Abstract

Lipid-soluble drugs are metabolized in the body to water-soluble compounds so that they can be excreted in the urine. Usually these metabolites are inactive, but sometimes drugs may be converted into metabolites that are pharmacologically active. A pro-drug is a drug that is inactive in its own right but is metabolized in the body to an active compound. An example is cyclophosphamide, which is metabolized to phosphoramide mustard in the liver, thus reducing intestinal toxicity. Alternatively the parent drug may be active and then metabolized into another active drug that may have beneficial or adverse effects. Morphine-6-glucuronide is an important example of an active metabolite that has useful analgesic activity in its own right but may cause respiratory depression.

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