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A prodrug is a medication or compound that, upon administration, becomes metabolized (i.e. converted in the body) into a pharmacologically active substance. Depending on the substance, it may or may not possess intrinsic pharmacological activity of its own.
Prodrugs may be subject to a rate-limiting step in the conversion from inactive to active substance: in which case, only the duration, and not the intensity of the effect increases. Additionally, they may display other differences relating to pharmacokinetic factors (i.e. how a substance is absorbed, distributed, metabolized and excreted) compared its nonprodrug form.[Controversial]
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- C. G. Wermuth, C. R. Ganellin, P. Lindberg, L. A. Mitscher; Ganellin; Lindberg; Mitscher (1998). "Glossary of terms used in medicinal chemistry (IUPAC Recommendations 1998)". Pure and Applied Chemistry. 70 (5): 1129. https://doi.org/10.1351/pac199870051129