Drug intelligence / Profile preview

pentazocine + acetaminophen

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Pentazocine + acetaminophen is an oral combination drug used for the relief of mild to moderate pain. It contains pentazocine, a Schedule IV opioid analgesic with mixed agonist/antagonist properties at opioid receptors, and acetaminophen, a non-opioid analgesic and antipyretic. Pentazocine primarily acts as an agonist at kappa opioid receptors and as a weak antagonist/partial agonist at mu opioid receptors, leading to pain relief while limiting some opioid side effects. Acetaminophen acts centrally to reduce pain and fever, though its exact mechanism is not fully understood. The combination provides additive analgesic effects and is intended for short-term use due to the risk of dependence, hepatotoxicity from acetaminophen overdose, and opioid withdrawal with abrupt cessation. This combination product was marketed under the brand name Talacen but has been discontinued in the United States[1][3][4][5].

Brand names
Talacen
Other names
pentazocine hydrochloride and acetaminophen
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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