Dezocine: Difference between revisions

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{{drugbox |
{{drugbox |
| IUPAC_name        = (5α,11α,13S)-13-amino-5,6,7,8,9,10,11,12-octahydro -5-methyl-5,11-methanobenzocyclodecen-3-ol
| IUPAC_name        = (5α,11α,13S)-13-amino-5,6,7,8,9,10,11,12-octahydro -5-methyl-5,11-methanobenzocyclodecen-3-ol
| image            = Dezocine.png
| image            = Dezocine Wiki Str.png
| width            = 140
| width            = 140
| CAS_number        = 53648-55-8
| CAS_number        = 53648-55-8
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| routes_of_administration = intramuscular injection
| routes_of_administration = intramuscular injection
}}
}}
 
__NOTOC__
{{SI}}
{{CMG}}
== Overview ==
'''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,<ref>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.</ref> but produces [[dysphoria]] and [[hallucinations]] at high doses, most likely due to action at [[Kappa opioid receptor|κ-opioid receptors]].<ref>Jacobs AM, Youngblood F. Opioid receptor affinity for agonist-antagonist analgesics. Journal of the American Podiatric Medical Association. 1992 Oct;82(10):520-4.</ref><ref>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.</ref>  
'''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,<ref>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.</ref> but produces [[dysphoria]] and [[hallucinations]] at high doses, most likely due to action at [[Kappa opioid receptor|κ-opioid receptors]].<ref>Jacobs AM, Youngblood F. Opioid receptor affinity for agonist-antagonist analgesics. Journal of the American Podiatric Medical Association. 1992 Oct;82(10):520-4.</ref><ref>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.</ref>  


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== References ==
== References ==
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Latest revision as of 15:32, 13 April 2015

Dezocine
Clinical data
SynonymsDezocine, Dalgan
Routes of
administration		intramuscular injection
ATC code
Pharmacokinetic data
MetabolismHepatic
Elimination half-life2.2 hours
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC16H23NO
Molar mass245.36 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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 the only primary amine known to be an active opioid. 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]


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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.

Template:Opioids

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