NUPC 107

Pharmacology
I. OVERVIEW

a) Definition of Terms:
 Pharmacology is the study of drugs (chemicals) that alter functions of living
organisms.
 Drug therapy, also called pharmacotherapy, is the use of drugs to prevent,
diagnose, or treat signs, symptoms, and disease processes.

Drugs given for therapeutic purposes are usually called medications.

 PHARMACOTHERAPEUTICS is the branch of pharmacology that uses drugs to

treat, prevent and diagnose.
 PHARMACODYNAMICS is the tudy of biochemical and physiological effects of
drugs; study of drugs mechanism of action.
 PHARMACOKINETICS is the study of the absorption, distribution, and
biotransformation (metabolism) and excretion of drugs.
 PHARMACOGNOSY is the study of drugs derived from herbal and other natural
sources.
 TOXICOLOGY - Study of poisons and poisoning.

b) Sources of Drug:
1. Plants
2. Animals
3. Minerals
4. Synthetic chemical

c) Drug Classification:
• Drugs are classified according to their effects on particular body systems, their
therapeutic uses.
A. PRESCRIPTION DRUGS
• Are those that have on their labels the prescription legend.
• May be prescribed by the physicians, dentists, veterinarians, or other
legally authorized health practitioner as part of their specific practice.
B. NON-PRESCRIPTION DRUGS
• The drugs that may be legally acquired by the client without the
prescription order.
• Also known as over the counter drugs (OTC)
C. INVESTIGATIONAL DRUGS
• A new drug which a manufacturer wishes to market.
• Must fulfill the requirements of FDA.
D. ORPHAN DRUG
• Are drugs that have been discovered but are not financially viable and
therefore have not been “adopted” by any drug company.
E. ELLICIT DRUG
• a.k.a. “street’ drugs are those which are used and/or distributed
illegally.

d) Legal Regulation of Drugs:

A. FDA Pregnancy Categories
B. Controlled Substances

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Joy Katrina O. Libatique, RN Module 1
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Pharmacology
A. FDA Pregnancy Categories

Category A

• Adequate studies in pregnant women have NOT demonstrated a risk in the

fetus in the first trimester of pregnancy and there is no evidence of risk in
later trimester.

Category B

• Animal studies have NOT demonstrated a risk for the fetus but there are No
adequate studies in pregnant women, or animal studies have shown an
adverse effect, but adequate studies in pregnant women have not
demonstrated a risk to the fetus during the first trimester, and there is no
evidence of risk on later trimester.

Category C

• Animal studies have shown an adverse effect on the fetus but there are no
adequate studies in humans, the benefits from the use of the drug in
pregnant women may be acceptable despite the potential risks, or there are no
animal reproduction studies and no adequate studies in humans.

Category D

• There is evidence of human fetal risk, but the potential benefits from the use
of the drug in pregnant women may be acceptable despite of its potential risks.

B. Controlled Substances

Schedule I

• Drugs that are not approved for medical use and have high abuse potentials:
heroin, lysergic acid diethylamide (LSD), peyote, mescaline,
tetrahydrocannabinol, marijuana.

Schedule II

• Drugs that are used medically and have high abuse potentials: opioid
analgesics (eg, codeine, hydromorphone, methadone, meperidine, morphine,
oxycodone, oxymorphone), central nervous system (CNS) stimulants (eg,
cocaine, methamphetamine, methylphenidate), and barbiturate sedative-
hypnotics (amobarbital, pentobarbital, secobarbital).

Schedule III

• Drugs with less potential for abuse than those in Schedules I and II, but abuse
may lead to psychological or physical dependence: an-drogens and anabolic
steroids, some CNS stimulants (eg, benzphetamine), and mixtures containing
small amounts of controlled substances (eg, codeine, barbiturates not listed in
other schedules).

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Schedule IV

• Drugs with some potential for abuse: benzodiazepines (eg, diazepam,

lorazepam, temazepam), other sedative-hypnotics (eg, phenobarbital, chloral
hydrate), and some prescription appetite suppressants (eg, mazindol,
phentermine).

Schedule V

• Products containing moderate amounts of controlled substances. They may be

dispensed by the pharmacist without a physician’s prescription but with
some restrictions regarding amount, record keeping, and other safeguards.
Included are antidiarrheal drugs, such as diphenoxylate and atropine
(Lomotil).

CLASSIFICATIONS

• Antipyretic
• Analgesics
• Antibiotics
• Antidepressants
• anti-hypertensives
• anti-diabetic
• Antihistamine
• Antitussive
• cholinergics
• Decongestants
• Diuretics
• Emetics
• Expectorants
• Hypnotics
• Laxatives
• Sedatives
• Tranquilizers
• Antipsychotic

DRUG NAMES

Individual drugs may have several different names, but the two most commonly used
are the GENERIC NAME and the TRADE NAME (also called the brand or proprietary
name).

a. The GENERIC NAME (eg, amoxicillin) is related to the chemical or official

name and is independent of the manufacturer.

b. The TRADE NAME is designated and patented by the manufacturer.

c. CHEMICAL NAME is the exact molecular formula of the drug; usually a long,
very difficult name to pronounce and of a little concern to the health care
worker.

d. OFFICIAL NAME is the name of the drug as it appears in the official reference,
the USP/NF; generally the same as the generic name.

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Joy Katrina O. Libatique, RN Module 1
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PRESCRIPTION AND NONPRESCRIPTION DRUGS

• Legally, consumers have two routes of access to therapeutic drugs:

1. PRESCRIPTION

2. OVER-THE-COUNTER (OTC)

DRUG APPROVAL PROCESSES

• The FDA (Food and Drug Administration) is responsible for assuring that new
drugs are safe and effective before approving the drugs and allowing them to
be marketed.

TESTING AND CLINICAL TRIALS

• The testing process begins with animal studies to determine potential uses
and effects.

• In Phase I, a few doses are given to a few healthy volunteers to determine safe
dosages, routes of administration, absorption, metabolism, excretion, and
toxicity.

• In Phase II, a few doses are given to a few subjects with the disease or
symptom for which the drug is being studied, and responses are compared with
those of healthy subjects.

• In Phase III, the drug is given to a larger and more representative group of
subjects.

• In phase IV, after a drug is approved for marketing, it enters a phase of

continual evaluation.

e) TERMS INDICATING DRUG ACTION

a. INDICATIONS
A list of medical conditions or diseases for which the drug is meant to be
used.
b. ACTIONS
A description of the cellular changes that occur as a result of the drug.
c. CONTRAINDICATIONS
A list of conditions for which the drug should not be given.
d. SIDE EFFECTS and ADVERSE REACTIONS
A list of possible unpleasant or dangerous effects, other than the desired
effects,
e. INTERACTIONS
A list of other drugs or foods that may alter the effects of the drug and
usually should not be given during the same course of therapy.

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Joy Katrina O. Libatique, RN Module 1
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Pharmacology
II. BASIC CONCEPTS AND PROCESSES

a. CELLULAR PHYSIOLOGY

• Cells are dynamic, busy, “factories”

b. DRUG TRANSPORT THROUGH CELL MEMBRANES

• Most drugs are given for effects on body cells that are distant from the sites of
administration (ie, systemic effects). To move through the body and reach
their sites of action, metabolism, and excretion drug molecules must cross
numerous cell membranes.

c. PHARMACOKINETICS

Pharmacokinetics involves drug movement through the body (ie, “what the body
does to the drug”) to reach sites of action, metabolism, and excretion.

1. ABSORPTION

• Absorption is the process that occurs from the time a drug enters the body to
the time it enters the bloodstream to be circulated.

PHYSICAL FACTORS INFLUENCING ABSORPTION:

1. BLOOD FLOW to the absorption site:

-blood flow to the intestine is much greater than the flow to the stomach;
thus absorption from the intestine is favored over that from the stomach.

2. TOTAL SURFACE AREA available for absorption:

-The absorption of the drug across the intestine is more efficient because
the intestine has a surface rich in microvilli.

3. CONTACT TIME at the absorption surface:

- anything that delays the transport of the drug from the stomach to the
intestine delays the rate of absorption of the drug.

BIOVAILABILITY

• Is the fraction of administered drug that reaches the systemic circulation.

2. DISTRIBUTION

• Distribution involves the transport of drug molecules within the body.

• Once a drug is injected or absorbed into the bloodstream, it is carried by the

blood and tissue fluids to its sites of pharmacologic action, metabolism, and
excretion

• Distribution depends largely on the adequacy of blood circulation.

• Drugs are distributed rapidly to organs receiving a large blood supply, such as
the liver, heart, and kidneys.

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Pharmacology
• Distribution to other internal organs, muscle, fat, and skin is usually
slower.

• Protein binding allows part of a drug dose to be stored and released as

needed.

• Some drugs also are stored in muscle, fat, or other body tissues and released
gradually when plasma drug levels fall.

• Drug distribution into the central nervous system (CNS) is limited because the
blood–brain barrier, which is composed of capillaries with tight walls, limits
movement of drug molecules into brain tissue.

• Drug distribution during pregnancy and lactation is also unique.

3. METABOLISM

• Metabolism is the method by which drugs are inactivated or bio transformed

by the body.

• Most often, an active drug is changed into one or more inactive metabolites,
which are then excreted.

• Some active drugs yield metabolites that are also active and that continue to
exert their effects on body cells until they are metabolized further or
excreted.

• Most drugs are lipid soluble, a characteristic that aids their movement across
cell membranes.

• However, the kidneys, which are the primary excretory organs, can excrete
only water-soluble substances.

• When drugs are given orally, they are absorbed from the GI tract and carried
to the liver through the portal circulation.

• Some drugs are extensively metabolized in the liver, with only part of a drug
dose reaching the systemic circulation for distribution to sites of action. This is
called the first-pass effect or presystemic metabolism.

• The LIVER is the major site of metabolism, but specific drugs may undergo
biotransformation in other tissues.

4. EXCRETION

• Excretion refers to elimination of a drug from the body.

• Effective excretion requires adequate functioning of the circulatory system and

of the organs of excretion.

• Most drugs are excreted by the kidneys and eliminated unchanged or as

metabolites in the urine.

• Some drugs or metabolites are excreted in bile, then eliminated in feces;

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• others are excreted in bile, reabsorbed from the small intestine, returned to
the liver (called enterohepatic recirculation),

• The lungs mainly remove volatile substances, such as anesthetic gases.

• The skin has minimal excretory function.

RENAL ELIMINATION OF DRUG

1. GLOMERULAR FILTRATION

• Drugs enter the kidney through renal arteries, which divide to form a
glomerular capillary plexus.

• Serum Drug Levels

A serum drug level is a laboratory measurement of the amount of a drug in the

blood at a particular time.

It reflects dosage, absorption, bioavailability, half-life, and the rates of

metabolism and excretion.

• A toxic concentration is an excessive level at which toxicity occurs.

Toxic concentrations may stem from a single large dose, repeated small doses,
or slow metabolism that allows the drug to accumulate in the body.

For most drugs, serum levels indicate the onset, peak, and duration of drug
action.

The drug level continues to climb as more of the drug is absorbed, until it
reaches its highest concentration and peak drug action occurs. Then, drug
levels decline as the drug is eliminated (ie, metabolized and excreted) from
the body.

• Serum Half-Life

Serum half-life, also called elimination half-life, is the time required for the
serum concentration of a drug to decrease by 50%. It is determined primarily
by the drug’s rates of metabolism and excretion. A drug with a short half-life
requires more frequent administration than one with a long half-life.

d. PHARMACODYNAMICS

• Pharmacodynamics involves drug actions on target cells and the resulting

alterations in cellular biochemical reactions and functions (ie, “what the drug
does to the body”).

• As previously stated, all drug actions occur at the cellular level.

VARIABLES THAT AFFECT DRUG ACTIONS

• Expected responses to drugs are largely based on those occurring when a

particular drug is given to healthy adult men (18 to 65 years of age) of
average weight (150 lb [70 kg]).

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Pharmacology
• However, other groups of people (eg, women, children, older adults, different
ethnic or racial groups, and clients with diseases or symptoms that the drugs
are designed to treat) receive drugs and respond differently than healthy
adult men.

DRUG-RELATED VARIABLES

** dose indicates the amount to be given at one time

** dosage refers to the frequency, size, and number of doses.

• Dosage is a major determinant of drug actions and responses, both therapeutic

and adverse.

- If dosage is too small or administered infrequently, no pharmacologic action

occurs. because the drug does not reach an adequate concentration at target
cells.
- If the amount is too large or administered too often, toxicity (poisoning) may
occur.

MINIMUM DOSE – a smallest amount of a drug that will produce a therapeutic

effect.

MAXIMUM DOSE – largest amount of a drug that will produce a desired effect
without producing symptoms of toxicity.

LOADING DOSE – initial high dose used to quickly elevate the level of the drug
in the blood (often followed by a series of lower doses)

MAINTENANCE DOSE – dose required to keep the drug blood level at a steady
state in order to maintain the desired effect.

TOXIC DOSE – amount of drug that will produce harmful effects or symptoms of
toxicity.

LETHAL DOSE – dose that can cause death.

THERAPEUTIC DOSE- dose that is customarily given; adjusted according to

variations from the norm.

e. ROUTE OF ADMINISTRATION:

There are two major routes of drug administration;

• ENTERAL
• PARENTERAL

a. ENTERAL

1. ORAL

- The most common route of drug administration.

2. SUBLINGUAL

- placement under the tongue.

3. RECTAL

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- both the sublingual and the rectal have the additional advantage that they
prevent the destruction of the drug by intestinal enzymes or low pH in the
stomach.

b. PARENTERAL

- IV (Intravenous) route is most effective and most rapid in producing drug

action.

- IM (Intramuscular) route also produces drug action within a few minutes.

- SQ Subcutaneous route requires absorption and is somewhat slower than the

IV route.

OTHERS:

1. INHALATION

2. INTRANASAL

3. INTRATHECAL

4. VAGINAL

5. TRANSDERMAL

6. TOPICAL

Drug–Diet Interactions

• Food may alter the absorption of oral drugs. In many instances, food slows
absorption by slowing gastric emptying time and altering GI secretions and
motility.

Drug–Drug Interactions

• The action of a drug may be increased or decreased by its interaction with

another drug in the body. Most interactions occur whenever the interacting
drugs are present in the body; some, especially those affecting the absorption
of oral drugs, occur when the interacting drugs are given at or near the same
time.

Increased Drug Effects

• Interactions that can increase the therapeutic or adverse effects of drugs are
as follows:

Additive effects

- Additive effects occur when two drugs with similar pharmacologic actions
are taken.

Synergism or potentiation

- Synergism or potentiation occurs when two drugs with different sites or

mechanisms of action produce greater effects when taken together than
either does when taken alone.

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Interference

- Interference by one drug with the metabolism or elimination of a second

drug may result in intensified effects of the second drug.

Displacement

- Displacement of one drug from plasma protein-binding sites by a second

drug increases the effects of the displaced drug. This increase occurs
because the molecules of the displaced drug, freed from their bound form,
become pharmacologically active.

Decreased Drug Effects

- Interactions in which drug effects are decreased are grouped under the
term antagonism.
- In some situations, a drug that is a specific antidote is given to antagonize
the toxic effects of another drug.
- Decreased intestinal absorption of oral drugs occurs when drugs combine to
produce nonabsorbable compounds.
- Activation of drug-metabolizing enzymes in the liver increases the
metabolism rate of any drug metabolized primarily by that group of
enzymes. Several drugs (eg, phenytoin, rifampin), ethanol, and cigarette
smoking are known enzyme inducers.
- Increased excretion occurs when urinary pH is changed and renal
reabsorption is blocked.

Client-Related Variables

• Age

-The effects of age on drug action are most pronounced in neonates, infants,
and older adults.

-Drug distribution, metabolism, and excretion differ markedly in neonates,

especially premature infants, because their organ systems are not fully
developed.

-Older infants (1 month to 1 year) reach approximately adult levels of protein

binding and kidney function, but liver function and the blood–brain barrier
are still immature.

-Children (1 to 12 years) experience a period of increased activity of drug-

metabolizing enzymes so that some drugs are rapidly metabolized and
eliminated.

- After approximately 12 years of age, healthy children handle drugs similarly

to healthy adults.

- In older adults (65 years and older), physiologic changes may alter all
pharmacokinetic processes.

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 Body Weight

-Body weight affects drug action mainly in relation to dose. The ratio between
the amount of drug given and body weight influences drug distribution and
concentration at sites of action.

• In general, people heavier than average need larger doses.

• Recommended doses for many drugs are listed in terms of grams or milligrams
per kilogram of body weight.

TOLERANCE AND CROSS-TOLERANCE

• Drug tolerance occurs when the body becomes accustomed to a particular drug
over time so that larger doses must be given to produce the same effects.

• Tolerance may be acquired to the pharmacologic action of many drugs,

especially opioid analgesics, alcohol, and other CNS depressants.

• Tolerance to pharmacologically related drugs is called cross-tolerance.

ADVERSE EFFECTS OF DRUGS

• the term adverse effects refers to any undesired responses to drug

administration, as opposed to therapeutic effects, which are desired
responses.

• Most drugs produce a mixture of therapeutic and adverse effects; all drugs can
produce adverse effects. Adverse effects may produce essentially any sign,
symptom, or disease process and may involve any body system or tissue.

• Some adverse effects occur with usual therapeutic doses of drugs (often called
side effects); others are more likely to occur and to be more severe with high
doses.

• Common or serious adverse effects include the following:

• CNS effects

• Gastrointestinal effects

• Hematologic effects

• Hepatotoxicity

• Nephrotoxicity

• Hypersensitivity

• Drug fever

• Drug dependence

• Carcinogenicity

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• Teratogenicity

Toxic Effects of Drugs

• Drug toxicity (also called poisoning, overdose, or intoxication) results from

excessive amounts of a drug and may cause reversible or irreversible
damage to body tissues.

• In some cases, the patient or someone accompanying the patient may

know the toxic agent (eg, accidental overdose of a therapeutic
drug, use of an illicit drug, a suicide attempt).

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