Introduction To Pharmacology: Dr. Zaid Al-Attar

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Introduction to

Pharmacology
Dr. Zaid Al-Attar
Pharmacology: represents the
scientific study of the origin,
nature, chemistry, effects, and
uses of drugs.

A drug: is any substance (other


than food) that, when inhaled,
injected, smoked, consumed,
absorbed via a patch on the
skin, or dissolved under the
tongue, causes a physiological
change in the body.
Five branches of pharmacology
1. Pharmacokinetics: deals with handling of
drugs by the body (refers to the absorption,
distribution, metabolism and excretion of
drug in a living organism). i.e (effect of the
body on the drug).
2. Pharmacodynamics: the study of the
biochemical and physiological effects of drugs
and the mechanisms of drug actions in living
organisms (i.e. effect of the drug on the body)
3. Toxicology: represents the study of undesirable
effects of drugs in living organisms
4. Pharmacotherapeutics: is the application of
drugs for treatment of disease
5. Pharmacognosy: deals with natural drugs (that
are-plants, animals or minerals and their
products.
Drug administration

Absorption

Distribution Excretion

Metabolism

Pharmacokinetics
Site of
action

Pharmacodynamics

Therapeutic effect Side effects


Pharmacokinetics
1. Absorption: is the transfer of a drug from its site of
administration to the blood stream. The rate of
absorption depends on the method of drug
administration.
2. Distribution: reversible transfer of a drug from one
location to another within the body. The drug may
reversibly leave the bloodstream , interstitial and
intracellular fluid to body tissues and vice versa.
3. Metabolism: the drug may be bio-transformed by
metabolism by liver or other tissues.
4. Elimination: the drug and its metabolites are
eliminated from the body in urine, bile or feces.
▪ Routes of Drug administration:
There are three major routes of drug
administration,
1. enteral
2. parenteral
3. topical
A. Enteral: (through digestive tract)
administering of drug by mouth is the simplest
and most common means of administering drugs.
When the drug is given by mouth (oral) it may be
swallowed, allowing oral delivery, or it may be
placed under the tongue (sublingual) facilitating
direct absorption into the bloodstream.
1. By mouth (oral): Giving a drug by mouth
provides many advantages to the patient.

1. Easily self-administered and limit the


number of systemic infections that could
complicate treatment (if given
parenterally).
2. Toxicities or overdose by the oral route may
be overcome with antidotes such as
activated charcoal.
3. Economical as compared with other
parenteral routes
4. No need for sterilization
Disadvantages
1. Ingestion of drugs with food, or in
combination with other drugs can influence
absorption (e.g. calcium supplement with
tetracyclines).
2. Drugs that are destroyed by acid (for example,
penicillin) become unavailable for absorption.
3. Slow onset, thus unsuitable for emergency
situations.
4. First pass effect
Note: Enteric coating of a drug protects it from
gastric acidic environment. the coating may
prevent gastric irritation e.g. aspirin
What is the 1st pass effect ?
• The first pass effect (or presystemic metabolism) is a drug
metabolism whereby the concentration of a drug is greatly
reduced before reaching the systemic circulation. A fraction
of drug lost during the process of absorption which is
generally related to metabolism in liver and gut wall (less
extent).
• After a drug is swallowed, it is absorbed by the digestive
system and enters the hepatic portal system. It is carried
through the portal vein to liver before it reaches the rest of
the body.
Benefits of presystemic effect:
•Lowers the toxicity of some drugs.
•Some drugs are given as prodrugs
(inactive form) and are converted from
inactive to active form. E.g. Codeine is
administered and bio transformed in
liver into its active form
•Disadvantages
•Lowers the concentration and effect of
some drugs
2. Sublingual: drug placement under the
tongue allows a drug to diffuse into the
capillary network and, therefore, to enter
the systemic circulation directly. E.g.angised
Advantages:
1. rapid absorption (as compared with oral
route).
2. Rapid onset of action
3. convenience of administration
4. avoidance of the harsh GI environment
(acidity , enzymes…)
5. avoidance of first-pass effect.
3. Rectal: (suppositories, cream
enema) the rectal route of
administration has the advantage
of
1. preventing the destruction of
drug by intestinal enzymes or
by low pH in stomach.
2. useful if the drug induces
vomiting when given orally,
3. Used for unconscious patient.
4. Used for children
5. Little or no 1st pass effect
B. Parenteral: The parenteral route
introduces drugs directly across the body's
barrier defenses into the systemic
circulation or other vascular tissues.
Advantages:
1. This route has the highest bioavailability and is
not subject to first-pass metabolism or harsh GI
environments.
2. Parenteral administration provides the most
control over the actual dose of drug delivered to
the body.

Disadvantages:
1. May cause pain, fear, infections and nerve
injury.

bioavailability : Amount of drug that reaches


systemic circulation.
Parenteral administration is used for:
1. Drugs that are poorly absorbed from the GI
tract (for example heparin)
2. Agents that are unstable in the GI tract (for
example, insulin).
3. Treatment of unconscious patients
4. Emergency situations that require a rapid
onset of action.
1) Intravenous (IV) (or intra-arterial):
Injection is the most common parenteral
route.
Advantages:
1. For drugs that are not absorbed orally,
there is often no other choice
2. With IV administration, the drug avoids
the GI tract problems as vomiting, first-
pass metabolism
Disadvantages :
1. Intravenous injection may
be affected by bacteria through
contamination at the site
of injection or IV injection.
2. May cause adverse
reactions (e.g. allergic
reactions) by the too-
rapid delivery of high
concentrations of drug
to plasma and tissues.
Therefore, the rate of
infusion must be
carefully controlled.
3. Not convenient ,
requires assistance
2) Intramuscular (IM): Drugs administered IM can be
aqueous solutions or specialized depot preparations.
Absorption aqueous solution is fast, whereas that
from depot preparations is slow (to provide long
lasting effect).

(depot special kind of drug preparation in which the drug is bound


to adsorbents to lower the release of the drug)

3) Subcutaneous (SC): This route of administration, like


that of IM injection, requires
absorption and is thus slower than
the IV route. Subcutaneous
injection minimizes the risks associated
with intravascular injection.
4. Intradermal injection
•is the injection of a substance
into the dermis, just below
the epidermis. This route has
the longest absorption time as
compared to subcutaneous
injections and intramuscular
injections. As a result, it is
used for sensitivity tests, like
allergy tests
5. Inhalation: Inhalation provides the rapid
delivery of a drug across large surface area of
mucous membranes of respiratory tract,
producing a systemic effect almost as rapidly
as with IV injection. Used for drugs that are
gases (e.g. some anesthetics)
5. Intrathecal:
Introducing drugs directly into the
cerebrospinal fluid.
e.g. antibiotics or antifungals to avoid
blood brain barrier
6. Transdermal: This route of administration
achieves systemic effects by application of
drugs to the skin, usually via a transdermal
patch such as the antianginal drug. It has the
advantage of avoiding 1st pass effect
C.Topical
• Topical application is used when a
local effect of the drug is desired
without affecting the rest of body

• A. Skin (Dermal):For example is


applied as a cream directly to the
skin. E.g. gels or creams

• B. Mucous membranes
• 1. Drops for eye , nose: This route
involves administration of drugs
directly into eye or nose. e.g. nasal
drops
• 2.Inhalation : Drugs dispersed in an aerosol to
provide local effect.
• This route is particularly effective and convenient
for patients with respiratory complaints (such as
asthma)

• 3. Gastrontestinal:
Nystatin for Rx of fungal infections
(nystatin is not absorbable via GIT
so it works only topically)
Factors affecting the choice of drug route
1. Physical and chemical properties of drug
2. Site of desired action
3. Rate and extent of absorption from
different routes
4. Effect of digestive juices and first pass
metabolism on the drug
5. Rapidity with which the response is
desired
6. Accuracy of dosage required
7. Condition of patient

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