Phase 1 Metabolism

Flashcards covering key concepts and vocabulary related to Phase 1 Metabolism and its implications in pharmacotherapy.

Phase I Metabolism

Converts the parent drug to a more polar metabolite by introducing or unmasking a functional group.

Cytochrome P450 (CYP)

A family of enzymes important in phase I drug metabolism, accounting for approximately 80% of this process.

Therapeutic Index

The ratio between the toxic dose and the effective dose of a drug, indicating its safety margin.

Narrow Therapeutic Index (NTI) drugs

Drugs with little separation between therapeutic and toxic doses, requiring careful monitoring.

First Pass Metabolism

The metabolism of a drug before it reaches systemic circulation, affecting drug dosing and therapeutic efficacy.

Drug Metabolism

The chemical alteration of a drug by the body, primarily in the liver, to facilitate elimination.

Polymorphism

Genetic variation that may affect an individual’s response to drugs due to differences in enzyme activity.

Substrate

A substance that is metabolized by an enzyme, such as a drug or hormone.

Inducers

Substances that increase enzyme activity, leading to enhanced metabolism of substrates.

Inhibitors

Substances that decrease or halt enzyme activity, potentially leading to increased drug levels in the body.