Bezitramide Explained

Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide.^[1] Bezitramide was discovered at Janssen Pharmaceutica in 1961.^{[2] [3] [4]} 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.^[5]

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.^[6] However, as of May 2021, it has never been marketed in the United States.

See also

• Benperidol
• Brorphine
• J-113,397

Notes and References

1. Meijer DK, Hovinga G, Versluis A, Bröring J, van Aken K, Moolenaar F, Wesseling H . Pharmacokinetics of the oral narcotic analgesic bezitramide and preliminary observations on its effect on experimentally induced pain . European Journal of Clinical Pharmacology . 27 . 5 . 615–8 . 1984 . 6519169 . 10.1007/BF00556902 . 23978449 .
2. US . 3196157 . patent . Benzimidalinyl Piperidines . 1963-06-11 . 1965-07-20 . Janssen PA .
3. Janssen PA, Niemegeers CJ, Schellekens KH, Marsboom RH, Herin VV, Amery WK, Admiraal PV, Bosker JT, Crul JF, Pearce C, Zegveld C . 6 . Bezitramide (R 4845), a new potent and orally long-acting analgesic compound . Arzneimittel-Forschung . 21 . 6 . 862–7 . June 1971 . 5109278 .
4. Knape H . Bezitramide, an orally active analgesic. An investigation on pain following operations for lumbar disc protrusion (preliminary report) . British Journal of Anaesthesia . 42 . 4 . 325–8 . April 1970 . 4913411 . 10.1093/bja/42.4.325 . free .
5. de Vos JC, Rohof OJ, Bernsen PJ, Conemans JM, van Unnik AJ . [Death caused by one tablet of Burgodin] . Nederlands Tijdschrift voor Geneeskunde . 127 . 34 . 1552–3 . August 1983 . 6633692 .
6. Web site: Title 21 United States Code (USC) Controlled Substances Act . 2011-09-29 . 2020-08-30 . https://web.archive.org/web/20200830032541/https://www.deadiversion.usdoj.gov/21cfr/21usc/812.htm . dead .