The pharmacokinetics of pentazocine and tripelennamine

Clin Pharmacol Ther. 1986 Jun;39(6):669-76. doi: 10.1038/clpt.1986.117.


The pharmacokinetics of single and combined doses of pentazocine HCl (40 and 80 mg) and tripelennamine HCl (50 and 100 mg) were studied in six healthy drug abusers. After intramuscular administration of 40 or 80 mg pentazocine alone, mean peak plasma concentrations at 15 minutes were 102 and 227 ng/ml, respectively, and mean plasma t1/2 values were 4.6 and 5.3 hours, respectively. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively. After concurrent administration of pentazocine with tripelennamine, plasma pentazocine and tripelennamine concentrations at all time points were not significantly different from those when pentazocine or tripelennamine was administered alone. Coadministration of pentazocine and tripelennamine had no effect on the distribution, elimination, and clearance of either pentazocine or tripelennamine. In conclusion, there did not appear to be a clinically significant metabolic interaction between pentazocine and tripelennamine.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Adult
  • Analysis of Variance
  • Chromatography, Gas
  • Double-Blind Method
  • Drug Combinations
  • Drug Interactions
  • Half-Life
  • Humans
  • Injections, Intramuscular
  • Kinetics
  • Male
  • Middle Aged
  • Pentazocine / administration & dosage
  • Pentazocine / blood
  • Pentazocine / metabolism*
  • Random Allocation
  • Tripelennamine / administration & dosage
  • Tripelennamine / blood
  • Tripelennamine / metabolism*


  • Drug Combinations
  • Tripelennamine
  • Pentazocine