Dezocine
| File:Dezocine.svg | |
| Systematic (IUPAC) name | |
|---|---|
|
(5R,11S)- 13-amino- 5-methyl- 5,6,7,8,9,10,11,12-octahydro- 5,11-methanobenzo[10]annulen- 3-ol | |
| Clinical data | |
| Routes of administration | Oral |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Metabolism | Hepatic |
| Biological half-life | 2.2 hours |
| Identifiers | |
| CAS Number | 53648-55-8 |
| ATC code | N02AX03 (WHO) |
| PubChem | CID 40841 |
| DrugBank | APRD00912 |
| Synonyms | WY-16,225 |
| Chemical data | |
| Formula | C16H23NO |
| Molar mass | 245.36 g/mol[[Script error: No such module "String".]] |
| Script error: No such module "collapsible list". | |
Dezocine (Dalgan) is an opioid analgesic related to pentazocine, with a similar profile of effects that include analgesic action and euphoria at low doses,[1] but produces dysphoria and hallucinations at high doses, most likely due to action at κ-opioid receptors.[2][3]
Dezocine has been found to be an effective painkiller comparable to meperidine (pethidine),[4] and so is a more effective analgesic than pentazocine, but causes relatively more respiratory depression than pentazocine.[5] It is a useful drug for the treatment of pain,[6] but side effects such as dizziness limit its clinical application,[7] and it can produce opioid withdrawal syndrome in patients already dependent on other opioids.[8]
Dezocine is unusual among opioids as it is one of the only primary amines known to be an active opioid (along with bisnortilidine, an active metabolite of tilidine). It is a mixed agonist-antagonist as with other drugs in this class,[9] 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.[10]
See also
References
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- ↑ 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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- Opioids
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