BASICS IN PHARMACOLOGY

Sources of Drugs
chemicals

animal

plants

Drug is defined as a substance obtained from mineral, chemical, animal, microbial or plant sources DRUG which is used in the diagnosis, prevention and treatment of disease in humans and animals.

microbial

Dose & Dosage form

Dose is the quantity of drug given at a time so that it results in the desired effect, without causing harm Drug is useful when available in a form in which it is easily handled and given to the patients, e.g. Capsules Tablets

Syrups

Routes Of Drug Administration

Inhalation Oral Sublingual

Topicals

Advantages Advantages Most convenient, most economical Vomiting and diarrhoea and in the patients Safer compared to parenteral unable to swallow administered Drugs that mightSelf irritate the stomach or Disadvantages which are not absorbed orally Irritant, unpalatable Rapid action Advantages Not useful in vomiting Accuracy of dose Site specific action And unconcious patients Disadvantages Decreased systemic adverse effects
Less safe Disadvantages More expensive Local irritation, inconvinience Inconvenient to use, self medication being difficult Liable to cause infection Rectal Injure important structures

Intramuscular

Subcutaneous

Intravenous

PHARMACOLOGYIs the science that deals with the study of drugs.

Pharmacology

PHARMACODYNAMICS DRUG BODY

PHARMACOKINETICS BODY DRUG

DRUG

PHARMACODYNAMICS

DRUG

PHARMACOKINETICS

PHARMACODYNAMICS
RECEPTORS
A Drug Receptor is a specialised target molecule present on the cell surface or intracellularly drug + receptor drug-receptor complex effect

AGONIST

activate the receptors when they occupy it Affinity Good intrinsic activity no activation when they occupy the receptor Affinity No intrinsic activity

ANTAGONIST

DRUG RECEPTOR COMPLEX FORMATION

RECEPTOR

DRUG

DRUG RECEPTOR COMPLEX

Agonist

Antagonist

Drug

Receptor

PHARMACOKINETICS

DRUG ADMINISTERED
ABSORPTION PLASMA

DISTRIBUTION IN THE TISSUES METABOLISM DRUG & METABOLITES IN PLASMA ELIMINATION DRUG & METABOLITES IN URINE, FEACES,BILE

AREA UNDER CURVE

Cmax = Maximum drug concentration Tmax = Time taken to reach Cmax t1/2 = Half life
C max

T max

t1/2

Drug given at this point

Half Life

Measure of the time elapsed for the plasma drug concentration to fall to half its original value (Cmax) Elimination half life from plasma is clinically important for safety profiles of drugs

Sites of Elimination

Renal Faecal Breast milk Pulmonary Saliva & Sweat glands

Additive Effect
1+1=2

When the total pharmacological action of

Two or more drugs administered together Is equivalent to the summation of their individual pharmacological actions e.g. : Ephedrine + Aminophylline treatment

of bronchial asthma
Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 45

Synergistic Effect
1 + 1= X (>2)

When the total pharmacological action of

two or more drugs administered together is more than the summation of their individual pharmacological actions e.g. :Cotrimoxazole (Sulphamethoxazole + Trimethoprim) Septran
Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 45

Drug Dosing

OD - Once daily BD - Twice daily TD - Thrice daily QD - Four times daily SOS - During emergency use hs - At bed time Stat - Immediately Bolus - Amount of drug given as IV at a controlled but rapid rate Loading dose - Initial higher dose

ADVERSE DRUG REACTIONS (ADR) (Contd.)

Side effects: occur at normal therapeutic doses & are expected Untoward effects occur at therapeutic doses & are unexpected Toxic effects occur at high doses & /or manifest when the drug is used for a longer duration

Clinical Trials
PHASE OF A CLINICAL TRIAL

Phase I (max. tolerated dose & safety, comprises of small no. of patients) Phase II ( therapeutic effect ) Phase III (comparative study with the current standard therapy, comprises of large no. of patients) Phase IV / Post-marketing Surveillance (PMS) : continuing evaluation that takes place after FDA approval, when drug or treatment procedure is already in the market & available for general use

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