Introduction to

Pharmacology
 Contents
1. Pharmacology
2. Drug and Medicine
3. Receptor, Affinity, Efficacy, Agonist, Antagonist
4. Synergistic & Antagonistic Drugs
5. Pharmacokinetics and Pharmacodynamics
6. Dose, Dosage Form and Dosage Regimen
7. Concept of Various Types of Dose
8. Pro-Drugs
9. Side Effect vs Adverse Effect
10. Routes of Administration
 Pharmacology

❑ The broader knowledge of how drugs interact with living

body to produce therapeutic effects and how body modifies a
drug is termed as pharmacology.

❑ It can be defined as the study of the effects of drugs on the

function of living systems.
 Drug and Medicine
Drug

❑ A drug can be defined as a chemical substance of known

structure, other than a nutrient or an essential dietary
ingredient, which when administered to a living organism,
produces a biological effect.

❑ Drugs may be synthetic chemicals, chemicals obtained

from plants or animals, or products of genetic engineering.
 Drug and Medicine
Medicine

❑ A medicine is a chemical preparation which contains one

or more drugs, administered with the intention of
producing a therapeutic effect.

❑ Medicines usually contain other substances (excipients,

stabilizers, solvents, etc.) besides the active drug, to make
them more convenient to use.
 Receptor, Affinity, Efficacy, Agonist, Antagonist

Receptor: Receptor is a macromolecule, lipoprotein in nature, situated at the cell

membrane, or sometimes, inside the cell, bind with specific ligands/drug
molecules and after binding, helps exert the physiological and biochemical
response.

Affinity: Tendency of drug molecule to bind with the receptor.

Efficacy: Pharmacological and biochemical response/effects of drug molecule

after binding with the receptor.
 Receptor, Affinity, Efficacy, Agonist, Antagonist

Agonist: An agonist is a chemical that binds to a receptor and activates

the receptor to produce a biological response.

Antagonist: An antagonist blocks the action of the agonist

 Synergistic & Antagonistic Drugs
Synergism:

➢ When two drugs are prescribed together, they tend to increase the activity
of each other, called as synergism, i.e. an interaction between two or more
drugs that causes the total effect of the drugs to be greater than the sum of
the individual effects of each drug.

➢ A synergistic effect can be beneficial or harmful. Various drug

combinations (e.g., NSAIDs and opioids; opioids and local anesthetics etc.)
frequently demonstrate synergistic effects. A combination of aspirin &
paracetamol increase the assumed total analgesic activity.

➢ Synergistic drug combinations must be administered carefully, because

unwanted and potentially toxic effects may also be potentiated.
 Synergistic & Antagonistic Drugs
Antagonism:

➢ A receptor antagonist is a type of receptor ligand or drug that blocks a biological

response by binding to and blocking a receptor rather than activating it like
an agonist. They are sometimes called blockers; examples include alpha
blockers, beta blockers, and calcium channel blockers.

➢ In pharmacology, antagonists have affinity but no efficacy for their receptors,

and binding will inhibit the function of an agonist .

➢ Antagonist activity may be reversible or irreversible depending on the longevity

of the antagonist–receptor complex, which, in turn, depends on the nature of
antagonist–receptor binding.
 Pharmacokinetics and Pharmacodynamics

➢ Pharmacodynamics is the study of how a drug affects the

body. It refers to the relationship between drug concentration
at the site of action and the resulting effect including the time
course and intensity of therapeutic and adverse effects.

➢Whereas, pharmacokinetics is the study of how the body

affects the drug. It is the study of drug absorption,
distribution, metabolism and excretion.
 Dose, Dosage Form and Dosage Regimen

• Dose: Amount of drug that is safe, measured and clinically effective for

human administration is called dose.

• Dosage Form: Any suitable form to which drug is supplied with

pharmaceutical technology and which is suitable for human

administration is called dosage form. Such as tablet, capsules, syrup,
suspension etc.

• Dosage Regimen: Dosage regimen is dosing guidelines for individual

based on the age, diseases and other differentiating parameters.

 Dose, Dosage Form and Dosage Regimen

• Practice:

Mr. Azam’s grandfather is a diabetic patient. He takes

metformin 500 mg tablets twice daily.

What is the Dose?

What is the Dosage form?
What is the Dosage Regimen?
 Concept of Various Types of Doses
• Therapeutic (effective dose) dose: Dose that is required to

produce the optimal therapeutic effect.

• ED50 (Median effective dose): The dose at which 50% of the

individual exhibit the specific effect.

• LD50 (Median lethal dose): Dose required to produce death in

50% experimental animal.

• TD50 (Median toxic Dose): Dose required to produce a

particular toxic effect in 50% of test animal.

• Maximum Dose: Largest dose of drug that is safe to administer

and produce no toxic effect is called maximum dose.

 Concept of Various Types of Doses

• Booster dose: Dose that is given after sometime of an initial dose to

enhance the effect (after months or years)

• Test Dose: Amount of drug given initially (before giving full

therapeutic dose) to see the sensitivity or response of tissue to the drug

is called test dose. Test dose is given to observe the sensitivity of the
tissue to the drug eg. Antibiotic sensitivity.

• Loading Dose: One or series of doses that may be given at the onset of

therapy with the aim of achieving the target concentration rapidly.

• Maintenance Dose: Dose required for maintaining the desired

therapeutic effect that is achieved by the loading dose.

 Pro-Drugs
• Pro drugs are inactive substances and must be bio transformed /
metabolized in the body to metabolites that have pharmacological
activity.

Objective of Pro drug design:

• To improve drug stability.

• To increase systemic drug absorption.

• To prolong the duration of activity.

• To avoid first pass metabolism (Pre systemic elimination).

• To reduce local adverse effect of drugs.

 Pro-drugs

 Antiparkinsonian agent, levodopa crosses blood brain barrier (BBB)

and is then decarboxylated in the brain to L-dopamine an active

neurotransmitter. L-dopamine does not easily penetrate the blood brain
barrier and therefore can not be used as a therapeutic agent.

 Another example is the hydrolysis of aspirin into salicylic acid and

this salicylic acid is the active drug. Here aspirin is the prodrug.

 In biotransformation of prodrug generally the hydrolysis and the

decarboxylation is occurred.
 Side Effects vs Adverse Effects
Side effects and adverse effects are both experienced by people in the
healthcare field. Often the words are interchanged or used instead of
the other, but wrongly so. There is ample difference in the meaning of
both words.

• Side Effect
➢A side effect of any substance is an effect beyond the chief or
primary action that is intended/known by the person, most often
the physician prescribing the drug.
➢ This extra action is foreseen by the doctor. For example, the
patient might not be aware of the side effect of diarrhea while using
certain antibiotics but the physician is very well aware about it.
 Side Effects vs Adverse Effects
➢ But not every side effect is a bad one. Some are downright welcome.
Minoxidil, originally marketed as an oral tablet for high blood pressure,
was found to grow hair in those using it. Today, as a topical lotion or foam, it
is a popular over-the-counter remedy for male pattern baldness.
➢ Side effects are mostly temporary and resolve spontaneously
whereas adverse effects are often longer lasting and need
intervention.
➢ Doctors generally advise patients not to pay attention to side effects
unless severe and often warn their patients regarding their possibilities. Side
effects are published by pharmaceutical companies as soon as a new drug is
launched in the market owing to the extensive clinical trials that are
conducted before launching it in the market for general use.
 Side Effects vs Adverse Effects
• Adverse Effect

➢ An adverse effect, in distinction, is an effect wherein the reaction occurs

over and beyond the chief and desired action of a drug. The adverse
reaction is unexpected by both the physician as well as the patient.

➢ Side effects are most often mild in nature and often self resolving but
adverse effects can be fatal and need to be reversed immediately. Adverse
effects reduce either by reducing the dose of the medicines or by stopping
the drug altogether.

➢ Occasionally, if the adverse effect is too serious, there might be a need for
hospitalization. Adverse effects can occur due to incorrect drug dosage or a
surgery too whereas side effects are produced due to medications alone.
 Routes of Administration
➢ No single method of drug administration is ideal for all drugs in all
circumstances.

➢ Factors governing the choice of route of administration-

1. Physical & chemical properties of drug solid/liquid/gas; solubility,
stability, pH, irritancy
2. Site of desired action- localized and approachable or generalized and
non approachable
3. Rate & extent of absorption from various routes
4. Effect of digestive juices & first pass effect
5. Rapidity of the desired response- emergency/routine
6. Accuracy of dosage
7. Condition of the patient- unconscious, vomiting
 Buccal
1
Oral 2
Sublingual 3 the
(Besides 4
Rectal
cheeks)

Intramuscul Subcutaneo Intra-

Intravenous ar (Into us (Into arterial
5
(veins) 6
skeletal
7
subcutaneou
8
(Into
muscle) s tissue) arteries)

Intra-
Intrathecal
articular Transdermal
9
(Synovial
10
(Cerebrospi 11
Inhalational 12
(As patches
nal fluids)
fluids) on skin)
 Intraperiton
Topical
Intranasal eal
13 on
(Rubbed 14
(Nose) 15(Eye)
Ocular 16
(Peritoneal
skin)
cavity)
 Routes of Administration
1. Oral
2. Sublingual
3. Buccal (Besides the cheeks)
4. Rectal
5. Intravenous (veins)
6. Intramuscular (Into skeletal muscle)
7. Subcutaneous (Into subcutaneous tissue)
8. Intra-arterial (Into arteries)
9. Intra-articular (Synovial fluids)
10. Intrathecal (Cerebrospinal fluids)
11. Inhalational
12. Transdermal (As patches on skin)
13.Topical (Rubbed on skin)
14. Intranasal (Nose)
15. Ocular (Eye)
16. Intraperitoneal (Peritoneal cavity)
Thank you!!