Pharmacodynamics 2 - Basic pharmacology theory ISCM core block notes PDF

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Pharmacodynamics 2 – receptor theory 11.10.2019 LO: -Receptor theory -concentration-effect / dose-response curves, affinity, efficacy -agonists, antagonists, allosteric modulators -therapeutic range and therapeutic index Drug receptor: Used to describe anything a drug interacts with to cause an effect Binding sites: -receptors have an active (orthosteric) binding site for their endogenous, activating ligand – agonist -have high specificity to select appropriate ligand -ligand binding induces conformational changes to activate receptor -secondary binding site (allosteric) for other ligands (NOT used to activating endogenous ligands Affinity: The ability of a ligand to bind a target Efficacy: The ability of a ligand to generate an effect Both affinity and efficacy determine potency – the ability of a ligand to generate a response

Concentration-effect curve when measuring effect of drug at target site

Dose-response curve when measuring the physiological response to systemically administered drug Affinity and efficacy VS

When y-axis is in the same level, they are in same efficacy (able to deliver response) The more left of the ligand concentration, the more affinity of the ligands (or molecules / drugs)

Agonist – bind to the receptor and activate the receptor Antagonists – bind to the target and prevent receptor activation by agonists Full vs partial agonists: Full – induce a maximal response (100% of the endogenous agonist) Partial – induce a submaximal response (...