Pharmacology
By
Abdulaziz mohamed
General Pharmacology
Learning Objectives
• At the end of this chapter the student will be able to:
– Define various terminologies used in Pharmacology
– discuss nature and sources of drugs
– describe pharmacodynamics and pharmacokinetics
– Identify adverse drug reactions and drug interactions
– describe new drug development and evaluation
Introduction to Pharmacology
Pharmacology
• 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
Drugs
• Drugs are chemicals that alter functions of living
organisms
• Drugs are generally given for the diagnosis, prevention,
control or cure of disease
Pharmacy
• It is the science of identification, selection, preservation,
standardization, compounding and dispensing of medical
substances
Pharmacodynamics
• The study of the biological and therapeutic effects of
drugs (i.e,“what the drug does to the body”)
Pharmacokinetics
• Study of the absorption, distribution metabolism and
excretion (ADME) of drugs (i.e, “what the body does
to the drug”)
Toxicology
• It’s the study of poisons. Many drugs in larger doses
may act as poisons
• Poisons are substances that cause harmful, dangerous
or fatal symptoms in living substances
Chemotherapy
• It’s the effect of drugs upon microorganisms, parasites
and neoplastic cells living and multiplying in living
organisms
Sources of drugs
Drugs are obtained from:
• Minerals: Liquid paraffin, magnesium sulfate,
magnesium trisilicate, kaolin, etc
• Animals: Insulin, thyroid extract, heparin, etc.
• Plants: Morphine, digoxin, atropine, castor oil, etc.
• Synthetic source: Aspirin, sulphonamides,
paracetamol, zidovudine, etc.
• Micro organisms: Penicillin, streptomycin and many
other antibiotics
• Genetic engineering: Human insulin, human growth
hormone etc.
• Out of all the above sources, majority of the drugs
currently in use are from synthetic source.
Pharmacodynamics
• Pharmacodynamics involves how the drugs act on
target cells to alter cellular function
Receptor and non-receptor mechanisms
• Most of the drugs act by interacting with a cellular
component called receptor
• Some drugs act through simple physical or chemical
reactions without interacting with any receptor
• Example: aluminium hydroxide and magnesium trisilicate
• Receptors are protein molecules present either on the
cell surface or with in the cell
Site of drug action
• A drug may act:
I. Extracellularly e.g: osmotic diuretics
II. On the cell surface e.g: penicillin
III. Inside the cell e.g: anti-cancer drugs
Dose Response relationship
• The exact relationship between the dose and the
response depends on the biological object under
observation and the drug employed
• The lowest concentration of a drug that elicits a
response is minimal dose
• The largest concentration after which further increase in
concentration will not change the response is the
maximal dose
• Median lethal dose (LD50)
• This is the dose (mg/kg), which would be expected to
kill one half of a population of the same species and
strain
• Median effective dose (ED50)
• This is the dose (mg/kg), which produces a desired
response in 50 per cent of test population
• Therapeutic index (T. I)
• 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
• Therapeutic index (T. I) =LD50/ED50
Pharmacokinetics
• Pharmacokinetics deals with the absorption,
distribution, metabolism and excretion drugs in the body
1. Drug absorption
• Absorption is the process by which the drug enters in to
the systemic circulation from the site of administration
through biological barrier
• In case of intravenous administration the drug bypasses
absorption processes and it enters into the circulation
directly
Pharmacokinetics…
• Passage of drug across membrane through
• Passive transfer
– Simple diffusion
– Facilitated diffusion
• Specialized transport
– Active transport
– Endocytosis
Pharmacokinetics…
Routes of drug administration
a) From the alimentary tract
– Buccal
– Sublingual
– Oral
– Rectal
b) Topical/ local route
c) Inhalation
Pharmacokinetics…
d) From the parenteral route
– Subcutaneous
– Intramuscular
– Intravenous
– Intraperitonial
– Intra-articular ……
Pharmacokinetics…
Bioavailability:
• It is the rate and amount of drug that is absorbed and
reaches the systemic circulation
• When a drug is given through IV, the bioavailability is
100%
• Drugs given by orally may be inactivated due to many
reasons
Pharmacokinetics…
Factors affecting drug absorption and bioavailability
1. Physico-chemical properties of drug
2. Nature of the dosage form
3. Physiological factors
4. Pharmacogenetic factors
5. Disease states
Pharmacokinetics…
2. Distribution of drugs
• Distribution is penetration of a drug to the sites of action
through the walls of blood vessels from the administered
site after absorption
3. Metabolism of drugs
• The process by which the body brings about changes in
drug molecule is referred as drug metabolism or
biotransformation
Pharmacokinetics…
4. Excretion of drugs
• Excretion of drugs means the transportation of unaltered
or altered form of drug out of the body
• The major routes 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
Pharmacokinetics…
Drug safety and effectiveness
• Individuals differ both in the degree and the character of
the response that a drug may elicit
• The optimum dose of a drug which produces the desired
therapeutic effect varies from person to person
Pharmacokinetics…
• The important factors which influence the effect of a
drug are:
1. Drug intolerance
2. Sex difference (Menstruation, Pregnancy,
Breast feeding)
3. Body Weight
4. Age
5. Disease state
6. Pharmacogenetics
7. Drug tolerance
Drug interactions
• The types of drug interactions are;
a) Pharmaceutical drug interactions
– Example: diazepam + infusion fluid
b) Pharmacokinetic drug interactions
i. Interaction during absorption
• Example: Tetracycline + antacid
ii. Interaction during distribution
• Example: Quinidine + digoxin
Drug interactions…
iii. Interaction during metabolism
• This can be explained by two mechanisms
– Enzyme induction
• Enzyme inducers: Rifampicine, phenytoin,
sulfonamides, Barbiturate, etc.
– Enzyme inhibition
• Enzyme inhibitors: Disulfiram, isoniazid,
allopurinol, cimetidine, Metronidazole, etc.
Pharmacokinetics…
iv. Interactions during excretion
• Some drugs interact with others at the site of excretion
i.e. in kidney
– Example: Penicillin + Probenecid → Increases the
duration of action of penicillin
Drug interactions…
C. Pharmacodynamic interactions
• Drug Synergism: When the therapeutic effect of two
drugs are greater than the effect of individual drugs
(a) Additive effect
A + B = AB
(b) Potentiation effect
AB > A + B
Drug interactions…
• Drug Antagonism: The phenomenon of opposing
actions of two drugs on the same physiological system is
called drug antagonism
Adverse drug reactions
• The drugs that produce useful therapeutic effect may
also produce unwanted or toxic effects.
• The adverse effects are
1) Side effects
2) untoward effects
3) allergic reactions
4) teratogenic effects
Development of new drugs
• New drug development and evaluation comprises of two
steps
a) Preclinical development
• The aim of the preclinical development phase is to
explore the drug efficacy and safety before it is
administrated to patients
• In this phase, varying drug doses are tested on animals
and/or in vitro systems
Development of new drugs…
B) Clinical development
• About one in 1000 New chemical entities (NCE) reach
this stage
• The steps to be studied in this stage include:
– Pharmaceutical study
– Pharmacological study
– Clinical trial
Development of new drugs…
• Clinical trial has 4 phases
– Phase - I: First exposure of the new drug on healthy
volunteers
– Phase - II: Small scale trials on patients
– Phase - III: Full scale evaluation of treatment
comparing it with standard treatment
– Phase - IV: It is also called post marketing
surveillance
Pharmaceutical dosage forms
• Solid dosage forms
– capsule, tablets, powder, suppository
• Semisolid dosage forms
– Ointment, Cream, paste etc
• Liquid dosage forms
– Solution, Suspension, emulsion
• Gas dosage forms
– Aerosol
Exercise
• 1) What are the different routes of drug administration
and write about their advantages and disadvantages
• 2) Define bio-availability and describe the factors
affecting drug absorption
• 3) Define adverse drug reactions
• 4) Write about the factors modifying drug action
• 5) Write about different types of drug interactions.
• 6) Write about the different types of dosage forms
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