Pentagin
Pentagin - General Information
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)
Pharmacology of Pentagin
Pentagin 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. Pentagin 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. Pentagin has about 1/50 the antagonistic activity of nalorphine. It also has sedative activity.
Pentagin for patients
Since sedation, dizziness, and occasional euphoria have been noted, ambulatory patients should be warned not to operate machinery, drive cars, or unnecessanly expose themselves to hazards. Pentazocine may cause physical and psychological dependence when taken alone and may have additive CNS depressant properties when taken in combination with alcohol or other CNS depressants.
Pentagin Interactions
Usage with Alcohol: Due to the potential for increased CNS depressants effects, alcohol should be used with caution in patients who are currently receiving pentazocine.
Pentagin Contraindications
TALWIN Nx should not be administered to patients who are hypersensitive to either pentazocine or naloxone.
Additional information about Pentagin
Pentagin Indication: For the relief of moderate to severe pain.
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.
Drug Interactions: Cimetidine Cimetidine increases the effect of the narcotic
Naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid dependent individuals
Food Interactions: Not Available
Generic Name: Pentazocine
Synonyms: L-pentazocine; Pentazocaine; Pentazocin
Drug Category: Adjuvants, Anesthesia; Analgesics, Opioid; Narcotic Antagonists; Narcotics
Drug Type: Small Molecule; Approved
Other Brand Names containing Pentazocine: Fortalgesic; Fortalin; Fortral; Liticon; Pentagin; Soseton; Sosigon; Talwan;
Absorption: Well absorbed from the gastro-intestinal tract.
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Hepatic
Half Life: 2 to 3 hours
Dosage Forms of Pentagin: Solution Intravenous
Tablet Oral
Chemical IUPAC Name: (1S,9S,13S)-1,13-dimethyl-10-(3-methylbut-2-en-1-yl)-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-4-ol
Chemical Formula: C19H27NO
Pentazocine on Wikipedia: https://en.wikipedia.org/wiki/Pentazocine
Organisms Affected: Humans and other mammals
