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PHARMACOLOGY

STUDENTS NOTES/ WORKBOOK

I. Course Code: NCM 106

II. Course Title:PHARMACOLOGY

III. Credit Units: 3 units lecture (54Hours)

IV. Course Description:

CHAPTER 3: DRUGS AFFECTING THE BODY SYSTEM

 DRUGS ACTING ON THE NERVOUS SYSTEM

CENTRAL NERVOUS SYSTEM – is the body’s primary nervous system.

Components:
1. Brain
2. Spinal Cord

PERIPHERAL NERVOUS SYSTEM(PNS) - is located outside the brain and spinal cord.
- After interpretation by the CNS, the PNS receives stimuli and initiates responses to those
stimuli.
Components/Divisions:

1. Autonomic Nervous System (ANS)/ Visceral System


- Innervates or acts in smooth muscles and glands; is involuntary over which the person has little
or no control. E.g. heartbeat, peristaltic action.
Function: control and regulation of the heart, respiratory system, GIT, bladder, eyes and glands.
Sets of Neurons in the ANS:
A. Afferent/ Sensory Neurons – sends impulses to the CNS where they are interprteted.
B. Efferent/ Motor Neurons – receives the impulses from the brain through the spinal cord to
the effector organ.
Branches:
a. Sympathetic Nervous System
b. Parasympathetic nervous System
2. Somatic Nervous system

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- Is a voluntary system unlike ANS; innervates skeletal muscles over which there is control.

SYMPATHETIC NERVOUS SYSTEM


- Is also called ADRENERGIC SYSTEM because at one time, it was believed that adrenalin was the
neurotransmitter that innervated the smooth muscle. Note: the neurotransmitter is
Norepinephrine.
Receptor Sites:
1. Alpha 1
2. Alpha 2
3. Beta 1
4. Beta 2

PARASYMPATHETIC NERVOUS SYSTEM


- Is also called CHOLINERGIC SYSTEM because the neurotransmitter at the end of the neuron that
innervates the muscle is Acetylcholine.
Important Considerations:
1. Drugs that mimics the neurotransmitters norepinephrine and acetylcholine produces
responses opposite to each other in the same organ.
2. Drugs that mimics the sympathetic nervous system can cause similar responses in the organ.

EFFECTS ON BODY ORGANS/STRUCTURES:

Body Organ/Structure Sympathetic Parasympathetic


1. Eyes dilates pupils constricts pupils
2. Lungs dilates bronchioles constricts bronchioles and
Increases secretions
3. Heart increase HR decrease HR
4. Blood vessels constriction dilation
5. GIT relaxes smooth muscles increase peristalsis
6. Bladder relaxes bladder muscle constricts bladder
7. Uterus relaxes uterine muscle -
8. Salivary Glands - increase salivation

DRUG ACTIONS:

I. Sympathetic Stimulants/ Sympathomimetics ( adrenergics, adrenomimetics, adrenergic agonists)


1. Increase BP 4. Dilates pupils
2. Increase HR 5. Relax uterine muscles
3. Relax bronchioles 6. Increase blood sugar
II. Sympathetic Depressants/ Sympatholytics ( adrenergic blockers, adrenolytics,adrenergic agonists)
1. Decrease PR
2. Decrease BP
3. Constricts bronchioles
III. Parasympathetic Stimulants/ Direct- Acting Parasympathetics ( cholinergic or cholinergic agonists)
1. Decrease BP 4. Constricts pupils
2. Increase HR 5. Increased urinary contraction
3. Constrictd bronchioles 6. Increased peristalsis
IV. Parasympathetic Depressants/ Parasympatholytics

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1. Increased PR 4. Increased urinary retention
2. Decreased mucus secretions 5. Dilate pupils
3. Decreased gastric motility

 CENTRAL NERVOUS SYSTEM DRUGS

I. ADRENERGICS AND ADRENERGIC BLOCKERS – are drugs that affects the sympathetic nervous
system.

A. ADRENERGICS ( Sympathomimetics or Adrenomimetics) – are drugs that stimulate the sympathetic


nervous system; they mimic the neurotransmitter Norepinephrine. They acr on done or more
adrenergic receptor sites located on the cells of smooth muscles.

Effects at Receptor Sites:

1. Alpha 1 – located in the vascular tissues o f smooth muscles.


a. Increases force of heart contraction
b. Vasoconstriction increases BP
c. Mydriasis
d. Decreased salivary secretions
e. Increased contraction and ejaculation of bladder and prostatic capsule.
Note: When Alpha 1 is hyperstimulated, blood flow is decreased in vital organs.
2. Alpha 2 – located in the postganglionic sympathetic nerve endings.
a. Inhibits release of norepinephrine leads to vasoconstriction.
b. Dilates blood vessels.
c. Decrease BP.
d. Decrease GIT motility and tone.
3. Beta 1 – located primarily in the heart
a. Increase HR and force of contraction
b. Increase rennin secretion that increases BP
4. Beta 2 – located in the smooth muscles of the lungs, arterioles of skeletal muscles and the uterine
muscles.
a. Dilates bronchioles.
b. Promotes GIT and uterine relaxation.
c. Promotes increase in blood sugar through glycogenolysis in the liver.
d. Increased blood flow in the skeletal muscles.
5. Dopaminergic Receptor - located in the renal, mesenteric, coronary and cerebral arteries.
a. Dilates blood vessels.
b. Increased blood flow.
Note: Only Dopamine can activate this receptor.

INACTIVATION OF NEUROTRANSMITTERS:
Note: After the neurotransmitters have performed its function, the action must be stopped to
prevent prolonging the effect.
1. Re-uptake of the transmitter back into the neuron.
2. Enzymatic transformation or degredation.
3. Diffusion away from the receptor.
Enzymes responsible for the degredation:

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1. Monoamine Oxidase (MAO)
2. Cathecol-O- Methyltransferase (COMT)
Drugs can stop the termination of the neurotransmitters by:
1. Inhibiting the norepinephrine re-uptake.
2. Inhibiting the degredation of the norepinephrine by enzyme action.
CLASSIFICATION OF ADRENERGICS:
1. Direct-Acting Sympathomimetic- directly stimulate the adrenergic receptors. E.g. epinephrine,
norepinephrine
2. Indirect- Acting Sympathomimetics – stimulates the release of norepinephrine from the
terminal nerve endings.
3. Mixed-Acting Sympatomimetics - both direct and indirect acting; stimulates adrenergic
receptor sites and stimulates the release of norepinephrine from the terminal nerve endings.

CATECHOLAMINES – are the chemical structures of a substance either endogenous or synthetic that can
produce a sympathomimetic response.
Examples:
1. ENDOGENOUS
a. Epinephrine
b. Norepinephrine
c. Dopamine
2. SYNTHETIC
a. Isoproterenol
b. Dobutamine
NON-CATHECOLAMINES
- stimulates the adrenergic receptors; have longer duration of action than cathecolamines.
Examples:
a. phenylephrine
b. metaproterenol
c. albuterol
NOTE: Many of these adrenergic drugs stimulate more than one receptor sites.

ADRENERGIC DRUGS:

1. EPINEPHRINE ( Trade Name: Adrenalin)


- Is a non-selective adrenergic drug that stimulates more than one receptor ssites.
- Acts on Alpha 1,beta 1 and beta 2 receptor sites.
- Response of stimulation results to:
a. Increased BP c. Increased HR
b. Pupil dilatation d. Bronchoconstriction
- During shock, it is useful because it increases BP, HR and airflow thru the lungs thru bronchodilation.
ROUTES:
a. SubQ c. Topical
b. IV d. Inhalation

Note: it should not be given orally because it is rapidly metabolized in the GIT and liver; thus
inadequate serum level occurs.

2. ALBUTEROL ( Proventil, Salbutamol, Ventolin)

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- Is selective for beta2 adrenergic receptors, so the response is purely bronchodialtion.
- Is well absorbed in the GIT and is extensively metabolized in the liver.
3. ISOPROTERENOL HCl ( Isuprel)
- Activates beta1 and beta2 receptor sites.
- Is more specific than epinephrine because it acts on two different adrenergic receptors but is
not completely selective.
- The response to beta 1 and beta 2 stimulation is bronchodilation and increased HR.
- When used excessively, sever tachycardia can result.
4. CLONIDINE (Catapres)AND METHYLDOPA(Aldomet)
- Are selective alpha2 adrenergic drugs that are used primarily to treat HPN.
- Regulate the release of norepinephrine by inhibiting its release.
- Produces cardiovascular depression by stimulating alpha2 receptors in the CNS leading to
decreased BP

B. ADRENERGIC BLOCKERS/ANTAGONISTS – are drugs that block the effects of the adrenergic
neurotransmitters by:

1. DIRECTLY – occupying the alpha or beta receptor sites;


2. INDIRECTLY – inhibiting the release of the neurotransmitters.

Receptor Sites:
1. Alpha 1
2. Beta 1
3. Beta2

ADRENERGIC BLOCKER AGENTS:

1. ALPHA-ADRENERGIC BLOCKERS (Alpha Blockers)


- Are drugs that block or inhibit a response at the alpha-adrenergic receptor sites.
- Promotes vasodilation thus causing decreased BP.
- It can be used to treat peripheral vascular disease.
2. BETA-ADRENERGIC BLOCKERS (Beta-Blockers)
- Decreases HR resulting to decreased BP and bronchodialtion.
- Some are non-selective, blocking both beta1 and beta2 receptor sites.
Intrinsic Sympathomimetic Activity (ISA)
- Causes partial stimulation of beta receptors.
Non-selective Beta Blockers:
1. Carteolol
2. Carvedilol
3. Penbutolol
4. Pindolol
Propanolol Hcl (Inderal)
- Was the first betablocker prescribed o treat angina, cardiac dysrhythmias and HPN.
3. ADRENERGIC NEURON BLOCKERS
- Are the drugs that block the release of norepinephrine from the sympathetic terminal neurons.
- Are used to decrease BP.
EXAMPLES:
1. Guanethidine monosulfate (Ismelin)

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2. Guanadrel So4 (Hylorel)

II. CHOLINERGICS (Parasympathomimetics)


- Are drugs that stimulate the parasympathetic nervous system, because they mimic the
parasympathetic neurotransmitter ACETYLCHOLINE.
Receptors:
1. Muscarinic Receptors
- Located in the smooth muscles of the GIT, GUT, glands and heart; stimulates smooth muscles
and slows HR.
2. Nicotinic Receptors (Neuromuscular)
- Affects the skeletal muscles

A. CHOLINERGIC AGENTS:

1. Direct-Acting Cholinergic Drugs


- Are drugs that resemble acetylcholine and act directly on the receptor; are primarily selective to
the muscarinic receptors but are non-specific.
Examples:
a. Bethanecol (Urecholine) – acts on the muscarinic receptor, used primarily to increase
urination.
b. Metoclopromide Hcl (Reglan) – is used to treat gastro-esophageal reflux (GERD) and
increase gastric emptying time.
c. Pilocarpine – constricts pupils; is used to treat glaucoma by rlieving fluid by opening the
canal of Schlemm to promote drainage of aqeous humor.
2. Indirect- Acting Cholinergics
-inhibits the action of the enzymes cholinesterase by forming a chemical complex, thus
permitting acetylcholine to persist and attach to the receptor.
- do not act on any receptor site but only inactivates cholinesterase permitting acetylcholine
to accumulate at the receptor site.
Types of Indirect-Acting Cholinergics:
a. Reversible Cholinesterase Inhibitors – produce papillary constriction in the terminal
glaucoma and increase muscle strength in Myesthenia Gravis.
Examples:
1. Neostigmine (Prostigmine)
2. Pyridostigmine Bromide (Mestinon)
3. Ambenonium Chloride ( Mytelase)
4. Edrophonium Chloride ( Tensilon)
b. Irreversible Cholinesterase Inhibitors – are potent agents because of their long lasting
effect; used to produce papillary constriction and manufacture organophosphate
insecticides

B. ANTI-CHOLINERGICS ( Parasympatholytics) - are drugs that inhibit the action of the


acetylcholine by occupying the acetylcholine receptors.
Types:
1. ATROPINE (Atropine SO4) - first derived from the belladonna plant and purified in 1831; is a classic
anticholinergic or muscarinic antagonist drug. It acts on the muscarinic receptor but have little
effect on the nicotinic receptor site.
USES:

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a. Pre-op medication to decrease salivary secretion.
b. Anti-spasmodic to treat peptic ulcers because it relaxes smooth muscles of the GIT and
peristalsis.
c. Agent to increase HR when bradycardia is present.
d. Antidote for muscarinic agonist poisoning.
2. ANTI-PARKINSON- ANTICHOLINERGIC DRUGS
EXAMPLE: Trihexyphenidyl - is well absorbed from the GIT; decrease involuntary
movements and diminishes signs and symptoms of tremors and rigidity that
occurs in Parkinson’s disease.
3. ANTIHISTAMINES FOR TREATING MOTION SICKNESS
a. Scopolamine – available in patch behind the ear.
b. Dimenhydrinate (Dramamine)
c. Meclizine Hcl (Bonamine)
d. Cycline (Marezine)

 NEUROLOGIC AND NEUROMUSCULAR AGENTS

I. CENTRAL NERVOUS SYSTEM STIMULANTS

1. AMPHETAMINES – stimulate the release of the neurotransmitters norepinephrine and dopamine


from the brain and sympathetic nervous sytem.
Effects:
a. Euphoria and alertness e. increased HR
b. Sleeplessness/ lnsomnia f. palpitations
c. Restlessness g. cardiac dysrrhythmias
d. Tremors h. increased BP
e. Irritability
Examples:
a. Amphetamine (Adderal)
b. Dextroamphetamine (Dexedrine)
c. Metamphetamine(Desoxyn)
AMPHETAMINE-LIKE DRUGS TO TREAT ADHD AND NARCOLEPSY
a. Methylphenidate (Ritalin)
b. Dexmethylphenidate ( Focalin)
c. Pemoline (Cylert)
d. Modafinil ( Provigil)
Mechanism of Action:
a. Increase child’s attention span and cognitive performance.
b. Decreases impulsiveness, hyperactivity and restlessness.
c. Treats narcolepsy.
Important Considerations:
a. Pemoline should not be considered a first-line drug for ADHD.
b. There is less potential abuse of Pemoline than Methylphenidate (Ritalin) thus is classified as
scheduled substance.

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c. These should not be taken in the evening.

2. ANOREXIANTS (Appetite Stimulants) – to treat obesity.


Examples:
a. Benzphetamine Hcl (Didrex)
b. Dextroamphetamine SO4 (Dexedrine)
c. Diethylpropion HCl (Dospon, Tenuate, Tenapil, Nobesine)
d. Phentermine HCl (Fastin, Ionamin, Zantryl, Adipex P, Obe-nix 30 )
e. Without Propanolamine HCl: Acutrim, Control, Dexatrim, Dexatrine Natural, Protamine
Important Considerations:
1. Amphetamines are recommended as anofexiants for SHORT term use only (4 12 weeks) or
not at all.
2. FDA ordered the removal of phenylpropanolamine fro OTC drugs, weight loss drugs and cold
remedies.
3. Studies showed that young women who took propanolamine added weight loss drugs has
increased risk for HPN, stroke, renal failure, psychosis and cardiac dysrhythmias.
4. Exercise, diet and lifestyle modification is still the best weight loss management.

3. ANALEPTICS – is a CNS stimulant that affects the brain stem and spinal cord but may also affect the
cerebral cortex.
Action: stimulates respiration
Examples:
a. Methylxanthines – caffeine and theophylline are the main drugs
b. Doxapram HCl (Dopram) - respiratory stimulant

4. RESPIRATORY NERVOUS SYSTEM STIMULANTS

Doxapram (Dopram) – is a CNS and respiratory stimulant used to treat respiratory depression caused
by:
a. Drug overdose
b. Pre and post op anesthetic respiratory depression
c. COPD
Note: should be used with caution for the treatment of neonatal apnea and over dosage leads to HPN,
tachycardia and convulsion.

5. HEADACHES: MIGRAINE AND CLUSTER

Migraine Headaches – are characterized by unilateral throbbing head pain accompanied by nausea and
vomiting and photophobia.

CAUSE: inflammation and dilatation of blood vessels in the cranium.

TYPES:
a. Classic Migraines – are associated with an aura that occurs minutes to one hour before onset.
b. Common Migraines – are not associated with an aura.

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Cluster Headaches - are characterized by a severe unilateral, n on-throbbing pain usually locat4d
around the eye. They occur in series of cluster attacks and are nit associated with an aura; do not cause
nausea and vomiting; men are more affected.
TREATMENT:
A. PREVENTIVE
1. Beta-adrenergic blockers
2. Anticonvulsants
3. Tricyclic antidepressants
B. TREATMENT OF ACUTE ATTACK
MILD
1. Aspirin
2. Acetaminophen
3. NSAIDS
4. Meperidine HCl
5. Butorphanol Nasal Spray (Stadol NS)
MODERATE
1. Ergotamine Tartrate
2. Dihydroergotamine
ACUTE ATTACKS
1. Triptans ( 5-HT< receptor agonist)

II. CENTRAL NERVOUS SYSTEM DEPRESSANTS

1. SEDATIVE HYPNOTICS – is the mildest form of CNS sedation which diminishes physical and mental
responses at lower dosages; increasing the drug dose can produce hypnotic effect but not hypnosis,
instead, natural sleep.
A. Barbiturates – were introduced as a sedative in the early 1900s.
a. Long-Acting Barbiturates - is used to control seizures in epilepsy.
e.g. Phenobarbital, Mephobarbital
b. Intermediate –Acting Barbiturates – is used as sleep sustainers for maintaining long periods of
sleep.
Examples: Amobarbital (Amytal), Aprobarbital (Alurate), Butabarbital ( Butisol)
c. Short-Acting Barbiturates – are used to induce sleep for those who have difficulty falling
asleep; may cause person to awaken early in the morning.
Examples: Secobarbital (Seconal), Pentobarbital (Nembutal)
d. Ultra –Short Acting Barbiturates – is used as general anesthesia.
Example: Thiopental Na (Pentothal)
NOTE: Barbiturates should be restricted to short-term use ( 2 weeks or less) because of their
numerous side effects including drug tolerance.

B. Benzodiazepines – are ordered as sedative-hypnotics for inducing sleep; increases the action of the
inhibitory neurotransmitter GABA to the GABA receptors.
Examples:
a. Flurazepam (Dalmane) e. Quazepam ( Doral)
b. Temazepam (Restril) f. Lorazepam ( Ativan)
c. Triazolam (Halcion) g. Diazepam ( Valium)
d. Estazolam (Prosom)

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Flumazenil – is the antidote for Benzodiazepine overdosage.

C. Non-Benzodiazepines – introduced in 1960; is used for short-term treatment of insomnia (10 days
only)Example: Zolpidem (Ambion)
D. Piperidinedimes – introduced mid 1950s; resemble benzodiazepine with effects similar to shrt-
acting barbiturates. It can be addictive and can cause severe rections.
E. Chloral Hydrate – was introduced in 1860s; is used to induce sleep and to decrease nocturnal
awakenings. It can be given with clients with mild liver dysfunction but should be avoided if severe liver
or renal disorder is present.

2. ANESTHETICS – are classified as local or general.


General Anesthesia – depress the CNS, alleviate pain and cause a loss of consciousness.
Nitrous Oxide (“Laughing Gas”) – was the first anesthesia used for surgery in 1800s; it is still an
effective anesthetic and is frequently used in dental surgery.
Ether and Chloroform – was introduced in the mid 1800s; but is now NOT USED.

STAGES OF ANESTHESIA:

A. Analgesia (Induction Stage) – begins with the consciousness and ends with the loss of
consciousness; speech is difficult, sensations of smell and pain are lost; dreams and ssuditory and visual
hallucinations may ossur.
B. Excitement and Delirium- produces a loss of consciousness caused by depression of the cerebral
cortex; confusion, excitement or delirium may occur; short induction time.
C. Surgical – surgical procedure is performed during this stage; as anesthesia deepens, the respiration
becomes shallow and RR increased.
D. Medullary Paralysis (Toxic Stage) – respirations are lost and circulatory collapse occurs; ventilator
assistance is necessary.

TYPES OF ANESTHESIA:

1. Inhalation Anesthetics –are used to deliver anesthesia during the third stage of anesthesia. It
provides smooth induction and recovery of consciousness occurs after 1 hour or minutes. Are
usually mixed with barbiturates, strong analgesics and a muscle relaxant for surgical procedures.

Examples:
a. Desflurane e. Halothane
b. Cyclopropane f. Cyclopropane
c. Methoxyflurane g. Methoxyflurane
d. Sevoflurane h. Sevoflurane
Side Effects:
a. Respiratory depression
b. Hypotewnsion
c. Dysrhythmias
d. Hepatic dysfunction
e. Hyperthermia
f.
2. Intravenous Anesthetics – maybe used for general anesthesia or for the induction of anesthesia;
have rapid onset and short duration of action.

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Examples:
a. Thiopental Na (Pentothal)
b. Droperidol (Innovar)
c. Etomidate (Amidate)
d. Ketamine HCl (Ketalar)
e. Midazolam (Versed)
f. Propofol (Diprivan)
Adverse Effects:
a. Respiratory depression
b. Cardiovascular depression
c. May support microbial growth and may increase risk of bacterial infection.

3. Topical Anesthetics – is limited to mucus membranes, broken or unbroken skin surfaces and
burns. It decreases the sensitive nerve endings of the affected area. It may come in different
forms such as solutions, liquid, spray, ointment, cream and gel.

4. Local Anesthetics – blocks pain at the site where the drug is administered allowing consciousness
to be maintained.
Uses:
a. Performing dental procedures.
b. Suturing skin lacerations
c. Performing short-term surgery at a localized area.
d. Blocking nerve impulses below the insertion of a spinal anesthesia.
e. Performing diagnostic procedures.
Examples:
a. Cocaine HCl
b. Procaine HCl
c. Lidocaine HCl
d. Pain free Pump System
5. Spinal Anesthesia – requires that a local anesthetic be injected in the subarachnoid space
between L3 and L4.

Sites:
a. Spinal Block – is the penetration of the anesthetic into the subarachnoid membrane
b. Epidural Block – is the placement of the local anesthetic in the outer covering of the
spinal cord.
c. Saddle Block – is given at the lower end of the spinal column to block the perineal area. It
is frequently used for women in labor during childbirth.
Important Considerations:
a. If the local anesthesia is given too high in the spinal column, the respiratory muscles
could be affected and respiratory distress could result.
b. Headaches might result following spinal anesthesia due to a decrease in the CSF
pressure caused by the leak of fluid at the needle insertion.
c. Encourage client to remain FLAT following surgery with spinal anesthesia and take
increased fluids.
d. Hypotension can occur following spinal anesthesia.
e. BP should be monitored during administration of these types of anesthesia because a
decrease in BP resulting from the drug might occur.

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f. Prepare the client for surgery by explaining the preparations and completing the pre-op
medications to enhance safety and effectiveness of anesthesia and surgery.

III. DRUGS FOR PAIN MANAGEMENT: NON-NARCOTIC AND NARCOTIC ANALGESIC

1. NARCOTIC ANALGESIC –are not addictive and are less potent than narcotic analgesics; it acts at the
PNS at the pain receptor sites. They are used to treat mild to moderate pain and maybe purchased over-
the –counter.
A. Salicylates and Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) – have an analgesic effect as
well as antipyretic and anti-inflammatory action.
Examples:
a. Aspirin (ASA)
b. Ibuprofen
c. Naproxen
B. Acetaminophen - is a popular non-prescription drug taken by infants, children and adults and
older adults to relieve pain, discomfort and fever. It is a non-narcotic drug but is not an NSAID.
It does not have any anti-inflammatory effect.
Examples:
a. Tylenol
b. Panadol
c. Tempra
d. Excedrin
2. NON-NARCOTIC ANALGESICS/ NARCOTIC AGONISTS – are prescribed for moderate and severe pain.
It acts mostly on the CNS. It does not only suppress pain impulses but also suppress respirations and
coughing by acting on the respiratory and cough cebnters in the medulla and brain stem. It has also an
antitussive and anti-diarrheal effect.
A. Opium - was used as early as 350 B.C. to relieve pain.
B. Morphine – is an extraction from opium, is a potent narcotic analgesic. It is used for acute pain
resulting from acute MI, cancer and dyspnea from pulmonary edema. It is also a pre-op
medication
Adverse Reactions:
a. Respiratory depression
b. Orthostatic hypotension
c. Miosis
d. Urinary retention
e. Constipation due to decreased bowel motility.
f. Cough suppression
C. Meperidine - has a shorter duration of action than morphine and its potency varies according to
the dosage, it is effective in GI procedures. It is preferred over morphine during pregnancy
because it soes not diminish uterine contractions and cause lesser neonatal respiratory
depression. It should not be prescribed for long-term use.
D. Hydromorphone (Dilaudid) – is a semisynthetic narcotic similar to morphine. The analgesic
effect is 6X more potent than morphine with fewer hypnotic effects and less GI distress. It has a
faster onset and shorter duration of action than morphine. It is given orally, rectally, subQ, IM
and IV and maybe administered by PCA.
E. Combination drugs ( Analgesic + Narcotic Analgesic) – is used to treat moderate to severe pain.
It helps to decrease drug dependency that may result from possible long-time use of a narcotic
agent.

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Example:
a. Hydrocodone + Ibuprofen
b. Acetaminophen + Codeine
F. Transdermal Opioid Analgesics – provide a continuous “round-the-clock” pain control that is
helpful to clients who suffer fro chronic pain. It is not useful for acute post-op pain.
Example: Fentanyl (Duragesic)

3. NARCOTIC AGONIST-ANATAGONIST (Mixed Narcotic-Agonist Antagonist)- is a mixture of agonist-


antagonist were developed in hopes of decreasing narcotic abuse. These are considered safe for use
during labor; however, their safety when taken during pregnancy has not yet been established.
Examples:
a. Naloxone (NArcan)
b. Pentazocine (Talwin)
c. Butorphanol tartrate (Stadol)
d. Buprenorphine (Buprenex)
e. Nalbuphine HCl (Nubain)
4. NARCOTIC ANTAGONISTS – are antidotes for overdoses of narcotic analgesics. It blocks the receptor
and displaces any narcotic that would normally be at the receptor, thus, inhibiting the narcotic action.
Examples:
a. Naloxone ( NArcan)
b. Naltrexone Hcl (Re Via)
c. Nalmefene (Revex)
METHADONE TREATMENT PROGRAM – is the treatment for narcotic addicted persons. It works by
replacing the narcotics with methadone, also a narcotic but causes less dependency than narcotic it
replaces. The half-life is longer than most of the narcotics so it is given OD. The dosage is 15-40 mg/day,
a maximum of 120 mg/day.
Types:
1. Weaning Program – the person receives a dose for the first 2 days that is approximately the same as
the dose of the “street” drug to which he is addicted. After 2 days, the dose maybe decreased by 5 -10
mg daily or as indicated until the person is weaned from the methadone.
2. Maintenance Program – the person is given the same dose every day. The dose maybe less than that
of the “street” drug, but it remains consistent throughout the course of the treatment.

IV. ANTI-CONVULSANTS/ ANTI-EPILEPTICS- are drugs used for epileptic seizures. It suppresses the
abnormal electrical impulses from the seizure focus to other cortical areas, thus, preventing the seizure
but not eliminating the cause of the seizure. They are usually taken throughout the person’s lifetime but
in some cases, it might be discontinued if there has not been a seizure for 3-5 years.
1. Hydantoins (Phenytoin) - was the first anticonvulsant used to treat seizures. It has the least toxic
effects, has a small effect on general sedation and is non-addicting. However. It has a high
teratogenic effect.
2. Barbiturates (Phenobarbital) – is a long-acting barbiturate used to treat grand mal seizures and
acute episodes of status epilepticus, meningitis, toxic reactions and eclampsia. Teratogenic effects
and other effects are lesser. NOTE: discontinue gradually to avoid recurrence of seizures.
3. Succinamides – are used to treat absence of petit mal seizures. They maybe used with combination
with other anti-convulsants to treat seizures.
Examples:
a. Ethosuximide (Zarontin)
b. Methsuximide (Celontin)

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c. Phensuximide (Milontin)
4. Oxalidines/Oxazolidinedones – are also used to treat petit malseizures. There are many severe
side effects associated with this drug group.
Examples:
a. Trimethadione
b. Paramethadione
5. Benzodiazepines
Examples:
a. Clorazepam
b. Clorazepat dipotassium
c. Diazepam
6. Iminostilbenes ( Carbamazepine) - is effective in treating refractory seizure disorders that have nit
responded to other anti convulsants. It is used to control grand mal seizures and a combination of
this seizures. It is also used for psychiatric disorders.
Note: An interaction may occur with grapefruit juice causing possible toxicity.
7. Valproate (Valproic Acid) – is used for petit mal seizure, grand mal seizure and mixed types of
seizures. Caution when administering with young children and clients with liver disease.

V. DRUGS FOR NEUROLOGIC DISORDERS: Parkinsonism and Alzheimer’s Disease


PARKINSONISM - is a chronic neurologic disorder that affects the extrapyramidal tract. It is considered
a syndrome because of its THREE MAJOR FEATURES:
1. Rigidity
2. Bradykinesia
3. Tremors
ANTI-PARKINSON DRUGS:
1. Anti- Cholinergics - reduces the rigidity and some of the tremors characteristic of Parkinsonism but
have minimal effects on bradykinesia.
Examples:
a. Trihexyphenidyl ) Artane )
b. Benztropine ( Cogentin )
c. Biperiden (Akineton )
d. Procyclidine ( Kemadrine )
e. Ethopropazine ( Parsidol)
f. Orphenadrine ( Norflex)
g. Diphenhydramine (Benadryl)
2. Dopaminergics
Examples:
A. Levodopa-- is the first dopaminergic developed and introduced in 1961. It is the most effective
drug for diminishing the symptoms of Parkinsonism. It’s major benefit is MOBILITY. It is initially
administered in low doses for one week and then gradually increased over a period of weeks.
B. Carbidopa and Levodopa ( 1 part Carbidopa : 10 parts Levodopa)
a. More dopamine reaches the basal ganglia.
b. A single dose per day is administered instead of multiple doses.
c. Smaller doses of levodopa are required to achieve the desired effect.
3. Dopamine Agonists - stimulates the dopamine receptors.
A. Amantadine HCl ( Symmetrel) – is an antiviral agent that acts on the dopamine receptors. It is
also used to treat drug-induced Parkinsonism. It maybe given alone or in combination with
levodopa or any anti-cholinergic drug.

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B. Bromocriptine mesylate ( Parlodel) – acts directly on the dopamine receptors in the CNS,
cardiovascular system, and GIT. It is more effective than amantadine and the anti-cholinergics;
however, is not as effective as levodopa in treating Parkinsonism.
4. MAO-B Inhibitor (Mono-amine B Oxidase Inhibitor) – causes catabolism of dopamine.
*Selegiline - inhibits MAO-B thus prolonging the action of levodopa. Large doses may inhibit
MAO-A.
5. COMT Inhibitors ( Catechol- O- Methyltransferase) – inactivates dopamine. When taken with
levodopa, in increases the amount of levodopa concentration in the brain.
A. Tolcapane ( Tasmar) - was the first COMT inhibitor taken with levodopa for advanced
Parkinson’s disease. It can affect liver cell function; thus, serum liver enzymes should be closely
monitored.
B. Entacapone (Comtan) - is the newest COMT inhibitor approved by the FDA.

ALZHEIMER’S DISEASE - is an incurable dementia illness characterized by chronic, progressive,


neurodegenerative conditions with marked cognitive dysfunction. The onset occurs between ages 45
and 65.

Causes:
1. Degeneration of the cholinergic neuron and deficiency in acetylcholine.
2. Neuritic plaques that form mainly outside the neurons and in the cerebral cortex.
3. Apolipoprotein E4 (Apo E4) that promotes formation of neuritic plaques which binds beta-
amyloid in the plaques.
4. Beta-amyloid protein accumulation in high levels that may contribute to neuronal injury.
5. Presence of neurfibrillary tangles with twists inside the neurons.
Stages:
1. Mild (Early Confusion) – cognitive decline in one or more areas, memory loss, decreased ability
to function in work situation, name finding deficit, some decreased in social functioning, recall
difficulty and anxiety.
2. Moderate – unable to perform complex tasks such as managing personal finances. Unable to
concentrate and no knowledge of current events.
3. Moderately Severe ( Early Dementia ) – usually needs assistance for survival. Need reminders in
bathing and needs help in selecting clothes and other daily functions. Maybe disoriented as to
time and recent events although this can fluctuate. May become tearful.
4. Severe (Dementia) – needs assistance with dressing, bathing and toilet functions. May forget
spouse. Family and caregivers’ names, details of their personal life. Generally unaware of their
surroundings. Has fecal and urine incontinence and increased CNS disturbance.
5. Very Severe ( Late Dementia) – unable to speak, may scream or make sounds. Unable to
ambulate, sit up, smile or feed self. Unable to hold head erect and will ultimately slip into stupor
and coma.
Treatment:
1. Ergoloid mesylate (Hydergine) – has not been successful in treating memory loss.
2. Tacrine ( Cognex) - improves cognitive function for clients with mild to moderate Alzheimer’s
disease. It increases the amount of Ach at the cholinergic synapses and tends to slow the
disease process.
3. Donepezil (Aricept)
4. Rivastigmine (Exelon) – permits more acetylcholine in the neuron receptors. It has an effective
penetration into the CNS, thus cholinergic transmission is increased.

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VI. DRUGS FOR NEUROMUSCULAR DISORDERS: Myesthenia Gravis, Multiple Sceloris And Muscle
Spasms

A. Myesthenia Gravis (MG)– is a lack of nerve impulses and muscle responses at the myoneural nerve
junctions causes fatigue and muscular weakness of respiratory system, facial muscles and extremities.

Cause: - inadequate secretion of acetylcholine (Ach) or a loss of Ach because of an increase in the
enzyme cholinesterase, which destroys Ach at the myoneural junction.

Treatment:
1. Neostigmine (Prostigmine) – is the first drug used to manage MG. it is a short acting
acetylcholinesterase inhibitor and has a half-life of 0.5- 1 hour. It is given every 2-4 hours and must
be given on time to prevent muscle weakness.
2. Pyridostigmine bromide (Mestinon) – has an intermediate action. Given every 3-6 hours.
3. Ambenonium Cl ( Mytelase) – is a long acting AChE inhibitor. It is usually prescribed when the
client does not respond to neostigmine or pyridostigmine.

B. Multiple Sclerosis (MS)- is an autoimmune disorder that attacks the myelin sheath of nerve fibers
in the brain and spinal cord, causing lesions that are called PLAQUES. The onset is usually slow and is
difficult to diagnose because there is no specific diagnostic test. It is a condition in which there is
remissions and exacerbations of multiple symptoms such as diplopia, weakness in the extremities or
spasticity.

Phases with Corresponding Treatment:


1. Acute Attack – fatigue, motor, optic neuritis.
Treatment:
a. Tapering course of glucocorticoids (Prednisone)
b. Adrenocorticotrophic Hormone (ACTH)
c. 6-alpha methylprednisolone Na Succinate
2. Remission- exacerbation – recurrence of clinical MS symptoms, spasticity.
Treatment:
a. Biologic (immune) response modifiers (BRM)
Interferon B (IFN B) – it reduces spasticity and improves muscle movement.
b. Immunosuppressant Drug
Azathioprine (Imuran) – reduces exacerbation/ relapses; used to decrease steroid
use.
3. Chronic Progressive- progressive MS symptoms.
Treatment: Cyclophosphamide (Cytoxan)

C. Muscular Spasms – have various causes including injury or motor neuron disorder resulting in the
following conditions:1) Cerebral Palsy;2) MS; 3) CVA; 4) Hemiplegia.
Treatment:
Muscle Relaxants – relieves muscular spasm and pain associated with traumatic injuries and spasticity
from chronic debilitating disorders.
Types:
1. Anxiolytics
a. Diazepam (Valium)

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b. Meprobanate ( Equanil, Miltown)
2. Centrally- Acting Muscle Relaxants (Spasticity)
a. Baclofen ( Lioresal) f. Cyclobenzapdine HCl(Flexeril, Cycloflex)
b. Tizanidine (Zanaflex) g. Methocarbamol ( Robaxin, Marbaxin)
c. Dantrolene Na (Dantrium) h. Orphenadrine Citrate ( Nirflex, Flexon)
d. Carisopradol (Soma)
e. Chlorzoxazone ( Parsaflex, Parafon Forte)
3. Depolarizing Muscle Relaxants
a. Pancuronium bromide (Pavulan)
b. Seccynilcholine bromide (Norcuron)
c. Vecuronium bromide (Nircuron)
d. Tubocurarine Chloride

 PSYCHIATRIC AGENTS

I. ANTIPSYCHOTICS AND ANXIOLYTICS

A. Anti-Psychotic Agents - blocks the actions of dopamine and thus may be classified as
dopaminergic antagonist.

Categories:
1. Typical/ Traditional
a. Phenothiazines - blocks norpinephrine, causing sedative and hypotensive effects early in
treatment.
Types:
 Alipathic phenothiazines – produce a strong sedative efect, decreased BP and may
cause moderate EPS (pseudoparkinsonism)Example: Chlorpromazine (Thorazine)
 Piperazine Phenothiazines – produce a low sedative and strong anti-emetic effect and
have alittle effect on the BP.Example: Fluphenazine (Perphenazine) (Trilafon)
 Piperidine Phenothiazines - have a strong sedative effect, cause few EPS, have low to
moderate effect on BP and have no anti-emetic effect.Example: Thioridazine
(Mellaril)

b. Non-Phenothiazines
Types:
 Butyrophenone – blocks only the dopamine neurotransmitter.
Example: Haloperidol (Haldol)
 Dibenzoxazepine Example: Loxapine (Loxitane)
 Dihypdroindolone ;Example : Molindone HCl Acid ( Moban)
 Thioxanthenes; Example: Thiothixene (Navane)
2. Atypical antipsychotics (Serotonin/ Dopamine Antagonist) – are effective in treating both positive
and negative symptom of schizophrenia.
a. Clozapine ( Clozaril) d. Quetiapine ( Seroquel)
b. Risperidone (Risperdal) e. Ziprasidone ( Geodon)
c. Olanzapine ( Zyprexa) f. Aripiprazole ( Ability)

B. ANXIOLYTICS/ ANTI ANXIETY DRUGS – are primarily used to treat anxiety and insomnia.

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1. Benzodiazepines
USES:
a. Anticonvulsants c. Pre-0p drug
b. Sedative- hypnotics d. Anxiolytics
Examples:
a. Chlordiazepoxide ( Librium) e. Alprazolam ( Xanax)
b. Diazepam ( Valium) f. Prazepam ( Centrax)
c. Lorazepam ( Ativan) g. Halazepam ( Paxipam)
d. Clorazepate dipotassium ( Tranxene)
2. Miscellaneous Anxiolytic; Buspirone HCl ( Buspar)

II. ANTI DEPRESSANTS AND MOOD STABILIZERS


Anti depressants/ Mood Elevators – are used for depressive episodes that are accompanied by
feelings of hopelessness and helplessness.

TREATMENT
1. Electroconvulsive Therapy (ECT) - was used to treat psychosis and depression before th
introduction of antipsychotics and anti depressants. It is used for clients who are extremely
depressed, suicidal or do not respond to antidepressant therapy. It does not affect the person’s
intellectual function and may affect short-term memory loss.

2. Herbal supplements
a. St. John’s Worth – decrease re-uptake of the neurotransmitters.
b. Gingko Biloba – for mild depression only.

3. Anti-Depressant Agents

A. Tricyclic Antidepresants (TCAs) – are used to treat major depression because they are
effective and less expensive than SSRI’s and other drugs. It blocks the uptake of the
neurotransmitters epinephrine and serotonin in the brain. The clinical response occurs
after 2- 4 weeks; if no improvement occurs, it is slowly withdrawn and another
antidepressant is prescribed. NOTE: Polydrug therapy should be avoided due to serious
side effects.
Examples:
a. Amiptriptyline ( Elavil) e. Desipramine
b. Imipramine HCl ( Tofranil) f. Nortriptyline
c. Trimipramine (Surmontil) g. Proptypline
d. Doxepine (Sinequan)

B. Selective Serotonin Reuptake Inhibitors (SSRI) - was the first classified as second
generation antidepressants. They block the reuptake of serotonin into the nerve terminal
of the CNS, thereby enhancing its transmission at the serotogenic synapse.
Examples:
a. Fluoxetine ( Prozac) d. Paroxetine ( Paxil)
b. Fluvoxamine ( Luvox) e. Citalopram ( Celexa)
c. Sertraline ( Zoloft) f. Escitalopram ( Lexapro)

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C. Atypical Anti depressants/ Heterocyclic Antidepressants/ Second-generation
Antidepressants - are used for major depression, reactive depression and anxiety. They
affect one or two of the three neurotransmitters: serotonin, norepinephrine and
dopamine.
Examples:
a. Amoxapine (Asendin) e. Trazadone ( Desyrel)
b. Bupropion (Wellbutrin) f. Mitrazapine ( Remeron)
c. Maprotiline ( Ludiomil) g. Venladaxine ( Efexor)
d. Nefazodone (Serzone) h. Reboxetine ( Vestra)
NOTE: they should not be taken with MAOI’s and should not be used within 14 days after
discontinuing MAOI’s

D. Monoamine Oxidase Inhibitors (MAOI’s) – inhibits the release of the enzyme monoamine
oxidase leading to the increased levels of the neurotransmitters norepinephrine,
dopamine, epinephrine and serotonin.

Examples:
a. Tranylcypromine SO4 (Parnate)
b. Isocarboxacid (Marplan)
c. Phenelzine SO4 ( Nardil)

Important Considerations:
1. MAOI’s are as effective as TCA’s for treating depression, but because of adverse effects, only 1% of
clients take MAOI.
2. MAOI’s are NOT the antidepressant of choice; but maybe given for mild anxiety, reactive and atypical
depression.
3. MAOI’s are ussually prescribed when the client does not respond to TCA’s or second generation
antidepressants.
4. MAOI’s and TCA’s should NOT be taken together when treating depression.
Mood Stabilizers
Lithium – was first used as a salt substitute in the 1940’s, but because of lithium toxicity,it was banned
from the market. It is used to treat bipolar afective disorder. It has a calming effect without impairing
intellectual activity. It controls any evidence of flight of ides and hyperactivity. It is an expensive drug
and must be monitored.

 IMMUNOLOGIC AGENTS

I.HIV AND AIDS-RELATED AGENTS

A. Anti retroviral Therapy


GOALS:
1. Suppress viral replication to slow the decline in the number of CD4+ cells.
2. Suppress viral replication to undetectable levels.
3. Reduce the incidence and seveity of opportunistic infections.
4. Minimize adverse effects of antiretroviral drugs.
5. Improve quality of life.
6. Improve survival and reduce mobility.

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ANTI RETROVIRAL AGENTS:
a. Nucleoside Reverse Transcriptase Inhibitors
 Zidovudine (AZT, ZDV, Retrovir) – improves CD4+ counts, improve survival rates and
survival times and decreases progression. It penetrates the CNS and maybe useful in
the treatment of dementia and thrombocytopenia. It is effctive in preventing infection
of infants, both in the utero and during delivery fro HIV infected women. It is
absorbed rapidly in the GIT; peak in 30 – 90 minutes. It is widely distributed and can
cross th blood-brain barrier. The tablets are taken on an empty stomach and
swallowed whole with plenty of water; capsules can be taken with or without food; IV
administration atleast 60 minutes.
b. Non-nucleoside Reverse Transcriptase Inhibitors (NNRTI’s)
 Efavirenz (Sustiva) – improves CD4+ counts and reduces viral load (VL). It should be
used only in combination with atleast one other nucleoside analogue. It is readily
absorbed following oral administration. Absorption is increased in fatty meals. The
peak concentration occurs in 3-8 hours. It is best taken with an empty stomach. It is
widely distributed with levels in the CSF, metabolized in the liver and excreted in the
feces unchanged and in the urine as metabolite.
c. Protease Inhibitors
 Lopinavir / Ritonavir ( Kaletra) - is used primarily for its antiretroviral activity. It
block protease. It reduces viral plasma level, slows HIV replication and reduces the
progression of hIV infection. It must be used in combination therapy and best taken
with food.
d. Antiretroviral Combinations/ Fusion Inhibitors
 Combivir ( Lamivudine and Zidovudine ) - given in combination and never a
monotherapy.
 Trizivir (Abacavir, Lamivudine and Zidovudine ) - maybe used alone or in
combination with other antiretroviral agents.
The Nurses’ Role in Antiviral Therapy:
1. Thorough assessment of the client’s physiologic and psychosocial health needs.
2. Analysis of the patient’s condition.
3. Facilitate adherence to therapy.
4. Educate client regarding therapy.
5. Identify the problems that require additional investigation and research.

B. Other Drugs for HIV

1. Hydoxyurea ( Hydra) – is used for sickle cell disease and is NOT FDA approved for HIV, but
is currently thought of as a possible drug.
2. Adefovir dipivoxil ( Preveon) – is an NRTI that is available to clients in whom atleast NRTI’s
and one protease inhibitor have failed.
3. Tenofovir ( Viread) – is potent inhibitor of HIV replication.
4. Enfuvirtide (Fuzeon) – Fusion Inhibitors – binds to viral particles and prevents adhesion to
CD4+ cells. It is administered twice daily as a subcutaneous injenction.
5. Atazanavir ( Reyataz) – is a once-a day protease inhibitor. The advantage over other
protease inhibitor is it does not increase the LDL or “bad cholesterol”.
6. Emtricitabine ( Emtriva)- is a once- a day NRTI and is similar to LAmivudine.
7. Fosamprenavir (Lexiva) - is a phosphate ester pro-drug of amprenavir.

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II. VACCINES AND IMMUNIZATIONS
Types of Immunity:
1. Active Immunity – occurs as a part of the human response, which is activated when a pathogen
invades the body; or maybe provoked by an immunization.
VACCINATION – involves the administ5ation of a small amount of antigen, which, although capable of
stimulating an immune response, does not typically produce a disease.
Types:
a. Inactivated / Killed microorganisms
b. Attenuated viruses
c. Toxoids
d. Conjugate vaccines
e. Recombinant subunit vaccines
2. Passive Immunity – occurs when an individual receives antibodies against a particular pathogen
from another source; or maybe acquired via the administration of antibodies pooled from several
human or animal sources tha have been exposed to disease-causing pathogens.
AGENTS USED IN PROVIDING PASSIVE IMMUNITY:
1. Immune Serums
a. Cytomegalovirus (CMV) Immune Globulin Intravenous, Human - is used in the prevention of
CMV in clients receiving kidney transplant.
b. Hepatitis B Immune Globulin - provides passive immunity for persons exposed to Hepa B.
c. Immune Globulin Intravenous – provides rapid increase in intravascular immunoglobulin levels
in clients with immune-deficiency syndrome.
d. Immune Globulin IM, gamma globulin – for the prevention or modification of Hepa A, measles
in susceptible contacts.
e. Lymphocyte Ig, Antihymocyte globulin -for the management of allograft rejection in renal
transplants.
f. Respiratory Syncytial Virus (RSV) Ig – prevents serious respiratory tract infections caused by
RSV in children less than 24 months with bronchopulmonary dysplasia.
g. Rho(D) Ig -is used for the suppression of the immune response of nonsensitized Rho(D)
negative persons who receive Rho(D) positive blood. It is also usewd for the prevention of
sensitization to the Rho(D) factor in RH-negative women who have ended a pregnancy with an
RH-positive fetus or newborn, thus preventing hemolytic anemia of the fetus in the subsequent
pregnancy. Example: RhoGam
h. Tetanus Ig – provides passive immunity in persons not actively immunized against tetanus or
whose immunity status is unknown.
i. Varicella- Zoster Ig - provides passive immunization of susceptible immunodeficient
children after exposure to varicella.
2. Antitoxins and Antivenins
a. Antivenin (Crtotalidae polyvalent) – contains protective substances against the venoms of the
crotalids (pit vipers) including rattlesnakes, cottonmouths, copperheads and moccasins.
b. Antivenin (Micrurus fulvius)- for the tresatment of North American coral snakebites.
c. Black Widow Spider Specie Antivenin(Lactrodectus mactans)- for the treatment of black
widow spider bites.
d. Diphtheria Antitoxin- for the prevention or treatment of diphtheria.
e. Tetanus Antitoxin- for the prevention of tetanus; used only when tetanus immune globulin is
not available.
AGENTS USED FOR ACTIVE IMMUNIZATION
1. Bacterial Vaccines

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a. BCG Vaccine (Tice Vaccine) – is used for TB prophylaxis in persons with tuberculin negative
skin tests exposed to TB.
b. Hemophilus b Conjugate Vaccine – for immunization of children 2 months to 6 years of age
caused by h. influenza b.
c. Meningococcal ( Qadrivalent) – for the prophylaxis of meningitis in high-risk populations.
d. Mixed Respiratory Vaccine (MRV) – is used for desensitization to common bacterial
organisms present in the respiratory system.
e. Pneumococcal Vaccine, polyvalent (Pneumovax 23) – is used for the protection against the
most common types of pneumococci for high risk persons , including those with a
chronic illness, those in chronic care facilities, convalescing clients and 50 years of age and
above.
f. Typhoid Vaccine – for the production of active immunization against typhoid for persons
exposed to typhoid carriers and those travelling to areas where typhoid is endemic.
2. Viral Vaccines
a. Hepa A Vaccines (Havrix, Vaqta)
b. Hepa A and B (Twinrix)
c. Hepa B Vaccine (Heptavax)
d. Influenza Virus Vaccine ( Influenza Virus Trivalent, Ypes A and B, Fluzone, Flumist)- for the
protection against strains of influenza viruses contained in vaccine and closely related
strains. Annual vaccination recommended for persons at increased risk for adverse
consequences from lower respiratory tract infections.
e. Japanese Encephalitis Virus Vaccine (Je-Vax) – for the active immunization against
Japanese encephalitis for persons over one year of age.
f. Measles, Mumps and Rubella Vaccine, live (MMR II) - stimulate immunization against
measles, mumps and rubella in children from 15 months to puberty.
g. Measles (Rubeola) Virus Vaccine, live, attenuated (Attenuvax)- active immunization of
children 15 months of age or older against measles.
h. Mumps Virus Vaccine, live ( Mumpsvax) – for the immunization against mumps in
children 12 months or older.
i. Poliovirus Vaccine, inactivated (IVP) – for the active immunization against poliomyelitis.
j. Rubella and Mumps Virus Vaccine, live (Biavax II)- for the simultaneous immunization
against rubella and mumps in children from 12 months of age to puberty.
k. Rubella Virus, live (Meruvax II) – for the immunization against rubella in children from 12
months of age to puberty. It may also be used to control rubella outbreak.
l. Varicella Vaccine – live, attenuated vaccine for active immunization for healthy children
over age 12 months and adults. Also effective in chicken pox and shingles.
m. Yellow Fever Vaccine (YF-Vax) – for the active immunization of travelers to countries
requiring vaccination; for use in persons 6 months and older.

3. Toxoids
a. Diphtheria and Tetanus Toxoids and Pertussis Vaccine (DTaP) - for the active
immunization of infants over 2 months and children under 7 years of age against
diphtheria, tetanus and pertussis.
b. Diphtheria and Tetanus Toxoids and Acellular Pertussis Vaccine (Datpacel) – for the active
immunization against diphtheria, tetanus and pertussis as the 4 th or 5th dose in children
from 15 months to 7 years of age.
c. Tetanus Toxoid (Tetanus toxod fluid; tetanus toxoid adsorbed) – for the active
immunization against tetanus for adults and children.

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NURSING RESPONSIBILITIES TOWARDS VACCINE ADMINISTRATION:
1. Obtain history of allergy before administering any agent affecting immunity.
2. Do not use agents beyond their expiration date.
3. Always administer these agents in settings where life support equipment is available.
4. Epinephrine injection 1:1,000 must immediately be available for the treatment of anaphylactic
reactions.
5. Observe client’s reaction to the drug for 20-30 minutes before discharge.
6. Update client’s immunization record.

 ANTI-INFLAMMATORY AND ANTI-INFECTIVES

I. ANTI-INFLAMMATORY AGENTS
Effects/Properties:
a. Analgesic
b. Antipyretic
c. Anticoagulation

A. Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) – inhibits the enzyme CYCLO-OXYGENASE


(COX). Also called “Prostaglandin Inhibitors” which are used primarily as an anti-inflammatory
agent to relieve inflammation and pain.

The 7 Groups:

1. Salicylates related to Aspirin


ASPIRIN (ASA- Acetyl Salicylic Acid) – is a prostaglandin inhibitor that decreases the
inflammatory process. It also decreases platelet aggregation decreasing blood clotting. It is the
drug of choice for alleviating inflammation and pain in arthritic conditions, but when given in
high doses, GI problems could occur.
2. Para-Chlorobenzoic Acid
a. Indomethacin ( Indocin) – is a potent prostaglandin inhibitor used for rheumatoid
arthritis, gouty arthritis and osteoarthritis. It is highly protein-bound and displaces other
protein-bound drugs resulting to potential toxicity. It has a moderate half-life and is very
irritating to the stomach.
b. Sulindac (Clinoril)
c. Tolmetin ( Tolectin)
3. Phenylacetic Acid Derivatives
a. Diclofenac Na ( Voltaren) – is indicated for rheumatoid arthritis, osteoarthritis,
ankylosing spondylitis.
b. Ketorolac ( Toradol) – is administered IM q 6 hours at 30-60 grams, is the first injectable
NSAID. It inhibits prostaglandin synthesis, but has greater analgesic properties than
other anti-inflammatory agents. It is recommended for short-term management of pain.
4. Propionic Acid Derivatives -are aspirin-like but have stronger effects and creates less GI
irritation .
a. Ibuprofen (Motrin) e. Ketoprofen ( Orudis)
b. Fenoprofen Ca ( Nalfan) f. Flurbiprofen ( Ansaid)
c. Naproxen ( Naprosyn) g. Oxaprozin ( Daypro)
d. Suprofen ( Profenal)
5. Fenamates – are used for chronic arthritic conditions.

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a. Meclofen –amate Na monohydrate ( Meclomen)
b. Mefenamic Acid (Ponstel)
6. Oxicams
Piroxicam ( Feldene) –is indicated for long-term arthritic conditions such as rheumatoid
arthritis and osteoarthritis.
7. Selective COX-2 Inhibitors ( Second-generation NSAIDs) – decreases inflammation and pain.
These are the drug of choice for clients with severe arthritic conditions who need high doses of
anti-inflammatory drugs.
a. Celecoxib ( Celebrex)
b. Nabumetone (Relafen)

B. Corticosteroids - are used as anti-inflammatory agents. They control inflammation by


suppressing or preventing many of the components of the inflammatory process at the injured
site. It has a long half-life and is administered ince a day in large prescribed doses.
a. Prednisone
b. Prednisolone
c. Dexamethasone

C. Disease-Modifying Anti-Rheumatic Drugs ( DMARDS) – are used when NSAID do not control
immune-mediated arthritic disease sufficiently. Although more toxic, they alter the disease
process.
1. Gold Drug Therapy - is used to arrest the progression of rheumatic arthritis and to prevent
deformities caused by the disease. It depresses the migration of leukocytes and suppresses
prostaglandin activity. It inhibits destructive lysosomal enzymes that are contained in
leukocytes which are released in joints.
 Auraofin ( Ridaura)
 Aurothioglucose( Solganal)
 Gold Na thiomelate ( Myochrysine)
2. Immunosuppressive Agents – are used to treat refractory rheumatoid arthritis.
 Azathioprine ( Imuran)
 Cyclophosphamide ( Cytoxan)
 Methotrexate ( Mexate)
3. Immunomodulators – treat moderate to severe rheumatoid arthritis by disrupting the
inflammatory process and delaying disease progression.

Group of Immunomodulators:

a. Interleukin ( Il-1) Receptor Antagonist


ANAKIRA (KINERET) – blocks the activity of IL-1 by inhibiting Il-I from binding t interleukin
receptors located in the cartilage of bone. It is administered subQ.
b. Tumor Necrosis Factor Blockers – binds to the TNF and blocks it from attaching to TNF
receptors on the synovial cell surfaces.
 Etanercept ( Enbrel)- is administered sub Q
 Infliximab ( Remicade)
 Adalimumab ( Humira)
 Leflunomide (Arava)

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4. Anti-Malarials – maybe used to treat rheumatoid arthritis when other treatment method
fails. They are usually used in combination with NSAIDs whose arthritis is not under control.

D. Anti-Gout Drugs

1. Colchicines – inhibit the migration of leukocytes to the inflamed site. It is effective in


alleviating acute symptoms of gout, but is not effective in decreasing inflammation occurring
in other inflammatory disorders. It does not inhibit uric acid synthesis and does not promote
uric acid secretion. It should not be used if the client has a severe renal, cardiac or GI
problem.
2. Uric Acid Inhibitor
Allopurinol (Zyloprim)- is not an anti-inflammatory drug but it inhibits the final steps of uric acid
biosynthesis and therefore lowers serum uric acid levels preventing the precipitation of an attack. It is
used as a prophylactic to prevent gout. It is the drug of choice for clients with chronic
tophaceous gout. It is also indicated for clients who have gout and renal impairments.
3. Uricosorics – increase the rate of uric acid excretion by inhibiting its reabsorption. They are
effective in alleviating chronic gout, but they are NOT to be used in acute attacks.
a. probenecid ( Benemid) – blocks the reabsorption of uric acid and promotes its
excretion. It can be taken with colchicines. It should be taken with meals if gastric
irritation occurs.
b. Sulfinpyrazone (Anturane)- is a metabolite of phenylbutazone and is more potent than
probenecid. It should be taken with meals or with antacids to prevent gastric irritation.
Severe blood dyscrasias might occur especially in clients with a history of blood
dyscrasia.

III. ANTI-BACTERIALS/ ANTIBIOTICS

Mechanisms of Action:
1. Inhibition of bacterial cell-wall synthesis.
2. Alteration of membrane permeability.
3. Inhibition of protein synthesis.
4. Inhibition of bacterial RNA and DNA synthesis.
5. Interference with metabolism within the bacterial cell.

A. PENICILLINS / BETA LACTAM ANTIBIOTICS - are natural antibacterial agents from the mold
genus “ Penicillium”. It interferes with bacterial cell wall synthesis by inhibiting the bacterial
enzyme that is necessary for cell division and cellular synthesis. It can be both bacteriostatic
and bactericidal depending on the drug dosage.
1. Pen G - was the first penicillin administered orally and by injection. Because of its poor
absorption, it is given by IM or IV is more effective in achieving the therapeutic level.
2. Pen V – is less potent than PenG. It is effective against mild to moderate infections
including anthrax.
3. Aminopenicillins/ broad- spectrum penicillins- are used to treat both gram positive
and gram negative bacteria. These are not penicillinase resistant however.
a. Ampicillin
b. Amoxicillin
c. Bacampicillin

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4. Antistaphylococcal Penicillin/ Penicillinase –resistant Penicillins – are used to treat
penicillinase producing staphylococcus Aureus.
a. Cloxacillin d. Oxacillin
b. Dicloxacillin
c. Nafcillin
5. Antipseudomonal Penicillins/ Extended-Spectrum Penicillins- is effective against
pseudomonas aeruginosa. They are also effective against many gram-negative organisms.
They are not penicillinase resistant and the action is similar to aminoglycosides, but they
are less toxic.
6. Beta-lactamase Inhibitors – are combination of a broad spectrum antibiotic with a beta-
lactamase inhibitor. It inhibits the bacterial beta-lactamase making the antibiotic
effective and extending its antimicrobial effect.
a. Amoxicillin-clauvinic acid
b. Ampicillin- sulbactam
c. Piperacin- tazobactam
d. Ticarcillin-clavulanic acid
B. CEPHALOSPORINS- is derived from the fungus cephalosporium acremonium. It is active against
gram-positive and gram negative bacteria and resistant to beta-lactamase. It has a beta-lactam
structure and acts by inhibiting the bacterial enzyme that is necessary for cell wall synthesis.
1. Cephalexins (Keflex) 6. Cefuroxime Na ( Zinacef)
2. Cefadroxil ( Duricef) 7. Cefclinir ( Omnicef)
3. Cephadrine (velosef) 8. Ceftibuten ( Cedax)
4. Cefaclor ( Ceclor) 9. Cefixime ( Suprax )
5. Cefuroxime axetil ( Ceftin) 10. Cefazolin Na ( Ancef, Kefzol)
C. MACROLIDES –are active against most gram positive bacteria and moderately active against
some gram negative bacteria. They are used to treat mild to moderate infections of the
respiratory tract, sinuses, GIT, skin and soft tissues as well as diphtheria, impetigo and
contagiosa and STDs.
1. Azithromycin (Zithromax)
2. Clarithromycin (Biaxin)
3. Dirithromycin ( Dynabac)
4. Erythromycin ( E-mycin)
D. LINCOSAMIDES – inhibit bacterial protein synthesis and have both bacteriostatic, bactericidal
actions, depending on drug dosage.
1. Clindamycin ( Cleocin)
2. Lincomycin ( Lincocin)
E. VANCOMYCIN (Vancocin)- IS USED AGAINST DRUG RESISTANT s.Aureus And in cardiac surgical
prophylaxis for individuals with penicillin allergies. It’s use was almost abandoned due to side
effects of nephrotoxicity and ototoxicity.
F. KETOLIDES- are new classification of antibiotics which are structurally related to macrolides.
Telithromycin (Ketek) – is used for adults 18 and above for the treatment of chronic
bronchitis.
G. TETRACYCLINES – is isolated from streptomyces aureofaciens in 1948. They were the first
broad-spectrum antibiotics effective against gram positive and gram negative bacteria. They
are not effective against S. aureus, pseudomonas or proteus. They are frequently prescribed for
oral use, although also available in IM and IV.
H. AMINOCLYCOSIDES –act by inhibiting bacterial protein synthesis. It is used against gram-
negative bacteria such as E.coli. it acts for serious infections.

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1. Streptomycin 4. Amikacin
2. Gentamycin 5. Netilmicin
3. Tobramycin
I. FLIUROQUINOLONES (QUINOLONES)- interferes with the enzyme DNA gyrase which is needed
to synthesize bacterial DNA. It kills both gram-positive and gram negative organisms.
1. Nalidixic Acid (Negram) 5. Levofloxacin ( Levaquin)
2. Cinoxacin ( Cinobac) 6. Sparfloxacin ( Zagam)
3. Ciprofloxacin ( Cipro) 7. Trovafloxacin ( Trivan)
4. Norfloxacin ( Noroxin )
J. SULFONAMIDES – are not classified as antibiotic because they are not obtained from biologic
substances. They are bacteriostatic because they inhibit bacterial synthesis of folic acid, which
is essential for bacterial growth. They are not effective against viruses and fungi.
1. Sulfisoxazole ( Gantrisin) 4. Sulfamerazine
2. Sulfamethoxazole ( Gantanol) 5. Sulfamethazine
3. Sulfadiazine
K. TRIMETHROPRIM AND CO-TRIMOXAZOLE
1. Trimethroprim ( Proloprim, Trimpex) - is an antibacterial agent that interferes with
bacterial folic acid synthesis similarly to sulfonamides. It is classified as urinary tract anti-
infectives that maybe used alone for complicated UTI.
2. Trimethroprim- sulfamethoxazole ( CO-trimoxazloe, BActrim, Septra)
L. UNCLASSIFIED ANTIBACTERIAL DRUGS
1. Chloramphenicol ( Chloromycetin) – is bacteriostatic; inhibits bacterial protein synthesis.
It is used only to treat severe infections.
2. Spectinomycin HCl (Trobicin) – for N.gonorrhea and for persons allergic to penicillin,
cephalosphorins and tetracycline.
3. Quinupristine/ dalfopristin (Synercid) – effective for treating vancomycin resistant
microorganism.

 ANTI-CANCER AGENTS

I. ALKYLATING DRUGS- cause cross linking of DNA strands, abnormal base pairing or DNA strand
breaks preventing the cell from dividing. It kills cells in various and multiple phases of the cell
cycle.
1. Cyclophosphamide ( Cytoxan)
2. Mechlorethamine ( Nitrogen mustard, Mustargen)
II. ANTI-METABOLITES – disrupt the metabolic process and some or the agents inhibits enzyme
synthesis. It is classified according to the substances with which they interfere and include
folic acid antagonists. They are used to treat acute leukemia, breast cancer and head and neck
cancer, lung cancer, osteosarcoma and non-Hodgkins lymphoma.
1. Methotrexate (MTX) - is a folic antagonist used for the treatment of both cancerous and
non-cancerous conditions. It acts as a substitute of folic acid needed for the synthesis of
proteins and DNA.
2. Fluorouracil (5FU) – is administered IV for solid tumors and topically for superficial basal
cell carcinoma. It blocks the enzyme action necessary for DNA and RNA synthesis.
III. ANTI-TUMOR ANTIBIOTICS – inhibits RNA synthesis and binds DNA causing fragmentation.
1. Bleomycin ( Blenoxane) 4. Mitomycin ( Mutacyn)

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2. Dactinomycin ( Actinomycin ) 5. Plimycin ( Mithracin)
3. Doxorubicin ( Adriamycin
IV. MITOTIC INHIBITORS –a re plant alkaloids and other compounds derived from natural products
that blocks cell division.
1. Vinblastin SO4 ( Velban) 4. Doceraxel ( Taxotene)
2. Vincristine SO4 ( Oncovin) 5. Paclitaxel (Taxol)
3. Vinerolbine ( Navelbine)
V. TARGETED CANCER THERAPIES – interferes with cancer cell growth and division in different
ways and at various points in the development, growth and spread of cancer. It may interfere
with proteins or enzymes in cancer cells leading to apoptosis. By blocking the signals that tell
cancer cells to grow and divide uncontrollably, it can stop the growth and division of cancer
cells.
1. Topoisomerase I Inhibitors/ Camptothecins - interferes with the action of Topoisomerase
Enzymes ( I and II) to destroy the structure of the DNA that is needed for replication.
a. Irinotecan c. Teniposide
b. Topotecan
2. Protein Tyrosine Kinases ( PTKs) -are enzymes that regulate signaling pathways in cells and
regulate cell proliferation, differentiation and antiapoptotic signals.
a. Gefinitib ( Iressa)
b. Imatinib mesylate ( Gleevec)
3. Proteasome Inhibitors- prevent the breakdown of certain proteins and transcription
factors and inactive genes and proteins that help cancer cells survive antineoplastic therapy,
causing cancer cell death.
Example: Bortezomib ( Velcade)
4. Monoclonal Antibodies ( Moabs, mAbs) – recognize proteins in specific cancer cells. It can
be used alone or can be used as vehicles to deliver drugs, toxins or radioactive material to
tumor site.
(a) Example : Trastuz2mab ( Herceptin )

VI. LIPOSOMAL CHEMOTHERAPY - is a new approach to deliver chemotherapy that involves the use
of anticancer drugs tha have been packaged inside synthetic fat globules called LIPOSOMES.
1. Doxorubicin
2. Daunorubicin
3. Vincristine

VI. HORMONAL AGENTS – several classes of hormonal agents are used in the treatment of cancer.

1. Corticosteroids - are anti-inflammatory agents that suppress the inflammatory process


that occurs as a result of tumor growth. These blocks steroid- specific receptors on the cell
surfaces.
Examples:
a. Prednisone c. Hydrocortisone
b. Dexametahsone d. Cortisone
2. Sex Hormones ( Estrogen, Androgen) – slow the growth of hormone-dependent tumors.
A. Estrogen Theraphy – is a palliative treatment used to decrease the progression of prostatic
cancer in men and to slow the growth of hormone-dependent breast cancer in women. It
suppress tumor growth and the drug promotes remission of the cancer for up to a year.
Examples

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a. Diethylstilberol ( DES< Stilberol) c. Chlorotrianase
b. Ethynil Estradiol ( Estryl) d. Conjugated estrogens( Premarin)
B. Progestins - is used to treat breast cancer, endometrial cancer and renal cancer. It acts by shrinking
the cancer tissues.
Examples:
a. Hydroxyprogesterone caproate ( Duralutin)
b. Medroxyprogesterone acetate ( Depo-provera)
c. Megestrol acetate ( Meagcel)
C. Androgens – are given to treat advanced breast cancer in premenopausal women. It promotes
regression of the tumor.
D. Anti- Estrogens - are used to treat breast cancer that are estrogen receptor positive.
Examples: a. Tamoxifen (Nolvadex); b. Raloxifene ( Evista)
E. Gonadotropin- Releasing Hormone - suppress the secretion of FSH and LH from the pituitary.
Initially, an increase in testosterone level is seen. With continued use, the pituitary glands become
insensitive to this stimulation which leads to a reduction in the production of androgens and estrogens.
Examples: a. Leuprolide ( Lupran); b. Goserelin ( Zoldex)
F. Anti-Androgens – are useful in treating clients or men with hormone-responsive prostate cancer that
has metastasized. It binds to androgen-receptors and blocks the effect of dihydrotestosterone on the
prostate cancer cells.
Examples: a. Dlutamide ( Eulexin); b. Nilutamide ( Nilandron); c. Bicalutamide ( Casodex)
G. Aromatase inhibitors – block the peripheral conversion of androgens to estrogen, thus suppressing
postmenopausal synthesis of estrogen and slowing tumor growth. They are used in the treatment of
hormonally sensitive breast cancer in postmenopausal women who had their ovaries removed.
Examples: a. Anastrozole (Arimidex); b. Letrozole ( Femora); c. Exemestane ( Aromasin)
H. Miscellaneous Agents: a. L- asparginase ( Elspar; b. Pegaspargase

VIII. BIOLOGIC RESPONSE MODIFIERS ((BRM)- are complex proteins produced by the cells of the
immune system.
Functions:
1. Enhance host immunologic function.
2. Destroy or interfere with tumor activities.
3. Promote differentiation of stem cells.
2. Interferons –are family of natirally occuring proteins discovered in 1950’s.
Interferon –a (IFN-a) – is produced by B- cells, T cells, macrophages and null dells in response
to the prescence of viruses or tumor.
Actions:
a. inhibits intracellular replication of the viral DNA.
b. Interferes with tumor cell growth.
c. Enhances natural killer cell.
Examples: Roferon-A, Intron A
1. Colony- Stimulating Factors- are proteins that stimulate or regulate the growth, maturation
and differentiation of bone marrow stem cells.
Actions:
a. Decrease the length of post treatment neutropenia reducing the incidence and duration
of infection.
b. Permits the delivery of higher doses of drugs.
c. Reduce bone marrow recovery time after transplantation.
d. Enhance macrophage or granulocyte tumor virus and fungus destroying ability.

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e. Prevent severe thrombocytopenia after myelosuppression chemotherapy.
A. Erythropoietin (EPO) (Proctil) - is a glycoprotein produced by the kidney that stimulates
RBC production in response tp hypoxia. It stimulates the division and differentiation of
commited RBC progeitors in the bone marrow.
B. Granulocyte and Pelfilgrastim (Neulasta) Colony-Stimulating Factor – are human
granulocyte colony-stimulating factor produced by recombinant DNA technology.
C. Granulocyte Macrophage- Colony Stimulating Factor – belongs to a group of growth
factors that support survival, clonal expression and differentiation or maturation of
hemopoetic progenitor cells. It induces partially committed progenitor cells to divide and
differentiate in the granulocyte macrophage- pathway.
2. Interleukins/ Lymphocytes – are group of proteins produced by the body’s WBC. Example :
Aldesleukin ( Proleukin)
3. Monoclonal Antibody – are engineered in the laboratory with the specific purpose of
targeting antigens and receptors that are expressed most frequently on cancer cells.
Examples:
a. Gefiinitib ( Iressa) d. Bevacizumab ( Avastin)
b. Cetuximab ( Erbitux) e. Rituximab ( Rituxan)
c. Trastuzumab ( Herceptin)

 GASTROINTESTINAL AGENTS

A. DRUGS FOR GIT DISORDERS

A. Vomiting ( Emesis)
Non-pharmacologic Measures:
1. Administration of weak tea, carbonated beverage and gelatin.
2. Gatorade and pedialyte for children.
3. Crackers and dry toast.
4. IVF if condition is severe to restore body fluid balance.
Non-Prescription Anti-emetics:
1. Dimenhydrinate ( Dramamine)
2. Cyclizine HCl ( Marezine)
3. Meclizine HCl ( Antivert)
4. Diphenhydramine HCl ( Benadryl)
Prescription Anti-emetics
1. Antihistamines and Anticholinergics – acts primarily on the vomiting center. It also act by
decreasing stimulastion of the chemoreceptor trigger zone ( CTZ) and vestibular pathways.
Examples: Hydroxyzine ( Vistaril, Atarax), Promethazine ( Phenergan)’
Scopolamine ( Transderm- Scop)
2. Dopamine Antagonists – suppress emesis by blocking dopamine receptors in the CTZ.
Examples:Phenothiazines: Chlorpromazine ( Thorazine ), Prochlorperazine edisylate
( Compazine) Promethazine ( Phenergan)
3. Benzodiazepines – indirectly control nausea and vomiting that may occur with cancer
chemotherapy.Example: Lorazepam ( Ativan), Diazepam ( Valium)
4. Butyrophenones- blocks the dopamine receptors in the chemoreceptor trigger zone. They
are used to treat post-operative nausea and vomiting and emesis associated with toxins,
cancer chemotherapy and radiation therapy.

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Examples:Haloperidol ( Haldol), Droperidol ( Inapsine)
5. Metochopramide ( Reglan) – suppress emesis by blocking the dopamine in the CTZ. It is used
in the teastment of post-operative nausea, cancer chemotherapy and radiation therapy.
6. Serotonin Receptor Antagonists – suppress nausea and vomiting by blocking the serotonin
receptors and the vagal nerve terminals in the upper GIT.
Examples:
a. Ondansentron ( Zofran)
b. Granisetron ( Kytril)
c. Dolasetron ( Anzernet)
d. Polanosetron ( Aloxil)
7. Glucocorticoids ( Corticosteroids)- suppress vomiting associated with chemotherapy.
Example: Dexamethasone ( Decadron), Methylprednisolone ( SoluMed)
8. Cannabinoids- alleviates nausea and vomiting from cancer treatment. It is used as appetite
stimulants for patients with AIDS. It is prescribed for those who do not respond to or unable
to take other anti-emetics.
Example: Dronabinol (Marinol
9. Miscellaneous Anti-emetics –
Example: Diphenidol ( Vontrol), Trimethobenzamide ( Tigan)
Emetics - are drugs used to induce vomiting to expel the substance before absorption
occurs. Example : Ipecac

B. Diarrhea
TREATMENT:
1. Opiates – decrease intestinal activity thereby decreasing peristalsis.
Examples: Codeine, Diphenoxylate ( Lomotil) , Difenoxin ( Motofen), Loperamide (Imodium)
2. Somatostatin – inhibits gastric acid, pepsinogen, gastrin. cholecystokini, and serotonin secretions
and intestinal fluids. It decreases smooth muscle contractility. It is usually prescribed for severe diarrhea
resulting from metastatic cancer. Example: Octreotide ( Sandostatin)
3. Adsorbents – act by coating the wall of the GIT and adsorbing the bacteria or toxins that cause
diarrhea. Examples: Kaolin, Pectin, Bismuth salts, Calestipol, Cholestyramine (Questran)

C. Constipation – is the accumulation of hard fecal materials in the large intestines.


TREATMENT: Laxatives and Cathartics
Types of Laxatives:
1. Osmotic ( Saline) Laxatives/ Hyperosmolar Laxative – includes saline products Lactulose and
Glycerin. It pulls water into the colon and increase water in the feces to increase bulk which
stimulates peristalsis.
2. Stimulant ( Contact, Irritant) Laxatives – increase peristalsis by irritating sensory nerve endings in
the intestinal mucosa. Examples: Bisacodyl ( Dulcolax), Senna( Senokot), Castor oil
3. Bulk-forming Laxatives- are natural fibrous substances that promote large, soft stools by
absorbing water into the intestines, increasing fecal bulk and peristalsis. Examples: Calcium
polycarbophil ( Fibercon) , Methylcellulose ( Citrucel).
4. Emollients ( Stool Softeners)- are stool softeners and lubricants used to prevent constipation,
decrease straining during defecation. It lowers the surface tension and promotes water retention
in the intestines and stool. Examples: Docusate Ca ( Surfak), Docusate K ( Dialose), Docusate Na
( Colace)

III. ANTI- ULCER DRUGS

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7 GROUPS:
1. Tranquilizers – have a minimal effect in preventing and treating ulcers; however, they reduce vagal
stimulation and decrease anxiety. Example: Librax
2. Anticholinergics – relieve pain by decreasing GI motility and secretions. They act by inhibiting
acetylcholine and blocking histamine and HCl acid. They delay gastric emptying, so they are used
more frequently for duodenal ulcers than for gastric ulcers. Example: Propantheline bromine ( Pro-
Bantine)
3. Antacids – promote ulcer healing by neutralizing the hCl acid and reducing pepsin activity.
a. Systemic Antacids – are systemically absorbed antacid. Example: Na Bicarbonate ( Alka-seltzer)
b. Non-Systemic Antacids – has a small degree of absorption. Example: Al Mg hydroxide ( Maalox
4. Histamine 2 Blockers ( H2 Receptor Antagonist) – prevent acid reflux in the esophagus.
It blocks the H2 receptor of the parietal cells in the stomach, thus reducing gastric acid secretion and
concentration. It is used to treat allergic reactions. Examples: Cimetidine ( Tagamet) , ranitidine
( Zantac), Famotidine ( Pepcid), Nizatidine ( Axid)
5. Proton Pump Inhibitors ( Gastric Acid Secretion Inhibitors, Gastric Acid Pump Inhibitors)-
- suppress gastric acid secfetion by inhibiting the hydrogen/ potassium adenosine triphosphate
(ATPase) enzyme located in the gastric parietal cells. Example: Omeprazole (PRisloec), Lansoprazole
( Prevacid)
6. Pepsin Inhibitor ( Mucosal Protective Drug) – is non-absorbanle and combines with protein to form a
viscous substance that covers the ulcer and protects it from acid and pepsin.
Example: Secralfate ( Carafate)
7. Prostaglandin Analogue Anti Ulcer Drug
Example: Misoprostol – suppress gastric acid secretion and increase cytoprotective mucus in the GIT.

 ENDOCRINE AGENTS

I. PITUITARY GLAND ( Hypophysis)

LOBES:
1. Anterior Pituitary ( Adenohypophysis) – secretes the following various hormones that target tissues
and glands.
A. Growth Hormone
B. Thyroid stimulating hormone
C. Adrenocorticotropic hormone
D. Gonadotropins
DRUG THERAPY:
A. Growth Hormone Deficiency- Somatren (Protropin); Somatropin ( Humatrope)
B. Growth Hormone Excess - Octreotide ( Sandostatin)
C. Thyroid Stimulating Hormone – stimulates the thyroid gland to release THYROXINE(T4) AND
TRIIODOTHYRONINE (T3) or LIOTHYRONINE. Excess secretion can cause hyperthyroidism; deficit can
cause hypothyroidism. Example: Thryotropin ( Thytropar)
D. Adrenocorticotropic Hormone ( ACTH) - stimulates the release of the following hormones:
1. Glucocorticoids ( Cortisol)
2. Mineralocortocoids ( Aldosterone)
3. Androgen ( Androgen)

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Example: Acthar
2. Posterior Pituitary Gland ( Neurohypophysis) - secretes the following hormones:
A. Anti-diuretic Hormone (ADH)
B. Oxytocin
Examples: Vasopressin ( Pitressin); Desmipressin ( DDAVP)
3. Thyroid Gland – secretes the following hormones: Thyroxine ( T4) and Triiodothyronine (T3)
Functions:
1. Regulate protein synthesis.
2. Regulate enzyme activity.
3. Stimulate mitochondrial oxidatioin.

Thyroid Gland Disorders:

A. Hypothyroidism
DRUG THERAPY:
a. Levothyroxine Na ( Levothroid, Synthroid) – is the drug of choice for replacement therapy
for treatment. It increase T3 and T4 levels.
b. Liothyroxine (Cytomel) – is a synthetic T3 that has a short half-life and duration of action.
It is better absorbed in the GIT than levothyroxine.
c. Liotrix ( Euthroid, Thyrolar) – is a mixture of levothyroxine na and liothyronine.

C. Hyperthyroidism

Grave’s Disease – is the most common type of hyperthyroidism caused by the hyper function of the
thyroid glands.
Treatment:
a. Subtotal Thyroidectomy
b. Radioactive Iodine Therapy
c. Drug Therapy - inhibits either the synthesis or the release of thyroid hormone. The purpose is to
reduce the excessive secretion of thyroid hormone production.
1. Thiomides - are the drug of choice used to decrease hormone production. It interferes with
synthesis of thyroid hormone. EXAMPLES: Propylthiouracil (RTU) ,Methimazole (Tapazole)
2. Lugol’s Solution – suppresses thyroid function for clients who have undergone surgery due to
Grave’s Disease.

4. Parathyroid Glands – secretes parathyroid hormones (PTH) which regulates calcium levels in the
blood. It increases calcium by:
a. mobilizing calcium from the bone.
b. promoting calcium absorption from the intestines.
c. promoting calcium reabsorption from the renal tubules.

CALCITONIN – is a hormone produced primarily by the thyroid glands and to lesser extent by the
parathyroid glands. It inhibits calcium reabsorption by the bone and increases renal excretion of
calcium.

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CALCITROL - is a vitamin analogue that promotes calcium absorption from the GIT and secretion of
calcium from bone to the blood.

5. Adrenal Glands - are paired glands consisting of the adrenal medulla and adrenal cortex.
Adrenal Cortex – produces two hormone or corticosteroids: GLUCOCORTICOIDS AND
MINERALOCORTICOIDS
Adrenal Gland Disorders:
A. Addison’s Disease – is a disorder due to decreased secretion or adrenal hyposecretion of
insufficiency.
B. Cushing’s Syndrome – is a disorder due to an increase in corticosteroid secretion or adrenal
hypersecretion.

DRUG THERAPY:

1. Glucocorticoids - are used to treat many diseases and health problems including inflammatory,
allergic and debilitating conditions.
a. Cortisol _ is the main glucocorticoid, has ana anti-inflammatory, anti-allergic and anti-stress effect.
b. Dexamethasone – is used for severe inflammatory response as a result of head trauma or allergic
ractions.
c. Prednisone – is an expensive glucocorticoid.
2. Glucocotricoid Inhibitors
a. Ketokonazole ( Nizoral) – is effective in treating clients with Cushing’s Syndrome and also ised as an
adjunct to surgery and radiation.
b. Mitotane (Lysedren) – is a n anti-neoplastic hormone antagonist.
c. Aminoglutethimide ( Cytadren) – inhibit glucocrticoid synthesis.
4. Mineralocorticoids – secretes aldosterone.

 ANTIDIABETIC AGENTS
- Are used primarily to control diabetes mellitus.
1. Insulin

2. Oral Anti –diabetic Drugs ( Oral Hypoglycemic Drugs)

A. First and Second Generation Sulfonylureas – are chemically related to sulfonamides but lacks
antibacterial activity. They stimulate beta cells to secrete more insulin. They increases insulin
cell receptors thus increasing the ability of the cells to bind insulin for glucose metabolism.
a. First Generation Sulfonylureas – could be short-acting, intermediate acting and long-
acting antidiabetics. EXAMPLE: Acetohexamide ( Dymelor).
b. Second Generation Sufonylureas – increases the tissue response to insulin and decrease
glucose production by the liver. They has a greater hypoglycemic potncy than first
generations. They has less displacement potential from protein binding sites or highly
protein-bound. EXAMPLES: Gliomepridine ( Amaryl); Glipizide ( Glucotrol)

B. Non-sulfoylureas – does not enhance insulin release and receptor interactions but affect the
hepatic and GI production of glucose.
a. Melformin ( Glucophage)- decreases hepatic production of glucose from stored fats. It
diminishes the increase in serum glucose following a meal. It decreases glucose

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absorption from the small intestines. it increases insulin receptor sensitivity and
peripheral glucose uptake at the cellular level.
b. Acarbose ( Precose) and Migitol ( Glycoset) – inhibit the digestive enzyme in the
small intestine responsible for the release of glucose from the complex carbohydrates
from the diet.
c. Meglitinides ; examples: Repaglinide ( Prandin) and Nateglinide ( Starlix) -
stimiulates beta cells to release insulin. Is used for type 2 diabetes and are short-acting.

Guidelines for Oral Antidiabetic Therapy ( Type 2- NIDDM)


1. Onset must be at age 40.
2. Diagnosis of diabetes for less than 5 years.
3. Normal weight or overweight.
4. FBS- equal to or less than 200 mg/d
5. Less than 40 “u” of insulin required per day.
6. Normal renal and hepatic functions.
C. Hyperglycemic Drugs

A. Glucagon – is a hyperglycemic hormone secreted by the alpha cells of the islets of


langerhans. It increases blood sugar by stimulating GLYCOGENOLYSIS in the liver. It protects
the body cells, especially those in the brain and retina, by providing the nutrients and
energy needed to maintain body function. It is used to treat insulin- induced hypoglycemia
when other methods of providing glucose are not available. It is available for parenteral
use. Recently, IV glucagon is used in the acute treatment of beta-blocker overdose and
profound shock.
B. Diazoxide ( Proglycem) – increases blood sugar by inhibiting insulin release from the beta
cells and stimulating release of epinephrine from the adrenal medulla.
D. Other Ant- Diabetics
A. Exenatide ( Byetta) – improves beta cell responsiveness improving glucose control in
people with NIDDM.
B. Pramlintide acetate ( Symlin) – for adults with type 1 and 2 Dm to improve postprandial
glucose control in diabetics who are using insulin but are unable to achieve or maintain
glucose control.

 CARDIOVASCULAR AGENTS

I. CARDIAC GLYCOSIDES, ANTI-ANGINALS, AND ANTI-DYSRRHYTMMICS

A. Cardiac Glycosides ( Digitalis Glycosides)- inhibits the Na-K pump; thus increasing intracellular
calcium causing the cardiac muscle fibers to contract.
Effect of Digitalis to the Heart:
a. A positive inotropic action.
b. A negative chronotropic action.
c. A negative dromotropic action
NOTE:
a. the increase in myocardial contractility increases cardiac, peripheral and kidney function
by:
 increasing cardiac output.

35 | P a g e
 Decreasing preload
 Improving blood flow to the periphery and kidneys.
 Decreasing edema.
 Increasing fluid excretion.
b. They are also used to correct atrial fibrillation and atrial flutter thru chronotropic effects
and negative dromotropic effects.
A. DIGOXIN (Lanoxin)- is a cardiac glycoside used to treat CHF, atrial tachycardia, flutter or
fibrillation. It inhibits the Na-K ATPase thus promoting increased force of cardiac contraction,
cardiac output and tissue perfusion. It decreases ventricular rate.
Digitalis Toxicity – occurs with overdosage or accumulation of diogoxin.
Note: Cardiotoxicity is a serious adverse reaction to digoxin leading to ventricular dysrrhythmias.

ANTIDOTE TO DIGITALIS TOXICITY:


1. Phenytoin and Lidocaine
2. Digoxin immune Fab ( Ovine, Digibind)

B. PHOSPHODIESTERASE INHIBITORS - is used to treat acute CHF or when there is no response to


the use of other agents. It inhib it’s the enzyme Phosphodiesterase promoting a positive inotropic
response.
C. OTHER AGENTS USED TO TREAT HEART FAILURE

1. Vasodilators – decrease venous blood return to the heart resulting to:


a. Decrease in cardiac filling.
b. Decreased ventricular stretching.
c. Decreased O2 demand.
Actions:
1. Reduces cardiac afterload increasing cardiac output.
2. Dilate arterioles of kidneys improving renal perfusion and increase fluid loss.
3. Improve circulation to the skeletal muscles.
2. Angiotensin-Converting Enzyme Inhibitors (ACE)- dilate venules and arterioles improving renal
blood flow decreasing blood volume.
3. Diuretics ( Thiazides, Furosemides) – are the first line drugs for reducing fluid volume
frequently prescribed with digoxin or other agents.
4. Spironolactone ( Aldactone ) – is a potassium-sparing diuretic used to treat moderate to severe
CHF. It improves heart rate variability and decreases myocardial fibrosis.
Note: Aldosterone secretions are increased in CHF promoting body loss of potassium and
magnesium needed by the heart.
5. Beta-blockers – are usually contraindicated for clients with heart failure because this drug class
reduces cardiac contractility; however, some have shown to improve cardiac performance.
Examples: Carvedilol ( Coreg), Metropolol tartrate ( Tropol – XL)
6. Nesiritide ( NAtrecor) – is an atrial natriuretic peptide hormone that inhibits anti-diuretic
hormone( ADH) by increasing Na loss. It isused in correcting CHF by promoting vasodilation,
ntriureis and dieresis. It is useful for treating clients who have acute decompensated CHF with
dyspnea at rest or who have dyspnea with little physical movement.
7. Bidil – is a combination of hydralazine and isosorbide.

B. Anti-Anginals– - are used to treat angina pectoris.

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1. Nitrates – cause generalalized vascular and coronary vasodilation, increasing blood flow
thru the coronary areties to myocardial cells.
a. Sublingual (SL) Nitroglycerin – is not swallowed because it undergoes first-pass effect
by the liver decreasing effectiveness. It is placedunder the ounge for faster absorption.
b. Isosorbide Dinitrate ( Isordil, Sorbitrate) – can be administered by SL by tablets and
orally by chewable tablets, immediate-release tablets, sustained release tablets and
capsules.
c. Isosorbide Mononitrate ( Monotel, Imdur)- can be given orally by immediate release
and sustained release tablets.
2. Beta-blockers - decrease he effects of the sympathetic nervous system by blocking the
action of the catecholamine epinephrine and norepinephrine, thereby decreasing HR and
BP. They are effective as an anti-anginals because by decreasing the HR and myocardial
contractility, the reduce need for O2 consumption and consequently, reduce angina pain.
Examples: Propanolol ( Inderal), Nadolol(Corgard), Pindolol( Visken),
Atenolol(Tenormin), Metropolol( Lopresor, Toprol-XL)
3. Calcium Channel Blockers/ Calcium Blockers
Actions:
a. Decrease cardiac contractility.
b. Decrease afterload.
c. Decrease peripheral resistance
d. Reduce workload of the heart.
e. Decrease the need for O2.
Examples: Amlodipine ( Norvasc), Bepridil HCl (Vascor), Diltiazem HCl( Cardizem),
Felodipine ( Plendil), Isradipine ( Dynaciro)
C. Antidysrhythmics–are used to restore the cardiac rhythm to normal.
1. Fast (Na) Channel Blockers – decrease the fast Na influx to the cardiac cells.
Subgroups:
a. I-A– slows conduction and prolongs repolarization.
b. I-B- slows conduction and shortens repolarization.
c. I-C- prolongs conduction with little to no effect to repolarization.
2. Beta-blockers – decrease conduction velocity, automaticity and recovery time.
3. Prolong Repolarization – are used in the emergency treatment of ventricular
dysrhythmias when other antidysrhythmias are ineffective. They increase the refractory
period and prolong the action potential duration.
Examples: Bretylium ( Bretylol), Amiodarone ( Cordarone)
4. Slow Calcium Channel Blockers – blocks calcium influx thereby decreasing the excitability
and contractility of the myocardium. It increases the refractory period of th AV node
which decreases ventricular response.
Examples: Verapamil ( Calan, Isoptin) , Diltiazem ( Cardizem)

II. DIURETICS – produce increased urine flow by inhibiting Na and water reabsorption from the
kidney tubules. It is used to decrease HPN and peripheral and pulmonary edema.
5 Categories:
1. Thiazide and thiazide-like Diuretics- acts on the disatal convoluted renal tubule beyond
the loop of Henle tho promote Na, Cl and H2O excretion. They are used to treat HPN
and peripheral edema and are primarily used for clients with normal renal function. It
causes a loss of Na, K, and magnesium but promots calcium absorption. It affects

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glucose tolerance, thus hyperglycemia can occur. Note: It is not effective for immediate
diuresis.
Examples: Chlorthiazide ( Diuril) , Indapamine ( Lozol)
2. Loop ( High-Ceiling) Diuretics – acts on the ascending loop of Henle by inhbiting chloride
transport of Na into the circulation. It can affect blood sugar and incease th uric acid
level. It is called “high-ceiling” because the effect is dose related.
Examples: Ethacrynic Acid ( Edecrin), Furosemide ( Lasix), Bumetanide ( Bumex)
3. Osmotic Diuretics – increase the osmolality of the plasma and fluids in the renal
tubules. It is used to decrease intracranial pressure, prevent renal failure and decrease
intraocular pressure.
Examples: Mannitol, Ureaphil
4. Carbonic Anhydrase Inhibitors – blocks the action of the enzyme carbonic anhydrase. It
is used primarily to decrease intraocular pressure (IOP) in clients with open-angle
glaucoma. It is also used for dieresis, management of epilepsy and treatment of high
altitude or acute mountain sickness.
5. Potassium- Sparing Diuretics- are used as mild diuretics or in combination with another
diuretic. It acts primarily on the collecting duct renal tubules to promote Na and water
retention.
Examples: Spironolactone ( Aldactone) , Triamterene( Dyrenium) Amiloride ( Midamor)

III. ANTI-HYPERTENSIVES
1. Diuretics – promote Na depletion which decreasesd extracellular fluid volume( ECFV)
they are effective as first-line drugs for treating mild HPN.
Example: Hydrochlorthiazide ( Hydrodiuril)
2. Sympatholytics ( Sympathetic Depressants)
a. Beta-adrenergic blockers c. alpha adrenergic blockers
b. Centrally acting alpha agonists d. adrenergic neuron blockers
3. Direct- Acting Arteiolar Vasodilators- act by relaxing the smooth muscles of the blood
vessels causing vasodilation. It promotes an increase in blood flow to the kidneys and
brain. With vasodilation, BP decreases and Na and water are rtained resulting peripheral
eema, reflex tachycardia is caused by the vasodialtors and decrease in BP.
Examples: Hydralazine, Minoxidil
4. Angiotensin Antagonist( angiotensin- converting enzyme [ACE] Inhibitors) – inhibits
ACE which in turn inhibits the formation of Anhiotensin II and blocks the relase of
aldosterone.
Examples: Captopril ( Capoten), Benazepril( Lotensin), Enalapril maleate ( Vasotec),
Fosinapril( Monopril) Lisinopril ( Prinivil, Zestril), Moexipril ( Univasc) Perindopril
( Aceon), Quinapril ( Accupril) , Ramipril ( Altace) , Trandopril( Mavik)
5. Angiotensin II receptor Antagonists ( A-II blockers or ARB) – is similar to ACE inhibitors
in that they prevent the release of the aldosterone. It acts on the rennin-angiotensin
system.
Examples: Lorasartan ( Cozaar), Valsartan( Diovan), Irbesartan( Avapro), Candesartan
cilexetil ( Atacand)
6. Cacium Channel Blockers ( Calcium Antagonists) – decrease calcium levels and
promote vasodilation. They are highly protein-bound and have a short halflife.
Examples: Verapamil ( Calan), Nifedipine ( Procardia), Amlodipine ( Norvasc)

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IV. ANTI-COAGULANTS, ANTI-PLATELETS AND THROMBOLYTICS
A. Anti-coagulants – are used to inhibit clot formation, but do not dissolve clots that have
already formed.
1. Heparin – is a natural substance in the liver that prevents clot formation. It is used
in open heart surgery to prevent blood from clotting and in the critically ill clients
with DIC. It is primarily used to prevent venous thrombosis, which can lead to
pulmonary embolism or stroke. It is not given orally because it is poorly absorbed
in the GIT and is destroyed by heparinase, an enzyme in the liver.
2. Oral Anticoagulants – inhibit hepatic synthesis of vit K, thus affecting the clotting
factors II, VII, IX and X. They are used primarily to prevent thromboembolic
conditions and to prolong clotting time.
Examples: Warfarin (Coumadin), Dicumarol, Anisindione ( Miradon) ,.
Parenteral Anticoagulants : Argatroban( Acova), Bivalirudin ( Angiomax), Lepirudin
( Rufludan)
Filmtabletten ( Exantha)- was recently dvloped to decrease the risk of blood clots
and stroke. it is used for clients with bleeding problems related to warfarin.
Vit. K1 (Phytonadione) – is the antidote for warfarin overdose or uncontrollable
bleeding. If bleeding is not controlled, fresh whole blood or fresh frozen plasma or
platelets are generally are given.
B. Anti-Platelet Drugs- are used to prevent thrombosis in arteries by suppressing platelet
aggregation. They are used mainly for prophylactic use:
a. Prevention of myocardial infarction or stroke for clients with familial history.
b. Prevention of a repeat MI or stroke.
c. Prevention of stroke in clients having transient attacks.
Examples: Aspirin, Cilostazol (Pletal), Clopidogrel( Plavix), Dipyradamole (Persantine)
C. Thrombolytics- are used ti promote Fibrinolytic Mechanism. ( the conversion of
plasminogen to plasmin, which destroys the fibrin in the blood clots.)
Note:
1. The thrombus or blood clots disintegrate when a thrombolytic drug is administered
within 4-6 hours after an acute MI.
2. The need for a cariac bypass or coronary angioplasty can be evaluated soon after
thrombolytic treatment.
3. It should be administered within 3 hours of thrombolytic stroke.
4. They are also used for pulmonary embolism, non-coronary arterial occlusion from
an acute thromboembolism amd thrombolic stroke.
Examples: Streptokinase, Urokinase, Tissue Plasminogen Activator ( TPA,Alteptase),
Anisoylated Plasminogen Streptokinase Activator Complex ( APSAC) Reteplase
( Retavase), Tenecleptase ( TNkase)

V. Anti-Lipidemics and Peripheral Vasodilators

A. Anti-Lipidemics – lower abnormal lipid levels.

Types:
1. Cholestyramine ( Questran) – is a rsin that binds with bile acids in the intestines. It
comes In a gritty powder which is mixed thoroughly in water or juice.

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2. Colestipol (Colestid) – is a resin antilipidemic similar to cholestyramine. It lowers
cholesterol level.
3. Clofibrate ( Atromid-S)}- are highly protein bound and should not be taken with an
4. Gemfibrozil (Lopid) } anticoagulant.
5. Statins are also called HMGCoA Reductase Inhibitors. It inhibits cholesterol
synthesis in the liver decreasing the concentration of cholesterol and decreases the
LDL and slightly increasing HDL. Note: reduction is seen in 2 weeks.
Examples: Atrovastatin Ca ( Lipitor), Fluvastatin ( Lescol), Lovastatin ( Mevacor),
Pravastatin Na ( Pravachol), Simvastatin ( Zocor), Rosuvastatin Na ( Crestor)
B. Peripheral Vasodilators – increase blood flow to the extremities. They are used in
peripheral vascular disorders of venous and arterial vessels.
Examples: Tolazoline ( Priscoline), Isoxsuprine ( Vasodilan), Nicotinyl alcohol,
Papaverine( Cerespan, Genabid), Prazosin( Minipres), Nifedipine ( Procardia),
Pentoxifylline (Trental)

 DRUGS ACTING ON THE RESPIRATORY SYSTEM

I. DRUGS FOR THE COMMON UPPER RESPIRATORY TRACT DISORDERS ( URI’s)

A. Anti-Histamines ( H1 blockers or H1 Antagonists) – compete with histamine for receptor sites


thus preventing histamine response. They decrease nasopharyngeal secretions by blocking H1
receptor sites. They are rapidly absorbed in 15 minutes; but is not fit for anaphylaxis.
1. First Generation Antihistamines –causes drowsiness, dry mouth and other anticholinergic
symptoms.
Example: Diphenhydramine ( Benadryl)
2. Second Generation Antihistamines- causes fewer anticholinergic effects.
Example: Cetrizine ( Zyrtec), Fexofenadine ( Allegra), Loratadine ( Claritin), Azelastatine
( Astelin, Optivar)

B. Nasal and Systemic Decongestants ( Sympathomimetic Amines)- stimulate the alpha adrenergic
receptors, thus producing vasoconstriction of the capillaries within the nasal mucosa. They are
primarily administered by nasal spray or drops,or in tablet , capsule or liquid form. They are used
primarily for allergic rhinitis, including hay fever and acute coryza .
Examples: Ephedrine, Phenylephrine ( Neo- Synephrine), Pseudoephedrine ( Sudafed)
C. Intranasal Glucocorticoids or Steroids – are effective for treating allergic rhinitis. Because they
are steroids, they have anti-inflammatory effect, thus decreasing the allergic rhinitis symptoms or
rhinorrhea, sneezing and congestion. It maybe used alone or in combination with H1
antihistamine.
Examples: Beclomethasone ( Beconase, Vancenase, Vanceril), Budesonide ( Rhinocort),
Dexamethasone (Decadron), Flunisolide(NAsalide), Fluticasone( Flonase), Triamcilone ( Nasacort)
D. Antitussives – act on the cough control center in the medulla to suppress the cough reflex. It is
used only if the cough is non-productive and irritating that causes a sore throat. Note: A cough
is a protective mechanism that clears the airway of secretions or any collected material.
Example: Dextromethorphan ( Robitussin)
E. Expectorants – loosen bronchial secretions so they can be eliminated by coughing. It can be used
with or without other pharmacologic agents.
Example: Guaifenesin

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II. DRUGS FOR ACUTE AND CHRONIC LOWER RESPIRATORY DISORDERS
1. Sympathomimetics: Alp[ha & Beta 2 Adrenergic Agonists
a. Albuterol – is effective for treatment and control of asthma by causing bronchodilation
with long duration of action.
b. Metaproterenol – can be administered orally or by inhalation with a metered dose
inhaler or a nebulizer; but is frequently administered by inhalation.
c. Isoproterenol ( Isuprel) – is used for bronchospasms.
d. Aerosol Inhaler
2. Anticholinergics
a. Ipratropium bromide (Atrovent) – treat asthmatic conditions by dialting the bronchioles.
b. Combivent (Ipratropium bromide + Albuterol So4) – treat chronic bronchitis.
3. Methylxanthine (Xanthine) Derivatives – is used to treat asthma. They stimulate the CNS and
respiration, dilate coronary and pulmonary vessels and cause dieresis.
a. Theophylline – relaxes smooth muscles of the bronchi and bronchioles.
b. Aminophylline
c. Caffeine
4. Leukotriene Receptor Antagonists and Synthesis Inhibitors (LT)- is a chemical mediator that
can cause inflammatory changes in the lungs. They are used for exercise induced asthma.
Examples: Zafirlukast ( Accolate), Zileuton ( Zyflo), Montelukast( Singulair) - reduces the
inflammatory process and decreae bronchoconstriction.
5. Cromolyn and Nedocromil
Example: Cromolyn Na – is used for prophylactic treatment of bronchial asthma and therefore
must be taken daily.
6. Mucolytics – act like detergents by liquefying and loosening thick mucus secretions so they can
be expectorated.
7. Antimicrobials – are used only if an infection results from retained mucus secretions.

 DRUGS FOR URINARY TRACT DISORDERS

I. Urinary Antiseptics/ anti-infectives and Antibiotics – are limited for treatment of UTI’s. the
action occurs in the renal tubules and bladder and thus is effective in reducing bacterial growth.
1. Nitrofurantoin ( Furalan, Macrodantin) is the bacteriostatic and bactericidal depending on
the dosage. It is effective against many gram positive and gram negative bacteria esp. E.
coli.
2. Methanamine ( Hiprex, Mandelamine)- produces bacterial effect whn the urine pH is less
than 5.5.
3. Trimethoprim (Proloprim, Trimpex) and Trimethoprim- Sulfamethoxazole – is used for the
treatment and prevention of acute and chronic UTI.
4.Flouroquinolones ( Quinolones) are effective against lower UTI’s.
Example: Nalidixic Acid ( Negram) , Norfloxacin ( Noroxin) Ciprofloxacin HCl ( Cipro),
Ofloxacin, lomefloxacin
II. Urinary Analgesics
Phenazopyridine HCl (Pyridium) – is used to relieve pain, burning sensation and the urgency
and frequency of ueriantion that are symptomatic of lower UTI.
III. Urinary Anti-Spasmodics/ Antimuscarinics -treats urinary spasms resulting fro infection or
injury.
Examples: Oxybutin( Ditropan), Flavoxate ( Urispus)

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 REPRODUCTIVE AND GENDER-RELATED AGENTS

I. Drugs Associated with the Female Reproductive Cycle I: Pregnancy and Preterm Labor
A. Tocolytic Therapy – is used to decrease uterine contractions. Examples: Terbutaline ( Brethrine),
MgSO4
Goals:
a. To interrupt or onhibit uterine contractions to create4 additional time for the utero-fetal
maturation.
b. To delay delivery so antenatal cortoecosteroids can be delivered to facilitate lung
maturation.
c. To allow safe transport of the mother to an appropriate facility.
B. Corticosteroid Therapy – accelerates lung maturation with resultant surfactant development in
the fetus in utero, thereby decreasing the incidence and severity if Respiratory Distress Syndrome
(RDS) with increased survival of preterm infants.
Examples: Bethamethasone ( Celestone), Dexamethasone
C. Drugs for PIH
a. Methyldopa ( Aldomet ) e.
Prazosine
b. Hydralazine ( Apresoline) f.
Nifedipine
c. Labetalol ( Trandate) g,
Clonidine
d. Betablockers

II. Drugs Associated with the Female Reproductive Cycle II: Labor, Delivery and the Preterm
Neonate

A. Analgesia
1. Sedative- Tranquilizer Drugs – promote rest and relaxation and decrease fear and anxiety,
but they do not provide pain relief.
Examples: Secobarbital Na ( Seconal), Pentobarbital Na( Nembutal) Promethazine
(Phenergan)
2. Narcotic Agonists – interfers with pain impulses at the subcortical level of the brain.
Examples: Morphine SO4, Meperidine HCl( Demerol), Fentanyl ( Sublimaze)
3. Mixed Narcotic Agonist-Antagonist – exert their effect at more than one site, often an agonist
at one side and an antagonist at the other.
Examples: BUtorphanol tartrate ( Stadol), Nalbuphine HCl ( Nubain)

B. Anesthesia (Regional and General)

Regional Anesthesia – achievs pain relief during labor and delivery without loss of consciousness.
Injected local anesthetics temporarily block conduction of pain impulses along sensory nerve pathways
to the brain.

1. Local Infiltration - can be used for performing and repairing episiotomies as well as
lacerations.

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2. Pudendal Block – blocks stimulus along pudendal nerve. It is given transvaginally behind each
sacrospinous ligament to block pudendal nerves.
3. Paracervial Block - is the transvaginal injection of an anestheric solution on each side of the
cervix.
4. Subarachnoid Block/ Spinal Anesthesia/ Spinal Block – provokes a painless delivery and does
not interfere with uterine contractions.

C. Drugs that Enhance Uterine Muscle Contractility

1. Oxytocin – is used for labor induction and augmentation. It facilitates smooth muscle
contraction in the uterus in a client with inadequate uterine contractility.
2. Ergot Alkaloids – act by smooth muscle cell receptor stimulation. They are used after delivery
for the prevention or control of postpartum hemorrhage and promotion of uterine involution.
Examples: Ergonovine Maleate ( Ergotrate), Methylergonovine maleate
( Methergine)
D. Surfactant Therapy in Preterm Birth
Synthetic Surfactant – is used to prevent Respiratory Distress Syndrome (RDS); to
maintain distention of alveoli sacs.
Examples: Beractant ( Survanta), Calfactant ( Infasurf), Poractant alfa ( Curosurf)

III. Drugs Associated with the Postpartum and the Newborn

Nurses’ Role in Postpartal Therapy:


1. To asses and provide postpartal physical changes and pain management with the client to
determine both healing progress within a standard and effectiveness of medications.
2. To teach the client and administer postpartal medications.
3. To teach the client and administer narcotic analgesics prescribed when pain control by
narcotic products is ineffective.
A. Pain Relief for Uterine Contraction: ibuprofen, Motrin, Ketorolac
B. Pain Relief for Perineal Wounds and Hemorrhoids: Hazel, NUprecainal ointment
C. Promotion of Bowel Function: Docusate Na ( Colace), Bicasodyl suppositories ( Dulcolax),
Magnesium hydroxide ( Milk og Magnesia), Senna( Senokot), Mineral Oil.
D. Immunizations of the mother:
a. Rho(D) Immune Globulin: Rhogam, RhoD
b. Rubella Vaccines- if a non-immunized contracts the virus during the first trimester, a high
rate of abortion and neurologic developmental sequale associated with congenital rubella
syndrome.
E. Drugs administered to the Newborn after delivery:
a. Erythromycin ophthalmic ointment - to provide prophylaxis against eye infections.
b. Vit. K – to prevent hemorrhagic disease of the newborn.
c. Anti-infectives
d. Immunization before discharge

 NUTRITIONAL SUPPORT

ROUTES OF ADMINISTRATION:
1. Enteral Nutrition ( NGT, OGT)- involves the GIT, can be given orally or by feeding tubes.
Nursing Responsibilities:

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a. Be sure that there is adequate small bowel function with digestion, absorption and GI
motility.
b. Assess for abdominal distention and decrease or absence of bowel sounds.
c. This method is used only for clients with intact gastric emptying time and decreased risk
of aspiration.
Components:
a. Carbohydrates in the form of dextrose, sucrose, lactose, starch or dextrin.
b. Protein in the form of intact proteins, hydrolyzed proteins or free amino acids.
c. Fat in the form of corn oil or soybean oil.
2. Enteral Medication: Precreatin ( Creon), Pancrelipase ( Viokase)
3. Total Parenteral Nutrition (TPN) or IV Hyperalimantation (IVH) – is the primary method
For providing complete nutrients by the parenteral or IV route.
Note: enteral nutrition should be considered before TPN.
 DRUG AND ALCOHOL ABUSE

I. Drug Abuse and Dependence


Drug Abuse – involves a persistent and excessive , non-medical or nonprescription use of chemical
substances.
Drug Dependence – is a complex phenomenon involving social, personal and pharmacological factors.
Types of Drug Dependence:
1. Narcotic Drug Dependence (Heroin, Morphine)
Treatment:
a. Methadone therapy
b. Naloxone
c. Complete abstinence
2. Barbiturate Drug Dependence – although barbiturates maybe used for inducing sleep over a period
of time without causing more than habituation, they also cause addiction.
Signs and Symptoms of addiction:
a. Drowsiness e. nystagmus
b. Poor judgment f. tremors
c. Emotional lability g. staggering gait
d. Slurred speech
Withdrawal Syndromes:
a. Apprehension f. disturbances in cardiovascular function
b. Weakness g. tremulousness
c. Anorexia h. insomnia
d. Nausea i. major motor convulsions
e. Vomiting j. delirium
Treatment:
a. Hospitalization
b. Psychotherapy
3. Sedative- Hypnotic Abuse ( Methaqualone, Meprobamate, Gluthethimide, Ethinamide)
4. Drug Dependence with CNS Stimulants ( Amphetamines, Cocaine)
5. Drug Dependence with Hallucinogen types:
a. LSD ( Lysergic acid diethylamide)- is usually taken orally as a tablet. It is a crystalline
powder or a liquid that can be deposited on sugar cubes, cookies or other foods.
b. Mescaline – is usually ingested orally, has a bitter taste. It increases sensory
awareness, visual imagery, anxiety, nausea and impaired coordination.

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c. Psilocybin – obtained from certain mushrooms fro Central America; same effects
with Mescaline.
d. DMT (Dimethyltryptamine)- obtained from a certain plant found in the West Indies.
Same effect with LSD.
e. STP ( Dimethoxamphetamine)- is a synthetic amphetamine; more powerful and
longer acting than LSD.
f. Marijuana
g. Metamphetamine HCl

APPROACHES TO THE DRUG ABUSE PROBLEMS:


1. Prevent its occurrence thru proper education.
2. Alleviate social and economic factors that are associat4ed with drug abuse.
3. Rehabilitation.
4. Avoid injudicious use of PRN narcotics, hypnotics, sedatives and other dependence-producing
agents.
5. Nursing interventions should be directed towards providing each patient confort and support so
that the need for drugs can be reduced or eliminated.
6. Careful destruction of used syringes and needles to prevent re-use.

II. ALCOHOL USE AND ABUSE


Beneficial Effects of Alcohol:
1. Increase HDL in the blood.
2. Decrease risk of Coronary Artery Disease (CAD)
Harmful Effects:
1. CNs depression removes inhibition producing euphoria.
2. Impairment of the ability to perform fine motor movements.
3. It dulls memory, discrimination, insight and concentration.
4. Unconsciousness.
5. Decreased blood sugar.
6. Nausea
7. Vomiting
8. Dizziness
9. Gastric irritation
Note: drug and alcohol abuse and dependence are not related merely to a few, specific, chemical
compounds; but a wide variety of substances are involved.

TOXICOLOGY- - is a branch of medicine that deals with the nature, properties, effects and detection of
poisons.

Types of Poisonig:

1. Acute Poisoning – occurs exposure to the noxious substance is sudden and severe. Symptoms
develop in a short period of time and death may follow rapidly. It is usually caused by a single
dose of a substance that is readily absorbed and has the ability to damage one or more vital
body processes. Recovery from acute poisoning maybe followed by later development of serious
symptoms.
2. Sub-acute Poisoning – result from the frequent exposure to a poison over a period of several
hours or days.

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3. Chronic Poisoning – occurs from repeated exposure over a long period of time of a substance
that has tendency to accumulate in the body.

General Action Of Poisons:


1. Local - irritation or destruction of tissues.
2. Systemic – absorbed into the blood into the target tissues.
3.
Emergency Treatment:
1. Call a physician or poison control immediately.
2. Attempt to identify the poison.
3. Implement first aid measures:
a. Delay absorption by oral ingestion of milk, egg whites or charcoal.
b. Induce emesis with ipecacx syrup. Tepid salt water, soapsud solution or simply touching the
back of the throat with a finger.
4. Effect chemical alterations of the ingested substance by administering a weak alkali such as milk
of magnesia for acidic substances; or vinegar if alkaline substance have been ingested.
5. Give specific antidotes.
6. Provide supportive care.
a. Maintain normal body temperature.
b. Give artificial respiration when required

 DRUG NAME ENDINGS

- caine Local anesthetics


-cillin Antibiotics
-mycin/micin
-dine Anti ulcer agent
-done Opiod Analgesic
-ide Oral Hypogylcemics

-lam Antianxiety
-pam
-mide Dieuretics
-zide
-olol Beta Blockers
-pril ACE inhibitors

-sone Steroids

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CHAPTER 4: APPROPRIATE COMMUNICATION TECHNIQUES ON THE PHARMACODYNAMICS/
PHARMACOKINETICS OF SPECIFIED DRUGS PRESCRIBE TO CLIENTS

DRUG ADMINISTRATION THROUGHOUT THE LIFE SPAN

Important Considerations:
1. Healthcare providers must understand normal growth and development patterns to provide
optimum care.
2. The development of a person is a complex process interweaving the biophysical
with the biopsychosocial, ethnocultural and spiritual components to make each individual a unique
human being.
A. DRUG ADMINISTRATION DURING PREGNANCY AND LACTATION
1. The focus must be to eliminate potentially toxic agents that may harm the mother or
the unborn child.
2. During all stages of pregnancy, the nurse should help the mother to assess all
medications or dietary supplements to determine if they are necessary.
3. Memorize the drug pregnancy categories for medications commonly prescribed for
their patients.
FDA PREGNANCY CATEGORIES:

CATEGORY A – have not shown an increased risk of fetal abnormalities. E.g. FeSo4
CATEGORY B - no evidence of harm to the fetus of animals based on animal study; but no adequate,
well-controlled studies in pregnant women. E.g. Cefaclor
CATEGORY C - animal studies have shown an adverse effect and there are no adequate, well-
controlled studies in pregnant women. E.g. Nifedipine
CATEGORY D – studies demonstrated risk to the fetus, however, the benefits of therapy may outweigh
the potential risk. E.g. Alprazolam, Diazepam
CATEGORY X – studies have demonstrated positive evidence of fetal abnormalities. The use of this
product is contraindicated in women who are or may become pregnant.
B. DRUG ADMINISTRATION DURING INFANCY( 0 -12 months)
1. Pharmacotherapy is directed towards:
a. Safety of the infant.
b. Proper disposing of prescribed drugs.
c. Teaching parents how to administer medications properly.
2. Oral medications should be administered slowly to avoid aspiration.
3. For rectal suppositories, the buttocks should be held together for 5 -10 minutes.
4. The vastus lateralis is the preferred site for IM injections.
5. The gluteal site is contraindicated because of the potential damage to the sciatic nerves.
6. Medications are often prescribed in mg/kg/day rather than according to the baby’s age in weeks
or in months.
7. Because the liver and kidneys of infants are immature, drugs will have a greater impact due to
the prolonged duration of action.
8. Consider age and size in determining safe dosages of medications for infants.
C. PHARMACOLOGY OF TODDLERS ( 1 – 3 Years)
Note : the child is curious and begins to explore and tends to put everything in the mouth.

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1. Teach parents that poisons come out in all shapes, sizes and forms and includes medications.
2. Oral medications that taste bad should be mixed with a vehicle such as jam, syrup or fruit juice if
possible.
3. IM injections for toddlers maybe given into the vastus lateralis.
4. IV injections may use scalp or feet veins.
5. Suppositories maybe difficult to administer due to the resistance of the child. Having a parent in
close proximity will usually reduce the toddler’s anxiety and increase cooperation.

D. PHARAMCOTHERAPY OF PRE-SCHOOLERS ( 3-5 YEARS) AND SCHOOL-AGE CHILDREN(6-12


YEARS)
1. They may cooperate in taking oral medications if they are crushed or mixed with food or other
flavored beverages.
2. IM injections are given at the dorsogluteal muscle after a child is walking for about a year.
3. Peripheral veins are used for IV injections.
4. Explain procedure to gain trust.
5. School age children may take chewable tablets and swallow tablets or capsules.
6. Administer parenteral medications quickly and compassionately.

E. PHARMACOLOGY OF ADOLESCENTS (13 – 16 YEARS)


1. There is an increased need for contraceptive information and counseling with sexually related
health problems.
2. Educate them about the hazards of tobacco use and illicit drugs.
3. The adolescent has a need for privacy and control in drug administration.
4. Explain the importance of medications and their adverse effects.
5. Be sensitive to their need for self-expression, privacy and individuality, particularly when
parents, siblings or friends are present.

F. PHARAMCOTHERAPY FOR ADULTS


1. The health status of younger adults (18-40 years) is generally good; absorption, metabolic
excretion mechanisms are at their peak.
2. There is minimal need for prescription drugs unless chronic diseases such as diabetes or immune
related conditions exist.
3. The use of vitamins. Minerals and herbal remedies are prevalent.
4. Medication compliance is positive as there is clear comprehension of benefit in terms of
longevity and feeling well.

G. PHARMACOLOGY FOR THE ELDERLY


Changes that affects pharmacotherapy in the elderly:
1. Increased pH and decreased peristaltic rate affects medication absorption.
2. The liver’s production of enzymes decreases, resulting in reduced hepatic drug metabolism.
3. The aging liver reduces albumin production, resulting to decreased plasma protein binding and
increased levels of free drug in the bloodstream, thus increasing the potential for drug-to-drug
interaction.
4. Reduced blood flow to the kidneys and decreased nephron function reduce drug elimination,
which increases serum drug levels and the potential for toxicity.
5. The percentage of body water decreases, making the effects of dehydration more dramatic.

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a. Risk for toxicity is boosted by fluid deficit.
b. Elderly patients who have reduced body fluids experience more orthostatic hypotension.
6. The ratio of body fat to water increased, enhancing storage of fat-soluble drugs and vitamins.
7. The aging cardiovascular system has decreased cardiac output and less efficient blood
circulation which slows drug absorption.
NOTE: Immune function diminishes with aging, so autoimmune diseases and infections occur more
frequently in elderly patients.

CHAPTER 6: CURRENT TRENDS AND CLINICAL ALERTS IN NURSING PHARMACOLOGY

MEDICATION ERRORS AND RISK REDUCTION

____________________________________
- Is any preventable event that may cause or lead to inappropriate medication use or patient
harm while the medication is in control of the health care professional, patient or consumer.
- It impedes pharmacotherapeutic outcomes and can cause serious illness or death.
- It can lead to litigation against the nurse, physician or health care agency.

Factors Leading to Medication Error:


1. Omission of the ten rights of drug administration; especially the first five.
2. Failure to perform a system check within an agency.
3. Failure to take into account patient variables, such as recent changes in renal or hepatic
function.
4. Giving medications based on verbal or telephone orders or at bedside that maybe
misinterpreted or undocumented.
5. Giving medications on incomplete orders, or an illegible order, where the nurse is unsure of the
correct drug, dosage or administration.
6. Increase in the number of drugs in th4 market.
7. Lack of drug knowledge, memory lapses, transcription of orders, dispensing of drugs or delivery
problems.
8. Inadequate monitoring of staff.
9. Distraction of staff while preparing the drug.
10. Overworked staff.
11. Lack of standardization.
12. Confusing packaging prescription.
13. Equipment failures.
14. Inadequate client history.
15. Poor interdepartmental coordination.

A Medication Error May Involve One or More of the Following:


1. Administration of the wrong medication or IVF.
2. The incorrect dose or rate.
3. Administration to the wrong client.
4. Incorrect route and schedule interval.

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5. Administration of allergic drug or IVF.
6. Omission of dose or discontinuation of medication or iVF that was nor discontinued.

REDUCING MEDICATION ERRORS:

1. Bar Coding – proposed by the Food and Drug Administration (FDA) in 2002; which uniquely
identifies the drug, its strength and dosage form.
2. Computerized Prescriber Order Entry (CPOE) - is a system under bar coding which interacts with
the laboratory, pharmacy and client data.

NURSES’ RESPONSIBILITIES IN REDUCING MEDICATION ERRORS:

I. ASSESSMENT
1. Ask the patient about allergies to food and medications, current health concerns, use of OTC
drugs and herbal supplements.
2. Ensure that the patient is receiving the right dose at the right time and by the right route.
3. Assess renal and liver function and for impairments of other body systems that may have an
impact on pharmacotherapy.
II. PLANNING
1. Have the patient state the prescribed outcome of the medication, including the right time to
take the medication and the right dose.
III. IMPLEMENTATION
1. Advise the client to take the medication as prescribed and to question the nurse if medications
“look different”.
2. Use drug references regularly.
3. Contact healthcare provider; do not guess about the order. DOCUMENT CLARIFICATION.
4. Double check all calculated dose.
5. Use leading zero (0.5); do not use trailing zero (5.0).
6. Avoid verbal orders; if needed, repeat it aloud to confirm.
7. Scan bar code at point of care.
8. Include pharmacist on client rounds.
9. Use a computerized order entry (CPOE).
10. Avoid dangerous abbreviations. e.g HCT – is it hydrocortisone or hydrochlorthiazide?
Note: always think critically.
IV. EVALUATION
1. Assess whether the expected outcomes of pharmacotherapy have been achieved and whether
the patient encountered adverse reactions.

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