Cytochrome P450 System

The hepatic cytochrome P450 system is a family of enzymes that is responsible for oxidative phase I metabolism. The major cytochrome P450 enzyme families that are active in humans are CYP1, CYP2, and CYP3. These families are further divided into subfamilies that include 1A2, 2C9, 2C19, 2D6, 2E1, and 3A4 (Lewis and Ito 2008).

Substrates are those agents that are metabolized by the cytochrome enzyme subsystems. An inhibitor may decrease or block enzyme activity required for drug metabolism and cause an elevated concentration of the circulating drug with potential to increase therapeutic or toxic effects. An inducer increases metabolic enzyme activity and results in a decreased concentration of circulating substrate drug and an increased concentration of metabolites (Pelkonen et al. 2008; Zhou 2008). This may lead to decreased therapeutic effect or to increased tox-icity due to the elevation of toxic metabolite concentrations. Knowledge of whether a drug has an inhibitory or inductive effect on a specific enzyme may help predict potential drug interactions.

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