Pentazocine
- Atc Codes:N02AD01
- CAS Codes:359-83-1#64024-15-3
- PHARMGKB ID:359-83-1#64024-15-3
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Fortal; Cyprus: Sosegon; Czech Republic: Fortral; France: Fortal; Greece: Fortal; Italy: Talwin; Luxembourg: Fortal, Fortral; Netherlands: Fortral; Poland: Fortral, Pentazocinum; Romania: Fortral; Slovakia: Fortral; Slovenia: Fortral; Spain: Pentazocina, Sosegón; UK: Fortral, Pentazocine.
North America
Canada: Talwin; USA: Talwin.
Asia
Japan: Hexat, Peltazon, Pentagin, Sosegon, Tosparyl.
Drug combinations
Pentazocine and Acetaminophen
Pentazocine and Aspirin
Pentazocine and Naloxone
Chemistry
Pentazocine: C~19~H~27~NO. Mw: 285.42. (1) 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, (2α,6α,11R*)-; (2)(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. CAS-359-83-1 (1963).
Pentazocine Hydrochloride: C~19~H~27~NO HCl. 321.88. 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(3-methyl-2-butenyl)-, hydrochloride, (2α,6α,11R*)-. CAS-64024-15-3 (1969).
Pharmacologic Category
Analgesics and Antipyretics; Opiate Partial Agonists. (ATC-Code: N02AD01).
Mechanism of action
Binds to opiate receptors in CNS, causing inhibition of ascending pain pathways, altering perception of and response to pain. Produces generalized CNS depression. Partial agonist-antagonist.
Therapeutic use
Relief of moderate-to-severe pain. Also used as sedative prior to surgery and as supplement to surgical anesthesia.
Pregnancy and lactiation implications
Teratogenic in animal studies. Crosses human placenta. Use should be avoided during labor and delivery of premature infants. Abstinence syndromes in newborn reported after long-term use of pentazocine during pregnancy. Excretion in breast milk unknown (use caution).
Unlabeled use
Contraindications
Hypersensitivity to pentazocine, naloxone, or any component of the formulation.
Warnings and precautions
May cause CNS depression. Severe sclerosis occurred at injection site following multiple injections (avoid SubQ use unless absolutely necessary). May cause hypotension (use with caution in hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics)). May obscure diagnosis or clinical course of acute abdominal conditions. Use with caution in adrenal insufficiency, including Addison’s disease, in biliary tract dysfunction (acute pancreatitis may cause constriction of sphincter of Oddi), and in CNS depression or coma. Potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. Use with caution due to potential for increased risk of CNS-depressant effects. Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure. Use with caution in hepatic dysfunction, in morbidly obese patients, in prostatic hyperplasia and/or urinary stricture, in renal dysfunction, and in pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function. Use with caution in history of seizure disorders, and in thyroid dysfunction. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in debilitated patients (greater potential for critical respiratory depression), and in the elderly. Injection may contain sulfites (may cause allergic reaction). Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with μ-opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.