General Pharmacology

Dr Nasim Ullah Siddiqui

What is Pharmacology?
Pharmacology:
Pharmacon (drugs) + Logos (studies) The study of drugs

Drugs & Medicines

Drugs:
Any substance that, when absorbed into the body of a living organism, alters (changes) normal body function Examples:
aspirin, Antibiotics, Nicotine, alcohol, Marijuana.
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Drugs & Medicines

Medicines:
In pharmacology, a drug is a chemical substance used in the:
treatment, cure, prevention, or diagnosis of disease Or used to enhance physical or mental well-being

Drugs & Medicines

Drug is called medicine when used in proper dosage form for safe administration All medicines are drugs but all drugs are not medicines

Clinical / Experimental
Clinical Pharmacology
deals with the study of drug effects in humans beings, i.e. healthy volunteers and patients

Experimental Pharmacology
deals with the study of drug effects in laboratory animals
In vitro Isolated tissue In vivo Intact organism

Definitions
Toxicology:
deals with adverse (undesired) reactions of drugs & their treatment

Pharmacogenetics:
How genetics influence the mode of drug actions (e.g.. Metabolism) and biological variations of drug responses

Definitions
Pharmacogenetics is generally regarded as the study or clinical testing of genetic variation that gives rise to differing response to drugs.

Pharmacogenetics refers to genetic differences in metabolic pathways which can affect individual responses to drugs, both in terms of therapeutic effect as well as adverse effects.
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Definitions
Pharmacokinetics:
How the body handles the drug Includes absorption, distribution , biotransformation, and elimination

Pharmacodynamics:
How drug handles the body Deals with the biochemical and physiological effects of drugs on man

Definitions Receptors
Biochemical receptors are large protein molecules that can be activated by the binding of a ligand (such as a hormone or drug). Receptors can be membrane-bound, occurring on the cell membrane of cells, or intracellular, such as on the nucleus or mitochondrion. Binding occurs as a result of noncovalent /covalent interaction between the receptor and its ligand, at locations called the binding site on the receptor.
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Potency is a measure of drug activity

expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug (e.g., morphine) evokes a larger response at low concentrations. while a drug of lower potency (acetylsalicylic acid) evokes a small response at low concentrations It is proportional to affinity and efficacy
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Definitions

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Definitions
Affinity is the ability of the drug to bind to a
receptor.

Efficacy is the relationship between receptor

occupancy and the ability to initiate a response at the molecular, cellular, tissue or system level. The response is equal to the effect(E), and depends on both the drug binding and the drugbound receptor then producing a response; thus, potency depends on both affinity and efficacy.
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Drug Responses
How are drug responses produced? By interaction with active binding sites called RECEPTORS
Drug may be agonist or antagonist for the receptors

Definitions
The agonist (ligand, drug or hormone) that
binds to the receptor and initiates the response.

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Definitions
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks agonistmediated responses. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally-defined binding sites on receptors. Antagonists have affinity but no efficacy for their receptors, and binding will disrupt the interaction and inhibit the function of an agonist at receptors.
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Antagonist
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. Physiological antagonists, substances that have opposing physiological actions, but act at different receptors. For example, histamine lowers arterial pressure through vasodilation at the histamine H1 receptor, while adrenaline raises arterial pressure through vasoconstriction mediated by -adrenergic receptor activation.
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Tachyphylaxis : Rapidly developed tolerance is

tachyphylaxis, is a medical term describing a decrease in the response to a drug due to previous exposure to that drug. Caused by depletion or marked reduction of the amount of neurotransmitter responsible for creating the drug's effect, or by the depletion of receptors available for the drug or neurotransmitter to bind to. Examples: Amphetamine, ephedrine (indirectly acting drugs) Tachyphylaxis is characterized by the rate sensitivity i.e, a high-intensity prolonged stimulus or oftenrepeated stimulus may bring about a diminished response also known as desensitization.
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Definitions