HLTH 471 & 671 (2022) - introduction to pharmacology, part 4

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University of Waterloo *

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471

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Health Science

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Oct 30, 2023

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Principles of Pharmacology Winter, 2022 HLTH 471/671

Key Points 1) Psychopharmacology defined. 2) Pharmacokinetics. 3) Pharmacodynamics.

cell surface R Internal R • agonist A molecule that selectively binds to a R, and evokes a response. • PHARMACODYNAMICS - Interaction of a drug molecule with a target tissue. - The initial site of action for many biologically active agents are large molecules known as receptors (R). Pharmacodynamics 15

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Pharmacodynamics ligands 16 drugs efficacy affinity ionotropic metabotropic transporter

• Rs recognise specific molecular structures. Continuum of Drug Activity full agonist partial agonist antagonist partial inverse agonist full inverse agonist Pharmacodynamics 17 n.b. drug agonists/antagonists are defined in relation to the ligand.

 drug antagonism Competitive Antagonist - competes with agonist for access to a binding site Non-competitive Antagonist - impairs agonist action by means other than activity at binding site morphine naloxone Pharmacodynamics 18

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se Pharmacodynamics 19 • DOSE-RESPONSE RELATIONSHIPS  dose-response curve - drug-receptor interactions are best described by the law of mass action : D + R DR biobehavioural effect monotonic dose-response curve A given biobehavioural effect ( ) for a given drug concentration ( ). Threshold minimum detectable respon ED50 dose that produces 50% of the maximal response

 potency and efficacy potency – dose required to produce an effect of a particular magnitude, relative to a given standard efficacy – maximal desirable effect that can be induced by a drug, relative to a given standard Pharmacodynamics 20

Pharmacodynamics drug administered absorption distribution excretion metabolism target interaction drug action drug effect receptors transporters pharmacodynamics 21

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