Dezocine

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Image:Dezocine.png
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 C16H23NO 
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.[1][1]

Dezocine has been found to be an effective painkiller comparable to meperidine (pethidine),[1] and so is a more effective analgesic than pentazocine, but causes relatively more respiratory depression than pentazocine.[1] It is a useful drug for the treatment of pain,[1] but side effects such as dizziness limit its clinical application,[1] and it can produce opioid withdrawal syndrome in patients already dependent on other opioids.[1]

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,[1] 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.[1]


References

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