Chapter 17: Pharmacology2 · Chapter 71:Pharmacology2 - 3 - Civil defense college Chapter 13:...

Chapter 71:Pharmacology2

Civil defense college - 1 -

EMT- PARAMEDIC Pharmacology 2



Moby's paramedic textbook

Brief content Section Three: Drugs That Affect the Nervous System } 3-14 {

Section Four: Drugs That Affect the Cardiovascular System} 15-20{

Section Five: Drugs That Affect the Blood } 21-23 {

Section Six : Drugs That Affect the Respiratory System } 24-22 {

Section Seven: Drugs That Affect the Gastrointestinal System } 22-31{

Section Eight: DRUGS That Affect The Eye And Ear } 32-33 {

Section Nine: Drugs That Affect the Endocrine System } 34-35{

Section Ten: Drugs That Affect the Reproductive System } 36-33 {

Section Eleven: Drugs Used in Neo-plastic Diseases } 32 {

Section Twelve: Drugs Used in Infectious Disease and Inflammation

}32-42{

Section Thirteen: Drugs That Affect the Immunologic System } 43{



Chapter 13: Pharmacology2

Section Three

Drugs That Affect the Nervous System

DRUGS THAT AFFECT THE AUTONOMIC NERVOUS SYSTEM 7. The nervous and endocrine systems are the major means of controlling and integrating body

functions

2. Common characteristics include the following:

a. High-level integration in the brain

b. Ability to influence processes in distant regions of the body

c. Extensive use of negative feedback mechanisms

3. Major difference between the two systems is in the mode of transmission of information

a. Endocrine system transmission is primarily chemical via blood-borne

hormones , The hormones are not targeted for a particular organ but instead diffusely affect

many cells and organs concurrently

b. The nervous system primarily relies on rapid electrical transmission of information over

nerve fibers

7) Chemical impulses only carry signals between nerve cells and their effector cells in a

very localized manner; perhaps affecting only a few cells

4. Classifications a. Autonomic drugs mimic or block the effects of the sympathetic and parasympathetic

divisions of the autonomic nervous system

These drugs can be classified into four groups: 1) Cholinergic (parasympathomimetic): drugs that mimic the actions of the

parasympathetic nervous system

2) Cholinergic blocking (parasympatholytic): drugs that block the actions of the

parasympathetic nervous system

3) Adrenergic (sympathomimetic): drugs that mimic the actions of the sympathetic

nervous system or the adrenal medulla

4) Adrenergic blocking (sympatholytic): drugs that block the actions of the sympathetic

nervous system or adrenal medulla

1. Cholinergic drugs 7) Acetylcholine has two major effects on the nervous system:

a) It has a stimulant effect on the ganglia, adrenal medulla, and skeletal muscle (the

Nicotinic effect of acetylcholine)

b) It also has stimulant effects at postganglionic nerve endings in cardiac muscle,

smooth muscle, and glands (the muscarinic effect of acetylcholine)

2) Cholinergic drugs act

*directly (choline esters) by combining with cholinergic receptors in postsynaptic

membranes or

*indirectly by inhibiting the enzyme that normally degrades acetylcholine

a) This inhibition results in the accumulation of acetylcholine, which causes a prolonged

and intensified response at various effector sites

3) Cholinergic drugs have little therapeutic value and generally are not considered

emergency medications

a) A major exception to this is physostigmine (Antilirium), an indirect-acting

cholinergic drug



b) May be used to manage extreme cases of poisoning resulting from atropine-type

drugs

2- Cholinergic blocking (anticholinergic)

agents are widely used in emergency medicine

a) These agents work by blocking the muscarinic effects of acetylcholine, thereby

decreasing acetylcholine’s effects on its effector organ

b) Atropine, the best-known cholinergic blocking drug, is a competitive antagonist

(7) Works by occupying muscarinic receptor sites, thereby preventing or reducing the

muscarinic response to acetylcholine

(2) Large doses of atropine do the following:

(a) Dilate the pupils

(b) Inhibit accommodation of the eyes

(c) Increase heart rate

3-Adrenergic drugs 7) Adrenergic drugs are designed to produce activities like those of neurotransmitters

2) Three types of agents: (a)direct-acting, (b)indirect-acting, and (c)dual-acting (direct and indirect)

A. Direct-acting agents

Three naturally occurring catecholamines are present in the body: (1)Epinephrine: acts mainly as an emergency hormone; released by the adrenal medulla

(2) Norepinephrine: acts as an important transmitter of nerve impulses

(3)Dopamine: a precursor of epinephrine and norepinephrine; has a transmitter role of its

own in certain portions of the CNS

(4) Examples include the following:

(a) Epinephrine (Adrenalin)

(b) Norepinephrine (Levophed)

(c) Dopamine (Intropin)

Catecholamines :

depend on their ability to act directly with alpha and beta receptors

(1) Alpha-1 receptors : are postsynaptic receptors located on effector organs; their

primary role is to stimulate the contraction of smooth muscle

(2) Alpha-2 receptors: are found on presynaptic and postsynaptic nerve endings

(a) When stimulated, presynaptic receptors inhibit the further release of

norepinephrine

(b) Like alpha-7 receptors, alpha-2 postsynaptic receptors mediate

vasoconstriction to increase resistance and thus increase blood pressure

(3) Beta-1 receptors: are located primarily in the heart

(4) Beta-2 receptors: are located predominantly in the bronchiolar and arterial

smooth muscle

(5) Beta receptors do the following:

(a) Stimulate the heart

(b) Dilate bronchioles

(c) Dilate blood vessels in the skeletal muscle, brain, and heart

(d) Aid in glycogenolysis

c) Norepinephrine

(7) Acts mainly on alpha receptors

(2) Causes almost pure vasoconstriction



d) Epinephrine

(7) Acts on alpha and beta receptors

(2) Produces a mixture of vasodilation and vasoconstriction, depending on the

relative number of alpha and beta receptors present in the target tissue

e) The most important alpha activities are as follows:

(7) Vasoconstriction of arterioles in the skin and splanchnic area, which results in a

rise in blood pressure and peripheral shunting of blood to the heart and brain due

to the shift of blood volume

(2) Pupil dilation

(3) Relaxation of the gut

f) The most important beta activities are as follows:

(7) Cardiac acceleration and increased contractility

(2) Vasodilation of arterioles supplying skeletal muscle

(3) Bronchial relaxation

(4) Uterine relaxation

B-Indirect- and dual-acting

Note: Because of the possibility of extravasation and tissue necrosis, all drugs with alpha effects

should be administered through a secure intravenous line that is well positioned in a large vein.

a) Indirect-acting adrenergic drugs act indirectly on receptors by triggering the

release of norepinephrine and epinephrine, which then activate alpha and beta

receptors

b) Dual-acting adrenergic drugs have indirect and direct effects

(7) Example: ephedrine (ephedrine sulfate)

e. Adrenergic blocking agents 7) May be classified into alpha- and beta-blocking drugs

2) Alpha-blocking drugs

a) Block the vasoconstricting effect of catecholamines

b) Used in certain cases of hypertension and to help prevent necrosis when

norepinephrine (Levophed) or dopamine (Intropin) has extravasated into the tissues

c) Limited clinical application in the prehospital setting

3) Beta-blocking agents

a) Have greater clinical application and frequently are used in emergency care

b) Block beta receptors, thereby inhibiting the action at their effector site

Beta-blocking agents are divided into two groups

(1) Selective blocking agents block beta-7 or beta-2 receptors

Selective beta-7 blocking agents also are known as cardioselective blockers because they

block the beta-7 receptors in the heart

Example: metroprolol (Lopressor) and atenolol (Tenormin), antihypertensives, and

antidysrhythmics

2) Selectivity is not 7001; even cardioselective drugs may affect the lungs and vice versa

(2)Nonselective: blocking agents block beta-7 and beta-2 receptor sites

e) Nonselective beta-blocking agents inhibit beta-7 receptors in the heart and beta-2

receptors in the smooth muscle of the bronchioles and blood vessels

f) Examples include the following:

(7) Antianginal antihypertensives

(a) Nadolol (Corgard) (b)Propranolol (Inderal)

(2) Antihypertensive labetalol (Normodyne, Trandate)

(a) Labetalol also has some alpha-blocking activity.



VI. NARCOTIC ANALGESICS AND ANTAGONISTS 1. Narcotic:- analgesics relieve pain

2. Narcotic antagonists:- reverse the narcotic effects of some analgesics

3. Pain has two components:

a. Sensation of pain:- involves the nerve pathways and the brain

b. Emotional response:- to pain may be a result of anxiety level, previous pain experience, age,

gender, and culture

4. Opiates

a. Opiates:- are drugs that contain or are extracted from opium

b. Opioids:- are synthetic drugs with pharmacological properties similar to those of opium or

morphine

c. They work by binding with opioid receptors in the brain and other body organs

7) Opiates alter the patient’s pain perception and emotional response to a pain-provoking

stimulus

►NOTE:-Endorphins serve as the body’s own supply of opiates by binding to opiate receptors,

thereby blocking pain.

d. Opioid analgesics:- include morphine (morphine sulfate, codeine (Methylmorphine),

hydromorphone (Dilaudid, Dilaudid HP), meperidine (Demerol), methadone (Dolophine,

Methadose), oxycodone (Percodan, Tylox, Percocet), hydrocodone (Lortab), and

propoxyphene (Darvon, Dolene)

e. Opioid analgesics may produce undesirable effects:

7) Nausea and vomiting

2) Constipation

3) Urinary retention

4) Cough reflex suppression

5) Orthostatic hypotension

6) CNS depression

f. Most of these side effects can be overcome by careful administration of the analgesic and

careful patient monitoring

5. Opioid antagonists

a. Opioid antagonists Block the effects of opioid analgesics (e.g., opioid-induced respiratory

depression and sedation) by displacing the analgesics from their receptor sites

b. Examples include the following:

7) Naloxone (Narcan)

2) Naltrexone (Trexan)

3) Nalmefene (Revex).

The half-life of naloxone (Narcan) is shorter than most opioids, so dosing may need to be repeated.

6. Opioid agonist-antagonist agents

a. Have analgesic and antagonist effects

b. Have pharmacokinetic and adverse effects similar to morphine

c. May competitively antagonize some opioid receptors but have varying degrees of agonist

effect at other opioid receptor sites

d. Examples include the following:

7) Butorphanol (Stadol)

2) Pentazocine (Talwin)

3) Nalbuphine hydrochloride (Nubain)



e. Generally have a lower dependency potential than opioids

7) Less severe withdrawal symptoms

2) May precipitate withdrawal symptoms in addicts .

VII. NON-NARCOTIC ANALGESICS 7. Act by a peripheral mechanism that interferes with local mediators released when tissue is

damaged , These mediators stimulate nerve endings and cause pain

2. When non-narcotic analgesics are present, the nerve endings in damaged tissues are less

frequently stimulated

a. This mechanism differs from that of narcotic analgesics, which act at the level of the CNS

3. Example: ketorolac (Toradol), a nonsteroidal anti-inflammatory drug that

exhibits analgesic activity

A.. Anesthetics 7. Anesthetics are CNS depressants that have a reversible action on nervous tissue

2. Three major categories of anesthesia:

a. General

7) Achieved by intravenous or inhalation routes

2) Most common type of anesthesia used during surgery to induce unconsciousness

b. Regional

7) Obtained by injecting a local anesthetic drug near a nerve trunk or other specific sites in a

large region of the body

2) Example: spinal block

c. Local

7) Achieved topically to produce a loss of sensation or by injection to ÒblockÓ an area

surrounding an operative field, making it insensitive to pain

2) Example: minor wound repair

VIII. ANTIANXIETY AND SEDATIVE HYPNOTIC AGENTS AND ALCOHOL 1. Antianxiety and sedative-hypnotic agents and alcohol:- have similarities in pharmacological

action

2. Antianxiety agents:-are used to reduce feelings of apprehension, nervousness, worry, or

fearfulness

3. Sedatives and hypnotics are drugs:- that depress the CNS, produce a calming effect, and help

induce sleep

4. The major difference between a sedative and a hypnotic is the degree of CNS depression

induced by the agent.

For example,

small dose:- of an agent administered to calm a patient is called a sedative;

large dose:- of the same agent sufficient to induce sleep would be called a hypnotic.

Therefore an agent may be both a sedative and a hypnotic, depending on the dose used.

5. Alcohol has actions characteristic of sedative-hypnotic or antianxiety drugs

a. The social use of alcohol is mainly as a self-prescribed antianxiety agent; it is considered a

major source of drug abuse and dependency

6. Reticular formation

a. Reticular formation consists of groups of nuclei scattered through the brain stem

b. Reticular formation and its neural pathways constitute a system known as the reticular

activating system (RAS)

7) Involved with the sleep-awake cycle



2) Through these pathways incoming signals from the senses and viscera are collected,

processed, and passed to the higher brain centers

3) RAS determines the level of awareness to the environment and governs actions and

responses to it

c. Antianxiety and sedative-hypnotic agents and alcohol act by depressing the RAS

3. Classifications a. Benzodiazepines: drug class most commonly used today to treat anxiety and insomnia

b. Barbiturates: older drug class with many uses, from sedation to anesthesia

A-Benzodiazepines 7)Thought to work by binding to specific receptors in the cerebral cortex and limbic system

major integrating system that governs emotional behavior)

2) Highly lipid-soluble and widely distributed in the body tissues

3) Highly bound to plasma protein (usually more than %01)

4) Four actions:

a) Anxiety-reducing

b) Sedative-hypnotic

c) Muscle-relaxing

d) Anticonvulsant

6) All benzodiazepines are schedule IV drugs because of their potential for abuse

NOTE:-Flumazenil (Romazicon) is a specific benzodiazepine receptor antagonist and has been

shown to be effective in reversing benzodiazepine-induced sedation and coma.

3) Commonly prescribed benzodiazepines:

a) Alprazolam (Xanax)

b) Chlordiazepoxide (Librium)

c) Clorazepate (Tranxene)

d) Diazepam (Valium)

e) Flurazepam (Dalmane)

f) Prazepam (Centrax)

g) Midazolam (Versed)

h) Lorazepam (Ativan)

i) Triazolam (Halcion)

B. Barbiturates 1) Once the most commonly prescribed class of medications for sedative-hypnotic effects,

but they have been virtually replaced by benzodiazepines

2) Divided into four classes according to their duration of action:

a) Ultra-short-acting

b) Short-acting

c) Intermediate-acting

d) Long-acting

3) Differences in onset and duration of action depend on their lipid-solubility and protein-

binding properties

a. Ultra-short-acting barbiturates

a) Used as intravenous anesthetics

b) Act rapidly and can produce a state of anesthesia in a few seconds

c) Example: thiopental sodium (Pentothal)



b. Short-acting barbiturates

a) Produce an effect in a relatively short time (70–75 minutes) and peak over a relatively

short period (3–4 hours)

b) Rarely used to treat insomnia

c) More commonly used for preanesthesia sedation and in combination with other drugs

for psychosomatic disorders

d) Examples include the following:

(7) Pentobarbital (Nembutal) (2) Secobarbital (Seconal)

c. Intermediate-acting barbiturates

a) Have an onset of 45 to 60 minutes and peak in 6 to % hours

b) Short-acting and intermediate-acting agents have similar patient responses in the

clinical setting

c) Examples include the following:

(7) Amobarbital (Amytal)

(2) Butabarbital (Butisol)

d. Long-acting barbiturates

a) Require over 60 minutes for onset and peak over a period of 70 to 72 hours

b) Used to treat epilepsy and other chronic neurological disorders and to sedate patients

with severe anxiety

c) Examples include the following:

(7) Mephobarbital (Mebaral)

(2) Phenobarbital (Luminal).

C. Miscellaneous sedative-hypnotic drugs a. Agents that are not benzodiazepines or barbiturates

b. More similar to barbiturates than benzodiazepines

c. Examples include the following:

7) Etomidate (Amidate)

2) Chloral hydrate (Noctec)

3) Ethchlorzynol (Placidyl)

d. Some antihistamines have pronounced sedative effects:

7) Hydroxyzine hydrochloride (Vistaril, Atarax)

IX . Alcohol intake and behavioral effects a. Alcohol is a general CNS depressant that can produce sedation, sleep, and anesthesia

b. Enhances sedative-hypnotic effects of other drug classes, including the following:

7) All general CNS depressants

2) Antihistamines

3) Phenothiazines

4) Narcotic analgesics

5) Tricyclic antidepressants

c. Blood alcohol is measured in milligrams per deciliter (mg/dL)

7) Behavioral effects can be predicted based on blood alcohol levels.

X.. ANTICONVULSANTS 1. Used to treat seizure disorders (most notably epilepsy)

a. Seizure disorders:- are neurological disorders characterized by a recurrent pattern of

abnormal neuronal discharges within the brain

b. These disorders result in a sudden loss or disturbance of consciousness

c. They are sometimes associated with motor activity, sensory phenomena, or inappropriate behavior



2. The exact mode and site of the action of anticonvulsants are not understood

a. These drugs depress the excitability of neurons that fire to initiate the seizure or suppress

generalization of the small focal depolarization that occurs

7) Prevent the spread of seizure discharge

2) Presumed to modify the ionic movements of sodium, potassium, or calcium across the

cell membrane

3) Reduce the response to incoming electrical or chemical stimulation

b. Benzodiazepines also stimulate major inhibitory neurotransmitters in the CNS

c. Many patients require drug therapy throughout their lives to control seizures

3. Classifications

a. Choice of drug depends on the type of seizure disorder (i.e., generalized, partial, status) and

the patient’s tolerance to the drug

b. Many anticonvulsant drugs produce undesirable side effects

c. Medication noncompliance is often encountered in these patients

d. Common anticonvulsants include the following:

7) Phenobarbital (Luminal)

2) Phenytoin (Dilantin)

3) Diazepam (Valium)

4) Magnesium sulfate

XI. CENTRAL NERVOUS SYSTEM STIMULANTS 7. Classified by where they exert their major effects in the nervous system:

on the cerebrum, the medulla and brainstem, or the hypothalamic limbic regions

a. All work to increase excitability either by blocking activity of inhibitory neurons or their

respective neurotransmitters, or by enhancing the production of the excitatory

neurotransmitters

b. Some of the more common CNS stimulant drugs include anorexiants and amphetamines

.Anorexiants

a. Anorexiants are appetite suppressants used to treat obesity

b. Work by producing a direct stimulant effect on the hypothalamic and limbic regions and

perhaps other areas of the nervous system


7) Phendimetrazine (Plegine)

2) Mazindol (Mazanor, Sanorex)

d. A new class of drug (GI lipase inhibitors, or called Fat blockers) block the absorption of

about 301 of dietary fat. These drugs sometimes are used in the management of obesity in

conjunction with a reduced-calorie diet. An example of a GI lipase inhibitor is orlistat

(Xenical)

NOTE:-A two-drug combination of fenfluramine and phentermine (ÒFen-PhenÓ) to manage

obesity was withdrawn from the market in 7991. It was found to produce serious complications

including potentially fatal primary pulmonary hypertension and valvular heart disease.

Amphetamines a. Amphetamines stimulate the cerebral cortex and reticular activating system, thereby

increasing alertness and responsiveness to environmental surroundings

b. Amphetamines are primarily used to treat the following:

1) Attention deficit hyperactivity disorder (ADHD)

a) Primarily seen in children and adolescents and is characterized by a short attention span



and impulsive behavior

** Narcolepsy a) People with narcolepsy experience excessive drowsiness, sudden sleep attacks during

daytime hours, and sometimes sleep paralysis

Examples of drugs used to treat these conditions include the following:

a) Methamphetamine (Desoxyn)

b) Amphetamine mixed salts (Adderall)

c) Dextroamphetamine tablets and elixir

4) Nonamphetamine CNS stimulant drugs used to treat ADD with hyperactivity include the

following:

a) Methylphenidate (Ritalin, Concerta)

b) Pemoline (Cylert)

5) Amphetamines and other stimulants have a paradoxical effect of calming children with

ADD with hyperactivity, probably by increasing neurotransmitter levels of dopamine.

XII. PSYCHOTHERAPEUTIC DRUGS 7. Psychotherapeutic drugs include the following:

a. Antipsychotic agents

b. Antidepressants

c. Lithium

2. Psychotherapeutic drugs are used to treat psychoses and affective disorders,

especially schizophrenia, depression, and mania

A.. CNS and emotions a. Neurotransmitters in the CNS that have major effects on emotion include the following:

1) Acetylcholine: released from central neural tissue into the cerebrospinal fluid during

activity

2) Norepinephrine and dopamine: widespread inhibitory effects on functions such as

sleep and arousal, affect, and memory

3) Serotonin: affects mood and behavior

4) Monoamine oxidase: enzyme that inactivates dopamine and serotonin that are produced

during intense emotional states

b. Alterations in the levels of these neurotransmitters are associated with changes in mood and

behavior

c. Drug therapy alleviates symptoms by temporarily modifying unwanted behavior

B.. Antipsychotic agents a. Uses:

7) Schizophrenia (primary use)

2) Tourette’s syndrome

3) Senile dementia associated with Alzheimer’s disease

b. Effective antipsychotic (neuroleptic) drugs block dopamine receptors in specific areas of the

CNS

c. These drugs can be classified into the following groups:

■ Phenothiazine derivatives

a) Chlorpromazine (Thorazine) .

b) Thioridazine (Mellaril) . c)Fluphenazine (Prolixin)

■ Butyrophenone derivatives

a) Haloperidol (Haldol)



■ Dihydroindolone derivatives

a) Molindone (Moban)

■ Dibenzoxapine derivatives

a) Loxapine (Loxitane)

■ Thienbenzodiazepine derivatives

a) Olanzapine (Zyprexa)

■ Atypical agents

a) Clozapine (Clozaril) . (b) Risperidone (Risperdal)

d. With continued use of antipsychotics, some patients develop supersensitivity of dopamine

receptors that leads to tardive dyskinesia.

Tardive dyskinesia is a potentially irreversible neurological disorder that is characterized by

involuntary repetitious movements of the muscles of the face, limbs, and trunk. Other

identifying features include excessive blinking of the eyelids, lip smacking, tongue

protrusion, foot tapping, and rocking side-to-side

C.. Antidepressants a. Antidepressants are used to treat affective disorders (mood disturbances), including

depression, mania, and elation

b. Tricyclic antidepressants and MAO inhibitors are prescribed for depression; lithium (an

antimanic drug) is the preferred treatment for mania

NOTE :-Depression may be exogenous and occur as a result of a person’s response to a loss or

disappointment (e.g., Other blues). Exogenous depression is considered Normal is usually

temporary, and remits without the use of drug therapy. Endogenous depression lasts 6 months or

more and is characterized by the absence of external causes; it may be the result of genetic or

biochemical alterations. Antidepressants are often needed to treat this disorder. Depression may

be defined as a unipolar (continuous or recurrent episodes) or a bipolar (manic-depressive)

disorder.

1.. Tricyclic antidepressants 7) Thought to treat depression by increasing levels (blocking reuptake) of the

neurotransmitters norepinephrine and serotonin

2) Examples include the following:

a) mirtazapine (Remron) . (b)Amitriptyline (Elavil)

2.. Selective Serotonin Reuptake Inhibitors (7) Block reabsorption or reuptake of serotonin so more is available for the brain

(2) Side effects include insomnia and difficulty reaching orgasm.

Examples include:

a. Floxetine (Prozac). b.Sertraline (Zoloft)

c. Paroxetine (Paxil). d. Fluvoxamine (Luvox)

e. Citalopram (Celexa)

3.. Monoamine oxidase (MAO) inhibitor antidepressants ** Central-acting monoamines, especially norepinephrine and serotonin, are thought to

cause depression and mania

a) MAO (an enzyme found in nerve cells that is thought to be produced during tense

emotional states) is responsible for metabolizing norepinephrine within the nerve

b) MAO inhibitors block this enzyme, leading to increased levels of norepinephrine

Examples of MAO inhibitors used to treat depression include the following:

a) Isocarboxazid (Marplan) . (b)Phenelzine (Nardil) . (c)Tranylcypromine (Parnate)



MAO inhibitors may also be used as antihypertensive agents

4.. Lithium A)Lithium is a cation that is closely related to sodium. Both cations are transported

actively across cell membranes.

B)lithium cannot be pumped as effectively out of the cell as sodium. Lithium therefore

accumulates in the cells. This results in a decrease in intracellular sodium and perhaps

an improvement in the symptoms of a manic state.

C) lithium appears to enhance some of the actions of serotonin, Lithium may decrease

levels of norepinephnine and dopamine. Lithium also appears to block the

development of dopamine receptor supersensitivity that may accompany long-term

therapy with antipsychotic agents. Lithium carbonate is used to treat manic disorders and comes in capsule,

tablet, arid syrup form (e.g., lithium citrate).

XIII. DRUGS FOR SPECIFIC CNS PERIPHERAL DYSFUNCTION Several movement disorders result from an imbalance of dopamine and acetylcholine. Two of the most

common are Parkinson’s disease (including parkinsonism syndromes) and Huntington’s disease.

1. Parkinson’s disease a. A chronic disabling disease characterized by rigidity of voluntary muscles and tremor of the

fingers and extremities

b. Most often affects people over age 60 but may occur in younger people, especially after acute

encephalitis, carbon monoxide or metallic poisoning, or the use of some illicit drugs

Parkinsonism syndromes mimic the characteristics of Parkinson’s disease. They are usually idiopathic, but

they may also result from treatment with antipsychotic drugs (drug-induced parkinsonism) that block

dopaminergic receptors (e.g., haloperidol, metoclopramide, and phenothiazines).

c. Thought to result from an abnormally low concentration of dopamine

2. Huntington’s disease

a. Inherited disorder characterized by progressive dementia and involuntary muscle twitching

(chorea)

b. Thought to be related to an imbalance of dopamine, acetylcholine, and perhaps other

neurotransmitters

XIV.. DRUGS WITH CENTRAL ANTICHOLINERGIC ACTIVITY 7. Drugs that inhibit or block acetylcholine are referred to as anticholinergic

2. Work by restoring normal dopamine-acetylcholine balance in the brain

3. Examples include the following:

a. Benztropine (tablets and injections)

b. Ethopropazine hydrochloride

. Drugs that affect brain dopamine a. Three classifications of drugs affect brain dopamine:

7) Those that release dopamine

2) Those that increase brain levels of dopamine

3) Dopaminergic agonists

b. Levodopa (L-Dopa)

7) Increases brain levels of dopamine

2) Current drug of choice in the treatment of movement disorders associated with dopamine-

acetylcholine imbalance



A..MAO inhibitors 7) MAO A metabolizes norepinephrine and serotonin

2) MAO B metabolizes dopamine

3) Selegiline (Deprenyl)

a) Selective inhibitor of MAO B

b) Retards the breakdown of dopamine

c) Often used in conjunction with levodopa because it enhances and prolongs the

antiparkinsonism effects of levodopa (allowing the dose of levodopa to be reduced) has some

alpha-blocking activity

XIV. SKELETAL MUSCLE RELAXANTS a. Skeletal muscle contraction is evoked by a nicotinic cholinergic transmission process

b. Such contraction can modification by drugs just as autonomic ganglionic transmission

c. Skeletal muscle relaxants can be classified as central-acting, direct-acting, and

neuromuscular blockers

1. Central-acting agents

a. Used to treat muscle spasms

b. Thought to work by producing CNS depression in the brain and spinal cord


7) Carisoprodol (Soma)

2) Cyclobenzaprine (Flexeril)

3) Diazepam (Valium)

2. Direct-acting muscle relaxants

a. Work directly on skeletal muscles to produce muscle relaxation, thereby resulting in

decreased muscle contraction

b. Example: Dantrolene (Dantrium)

3. Neuromuscular blockers

a. Produce complete muscle relaxation and paralysis by binding to the nicotinic receptor for

acetylcholine at the neuromuscular junction

7) Neurmuscular transmission is thus inhibited and remains so for a variable period,

depending on the type and amount of neuromuscular blocker used

b. Sometimes used for the following purposes:

7) To achieve total sedation before ET intubation

2) To relieve muscle spasms of the larynx

3) To suppress tetany

4) During electroconvulsive therapy (ECT) for depression

5) To allow for breathing control by a respirator

c. Because these blocking agents produce complete paralysis, ventilatory support must be

provided and the efficacy of ventilation and oxygenation closely monitored

d. Muscle relaxants do not inhibit pain or seizure activity

e. Examples include the following:

7) Pancuronium (Pavulon)

2) Vecuronium (Norcuron)

3) Succinylcholine (Anectine).



Section Four:

Drugs That Affect the Cardiovascular System I. REVIEW OF ANATOMY AND PHYSIOLOGY

. The Heart Is Composed of Many Interconnected Branching Fibers or Cells That Form the

Walls of the Two Atria and Two Ventricles

7. Some cells are specialized to conduct electrical impulses

2. Some have contraction as their primary function

3. Cardiac drugs are classified by their effects on the different heart tissues

. Pharmacological Terms to Describe Actions of Cardiovascular Drugs

1. Chronotropic drugs

a. Affect heart rate

b. A drug that accelerates heart rate is said to have a positive chronotropic effect (epinephrine)

c. A drug that decreases the heart rate is said to have a negative chronotropic effect (verapamil)

2. Dromotropic drugs

a. Affect conduction velocity through the conducting tissues of the heart

b. If a drug speeds conduction, it is said to have a positive dromotropic effect (isoproterenol)

c. If a drug slows conduction, it is said to have a negative dromotropic effect (adenosine)

3. Inotropic drugs

a. Affect force of contraction

b. A drug that strengthens or increases the force of contraction is said to have a positive

inotropic effect (epinephrine)

c. A drug that weakens or decreases the force of contraction is said to have a negative inotropic

effect (propranolol)

A.. Cardiac Glycosides 7. Cardiac glycosides are naturally occurring plant substances that have characteristic actions on the

heart

2. These compounds contain a carbohydrate molecule (sugar) that, when combined with water, is

converted into a sugar plus one or more active substances

3. Glycosides may work by blocking certain ionic pumps in the cellular membrane; this indirectly

increases the calcium concentration of the contractile proteins

4. An important cardiac glycoside is digoxin (Lanoxin)

a. Used to treat heart failure and to manage certain tachycardias

5. Digitalis glycosides can affect the heart in two different ways:

a. Increase the strength of contraction (positive inotropic effect)

b. Dual effect on the electrophysiological properties of the heart

7) Modest negative chronotropic effect, causing slight slowing

2) More profound negative dromotropic effect, decreasing conduction velocity

6. Many patients who take cardiac glycosides develop side effects at one time or another because of

the small therapeutic index. The symptoms may be neurological, visual, gastrointestinal, cardiac,

or psychiatric.

The most common side effects include:

a. Anorexia

b. Nausea and vomiting

c. Visual disturbances



These symptoms often are vague and can be easily attributed to a viral illness; therefore a high index of

suspicion must be maintained in patients taking cardiac glycosides.

7) Flashing lights 2) Altered color vision

d. Cardiac rhythm disturbances; usually a slowing with varying degrees of blocked conduction

3. Toxic effects

a. Toxic effects of cardiac glycosides are dose-related

b. Effects may be increased by the presence of other drugs such as diuretics, which may

predispose the patient to cardiac rhythm disturbances

c. Dysrhythmias may include bradycardias, tachycardias, and even ventricular fibrillation;

patients with these conditions require close monitoring

d. Treatment may include the following:

7) Correction of electrolyte imbalances

2) Neutralization of the free drug

3) Use of antidysrhythmics

B.. Antidysrhythmics 7. Used to treat and prevent disorders of cardiac rhythm

2. Work by direct action on the cardiac cell membrane (lidocaine), by indirect action that affects the

cell (propranolol), or both

5. Classifications a. Based on the fundamental mode of action on cardiac muscle

b. Drugs that belong to the same class do not necessarily produce identical actions

c. All antidysrhythmics have some ability to suppress automaticity

1-Class I : Sodium channel blocker

Class I (subdivided into classes I-A, I-B, and I-C)

1) Class I-A :- Decrease conduction velocity and prolong the electrical potential of cardiac tissue

Examples include quinidine (Quinaglute, Duraquin) and procainamide (Pronestyl)

2) Class I-B :- Decrease or have no effect on conduction velocity

Examples include lidocaine (Xylocaine) and phenytoin (Dilantin)

3) Class I-C

a) Have profoundly slow conduction

b) Indicated only for control of life-threatening ventricular dysrhythmias

c) Example is flecainide (Tambocor) .

Class I-C medications are not administered in the prehospital setting.

2-Class II :- Beta-blocking agents

7) Beta-blocking agents that reduce adrenergic stimulation of the heart

Example: propranolol (Inderal).

3-Class III:- potassium channel blockade

7) which increases contractility

2) Drugs in the group do not suppress automaticity and have no effect on conduction

velocity

3) Believed to terminate dysrhythmias that result from the reentry of blocked impulses

4) An example is amiodarone (Cordarone)

4-Class IV :- Calcium channel blockers

7)Believed to work by blocking the inflow of calcium through the cell membranes of cardiac

and smooth muscle cells

2) This action depresses the myocardial and smooth muscle contraction, decreases



automaticity, and, in some cases, decreases conduction velocity

3) Examples include verapamil (Isoptin) and diltiazem (Cardizem)

C.. Antihypertensives a. The exact mechanism of action of many antihypertensive drugs is unknown

b. The ideal antihypertensive drug should do the following:

7) Maintain blood pressure within normal limits for various body positions

2) Maintain or improve blood flow without compromising tissue perfusion or blood supply

to the brain

3) Reduce the workload on the heart

4) Have no undesirable side effects

5) Permit long-term administration without intolerance

. Classifications a. Antihypertensives are usually given in low-dose combinations and titrated to effect

b. Major categories include:

7) Diuretics

2) Sympathetic blocking agents (sympatholytic drugs)

3) Vasodilators

4) Angiotensin-converting-enzyme (ACE) inhibitors

5) Calcium channel blockers

6) Angiotensin II receptor antagonists

1) Diuretics 7) Considered the drugs of choice in managing hypertension

2) Frequently used with other antihypertensive agents

3) Cause a loss of excess salt and water from the body by renal excretion

a) The decrease in plasma and extracellular fluid volume (which decreases preload and

stroke volume), plus a direct effect on arterioles, results in lowered blood pressure

b) This response causes an initial decline of cardiac output followed by a decrease in

peripheral vascular resistance and a lowering of the blood pressure

a. Thiazide diuretics

a) Moderately effective in lowering blood pressure

b) Many antihypertensive agents cause retention of sodium and water, and thiazides may

be given concomitantly to help prevent this side effect

c) Example of a thiazide diuretic is hydrochlorothiazide (HCTZ)

b.Loop diuretics

a) Powerful short-acting agents that inhibit sodium and chloride reabsorption in the loop

of Henle

b) Cause excessive loss of potassium and an increase in the excretion of sodium and

c) Produce fewer side effects than most other antihypertensives, although hypokalemia

and profound dehydration can result from their use

d) Prescribed to patients who have renal insufficiency or who cannot take other diuretics

e) Example: Furosemide (Lasix).

Since many drugs are excreted by the kidneys, patients with renal system dysfunction (acute

or chronic renal failure) may accumulate drugs in their systems. These patients often require

modifications in drug doses and dosing intervals as well as diet modification and fluid

restriction.

c. Characteristics of potassium-sparing diuretics



7) Can be effective when used in combination with other diuretics

2) Promote sodium and water loss without an accompanying loss of potassium

3) Used to treat hypertensive patients who become hypokalemic with other diuretics or who

are apparently resistant to the antihypertensive effects of other diuretics

4) Can be used to treat some edematous states such as cirrhosis of the liver with ascites

5) Example: spironolactone (Aldactone)

2.. Sympathetic blocking agents 7) May be classified as beta-blocking agents and adrenergic inhibiting agent

A. Beta-blocking agents

a) Are used to treat cardiovascular disorders, including hypertension, suspected MI, and

high-risk unstable angina

b) Work by decreasing cardiac output and inhibiting rennin secretion from the kidneys

c) Both actions result in lower blood pressure

d) In addition, beta-blocking drugs compete with epinephrine for available beta-receptor

sites, inhibiting tissue and organ response to beta stimulation

e) Examples:

(7) Beta-7-blocking agents (cardioselective)

(a) Acebutolol (Sectral)

(b) Atenolol (Tenormin)

(c) Metoprolol (Lopressor)

(2) Beta-7 and beta-2 blocking agents (nonselective)

(a) Labetalol (Normodyne, Trandate); also has alpha-7-blocking properties

(b) Nadolol (Corgard)

(c) Propranolol (Inderal)

B.Adrenergic-inhibiting agents

a) Work by modifying the sympathetic nervous system

(7) Arterial pressure is influenced through various mechanisms of the heart, blood

vessels, and kidneys

(2) Sympathetic stimulation increases heart rate and force of myocardial contraction,

constricts arterioles and venules, and causes the release of renin from the kidneys

(3) Blocking this sympathetic stimulation can reduce blood pressure

b) Classified as centrally acting adrenergic inhibitors or peripheral adrenergic inhibitors

c) Mechanism by which many of these agents work is unknown

(7) It generally is believed that most have multiple sites of action


(7) Centrally acting adrenergic inhibitors

(a) Clonidine hydrochloride (Catapres)

(b) Methyldopa (Aldomet)

(c) Prazosin hydrochloride (Minipress)

(2) Peripheral adrenergic inhibitors

(a) Doxazosin (Cardura). (b)Guanethidine sulfate (Ismelin)

(c) Reserpine (Sandril, Serpasil). (d)Phentolamine (Regitine)

(e) Phenoxybenzamine (Dibenzyline). (f)Terazosin (Hytrin)

3-Vasodilator drugs 7) Act directly on the smooth muscle walls of the arterioles, veins, or both, lowering



peripheral resistance and blood pressure

2) Stimulate the sympathetic nervous system and activate the baroreceptor reflexes, leading

to an increase in heart rate, cardiac output, and renin release

a) Combined therapy usually is prescribed to inhibit the sympathetic response

3) Some vasodilator drugs are effective for treating angina pectoris (ischemic chest pain).

For example, nitrates dilate veins and arteries. Their dilating effects on veins lead to

venous pooling and a decreased blood return to the heart, thus reducing left ventricular

end-diastolic volume and pressure. The subsequent decrease in wall tension helps reduce

myocardial oxygen demand and the chest pain associated with myocardial ischemia.

4) Vasodilator drugs are classified:-as A)arteriolar dilators andB) arteriolar and venous

dilatory drugs

A) Arteriolar dilator drugs

a) Diazoxide (Hyperstat IV)

b) Hydralazine (Apresoline)

c) Minoxidil (Loniten)

B) Arteriolar and venous dilator drugs

a) Sodium nitroprusside (Nipride, Nitropress)

b) Nitrates and nitrites

c) Amyl nitrite inhalant

d) Isosorbide dinitrate (Isordil, Sorbitrate)

e) Nitroglycerin sublingual tablet (Nitrostat and others)

f) Nitroglycerin paste (Nitro-Bid, Nitrostat, Nitrol)

g) Intravenous nitroglycerin (Tridil)

4- ACE inhibitor drugs 7) The renin-angiotensin-aldosterone system plays an important role in maintaining blood

pressure and sodium and fluid balance. A disturbance in this system can result in

hypertension. In addition, kidney damage can result in an ability to regulate the release of

renin through normal feedback mechanisms, thereby causing elevated blood pressure in

some patients.

2) Angiotensin II is a powerful vasoconstrictor

a) It raises blood pressure and causes the release of aldosterone, which contributes to

sodium and water retention

b) By inhibiting conversion of the precursor angiotensin I to the active molecule

angiotensin II (which is brought about through ACE), the renin-angiotensin-

aldosterone system is suppressed and blood pressure is lowered

Examples of ACE inhibitors include the following: a) Captopril (Capoten) . (b)Enalapril (Vasotec) . (c)Lisinopril (Prinivil).

5- Calcium channel blockers 7) Calcium channel blocking agents reduce peripheral vascular resistance by inhibiting the

contractility of vascular smooth muscle

a) They dilate coronary vessels through the same mechanism

b) Effects of these drugs are important in treating hypertension, decreasing the oxygen

requirements of the heart (through decreased afterload) and increasing oxygen supply

(by abolishing coronary artery spasm), thus relieving the causes of angina pectoris

c) Various drugs in this class differ in degree of selectivity for coronary (and peripheral)

vasodilation or decreased cardiac contractility


(7) Verapamil (Isoptin, Calan)



(2) Nifedipine (Procardia)

(3) Diltiazem (Cardizem)

Angiotensin II Receptor Antagonists 7) Block the renin-angiotensin-aldosterone system better than ACE inhibitors

2) Lower blood pressure by inhibiting angiotensin II receptors

3) Can be used if patient can’t tolerate ACE inhibitors

4) Lower systolic and diastolic BP

5) Examples include:

a) candesartan (Atacand)

b) Irbesartan (Avapro)

b) Losartan (Cozaar)

c) Valsartan (Diovan)

Antihemorheologic Agents 7. Antihemorheologic agents are used to treat peripheral vascular disorders caused by pathological

or physiological obstruction (e.g., arteriosclerosis)

2. These drugs improve blood flow (and the delivery of oxygen) to ischemic tissues by restoring

red blood cell flexibility and lowering blood viscosity

3. Example: pentoxifylline (Trental).



Section Five:

Drugs That Affect the Blood I. ANTICOAGULATNS, FIBRINOLYTICS, AND BLOOD COMPONENTS

Bleeding and thrombosis are altered states of hemostasis. Understanding the drugs that affect blood

coagulation and the use of fibrinolytic agents and blood components is a necessary component of

prehospital patient management.

Anticoagulants 7. Blood coagulation :- A process that results in the formation of a stable fibrin clot that entraps

platelets, blood cells, and plasma

a. Results in a blood clot or thrombus

2. Abnormal thrombus formation (intravascular clotting) is a major cause of myocardial infarction

(from coronary thrombosis) and stroke (from cerebrovascular thrombosis)

3. Arterial thrombi are commonly associated with the following:

a. Atherosclerotic plaques

b. Hypertension

c. Turbulent blood flow that damages the endothelial lining of blood vessels

The coagulation process also occurs in the venous system, although the underlying mechanisms

responsible for the thrombosis differ.

Damage to the endothelium causes platelets to stick and aggregate in the arterial system. Arterial

thrombi are composed mostly of platelets but also involve the chemical substances that contribute to the

coagulation process (in particular, fibrinogen and fibrin). Myocardial infarctions and strokes are

frequently the result of arterial thrombi.

Major risk factors for various thromboses

A)stasis, (B)localized trauma, and (C)hypercoagulable states

a. Stasis

7) Results from immobilization or venous insufficiency

2) Responsible for increased incidence of deep vein thrombosis (DVT) in most bedridden

patients

b. Localized trauma

7) May initiate the clotting cascade and cause arterial and venous thrombosis

c. Hypercoagulable states

7) Mechanism behind the increased incidence of DVT in women who take birth control pills

2) Also responsible for many familial thrombotic disorders

. Agents That Affect Blood Coagulation Drugs that affect blood coagulation may be classified :

1)antiplatelet, (2)anticoagulant, and (3)flbrinolytic agents

1. Antiplatelet (antithrombic) agents

a. Drugs that interfere with platelet aggregation

b. Sometimes prescribed prophylactically for patients at risk for arterial clots and those who

have suffered myocardial infarctions or cerebrovascular accidents

c. Also used to treat certain valvular heart diseases, valvular prosthesis, and various intracardiac

shunts

d. Common antiplatelet drugs

7) Aspirin. 2)Dipyridamole (Persantine) . 3)Clopidogrel (Plavix)

4) Ticlopidine (Ticlid) . 5) Abciximab (ReoPro)



2. Anticoagulant agents a. Used to prevent intravascular thrombosis by decreasing blood

coagulability

b. Used to prevent postoperative thromboembolism

7) Also used during hemodialysis

2) Used in reperfusion therapy for select patients with acute coronary syndromes

c. Therapy is primarily prophylactic against future clot formation

7) Has no direct effect on a blood clot that has already formed or on ischemic tissue injured

by inadequate blood supply as a result of thrombus

d. Major side effect of therapy is hemorrhage

e. Examples:

7) Warfarin (Coumadin)

2) Heparin (Liquaemin)

f. Recent studies indicate that the administration of a glycoprotein (GP) Iib/IIIa receptor

antagonist may reduce ischemic complications after plaque fissure or rupture by inhibiting

GP receptors in the membrane of platelets.

C. Fibrinolytics Agents

7.Fibrinolytic drugs used to Dissolve clots after their formation by promoting the digestion of

fibrin

2. Treatment of choice for treating acute myocardial infarction in certain groups of patients, and in

the management of some stroke patients

a. Goal is to reestablish blood flow and prevent ischemia and tissue death

3. Also used to treat acute pulmonary embolism, DVT, and peripheral arterial

occlusion

4. Used in the prehospital setting in several areas of the United States

5. Examples

a. Anisoylated plasminogen steptokinase activator (Anistreplase)

b. Streptokinase (Streptase)

c. Tissue plasminogen activator (t-PA, Alteplase)

d. Reteplase (Retavase)

. Antihemophilic Agents 1. Hemophilia is a group of hereditary bleeding disorders in which there is a deficiency of one of

the factors necessary for the coagulation of blood

a. Characterized by persistent and uncontrollable hemorrhage after even minor injury

b. Bleeding may occur into joints, the urinary tract, and, on occasion, the central nervous

system

2. Hemophilia A (classic hemophilia) is caused by a deficiency of factor VIII

3. Hemophilia B (ÒChristmas diseaseÓ) results from a deficiency in factor IX complex

4. Replacement therapy of the missing clotting factor can be effective in the management of

hemophilia

a. Factor VIII (Factorate)

b. Factor IX (Konyne)

c. Antiinhibitor coagulant complex (Autoplex)

. Hemostatic Agents 7. Hemostatic agents hasten clot formation to reduce bleeding

2. Systemic hemostatic agents are generally used to control rapid blood loss after surgery by

inhibiting fibrinolysis : e.g., Amicar and Cyklokapron)



F. Blood and Blood Components 7. The healthy body maintains a normal balance of blood and its components. Illness and injury,

however, may impair this balance and require replacement therapy. Examples of conditions

include:

a. Hemorrhage

b. Burns

c. Dehydration

2. The usual treatment of choice in managing an imbalance of blood or blood components is to

replace the sole blood component that is deficient. Replacement therapies include:

a. Whole blood (rarely used)

b. Packed red blood cells

c. Fresh-frozen plasma

d. Plasma expanders (Dextran)

e. Platelets

f. Coagulation factors

g. Fibrinogen

h. Albumin

i. Gamma Globulins

G. Antihyperlipidemic Drugs 7. Hyperlipidemia refers to an excess of lipids in the plasma

2. Antihyperlipidemic drugs are sometimes used in conjunction with diet and exercise to control

serum lipid levels

3. Antihyperlipidemic drugs do not reverse existing atherosclerosis


a. Atorvastatin (Lipitor)

b. Cerivistatin (Baycol)

c. Cholestyramine (Questran)

d. Niacin (Nicobid)

e. Pravastatin (Pravachol)

f. Lovastatin (Mevacor)

g. Simvastatin (Zocor)



Section Six: Drugs

That Affect the Respiratory System A. The Respiratory System

7. Includes all structures involved in the exchange of oxygen and carbon dioxide

2. Serious Narrowing of Any Portion of the Respiratory Tract May Be an Indication for

Pharmacological Therapy

B. Emergencies Involving the Respiratory System Are Usually Caused by Reversible Conditions

7. Asthma

2. Emphysema with infection

3. Foreign body obstruction

C. Smooth Muscle Fibers of the Tracheobronchial Tree Directly Influence the Diameter of the

Airways

7. Bronchial smooth muscle tone is maintained by impulses from the autonomic nervous system

a. Parasympathetic fibers from the vagus nerve innervate bronchial smooth muscle through the

release of acetycholine

7) Interacts with the muscarinic receptors on the membranes on the cell, producing

bronchoconstriction

b. Sympathetic fibers primarily affect beta-2 receptors through the release of epinephrine from

the adrenal medulla and the release of norepinephrine from the peripheral sympathetic

nerves

7) Epinephrine reaches the lungs by way of the circulatory system and interacts with beta-2

receptors to produce smooth muscle relaxation and bronchodilation

2. Beta-2 receptors play the dominant role in bronchial muscle tone

3. Beta-7 receptors also are found on bronchial smooth muscle; their ratio to beta-2 receptors is 7:3

. Bronchodilators a. Bronchodilator drugs are the primary treatment modality for obstructive pulmonary disease

such as asthma, chronic bronchitis, and emphysema

b. These drugs may be classified into the following categories:

7) Sympathomimetic drugs

2) Xanthine derivatives

c. Many of these agents are administered by inhalation by means of a nebulizer or pressure

cartridge

a. Sympathomimetic drugs a. Grouped according to their receptor action:

7) Nonselective adrenergic drugs have alpha, beta-7 (cardiac), and beta-2 (respiratory)

activities

2) Nonselective beta-adrenergic drugs have both beta-7 and beta-2 effects

3) Selective beta-2 receptor drugs act primarily on beta-2 receptors in the lungs (bronchial

smooth muscle)

See Page Box 71-25.

1.Nonselective adrenergic drugs

7) Stimulate alpha and beta receptors

a) Alpha activity mediates vasoconstriction to reduce mucosal edema

b) Beta-2 activity produces bronchodilation and vasodilation

c) Undesirable effects on beta-7 receptors include an increase in heart rate and force of



contraction

d) Undesirable beta-2 effects include muscle tremors and CNS

stimulation


a) Epinephrine inhalation aerosol (Bronkaid Mist, Primatene Mist)

b) Epinephrine inhalation solution (Adrenalin)

c) Racemic epinephrine inhalation solution (Asthma Nefrin, Micro-Nephrin, and others)

2- Nonselective beta-adrenergic drugs

7) Not selective for beta-2 receptors

2) Have a wide range of effects

3) Examples of nonselective beta-adrenergic drugs with some alpha activity:

a) Epinephrine (Adrenalin, Asmolin)

b) Ephedrine (Ephed II)

c) Ethylnorepinephrine

4) Examples of nonselective beta-adrenergic drugs:

a) Isoproterenol inhalation solution (Aerolone, Vapo-Iso, Isuprel)

b) Isoproterenol inhalation aerosol (Isuprel Mistometer, Norisodrine Aerotrol)

3. Beta-2 selective drugs

7) Lessen incidence of unwanted cardiac effects caused by beta-7 adrenergic agents

2) Patients with hypertension, cardiac disease, or diabetes can better tolerate this group of

bronchodilators


a) Albuterol (Proventil, Ventolin)

b) Levalbuterol (Xopenex)

c) Pirbuterol (Maxair)

d Bitolterol (Tornalate)

e) Salmeterol (Serevent)

f) Formoterol (Foradil Aerolizer)

B. Xanthine derivatives a. Xanthine drugs include caffeine, theophylline, and theobromine

b. Actions

7) Relax smooth muscle (particularly bronchial smooth muscle)

2) Stimulate cardiac muscle and CNS

3) Increase diaphragmatic contractility

4) Promote diuresis through increased renal perfusion

c. Action of theophylline compounds depends on theophylline content

d. Products vary in rate of absorption and therapeutic effects


7) Aminophylline (Amoline, Somophyllin, Theo-Dur, Aminophyllin)

2) Dyphylline (Dilor, Droxine, Lufyllin)

3) Theophylline (Bronkodyl, Elixophyllin, Somophyllin-T)

f. Theophylline preparations generally are not considered a first-line drug in the treatment of

acute reactive airway disease



Other respiratory drugs a. Other agents can be used to treat asthma and other obstructive pulmonary diseases.

These agents include the following:

1) Prophylactic asthmatic agents

a) Cromolyn sodium (Intal, Sodium Cromoglycate)

2) Aerosol corticosteroid agents

a) Beclomethasone dipropionate (Vanceril Inhaler, Beclovent)

b) Dexamethasone (Decadron)

3) Antileukotrienes

a) Montelukast (Singulair)

b) Zafirlukast (Accolate)

4) Muscarinic antagonists (anticholinergics)

a) Ipratropium (Atrovent)

b) Glycopyrrolate (Robinul)

b. These medications reduce the allergic or inflammatory response to a variety of stimuli or

have an effect on bronchial smooth muscle

c. In the acute care setting, intravenous steroids (e.g., methyl-prednisolone [Solu-Medrol]) may

be given in an attempt to decrease the inflammatory response and improve airflow

Mucokinetic drugs a. Mucokinetic drugs are used to move respiratory secretions, excessive mucus, and sputum

along the tracheobronchial tree

b. They work by altering the consistency of these secretions so that they can more easily be

removed from the body

c. Persons with COPD often use mucokinetic drugs to clear their respiratory passages and to

improve ciliary activity

Mucus is a normal secretion produced by the surface cells in the mucous membranes. Sputum is

an abnormal viscous secretion that consists mainly of mucus and that originates in the lower

respiratory tract.

d. Mucokinetic drugs include diluents (water, saline solution), aerosols, and mucolytic drugs or

expectorants (Mucomyst)

Oxygen and miscellaneous respiratory agents Oxygen

7) Mainly used to treat hypoxia and hoxemia

2) Colorless, odorless, and tasteless gas essential for sustaining life

1- Direct respiratory stimulants (analeptics)

7) Act directly on the medullary center of the brain to increase rate and depth of respirations

2) Considered inferior to mechanical ventilatory measures to treat respiratory depression

and to counteract drug-induced respiratory depression caused by anesthetics

3) Example: doxapram (Dopram)

2-Reflex respiratory stimulants

7) Spirits of ammonia is the only drug given by inhalation as a reflex respiratory stimulant

a) Administered during cases of fainting

2) Works by irritating sensory nerve receptors in the throat and stomach

a) Following inhalation, respirations are stimulated through afferent messages to the

control centers of the brain



3- Respiratory depressants

7) Respiratory depressants include those of the opium and barbiturate groups of drugs

2) Respiratory depression is a common side effect of these drugs

3) Seldom given to intentionally inhibit rate and depth of respiration

4-. Cough suppressants

7) A cough is a protective reflex to expel harmful irritants

2) Coughs may have the following characteristics:

a) Productive (when removing irritants or secretions from the airway)

b) Nonproductive (dry and irritating)

3) When the cough is prolonged or secondary to an underlying disorder, treatment with

antitussive drugs may be indicated


a) Narcotic agents

(7) Codeine

b) Nonnarcotic agents

(7) Benzonatate (Tessalon)

(2) Dextromethorphan (Sucrets, Robitussin DM)

C. Antihistamines

7) Histamine is a chemical mediator found in almost all body tissues

a) Concentration is highest in the skin, lungs, and GI tract

2) Histamine is released when exposed to an antigen such as pollen or an insect sting

a) Results in increased localized blood flow, increased capillary permeability, and

swelling of the tissues

b) Produces contractile action on bronchial smooth muscle

3) Allergic responses involving histamines and other chemical mediators include local

effects such as angioedema, eczema, rhinitis, urticaria, and asthma. Systemic effects may

result in anaphylaxis

4) Antihistamines compete with histamine for receptor sites, thereby preventing the

physiological action of histamine

5) There are two types of histamine receptors:

a) H7 receptors (act primarily on the blood vessels and the bronchioles)

b) H2 receptors (act mainly on the GI tract)

6) Antihistamines also have anticholinergic or atropine-like action

a) May result in tachycardia, constipation, drowsiness, sedation, and the inhibition of

secretions

1) Most antihistamines also have a local anesthetic effect that may soothe skin irritation

caused by an allergic reaction

%) Primary clinical use is for allergic reactions

a) Also prescribed to control motion sickness or as a sedative or antiemetic


a) Dimenhydrinate (Dramamine)

b) Diphenhydramine (Benadryl)

c) Hydroxyzine (Vistaril)

d) Promethazine (Phenergan)

e) Loratidine (Claritin)

f) Fexofenadine (Allegra)



Serotonin

7) A naturally occurring vasoconstrictor material found in platelets and in the cells of the

brain and intestine

2) Has several pharmacological actions that are exerted on various smooth muscles and

nerves

3) Not administered as a drug, but has a major influence on other drugs and some disease

states

a) Helpful in repairing damaged blood vessels

b) Stimulated smooth muscle contraction

c) Acts as a neurotransmitter in the CNS where it has an effect on sleep, pain perception,

and some mental illnesses

Antiserotonins 7) Antiserotonins (serotonin antagonists) work to inhibit responses to serotonin and its

influence on other drugs and disease states

2) Specific antiserotonins block smooth muscle contraction and vasoconstriction and inhibit

the action of serotonin in the brain

3) Some are used to treat vascular headaches and allergic disorders


a) Cyproheptadine (Periactin)

b) Lysergic acid diethylamide (LSD)

c) Methysergide maleate (Sansert)



Section Seven:

Drugs That Affect the Gastrointestinal System A. GI System

7. Comprises the digestive tract, the biliary system, and the pancreas

B. Primary Function of the GI System

7. Provides the body with water, Electrolytes, and other nutrients used by cells

C. Drug Therapy for the GI System

7. Drugs that affect the stomach

2. Drugs that affect the lower GI tract

D. In Emergency Care, Conditions of the Stomach or Gastrointestinal Tract That May Require

Drug Therapy

7. Usually limited to nausea and vomiting

A. Drugs That Affect the Stomach Conditions of the stomach that may require drug therapy include hyperacidity, hypoacidity, ulcer

disease, nausea, vomiting, and hypermotility

1.. Antacids

a. Buffer or neutralized hydrochloric acid in the stomach

b. Prescribed for relief of symptoms associated with hyperacidity

7) Peptic ulcer

3) Esophagitis

4) Heartburn

5) Hiatal hernia

c. Common over-the-counter actacids: Alka-Seltzer, Gaviscon, and Rolaids

2.. Antiflatulents a. Prevent formation of gas in the GI tract

b. Gas retention is common with the following conditions:

7) Diverticulitis

2) Ulcer disease

3) Spastic or irritable colon

c. Sometimes used in combination with antacids

d. Example: simethicone (Mylicon)

3.. Digestants a. Promote digestion in the GI tract by releasing small amounts of digestive enzymes in the

small intestine

b. Examples: pancreatin and pancrelipase (Pancrease)

4.. Emetics and antiemetics a. Vomiting is an involuntary action coordinated by the emetic center of the medulla

7) May be initiated in the following ways:

a) By the CNS as a secondary reaction to emotion, pain, or disequilibrium (motion

sickness)

b) Irritation of the mucosa of the GI tract or bowel

c) Simulation from the chemoreceptor trigger zone of the medulla by circulating drugs

and toxins (e.g., opiates or digitalis)

b. Emetics

7) Used to induce vomiting as part of the treatment for certain drug overdoses and



poisonings

2) Examples: apomorphine and syrup of ipecac

c. Antiemetics 7) Drugs used to treat nausea and vomiting include antagonists of histamine, acetylcholine,

dopamine, and other drugs whose actions are not clearly understood

2) Most effective when administered before rather than after nausea and vomiting have

begun

a) Drugs used to treat motion sickness or vertigo should be taken 30 minutes before

traveling


a) Scopolamine (TransdermScop)

b) Dimenhydrinate (Dramamine)

c) Diphenhydramine (Benadryl)

d) Hydroxyzine (Vistaril)

e) Meclizine (Antivert)

f) Promethazine (Phenergan)

g) Prochlorperazine (Compazine)

h) Ondansetron (Zofran)

NOTE :-Cannabinoids are drugs derived from hemp plants. They have been used experimentally

as an antiemetic in patients receiving cancer chemotherapy. Examples of these drugs include

dronabinal (Marinol) and nabilone (Cesamet). These drugs use a synthetic derivative of the

active ingredient in marijuana.

d. Cytoprotective agents 7) Protect cells from damage

2) Used along with other drugs to treat peptic ulcer disease by protecting the gastric mucosa


a) Sucralfate (Carafate)

b) Misprostol (Cytotec)

e. H2 receptor antagonists 7) Action of histamine is mediated through H2 receptors

a) Has been associated with gastric acid secretion

2) H2 receptor antagonists block H2 receptors and reduce volume of gastric acid secretion

and its acid content


a) Cimetidine (Tagamet)

b) Ranitidine (Zantac)

c) Famotidine (Pepcid)

f. Proton pump inhibitors (PPIs) 7) Used to treat gastroesophageal reflux disease (GERD) and erosive

esophagitis

2) Some agents used in combination with antibiotics for the treatment of helicobacter pylori

(associated with duodenal ulcers)

3) The proton pump (potassium adenosine triphosphate enzyme system) is the final pathway

for secretion of hydrochloric acid by parietal cells in the stomach

a) Inhibiting the action of these cells decreases HCl secretion and alters stomach pH

4) Examples include:



a) Esomeprazole (Nexium)

b) Lansoprazole (Prevacid)

c) Omeprazole (Prilosec)

d) Rabeprazole (Aciphex)

B. Drugs That Affect the Lower GI Tract . Constipation and diarrhea are two common conditions of the lower GI tract that may require

drug therapy. Drugs used to manage these conditions include laxatives and antidiarrheals

1. Laxatives

a. Produce defecation

b. Used to evacuate the bowel and to soften hardened stool for easier passage

c. Situations that may indicate the need for laxative use include the following:

7) Constipation

2) Neurological diseases (e.g., multiple sclerosis, Parkinson’s disease)

3) Pregnancy

4) Rectal disorders

5) Drug poisoning

6) Surgery and endoscopic examination

d. There are numerous types of laxatives; many can be bought without a prescription


7) Saline laxatives (Epsom salts, Milk of Magnesia)

2) Stimulant laxatives (Dulcolax, Castor Oil, Ex-Lax)

3) Bulk-forming laxatives (Mitrolan, Metamucil)

4) Lubricant laxatives (mineral oil)

5) Fecal moistening agents (Colace, glycerin suppositories)

6) Bowel evacuating agents (GoLYTELY, Chronulac)

f. Regular or excessive use of laxatives is common in the older adult and in those with eating

disorders.

Laxative abuse may result in permanent bowel damage and electrolyte imbalance

3. Antidiarrheals

a. Used to reduce an abnormal frequency of bowel evacuation

b. Common causes of acute and chronic diarrhea include bacterial or viral invasion, drugs, diet,

and numerous disease states (e.g., diabetes insipidus, inflammatory bowel syndromes)

c. Examples include:

1) Absorbents: bismuth subsalicylate (Pepto-Bismol)

2) Anticholinergics: Donnatal

3) Opiates: Paregoric, codeine

4) Other agents : a)Diphenoxylate (Lomotil) . b)Loperamide (Imodium).



Section Eight

DRUGS THAT AFFECT THE EYE AND EAR I. DRUGS THAT AFFECT THE EYE A. Drugs Used to Treat Eye Disorders 7)Include Antiglaucoma Agents, Mydriatics and Cycloplegics, Antiinfective/Antiinflammatory

Agents, and Topical Anesthetics

A. Antiglaucoma Agents 7. Glaucoma

a. Glaucoma:- is an eye disease in which the pressure of the fluid in the eye is so abnormally

high that it causes compression or obstruction of the eye’s small internal blood vessels, the

fibers of the optic nerve, or both

b. The result of the condition is nerve fiber destruction and partial or complete loss of vision

c. Glaucoma is common in people over age 60 and is responsible for 751 of blindness in adults

in the United States

2. Agents used to reduce the pressure in chronic glaucoma include cholinergic and

anticholinesterase drugs

a. Some of these drugs (e.g., pilocarpine) dilate the pupil of the eye

b. Some of the drugs constrict the pupil

c. Others (e.g., acetazolamide) slow the secretion of aqueous fluid

3. If these drug therapies fail, surgery may be indicated

4. If diagnosed early, drugs can control glaucoma for a lifetime. Most physicians recommend

testing for glaucoma every 2 years after age 35.

B. Mydriatic and Cycloplegic Agents 7. Applied topically to cause pupil dilation and paralysis of accommodation to light

2. Uses: a. To treat inflammation and to relieve ocular pain by putting the eye to rest

b. During routine eye examinations

c. For ocular surgery


a. Atropine ophthalmic solution

b. Cyclopentolate hydrochloride ophthalmic solution (Cyclogyl)

c. Homatropine ophthalmic solution (Isopto Homatropine)

d. Epinephrine

e. Oxymetazoline (Ocu Clear)

C. Antiinfective/Antiinflammatory Agents 7. Used to treat eye conditions such as conjunctivitis, sty, and keratitis (corneal inflammation

caused by bacterial infection)


a. Bacitracin (Baciguent)

b. Chloramphenicol (Chloroptic)

c. Erythromycin (Ilotycin)

d. Natamycin (Natacyn)

E. Topical Anesthetic Agents

7. Used to prevent pain during the following:

a. Surgical procedures

b. Eye examinations



c. Treatment of some eye injuries (e.g., corneal abrasion)

2. Usually have a rapid onset (within 20 seconds) and last 75 to 20 minutes


a. Proparacaine (HCL (Opthaine)

b. Tetracaine HCL (Pontocaine)

F. Others

7. Artificial tear solutions

2. Lubricants

3. Irrigation solutions

4. Antiallergic agents.

II. DRUGS THAT AFFECT THE EAR A. Drugs Used to Treat Disorders of the External Ear Canal

7.Include Antibiotics, Steroid/Antibiotic Combinations, and Miscellaneous Preparations

B. Antibiotics

7. Used to treat infections

a. Examples include the following:

7) Chloramphenicol (Chloromycetin Otic)

2) Gentamicin sulfate (Garamycin)

C. Steroid/Antibiotic Combinations

7. Used to treat superficial bacterial infections

a. Examples include the following:

7) Neomycin sulfate/polymyxin B sulfate/hydrocortisone (Cortisporin Otic)

2) Neomycin/colistin/hydrocortisome (Coly-Mycin S Otic)

D. Miscellaneous Preparations

7. Used to treat earwax accumulation, inflammation, pain, fungal infections, and other minor

conditions

a. Examples include the following

7) Boric acid in isopropyl alcohol (Aurocaine 2)

2) Triethanolamine with chlorbutanol in propylene glycol (Cerumenex)

E. People with Inner Ear Infections or Serious Illness Associated with Hearing Impairment May

Require Systemic Antibiotics and a thorough Evaluation by a Physician to Prevent Complications



Section Nine:

Drugs That Affect the Endocrine System

I. REVIEW OF ANATOMY AND PHYSIOLOGY

7. Hormones are natural chemical substances that act after being secreted into the bloodstream from

endocrine glands (ductless glands that secrete internally)

2. These glands include the7) anterior and posterior pituitary, the (2)thyroid, the parathyroid and

(3)adrenal glands, (4)thymus, (5)pancreas, testes, and ovaries

3. Hormones from the various endocrine glands work together to regulate vital processes, including

the following:

a. Secretory and motor activities of the digestive tract

b. Energy production

c. Composition and volume of extracellular fluid

d. Adaptation (e.g., acclimatization, immunity)

e. Growth and development

f. Reproduction and lactation.

.. Drugs That Affect Specific Glands 1. Drugs affecting the pituitary

a. Hormones of the anterior and posterior pituitary gland exert an important effect in regulating

the secretion of other hormones

b. Anterior pituitary drugs: treat growth failure in children that is caused by growth hormone

deficiency

7) Somatrem (Protropin)

2) Somatropin (Humatrope)

c. Posterior pituitary drugs: treat symptoms of diabetes that result from antidiuretic hormone

(ADH) deficiency

7) Vasopressin (Pitressin)

2. Drugs affecting the thyroid and parathyroid

a. Thyroid hormone controls the rate of metabolic processes

7) Required for normal growth and development

b. Parathyroid hormone regulates the level of ionized calcium in the blood through the

following mechanisms:

7) Release of calcium from bone

2) Absorption of calcium from the intestine

3) Rate of excretion of calcium by the kidneys

c. Thyroid gland disorders

7) Goiter (enlargement of the thyroid gland)

2) Hypothyroidism (thyroid hormone deficiency)

3) Hyperthyroidism (thyroid hormone excess)

4) Drugs to treat hypothyroidism and prevent goiters

a) Thyroid (synthroid)

b) Iodine products

c) Levothyroxine

d. Parathyroid disorders

7) Hypoparathyroidism and hyperparathyroidism

2) Drugs to treat hyperparathyroidism:



a) Vitamin D

b) Calcium supplements

3. Drugs affecting the adrenal cortex

a. Adrenal cortex secretes three major classes of steroid hormones:

7) Glucocorticoids (cortisol)

a) Raise blood glucose

b) Deplete tissue proteins

c) Suppress the inflammatory reaction

2) Mineralocorticoids (primarily aldosterone)

a) Regulate electrolyte and water balance

3) Sex hormones (small amounts of estrogen, progesterone, and testosterone produced in

both men and women)

a) Have few physiological effects under normal circumstances

b. Glucocorticoids

7) Betamethasone (Celestone)

2) Dexamethasone (Decadron)

3) Methylprednisolone (Solu-Medrol)

c. Mineralocorticoids

7) Desoxycorticosterone acetate (DOCA)

2) Fludrocortisone (Florinef)

d. Adrenal steroid inhibitors

7) Aminoglutethamide (Cytadren)

2) Metyrapone (Metopirone).

note :- Two disorders of the adrenal cortex are Addison’s disease (adrenal cortical hypofunction)

and Cushing’s disease (adrenal cortical hyperfunction). See Chapter 32: Endocrinology.

4. Drugs affecting the pancreas

a. The pancreas is an exocrine and an endocrine gland

1) Exocrine gland: provides digestive juices to the small intestine

2) Endocrine gland: consists of pancreatic islets (islets of Langerhans), which produce the

hormones that enter the circulatory system

b. Hormones of the pancreas

1) Insulin

a) Primary hormone that regulates glucose metabolism

b) Increases ability of the liver, adipose tissue, and muscle to take up and use glucose

c) Glucose not immediately needed as an energy source is stored in skeletal muscle,

liver, and other tissues as glycogen

2) Glucagon

a) mainly influences the liver, although it has some effect on skeletal muscle and

adipose tissue

b) Stimulates the liver to break down glycogen so that glucose is released into the blood

(7) Also inhibits uptake of glucose by muscle and fat cells

3) Balancing action of these two hormones protects the body from hyperglycemia and

hypoglycemia

4) Balance of hormonal actions is important when considering the metabolic derangements

that can occur in diabetes mellitus

The relationship of glucagon and inst to other hormones and substances such as dextrose

(D50) and thiamine (vitamin B7

See Page316 Box 71-32.



Section Ten Drugs That Affect the Reproductive System

I. DRUGS THAT AFFECT THE FEMALE REPRODUCTIVE SYSTEM

A. Drugs Affecting the Female Reproductive System

7. Include Synthetic and Natural Substances Such as Hormones, Oral Contraceptives, Ovulatory

Stimulants, and Drugs Used To Treat Infertility

B. Female Sex Hormones

1. Two main types of hormones are secreted by the ovary:

a. Estrogen

b. Progesterone

2. Supplemental estrogen is indicated for the following:

a. Estrogen deficiency or replacement

b. Treatment of breast cancer

c. Prophylaxis for osteoporosis in postmenopausal women

3. Progesterone (and synthetic progestins) is used to do the following:

a. Treat hormonal imbalance

b. Treat endometriosis

c. Treat specific cancers

d. Prevent pregnancy when properly used

C. Oral Contraceptives

7. Oral contraception is the most effective form of birth control

2. Commonly known as The pills

a. Combination of estrogen and progesterone that results in suppression of

ovulation

3. Available in several different types

4. All are nearly 7001 effective for the prevention of pregnancy

D. Ovulatory Stimulants and Infertility Drugs

7. Absence of ovulation (anovulation) may be a pathological condition in women with abnormal

bleeding or infertility

2. Sometimes treated with the following:

a. Gonadotropins

b. Thyroid preparations

c. Estrogen

d. Synthetic agents

3. Clomiphene citrate (Clomid) is used to induce ovulation and increase fertility

4. Drugs used during labor and delivery to increase or decrease uterine contractility include

oxytocin (Pitocin) and ritodrine (Yutopar), respectively

5. In prehospital care, oxytocin (Pitocin) is used to control postpartum hemorrhage after infant and

placental delivery.

II. DRUGS THAT AFFECT THE MALE REPRODUCTIVE SYSTEM

A. Testosterone Therapy

7. Indicated for treatment of hormone deficiency (e.g., testicular failure), impotence, delayed

puberty, female breast cancer, and anemia

2. Choice of dosage and length of therapy depend on the diagnosis, the age of the patient, and the

intensity of side effects and adverse reactions

3. Example of an oral testosterone drug is methyltestosterone (Metandren)



III. DRUGS THAT AFFECT SEXUAL BEHAVIOR

A. Sexual Drive (Libido) Can Be Affected by Psychological, Social, and Physiological Factors

7. Negative Effects of These Factors Can Result in a Lack of Interest in Sexual Activity in Both

Men and Women and Impotence In Men.

B. Drugs That Impair Libido and Sexual Gratification

7. Some drugs interfere with sympathetic nervous stimulation and occasionally cause sexual

dysfunction by inactivating the nervous mechanisms (both directly and indirectly) that are

responsible for sexual arousal

2. Some of these drugs include antihypertensives, antihistamines, antispasmodics, sedatives,

tranquilizers, antidepressants, alcohol, and barbiturates

C. Drugs That Enhance Libido and Sexual Gratification

7. In addition to changing medications (under physician supervision) to avoid drug-induced sexual

dysfunction, a patient may be prescribed drugs to enhance libido and sexual gratification

2. Drugs that enhance sexual function include levodopa (L-Dopa) and sildenafil citrate (Viagra),

vardenafil (Levitra), tadalafil (Cialis).

a. The administration of nitroglycerin or nitrate/nitrite medications is contraindicated in patients

taking Viagra within the previous 24 hours because the combination can cause a lethal drop

in blood pressure

b. Other drugs that may produce untoward effects in patients taking Viagra include some

antibiotics, cimetidine, and some blood pressure–lowering medications

c. Always ask the patient about Viagra, Levitra, and Cialis use before administering any

medications



Section Eleven

Drugs Used in Neoplastic Diseases I. ANTINEOPLASTIC AGENTS A. Antineoplastic Agents 7. Used in Cancer chemotherapy to prevent the proliferation of malignant cells

2. These drugs do not directly kill tumor cells

a) They interfere with cell reproduction or replication through various mechanisms

NOTE :: any person who handle antineoplastic agents should be properly trained in safety

procedures. These drugs are considered cytotoxic (toxic to human cells).

3. Antineoplastic agents are nonselective and all cells in the body

4. Side effects from these drugs may include infection, hemorrhage, nausea and vomiting, and

changes in bowel habits

5. Short-term toxicity from these agents may affect the pulmonary, cardiovascular, renal, and

integumentary systems

6. Prehospital care for these patients primarily is supportive and is aimed at providing comfort

measures and emotional support

Example of Antineoplastic agents :-

1-Doxorubicin (Adriamycin)

2-Fluorouracil (Adrucil ) ,

3-Mechlorethamine ( Mustargen)

4-Mehtotrexate (Amethopterin)

5-Streptozocin(Zanosar).



Section Twelve

Drugs Used in Infectious Disease and Inflammation I. ANTIBIOTICS A. Antibiotics Are Used to Treat Local or Systemic Infection

7. They kill or suppress the growth of microorganisms in the following ways:

a. Disrupting the bacterial cell wall

b. Disturbing the functions of the cell membrane

c. Interfering with the cell’s metabolic functions

2. They include penicillins, cephalosporins and related products, macrolide antibiotics,

tetracyclines, fluoroquinolones, and miscellaneous antibiotic agents (e.g., metronidazole [Flagyl]

and spectinomycin [Trobicin])

3. Antibiotics are much more toxic to bacteria than they are to a patient. Some antibiotics, however,

may produce marked hypersensitivity that can lead to a fatal reaction if the drug is later

administered to a sensitized patient

B. Penicillins

7. Very active against gram-positive and some gram-negative bacteria

2. Used in the treatment of many infections including tonsillitis, pharyngitis, bronchitis, and

pneumonia

3. Capable of producing extremely severe anaphylactic reactions

4. Examples: amoxicillin (Amoxil), ampicillin (Amcill), dicloxacillin (Dynapen), and penicillin V

potassium (Pen Vee K)

C. Cephalosporins

7. Resemble penicillins but are active against both gram-positive and gram-negative bacteria

2. Widely used to treat ear, throat, and respiratory infections

3. Particularly useful in the treatment of urinary tract infection (UTI), which is often caused by

bacteria resistant to penicillin-type antibiotics

4. Examples: cefazolin (Ancef), cephalothin (Keflin), cefoxitin (Mefoxin), and cefotaxime

(Claforan)

5. About 61 to 701 or those people allergic to penicillins are also allergic to cephalosporins

D. Macrolide (Erythromycin) Antibiotics

7. Used to treat infections of the skin, chest, throat, and ears

2. Particularly useful in the treatment of pertussis (Òwhooping coughÓ) and legionnaires’ disease

3. Examples: Eryc, E-Mycin, E.E.S., Erythrocin

4. Other antibacterial agents include azithromycin (Zithromax) and clarithromycin (Biaxin)

E. Tetracyclines

7. Active against many gram-negative and gram-positive organisms (Òbroad-spectrumÓ)

2. Used to treat conditions including acne, bronchitis, syphilis, gonorrhea, and certain types of

pneumonia

3. Tetracyclines may discolor developing teeth and are therefore not usually prescribed for children

under the age of 72 or for pregnant women

4. Examples: demeclomycin (Declomycin) doxcycline (Vigramycin), and tetracycline

(Achromycin)

F. Fluoroquinolones

7. Treatment of choice for some gastrointestinal infections, particularly food-borne illnesses caused

by campylobacter or salmonellae bacteria

2. Also used to treat UTIs, venereal disease, bone and joint infections, some pneumonias and other

illnesses



3. Examples include:

a. Ciprofloxacin (Cipro)

b. Levofloxacin (Levaquin)

II. ANTIFUNGAL AND ANTIVIRAL DRUGS A. Antifungal Drugs 7. Some fungi are harmlessly present at all times in areas of the body such as the mouth, skin,

intestines, and vagina

a. They are prevented from multiplying through competition from bacteria and from actions of

the immune system

2. Fungal infections are more common and serious in people who have the following

characteristics:

a. Are taking long-term antibiotics (which destroy the bacterial competition)

b. Are immunosuppressed as a complication of illness (e.g., HIV)

c. Are taking corticosteroids or immunosuppressant drugs

3. Fungal infections can be broadly classified into superficial infections, subcutaneous infections,

and deep infections

a. Examples of superficial infections

7) Candidiasis (thrush) affecting the genitals or inside of the mouth, vaginal, intertriginous

area

2) Tinea (including ringworm, athlete’s foot, jock itch) affecting external areas of the body

b. Examples of infections (rare)

7) Sporotrichosis that may follow inoculation of spores through a puncture or scratch

2) Mycetoma (ÒMadura footÓ) that occurs in tropical countries

c. Examples of deep infections

4. Examples of antifungal drugs: tolnaftate (Tinactin), fluconazole (Diflucan), and nystatin

(Mycostatin)

5. There are about 50 species of fungi that can cause illness and sometimes fatal disease in humans

B. Antiviral Drugs

7. To date, few effective drugs exist to treat minor viral infections, such as colds

a. In fact, very few drugs exist for use in any viral infections

b. This is due in part to the relative delay in symptoms that occur in viral diseases, making drug

therapy difficult once the disease is established

2. Viral infections range from trivial and harmless (e.g., warts) to extremely serious diseases such

as influenza, rabies, AIDS, and probably some types of cancers

3. Few antiviral drugs have proved effective against specific virus-infected cells without toxic

effects to uninfected cells

4. Examples of specific antiviral drugs include the following:

a. Acyclovir (Zovirax), which is effective against herpes infection

b. Zidovudine (Retrovir, AZT, ZDV) and lamivudine (Epivir), and a combination drug

lamivudine/zidovudine (Combivir) which are currently used to treat HIV infection

C. Protease Inhibitors

7. Complete mechanism of action is not clearly understood

2. Appear to inhibit the replication of retroviruses (e.g., HIV) in both acute and chronically infected

cells

3. Side effects and adverse reactions include nausea and vomiting, headache, malaise, fever, and

flu-like symptoms

4. Examples: indinavir (Crixivan), ritonavir (Norvir), and saquinavir (Invirase)

5. Administration of antiviral drugs and protease inhibitors for a health care worker who has been



exposed to body fluids that may contain HIV or another virus known or suspected to be resistant

to antiviral drugs is important and is a postexposure prophylaxis (PEP) recommendation of the

Centers for Disease Control and Prevention

III. OTHER ANTIMICROBIAL DRUGS AND ANTIPARASITIC DRUGS A. Various Drugs Are Used to Treat Atypical Microbial Infection (E.G., Mycobacterium

Tuberculosis, Mycobacterium Leprae) and Infection and Disease Caused by Parasite and Insect

Vectors (e.g., Trichomoniasis, Malaria)

Example of antimicrobial and antiparastitc druges see page 320 pox 13-36

IV. ANTIINFLAMMATORY AND NONSTEROIDAL ANTIINFLAMMATORY DRUGS A. Inflammation

7. A defense mechanism of body tissues in response to physical trauma, foreign biological or

chemical substances, surgery, radiation, and electricity

a. Regardless of the event producing inflammation, the inflammatory response is similar

2. Inflammation can be localized or systemic

a. Local inflammation is confined to a specific area of the body

7) Symptoms include redness, heat, swelling, pain, and loss of function

b. Systemic inflammation occurs in many parts of the body

7) In addition to local symptoms, the following occurs:

a) Red bone marrow produces and releases large numbers of neutrophils that promote

phagocytosis

b) Pyrogens stimulate fever production

c) Increased vascular permeability in severe cases may result in decreased blood volume

c. Drugs used to treat inflammation or its symptoms may be classified as analgesic-antipyretic

drugs and nonsteroidal anti-inflammatory drugs (NSAIDs)

B. Analgesic-Antipyretic Drugs

7. The body’s thermoregulatory mechanism is located in the anterior hypothalamus (the Thermostat

of the body). Normally the Onset pinto of this hypothalamic center is about 9%86 F (31 C).

2. When there is an inflammatory response in the body, endogenous pyrogens are released by the

phagocytic leukocytes, producing fever.

3. Antipyretics reduce fever

4. Analgesic-antipyretic drugs work by reversing the effect of the pyrogen on the hypothalamus

so that the set point of the hypothalamus is returned to normal

5. Analgesic effects of these drugs act on peripheral pain receptors to block activation


a. Acetaminophen (Datril, Tylenol, Panadol)

b. Aspirin/acetylsalicylic acid (ASA, Aspergum, Bayer Aspirin)

c. Aspirin/buffered (Aluprin, Bufferin, Alka-Seltzer)

C. Nonsteroidal Antiinflammatory Drugs

7. Aspirin is the prototype of the NSAIDs

a. New drugs have been developed that, like aspirin, are analgesic, antipyretic, and

antiinflammatory

2. Often prescribed for patients with various inflammatory conditions such as rheumatoid arthritis

and especially for those who cannot tolerate aspirin

a. May be used to treat painful joint disorders (with or without inflammation) such as

osteoarthritis, low back pain, and gout

3. Like aspirin, the other NSAIDs may decrease platelet activity, and may cause gastrointestinal

bleeding



4. NSAIDs are thought to act by inhibiting specific enzymes so that prostaglandins (substances that

promote inflammation and pain) are not formed

5.Long term use of some NSAIDs has been linked to an incensed risk for heart attack and stork

Gout : is a metabolic disease associated with high levels of uric acid in the blood (hyperuricemia)

and that is characterized by attacks of acute pain, swelling, and tenderness of joints. The condition is

treated with uricosuric drugs, colchicine, and NSAIDs.


a. Aspirin (Bayer timed-Release, Bufferin)

b. Diflunisal (Dolobid)

c. Ibuprofen (Advil, Motrin, Nuprin)

d. Indomethacin (Indocin)

e. Naproxen (Anaprox, Aleve, Naprosyn)

f. Sulindac (Clinoril)

g. Ketorolac (Toradol)

h. Cox-2 inhibitors

7) Celecoxib (Celebrex)

2) Rofecoxib (Vioxx).



Section Thirteen

Drugs That Affect the Immunologic System I. REVIEW OF ANATOMY AND PHYSIOLOGY

A. Overview

7. The immunological system comprises cells and organs that defend the body against invasion by

foreign substances

2. Organs and tissues of the immune system include the spleen, tonsils, lymph nodes, and thymus

B. Immunosuppressants

7. Reduce the activity of the body’s immune system by suppressing the production and activity of

lymphocytes

2. Uses

a. Prescribed after transplant surgery to prevent rejection of foreign tissues

b. Sometimes given to halt the progress of autoimmune disorders when other treatments are

ineffective

3. Examples: antirejection drugs (used in organ transplantation), anticancer drugs, and

corticosteroids

C. Immunomodulating Agents

7. Increase the efficiency of the body’s immune system by activating immune defenses or by

modifying a biological response to an unwanted stimulus

2. Include vaccines that protect against specific infectious agents

3. Examples

a. Interferons: used to treat viral infections such as hepatitis C and certain types of cancer

b. Zidovudine: used to treat AIDS

4. Some immunomodulating agents enhance the ability of a vaccine to stimulate the immune

system and are added to the vaccine for this reason

D. Serums and Vaccines

1. Serums

a. Serum is the clear fluid that separates from blood when it clots

7) Contains salts, glucose, and other proteins (including antibodies formed by the body’s

immune system to protect against infection)

b. Can be prepared from the blood of a person (or rarely, an animal) infected with a

microorganism that usually contains antibodies to protect against that organism

7) Forms the basis for passive immunization

2. Vaccines

a. Contain killed or modified microorganisms (Òlive attenuated organismsÓ) that usually do

not cause the disease

b. Administered to produce specific immunity to a disease-causing bacterial toxin, virus, or

bacterium (active immunization)

7) If the particular infectious agent invades the body at a later time, the sensitized immune

system quickly produces antibodies to destroy the agent or the toxin it produces

c. Examples of live attenuated vaccines are those given to protect against measles, mumps,

rubella, yellow fever, and polio

d. Diphtheria and tetanus vaccines contain inactivated bacterial toxins

e. Cholera, typhoid fever, pertussis, rabies, viral hepatitis B, influenza, and Salk injected polio

vaccines contain killed organisms

7) In the case of hepatitis B, the vaccine contains only part of the hepatitis B virus

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