Pentazocine Stats & Data
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DrugBankDescription
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)
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.
Pharmacodynamics
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.
Absorption
Well absorbed from the gastro-intestinal tract.
Indication
For the relief of moderate to severe pain.
Toxicity
PubChemThe preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor.
Carcinogenicity
No indication of carcinogenicity to humans (not listed by IARC).
Health effects (PubChem excerpts)
Medical problems can include congested lungs, liver disease, tetanus, cardiovascular effects, infection of the heart valves, skin abscesses, anemia and pneumonia. Death can occur from overdose.
Effect Profile
Curated + 3 ReportsStrong euphoria with mild sedation and itching/nausea
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Acute tolerance: develops within a single session — the reset numbers above apply after sustained heavy use, not after one binge. Within-session tachyphylaxis usually resets largely overnight.
Experience Report Analysis
ErowidDemographics
Gender Distribution
Age Distribution
Reports Over Time
Form / Preparation
Most common forms and preparations reported
Opioid Equivalence (MME)
NIH HEAL 2024 & CDC 2022Pentazocine 27 mg oral ≈ 10 mg Morphine oral