The pharmacokinetics of pentazocine and tripelennamine

@article{Yeh1986ThePO,
  title={The pharmacokinetics of pentazocine and tripelennamine},
  author={S. Y. Yeh and G. Daniel Todd and R. E. Johnson and Charles W. Gorodetzky and W. Robert Lange},
  journal={Clinical Pharmacology \& Therapeutics},
  year={1986},
  volume={39}
}
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 t½values 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… 
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Author index
Clinical Pharmacology and Therapeutics (1986) 39, 707–714; doi:10.1038/clpt.1986.126

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The studies suggest that the antihistamine tripelennamine has abuse potential, and that in combination with pentazocine, the euphoric effects of the opioid are enhanced and its dysphoric properties attenuated.
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TLDR
A spectrophotofluorometric method for the quantitative determination of pentazocine plasma levels in man, which detects concentrations as low as 0.03 µg per milliliter is described, which coincides closely with onset, duration, and intensity of analgesia, as well as with other pharmacologic effects.
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TLDR
Pentazocine was well absorbed by all the common routes of administration and the rate of metabolism seemed to be the factor which controlled the blood levels achieved and it is hoped that studies such as this can be useful in providing greater therapeutic efficiency and a reduction in side effects.
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  • S. Yeh
  • Medicine, Chemistry
    Pharmacology Biochemistry and Behavior
  • 1986
TLDR
Results of this study demonstrate that pentazocine antinociception can be potentiated by several antihistamines and that the potentiation was not due to a mutual effect on metabolism but rather through an as yet undefined mechanism.
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TLDR
The findings suggest that addition of a vasoconstrictor to tripelennamine and diphenhydramine might increase the depth and duration of anesthesia and aid hemostasis.
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