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Introduction To Pharmacology

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The key takeaways are the definitions and basic concepts of pharmacology including pharmacokinetics, pharmacodynamics and pharmacotherapeutics.

Drugs can be classified based on source, chemical structure, therapeutic use and pharmacologic effects.

Factors like age, disease, diet, organ functions and other drug interactions can affect how a patient responds to drugs.

Introduction to

Pharmacology
Learning objectives
At the end of this session the student should
able to
• Define pharmacology
• Explain principles of pharmacology
• List source of the drug
• Mention common names of drugs
• Explain common routes of drug
administration
Definition Pharmacology
Pharmacology is the scientific study of the origin,
nature, chemistry, effects, and uses of drugs. This
knowledge is essential to providing safe and
accurate medication administration to your patient.
Pharmacology is the study of interaction of drugs
with living organisms. It also includes history,
source, physicochemical properties, dosage
forms, methods of administration, absorption,
distribution mechanism of action,
biotransformation, excretion, clinical uses and
adverse effects of drugs.
In general
The chapter reviews the three basic
concepts pharmacology.
 Pharmacokinetics : the absorption,
distribution, metabolism, and excretion of
drugs by the body.
 Pharmacodynamics: the biochemical
and physical effects of drugs and
mechanism of drug action.
Con..
Drug:-is any substance that alters the
physiologic function of the body, with
the potential of affecting health.
Medication: -is a drug that is used for
therapeutic/curative purpose.
In general we can say a drug or
medication is any substance that
modifies body function when taken
into the living organism.

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Continue
Pharmacotherapeutics: the use of drug to
prevent and treat disease.
In addition, it discusses other important
aspects of pharmacology, including
How drug are named and classified
How drugs are derived
How drugs are administered
How new drugs are developed
Nomenclature of drugs
One drug can have several names.
These include:
The chemical name:-is a precise
description of a drug’s chemical
composition; it identifies the drug’s
atomic & molecular structure. This
name is significance to pharmacists.
The generic name: - is the name
designed by the manufacturer that
first develops the drug. Often the
generic name is derived from the
chemical name. 7
Con..
The official name:-is the name by
which the drug is identified in the
official publication.
The trade name:-also referred to as
brand name or proprietary name, is
selected by the drug company that
sells the drug & is copyrighted. A drug
can have several trade names when
produced by different manufacturers.
The nurse should be familiar with the
drug’s generic and trade name. E.g.
Acetaminophen (generic) = (Tylenol, tempra,
& liquiprin) (trade) 8
Classifications of drugs
Drugs can be classified from d/t
perspectives. For example;
– By body system affected by the
drug(drugs that affect the respiratory
system, the cardiovascular system),
– By the symptom relieved by the drug
(antipain, analgesics),
- By the clinical indications for the
drug (antibiotics, antifungal …)

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Where drugs come from
Traditionally, drugs were derived from
natural sources, such as
Minerals: Liquid paraffin, magnesium
sulfate, magnesium trisilicate, etc.
Animals: Insulin, thyroid extract, heparin
and antitoxin sera, etc.
Plants: Morphine, digoxin, atropine, castor
oil, etc.
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Today, however, laboratory researchers have used
traditional knowledge, along with chemical science, to
develop synthetic drug source.
One advantage of chemically developed drugs is that
they’re free from the impurities found in natural
substances.
Also researchers and drugs developers can
manipulate the molecular structure of substance such
as antibiotics so that a slight change in the chemical
structure makes the drug effective against different
organism.
the first , second , third and fourth –generation
cepholosporins are an example.
How drugs are administered ?
Dug's administration route influences the
quantity given and the rate at which the
drug is absorbed and distributed. These
variables affect the drug ‘s action and the
patient response .
Routes of admistration
Buccal, sublingual, and transligual
Certain drugs, such as netro-glycerin are
given bucally (in the pouch b/w the cheek
and teeth ) , subligually (under the tongue
) or transligual (on the tangue) to prevent
their destruction or transformation in the
stomach or small intestine.
Gastric and Intradermal
The gastric route allows direct
administration of a drug into the GI system.
This route is used when patients can’t ingest
the drug orally.
In intradermal adminstration, drugs are
injected into skin. A needle is inserted at a
10-15 degree angle so that it punctures only
the skin surface. This form of administration
is used mainly for diagnose purposes, such
as testing for allergic or tuberculosis.
Subcutaneous route
In subcutaneous administration, small amounts
of a drug are injected beneath the dermis and
into the subcutaneous tissue, usually in the
patient’s upper arm, thigh, or abdomen. This
allows the drug to move into the blood stream
more rabidly than if given by mouth. Drug
given subcutaneously include nonirritating
aqueous solution and suspension contained
in 0.5ml to 2ml of fluid, such as heparin and
insulin.
Intramuscular routes
The I.M. route allows drugs to be injected
directly into various muscle group at
varying tissue depth. This form of
administration provides rapid systemic
action and allows for absorption of
relatively large dose (up to 5ml). Aqueous
suspensions and solutions in oil as well as
drugs that aren’t available in oral are given
I.M.
Intravenous routes
The I.V. route allow injection of drugs and
other substance directly into the blood
stream through a vein . Appropriate
substance to administer I.V. including
drugs , fluids, blood or blood products and
diagnose contrast agents. Administration
can range from a single dose to an
ongoing infusion that’s delivered with great
precision.
Oral route
Oral administration is usually the safest,
most convenient and last expensive route.
Oral drugs are administered to patients
who are conscious and able to swallow.
Rectal route
Suppositories, oitment, creams or gels
may be instilled into the rectum or vagina
to treat local irritation or infection. Some
drugs are applied to the mucosa of the
rectum or vagina can also be absorbed
systemically.
Respiratory route
Drugs that are available as gases can be
administered into the respiratory system
through inhalation. These drugs are
rapidly absorbed. In addition, some of
these drugs can be self –administered by
devices such as metered dose inhaler.
The respiratory route also used in
emergency for example , to administer
some injectable drugs directly into the
lungs via an endotracheal tube.
Topical route
The topical route is used to deliver a drug
via the skin or mucous membrane. This
route is used for dermatologic ,
ophthalmic. Otic, and nasal preparation.
Specialized infusion
Drugs may also be given as specialized infusion.
They are given directly to a specific site in the
patient’s body. Type of infusions include
Epidural infusion- the drug is injected into the
epidural space
Intraperitoneal infusion- the drug is injected into
peritoneal cavity.
Intraosseous infusion- the drug is injected into
rich vascular network of long bones
Intra-articular infusion- the drug is injected into a
joint .
Pharmacokinetics
The term kinetics refers to movements. Pharmacokinetics
deals with drug action as it moves through the body.
There fore pharmacokinetics discusses how drug is
• absorbed (take into the body)
•Distributed (moved into various tissue )
•Metabolism (changed into form that can be excreted )
•Excreted (removed from the body ).
This branch of pharmacology is also concerned with a
drug’s onset of action, peak concentration level, and
duration of action .
Absorption
Drug absorption covers the progress of a
drug from the time it’s administered,
through the time it passes to the tissue,
until it be comes available for use by the
body.
Bioavailability
It is the rate and amount of drug that is
absorbed from a given dosage form and
reaches the systemic circulation following
non-vascular administration.
When the drug is given IV, the bioavailability
is 100%. It is important to know the manner in
which a drug is absorbed.
The route of administration largely
determines the latent period between
administration and onset of action.
Factors affecting absorption
•Various factors- such as the route of
administration, the amount of blood flow and
the form of the drug can effect the rate of
adrug’s absorbed.
•If only a few cells separate the active drug
from systemic circulation, absorption occur
rapidly and the drug quickly reaches
therapeutic levels in the body. Typically drug
absorption occur with in seconds or minutes
when administered sublingually, I.V. or by
inhalation.
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Absorption occur at slower rate when
drugs are administered by the oral,
I.M., or subcutaneous routes because
the complex membrane system of GI
mucosal layers, muscle and skin delay
drug passage.
Distribution

Drug distribution is the process by which


the drug is delivered to the tissue and fluid
of the body. Distribution of an absorbed
drug within the body depends on several
factors
•Blood flow
•Solubility
•Protein binding
Metabolism of drugs:
•Drugs are chemical substances, which interact
with living organisms and produce some
pharmacological effects and then, they should be
eliminated from the body unchanged or by
changing to some easily excretable molecules.
•The process by which the body brings about
changes in drug molecule is referred as drug
metabolism or biotransformation.
Excretion of drugs
•Excretion of drugs means the transportation
of unaltered or altered form of drug out of the
body.
•The major processes of excretion include
renal excretion, hepatobiliary excretion and
pulmonary excretion.
•The minor routes of excretion are saliva,
sweat, tears, breast milk, vaginal fluid, nails
and hair.
Half life =Half the drug

Half life (t1/2) of a drug is the time taken


for the concentration of drug in the blood
or plasma to decline to half of original
value or the amount of drug in the body
to be reduced by 50%.
It has two phases i.e. half-life of
distribution and half-life of elimination.
Onset, peak and duration
In addition to absorption, distribution,
metabolism and excretion, three other
factors play important roles in a drug’s
pharmacokinetics.
Onset of action
Peak concentration
Duration of action.
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Onset of action refers to the time intervals
that starts when the drug is administered
and end when the therapeutic effect
actually by begins. Rate of onset varies
depending on the routes of administration
and other pharmacokinetic properties.
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As the body absorbs more drug, blood
concentration levels rise. The peak
concentration level is reached when the
absorption rate equals the elimination rate.
However, the time of peak concentration
isn’t always the time of peak response.
The duration of action is the length of time
the drug produces its therapeutic effect.
Pharmacodynamics
Pharmacodynamics is the study of drug
mechanism that produce biochemical or
physiologic changes in the body. The
interaction at cellular level b/w a drug and
cellular components, such as the complex
protein that make up the cell membrane,
enzyme or target receptors, represents
drug action. The response resulting from
this drug action is called the drug effect.
Agonist Vs antagonist
Agonist is an example of a drug that
interacts with receptors. An agonist drug
has an attraction, or affinity, for a receptor
and stimulates it. The drug then binds with
the receptor to produce its effect. The
drug’s ability to initiate a response after
binding with receptor to as intrinsic activity.
antagonist
If a drug has an affinity for a receptor but
displays little or no intrinsic activity, it is
called an antagonist. The antagonist
prevents response from occurring.
Antagonist can be competitive and non
competitive
Competitive
Competitive antagonist competes with the
agonist for receptor sites. Because this type
of drug binds reversibly to the receptor site,
administering a large doses of an agonist
can overcome the antagonist effect.
Non competitive antagonist binds to
receptor sites and blocks the effects of the
agonist. Administering large dose of the
agonist can’t reverse its action.
Drug safety and
effectiveness
Therapeutic index: It is an approximate
assessment of the safety of the drug. It is the
ratio of the median lethal dose and the median
effective dose. Also called as therapeutic
window or safety.
The therapeutic index usually measures the
difference b/w
•An effective dose for 50% of the patient treated
•The minimal dose at which adverse reaction
occur
Narrow index =potential
danger
A drug with a low or narrow therapeutic
index has narrow range safety b/w an
affective dose and lethal one. On other
hand, a drug with high therapeutic index
has a wide range of safety and less risk
of toxic effect.
Pharmacotherapeutics

Pharmacotherapeutics is the use of drug


to treat disease. When choosing a drug
to treat a particular condition, health care
providers consider the drug’s
effectiveness as well as such factors as
the type of therapy the patient will
receive.
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The type of therapy prescribed depends on the severity, urgency and
prognosis of patient’s condition. Therapy types include :
•Acute therapy, if the patient is critically ill and requires acute intensive
therapy.
•Empiric therapy, based on practical experience rather than on pure
scientific data .
•Maintenance therapy, for patients with chronic conditions that don’t
resolve
• supplemental or replacement therapy, to replenish or substitute for
missing substance in the body.
•Supportive therapy, which does not treat the cause of the disease but
maintain other threatened body system until the patient’s condition
resolved.
• palliative therapy , used for end stage or terminal diseases to make the
patient as comfortable as possible.
Factors affecting patients
respond to a drug
Patient responses to a drug can vary greatly, depending on such
factors as
•Age
•Cardiovascular function
•Diet
•Disease
•Drug interaction
•GI function
•Hepatic function
•Infection
•Renal function
•Gender
Drug interactions
It is usual for patients to receive a number
of drugs at the same time. It is a
phenomenon which occurs when the
effects of one drug are modified by the
prior or concurrent administration of
another drug(s). A drug interaction may
result in beneficial or harmful effects and
may be classified into:
Pharmaceutical drug interactions

Serious loss of potency can occur from


incompatibility between an infusion fluid
and a drug that is added to it.
For example diazepam if added to infusion
fluid there will be a precipitate formation →
loss of
therapeutic effect.
Pharmacokinetic drug interactions:

Interaction during absorption: Drugs


may interact in the gastrointestinal tract
resulting in either decreased or
increased absorption.
e.g. Tetracycline + Calcium →
Decreased absorption of tetracycline.
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Interaction during distribution: A drug which is
extensively bound to plasma protein can be
displaced from its binding sites by another drug
or displacement from other tissue binding
sites. e.g. (i) Sulfonamide can be displaced by
salicylates from plasma proteins and it leads to
sulfonamide toxicity.
(II)Quinidine displaces digoxin from binding sites
in tissues and plasma and leads to digoxin
toxicity.
Pharmacodynamic
interactions:
Drug Synergism: When the therapeutic effect
of two drugs are greater than the effect of
individual drugs, it is said to be drug synergism.
(a) Additive effect: When the total
pharmacological action of two or more drugs
administered together is equivalent to the
summation of their individual pharmacological
actions is called additive effect. i.e A + B = AB
e.g.
Combination of ephedrine and aminophyllin in
the treatment of bronchial asthma.
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•Potentiation effect: When the net
effect of two drugs used together is
greater than the sum of
individual effects, the drugs are said to
have potentiation effect.
i.e. AB > A + B
e.g. Trimethoprim+sulfamethoxazole
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