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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.[1] Inactive prodrugs are pharmacologically inactive medications that are metabolized into an active form within the body.

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.[citation needed]











External links


  1. 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.
  2. The advantages of benzonal as an inducer of the liver mono-oxygenase enzyme system compared to phenobarbital. ( / NCBI) |
  3. Benzonal metabolism in guinea pigs. ( / NCBI) |
  4. 4.0 4.1 Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. ( / NCBI) |
  5. Deposition of diazepam and its metabolites in hair following a single dose of diazepam. ( / NCBI) |
  6. Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. ( / NCBI) |
  7. Sawynok J (January 1986). "The therapeutic use of heroin: a review of the pharmacological literature". Can. J. Physiol. Pharmacol. 64 (1): 1–6. doi:10.1139/y86-001. PMID 2420426. 
  8. Morphine: pharmacokinetics and clinical practice. ( / NCBI) |
  9. Development of a sensitive method for the determination of oxycodone and its major metabolites noroxycodone and oxymorphone in human plasma by liquid chromatography-tandem mass spectrometry. ( / NCBI) |
  10. Recent Advances in Anaesthesia and Intensive Care |
  11. 11.0 11.1 11.2 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. ( / NCBI) |
  13. (Major and minor metabolites of cocaine in human plasma following controlled subcutaneous cocaine administration. ( / NCBI) |
  14. (S)-(-)-Cotinine, the major brain metabolite of nicotine, stimulates nicotinic receptors to evoke [3H]dopamine release from rat striatal slices in a calcium-dependent manner. ( / NCBI) |