Introduction to

Pharmacology Course

Daverly M. Cañeda,
R.N., M.N.

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 Objectives
• Define the common terms related to Pharmacology.
• Explain how drugs are named.
• Explain the concepts of drugs in terms of pharmacokinetics,
pharmacodynamics and pharmacotherapeutics.
• Identify the common drug interactions.
• Identify the common patient variables affecting drug action.
• List the various routes of administration and the role of
nurses in drug administration.

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Definition of Pharmacology
• is the study of drugs and its origin,
chemical structure, preparation,
administration, action, metabolism and
excretion.

• The study of drugs that alter

functions of living organisms.

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Implication of Pharmacology
to Nursing

– Responsible for drug administration

– Responsible for the administration of

medications that they direct others to give.

– Ethical and legal responsibilities

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Basic Concepts of
Pharmacology
• Drugs
– are chemicals that
alter
physiochemical
processes in body
cells.
– They can stimulate
or inhibit normal
cellular functions.
– Used
interchangeably with
medicines.
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Drug Names
1. Generic or Nonproprietary Name:
name approved by the Medical or Pharmaceutical
Associations in the original country of manufacture
and is adopted by all countries.
e.g. Paracetamol
2. Brand name or trade name:
name given by the manufacturer of the drug
e.g. Adol or Panadol
3. Chemical name
name that describes the atomic or chemical structure
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Drug Names

Meperidine

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Demerol

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Ethyl-1-methyl-4-
phenylisonipecotate 7
hydrochloride
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Example
Exercise 1: Reading the Label

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Pharmacokinetics

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Pharmacokinetics-activities
within the body
• It includes:
• Absorption
• Distribution
• Metabolism
• Excretion
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 Absorption
• Involves the way a drug enters the body and passes
into the fluids and tissues.
– Passive transport
– Active transport
– Pinocytosis

• Rate of Absorption:
– Drug Solubility –
• water soluble drugs
• lipodystrophy
– Route of Administration – IV, IM, SC, Oral
– Degree of blood flow
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through the tissues
Factors affecting
Absorption
– Drug Solubility –
• water soluble drugs
• lipodystrophy
– Bioavailability- the extent to which active ingredients
are absorbed and transported to sites of action.
– pH
– Drug concentration
– Circulation to site of absorption
– Absorbing surface
– Route of administration
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– Presence of body conditions
 Distribution
• Is defined as the way the drug moves from the
circulating body fluids to its site of action.
Note: The greater the blood supply in a body organ,
the faster the medication is absorbed

– Therapeutic effect – certain blood level is

maintained for the drugs to be effective.
– Toxic effect - when blood level increase
significantly over the therapeutic level.

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 Bioavailability
• is defined as the extent to which active ingredients are
absorbed and transported to sites of action.
• Factors
1. Drug solubility
2. Pharmaceutical formulation
3. pH
4. Food

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Metabolism or
Biotransformation
• is defined as the process by which drug is
converted by the liver to inactive compounds
through a series of chemical reactions.

– Plasma, kidneys and membranes of intestines.

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Excretion
• Is the elimination of drugs from the
body

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 Half-life
• Refers to the time required for the body to eliminate 50% of
the drug.
– It is important in planning the frequency of dosing.

• Short half-life (2-4 hours) : needs to be given frequently

• Long half life: (21-24 hours): requires less frequent dosing

Note: It takes 5 to 6 half lives to eliminate approximately 98% of a drug from

the body

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 Half-life
• Liver and kidney disease patients may have
problems of excreting a drug.

• Difficulty in excreting a drug increases the half-life

and increases the risk of toxicity.

• Implication: may require frequent diagnostic tests

and measuring renal and hepatic function.

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Drugs and the body

Pharmacodynamics and
Pharmacokinetics
 Definition of terms
absorption: what happens to a drug from the time it enters
the body until it enters the circulating fluid; intravenous
administration causes the drug to directly enter the circulating
blood, bypassing the many complications of absorption from
other routes
active transport: the movement of substances across a cell
membrane against the concentration gradient; this process
requires the use of energy
chemotherapeutic agents: synthetic chemicals used to
interfere with the functioning of foreign cell populations,
causing cell death; this term is frequently used to refer to the
drug therapy of neoplasms, but it also refers to drug therapy
affecting any foreign cell
critical concentration: the concentration a drug must reach in
the tissues that respond to the particular drug to cause the
desired therapeutic effect
distribution: movement of a drug to body tissues; the places
where a drug may be distributed depend on the drug’s solubility,
perfusion of the area, cardiac output, and binding of the drug to
plasma proteins
enzyme induction: process by which the presence of a
chemical that is biotransformed by a particular enzyme system
in the liver causes increased activity of that enzyme system
excretion: removal of a drug from the body; primarily occurs in
the kidneys, but can also occur through the skin, lungs, bile, or
feces
first-pass effect: a phenomenon in which drugs given orally
are carried directly to the liver after absorption, where they may
be largely inactivated by liver enzymes before they can enter
the general circulation; oral drugs frequently are given in higher
doses than drugs given by other routes because of this early
breakdown
glomerular filtration: the passage of water and water-soluble
components from the plasma into the renal tubule
half-life: the time it takes for the amount of drug in the body to
decrease to one half of the peak level it previously achieved
hepatic microsomal system: liver enzymes tightly packed
together in the hepatic intracellular structure, responsible for the
biotransformation of chemicals, including drugs
loading dose: use of a higher dose than what is usually used
for treatment to allow the drug to reach the critical concentration
sooner
passive diffusion: movement of substances across a
semipermeable membrane with the concentration gradient; this
process does not require energy
pharmacodynamics: the study of the interactions between the
chemical components of living systems and the foreign
chemicals, including drugs, that enter living organisms; the way
a drug affects a body
pharmacogenomics: the study of genetically determined
variations in the response to drugs
pharmacokinetics: the way the body deals with a drug,
including absorption, distribution, biotransformation, and
excretion
placebo effect: documented effect of the mind on drug therapy;
if a person perceives that a drug will be effective, the drug is
much more likely to actually be effective
receptor sites: specific areas on cell membranes that react with
certain chemicals to cause an effect within the cell
selective toxicity: property of a chemotherapeutic agent that
affects only systems found in foreign cells without affecting
healthy human cells (e.g., specific antibiotics can affect certain
proteins or enzyme systems used by bacteria but not by human
cells)
 Pharmacodynamics

Cellular Response/
Drug
Components Drug Effect

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 PHARMACODYNAMICS
Pharmacodynamics is the study of the
interactions between the chemical
components of living systems and the foreign
chemicals, including drugs, that enter those
systems. All living organisms function by a
series of complicated, continuous chemical
reactions. (Karch)
“what the drug does to the body”
 Drugs usually work in one of four
ways:
1. To replace or act as substitutes for missing
chemicals
2. To increase or stimulate certain cellular activities
3. To depress or slow cellular activities
4. To interfere with the functioning of foreign cells,
such as invading microorganisms or neoplasms
leading to cell death (drugs that act in this way are
called chemotherapeutic agents).
(KARCH)
 Mechanism of Drug Action
1. Stimulation
2. Depression
3. Irritation
4. Replacement
5. Cytotoxic action
6. Antimicrobial action
7. Modification of the immune status
(MCCUISTION)
Stimulation: drug that stimulates enhances intrinsic activity (e.g.,
adrenergic drugs that increases heart rate, sweating and respiratory rate
during fight-or-flight response
Depression: Depressant drugs decrease neural activity and bodily
functions (e.g., barbiturates and opiates)
Irritation: Drugs that irritate have a noxious effect, such as
astringents, laxatives irritate the inner wall of the colon, thus
increasing peristalsis and defecation. This can occur on all types of
body tissues in the body and may result in inflammation, corrosion
and necrosis of cells
Replacement: drugs may be used for replacement when there is
deficiency of natural substances like hormones ,metabolites or
nutrients ,e.g., insulin in diabetes, iron in anemia ,vitamin C in
scurvy.
Cytotoxic action: drugs selectively kill invading parasites
or cancers.
Antimicrobial action: drugs prevent, inhibit, or kill
infectious organism
Modification of immune status: vaccines and sera act by
improving our immunity while immune-suppressants act
by depressing immunity, e.g., glucocorticoids, interferons
and methotrexate
RECEPTOR SITES
Many drugs are thought to act at specific areas on cell
membranes called receptor sites. The receptor sites react
with certain chemicals to cause an effect within the cell. In
many situations, nearby enzymes break down the reacting
chemicals and open the receptor site for further stimulation.
To better understand this process, think of how a key works in
a lock. The specific chemical (the key) approaches a cell
membrane and finds a perfect fit (the lock) at a receptor site
The interaction between the chemical and the receptor site
affects enzyme systems within the cell. The activated enzyme
systems then produce certain effects, such as increased or
decreased cellular activity, changes in cell membrane
permeability, or alterations in cellular metabolism.
 Drug Attachment
Medication chemically binds to specific
sites called “receptor sites”

– Agonist-chemical fits at receptor site well

– Antagonist- a chemical blocks another
chemical from getting to a receptor
– Partial agonist - attach to the receptor
but only produce a small effect

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Some drugs interact directly with receptor sites to cause the same activity
that natural chemicals would cause at that site. These drugs are
called agonists. For example, insulin reacts with specific insulin-receptor
sites to change cell membrane permeability, thus promoting the movement
of glucose into the cell.
MAO an enzyme involved in removing the neurotransmitters
norepinephrine, serotonin and dopamine in the brain
Norepinephrine is a naturally occurring chemical in the body that acts as
both a stress hormone and neurotransmitter (a substance that sends
signals between nerve cells). It's released into the blood as a stress
hormone when the brain perceives that a stressful event has occurred
Serotonin is a chemical that has a wide variety of functions in the human
body. It is sometimes called the happy chemical, because it contributes to
wellbeing and happiness. It is mainly found in the brain, bowels, and blood
platelets.
Other drugs act to prevent the breakdown of natural chemicals that are
stimulating the receptor site. For example, monoamine oxidase inhibitors
(MAOIs) block the breakdown of norepinephrine by the enzyme MAO.
(Normally, MAO breaks down norepinephrine, removes it from the receptor
site, and recycles the components to form new norepinephrine.) The
blocking action of MAO inhibitors allows norepinephrine to stay on the
receptor site, stimulating the cell longer and leading to prolonged
norepinephrine effects. Those effects can be therapeutic (e.g., relieving
depression) or adverse (e.g., increasing heart rate and blood pressure).
Selective serotonin reuptake inhibitors (SSRIs) work similarly to MAO
inhibitors in that they also exert a blocking action. Specifically, they block
removal of serotonin from the nerve synapse, allowing it to remain in the
synapse longer, leading to further stimulation of receptor sites. This action
leads to prolonged stimulation of certain brain cells, which is thought to
provide relief from depression.
Some drugs react with receptor sites to block normal stimulation, producing
no effect. For example, curare (a drug used on the tips of spears by
inhabitants of the Amazon basin to paralyze prey and cause death) occupies
receptor sites for acetylcholine, which is necessary for muscle contraction
and movement. By blocking the action of acetylcholine at this receptor site,
curare prevents muscle stimulation, causing paralysis. Curare is said to
be a competitive antagonist of acetylcholine
Still other drugs react with specific receptor sites on a cell and, by reacting
there, prevent the reaction of another chemical with a different receptor
site on that cell. Such drugs are called noncompetitive antagonists. For
some drugs the actual mechanisms of action are unknown. Speculation
exists, however, that many drugs use receptor site mechanisms to bring
about their effects.
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 Nonspecific and Nonselective Drug Effects
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
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
 DRUG-ENZYMES INTERACTIONS
Drugs also can cause their effects by interfering with
the enzyme systems that act as catalysts for various
chemical reactions. Enzyme systems work in a
cascade fashion, with one enzyme activating another,
and then that enzyme activating another, until a
cellular reaction eventually occurs. If a single step in
one of the many enzyme systems is blocked, normal
cell function is disrupted. Acetazolamide (Diamox) is
a diuretic that blocks the enzyme carbonic
anhydrase, which subsequently causes alterations in
the hydrogen ion and water exchange system in the
kidney, as well as in the eye.
 SELECTIVE TOXICITY
Ideally, all chemotherapeutic agents would act only on
enzyme systems that are essential for the life of a
pathogen or neoplastic cell and would not affect
healthy cells. The ability of a drug to attack only those
systems found in foreign cells is known as selective
toxicity. Penicillin, an antibiotic used to treat bacterial
infections, has selective toxicity. It affects an enzyme
system unique to bacteria, causing bacterial cell death
without disrupting normal human cell functioning.
SELECTIVE TOXICITY
Unfortunately, most other chemotherapeutic agents
also destroy normal human cells, causing many of the
adverse effects associated with antipathogen and
antineoplastic chemotherapy. Cells that reproduce or
are replaced rapidly (e.g., bone marrow cells,
gastrointestinal [GI] cells, hair follicles) are more
easily affected by these agents. Consequently, the
goal of many chemotherapeutic regimens is to deliver
a dose that will be toxic to the invading cells yet
cause the least amount of toxicity to the host.
 Basics of Drug Action
Desired action – the expected response of a
medication
Side effects –known and frequently experienced,
expected reaction to drug.
Adverse reaction –unexpected, unpredictable
reactions that are not related too usual effects of a
normal dose of the drug.
Primary Effects - drug’s desired or therapeutic effect
Secondary Effects – all other effects whether
desirable or undesirable. 51
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.
Drug Interaction
• Takes place when one drug alters the
action of another drug.
• Some are helpful but often produce
adverse effects.

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Common Drug Interactions

• Additive effect- takes place when 2 drugs

are given together & double the effect is
produced.

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Alcohol + aspirin= Pain relief

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Common Drug Interactions

• Antagonistic effect- takes place when 1

drug interferes with the action of another
drug.

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– Protamine sulphate to counteract heparin
toxicity

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 Common Drug Interactions

• Displacement effect - takes place

when 1 drug replaces another at the
drug receptor site, increasing the
effect of the 1st drug.

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Common Drug Interactions

• Incompatibility –occurs when 2 drugs

mixed together in a syringe produce a
chemical reaction so they cannot be
given.
e.g. Protamine sulfate & vitamin K

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 Common Drug Interactions

• Interference- occurs when 1 drug promotes

the rapid excretion of another, thus reducing
the activity of the 1st.

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• Synergistic effect takes place when the
effect of 2 drugs taken at the same time is

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greater than the sum of each drug given
alone.

E.g. combining diuretics & adrenergic

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blockers to lower the BP

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 age

Body wt illness

Pt.
variables

Cumulative
Dependence
effect

Psychological
overlay
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Session 1Pharmacology
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Pharmacotherapeutics
 Pharmacotherapeutics
• Is defined as the use of drugs to treat

diseases.
 Depends on:
 Severity
 Urgency
 Prognosis of patient’s condition

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Routes of Drug
Administration
 1: Enteral Medications
• administered directly into the G.I.T. through
the oral, nasogastric (NG) or rectal routes

Advantages:
Convenience for nurse & patient
Most medications are available in oral route
Inexpensive to make oral preparations
Can be removed by gastric lavage or make to
vomit

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 Disadvantages
• cannot be administered to very
nauseated/vomiting or unconscious
persons
• some loose their effectiveness if mixed
with gastric secretions
• onset of action may vary due to changes in
absorption in the GIT

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 Forms of Oral Medication
• Capsules-are gelatin containers that hold
powder or liquid medicine.
• Elixirs- clear liquids made up of drugs dissolved
in alcohol & water with coloring & flavoring
agents added.
• Emulsions-are solutions that have small
droplets of water & medication dispersed in oil,
or oil & medication dispersed in water.

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 Forms of Oral Medication
• Lozenges- are medicines mixed with a
hard sugar base to produce a small,

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hard preparation of various shapes &
sizes.

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• Suspensions- are liquids w/ solid,
insoluble drug particles dispersed

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throughout.
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Forms of Oral Medication
• Syrups-are liquids w/ a high sugar content
designed to disguise the bitter taste of a
drug. Pediatric use.

• Tablets-dried, powdered drugs compressed

into small shapes.

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Session 1Pharmacology
 2.Parenteral Administration
• Reasons:
1. When the patient cannot take an oral
medication
2. When the medication must be given quickly
3. When medication might be destroyed by
gastric enzymes
4. When medication must be given at a
controlled rate
5. When the medication is not available in an
enteral form.

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 Parenteral Medications
• INTRAMUSCULAR – 90 °
– Provides faster medication absorption because of
muscle’s greater vascularity

• SUBCUTANEOUS- 45 °
– Placing medications in the loose connective tissue
under the dermis
• INTRADERMAL- 15 °

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Other Routes of
Administration
• Topical administration – skin
– Cleanse
– Soften
– Disinfect
– Lubricate
– E.g. clotrimazole –cream
dermatophytosis
– atropine- eye-dilate the pupil
• Transdermal route -
nitroglycerin (skin patch) systemic
vasodilation in angina

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Session 1Pharmacology
Other Routes of
Administration
• Inhalation – provides rapid delivery of
drugs to a large area of mucus
membranes & tissues of the respiratory
system.
– Anesthesia
– Bronchodilators
• Intranasal – desmopressin for diabetes
insipidus
– Calcitonin- a peptide hormone for tx of
osteoporosis

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Session 1Pharmacology
 Other Routes of
Administration
• Intrathecal injection- introduction of hypodermic
needle into the subarachnoid space for the purpose
of instilling a material for diffusion throughout the
spinal fluid.

• Intraventricular- space into the ventricle

– Both gains access to the CSF e.g. amphotericin B

–in meningitis

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Ms. Maria Jose
First-Pass Effect
• Drugs taken orally are absorbed from the small
intestine directly into the portal venous system. The
portal veins deliver these absorbed molecules into
the liver, which immediately transforms most of the
chemicals delivered to it by a series of liver
enzymes.
active
metabolites

Inactive (excreted)
Protein Binding
• Most drugs are bound to some extent to
proteins in the blood to be carried into
circulation.

• The protein-drug complex is relatively

large & cannot enter into capillaries & then
into tissues to react. The drug must be freed
from the protein’s binding site at the tissues.
 Protein Binding
• Tightly bound – released very slowly. these
drugs have very long duration of action (not
freed to be broken down or excreted) , slowly
released into the reactive tissue.

• Loosely bound – tend to act quickly and

excreted quickly

• Compete for protein binding sites – alters

effectiveness or causing toxicity when 2 drugs
are given together.
 Half-Life
• Half life of a drug is the time it takes for the
amount of drug in the body to decrease to one-
half of the peak level it previously achieved.
• e.g.
– 20 mg of a drug with half-life of 2 hours, 10 mg of the
drug will remain 2 hours after administration. Two
hours later, 5 mg will be left (one-half of the previous
level); in 2 more hours, only 2.5 mg will remain.
Why to know half-life?
– To determine the appropriate timing for a
drug dose or
– determining the duration of a drug’s effect
on the body.
 Determining the Impact of
Half-Life on Drug Levels
• A patient is taking a drug that has a half-
life of 12 hours. You are trying to
determine when a 50-mg dose of the drug
will be gone from the body.
– In 12 hours, half of the 50 mg (25 mg) would be in
the body

– In another 12 hours (24 hours) half of 25 mg (12.5

mg) would remain in the body.
Determining the Impact of
Half-Life on Drug Levels
– After 36 hours, half of 12.5 mg (6.25 mg)
would remain
– After 48 hours, half of the 6.25 mg
(3.125 mg) would remain
– After 60 hours, half of the 3.125 mg
(1.56 mg) would remain
– After 72 hours, half of the 1.56 mg (0.78
mg) would remain
Determining the Impact of
Half-Life on Drug Levels
– After 84 hours, half of the 0.78 mg (0.39
mg) would remain
– Twelve more hours (for a total of 96
hours) would reduce the drug amount
to 0.195 mg
– Finally,12 more hours (108 hours)
would reduce the amount of the drug
into the body to 0.097 mg, which is
negligible
– Therefore, it would take 4 ½ to 5 days to
clear the drug from the body.