List of prodrugs

See also: Naturally occurring sources § Precursors
Commons-emblem-notice.svg Please don't add precursors to this page but to List of precursors.

A prodrug is a chemical compound that, after administration, is metabolized (i.e. converted within the body) into a pharmacologically active substance.[1] Inactive prodrugs are pharmacologically inactive compounds that are metabolized into an active form within the body. Instead of administering a drug directly, a corresponding prodrug might be used instead to improve how a medicine is absorbed, distributed, metabolized, and excreted (ADME).

Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug.

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]

Examples of recreational psychoactive substances that act as prodrugs include GBL (prodrug for GHB), psilocybin (prodrug for psilocin), ALD-52 (prodrug for LSD).

List

Depressants

Hallucinogens

Cannabinoids

Deliriants

Dissociatives

Psychedelics

Nootropics

Stimulants

Miscellaneous

See also

External links

References

  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. https://doi.org/10.1351/pac199870051129
  2. ↑ Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/19502531
  3. ↑ The advantages of benzonal as an inducer of the liver mono-oxygenase enzyme system compared to phenobarbital. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/1305441
  4. ↑ Benzonal metabolism in guinea pigs. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2792358
  5. ↑ Deposition of diazepam and its metabolites in hair following a single dose of diazepam. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/27534563
  6. ↑ Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/7654478
  7. ↑ https://erowid.org/archive/rhodium/chemistry/ghb.html#GHV
  8. ↑ 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. 
  9. ↑ Morphine: pharmacokinetics and clinical practice. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2245160
  10. ↑ 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. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26655109
  11. ↑ The excretion of pethidine and its derivatives (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1703639/
  12. ↑ <https://pubchem.ncbi.nlm.nih.gov/compound/826660/
  13. ↑ <https://pubchem.ncbi.nlm.nih.gov/compound/826660
  14. ↑ Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28903606
  15. ↑ Recent Advances in Anaesthesia and Intensive Care | https://books.google.co.uk/books?id=ei1edut0AqAC&pg=PA42&redir_esc=y#v=onepage&q&f=false
  16. ↑ 16.0 16.1 16.2 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/19515014
  17. ↑ https://www.erowid.org/library/books_online/pihkal/pihkal062.shtml
  18. ↑ Effects of 3,4-methylenedioxymethamphetamine (MDMA) and its main metabolites on cardiovascular function in conscious rats (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3874698/
  19. ↑ Short-term effects of 2,4,5-trihydroxyamphetamine, 2,4,5-trihydroxymethamphetamine and 3,4-dihydroxymethamphetamine on central tryptophan hydroxylase activity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/8496826
  20. ↑ Major and minor metabolites of cocaine in human plasma following controlled subcutaneous cocaine administration. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17132243
  21. ↑ Determination of aminorex in human urine samples by GC-MS after use of levamisole. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/21531521
  22. ↑ (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. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/10027825
  23. ↑ 23.0 23.1 Active drug metabolites. An overview of their relevance in clinical pharmacokinetics. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2861928
  24. ↑ Metabolites of naloxone in human urine. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/5129377
  25. ↑ Atypical Psychotropic Agents | https://books.google.at/books?id=KfHEDgAAQBAJ&pg=PA460&redir_esc=y#v=onepage&q&f=false
  26. ↑ Comparative Pharmacology of Risperidone and Paliperidone. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2861928
  27. ↑ Engberg, G. O. R. A. N., Elebring, T. H. O. M. A. S., & Nissbrandt, H. (1991). Deprenyl (selegiline), a selective MAO-B inhibitor with active metabolites; effects on locomotor activity, dopaminergic neurotransmission and firing rate of nigral dopamine neurons. Journal of Pharmacology and Experimental Therapeutics, 259(2), 841-847.


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