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What is PHARMACOLOGY?
OVERVIEW
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
Study of biochemical and
physiological effects of drugs; study
of drugs mechanism of action.
PHARMACOKINETICS
Study of the absorption, distribution,
and biotransformation (metabolism)
and excretion of drugs.
PHARMACOGNOSY
Study of drugs derived from herbal
and other natural sources.
TOXICOLOGY
Study of poisons and poisoning.
involves the study of the adverse
effects of chemical substances on
living organisms and the practice of
diagnosing and treating exposures to
toxins and toxicants.
SOURCES OF DRUGS
Plants
Animals
Minerals
Synthetic chemical
Microbiological
SOURCES OF DRUGS
Plant Sources:
◦ Plant source is the oldest source of
drugs.
◦ Most of the drugs in ancient times were
derived from plants.
◦ Almost all parts of the plants are used
i.e. leaves, stem, bark, fruits and roots.
SOURCES OF DRUGS
Plant Sources:
◦ The leaves of Digitalis Purpurea are
the source of Digitoxin and
Digoxin, which are cardiac
glycosides.
◦ Poppy papaver somniferum gives
morphine (opoid)
SOURCES OF DRUGS
Animal Sources:
◦ Pancreas is a source of Insulin, used
in treatment of Diabetes.
◦ Cod liver is used as a source of
vitamin A and D
◦ Blood of animals is used in
preparation of vaccines.
SOURCES OF DRUGS
Mineral Sources:
◦ Iron is used in treatment of iron
deficiency anemia.
◦ Gold salts are used in the
treatment of rheumatoid arthritis.
◦ Iodine is antiseptic. Iodine
supplements are also used.
SOURCES OF DRUGS
Synthetic Sources:
◦ When the nucleus of the drug from
natural source as well as its chemical
structure is altered,
◦ majority of drugs used in clinical
practice are prepared synthetically,
such as aspirin, oral antidiabetics,
antihistamines, amphetamine,
chloroquine etc.
SOURCES OF DRUGS
Microbiological Sources:
◦ Penicillium notatum is a fungus
which gives penicillin.
◦ Actinobacteria give Streptomycin.
◦ Aminoglycosides such as gentamicin
and tobramycin are obtained from
streptomycis and micromonosporas.
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
the term that refers to drugs that
have received FDA approval for
human testing, including
those drugs still undergoing clinical
trials , but are not approved for
marketing to the general public.
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. ILLICIT DRUG
a.k.a. “street’ drugs are those which
are used and/or distributed illegally.
ellicit drugs refer to highly addictive
and illegal substances such as
heroin, marijuana and meth
Legal Regulation of Drugs
Antipyretic Decongestants
Analgesics Diuretics
Antibiotics Emetics
Antidepressants Expectorants
anti-hypertensives Hypnotics
anti-diabetic Laxatives
Antihistamine Sedatives
Antitussive Tranquilizers
cholinergics 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).
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…
The TRADE NAME is designated
and patented by the manufacturer.
CAPITALIZED FIRST LETTER
For example, amoxicillin is
manufactured by several
pharmaceutical companies, some of
which assign a specific trade name
(eg, Amoxil, Trimox)
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.
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.
GENERIC TRADE NAME
NAME
ibuprofen Advil
lorazepam Ativan
diphenhydramine Benadryl
captopril Capoten
GENERIC NAME TRADE NAME
clonidine Catapres
celecoxib Celebrex
metformin Glucophage
misoprostol Cytotec
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.
Clinical trials, also known as clinical
studies, test potential treatments in human
volunteers to see whether they should be
approved for wider use in the general
population.
A treatment could be a drug, medical device, or
biologic, such as a vaccine, blood product, or
gene therapy.
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
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.
DRUG ACTION:
Pharmaceutic,
Pharmacokinetic &
Pharmacodynamic Phases
A. Pharmaceutic Phase
• The first phase of drug action
• Drug becomes a solution so that it can
be absorbed
•2 Pharmaceutic phases: Disintegration &
Dissolution
• Disintegration – is the breakdown of a
tablet into smaller particles
• Dissolution – is the dissolving of the
smaller particles in the GI fluid before
absorption
Factors Affecting
Pharmaceutic phase
pH
• Drugs are both disintegrated and
absorbed faster in acidic fluids than
alkaline fluids
Age
• Both very young and elderly have less
gastric acidity. Therefore, drug absorption
is generally slower
Factors Affecting Pharmaceutic phase
Enteric-coated tablets/capsules
• Resist disintegration in the gastric acid of
the stomach
• Disintegration only happens in the
alkaline environment of the small
intestine
• Enteric-coated tablets or capsules and
sustained-release (beaded) capsules
should not be crushed
Factors Affecting Pharmaceutic phase
Food
• may interfere with the dissolution and
absorption of certain dugs in the GIT
• Can also enhance absorption of other
drugs
B. Pharmacokinetic Phase
• The of drug movement to
achieve drug action
• The Process are:
• ABSORPTION
• DISTRIBUTION
• METABOLISM
• EXCRETION
B. Pharmacokinetic Phase
• Pharmacokinetics involves drug
movement through the body (ie,
“what the body does to the
drug”) to reach sites of action,
metabolism, and excretion.
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.
• Is the movement of drug particles
from the GI tract to body fluids by
passive absorption, active
absorption, or Pinocytosis
ABSORPTION
• Most oral drugs are absorbed into
the surface area of the small
intestine through the action of
mucosal villi
• Absorption is reduced if the villi
are decreased in number because
of disease, drug effect or removal
of small intestine
3 Major Process of drug Absorption
• Passive absorption – occurs mostly by
diffusion (movement from higher
concentration to lower concentration)
• Active absorption – requires a carrier
such as enzyme or protein to move the
drug against a concentration agent
• Pinocytosis – is a process by which cells
carry a drug across their membrane by
engulfing the drug particles
FACTORS AFFECTING
ABSORPTION
• BLOOD FLOW – poor circulation as a result of
shock, vasoconstrictor drugs, or disease hampers
absorption
• PAIN, STRESS & FOODS – slows gastric emptying
time, so the drug remains in the stomach longer
• EXERCISE – decreases blood flow by causing more
blood to flow to the peripheral muscle, thereby
decreasing blood circulation to the GI tract
• BLOOD SUPPLY – drugs given IM are absorbed
faster in muscles that have more blood vessels (e.g.
deltoids) than in those that have fewer blood
vessels (Subcutaneous tissue)
• FIRST PASS EFFECT – the process in
which the drug passes to the liver first,
metabolizing the drug to an inactive form
which may then be excreted. E.g. Warfarin
(Coumadin) and Morphine
Urine pH
• Urine pH varies from 4.5 – 8
• Acidic urine promotes elimination of
weak base drugs
• Alkaline urine promotes elimination of
weak acid drugs e.g. aspirin
Factors Affecting EXCRETION
Kidney Diseases
• Results in decrease glomerular filtration
rate (GFR) – decrease drug excretion
causing drug accumulation (drug toxicity)
C. Pharmacodynamic Phase
• Is the study of drug concentration
and its effects on the body
• The study of the mechanisms of
drug action that produce
biochemical or physiologic changes
in the body
C. Pharmacodynamic Phase
• 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
C. Pharmacodynamic Phase
• Drug response can cause a primary
or secondary physiologic effect or
both
• E.g. Diphenhydramine (Benadryl) –
antihistamine, primary effect is treat
symptoms of allergy, secondary
effect – CNS depression that causes
drowsiness
ONSET, PEAK & DURATION of
Action
1. ONSET OF ACTION – is the time it
takes to reach the minimum effective
concentration after a drug is
administered
2. PEAK ACTION – occurs when the drug
reaches its highest blood or plasma
concentration
3. DURATION OF ACTION – is the
length of time the drug has a
pharmacologic effect
Receptor Theory
• Most receptors, protein in structure are
found on cell membranes
• Drugs act through receptors by binding
to the receptor to produce (initiate) a
response or to block (prevent) a
response.
Receptor Theory
• 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”
(similar to lock and key
concept)
AGONISTS & ANTAGONISTS
• AGONISTS – drugs that produce a
response
• ANTAGONISTS – drugs that block a
response
• E.g. Isoproterenol (Isuprel) simulates the
beta 1 receptor (agonist), Cimetidine
(Tagamet), an antagonist, blocks the
histamine (H2) receptor, thus preventing
excessive gastric acid secretion
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
Categories of Drug Action
• 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.
Categories of Drug Action
• 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
• 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
and lethal dose (LD) in 50% of people
• The closer the ratio to 1, the greater the
danger of toxicity
• Formula:
THERAPEUTIC INDEX
• For example, if the LD50 is 200 and the
ED50 is 20 mg, the TI would be 10.
• TI = LD50 = 200 = 10
ED50 20
Empiric Therapy
◦ Based on practical experience rather
than on pure scientific data
◦ E.g. Acetaminophen – given to a
patient for fever even the cause of
fever is not known
Types of drug therapy:
Supplemental or Replacement
Therapy
◦ Replenishes or substitutes for
missing substances in the patient’s
body
◦ Substances is needed either because
it cannot be made by the body or it
is produced in insufficient quantity
◦ E.g. essential nutrients – Iron and
calcium, Insulin – for diabetic patient
Prophylactic Therapy
Provided to prevent illness or
undesirable outcome
E.g. malarial drug – before entering
malarial endemic area
Antibiotic therapy – patient who has
incision on the skin and for possibility of
bacterial invasion
IMPORTANT TERMS:
Pharmacology
◦ The study of the biological effects of chemicals
◦ The study of drugs, their uses (pharmacology)
,various dosage forms (Pharmaceutics) how the
body responds to drugs (pharmacodynamics) and
the absorption, distribution, metabolism and
excretion of drugs (pharmacokinetics) are
essential for the safe administration of drugs
Drugs
◦ Chemicals that are introduced into the body to
cause some sort of change
• LOADING DOSE
a large initial dose to initiate
immediate drug response or achieve a
rapid minimum effective concentration
in the plasma
After a large initial dose, a prescribed
dosage per day is ordered
• SIDE EFFECTS
are physiologic effects not related to
desired drug effects
• ADVERSE REACTIONS
are more severe than side effects,
undesirable effects of drugs that cause
mild to severe side effects
Drug Names and Classes:
Chemical name
◦ The scientific name that precisely describes its atomic
and molecular structure
Generic name
◦ Nonproprietary name
◦ Typically is an abbreviation of its chemical name
Trade Name
◦ Also known as the brand or proprietary name
selected by the drug manufacturer
◦ Protected by copyright
Classification of Drug:
Pharmacologic
◦ Chemical class
◦ Drugs are grouped according to the same chemical
characteristics
Therapeutic
◦ Drugs are classified according to their function or the
disorder they treat
Example:
All drugs used to treat hypertension belong to the
same therapeutic class even if they belong to different
pharmacologic classes.
Classification of Drug:
Example:
◦ Losartan
Therapeutic class: Antihypertensive
Pharmacologic class: angiotensin II
receptor Anatagonist
◦ Metoprolol
Therapeutic class: Antihypertensive
Pharmacologic class: beta 1 - blocker
IMPORTANT TERMS:
• TOXIC EFFECTS or TOXICITY
drug level exceeds the
therapeutic range resulting from
overdosing or drug accumulation
• TOLERANCE
refers to a decreased
responsiveness over the course
of therapy
IMPORTANT TERMS:
• ADDITIVE EFFECTS
Occurs when two drugs with
similar actions, combining them
at reduced doses produces an
effect equal to a higher dose
E.g. combining 2 different
analgesics such as Aspirin and
Codeine (Opioid)
IMPORTANT TERMS:
• SYNERGISTIC EFFECTS
Happens if two drugs with the same
effect produce a greater response
when given together than when
taken alone
E.g. Combining
Hydrochlorothiazide and Enalapril
for the treatment of Hypertension
IMPORTANT TERMS:
• PLACEBO EFFECT
is a psychologic benefit from a
compound that may not have the
chemical structure of a drug effect
Sometimes patients given a
placebo treatment will have a
perceived or actual improvement in
a medical condition
• POTENTIATION
The effect of drug which enhances
the actions or effect of the other
IMPORTANT TERMS:
• ANTAGONISTIC EFFECT
Develops when the combined
response of two drugs is less
than the response produced by
either drug alone
Opposite of potentiation
E.g An Antacid given with
tetracycline – results in
decreased absorption of the
tetracycline
IMPORTANT TERMS:
• DRUG-DRUG INTERACTION
the effects of a combination of
drugs may be greater than,
equal to, or less than the effects
of a single drug
• FOOD-DRUG INTERACTION
the effects of selected foods
may speed, delay or prevent
absorption of specific drugs