Drug metabolism

[Merna]

Drug metabolism is the chemical alteration of a drug by the body.
Some drugs are chemically altered by the body (metabolized). The substances that result from metabolism (metabolites) may be inactive, or they may be similar to or different from the original drug in therapeutic activity or toxicity. Some drugs, called prodrugs, are administered in an inactive form, which is metabolized into an active form. The resulting active metabolites produce the desired therapeutic effects. Metabolites may be metabolized further instead of being excreted from the body. The subsequent metabolites are then excreted. Excretion involves elimination of the drug from the body, for example, in the urine or bile.
Most drugs must pass through the liver, which is the primary site for drug metabolism. Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms. The liver’s primary mechanism for metabolizing drugs is via a specific group of cytochrome P-450 enzymes. The level of these cytochrome P-450 enzymes controls the rate at which many drugs are metabolized. The capacity of the enzymes to metabolize is limited, so they can become overloaded when blood levels of a drug are high (see Genetic Makeup and Response to Drugs).
Many substances (such as drugs and foods) affect the cytochrome P-450 enzymes. If these substances decrease the ability of the enzymes to break down a drug, then that drug