What is the Origin of Cytochrome P450 Inhibition?

The term is rooted in biochemistry and pharmacology, stemming from the discovery and naming of the Cytochrome P450 enzyme superfamily, which is crucial for drug metabolism. The concept of inhibition is a pharmacological principle where a molecule interferes with the normal function of an enzyme. Clinical understanding of this process is paramount for safe and effective prescribing practices.

What is the Mechanism of Cytochrome P450 Inhibition?

Inhibitory molecules typically bind directly to the active site of the CYP enzyme, either reversibly or irreversibly, thereby blocking the access of the normal substrate. Reversible inhibition often involves competitive or non-competitive binding, while irreversible (mechanism-based) inhibition results in the formation of a stable, inactive enzyme-inhibitor complex. This reduction in enzymatic capacity slows the metabolic breakdown of substrates, altering their pharmacokinetics and extending their biological half-life.

Cytochrome P450 Inhibition

Meaning

Cytochrome P450 (CYP) inhibition is a drug-drug or drug-nutrient interaction where a substance decreases the metabolic activity of one or more enzymes in the CYP450 family. These enzymes are primarily responsible for the biotransformation and clearance of endogenous compounds, including hormones, and exogenous substances like medications. Inhibition can lead to elevated plasma concentrations of co-administered drugs or hormones, potentially causing toxicity or enhanced therapeutic effects.