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4.9: Dose-Response Relationship: Potency and Efficacy

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JoVE Core
Pharmacology

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Dose-Response Relationship: Potency and Efficacy
 
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4.9: Dose-Response Relationship: Potency and Efficacy

The potency of a drug is the measure of its ability to produce a biological response and can be compared by looking at the half-maximum effective concentration or EC50 values of different drugs. A lower EC50 value indicates higher potency of the drug. In the dose–response curve of two antihypertensive drugs, candesartan and irbesartan, a significant difference is observed in their EC50 values. A lower EC50 value for candesartan indicates that it is more potent than irbesartan, as it produces the same desired effect at a lower dose. It is noteworthy that both drugs exhibit similar maximum effect or Emax values, implying that they possess equal efficacy. Efficacy depends on the number of drug–receptor complexes formed and the extent of receptor activation. Maximal efficacy is achieved when all receptors are occupied, rendering further increases in drug concentration incapable of eliciting additional responses. Full agonists have high efficacy, as they activate receptors entirely and elicit a complete response. The efficacy of partial agonists is lower, as they activate receptors to a lesser extent. Antagonists, in contrast, exhibit zero efficacy by not activating the receptors. Instead, they act as blockers and either reduce the number of available receptors for agonist binding or induce conformational changes that prevent effective agonist binding. Overall, these factors play a crucial role in determining the efficacy and potency of drugs, which, in turn, can determine their usefulness in treating various medical conditions.

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Dose-response Relationship Potency Efficacy EC50 Value Antihypertensive Drugs Candesartan Irbesartan Maximum Effect Emax Value Drug-receptor Complexes Receptor Activation Full Agonists Partial Agonists Antagonists Zero Efficacy

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