PHARMACOLOGY (NCM 106)

Placement: FIRST SEMESTER

Course Credits: 3 UNITS

MODULE # 1

Introduction to Pharmacology

Learning Objectives:
1. Integrate knowledge of physical, social, natural and health sciences and humanities
in nursing pharmacology.
2. Apply appropriate nursing concepts and actions holistically and comprehensively:
a. Discuss the pharmacodynamics of specific drugs

References
Linda E. McCuistion, J. L. (2014). Pharmacology_ A Patient-Centered Nursing Process Approach. St.
Louis, Missouri: Saunders.

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Content:

INTRODUCTION TO PHARMACOLOGY

I. DEFINITION OF TERMS

 PHARMACOLOGY is the science that deals with the study of drugs and their interaction with the
living systems.
 The word Pharmacology is derived from Greek – pharmacon means drug and logos means study.

DRUG:
 Drug is a substance used in the diagnosis, prevention or treatment of disease.

PHARMACOKINETICS:
 Pharmacokinetics is the study of the absorption, distribution, metabolism and excretion of drugs
[i.e. what the body does to the drug (in greek kinesis = movement)]

PHARMACODYNAMICS:
 Pharmacodynamics is the study of the effect of the drugs on the body and their mechanism of
action, i.e. what the drug does to the body.

THERAPEUTICS:
 Therapeutics deals with the use of drugs in the prevention and treatment of disease.

TOXICOLOGY:
 Toxicology deals with the adverse effect of the drug and also the study of poisons, i.e. detection,
prevention and treatment of poisoning (Toxicon =poison in Greek).

CHEMOTHERAPY:
 Chemotherapy is the use of chemicals for the treatment of infections; the term now also includes
the use of chemical to treat malignancies.

PHARMACY:
 Pharmacy is the science of identification, compounding and dispensing of drugs. It also includes
collection, isolation, purification, synthesis and standardization of medical substances.

SOURCES OF DRUGS

A. NATURAL SOURCES:
1. PLANTS (Atropine, Morphine, Quinine, digoxine, pilocarpine, physostigmine).
2. ANIMALS (Insulin, heparin, gonadotropins and antitoxic sera).
3. MINERALS (Magnesium sulphate, Aluminium hydroxide, iron, sulphur and radioactive
isotopes).
4. MICROORGANISMS (obtained from some bacteria and fungi; pencillins,
cephalosporins, tetracycline and other antibiotics.
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II. DRUG CLASSIFICATIONS

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 fulfil 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.

Drugs are also classified according to their clinical indication and chemical action.
• Antipyretic • Antitussive • Hypnotics
• Analgesics • Cholinergics • Laxatives
• Antibiotics • Anticholinergics • Sedatives
• Antidepressants • Decongestants • Tranquilizers
• Anti-Hypertensives • Diuretics • Antipsychotic
• Anti-Diabetic • Emetics
• Antihistamine • Expectorants

III. DRUG STANDARDS AND DRUG INFORMATION

LEGAL REGULATION OF DRUGS

A. FDA Pregnancy Categories

1. 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.

2. 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

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 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.

3. 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.

4. 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
1. Schedule I
• Drugs that are not approved for medical use and have high abuse potentials: heroin,
lysergic acid diethylamide (LSD), peyote, mescaline, tetrahydrocannabinol,
marijuana.

2. 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).

3. 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).

4. 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).

5. 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).

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 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).
• The GENERIC NAME (eg, amoxicillin) is related to the chemical or official name and is
independent of the manufacturer.
• Differentiated from Trade Name by initial lowercase letter; NOT CAPITALIZED…
• 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.

PRESCRIPTION AND NONPRESCRIPTION DRUGS

• Legally, consumers have two routes of access to therapeutic drugs.
• One route is by PRESCRIPTION or order from a licensed health care provider, such as a
physician, dentist, or nurse practitioner.
• The other route is by OVER-THE-COUNTER (OTC) purchase of drugs that do not require a
prescription.

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.

TERMS INDICATING DRUG ACTION

INDICATIONS
• A list of medical conditions or diseases for which the drug is meant to be used.

ACTIONS
• A description of the cellular changes that occur as a result of the drug.

CONTRAINDICATIONS
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 • A list of conditions for which the drug should not be given.

SIDE EFFECTS and ADVERSE REACTIONS

• A list of possible unpleasant or dangerous effects, other than the desired effects.

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.

IV. PHARMACODYNAMICS

• Pharmacodynamics involves drug actions on target cells and the resulting alterations in
cellular biochemical reactions and functions (i.e. “what the drug does to the body”).
• As previously stated, all drug actions occur at the cellular level.

PHARMACODYNAMIC PHASE

Pharmacodynamics is the study of the way drugs affect the body. Drug response can cause a
primary or secondary physiologic effect or both. The primary effect is desirable, and the secondary
effect may be desirable or undesirable. An example of a drug with a primary and secondary effect is
diphenhydramine (Benadryl), an antihistamine. The primary effect of diphenhydramine is to treat
the symptoms of allergy, and the secondary effect is a central nervous system depression that
causes drowsiness. The secondary effect is undesirable when the patient drives a car, but at
bedtime it could be desirable because it causes mild sedation.

Dose Response and Maximal Efficacy

Dose response is the relationship between the minimal versus the maximal amount of drug dose
needed to produce the desired drug response. Some patients respond to a lower drug dose, whereas
others need a high drug dose to elicit the desired response. The drug dose is usually adjusted to
achieve the desired drug response.

All drugs have a maximum drug effect (maximal efficacy). For example, morphine and tramadol
hydrochloride (Ultram) are prescribed to relieve pain. The maximum efficacy of morphine is greater
than tramadol hydrochloride, regardless of how much tramadol hydrochloride is given. The pain
relief with the use of tramadol hydrochloride is not as great as it is with morphine.

Onset, Peak, and Duration of Action

One important aspect of pharmacodynamics is knowing the drug’s onset, peak, and duration of
action. Onset of action is the time it takes to reach the minimum effective concentration (MEC) after
a drug is administered. Peak action occurs when the drug reaches its highest blood or plasma
concentration.

Duration of action is the length of time the drug

has a pharmacologic effect. Figure 1-6 illustrates
the areas in which onset, peak, and duration of
action occur. Some drugs produce effects in
minutes, but others may take hours or days. A
time-response curve evaluates three parameters
of drug action: the onset of drug action, peak

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action, and duration of action. Figure 1-6 indicates these parameters by using T (time) with
subscripts (e.g., T0, T1, T2, T3).

It is necessary to understand the time response in relationship to drug administration. If the drug
plasma or serum level decreases below threshold or MEC, adequate drug dosing is not achieved; too
high a drug level above the minimum toxic
concentration (MTC) can result in toxicity.

Receptor Theory
Drugs act through receptors by binding to the receptor to
produce (initiate) a response or to block (prevent) a response.
The activity of many drugs is determined by the ability of the
drug to bind to a specific receptor. The better the drug fits at
the receptor site, the more biologically active the drug is. It is
similar to the fit of the right key in a lock. Figure 1-7
illustrates a drug binding to a receptor.

Most receptors, which are protein in nature, are found in

cell membranes. Drug-binding sites are primarily on
proteins, glycoproteins, proteolipids, and enzymes. There are
four receptor families: (1) kinase-linked receptors, (2) ligand-gated ion channels, (3) G protein–
coupled receptor systems, and (4) nuclear receptors. The ligand-binding domain is the site on the
receptor at which drugs bind.
• Kinase-linked receptors. The ligand-binding domain for drug binding is on the cell surface.
The drug activates the enzyme (inside the cell), and a response is initiated.
• Ligand-gated ion channels. The channel spans the cell membrane and, with this type of
receptor, the channel opens, allowing for the flow of ions into and out of the cells. The ions
are primarily sodium and calcium.
• G protein–coupled receptor systems. There are three components to this receptor response: (1)
the receptor, (2) the G protein that binds with guanosine triphosphate (GTP), and (3) the
effector that is either an enzyme or an ion channel. The system works as follows:

• Nuclear receptors. Found in the cell nucleus (not on the surface) of the cell membrane.
Activation of receptors through the transcription factors is prolonged. With thefirst three
receptor groups, activation of the receptors is rapid.

Agonists and Antagonists

Drugs that produce a response are called agonists, and drugs that block a response are called
antagonists. Epinephrine (Adrenalin) stimulates beta1 and beta2 receptors, so it is an agonist.
Atropine, an antagonist, blocks the histamine (H2) receptor, thus preventing excessive gastric acid
secretion. The effects of an antagonist can be determined by the inhibitory (I) action of the drug
concentration on the receptor site. IC50 is the antagonist drug concentration required to inhibit
50% of the maximum biological response.

Nonspecific and Nonselective Drug Effects

Many agonists and antagonists lack specific and selective effects. A receptor produces a variety of
physiologic responses, depending on where in the body the receptor is located. Cholinergic receptors

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are located in the bladder, heart, blood vessels, stomach, bronchi, and eyes. A drug that stimulates
or blocks the cholinergic receptors affects all anatomic sites of location. Drugs that affect various
sites are nonspecific drugs and have properties of nonspecificity. Bethanechol (Urecholine) may be
prescribed for postoperative urinary retention to increase bladder contraction. This drug stimulates
the cholinergic receptor located in the bladder, and urination occurs by strengthening bladder
contraction. Because bethanechol affects the cholinergic receptor, other cholinergic sites are also
affected. The heart rate decreases, blood pressure decreases, gastric acid secretion increases, the
bronchioles constrict, and the pupils of the eye constrict (Figure 1-8). These other effects may be
either desirable or harmful. Drugs that evoke a variety of responses throughout the body have a
nonspecific response.

Drugs may act at different receptors. Drugs that affect various receptors are nonselective drugs or
have properties of nonselectivity. Chlorpromazine (Thorazine) acts on the norepinephrine,
dopamine, acetylcholine, and histamine receptors, and a variety of responses result from action at
these receptor sites. Epinephrine acts on the alpha1, beta1, and beta2 receptors (Figure 1-9). Drugs
that produce a response but do not act on a receptor may act by stimulating or inhibiting enzyme
activity or hormone production.

Categories of Drug Action

The four categories of drug action include (1) stimulation or depression, (2) replacement, (3)
inhibition or killing of organisms, and (4) irritation. In drug action that stimulates, the rate of cell
activity or the secretion from a gland increases. In drug action that depresses, cell activity and
function of a specific organ are reduced. Replacement drugs such as insulin replace essential body
compounds. Drugs that inhibit or kill organisms interfere with bacterial cell growth (e.g., penicillin
exerts its bactericidal effects by blocking the synthesis of the bacterial cell wall). Drugs also can act
by the mechanism of irritation (e.g., laxatives irritate the inner wall of the colon, thus increasing
peristalsis and defecation).

Therapeutic Index and Therapeutic Range (Therapeutic Window)

The safety of drugs is a major concern. The therapeutic index (TI) estimates the margin of safety of
a drug through the use of a ratio that measures the effective (therapeutic) dose (ED) in 50% of
people (ED50) and the lethal dose (LD) in 50% of people (LD50) (Figure 1-10). The closer the ratio is
to 1, the greater the danger of toxicity.

TI = LD50
ED50

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In some cases, the ED may be 25% (ED25) or 75% (ED75). Drugs with a low therapeutic index have
a narrow margin of safety (Figure 1-11, A). Drug dosage might need adjustment, and plasma
(serum) drug levels need to be monitored because of the small safety range between the ED and LD.
Drugs with a high therapeutic index have a wide margin of safety and less danger of producing toxic
effects (Figure 1-11, B). Plasma (serum) drug levels do not need to be monitored routinely for drugs
with a high TI.

The therapeutic range (therapeutic window) of a drug concentration in plasma is the level of drug
between the minimum effective concentration in the plasma for obtaining desired drug action and
the minimum toxic concentration (the toxic effect). When the therapeutic range is given, it includes
both protein-bound and unbound portions of the drug. If the therapeutic range is narrow, such as
for digoxin (0.5 to 1 ng/mL), the plasma drug level should be monitored periodically to avoid drug
toxicity. Monitoring the therapeutic range is not necessary if the drug is not considered highly toxic.
When the therapeutic range is given, it includes both protein-bound and unbound portions of the

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 drug. Table 1-3 lists the therapeutic ranges and
toxic levels for anticonvulsants.

Peak and Trough Drug Levels

Peak drug levels indicate the rate of absorption of
the drug, and trough drug levels indicate the rate
of elimination of the drug. Peak and trough levels
are requested for drugs that have a narrow
therapeutic index and are considered toxic, such
as the aminoglycoside antibiotics (Table 1-4). If

either the peak or trough level is too high, toxicity can occur. If the peak is too low, no therapeutic
effect is achieved. Peak drug level is the highest plasma concentration of drug at a specific time.
Peak drug levels indicate the rate of absorption. If the drug is given orally, the peak time might be 1
to 3 hours after drug administration. If the drug is given IV, the peak time might occur in 10
minutes. If a peak drug level is ordered, a blood sample should be drawn at the proposed peak time,
according to the route of administration. The trough drug level is the lowest plasma concentration
of a drug, and it measures the rate at which the drug is eliminated. Trough levels are drawn
immediately before the next dose of drug is given, regardless of route of administration.

Loading Dose
When immediate drug response is desired, a large initial dose, known as the loading dose, of drug
is given to achieve a rapid minimum effective concentration in the plasma. After a large initial dose,
a prescribed dosage per day is ordered. Digoxin (Digitek, Lanoxicaps, Lanoxin), a digitalis
preparation, requires a loading dose when first prescribed. Digitalization is the process by which the
minimum effective concentration level for digoxin is achieved in the plasma within a short time.

Side Effects, Adverse Reactions, and Toxic Effects

Side effects are physiologic effects not related to desired drug effects. All drugs have desirable or
undesirable side effects. Even with a correct drug dosage, side effects occur and are predicted. Side
effects result mostly from drugs that lack specificity, such as bethanechol (Urecholine). In some
health problems, side effects may be desirable (e.g., the use of diphenhydramine HCl [Benadryl] at
bedtime when its side effect of drowsiness is beneficial). At times, however, side effects are called
adverse reactions. The terms side effects and adverse reactions are sometimes used interchangeably
in the literature and in speaking, but they are different. Some side effects are expected as part of
drug therapy. The occurrence of these expected but undesirable side effects is not a reason to
discontinue therapy. The nurse’s role includes teaching patients to report any side effects. Many
can be managed with dosage adjustments, changing to a different drug in the same class of drugs,
or implementing other interventions. It is important to know that the occurrence of side effects is
one of the primary reasons patients stop taking the prescribed medication. Adverse reactions are
more severe than side effects. They are a range of untoward effects (unintended and occurring at
normal doses) of drugs that cause mild to severe side effects, including anaphylaxis (cardiovascular
collapse). Adverse reactions are always undesirable. Adverse effects must always be reported and
documented because they represent variances from planned therapy. Toxic effects, or toxicity, of
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a drug can be identified by monitoring the plasma (serum) therapeutic range of the drug. However,
for drugs that have a wide therapeutic index, the therapeutic ranges are seldom given. For drugs
with a narrow therapeutic index, such as aminoglycoside antibiotics and anticonvulsants, the
therapeutic ranges are closely monitored. When the drug level exceeds the therapeutic range,
toxic effects are likely to occur from overdosing or drug accumulation.

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