The pharmacokinetics of pentazocine and tripelennamine

  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},
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… 
Metabolic profile of tripelennamine in humans.
  • S. Yeh
  • Chemistry, Medicine
    Journal of pharmaceutical sciences
  • 1991
Tripelennamine and its metabolites were identified by GC/MS and total amounts 2-[alpha-hydroxybenzyl(2-dimethylaminoethyl)amino]pyridine(alpha- hydroxytripelennamines) plus an unidentified metabolite were found to be 0.85% of the dose, respectively.
Potentiation of pentazocine conditioned place preference by tripelennamine in rats
It is suggested that the dopaminergic system, especially at the D1 receptor, plays an important role in the potentiation effect of tripelennamine on the pentazocine-induced place preference.
Influence of pentazocine on serum lipids and selected enzymes of male wistar rats
Administration of pentazocine to adult male rats (3 mg/kg body weight/day) for 10 or 20 days decreased their body weight significantly. The protein content of the serum also decreased significantly,
In vitro characterization of cytochrome P450 2D6 inhibition by classic histamine H1 receptor antagonists.
It is demonstrated that classic histamine H1 receptor antagonists, available in over-the-counter preparations, inhibit CYP2D6 in vitro, suggesting that, under specific circumstances, clinically relevant interactions between classic antihistamines and CYP 2D6 substrates might occur.
Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes
All five H1-antihistamines studied inhibited CYP2D6 markedly, but only cyclizine and promethazine inhibited CyP2C9 at concentrations above that usually seen in plasma.
Quantification of Pentazocine in Human Plasma by HPLC with Electrochemical Detection
Abstract A rapid and sensitive high performance liquid chromatographic method with electrochemical detector was described to measure pentazocine concentrations in plasma. The separation of
Pharmacokinetic analysis of the FAK scaffold inhibitor C4 in dogs
The pharmacokinetic study revealed that C4 has linear pharmacokinetics and does not accumulate following multiple-dose administration, which will help facilitate further development of C4.
Pentazocine inhibits norepinephrine transporter function by reducing its surface expression in bovine adrenal medullary cells.
Findings suggest that PTZ inhibits the NET function by reducing the amount of NET in the cell surface membranes through an opioid and σ-receptor-independent pathway.
HRGC assay of antihistaminic drugs in plasma samples using a nitrogen-phosphorus detector
Thirteen antihistaminic drugs are separated on a CP-Sil 5 capillary column and are evaluated by a NP detector after extraction of spiked plasma samples, alkalinized, in a solvent mixture of
Author index
Clinical Pharmacology and Therapeutics (1986) 39, 707–714; doi:10.1038/clpt.1986.126


The clinical pharmacology of pentazocine and tripelennamine (T's and Blues).
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.
Relationship of pentazocine plasma levels to pharmacological activity in man
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.
The absorption and excretion of pentazocine after administration by different routes.
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.
The effect of antihistaminic drugs on pentazocine antinociception in the rat
  • S. Yeh
  • Medicine, Chemistry
    Pharmacology Biochemistry and Behavior
  • 1986
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.
Characterization of the interaction of pentazocine and tripelennamine: Drug discrimination and mu-receptor binding assay
It is concluded that the addition of T to P increases the mu-like subjective effects of P and this effect may be due to enhanced affinity of P for themu-receptor.
Increased brain uptake of morphine in the presence of the antihistamine tripelennamine
Data suggest that pharmacokinetic factors play a role in the potentiation of opiate effects by antihistamine on concurrent i.v. administration of the two drugs.
Analgesic potentiation and the distribution of morphine in the presence of triplennamine in mice.
Naloxone completely reversed the analgesia of MS and the MS-TRP combination and the distribution of 3H morphine in representative brain areas and plasma was not different in the presence or absence of triplennamine.
Potentiation of narcotic-induced antinociception by tripelennamine in morphine-tolerant and drug-naive mice.
It is concluded that the abuse of various narcotic-tripelennamines combinations can be attributed, at least in part, to a specific property of tripelennamine to potentiate narcotic effects in the drug-naive and morphine-tolerant state.
Effects of short‐ and long‐term administration of pentazocine in man
It is concluded that pentazocine has an abuse potential which is less than that with morphine but greater than that that with nalorphine.
The findings suggest that addition of a vasoconstrictor to tripelennamine and diphenhydramine might increase the depth and duration of anesthesia and aid hemostasis.