|Systematic (IUPAC) name|
|Mol. mass||245.36 g/mol|
|Half life||2.2 hours|
Dezocine (Dalgan, WY-16225) is an opioid analgesic related to pentazocine, with a similar profile of effects that include analgesic action and euphoria at low doses, but produces dysphoria and hallucinations at high doses, most likely due to action at κ-opioid receptors.
Dezocine has been found to be an effective painkiller comparable to meperidine (pethidine), and so is a more effective analgesic than pentazocine, but causes relatively more respiratory depression than pentazocine. It is a useful drug for the treatment of pain, but side effects such as dizziness limit its clinical application, and it can produce opioid withdrawal syndrome in patients already dependent on other opioids.
Dezocine is unusual among opioids as it is the only primary amine known to be an active opioid. It is a mixed agonist-antagonist as with other drugs in this class, and despite having a stronger respiratory depressant effect than morphine, dezocine shows a ceiling effect on its respiratory depressive action so above a certain dose this effect does not get any more severe.
- ↑ Zacny JP, Lichtor JL, de Wit H. Subjective, behavioral, and physiologic responses to intravenous dezocine in healthy volunteers. Anesthesia and Analgesia. 1992 Apr;74(4):523-30.
- ↑ Jacobs AM, Youngblood F. Opioid receptor affinity for agonist-antagonist analgesics. Journal of the American Podiatric Medical Association. 1992 Oct;82(10):520-4.
- ↑ Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J. Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacology. 2006 Jan 25;6:3.
- ↑ Camu F, Gepts E. Analgesic properties of dezocine for relief of postoperative pain. Acta Anaesthesiologica Belgica. 1979;30 Suppl:183-91.
- ↑ Wuest HP, Bellville JW. The respiratory effects of dezocine and pentazocine in man. Journal of Clinical Pharmacology. 1979 Apr;19(4):205-10.
- ↑ O'Brien JJ, Benfield P. Dezocine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs. 1989 Aug;38(2):226-48.
- ↑ Oosterlinck W, Verbaeys A. Preliminary clinical experience with dezocine, a new potent analgesic. Current Medical Research and Opinion. 1980;6(7):472-4.
- ↑ Strain EC, Preston KL, Liebson IA, Bigelow GE. Opioid antagonist effects of dezocine in opioid-dependent humans. Clinical Pharmacology and Therapeutics. 1996 Aug;60(2):206-17.
- ↑ Young AM, Stephens KR, Hein DW, Woods JH. Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids. Journal Pharmacology and Experimental Therapeutics. 1984 Apr;229(1):118-26.
- ↑ Romagnoli A, Keats AS. Ceiling respiratory depression by dezocine. Clinical Pharmacology and Therapeutics. 1984 Mar;35(3):367-73.
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