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Agonism and Antagonism: Quantification

JoVE Central
Pharmacokinetics and Pharmacodynamics
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JoVE Central Pharmacokinetics and Pharmacodynamics
Agonism and Antagonism: Quantification

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01:14 min

October 10, 2024

When drugs are administered, they can elicit either an agonist or antagonist effect on the body. Agonism occurs when a drug activates a specific receptor, triggering a biological response. On the other hand, antagonism happens when a drug binds to the same receptors but blocks their activation, thereby preventing a biological response.

To quantify these effects, researchers use a dose-response curve, which provides valuable information about the potency and efficacy of a drug. Potency refers to the amount of drug required to produce a particular response, while efficacy measures the maximum therapeutic effect achievable with the drug.

In addition to agonism and antagonism, drug interactions play a significant role in determining the overall effect. Drug interactions can be additive or synergistic. Additive effects occur when the combined effect of two drugs equals the sum of their individual effects. For example, if one drug lowers blood pressure by ten units and another drug lowers it by fifteen units, their combined effect would be a reduction of twenty-five units in blood pressure.

Synergism, on the other hand, happens when the combined effect of two drugs exceeds the sum of their individual effects. This is commonly observed in the treatment of heart disease, where the combined effect of aspirin and clopidogrel on preventing blood clots surpasses what either drug could achieve alone.

To visually represent these interactions, researchers often use isobolograms. Isobolograms provide a graphical representation of the quantitative relationship between two drugs and their combined effect. This visual tool enables researchers to analyze and understand the nature of drug interactions more effectively.

Understanding the dynamics of drug effects and interactions is crucial in developing safe and effective treatments. Researchers can optimize drug therapy regimens, minimize adverse effects, and maximize therapeutic outcomes by comprehending the mechanisms of agonism, antagonism, and synergism.