What is the Origin of CYP2C19 Inhibition?

This concept is central to clinical pharmacology and drug metabolism studies, specifically concerning the Cytochrome P450 system located predominantly in the liver's endoplasmic reticulum. CYP2C19 is polymorphic and metabolizes numerous therapeutic agents, including proton pump inhibitors and certain antidepressants. Inhibition studies are essential for establishing safe medication protocols.

What is the Mechanism of CYP2C19 Inhibition?

Inhibition typically involves a competitive or non-competitive binding of the inhibitor molecule to the active site of the CYP2C19 enzyme, preventing the intended substrate from undergoing oxidative metabolism. The resulting functional reduction in enzyme activity prolongs the half-life of substrate drugs, thereby altering their systemic exposure and pharmacological effect. This mechanism underscores the need for careful review of concomitant medications.

CYP2C19 Inhibition ∞ Area

CYP2C19 Inhibition

Meaning

CYP2C19 inhibition describes the process where a substance directly or indirectly reduces the metabolic activity of the Cytochrome P450 2C19 enzyme, a major hepatic enzyme involved in drug clearance. The consequence of this inhibition is a decreased rate of substrate breakdown, potentially leading to elevated plasma concentrations of co-administered drugs and an increased risk of adverse effects or toxicity. Clinical assessment of drug-drug interactions often focuses on this pathway.