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Bezitramide

Opioid analgesic drug

Opioid analgesic drug

Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica in 1961. It is most commonly marketed under the trade name Burgodin.

The drug was pulled from the shelves in the Netherlands in 2004 after fatal overdose cases, including one where a five-year-old child took one tablet from his mother's purse, ate it, and promptly died.

Bezitramide is regulated much the same as morphine in all known jurisdictions and is a Schedule II substance under the United States' Controlled Substances Act of 1970, with an ACSCN of 9800 and zero annual manufacturing quota. However, as of May 2021, it has never been marketed in the United States.

References

References

  1. Anvisa. (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial". [[Diário Oficial da União]].
  2. (1984). "Pharmacokinetics of the oral narcotic analgesic bezitramide and preliminary observations on its effect on experimentally induced pain". European Journal of Clinical Pharmacology.
  3. "Benzimidalinyl Piperidines".
  4. (June 1971). "Bezitramide (R 4845), a new potent and orally long-acting analgesic compound". Arzneimittel-Forschung.
  5. (April 1970). "Bezitramide, an orally active analgesic. An investigation on pain following operations for lumbar disc protrusion (preliminary report)". British Journal of Anaesthesia.
  6. (August 1983). "[Death caused by one tablet of Burgodin]". Nederlands Tijdschrift voor Geneeskunde.
  7. "Title 21 United States Code (USC) Controlled Substances Act".
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synthetic-opioids prodrugs benzimidazoles piperidines nitriles ureas propionamides mu-opioid-receptor-agonists janssen-pharmaceutica belgian-inventions benzimidazole-opioids
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