half life of 0.5-1 hour
• Must be given on time to prevent muscle weakness

Pyrodostigmine
• Half-life of oral pyrodostigmine is 3-7 hours and is 2-33 hours for IV
• Given every 4-6 hours
• Increases muscle strength
Take note that overdosing or under dosing of acetylcholinesterase inhibitors has an effect it could be
Myasthenic crisis or cholinergic crisis.it is

Myastheic Crisis
- Underdosage of acetylcholinesterase inhibitor
- Severe complication manifested as generalized muscle weakness that may involve the muscles of
respiration
- Triggered by infection,emotional stress,menses,pregnancy,surgery, trauma,hypokalemia,temperature
extremes and alcohol intake
- Occurs 3-4 hours after taking certain medications like
aminoglycosides,phenytoin,macrolides,fluoroquinolones,quinine,quinidine,magnesium salt,psychotropic
medications and neuromuscular blocking agents.

Cholinergic Crisis
- And overdosage of the acetylcholinesterase inhibitor
- Occurs within 30-60 mins after taking anticholinergic drugs,this complication is due to continuos
depolarization of post synaptic membranes that creates neuromuscular blockade
- Often has severe muscle weakness that can lead respiratory paralysis and arrest accompanying
symptoms include meiosis or abnormal pupil constrictiom,power,sweating,vertigo,excessive
salivation,nausea vomiting,abdominal cramping,diarrhea,bradycardia and fasciculations or
involuntarymuscle twitching.

Endrophonium
- is a ultra short acting cholinesterase inhibitor may be used to distinguish between the myasthenic crisis
from cholinergeic crisis.
- Used to diagnose myasthenia gravis its ultra short duration of 5 to 30 mins. Increases muscle strength
immediately.

If unresponsive to AChE inhibitors:


• Prednisone- Drug choice but like other immunosuppressants it reduces the presence of antibodies.
• Plasma exchange
• IV immune globulin
• Immunosuppressive drugs

Side effects and adverse reactions of AChE Inhibitors:


- Nausea - Abdominal cramps - Blurred Vision
- vomiting - Increased salivation - Tachychardia
- diarrhea - Tearing - Hypotension
- abdominal cramps - Miosis

Pyrodistigmine

Assesment:

• Obtain a drug history


• Observe the patient’s drug profile.
• Record baseline vital signs.
• Assess for s/s of myasthenic crisis

Nursing Diagnosis:

• Ineffective breathing pattern related to weak respiratory muscle


• Activity intolerance related to fatigue
Planning:
• Patient’s symptoms of muscle weakness,difficult in breathing, and difficulty in swallowing
caused by MG will be eliminated or rediced in 2-3 days.

Nursing interventions:
• Monitor effectiveness of drug therapy.
• Administered prescribed AChE inhibitor following dosage recommendation
• Observe for cholinergic crisis
• Have antidote for cholinergic crisis ready: Atroponine Sulfate

Patient teaching:
• Teach patient to take drugs as ordered
• Encourage pt. to wear a medical ID or necklace that indicates health problem
• Teach pt.about side effects
• Inform pts to take the drug meals for best absorption
Evaluation:
• Evaluate effectiveness of drug therapy
• Determine the absence of respiratory distress
• Evaluate the correct use of the drug by the patient

Drugs for multiple Sclerosis


- Is a autoimmune disorder that attacks the myelin sheath of the nerve fibers in the brain and the spinal
cord which results in the lesions called plaque.
- Cause is unknown,it is thought that the disease develops in a genetically susceptible person as a results
of environmental exposure like an infection the onset of multiple sclerosis is usually slow
- It is a condition in which there are remissions and exacerbations of multiple symptoms

Problems:
• Motor
• Sensory
• Neurologic
• Cerebellar
• Emotional

Immunomodulators
• Are disease-modifying drugs
• The first line of treatment for MS
• Examples:
-Beta interferon
Interferon beta 1-a
Interferon beta 1-b
-Glatiramer acetate
-Teriflunomide

Other medications for MS:.


Alemtuzumab
- A monoclonal Antibody
Corticosteroids
- Lowers inflammation in the body
- Reduces immune system activity

Beta 1-b and Glatiramer acetate


- Administered subcutaneously either once daily or 3x a week depending on the health care provider’s
order
Teriflunomide
- Is an oral drug
- Administered daily
Alentuzumab
- Requires a daily IV dose of 12 mg for 5 consecutive days and in 12 months ,an additional 12 -mg dose
for 3 consecutive days

Corticosteroids
- Used to manage exacerbation of MS
antipsychotic agents - are also known as neuroleptics or psychotropics but the preferred name for
this group is either antipsychotics or neuroleptics.
neuroleptic - refers to any drug that modifies psychotic behavior and exerts an antipsychotic effect

antipsychotic agents and its indication

Psychosis - is defined as the loss of contact with reality

manifestations or signs and symptoms of psychosis include the following:


1.difficulty processing information
2.disorganized thought
3.distortion of reality
4.delusion
5.Hallucination
6.incoherence
7.catatonia
8.aggressive or violent behavior

Schizophrenia- a chronic psychotic disorder is the major category of psychosis in which many of the
mentioned symptoms are manifested

antipsychotic agents are divided into two categories:


the typical antipsychotic agents and the atypical antipsychotic agents
the typical antipsychotic agents are effective in treating positive symptoms of schizophrenia while for
the atypical antipsychotic
agents these are effective in treating both
the negative and the positive symptoms of schizophrenia
typical antipsychotic agents have specific subclassifications which include
phenothiazine and non-phenothiazine
Under the phenylphiasin group examples of which are the aliphatic
Phenothiazines ,the biperazine and ,the bipyridine

non-phenothiazine
we have the buterophenones ,the benzoxazipines ,the hydroendolones and the thiosunthenes.

examples of medications for the atypical antipsychotic agents include clozapine(Clozaril),


olanzapine(Zyprexia) ,respiridone(Rispedal) quetiapine(seroquel) ,zipracidone(ziprasidone) ,and
aripiprazole(abilify)

antipsychotic agents block the action of dopamine and thus may be classified as dopaminergic
antagonists specifically it blocks the dopamine receptors

there are five subtypes of dopamine receptors


numbered as d1 through d5 all antipsychotic agents block the d2 or the dopaminergic receptor which
in turn promotes the presence of extrapyramidal symptoms.
extra extrapyramidal symptoms include shoulda parkinsonism, akathesia dystonia and tardive
dyskinesia

on the other hand atypical antipsychotics have a weak affinity to detail receptors and a stronger affinity
to d receptors and they block the serotonin receptor. these agents cause fewer extra pyramidal
symptoms than typical antipsychotic agents which have strong affinity to detail receptors

phenothiazinegroup
1. Aliphatic -aliphatic medications produce a strong sedative effect decrease blood pressure and may
cause moderate extrapyramidal symptoms. an example of an aliphatic medication is chlorpromazine
hydrochloride thorazine

2. piperazine- piperacin produce more extrapyramidal symptoms dry mouth urinary retention and
aggranocytosis. an example of this medication is the flofenazine and perfinazine

3. Piperidine- has a strong sedative effect few extra pyramidal symptoms has a low to moderate effect
on blood pressure and has no anti-emetic effect. an example of this classification of medication is
thioridazine.
most antipsychotics can be given orally in a form of tablet or liquid. it can also be given intramuscularly
or intravenously. for oral use the liquid form might be preferred because some patients may hide tablets
in their cheek or under their tongue to avoid taking them. mouth checks are necessary for non-compliant
patients.

phenothiazine metabolites may cause a harmless pink to red brown urine color the
Full therapeutic effect of oral antipsychotics may not be evident for three to six weeks following initiation
of their therapy but an observable therapeutic response may be apparent after seven to ten days.

Nonphenothiazine
1. butyrophenone group- a frequently prescribed nonphenothiazine
specifically under butyrophenone is haloperidol (Haldol)
haloperidol's pharmacologic behavior is similar to that of the phenothiazines.
it is a potent antipsychotic drug in which the equivalent prescribed dose is smaller than that of drugs of
lower potency

the drug dose for haloperidol is 0.5 To 5 milligrams


Administration precautions should be taken to prevent soreness and
inflammation at the injection site

that is if the medication is administered intramuscularly. because the medication is a viscous liquid a
large gauge needle such as gauge 21 should be used with a z track method for administration in a
deep muscle. the injection site should not be massaged and sites should be rotated

these medications should not remain in a plastic syringe longer than minutes take note
this is true if the medication is administered intramuscularly
there are also capsules or tablet forms of haloperidol
2. Dibenzoxazepine- this classification of medication has moderate sedative and orthostatic
hypotensive effect an example of this medication
is loxapine

3. dihydroindolone -this medication has low sedative and orthostatic hypotensive effect
an example of this classification of medication is molindone

4. thioxanthene -produces low sedative and orthostatic hypotensive effect


an example of this classification of medication is a thiothexine

side effects and adverse reactions of antipsychotic medications include:


A. drowsiness
B. dry mouth
C.increased heart rate
D.urinary retention
E.Constipation
F.decreased blood pressure
G.blood dyscrasias
H.photosensitivity
I.extrapyramidal symptoms

Under extrapyramidal symptoms it includes Pseudoparkinsonism, Akathisia, Dystonia, Tardive


dyskinesia

Pseudoparkinsonism- characterized by stupid posture ,shuffling gate, rigidity bradykinesia, tremors


at rest and pill rolling motion on the hand

characteristics of akathisia include restlessness, trouble standing still, paces the floor
and feet in constant motion ,rocking back and forth
acute dystonia is characterized by facial grimacing ,involuntary upward eye movement ,muscle
spasms on the tongue face neck and back (the back muscle spasms cause trunk to arch forward)
further in acute dystonia there is
laryngeal spasms
tardive dyskinesia is characterized by protrusion and rolling of the tongue,
sucking and smacking movements of the Lips, chewing motion ,facial dyskinesia And, involuntary
movements of the body and extremities

these extrapyramidal symptoms can begin within-days after initiation of antipsychotic therapy and are
most prevalent with the Phenothiazines, butyrophenones and thiosanthines
tardive dyskinesia may develop in 20% of patients taking antipsychoticsfor long-term therapy
Neuroleptic malignant syndrome is a rare but potentially fatal condition associated with antipsychotic
drugs

predisposing factors include excess agitation, exhaustion and dehydration

neuroleptic symptoms involve muscle rigidity ,hyperthermia altered mental status, profuse diaphoresis,
blood pressure fluctuations, tachycardia ,dysrhythmias, seizure rhabdomyolysis ,acute renal failure,
respiratory failure ,and coma.

treatment of neuroleptic malignant syndrome involves immediate withdrawal of


Antipsychotics, adequate hydration, hypothermic blankets, administration of antibiotics ,
benzodiazepines and muscle relaxants such as dendrolene

atypical antipsychotic agents -these are effective in treating both positive and negative symptoms of
schizophrenia

these are not likely to cause extrapyramidal syndrome


drug examples of atypical antipsychotic agents include :
clozapine
olanzapine
Respiradone
Quetiapine
Ziprasidone
Aripiprazole

common side effects of atypical antipsychotic agents include:


weight gain
drowsiness
Unsteadt gait
Headache
insomnia
depression
diabetes mellitus
Dyslipidemia

drug to drug interactions

phenothiazines can decrease the effect of anticonvulsants thus an adjustment on the dosage of the
anticonvulsant may be necessary but take note that it has to be prescribed by the physician so you as
a nurse your responsibility here if and when the patient has seizure and is taking an anti-seizure
medication is that you need to inform the physician right away so that the physician can adjust the
dosage of the medication

potentiates the effect of antipsychotic medication: the alcohol, hypnotics ,sedatives


Narcotics, benzodiazepines and atropine

Antihypertensive medications can cause additive hypotensive effects


you need to monitor the vital signs of the patient particularly the blood pressure

What should comprise your assessment for a


patient who's taking a phenothiazine or a non-phetothiazine Medication or in general an antipsychotic:
you must assess baseline vital signs for use in future comparisons

obtain a patient health history that includes present drug therapy


if the patient is taking an anticonvulsant the drug dose might need to be increased because
antipsychotics tend to lower the seizure

assess mental status and cardiac eye and respiratory disorders before starting drug therapy and
continue daily assessment
Possible nursing diagnosis you can formulate are
ineffective relationship related to social withdrawal
risk for loneliness

what is our plan why are we administering phenothiazine or nonphenothiazine medication to our
patients ? it is to improve the psychotic behavior of our patients through medications, psychotherapy
and, adjunct therapy

Nursing Interventions antipsychotic medications


A.to monitor vital signs because orthostatic hypotension is likely to occur
B.remain with patients while medication is taken and swallowed because some patients hide
antipsychotic medications in the mouth
C.to avoid taking them avoid skin contact with liquid concentrates to prevent contact dermatitis liquid
medications must be protected from light
D.Should be diluted with fruit juice administer oral doses with food or milk
to decrease gastric irritation dilute oral solution of lofenazine in fruit juice
water or milk avoid apple juice and caffeinated drinks
E.Administer deep into muscle because drug irritates fatty tissue
F. Record urine output because urinary retention may result
G.Monitor serum glucose level
H.inform patientsthat medication may take six weeks or longer to achieve full clinical effect
I.teach smoking cessation
J.guide patients to maintain good oral hygiene
K.instruct them to promptly report symptom to a healthcare provider
L.encourage patients to wear sunglasses for photosensitivity to limit exposure to direct sunlight and to
use sunscreen and protective clothing to prevent a skin rash
M.suggest lozenges or hard candy if mouth dryness occurs
N. advise patients to rise slowly
Evalution:
⚫ effectiveness of the drug and whether the patient has acceptably reduced psychotic symptoms at
the lowest dose possible ascertain whether the patient can cope with everyday living situations and
Attend to activities of daily living
⚫ determinewhether any side effects have adversereactions to the drug have occurred

anxiolytics
- primarily used to treat anxiety and insomnia

signs and symptoms of severe anxiety:


⚫ dyspnea
⚫ Choking
⚫ chest pain
⚫ heart palpitation
⚫ dizziness
⚫ faintness
⚫ Sweating
⚫ trembling
⚫ shaking
⚫ fear of losing control

Non-Pharmacologic measures of anxiety attack


1. relaxation technique
2. Psychotherapy
3. Support groups

Medication: benzodiazepine
-multiple uses such as anticonvulsant , sedative hypnotic ,pre-operative drug
substance abuse withdrawal, and anxiolytic
-mainly for severe or prolonged anxiety examples

Examples of benzodiazepines
⚫ Chlordiazepoxide
⚫ Diazepam
⚫ Clorazepate dipotassium
⚫ Lorazepam- the most frequently prescribed
⚫ Alprazolam
Assessment:
Assess for suicidal ideation
Determine the patients support system
Obtain a drug history

Diagnosis;
Anxiety related to situational crisis

Planning:
aim to reduce the anxiety and stress of the patient through pharmacologic methods like the use of
benzodiazepines or support in group therapy

Nursing interventions:
Observe patient for side effects
Monitor vital signs
Encourage family to be supportive of thepatient
Advise patients not to drive a motorvehicle
Warn patients not to consume alcohol or cns depressants
Inform patients that an effective response may take one to two weeks
Encourage patients to rise slowly from sitting to standing positions to avoid dizziness fro orthostatic
hypotension

Evaluation:
Evaluate the effectiveness of drug therapy
Determine whether the patient is taking the anxiolytic drug as prescribed

ANTIDEPRESSANT AGENTS
-that are used to treat clinical depression or prevent it from recurring

Depression
⚫ most common mental illness
⚫ Characterized primarily by mood changes and loss of interest in normal activities
Types:
1. Reactive
2. Major depression
3. Bipolar Disorder

5 groups of Antidepressants
1.Tricyclic antidepressants or (tca) or trycyclics
2.selective serotonin reuptake inhibitors or (ssris)
3.Serotonin norepinephrine reuptake inhibitor or (snris)
4.atypical antidepressants
5. monoamine oxidase inhibitors (MAOIs)

1. Tricyclic antidepressants or (tca) or trycyclics


- used to treat major depression because this blocks the uptake of neurotransmitter
norepinephrine and serotonin in the brain
- clinical response is after two to four weeks of drug therapy

side effects and adverse reactions :


⚫ orthostatic hypotension
⚫ Sedation
⚫ anticholinergic effects
⚫ Cardiotoxicity seizure

we've been mentioning anticholinergic effects what is the most common anticholinergic effect that we've mentioned
ever since we started this topic that is urinary retention

Drug examples:
⚫ Amitriptyline HCL
⚫ imipramine
⚫ trimipramine
⚫ Doxepin
⚫ Clomipramine HCL
Alcohol hypnotics sedatives and barbiturates potentiate the cns depression when taken with tca

2. selective serotonin reuptake inhibitors or (ssris)


-this group of antidepressants block the reuptake of serotonin in the nerve terminals of the cns
-used for major depressive disorders

Drug examples:
⚫ Fluoextine
⚫ Fluvoxamine
⚫ sertraline
⚫ Paroxetine
⚫ Citalopram
⚫ escitalopram

-Many ssris have an interaction with grapefruit juice that can lead to possible toxicity

Side Effects:
⚫ dry mouth
⚫ blurred vision
⚫ Insomnia
⚫ headache
⚫ nervousness
⚫ anorexia
⚫ nausea
⚫ diarrhea
⚫ suicidal ideation

3. Serotonin norepinephrine reuptake inhibitor or (snris)


-inhibits the re-uptake of serotonin and norepinephrine
-used for major depression

Drug Examples:
⚫ Venlafaxine
⚫ Duloxetine
⚫ Desvenlafaxine
Side Effects:
⚫ drowsiness
⚫ Dizziness
⚫ insomnia
⚫ headache
⚫ euphoria
⚫ amnesia
⚫ blurred vision
⚫ ejaculatory dysfunction

Adverse Reactions:
⚫ Hypertension
⚫ Tachycardia
⚫ angioedema
⚫ seizures
⚫ suicidal ideation

4. atypical antidepressants
-the second generation
antidepressant
-used for major depression reactive depression and anxiety
-affects one or two of the three neurotransmitters which are serotonin,norepinephrin ,and dopamine

Drug Examples:
⚫ amoxipine
⚫ nephazodone
⚫ moprotiline
⚫ trazodone

should not be taken with maois and should not be used within 14 days after discontinuing maoi's

5. monoamine oxidase inhibitors (MAOIs)


-this group inhibits MAO-A and MAO-B
-mao a inactivates dopamine in the brain and mao-b inactivates norepinephrine and
Serotonin
-is used for mild reactive and atypical depression
drug examples:
⚫ Tranycypromine sulfate
⚫ Isocarboxazid
⚫ Selegiline HCLl
⚫ Phenelzine sufate

MAOI + CNS stimulants or sympathomimetics may result in hypertensive crisis


hypertensive crisis- is a severe increase in blood pressure that can lead to stroke

MAOI + tyramine rich food result to hypertensive crisis

Examples of tyramine rich food:


⚫ Cheese
⚫ cream
⚫ Yogurt
⚫ Coffee
⚫ chocolate
⚫ bananas
⚫ raisins
⚫ italian green beans
⚫ Liver
⚫ pickled foods
⚫ sausage
⚫ soy sauce
⚫ Yeast
⚫ Beer
⚫ red wines

Nursing Action: Monitor BP

Side Effects:
⚫ agitation
⚫ Restlessness
⚫ Insomnia
⚫ orthostatichypotension
⚫ anticholinergic effects

MOOD STABLIZERS
- used to treat bipolar affective disorder (is a psychological illness that involves severe mood
swings)
these mood swings take the form of depression or mania and may last for several months at a
time
during the time of depression patients often have a great sadness guilt no appetite poor sleep
and cannot enjoy themselves
mania is the opposite of this with patients experiencing erratic and excited behavior

drug examples:
⚫ lithium
⚫ Carbamazepine
⚫ Valproic acid
⚫ Divalproex
⚫ Lamotrigine

These are considered as the first line of drugs for bipolar disorder

Lithium
-is an inexpensive drug that must be closely monitored because it has a narrow therapeutic
serum range of 0.8 to 1.2 ml equivalent per liter

-serum sodium levels also need to be monitored because lithium tends to deplete sodium

side effects:
Dry mouth
Thirst
increased urination
weight gain
bloated feeling
metallic
taste
edema on the hands and ankle
Opioid Analgesic
- narcotic medications that treats severe pain (ex. Headache or muscle)

Examples of Opiod Analgesic:

1. Morphine Sulfate (Duramorph)


-supress pain impluses but also respiration and coughing

Indication:
-relief of moderate to severe pain,
-pre-operative medication
-as supplement to anesthesia

Contraindication
-head injury
-shock or very low blood pressure

Side effects and adverse reactions:


-drowsiness
-respiratory depression
-sedation
-euphoria
-hallucination
-headache
-palpitation
-Orthostatic hypotension
-Physiologic dependence
-Urinary retention
-Constipation

Antidote: (overdosage requirement)


Naloxone

ADPIE/ NURSING PROCESS

Assessment:
a. Obtain Medical history
- contraindications for morphine sulfate
include severe respiratory disorders
increased intracranial pressure, seizures may be present when taking these

b. Determine a drug history and check for drug allergies


- morphine increases effects of alcohol sedatives and hypnpotics, antiphsychotic drugs and muscle relaxants
-can cause respiratory depression
3. Assess vital signs
- can commonly decrease respirations and systolic blood pressure
-meisosis: constriction of pupils

4. Monitor urinary output


-morphine can cause urinary retention
Assess the type of pain, location, duration before giving opiods

Nursing Diagnosis
- Acute pain related to surgical tissue injury
-Ineffective breathing pattern related to excess morphine dosage

Planning
- To reduce and alleviate patient’s pain

Interventions:
-Administer morphine sulfate before pain reaches its peak
-Monitor vital signs – fewer than 10 respirations/min can indicate respiratory distress
-Record urine output – should be at least 600ml/day
-Check bowel sounds
-Check for pupil changes and reaction. Pinpoint pupils can indicate morphine overdose
-Have naloxone available
-Encourage patient not to use alcohol or CNS depressants
-Suggest non-pharmacologic measures to relieve pain
-Alert patient that continuous use of morphine sulfate can be addicting

Evaluation
- Evaluate the effectiveness of morphine in lessening or alleviating the pain in using consistent pain scale
-Determine the stability of vital signs

2. Meperidine
- can be given orally, Intramuscularly or IV routes
- primarily effective in GI procedures
-preffered during pregnancy (does not diminish contraction, and causes neonatal respiratory depression)
-not indicated to patients with chronic pain, sever liver dysfunction, sickle cell disease, history of seizure, severe CAD, and
cardiac dysrhythmia

3. Hydromorphone
-6x more potent than morphine
-for relief of moderate or severe pain
-when given IV, dilution of each dose with 5ml sterile water or NSS is preferred
-Direct administration of 2mg or less should be given over 2-3 minutes

Treatment of Migraine Headaches

Migraine Headaches
- characterized by unilateral throbbing head pain accompanied by nausea, vomiting, photophobia

For migraine attacks:


(prescribed medications)
-opioid analgesics
-ergot alkaloids (Ex. Dihydroergotamine mesylate)
-selective serotonin receptor agonists (triptan)
Ex. Of triptans: Sumatriptan, Naratriptan, Almotriptan

Mild migraine:
-aspirin
-acetamoniphen
-NSAIDS (ibuprofen and naproxen)
Nonopioid Analgesic – less potent than opioid and used to treat mild to moderate pain

Examples of Nonopioid drugs:


1.) NSAIDS -
2.) ACETAMINOPHEN - An analgesic and antipyretic drug
- A nonopioid drug but not an NSAID
- Causes little to no gastric distress and does not interfere with
platelet aggregation
- Overdose of this drug can be extremely toxic to liver cells

Fundamental Assessment for patients taking Acetaminophen:


Obtain medical history of liver dysfunction
Ascertain the severity of Pain

Nursing Diagnosis:
Risk for Injury
Acute pain related to edema from the surgical incision
Planning:
To alleviate the pain from the patient
Interventions:
Check hepatic enzyme tests
Teach patients to keep acetaminophen out of childrens reach
Advice patients not to self-medicate with acetaminophen for more than 10
days
Teach patients to check acetaminophen dosages on the label of OTC drugs.
4g/day
Avoid alcohol ingestion while taking the drug
Antidote for acetaminophen is acetylcysteine
Evaluation
Evaluate the effectiveness of the drug in terms of relieving pain using
consistent pain scale.
Determine whether the patient is taking the recommended dosage

ANTI-INFLAMMATORIES:
1.) NSAIDS
2.) CORTICOSTEROIDS
3.) DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
4.) ANTIGOUT DRUGS

1.) Nonsteroidal Anti-inflammatory drugs (NSAIDs) – its called non-steroidal


because its not related to corticosteroid (are a class of drug that lowers
inflammation in the body).
7 Groups of NSAIDs:

A.)Salicylates – derived from salicylic acid


Examples: Aspirin, Diflunisal, Olsalazine sodium and sulfasalazine

Note: Aspirin should not be taken during last trimester of pregnancy and children
with flu.

B.)Para-Chlorobenzoic Acid – used for rheumatoid arthritis, gouty arthritis, and


osteoarthritis.
Examples: indomethacin, Sulindac, and tolmetin

Note: indomethacin is very irritating to stomach and should be taken with food,
these types of drugs may also cause sodium and water retention and increase in
BP.

C.) Phenylacetic Acid Derivatives –


Examples: Diclofenac, Ketorolac tromethamine, and Etodolac

Note: Ketorolac are recommended for short term management of pain, like after
surgery bc its very effective in alleviating pain.

D.) Propionic Acid Derivatives – are aspirin-like but have stronger effects and
creates less GI irritation
Examples: Fenoprofen CA, Flurbiprofen, Ibuprofen, Ketoprofen,
Naproxen, and Oxaprozin

Note: its effect is decreased when taken with aspirin

E.)Fenamates – used for acute and chronic arthritis conditions


Examples: Meclofenamate sodium monohydrate, and Mefenamic Acid

Note: Gastric Irritation is a common side effect, therefore should be taken with
food.

F.) Oxicams – used for long term rheumatoid arthritis and osteo
Examples: piroxicam and meloxicam

Note: It can cause GI problems like ulceration and epigastric distress, it should not
be taken with aspirin and other nsaids.

G.) COX-2 inhibitor – Celecoxib (the only cox-2 inhibitor)

Indications: osteo and rheumatoid arthritis, dysmenorrhea, moderate to severe


pain, ankylosing spondylitis

Side effects: headache, dizziness, sinusitis, and abdominal pain

Adverse Reactions: Peripheral edema, bleeding, hypertension and stroke.

2.) CORTICOSTEROIDS – Controls inflammation by suppressing or preventing


many of the components of the inflammatory process at the injured site

Ex. Drugs: Prednisolone, Prednisone, and Dexamethasone

3.) DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDs) – Includes


Immunosuppressive agents, Immunomodulators, and antimalarials

4.) ANTIGOUT DRUGS – Gout is inflammatory condition that attacks joints,


tendons, and other tissues. There are three types

• Anti-inflammatory gout drug - acts as inhibitor in the migration of


leukocytes to the inflamed site.
Ex. Colchicine

• Uric-Acid Biosynthesis Inhibitors – inhibits the final step of uric acid


biosynthesis.
Ex. Allopurinol

• Uricosurics – Increase the rate of uric acid excretion.


Ex. Probenecid and Sulfinpyrazone
NOTE: ASPIRIN SHOULD BE AVOIDED BY PATIENTS WITH GOUTY
ARTHRITIS.

SUMMARY:

Nonopioid Analgesic – less potent than opioid and used to treat mild to moderate pain

Examples of Nonopioid drugs:


1.) NSAIDS
2.) ACETAMINOPHEN

ANTI-INFLAMMATORIES:
1.) NSAIDS
2.) CORTICOSTEROIDS
3.) DISEASE-MODIFYING ANTIRHEUMATIC DRUGS
4.) ANTIGOUT DRUGS

4 Therapeutic effects of NSAIDs:


• Anti-inflammatory effect -
• Analgesic effect – alleviate pain
• Antipyretic effect – it lowers body temp.
• Anticoagulant effect – it decreases platelet aggregation

7 Groups of NSAID:
1.) Salicylates
2.) Para-Chlorobenzoic Acid
3.) Phenylacetic Acid Derivatives
4.) Propionic Acid Derivatives
5.) Fenamates
6.) Oxicams
7.) COX-2 Inhibitors

Important note: the first 6 groups of NSAIDs have the same mechanism of action which is to
block COX-1 and COX-2 and the 7th has a mechanism of only blocking COX-2. COX stands for
cyclooxygenase.

What happens when COX-1 and COX-2 is blocked:


COX-1 – stomach bleeding and ulcer may occur, and decreased in platelet aggregation.
COX-2 – Pain and Fever are reduced and Inflammation is suppressed.

GENERAL SIDE EFFECTS AND ADVERSE EFFECTS OF 1st generation NSAIDs


- Gastric irritation is common when NSAID is taken without food
- Sodium and Water retention may occur
- Alcoholic beverages when taken with NSAID may increase gastric irritation.
Thus, should be avoided.
AUTONOMIC NERVOUS SYTEM (ANS)

⁃ part of the nervous system that regulates activities of internal organs.

⁃ Is largely AUTONOMOUS, acting independently of the body's consciousness and voluntary


control.

⁃ It has two main divisions:

⁃ � Sympathetic, SNS

⁃ � Parasympathetic, PSNS

✏️ in situations that requires alertness and energy, such as facing danger or doing physical
activities, the ANS activates its sympathetic division to mobilize the body for action.

✏️This division increases:

� cardiac output

� accelerates respiratory rate

� releases stored energy

� dilates pupil

✏️ it also inhibits body processes that are less important in emergencies, such as:

� digestion and urination

✏️On the other hand, during ordinary situations, the parasympathetic division:

� conserves and restores

� it slows heartbeats, decreases respiratory rate, stimulates digestion, removes waste and stores
energy.

� � The sympathetic division is therefore known as the "FIGHT or FLIGHT" response, while the
parasympathetic division is associated with the "REST and DIGEST" state.

Despite having opposite effects on the same organ the S&S and PS NS are not mutually exclusive
in most organs both systems are simultaneously active producing a background rate of activity
called the autonomic tone a balance between sympathetic and parasympathetic inputs.

This balance shifts one way or the other in response to the body's changing needs some organs,
however receive inputs from only one system, for example the smooth muscles of blood vessels
only receives sympathetic fibers which keep them partially constricted and thus maintaining
normal blood pressure an increase in sympathetic firing rate causes further constriction and
increases blood pressure. While a decrease in firing rate dilates blood vessels lowering blood
pressure.

The autonomic nerve pathways from the control centers in the central nervous system

✏To the target organs are composed of two neurons which meet and synapse in an autonomic
ganglion

Accordingly, these neurons are called pre ganglionic and post ganglionic in the SNS the pre
ganglionic

neurons arise from the thoracic and lumbar regions of the spinal cord their fibers exit by way of
spinal nerves to the nearby sympathetic chain of ganglia.

✏Once in the chain preganglionic fibers may follow any of three routes

some fibers synapse immediately with post ganglionic neurons

Some travel up or down the chain before synapsing

ANS 1

Afferent/Sensory Neurons – sends impulses to the CNS where they are interpreted or
integrated

Efferent/Motor Neurons – receives the impulses or informationfrom the brain and transmits
these impulses through the spinal cord to the effector cells

SYMPATHETIC NERVOUS SYSTEM PARASYMPATHETIC NERVOUS


SYSTEM
- “adrenergic system” - “cholinergic system”
- Neurotransmitter: Norepinephrine - Neurotransmitter: Acetylcholine
- 4 main types of adrenergic receptor (innervates the muscle at the end of the
organ cells: alpha1, alpha2, beta1, neuron)
beta2 - The cholinergic receptors at organ cell:
nicotinic, muscarinic

*Both act on the same organ but produce opposite responses to provide homeostasis or balance ;
can act as stimulating agent or a depressing agent

*Acetylcholinesterase is an enzyme that may inactivate acetylcholine before it reaches the


receptor cell.

Drugs that affect the Sympathetic Nervous System

1. Adrenergic Agonists
- Drugs that stimulate the sympathetic nervous system
- Also called as “adrenergics” or “sympathomimetics”
- They mimic the sympathetic neurotransmitters norepinephrine and epinephrine
- They act on one or more adrenergic receptor sites located in the effector cells of muscles
(such as the heart, bronchiole walls, GI tract, urinary bladder and ciliary muscles of the
eyes)

Inactivation of Neurotransmitters:
1. Reuptake of the transmitter back into the neuron (nerve cell terminal)
2 enzymes that inactivates Norepinephrine:
Monoamine Oxidase (MAO) – located inside the neuron
Catechol-O-methyltransferase (COMT) – located outside the neuron
*These medications can prolong the action of neurotransmitter by either inhibiting the reuptake
or inhibiting the degradation by enzymatic action
2. Enzymatic transformation or degradation
3. Diffusion away from the receptor

Effects of Adrenergic Agonist at Receptors

ALPA 1 [Blood vessels, Eye, Bladder, Prostate]

ALPHA 2 [Smooth muscle or GI tract, Blood vessels]

BETA 1 [Heart, Kidney]

BETA 2 [Uterus, Liver, Smooth muscle or GI tract, Lungs]

Dopaminergic [Coronary, Cerebral artery, Renal, Mesentric]

Classification of Sympathomimetics

 Direct-acting sympathomimetics  directly stimulates the adrenergic receptor (ex:


Norepinephrine and Epinephrine)
 Indirect-acting sympathomimetics  stimulates the release of norepinephrine from
the terminal nerve endings (ex: Amphetamine)
 Mixed-acting sympathomimetics  both direct and indirect (ex: Pseudoephedrine)

Catecholamines

- Chemical structures of a substance


- Either endogenous (natural) or synthetic (artificial)
- Can produce sympathomimetic effects
- Also responsive for fight-or-flight response for stressful situations

Examples for Endogenous: Epinephrine, Norepinephrine, Dopamine

Examples for Synthetic: Isoproterenol, Dobutamine

Non-Catecholamines

- Poor substrates of MAO ; resistant to COMT


- Stimulates adrenergic receptors
- Have longer duration of action than the endogenous and synthetic catecholamines

Examples: Phenylephrine, Metaproterenol, Albuterol

DRUGS THAT AFFECT SYMPATHETIC NERVOUS SYSTEM


ADRENERGIC ANTAGONIST

Ø Drugs that block the effects of adrenergic receptors

Ø Also called adrenergic blockers or sympatholytics

Ø It blocks the effects of the neurotransmitter either directly by occupying the receptors or
indirectly by inhibiting the release of the neurotransmitters norepinephrine and epinephrine

ANS 2

EPINEPHRINE

Brand Names: Adrenin, Epix, Ephedrix

Classification: Sympathomimetic adrenergic agonist

Pregnancy category C

Dosage: Adult: subcut/IM: 0.3 mg Epipen Auto injector, may repeat in 5-20 mins

PRN: maximum of 2 dosage

IV: 0.1-01.25 mg of 0.1 mg/ml solution, may repeat q 5-15 mins

PRN: may follow with 1-4 mcg/min infusion

MOA: (mechanism of action)

Acts on alpha and beta receptors; promotion of CNS and cardiac stimulation and
bronchodilation, strengthens cardiac contraction, increases cardiac rate and cardiac output;
reduces mucosal congestion by inhibiting histamine release; reverse anaphylactic reactions

Indications:

- Nasal Congestion
- Allergic reaction
- Anaphylaxis
- Asthma
- Bronchospasm
- Angioedema
- Status Asthmaticus (severe type of asthma)
- Cardiac arrest
- Cardiac resuscitation
Contraindications:

- Cardiac tachydysrhythmias
- Cerebral arteriosclerosis
- Labor
- Closed-angle glaucoma

Caution

-Hypertension

-Prostatic hypertrophy

-Hyperthyroidism

-Pregnancy

-Diabetes mellitus

SIDE EFFECTS

-Anorexia

-Nausea and vomiting

-Restlessness

-Tremors

-Agitation

-Sweating

-Headache

-Pallor

-Insomnia

-Weakness

-Dizziness

-Hyperglycemia

ADVERSE REACTIONS

-palpitations

-tachycardia

-hypertension

-dyspnea

-tissue necrosis of IV Site upon infiltration


LIFE THREATENING

-Ventricular fibrillation

-Pulmonary edema

DRUG INTERACTIONS:

-Increased effects with TCAs and MAOIs

-Methyldopa and beta blockers antagonize epinephrine effects

-Digoxin can cause dysrhythmias

ALBUTEROL SULFATE

Brand names: Ventolin, Proventil, Salbutamol

Classification: Selective beta2 adrenergic agonist Pregnancy category C

Dosage: Acute bronchospasm: A/adol : MDI: 2 inhal (90mcg/inhal) q4-6h

Bronchospasm prophylaxis : Immediate release: A/ado: PO: Initially 2-4 mg q6-8h: max 32 mg/d

C: 6-12 years: PO: Initially 2 mg tid/qid; max 24 mg/d

Extended release: A/adol: PO: 4-8mg q12h; max 32 mg/d C: 6-12y:PO initially 4 mg q12h; max
24 mg/d

Well absorbed in GI TRACT

MOA: Stimulates beta2 adrenergic receptors in the lungs, which relaxes the bronchial smooth
muscle, thus causing bronchodilation

Albuterol sulfate

Indications:

- To treat Asthma
- For prophylaxis and treatment of acute bronchospasm
Contraindications:

- Hypersensitivity
- Milk protein hypersensitivity
Caution

- Coronary artery disease


- Hypertension
- Hyperthyroidism
- Diabetes mellitus
- Renal Dysfunction
- Advanced age
- Seizures
- MAIO Therapy
- Pregnancy
SIDE EFFECTS

-Tremor

-Dizziness -nasopharyngitis

-Drowsiness -Insomnia

-Nervousness -Weakness

-Restlessness -Nausea

-Agitation -Diarrhea

-Anxiety -Muscle Cramps

-Sweating

-Headache

ADVERSE REACTIONS

-palpitations -tachycardia

-hypertension -infection

- Hyperglycemia -Hypokalemia

LIFE THREATENING

- Cardiac dysrhythmia
- Angioedema
- Bronchospasm
- Steven-Johnson Syndrome
ALBUTEROL SULFATE

Drug-lab Interactions:

-Increased effects with TCAs and MAIOs

-beta blocker inhibits its effect

-digoxin can cause dysrhythmias

-may increase glucose level slightly


ADRENERGIC AGONIST

Alpha 1 agonist

-Midodrine hydrochloride

-Phenylephrine hydrochloride

Alpha 1 and Beta 1 agonist

- Norepinephrine bitartrate
- Dopamine hydrochloride
Alpha 1, Beta 1 and Beta 2 agonist

- Epinephrine
- Ephedrine hydrochloride
Beta 1 agonist

- Dobutamine hydrochloride
Beta 2 agonist

- Metaproterenol sulfate
- Terbutaline Sulfate
Nursing Assessment

1. Record baseline vital signs


2. Assess the patient’s drug history
3. Determine patient’s health history
4. Determine baseline glucose level
Nursing Interventions

1. Administer epinephrine 1mg (10 mL of a 1:10,000 concentration per AHA guidelines) IV


for cardiac resuscitation; may repeat every 3-5 min. Follow each dose with 20mL saline
flush to ensure proper delivery. Normally, epinephrine is administered of 1mg IV over 1
minute or more
2. Monitor IV site frequently when administering norepinephrine bitartrate or dopamine.
Dilute sufficiently in IV Fluids
*extravasation of the drugs can cause tissue damage and necrosis after 12 hours.

3. Administer antidote, phentolamine mesylate, 5-10 mg, diluted in 10-15 mL, of saline
infiltrated into the areas of IV extravasation of norepinephrine and dopamine.

4. Report patient’s vital sign and check blood pressure every 3-5 mins or as indicated to avoid
severe hypertension
5. Monitor the ECG for dysrhythmia when adrenergic agonists given intravenously.

6. Report side effect of Adrenergic drugs such tachycardia, palpitations, tremors, dizziness,
and increased blood pressure.

7. Check patient’s urinary output and assess for bladder distension.

8. Offer food to the patient when giving adrenergic agonists.

9. Evaluate blood glucose levels in patients with diabetes mellitus for potential elevation.

CLIENT TEACHING

General

1. Advise the patient to read labels on all over the counter (OTC) drugs for cold symptoms
and diet pills.
2. Explain continuous use of nasal sprays or drops that contain adrenergic agonists may
result in rebound nasal congestion.
Self- Administration

1. Encourage patient to take medication as prescribed.


2. Advise the patient and family on proper administration of the drug and allow a return
demonstration. Also let client check the drug and check in an upright position of
head.because it might cause systemic absorption
3. Notify the health care provider if an EpiPen is needed more than twice a week.
4. 4. Encourage patient to have an EpiPen readily available at all times and to store additional
medication in a cool dark place.
5. Teach patient and family the EpiPen must be used immediately upon the initial occurrence
of difficulty breathing, wheezing, hoarseness, hives, itching or swelling of lips or tongue.
6. Teach patients to administer EpiPen Properly. 90-degree angle after administration
massage for 10 secs
Cultural Consideration

1. Avoid use of jargons


Evaluation

1. Patient’s response to adrenergic agonist


2. Vital signs and report abnormal findings
3. Report possible drug to drug or herb or food interaction.

ANS 3

ALPHA – ADRENERGIC ANTAGONIST

Ø Also called alpha blockers


Ø Drugs that block or inhibit a response at the alpha adrenergic receptor site

Ø Divided into 2 groups:

o Selective alpha blockers – blocks alpha 1 receptor

o Nonselective alpha blockers – blocks alpha 1 and 2 receptor

Effects of Adrenergic Blockers at Receptors

Alpha 1 Receptor

· Blood vessels – vasodilation, decrease in blood pressure resulting to orthostatic hypotension,


treat peripheral vascular diseases such as Raynaud’s Disease – condition that results in
discoloration of fingers and toes after exposure to changes in temperature or emotional events or
abnormal spasm of the blood vessels that causes diminished blood supply to local tissues

· Eye – increased pumping of heart can cause reflex tachycardia – can result in constriction of
pupils or miosis

· Bladder – reduce contraction of smooth muscle

· Prostate – suppresses ejaculation; alpha-adrenergic blockers can help in decreasing the


symptoms of benign prostatic hyperplasia (BPH) – enlarged prostate; causes uncomfortable
urinary symptoms like blocking flow of urine out of the bladder – by relaxing smooth muscles of
prostate

BETA – ADRENERGIC ANTAGONIST

Ø Also called beta blockers

Ø Divided into 2 groups:

o Selective beta blockers – blocks beta 1 receptor

§ Ex: Atenolol and metoprolol tartrate

§ Beta 1 blocker with ISA (intrinsic sympathomimetic activity – term used to descibe the ability
of a certain beta blocker to bind with a beta receptor which produces a complete activation) :
acebutolol

o Nonselective beta blockers – blocks both beta 1 and 2 receptors

§ Ex: Propanolol hydrochloride

§ with ISA : carvedilol, penbutolol, and pindolol

Effects of Adrenergic Blockers at Receptors


Beta 1 Receptor

· Heart – decreases heart rate and blood pressure, reduces force of contraction – beta adrenergic
blockers useful in treating mild and moderate hypertension, angina, heart failure, and myocardial
infarction

· Kidney – suppresses renin angiotensin aldosterone system (RAAS) – decreases blood pressure

Beta 2 receptor

· Smooth muscle (gastrointestinal tract) – increases gastrointestinal tone and motility

· Lungs – constricts bronchioles

· Uterus – contracts the uterine smooth muscles

· Liver – inhibits glycogenolysis or breakdown of glycogen, reducing blood sugar level

Atenolol

ü Brand names: Tenormin

ü Classification: beta 1 adrenergic blocker (selective)

ü Pregnancy Category D

ü Dosage: Hypertension – Adult: PO: Initially 25-50 mg/d; may increase to 100 mg/d after 7 days;
max of 100 mg/d

ü MOA: selectively blocks beta 1 – adrenergic receptor sites, decreases sympathetic outflow to
periphery, suppresses renin – angiotensin – aldosterone system

ü Crosses blood-brain barrier and is 50-60% absorbed by the GI tract

ü Indications: to treat hypertension, angina, prophylaxis and treatment of acute myocardial


infarction

ü Contraindications: sinus bradycardia, heart block greater than first degree (exhibits decrease in
heart rate – reason why contraindicated), cardiogenic shock (heart suddenly can’t pump enough
blood to body), pulmonary edema (excess fluid in lungs), acute bronchospasm, pregnancy and
lactation Caution: Renal dysfunction, diabetes mellitus

ü Side effects: drowsiness, dizziness, depression, weakness, nausea, diarrhea, headache,


hypoglycemia, cold extremities, erectile dysfunction *common in red

ü Adverse reactions: Bradycardia, hypotension, Heart failure, dyspnea. Life threatening:


Bronchospasm, Dysrhythmia, thrombocytopenia (decreased number of platelets in blood)

ü Drug interactions:
o Increased absorption with atropine and other anticholinergics

o Decreased hypotensive effects w/ NSAIDS

o Increased risk of hypoglycemia with insulin and sulfonylureas (note medication decreases blood
sugar)

o Increased hypotension w/ prazosin and terazosin (anti-hypertensive meds)

o Increased lidocaine and verapamil levels w/ toxicity

Phentolamine mesylate

ü Brand names: Regitine, OraVerse, Phentosol

ü Classification: alpha 1 adrenergic blocker

ü Pregnancy Category C

ü Antidote of the extravasation of medications dopamine and epinephrine

ü Dosage: Adult: subcut: 5-10 mg in 10 ml NS injected into extravasation area to prevent dermal
necrosis

ü MOA: Binds to alpha-1 receptors, resulting in a decrease in peripheral vascular resistance and
vasodilation

ü Indications: Pheochromocytoma (rare tumor in adrenal gland tissue, resulting in release of too
much epinephrine and norepinephrine hormones that controls the heart rate, metabolism, and
blood pressure) diagnosis, hypertension in pheochromocytoma surgery, dermal necrosis due to
epinephrine/norepinephrine extravasation (antidote)

ü Contraindications: Myocardial infarction/Heart attack, coronary insufficiency/heart failure,


angina/chest pain, hypersensitivity to phentolamine

ü Side effects: Weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea,
vomiting

ü Adverse reactions: acute to prolonged hypotensive episodes, tachycardia, cardiac arrhythmias

Examples of Medications under Adrenergic Antagonist

Alpha 1 blockers

· Phentolamine mesylate

· Doxazosin mesylate

· Prazosin hydrochloride
· Terazosin hydrochloride

Alpha 1, Beta1, and Beta2 blockers

· Carvedilol,

· Labetalol

Selective Beta blockers

· Metoprolol tartrate

· Atenolol

· Acebutolol hydrochloride

· Betaxolol

· Bisoprolol fumarate

· Esmolol hydrochloride

Beta 1 and Beta 2 blockers

· Propanolol hydrochloride

· Nadolol

· Pindolol

· Sotalol

· Timolol maleate

Reserpine

ü Brand names: Serpasil, Serpine

ü Classification: adrenergic neuron antagonist (drugs that blocks the release of norepinephrine
from the sympathetic terminal neurons)

ü Pregnancy Category C

ü Dosage: Hypertension – Adult: PO: initially 0.5 mg/d for 1-2 weeks; maintenance: 0.1 – 0.25
mg/d

ü MOA: an adrenergic neuron antagonist that blocks the release of norepinephrine from the
sympathetic terminal neurons; reduces the serotonin and catecholamine transmitters
ü Also crosses placenta and blood-brain barrier and enters the breast milk, fully absorbed from
GI tract

ü Indications: Hypertension

ü Contraindications: Active peptic ulcer (stimulates HCl secretion in stomach and might cause
further peptic ulcer), history of mental depression, Parkinson’s disease Caution: Myocardial
infarction, cardiac arrhythmias, gallstones, epilepsy, pregnancy, lactation

ü Side effects: nasal congestion, headache, drowsiness, dizziness, GI disturbance, hypotension

ü Adverse reactions: CNS symptoms including depression, lethargy (tiredness, fatigue),


extrapyramidal effects EPS (involuntary/uncontrolled movements)

ü Drug interactions:

o Enhanced hypotensive effects with thiazide diuretics and other hypertensives

o Enhances the effects of CNS depressants

o Decreased antihypertensive effects with TCAs

Nursing Assessment

1. Obtain baseline data and electrocardiogram for future comparison

2. Determine the drugs pt currently takes

3. Obtain pt’s health history

Nursing Interventions

1. Monitor vital signs – BP and HR

2. Report any complaints like dizziness, lightheadedness, early morning insomnia, mental
depression or chest pain

3. Assist patient with ambulation to avoid falls from orthostatic hypotension

4. Note any complaint of stuffy nose because vasodilation may result and nasal congestion can
occur

Client Teaching

General

1. Encourage pt to adhere to the drug regimen


2. Advise pt that the therapeutic effects of adrenergic neuron antagonists may not occur for 2-3
weeks after initiation of therapy

Self-administration

1. Teach the pt and the family how to take pulse and blood pressure

2. Encourage pt to take adrenergic neuron antagonists at the same time every day and not to
discontinue it w/o permission from the health care provider (may cause rebound effect)

Side effects

1. Encourage pt to avoid orthostatic hypotension by slowly standing from supine or sitting


positions to standing

2. Inform pt and family of possible psychological changes when taking adrenergic neuron
antagonist, which occur because of catecholamine depletion

3. Warn pt that med may cause erectile or ejaculation dysfunction which is usually dose related

4. Advise pt not to drive or operate dangerous equipment until drug response is known

Cultural considerations

1. Obtain an interpreter when necessary

2. Provide an interpreter with the same ethnic background and gender if possible, especially when
sensitive topics are being addressed

Evaluation

1. Pt’s response to adrenergic antagonist

2. Vital signs and report abnormal findings

3. Report possible drug to drug or herb to herb interaction

ANS 4
Bethanechol Chloride
Brand name: Urecholine ,urotone
Pregnancy category C
Classification:Direct acting cholinergic agent
Dosage: Urinary retention
Adult: PO: initially 5-10 mg tid/qid; maintenance: 10-50mg
tid/qid;maximum:200mg/d
Adult;subcut: 5mg tid/qid; maximum 40 mg/d
MOA: stimulates the cholinergic(muscarinic) receptors: promotes contraction of the bladder ;
increases GI secretion and peristalsis, pupillary constriction and bronchoconstriction(pporly
absorbed in the GI tract but mostly secreted in the urine)

Indications:
 Urinary retention
 Neurogenic bladder
Contraindications:
 Intestinal or urinary tract obstruction
 Irritable bowel syndrome
 Bradycardia
 Hypotension
 COPD
 Asthma
 Peptic ulcer
 Hyperthyroidism
 Seizures
 parkinsonism

Side effects
 Hypotension
 Tachycardia
 Blurred vision
 Excessive salivation
 Increase gastric acid secretion
 Abdominal cramps
 Diarrhea
 bronchoconstriction
Adverse reactions:
 Tachycardia
 weakness
Life threatening:
 Bronchospasm

Drug Food Label Interactions:


 Antidysrhythmias decreases bethanechol effect
 Ganglion blocking agents causes significant hypotension following severe
abdominal symptoms
 False test result of amylase and lipase

Direct acting Cholinergist agonist:

1. Metoclopramide hydrochloride
-prescibed to treat gastroparesis, nausea and GERD.
-in low doses, it enhances gastric motility and thus accelerate gastric
emptying time.
2. Pilocarpine( for the eyes)
- acts on the nicotinic receptor
MOA: constricts the pupil of the eye that results in opening the schelm
canal to promote drainage of aqueous humor
IND: used to treat glaucoma by relieving fluid pressure in the eye and
promote miosis in eye surgery and examinations
-oral form is used to relieve xerostomia(dry mouth)

Indirect acting Reversible Cholinesterase Inhibitors

Drug samples: neostigmine(prostigmine), edrophonium chloride(Tensilon),


pyridostigmine bromide(Mestinon), ambenonium chloride, physostigmine( Antilirium)

Classification: Indirect acting reversible cholinesterase Inhibitors


(do not act on receptor they inhibit or in activate the cholinesterase
permitting the acetylcholine to accumulate at the receptor sites)
MOA: stimulates binds with cholinesterase, allowing acetylcholine to activate the
muscarinic and nicotinic cholinergic receptors.
Indications: primarily to treat myasthenia gravis and alzheimer disease, produce
pupillary constriction in the treatment of glaucoma

Side effects:
 Hypotension
 Bradycardia sweating
 Hypersalivation
 GI Distress
Contraindications:
 Intestinal or urinary obstruction
 Give caustion to client with bradycardia, asthma ,peptic ulcer, hyperthyroidism

Physostigmine- antidote for atropine


Nursing Assessment:
 Assess baseline vital signs for further comparisons
 Assess urine output( should be 1500ml/day,: 30-60 ml/hr)
 Obtain patient history of health problems
Nursing Interventions:
 Monitor vital signs
 Record fluid intake and output
 Give cholinergic agonist 1 hour before or 2 hours after meals
 Check serum amylase, lipase, aspartate aminotransferase, and bilirubin levels.
 Observe patient for side effects
 Auscultate the breath sounds

ANS 5

DRUGS THAT AFFECT THE PARASYMPATHETIC NERVOUS SYSTEM


CHOLINERGIC ANTAGONIST- Inhibits the action of acetylcholine by occupying the
acetylcholine receptors

-affects the major organs,respiratory system,GI tract,bladder, and exocrine glands

EFFECTS OF CHOLINERGIC ANTAGONISTS

● CARDIOVASCULAR
● GASTROINTESTINAL
● URINARY TRACT
● CENTRAL NERVOUS SYSTEM-TREMORS OF THE MUSCLE
● BRONCHIAL
● GLANDULAR-DECREASES THE SALIVATION AND BRONCHIAL SECRETIONS
● OCULAR- DILATES PUPIL

ATROPINE

● Brand name- isopto atropine


● classification-Anticholinergic
● Pregnancy- category C
● dosage-Bradycardia
● MOA: inhibits acetylcholine by occupying the receptors; increases heart rate by blocking
vagus stimulations; promotes pupil dilation by blocking sphincter muscle
INDICATIONS

● OCULAR DIAGNOSTIC EXAM


● Preoperative medications to reduce salivation
● Patients with bradycardia
CONTRAINDICATIONS

● Narrow angle glaucoma


● Obstructive GI idsorders
● Paralytic ileus
● Tachycardia
● Benign prostatic hyperplasia
● Myocardial ischemia
● Hypersensitivity
SIDE EFFECTS color red common side effects

● Dry mouth
● Decreased perspiration
● Nausea
● Head ache
● Amnesia
● Constipation
● Dry skin
● Flushing
● Mydriasis
● Blurred vision
● Anxiety
● Photophobia
● Urinary retention
● Hyperflexia
● Ataxia

ADVERSE EFFECT

● Tachycardia
● Paradoxic bradycardia
● Hypertension
● Hypotension
● Angina
● Pulmonary edema
● Seizure

Life threatening:

● Dysrythmias
● Laryngospasm
● Steven johnson syndrome
● Coma
DRUG INTERACTIONS

● Phenothiazines, antihistamines, amatidine,quinidine increases anticholinergic effect


● High dose anticholinergetics decreases effects of cardidopa/levodopa

BENZTROPINE

● Brand name- cogentin


● classification-Antiparkinson:anticholinergic agent
● Pregnancy- category C
● dosage-Anti parkinsonsonism
● MOA: Blocks cholinergic(muscarinic) receptors, thus decreasing acetylcholine to reduce
excess cholinergic activity also blocks dopamine reuptake to prolong dopamine effects
and decreases movement
INDICATIONS
● To Decrease involuntary symptoms of parkinsonism or drug induces parkinsonism
CONTRAINDICATIONS

● Closed angle glaucoma


● Tardive dyskinensia
● Myasthenia gravis
● children
caution

● Tachycardia
● Cardiac neuropathy
● Prostatic hypertrophy
● Psychosis

SIDE EFFECTS

● Nausea
● vomitting
● Dry mouth
● Constipation
● anhidrosis
● headache
● drowsiness
● Blurred vision
● cofusion
● depression

ADVERSE EFFECT

● Tachycardia
● Urinary retention
● Ocular hypertension

BENZTROPINE

Drug interactions- Increases anticholinergic effect with phenothiazines, tricyclic


antidepresants and other antichilinergics
Anti-cholinergic for treating Motion Sickness

Drug sample

-scopolamine

Demehydrinate cyclicine and meclizine and hydrocholride

Classification: antihistamine for motion sickness

MOA: blocks acetylcholine in the CNS

Routes: Wristbands ginger gum and candy transdermal scopolamine

NURSING ASSESSMENT

● Obtain baseline vital signs for future comparisons


● Asses urine output
● Check the patients medical/drug history
Nursing interventions

● Montor vital signs


● Record fluid intake and output
● Assess bowel sounds
● Examine for constipation caused by a decreased in gi motility
● Used bed alarms for patient who are confused and debilitated
● Mouth care
● Administer iv atropine or diluted in 10ml of sterile water rate of administration is 1 mg
or some fraction thereof per minute
CLIENT TEACHING

● Direct patients avoid hot environemnts and excessive physical exertion


● Teach patients with narrow glaucoma avoid atrophine drugs
● Instruct patients not tro drive vehicle that requires alertness
● Tell the patient with mydriasis an eye examination to use a sunglasses in bright light
because of photophobia
Side effects

● Advise of common side effects such as dry mouth


● Direct patient increase fluid intake and consume high fiber food
● Instruct patient to urinate before taking anticholinergic
● Advise patient to report any marked decrease in urine output
● Suggest that patients use hard candy ice chips or chewing gum
● Encourage the patient the use eye drops to moisten dry eyes
Cultural consideration

● Obtain interpreture when needed


● Ask open ended questions
Evaluation

● Patients response to anticholinergic


● Stability of patients vital signs and note presence of side effects or adverse reactions

Endocrine System
 Regulates calcium levels in the blood
Organs involved in the Endocrine System:
Thyroid gland
 Pituitary gland (anterior and posterior
pituitary gland)  Thyroxine (T4)
 Parathyroid gland
 Thyroid gland  Affect the tissue and organ may control
 Adrenal glands the metabolic rate and activity.
 Pancreas
 Gonads  Triiodothyronine (T3)

 Affect the tissue and organ may control


Pituitary gland the metabolic rate and activity.

o Anterior pituitary gland Take note: the thyroid hormone levels in the
blood are regulated by the negative feedback; it
 Thyroid stimulating hormone is the anterior pituitary gland secretes TSH
which stimulates the thyroid gland to produce
 Responds to the presence of thyroid T4 and T3
releasing hormone
 Stimulates the release triiodothyronine (T3) Pancreas- exocrine and endocrine gland
and thyroxine (T4) from the thyroid gland
 Islets of langerhans (has two important cells)
 Adenocorticotropic hormone
 Alpha Islet cells- produces glucagon (breaks
 It is released in response to the glycogen down to glucose in the liver)
corticotropin releasing hormone in the
hypothalamus.  Beta Islet cells- produces insulin (responsible
 Stimulates the release of glucocorticoids for the uptake of glucose, amino acids, fatty
(cortisol), mineralocorticosteriod acids to converts them to substances that are
(aldosterone), and androgen from the stored in the body cells)
adrenal cortex.
Gonads
o Posterior pituitary gland- storage for
the hormones  Female: Ovaries

 Antidiuretic hormone (Vasopressin)  Follicle Stimulating Hormone - promotes the


maturation of follicles in the ovaries
 produces from the hypothalamus
 Promotes water reabsorptions from the  Luteinizing Hormone with Follicle Stimulating
renal tubules to maintain water balance Hormone- follicle maturation and estrogen
in the body fluids. production

 Oxytocin  Prolactin- stimulates milk formation in the


 Produces from the hypothalamus glandular breast tissue after childbirth
 Stimulates the uterus to promote uterine
contraction during labor and delivery  Male: Testes

Parathyroid gland  Follicle Stimulating Hormone- initiates the


sperm production in the testes
 Parathormone (Parathyroid Hormone)
 Luteinizing Hormone- promotes antagonist, dopamine agonist,
secretion of testosterone from the testes somatosatin analogue
Growth Hormone
Common side effects:
 Also known as somatotropin hormone
 Hyperglycemia
 Acts on all body tissue particularly the
bones and skeletal muscles, the release of
the growth hormone is regulated by the Growth hormone replacements leans to linear
presence of GH-RH and GH-IH growth when there is a growth hormone
(Somatostatin) deficiency.

 No specific target gland, it affects the body Take note: Growth hormone can't be
tissues and bones administered orally because it will be inactivated
 Established as a counter regulatory by the gastrointestinal enzymes.
hormone for insulin
 Stimulates lipolysis which results free fatty Routes of Administration: Subcutaneous,
acids from the adipose tissue to the Intramuscular
circulation.
Factors to be qualified for growth hormone
o Presence of free fatty acids (FFA) therapy:
can induced insulin resistance,
increased FFA by hepatocytes 1. Growth hormone should be administered
results in oxidation and before it epiphysis or fused because it only
accumulation of key enzymes for acts on newly forming bone.
gluconeogenesis resulting in a
increase blood glucose level Drugs for clients with growth hormone
deficiency:
 Clients with increased growth hormone-
increases glucose production through Somatropin or Genatropin- used to treat growth
gluconeogenesis and glycogenesis from failure in children because of pituitary growth
the liver and kidney hormone deficiency

Somatropin
-mimics the natural occurring GH in the
Growth Hormone Therapy body.
-also known as recumbenant growth
-for patients who has excess or deficiency with hormone
growth hormone usually treated with a
replacement hormone. Side effects:

-very expensive that is why the patient needs to  Paresthesia


go to various treatment/ diagnostic examination.  Arthralgia
 Myalgia
We either do;  Peripheral edema
 Weakness
o Recumbinant growth hormone- adds  Cephalgia
growth hormones
Adverse effect:
o Inhibitors (due to excess hormone):
growth hormone receptor  Seizures
 Intracranial hypertension
 Secondary malignancy  Somatostatin analogue

Metabolic complications: Side Effects:


 Glucose fluctuations
 Hypothyroid  Mild gastrointestinal disturbances
 Hematuria
 Flu-like symptoms  Drug: Octreotide acetate (Sandosatin)
 Hyperpigmentation of the skin
 Formulations:
 Depot
Contraindications:  Interval: once a month
 Route: subcutaneous
 Pradder-willis syndrome
 Severe obesity  Immediate release
 Severe respiratory impairment  Interval: 3 times a day
 Route: subcutaneous
Take note: has a higher mortality rate.
 Indicated:
 Treat severe diarrhea with metastatic carcinoid
Drugs for clients with excess growth hormone: and other tumors

Conditions:  Drug: Lanreotide acetate (Somutoline


depot)
 Gigantism- excessive growth during
childhood  Formulations:
 Acromegaly- excessive growth after  Interval: every 4 weeks
puberty  Route: deep subcutaneous

Treatment: Prescribed with growth hormone


suppressants.  Pegvisomant or GH receptor
Classified as: anatagonist

 Dopamine agonist -growth hormone receptor anatgonist


-blocks the growth hormone receptor site,
 Drug: Bromocriptine mesylate (Parlodel) preventing abnormal growth by normalizing
insulin-like growth factor level
 Prolactin released inhibitor which antagonizes the
release of growth hormone from the anterior Route: injection
pituitary gland.
 Available: PO Side effects:
 Fewer side effects
 Hyperhidrosis
Side Effects:  Cephalgia
 Nausea  Fatigue
 Anorexia
 Dyspepsia Adverse effect:

Adverse reactions:  Chest pain


 Hypertension
 Cardiac toxicity  Elevated hepatic transaminases
 Cerebrovascular toxicity
Nursing Considerations for clients taking growth > Ablation
hormone:
Thyrotropin (only available in a VIAL form;
 Monitor blood glucose and electrolyte level should be given IM)
(risk: hyperglycemia) Route: Intramuscular
 Advice athletes not to take drug without
prescription
 Inform patients with diabetes to monitor
Site: Gluteus muscle
blood glucose closely (insulin regulations
maybe necessary) Frequency: 2 doses only
 Rotate injection sites to avoid
complications Interval: 24 hours
Drugs for Clients with: Deficiency in Thyroid
Stimulating Hormone
DRUGS FOR CLIENTS WITH A DEFICIENCY
Thyrotropin
IN THYROID HORMONE (T3 AND T4)
Brand Name: Thyrogen and Thytropar
Hypothyroidism
- a purified extract of thyroid stimulating
- a condition wherein there is a DECREASE
hormone
thyroid hormone production by the thyroid gland
- it is used to differentiate between primary and
- treated with hormones containing T3 and T4 or
secondary hypothyroidism
a combination of both
Hypothyroidism can be primary or secondary in
Levothyroxine sodium (Synthroid)
nature
Formulation: tablet and IV solution
Primary Hypothyroidism
Route: oral and intravenous
- is due to the destruction of thyroid gland
caused by autoimmunity or an intervention such Drug of choice for hypothyroidism
as surgery, radioiodine or radiation thus, a
decreased in thyroid stimulating hormone levels - drug of choice for replacement therapy for the
in the blood treatment of hypothyroidism

Secondary Hypothyroidism Liothyronine sodium (Cytomel)

- involves decreased activity of the thyroid gland Formulation: tablet and injection solution
usually due to a tumor in the region of the
Route: oral and intravenous
pituitary which resulting to a decreased thyroid
stimulating hormone in the blood Contains synthetic T3 only and has a short half -
life duration of action
* aside of the diagnostic usage of thyrotropin, it
is also given for clients with thyroid cancer but it Drug of choice for initial treatment of Myxedema
is not used to treat thyroid cancer alone but
rather it is used as an, *not recommended for maintenance therapy but
it is frequently used as initial therapy for treating
Adjunct Therapy for Well Differentiated Thyroid Myxedema because of its rapid onset of action
Cancer:

> Thyroglobulin Testing

Liotrix (Thyrolar)
Formulation: tablet  Cardiovascular collapse
Route: oral

Contains T3 and T4 (4:1) Nursing Considerations:


- for treating hypothyroidism; there is no Assess heart rate and blood pressure prior
significant advantage of using this to and periodically during therapy
medication because Liothyronine sodium
contains T3 and T4 in the peripheral Assess for tachycardia and chest pain
tissues For Children: Monitor height, weight and
psychomotor development

Mechanism of Action For diabetic patients: Monitor blood and


urine glucose level
*These drugs increases endogenous
thyroid hormone in the body thus, Observe for signs and symptoms of
increase metabolic rate of tissue, hyperthyroidism which are the following:
promotion of gluconeogenesis, tachycardia, chest pain, nervousness,
increase utilization and mobilization of insomnia, diaphoresis, tremors and weight
glycogen stores, stimulation of protein loss
synthesis, promotion of cell growth and Monitor serum thyroid level prior and
differentiation during therapy
Contraindication: Drugs for Clients with excess Thyroid
 Thyrotoxicosis Hormone (T3 and T4)
 Myocardial infarction Hyperthyroidism
 Severe renal disease
 Adrenal insufficiency - a condition wherein there is an increase
in production of thyroid hormones by the
Side effects: thyroid gland
 Nausea and vomiting - a condition wherein there is an increase
 Anorexia in circulating T4 and T3 which is usually
 Diarrhea caused by an overactive thyroid gland
 Cramps
*hyperthyroidism is managed
 Tremors
pharmacologically by giving anti – thyroid
 Nervousness
drug or thoimides
 Irritability
 Insomnia Drugs for Clients with Hyperthyroidism:
 Headache Weight loss
Thiomides
 Diaphoresis
 Amenorrhea - Propylthiouracil (PTU)

Formulation: tablet

Route: Oral
Adverse Effects: Inhibits synthesis of thyroid hormones
 Tachycardia - Methimazole (Tapazole)
 Hypertension
Formulation: tablet
 Palpitations
 Osteoporosis Route: Oral
 Seizure
 Thyroid Crisis Does not inhibit synthesis of thyroid
 Angina pectoris hormone
 Atrial fibrillation
Does not inhibit the peripheral conversion Monitor thyroid function before and during
of T3 to T4 as does PTU but it is 10 times therapy
more potent and has a longer half life than
PTU WBC and differential count should be
monitored periodically
PTU
Advise patient to report sore throat, fever,
- Does not reverse hyperthyroidism rapidly chills, headache, malaise, weakness,
yellowing of eyes or skin and unusual
- More side effects bleeding immediately
- Has potential for liver damage *aside from thiomides, patients with
- Last resort when methimazole is not hyperthyroidism is also given iodine
appropriate Potassium iodide (SSKI)
Methimazole - iodine is necessary component of the
- Reverses hyperthyroidism rapidly thyroid hormone

- Has fewer side effects Formulation: oral solution

Prolonged Use of Thiomides may cause: Route: oral


Goiter Mechanism of Action:
* minimal doses of Thiomides should be Inhibits the release and synthesis of
given when indicated to avoid this thyroid hormone
Contrainidications: Decreases the vascularity of the thyroid
 Hypersensitivity gland
 Lactating mothers (methimazole) Decrease the thyroidal uptake of
Side effects: radioactive iodine following radiation
emergencies or administration of
 Drowsiness radioactive iodine iotopes
 Headache
*iodine is a necessary compontent of
 Vertigo
thyroid hormone
 Nausea and vomiting
 Diarrhea Contraindications:
 Loss of taste
 Hypersensitivity
 Rash
 Hyperkalemia
 Skin discoloration
 Pulmonary edema
 Urticaria
 Impaired renal function
 Hypothyroidism
 Side Effects:
Adverse Effects  Confusion
 Weakness
 Hepatotoxicity
 Nausea and Vomiting
 Agrunolocytosis
 Hypothyroidism
 Goiter
 Hyperkalemia
Nursing Considerations:  Tingling
Monitor response of symptom of  Joint pain
hyperthyroidism

Assess patient for developing Adverse Effects:


hypothyroidism
 Gastrointestinal bleeding
Assess patient for skin rash or swelling of
 Diarrhea
cervical lymph nodes
 Acroneiform eruptions  Available in tablet, injection
solution, creams, lotions,
ointments and inhaler
Nursing Considerations:  Given oral route, IM or IV, topical,
aerosol
Assess for signs and symptoms for Iodism  Major action of these drugs is to
which are metallic taste, stomatitis, skin o suppress acute
lesions, cold symptoms, severe inflammatory response
gastrointestinal upset and for
Immunosuppression –
Monitor response symptoms of prevents cell mediated
Hyperthyroidism response
Monitor for hypersensitivity reactions  indications:
o Addison’s disease
Monitor thyroid function and serum o Inflammatory disorders –
potassium before and during therapy autoimmune disease
 Multiple sclerosis
Cortisone Drug
 Rheumatoid
 Cortisol is the main arthritis
glucocorticosteroid  Myasthenia gravis
 Addison’s Disease – deficiency in o Allergic conditions
cortisol  Asthma
o Manifest symptoms:  Drug reactions
 Hypoglycemia  Anaphylaxis
 Muscle weakness o Debilitating conditions
 Apathy caused by malignancies
 Depression  Organ transplant patients needs to
 Fatigue prevent organ rejection by
 Nausea and vomiting suppressing the immune system
 Abdominal pain  Contraindications
 Tachycardia o Hypersensitivity
 Hypotension o Psychosis
 Cardiovascular collapse o Fungal infections
 Hypovolemia o Peptic ulcer disease
 Hyponatremia  Side effects
 Hyperkalemia o Nausea
 Anemia o Diarrhea
 Examples of synthetical produced o Abdominal distention
cortisone drugs o Increased appetite
o Dexamethasone o Sweating
o Prednisone o Headache
 Drugs ending in “s-o-n-e” are o Depression
cortisone drug o Flushing
 Sub-classified into: o Mood changes
o Short Acting Drugs o Cataracts
 Cortisone Acetate o Amenorrhea
 Hydrocortisone  Adverse effects
o Intermediate Acting Drugs o Petechia
 Methyl-prednisolone o Ecchymosis
 Prednisolone o Hypertension
 Prednisone o Tachycardia
o Long Acting Drugs o Osteoporosis
 Beclamethasonedipropionate o Muscle wasting
 Betamethasone o Sodium and fluid retention
 Dexamethasone o GI hemorrhage
o Pancreatitis
o Circulatory collapse o Can be given with
o Thrombophlebitis glucocorticoidsteriod
o Embolism o Indications:
 Nursing considerations  Sodium loss and
o Assess serum electrolyte hypotension due
and blood glucose levels to adrenal
o Obtain patient’s weight insufficiency
and urine output and o Contraindications
record daily  Hypersensitivity
o Monitor blood pressure o Side effects
o Watch signs and  Dizziness
symptoms of hypokalemia  Headache
 Nausea and  Arrhythmias
vomiting  Edema
 Muscular  Hypertension
weakness  anorexia
 Abdominal  nausea
distention  adrenal
 Paralytic ileus suppression
 Irregular heart  weight gain
rate  hypokalemic
o Advise patient not to alkalosis
abruptly stop medication –  arthralgia
results to adrenal crisis o adverse effects
o Monitor older adults for  ascending
signs and symptoms of paralysis
osteoporosis – promotes
calcium loss from bones Antidiabetics part 1
o Report changes for Diabetes mellitus is a chronic disease
muscle strength resulting to a deficient glucose
o Take medications after metabolism. Its causes depend on the
meal to avoid gastric type of the diabetes mellitus,
irritation
o High potassium diet Types of Diabetes Mellitus
 Mineralocorticosteroid
Type 1- insufficient insulin production by
o Second kind of
the beta cells in the islets of langerhans
corticosteroid which
- may be due to genetics,
produces aldosterone -
virus, or autoimmunity
influenced by Renin-
- problem in insulin
angiotensin system
production
o Maintains homeostasis of
the body’s fluid by Type 2- the most common type that is
promoting water believed to be due to insensitivity of insulin
reabsorption of sodium to uptake glucose caused by prolonged
from the renal tubules exposure of the body to high-glucose
which may result to levels, obesity, or hereditary.
hypokalemia
 Fludrocortine (Florinef)  no problem in insulin
o Formulation: tablet production
o Route: oral
Secondary Diabetes
o Cause sodium
reabsorption, hydrogen Hyperglycemia occurs due to the influence
and potassium excretion of some medications like somatropin,
and water retention by its prednisone, hydrochlorothiazide. Once
effects on the distal renal these medications are stopped, blood
tubule glucose levels return to normal
Gestational Diabetes  Onset: 30 minutes
 Peak: 2-3 hours
 Usually happens when a
 Duration: 3-6 hours
woman is on her second or
third trimester. Progesterone, Examples:
cortisol, and HPL (Human
placental lactogen) increases
which can inhibit insulin
usage. After delivery, patient’s
blood sugar levels return to
normal but some will progress
to Type II Diabetes Mellitus.

Commercially Produced Insulin

 Only available in injection solution


because gastrointestinal enzymes
decreases the potency of the drug
when taken orally Intermediate Acting Insulin

Routes of Administration  Onset: 2-4 hours


o Subcutaneous  Peak: 4-12 hours
o Intravenous  Duration: 12-18 hours

Characteristics: - Used less often than other types of


o Onset – the length of time before the insulin
insulin reaches the bloodstream and - Useful for overnight insulin coverage
begins lowering blood sugar
o Peaktime – the time during which Examples:
insulin is at its maximum strength in
terms of lowering the blood sugar
o Duration – how long insulin continues
to lower blood glucose

 Rapid Acting Insulin


o Onset – 15 minutes
o Peak – 1-2 hours
o Duration – 2-4 hours

 Given BEFORE meals to minimize the


rise of glucose after eating
Long Acting Insulin
 Commonly given to type 1. It can also
be given to type 2 diabetic patients - Reaches the bloodstream several
Examples: hours after injection
- Good for 24 hours insulin coverage
- Lowers blood glucose for 24 hours
- Covers all day insulin needs
- The idea is to inject it once a day and
it will cover the insulin needs for 24
hrs

Examples:

Regular or Short Acting Insulin


- A rapid acting inhaled insulin
that is administered before
each meal and can be used
by adult patients with type 1 or
2 diabetes mellitus.
- It is not a substitute for long-
acting insulin and must be
used in combination just like
any other type of rapid insulin.

Combination Insulins

- Helpful for people who have trouble


drawing up insulin out of 2 bottles and
reading the correct direction and dosages
- Helpful for people with poor eyesight
or dexterity

Examples:

CONTRAINDICATIONS OF INSULIN

 Patients who have


hypoglycemia and
hypersensitivity

SIDE EFFECTS OF INSULIN

 Confusion
 Agitation
 Tremors
 Headache
 Flushing
 Hunger
Ultra-Long Acting Insulin
 Weakness
- Reaches the bloodstream in  Lethargy
six hours, DOES NOT peak  Fatigue
and last about 36 hrs or longer  Urticaria
 Irritation at injection site
Examples:
ADVERSE EFFECTS OF INSULIN

 Tachycardia
 Palpitations
 Hypoglycemic reactions
 Somogyi effect
 Lipodystrophy
 Anaphylaxis
 Shock

Inhaled insulin ( AFREZZA ) Aside from a regular timing and


dosage of giving insulin, there is
also what we call as sliding scale
insulin coverage. It is the monitoring and carbohydrate
administration of adjusted dose of counting
insulin based on the individual  Computerized and can be pre-
blood glucose result. Provides programmed and used as an
more constant blood glucose insulin reservoir in continuous
level. administration of rapid acting
insulin at various amounts at
different times all throughout
PROPER STORAGE OF INSULIN the day.

 Unopened – must be kept in


a cold storage but not in a
 Implantable Insulin Pump
freezer
 Opened insulin – Room - Surgically implanted in the
temp: 1 month ; Cold temp: 3 abdomen
months - It delivers both basal infusion
INSULIN ADMINISTRATION DEVICES or the continuous release of
small amounts of insulin or
 Insulin pen injector bolus, additional doses with
o It resembles a fountain meals
pen and it contains - It is administered
disposable needle and intraperitoneally
disposable insulin-filled
cartridge  Portable or External Insulin
o Delivers more accurate Pumps / Continuous
dose Subcutaneous Insulin Infusion
o Increases compliance - It is placed under the skin
- The needle is inserted into the
 Two types: abdomen, upper thigh, or
 Prefilled upper arm
 Reusable - This type of pump is worn
outside the body and placed
in a pocket or bra
- It also delivers basal and
bolus insulin
- Infusions are programmed by
the patient
- Only rapid acting insulin is
used

These devices decrease the risk


of sever hypoglycemic reactions
and maintains glucose control.
Blood glucose should be
monitored at least 4x a day

Success of insulin pump depends on:

 Individual’s knowledge and


compliance related on insulin
and the diabetic state
 Insulin Pump
 Highly recommended for
 An alternative to daily
patients with type 1 DM
injections used in association
with the blood glucose
Insulin Jet Injectors  Sulfonylureas
 Biguanides
- This device shoots insulin
 Alpha Glucosidase Inhibitors
without a needle, directly
 Thiazolidinediones
through fatty tissue
- Insulin is delivered in high  Meglitinides
pressure making it painful  Glucagon-like-peptide-1 agonists
- Not recommended for children or Selective sodium-glucose
and older adults transporter 2 inhibitors (SGLT2
- Expensive inhibitors)
 Amylin analogue
 Fixed Combination Oral diabetics

NURSING CONSIDERATIONS

 Identify the drugs the patient ORAL HYPOGLYCEMICS


is taking
 Monitor vital signs CLASSIFICATIONS
 Check for S/S of 1. Sulfonylureas
hypoglycemia
 Explain that orange juice, - Group of antidiabetics chemically related
sugar-containing drinks, hard to sulfonamides but does not have
candies maybe taken when antibiotic effects.
hypoglycemia starts - stimulates pancreatic beta cells to
 Follow the diabetic diet produce more insulin, this increases the
recommended by the insulin cell receptors, increases the ability
nutritionist of the cell to bind with insulin for glucose
metabolism.

DIVIDED INTO 2 GENERATIONS


ORAL HYPOGLYCEMICS
1. First generation
Indications:
-lower hypoglycemic potency
 Type 2 DM - short duration
 Type 1 DM (for some EX. Tolbutamide (Orinase),
classifications) Intermediate acting Tolazamide
(Tolinase), Long Acting Diabenese
Criteria for using Oral
2. Second generation
Hypoglycemics Agent
- higher hypoglycemic potency
Onset age is > 40 y.o - longer duration of action
- lesser side effects
Diagnosed with DM <5 EX. Gliplizde(Glucotrol), Glyburide
years
(Diabeta, Glynase, Micronase),
Normal or overweight Glimeperide (Amaryl)

FBS <- 200 mg/dL

<40 units insulin reqts/day 2.Biguanides Metformin(Glucophage)


- acts by decreasing the hepatic
Normal renal & hepatic
production of glucose from stored
function
glycogen.
- diminishes the increase in serum glucose
following a meal and blunts the degree of
ORAL ANTIDIABETICS postprandial hyperglycemia.
CLASSIFICATIONS - It decreases the absorption of glucose in
the small intestine and increase insulin
receptor sensitivity and glucose uptake by Meglitinides
cells.
- Does not cause hypoglycemia but - Repaglidine (Prandin)
causes GI disturbances. - Nateglidine (Starlix)

If you patient is to go contrast IV -Stimulate the beta pancreatic


biostudies, such as CT scan with contrast cells to stimulate insulin production
Metformin should be stop for 48 hours
Contraindication:
because it causes lactic acidosis or acute
renal failure. Contraindicated by patients - patients with liver dysfunction
with renal impairment Incritin Modifier
3. Alpha Glucosidase Inhibitors - Sitagliptin Phosphate
- it acts by inhibiting the digestive (Januvia)
enzymes in the small intestines. - Saxagliptin (Onglyza)
By inhibiting alpha glucoside,
absorption of complex CHO is -Increases incretin hormones
delayed -increase insulin production
-it does not cause hypoglycemic - decrease glucagon secretion
effects -used as an adjunct treatment with
exercise and diet to reduce both fasting
SUBDIVIDED INTO: and postprandial blood glucose levels
Acarbose (precose)
- a complex oligosaccharide Incretin hormones
- delays the digestion of -are gut hormones that are secreted from
carbohydrates thereby resulting in enteroendocrine cells
smaller rice in blood glucose -regulates the amount of insulin secreted
concentration following meal. after eating.
- use if lowering blood sugar to
normal level is not achieve by diet Selective sodium glucose transporter 2
alone. inhibitor
Miglitol (Glyset) - it lowers blood sugar by causing the
- a desoxynojirimycin derivative kidneys to remove sugar from the body
- delays digestion of ingested through the urine
carbohydrates
Fixed dose combination
4. Thiazolidinediones - It offers a simplified dosing regimen that
- acts to decrease insulin may improve patient compliance.
resistance and improves blood
glucose control
OTHER HYPOGLYCEMIC AGENTS
Contraindication: 1. GLP-1 Agonist
- symptomatic heart disease
- Classes III and IV congestive
Exanatide (Byetta)
heart failure
- injected 2x a day
Pioglitazone (Actos) - has significantly improved the
- it can be taken along with hba1c levels and weight loss in
sulfonylurea insulin patients
Rosiglitazone (Avandia)
-maybe taken along with Liraglutide (Victoza)
metformin, but in 2007 the FDA - it is given subcutaneously once a
issued a warning that patients day.
taking this drug higher risk of heart
attack and death. These drugs improve beta cells
responses, which improve glucose control.
It enhances insulin secretion, increase (adrenalin), from the adrenal medulla.
beta cells responsiveness, suppress - has a long half-life
glucagon secretion, slow gastric emptying
and reduce food intake. Formulation:
Oral and Parenteral Solution
Contraindications:
- Type 1 Diabetes Mellitus Route:
- Diabetic Ketoacidosis Oral and Intravenous
- Severe renal dysfunction or severe GI Onset: 1 hour
Disease
Duration: 8 hours
Side Effects:
- Headache Indication:
- Dizziness Chronic hypoglycemia cause by
- Jitterness hyperinsulinism due to islet malignancy or
- Nausea hyperplasia
- Vomiting
- Diarrhea

Amylin analogue
- used for type 1 and type 2 Diabetes
Mellitus patients
- administered before meals
- inhibits the release of glucagon while
eating
- slows food emptying in the stomach DRUGS FOR WOMEN’S HEALTH
- has a severe hypoglycemic effect

Side Effects:
- nausea Endometriosis – the abnormal location of
- vomiting the endometrial tissue outside the uterus.
- headache It is the common cause of dysmenorrhea,
chronic pelvic pain, and infertility.
HYPERGLYCEMIC DRUGS
- given to patients who experiences
induced hypoglycemia or other causes of
Ectopic endometrial implant responds to
hypoglycemia
endometrial control; particularly the
Glucagon estrogen. When menstruation occurs, the
- it protects the body cells especially in the ectopic endometrial implant proliferates
brain and retina by providing nutrients and and bleed.
energy needed to maintain body function
Increased Number of menstrual cycle
- available for parenteral use only
- use to treat insulin induced hypoglycemia
when other methods of providing glucose
are not available Inflammation of the surrounding organ
- blood glucose begin to rise in 10 minutes tissue
after administration.

Route of Administration Scar formation and adhesion


- subcutaneous
- intramuscular = This causes pelvic pain
- intravenous

Diazoxide
- it increases blood sugar by inhibiting TREATMENT
insulin release from the beta cells and
stimulating release of epinephrine
The goal of treatment is to decrease the
amount of circulating estrogen and limit or
eliminate estrogen. GN-RH AGONIST

This interrupts internal bleeding and - Potent drugs that inhibit GNRH
irritation associated with the ectopic release
endometrial implant and may even cause - Creates a hypoestrogenic
them to recede. environment

Examples:

COMBINED HORMONAL Parenteral Solution:


CONTRACEPTIVE PILLS (CHC) Leuprolide (Lupron Depot 3.75 mg)
- Suppress GN-RH prevents Given in 3.75 mg IM
- Prevents Ovulation
= which causes atrophy of the Monthly for up to 6 months
uterine lining
- This is thought to relieve pelvic
pain by causing regression of the Leuprolide (Lupron Depot – 3 month 11.25
endometrial implants. mg)
- Relieves pelvic pain of almost
75% of women having Given via IM injection
endometriosis.
Once every 3 months; for up to 6 months

!!! Leuprolide should be initiated in the first


PROGESTATIONAL PRODUCTS 3 days of the menstrual cycle. There is a
chance of pregnancy so a barrier method
- Suppresses ovulation and causes of contraception should be used.
long-term endometrial atrophy
- Inhibit Gonadotropin Releasing
Hormone similar to CHCs.
Goserelin (Zoladex)
- Overtime, Progestins can shrink or
eliminate endometrial plants Administered in a 3.6 mg dose
Example: Depot-Medroxyprogesterone Formulation: Parenteral Solution
Acetate (DMPA)
Route: Subcutaneous (Abdomen)
Solution in the form of Depo-Provera and
depo-subQ provera 104 = Frequency: Every 28 days for 6 months

 70-90% of patients experience


relief of symptoms associated with INTRANASAL
endometriosis
Nafarelin (Synarel) nasal spray

Administered in a 400 mcg/day dose


Oral Form:
One spray or 200 mcg in the other nostril
Norethindrone Acetate (Aygestin) in the evening for up to 6 months
Formulation: Tablet

Route: Oral Side Effects:


Dosing: 6-9 months - Menopause
Loading dose: 5 mg x 2 weeks DAILY - Hot flushes
- Atrophic Vaginitis
Additional 2.5 mg every 2 weeks until 15 - Vaginal dryness
mg/day is reached - Decreased sex drive
- Potential for bone loss  The manufacture of protein within
the target cells result in the build-
up of cellular tissue or anabolism
DRUGS FOR MEN’S HEALTH specially in muscles. This leads to
the development of secondary
Hypogonadism – a defect of the sex characteristics such as pubic
reproductive system that results in failure hair growth, beard, and body hair.
of the testis to produce testosterone,
sperm, or both. SIDE EFFECTS:

Exogenous supplemental testosterone is  Priapism


absorbed when taken orally but 50% of it  Gynecomastia
is metabolized in the liver. A higher dose is  Oligospermia (for 3 months or
recommended. more)
 Abdominal pain
Synthetic androgens have longer half-life;  Nausea
thus, this is more common to be given
 Diarrhea or constipation
orally.
 Hives or redness
Examples are:  Increased salivation
 Mouth soreness
STRIANT – a buccal adhesive system is  Increased or decreased sexual
available at 30 mg dose every 12 hours desire
 Advice the patient to place the ADVERSE EFFECT:
rounded side surface of the
system against the gum above an  Hypercalcemia
incisor tooth and hold firmly in
place with finger over lip and
against the product for 30
seconds.
 To remove, slide gently
downwards toward tooth to avoid
scratching gums
 Rotate sites
 If the product falls off within the
12-hour dosing interval or falls
out of position within 4 hours
before the next dose, remove and
apply a new system.
 Do not chew or swallow tablet
 Regularly inspect gums before
application

VIRILIZATION – development of male’s


secondary sex characteristics in women or
hypogonadal males.

 The action of striant is that


Hormones bind to site on certain
responsive genes causing
changes to take place in the target
cell.
 The effects of testosterone
depends on the receptor it
activates.
Drugs related to the Digestive System
Pathophysiology

Nausea and Vomiting


Medulla oblongata
● vomiting center

CTZ - Chemoreceptor trigger zone


● close to the Medulla oblongata
● Receives most impulses from
○ Drugs
○ Toxins
○ Vestibular center of the ear
● Transmits these impulses to the vomiting center
● Dopamine stimulates CTZ = stimulates vomiting center = Vomiting

Note: Both are responsible for vomiting

Diarrhea
● Microorganisms in the GI tract disrupts epithelium of the intestine
● This results to poor water absorption
● Leading To diarrhea
● Loose, watery stool and possibly more frequent bowel movements

Constipation
● Accumulation of hard fecal material

Ulcer Formation
● Hypersecretion of hydrochloric acid and pepsin which erodes the GI mucosal lining
(Peptic Ulcer)

Nursing problems
● Nausea
● Diarrhea
● Constipation
● Risk for deficient fluid volume
● Pain
● Imbalanced nutrition: less than body requirements
● Anxiety
● Deficient knowledge
Drugs related to the Digestive System
Antiemetics
● Prevents nausea, vomiting, vertigo and motion sickness
● Not recommended during pregnancy
○ If vomiting and nausea threatens the mother and fetus
○ trimethobenzamide (tigan) is given
○ Pregnancy Category C
OTC / Nonprescription Prescription

Antihistamines Antihistamine

Bismuth Subsalicylate Dopamine antagonists

Phosphorated Benzodiazepines
Carbohydrate Solution

Serotonin Antagonists

Glucocorticoids

Cannabinoids

Miscellaneous antiemetics

Antihistamines
● MOA: Blocks h1 receptor sites - inhibiting stimulations of CTZ and vestibular
pathways
● Can be OTC or prescribed but differ in length of effect, side and adverse effects.

Non prescription antiemetics


● Used to prevent motion sickness
● Minimal effects on controlling severe vomiting resulting from anticancer agents,
radiation and toxins

-Antihistamines
● Examples
○ Cyclizine HCl (Marezine)
○ Dimenhydrinate (Dramamine)
○ Meclizine HCl (Antivert)
● Administer 30-60 minutes before travel
○ Not effective if taken after vomiting has occurred
○ Should be taken after meals

-Bismuth Subsalicylate (Pepto-Bismol)


● Act directly on the gastric mucosa to suppress vomiting
● Also for gastric upset, diarrhea

-Phosphorated Carbohydrate Solution (Emetrol)


● Changes pH of the stomach and it also decreases smooth muscle contraction
● Effectiveness as antiemetic is not verified
● Diabetic patients should avoid them because they contain high sugar content

Prescription Antiemetics
-Antihistamines
● Same MOA with OTC
● For postoperative nausea and vomiting and vertigo
● Examples
○ Hydroxyzine (Vistaril)
○ Promethazine (Phenergan)
● Administered preoperatively with narcotics
● Give hydroxyzine deep IM
● Side effects:
○ Drowsiness
○ Dry mouth
○ Blurred vision
○ Constipation
○ Hypertension
○ Transient leukopenia
○ Urinary retention
○ Photosensitivity

-Anticholinergics
● MOA: Act primarily on the vomiting center of the brain by decreasing stimulation of
the CTZ and vestibular pathways
● Scopolamine (Transderm-scop)
○ 3 days efficacy
○ Apply behind ear at least 4 hours before antiemetic effect is required
○ Alternate ears if using for longer than 3 days
○ Wash hands after applying patch
○ Apply no more than 1 patch at the same time

-Dopamine Antagonists
● MOA: block dopamine 2 receptors in the CTZ = suppression of vomiting
● 3 Categories
○ Phenothiazines, Butyrophenones Benzodiazepines

>Phenothiazines
● MOA: inhibit CTZ
● 2 uses:
○ Primary - treatment of severe nausea and vomiting
○ Secondary - reduce anxiety, tension and for psychosis

● Note: For vomiting the dose is smaller than when used for psychiatric problems
● Examples:
○ Prochlorperazine maleate (Compazine)
○ Promethazine (Phenergran)
○ Chlorpromazine (Thorazine)
● Antipsychotic

>Butyrophenone
● MOA: blocks the dopamine 2 receptors in the CTZ used in prevention of nausea and
vomiting during surgical and diagnostic procedures
● Examples:
○ Droperidol (Inapsine)
○ Haloperidol (Haldol)
● Antipsychotic

>Benzodiazepines
● For prevention of nausea and vomiting resulting from cancer chemotherapy together
with metoclopramide
● Example: Lorazepam (Ativan)
● Provides emesis control, sedation, anxiety reduction and amnesia
● Anxiolytic

Dopamine antagonists = Have effects on the dopamine in the brain

Adverse effects
● EPS/Extrapyramidal symptoms
○ Antiemetic doses does not cause EPS
○ Used for an extended time may result to EPS

Extrapyramidal Symptoms
● Drug induced movement disorder
● Dystonia - continuous spasms and muscle contractions
● Akathisia - Motor restlessness, rocking feet, rubbing face
● Parkinsonism - rigidity
● Tardive dyskinesia - Irregular jerky movements, involuntary facial movements.

CNS effects
● Restlessness
● Weakness
● Agitation
● Hypotension

-Serotonin (5-HT3) Receptor Antagonists


● MOA: Block the serotonin receptors in the CTZ; block afferent vagal nerve terminals
in the upper GI tract = signals are not sent to the brain for vomiting
● Most effective of all antiemetics in suppressing nausea and vomiting caused by
cancer chemo
● Drugs usually ends with suffix -setron
● Examples:
○ Ondasetron (Zofran)
○ Granisetron (Kytril)
○ Dolasetron (Anzemet)
○ Palonsetron (Aloxi)
● Do not cause EPS
● Side effects:
○ Headache
○ Diarrhea
○ Dizziness
○ Fatigue

● Oral and IV - Administer 30-60 mins before chemo and 12 hrs after chemo

-Glucocorticoids (Corticosteroids)
● Suppress emesis associated with cancer chemo
● Minimized side effects because administered for a short while via IV
● Examples
○ Dexamethasone (Decadron)
○ Methylprednisolone (Solumedrol)
-Cannabinoids
● Active ingredients in marijuana
● Acts as agonists antiemetics via the activation of cannabinoid receptors in both the
brainstem and the enteric nervous system
● For alleviation of nausea and vomiting resulting from cancer treatment
● Prescribed for people in chemo
● Last resort of antiemetic = highly addictive
● Example: Dronabinol (Marinol) CSS III
○ Administer 24 hrs after chemo
○ Make sure the client is not suffering from any psychiatric disorder

● Side effects:
○ Mood changes
○ Euphoria
○ Drowsiness
○ Dizziness
○ Headaches
○ Depersonalization
○ Nightmares
○ Confusion
○ Incoordination
○ Memory lapse
○ Dry mouth
○ Tachycardia
○ Orthostatic hypo or hypertension

● Most common side effects are psychological problems hence assessment is very
important.

-Miscellaneous Antiemetics
● Do not act strictly as antihistamines, anticholinergics or phenothiazines
● MOA: suppress impulses to the CTZ and inhibiting impulses to the vestibular area
● Examples:
○ Diphenidol (Vontrol)
○ Trimethobenzamide (Tigan)
○ Aprepitant (Emend)
○ Metoclopramide HCl (Reglan)

>Metoclopramide HCl (Reglan)


● MOA: Blocks dopamine receptors in the CTZ
● Used in the treatment of postoperative emesis, chemo and rad therapy
● High doses can cause sedation and diarrhea
● Contraindications:
○ GI blockage
○ Hemorrhage
○ Perforation

● Side and adverse effects


○ Drowsiness
○ Anticholinergic symptoms
○ Hypotension
○ Diarrhea
○ EPS

● Instruct clients to avoid alcohol and CNS depressants

Emetics
● MOA: Stimulate the CTZ in the medulla and acting directly in the gastric mucosa
● Many ways to induce vomiting like putting finger on the back of the throat
● We induce vomiting if clients have ingested dangerous substances
● Only applicable of aspired substance in non-corrosive = Add injury to the GI tract of
emetics are taken
○ Examples of corrosive substance
■ Ammonia
■ Chlorine bleach
■ Lay
■ Toilet cleaners
■ battery acid

-Ipecac syrup
● Should be taken within 60 minutes of poisoning
● Victim should be alert and conscious
● Not given to unconscious individual
● Keep away from patients reach

Antidiarrheals
● For diarrhea and decreasing hypermotility or increased peristalsis
● Should not be used for more than 2 days and if fever is present

-Opiates and Opiate related Agents


● MOA: decrease intestinal motility = decreased peristalsis
● Example:
○ Deodorized opium tincture
○ Difenoxin and atropine (Motofen)
○ Diphenoxylate with atropine (Lomotil)
○ Loperamide HCl (Imodium)
● Can cause CNS depression when taken with alcohol, sedative or tranquilizers

>Diphenoxylate with atropine (Lomotil)


● Less potential for causing drug dependence
● Traveler’s diarrhea

>Difenoxin and atropine (Motofen)


● Metabolite of diphenoxylate (Difenoxin)
● More potent than diphenoxylate
● Non-specific and chronic diarrhea
Note: They are administered with Atropine - to decrease abdominal cramping, intestinal
motility and hypersecretion

>Loperamide (Imodium)
● Structurally related to diphenoxylate
● Causes less CNS depression than the 2 former
● Most common OTC antidiarrheals
● Reduces fecal volume, decreases intestinal fluid and electrolyte losses.

Side effects of Opiates and Opiate related Agents


● Drowsiness
● Dizziness
● Dry mouth
● Weakness
● Flush
● Rash
● Blurred vision
-Adsorbents
● MOA: coat the wall of the GI tract and adsorb bacteria or toxins that cause diarrhea
● Used in combination of OTC antidiarrheals
● Examples :
○ Bismuth Subsalicylate (Pepto-Bismol)
○ Kaolin-pectin (Kaolin with pectin)

Nursing management
● Continuous monitoring of loose bowel movement
● Administer every after loose stool

Laxatives and cathartics


● Used to treat constipation by elimination fecal matter

-Laxatives
● Soft stool
● Help evacuation of formed fecal matter from the rectum

>Chloride Channel Activators


● New category of laxatives
● MOA: activate chloride channels in the lining of the small intestine = increase in
intestinal fluid secretion and motility = enhances passage of stool and relieve
constipation
● For idiopathic constipation in adults
● Lubriporstone (Amitiza)

>Emollients (Stool softeners)


● Surface acting or wettin drugs
● Increase retention of water in stool
● MOA: lowers surface tension and promoting water accumulation in the intestine and
stool = draw water to the stool = decreased straining during defecation
● Examples:
○ Docusate calcium (Surfak)
○ Docusate sodium (Colace)
○ Docusate sodium with senna (Peri-colace)

● Contraindicated for children and older adults with debilitating diseases


○ May aspirate mineral oil resulting in lipid pneumonia

>Bulk-forming laxatives
● Natural, non absorbable
● MOA: Absorb water in the intestine, increases fecal matter size = distends GI tract
and stimulates peristalsis
● Examples:
○ Polycarbophil (FiberCon)
○ Polyethylene glycol (Miralax)
○ Methylcellulose (Citrucel)
○ Psyllium (Metamucil)

● Mix in a glass of water or juice and consume immediately and drink half to a full glass
of water
● Insufficient fluid intake will result to obstruction
● May take 8-24 hours to take effect
● May take 3 days for stool to be wet and well formed

>Osmotic (Saline) Laxatives


● Hyperosmolar laxatives
● Salt or saline products, lactulose, glycerine
● MOA: Pulling and retain water in the colon through osmotic activity = fluid retention
and increased fecal bulk size = increased peristalsis = bowel movement
● These contain salt - good renal function is needed
● Contraindicated for patients with heart failure
● Examples:
○ Glycerin
○ Lactulose (Cephulac, Chronulac, Duphalac)
○ Magnesium citrate (Citroma)
○ Magnesium hydroxide (Milk of magnesia)
○ Magnesium oxide (Mag-ox)
○ Sodium biphosphate (Fleet phospho-soda)
○ Polyethylene glycol with electrolytes (GoLYTELY)

= Polyethylene glycol with electrolytes (GoLYTELY)


● Used for bowel prep
● Needs ingestion of 3-4 liters of the solution over 3 hrs
● Advised to store in refrigerator
● Isotonic, nonabsorbable = can be used for patients with renal impairment

=Lactulose (Duphalac)
● Commonly found in the area
● Decreases serum ammonia level
● Good clients with liver disease
● Contains glucose and fructose = diabetics should avoid

Note: Monitor serum electrolyte levels for patients taking osmotic laxatives = to avoid
electrolyte imbalance
They contain magnesium or sodium and a small amount is systematically absorbed.

>Stimulant (Contact) laxatives


● MOA: Drug gets in contact with the colon = stimulates sensory nerve endings in the
intestinal mucosa = ↑ peristaltic movement
● To empty the colon before diagnostic tests like barium enema
● Examples:
○ Castor oil (Neoliod, Purge)
○ Senna (senokot)
○ Bisacodyl (Dulcolax)

=Castor oil
● Don't administer at bedtime
● Action is quick 2-6 hrs
● Not given in early pregnancy, may stimulate uterine contraction = spontaneous
abortion

=Senna (Senokot)
● Long term use injures the nerves of the colon = loss of intestinal muscular tone
● Side effect is reddish brown urine = secretion phenolphtaleine, senna or cascara

=Bisacodyl (Dulcolax)
● Most abused laxative OTC
● May cause electrolyte imbalance of calcium and potassium
● Absorption is minimal there are minimal side effects

Side effects
● Diarrhea
● Abdominal cramping
● Nausea
● Vomiting
● Weakness

Laxative abuse and dependence


● To double weight loss, lose unwanted calories
● Leads to dependence
● Prolonged use lead to:
○ Electrolyte imbalance
○ Dehydration
○ Mineral deficiencies
○ Serious damage to the digestive system
○ Chronic constipation
○ Damage to the nerves and muscles

Health teachings
● Proper use of laxatives
● Correct misconceptions of laxative use
-Cathartics
● Soft watery stool with cramping
● Help evacuation of unformed usually watery fecal material from the whole colon

Note: Both serve the same purpose despite different site of action

Antiulcers (TAAHPPP)
● Tranquilizers
● Anticholinergics
● Antacids
● Histamine 2 blockers
● Proton pump inhibitors
● Pepsin inhibitor
● Prostaglandin analogues
● Drugs to treat ulcers
● Tranquilizers and anticholinergics are used infrequently due to potential adverse
effects

>Tranquilizers
● MOA: Reduce vagal stimulation
● Vagus nerves - role in gastric secretions = aroused by taste, sight, odor of food =
cause release of ACh at vagus nerve endings in stomach wall = transmission of
impulses to acid secreting cells
● Examples
○ Chlordiazepoxide (Librium)
○ Clidinium bromide (Quarzan)

● Adverse effects
○ Edema
○ Ataxia
○ Confusion
○ EPS
○ Agranulocytosis

>Anticholinergics/ Antimuscarinics/ Parasympatholytics


● MOA: Inhibit ACh = block histamine and HCl = ↓ GI motility and secretion = delays
gastric emptying time
● More frequently used for duodenal ulcers than for gastric ulcers
● DOC: Peptic ulcers with antacids
● Adjunctive therapy
● Examples
○ Clidinium bromide and chlordiazepoxide HCl (Robinul)
○ Propantheline bromide (Probanthine)

● Administer before meals


● Followed by antacids 2 hours after
● Side effects: Anticholinergic effects

>Antacids
● MOA: Neutralize HCl and reduce pepsin activity

=Systemic (effects) Antacids


● Sodium bicarbonate (Alka-seltzer)
○ Seldomly used due to side effects
○ Sodium excess = hypernatremia and water retention
○ Metabolic alkalosis = excess of bicarbonate
○ Acid rebound

● Calcium carbonate
○ Most effective in neutralizing acid
○ Cause acid rebound
○ ½ of drug can be absorbed systemically
○ Excessive use might lead to Burnett’s syndrome

=Non-systemic antacids
● Compose of alkaline salts such as aluminum and magnesium, aluminum hydroxide,
magnesium hydroxide, magnesium trisilicate

● Magnesium hydroxide
○ Greater neutralizing power than aluminum hydroxide
○ Contraindicated to severe renal impairment = may lead to hypermagnesemia

● Aluminum
○ Small degree of absorption
○ Causes hypophosphatemia

Long term use of


Magnesium - Diarrhea (Magtatae)
Aluminum - Constipation (Metal is hard)

Magnesium + Aluminum = Neutralizes gastric acid without causing severe diarrhea or


constipation

● Best given 1-3 hours after meals and at bedtime

>Histamine 2 blockers
● MOA: Block H2 receptors of parietal cells in stomach = reducing gastric acid
secretion and concentration
● Usually ends with -tidine
○ Cimetidine (tagamet)
○ Famotidine (Pepcid)
○ Nizatidine (Axid)
○ Ranitidine (Zantac)

=Cimetidine (Tagamet)
● 1st H2 blocker
● Short half life and duration of action
● Blocks 70% of acid secretion for 4 hrs.
● 50-80% is excreted unchanged in the urine
● Taken with antacid = ↓ effectiveness

=Famotidine (Pepcid), Nizatidine (Axid), Ranitidine (Zantac)


● More potent than cimetidine
● Promote ulcer healing
● Longer duration of action = decreased frequency of dosing
● Fewer side effects and drug interactions
=Ranitidine
● 5 times more potent than cimetidine
● Less potent than famotidine

=Nizatidine
● Relieves nocturnal gastric acid secretions for 12 hrs

● Block H2 receptor
● Best given before meals and at bedtime
● 1 hr interval with antacid = maintain efficacy

Side effects and adverse rxns


● Headache
● Dizziness
● Constipation
● Skin rash
● Pruritus skin
● Gynecomastia
● Decreased libido
● Impotence
● Note: Ranitidine and famotidine = fewer side effects than cimetidine

>Proton pump inhibitors


● Gastric acid secretion inhibitors
● Gastric acid Pump inhibitors
● MOA: block the final step of acid production thru inhibiting the stimulation of the
enzyme system, hydrogen/potassium adenosine triphosphate in the gastric parietal
cells
● Inhibit gastric acid secretion up to 90% greater than histamine 2 blockers
● Usually ends with prazole
○ Omeprazole (Prilosec)
○ Lansoprazole (Prevacid)
○ Rabeprazole (Aciphex)
○ Pantoprazole (Protonix)
○ Esomeprazole (Nexium)
○ Dexlansoprazole (Dexilant)

● DOC: Gastroesophageal reflux disease (GERD)


● Administer before meals and at bedtime

>Pepsin inhibitor
● Mucosal protective drug
● MOA: Covers the ulcer and protects it from acid and pepsin
● Does not neutralize or inhibit acid secretions
● Sucralfate (Carafate)
● Before meals and at bedtime

>Prostaglandin analogue Antiulcer drug


● MOA: Increase cytoprotective mucus in the GI Tract = suppression of gastric acid
and pepsin secretion
● Misoprostol (Cytotec)
● Note: Do not give to pregnant women = Abortificient drug = causes abortion

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