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Dezocine
Systematic (IUPAC) name
(5α,11α,13S)- 13-amino- 5,6,7,8,9,10,11,12- octahydro- 5-methyl- 5,11-methanobenzocyclodecen- 3-ol
Identifiers
CAS number 53648-55-8
ATC code N02AX03
PubChem 40841
DrugBank APRD00912
Chemical data
Formula C 16H23NO 
Mol. mass 245.36 g/mol
Synonyms Dezocine, Dalgan
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 2.2 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes intramuscular injection

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,[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]

References

  1. ^ 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.
  2. ^ Jacobs AM, Youngblood F. Opioid receptor affinity for agonist-antagonist analgesics. Journal of the American Podiatric Medical Association. 1992 Oct;82(10):520-4.
  3. ^ 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.
  4. ^ Camu F, Gepts E. Analgesic properties of dezocine for relief of postoperative pain. Acta Anaesthesiologica Belgica. 1979;30 Suppl:183-91.
  5. ^ Wuest HP, Bellville JW. The respiratory effects of dezocine and pentazocine in man. Journal of Clinical Pharmacology. 1979 Apr;19(4):205-10.
  6. ^ 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.
  7. ^ Oosterlinck W, Verbaeys A. Preliminary clinical experience with dezocine, a new potent analgesic. Current Medical Research and Opinion. 1980;6(7):472-4.
  8. ^ 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.
  9. ^ 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.
  10. ^ Romagnoli A, Keats AS. Ceiling respiratory depression by dezocine. Clinical Pharmacology and Therapeutics. 1984 Mar;35(3):367-73.
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