QuickView for Pentazocine (compound)

Summary
General Info

PubChem

PubChem Compound 107799

Name:	Pentazocine
PubChem Compound ID:	107799
Description:	The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
Molecular formula:	C₁₉H₂₈ClNO
Molecular weight:	321.884 g/mol
Synonyms:	2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, hydrochloride, (2alpha,6alpha,11R)-; 68964-90-9; 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, hydrochloride, (2R,6R,11R)-rel-; 64024-15-3; (2alpha,6alpha,11R)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(3-methylbut-2-enyl)-2,6-methano-3-benzazocin-8-ol hydrochloride; Talwin (as hydrochloride); Pentazocine hydrochloride [USAN]; EINECS 264-612-1; Pentazocine hydrochloride; 359-83-1. show more » 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, hydrochloride, (2alpha,6alpha,11R)-; 68964-90-9; 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, hydrochloride, (2R,6R,11R)-rel-; 64024-15-3; (2alpha,6alpha,11R)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(3-methylbut-2-enyl)-2,6-methano-3-benzazocin-8-ol hydrochloride; Talwin (as hydrochloride); Pentazocine hydrochloride [USAN]; EINECS 264-612-1; Pentazocine hydrochloride; 359-83-1; (+-)-Pentazocine hydrochloride; (2R,6R,11R*)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol hydrochloride show less «

DrugBank

Identification

Name:	Pentazocine
Name (isomeric):	DB00652
Drug Type:	small molecule
Description:	The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
Synonyms:	Pentazocaine; Pentazocin; L-pentazocine
Brand:	Pentagin, Fortral, Fortalin, Talwan, Fortalgesic, Soseton, Sosigon, Liticon
Brand name mixture:	Talwin(pentazocine + naloxone), Talacen(pentazocine + acetaminophen)
Category:	Adjuvants, Anesthesia, Narcotic Antagonists, Narcotics, Analgesics, Opioid
CAS number:	359-83-1

Pharmacology

Indication:	For the relief of moderate to severe pain.
Pharmacology:	Pentazocine is a potent analgesic which when administered orally in a 50 mg dose appears equivalent in analgesic effect to 60 mg (1 grain) of codeine. Onset of significant analgesia usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer. Onset and duration of action and the degree... show more » Pentazocine is a potent analgesic which when administered orally in a 50 mg dose appears equivalent in analgesic effect to 60 mg (1 grain) of codeine. Onset of significant analgesia usually occurs between 15 and 30 minutes after oral administration, and duration of action is usually three hours or longer. Onset and duration of action and the degree of pain relief are related both to dose and the severity of pretreatment pain. Pentazocine weakly antagonizes the analgesic effects of morphine and meperidine; in addition, it produces incomplete reversal of cardiovascular, respiratory, and behavioral depression induced by morphine and meperidine. Pentazocine has about 1/50 the antagonistic activity of nalorphine. It also has sedative activity. show less «
Mechanism of Action:	The preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor.
Absorption:	Well absorbed from the gastro-intestinal tract.
Biotransformation:	Hepatic
Half Life:	2 to 3 hours
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take without regard to meals. Avoid alcohol.

Drug interaction:

Triprolidine

The CNS depressants, Triprolidine and Pentazocine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Targets

Mu-type opioid receptor

Kappa-type opioid receptor

Sigma 1-type opioid receptor