Novel depots of buprenorphine prodrugs have a long-acting antinociceptive effect

Anesthesia and Analgesia
Kuo-Sheng LiuJhi-Joung Wang

Abstract

An analgesic with a prolonged duration may be desirable in patients with long-lasting pain. In this study, we evaluated the antinociceptive effects and durations of action of three novel depots of buprenorphine esters buprenorphine propionate, enanthate, and decanoate given by IM injection, in rats. The pharmacokinetic profiles of buprenorphine in blood after IM injection of these depots were also evaluated. Antinociception was evaluated using the plantar test. Buprenorphine concentrations in blood were assayed using high-performance liquid chromatography. We found that the traditional form of buprenorphine HCl (in saline) produced a dose-related antinociceptive effect. A dose of 0.6 micromol/kg buprenorphine HCl (in saline) produced a significant antinociceptive effect lasting 5 h. The same dose of buprenorphine base, propionate, enanthate, and decanoate (in oil) also produced a significant antinociceptive effect with longer durations of action of 26, 28, 52, and 70 h, respectively. The pharmacokinetic studies demonstrated that all the buprenorphine esters were prodrugs of buprenorphine. We conclude that the novel depots of buprenorphine prodrugs: buprenorphine propionate, enanthate, and decanoate produced a long-acting antino...Continue Reading

References

Jul 1, 1976·Journal of Pharmaceutical Sciences·A J Sedman, J G Wagner
Feb 1, 1996·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·J Lerman
Oct 1, 1996·Pharmaceutical Research·A L StinchcombG L Flynn
Mar 7, 2001·The Journal of Clinical Endocrinology and Metabolism·A KamischkeE Nieschlag
Mar 23, 2005·Journal of Pain and Symptom Management·Rolley E JohnsonRichard Payne

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Citations

Jul 14, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jhi-Joung WangJia-You Fang
Apr 1, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Susan Weng LarsenClaus Larsen
Jul 30, 2020·European Journal of Pharmacology·Christina M LarsonCarolyn A Fairbanks

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