Summary
The interaction between a single oral dose of 130 mg propoxyphene and 0.5 g/kg body weight ethanol was investigated in 12 healthy male volunteers by 9 objective performance tests, 8 visual analogue self-rating scales and the measurement of plasma propoxyphene, norpropoxyphene and ethanol concentrations, using a double-blind threeway crossover design. Volunteers were each given one of three treatments, propoxyphene + ethanol, placebo + ethanol and propoxyphene alone, separated by a two week interval. The performance tests were completed before and 1.25 and 4 h after drug intake, and the self-rating scales before and 1.25, 4 and 10 h after it.
Ethanol was shown to enhance the bioavailability of propoxyphene by 25% probably by reducing its first-pass metabolism. However, despite this pharmacokinetic effect no pharmacodynamic interaction was found. Subjective ratings disclosed that the effect of ethanol on physical and mental sedation predominated over the effects of propoxyphene.
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References
Ali NA, Marshall EM, Allen DF, Richens A (1985) Comparison of the effects of therapeutic doses of meptazinol and a propoxyphene/paracetamol mixture alone and in combination with ethanol on ventilatory function and saccadic eye movements. Br J Clin Pharmacol 20: 631–637
Bond A, Lader M (1974) The use of analogue scales in rating subjective feelings. Br J Med Psychol 47: 211–218
Bradley CM, Nicholson AN (1987) Studies on performance with aspirin and paracetamol and with the centrally acting analgesics meptazinol and pentazocine. Eur J Clin Pharmacol 32: 135–139
Due AL, Sullivan HR, McMahon RE (1976) Propoxyphene: pathways of metabolism in man and laboratory animals. Biomed Mass Spectrom 3: 217–225
Finkle BS, McCloskey KL, Kiplinger GF, Bennett IF (1976) A national assessment of propoxyphene in post-mortem medicolegal investigation 1972–1975. J Forensic Sci 21: 706–742
Girre C, Bertaux L, Dussaucy E, Bonnet D, Palombo S, Fournier PE (1990) Comparison of the effect of two prazepam formulations on psychomotor and cognitive function in healthy volunteers. Inter Clin Psychopharmacol 5: 57–64
Gram LF, Schou J, Way WL, Heltberg J, Bodin NO (1979) Propoxyphene kinetics after single oral and intravenous doses in man. Pharmacol Ther 26: 473–482
Hindmarch I (1980) Psychomotor function and psychoactive drugs. Br J Clin Pharmacol 10: 189–209
Kiplinger GF, Sokol G, Rodda BE (1974) Effect of combined alcohol and propoxyphene on human performance. Arch Int Pharmacodyn 212: 175–180
Mezey E (1976) Ethanol metabolism and ethanol-drug interactions. Biochem Pharmacol 25: 869–875
Oguma T, Levy G (1981) Acute effect of ethanol on hepatic first-pass elimination of propoxyphene in rats. J Pharmacol Exp Ther 219: 7–13
Olsen H, Bodd E, Meyer T, Morland J (1983) Ethanol interaction with propoxyphene and norpropoxyphene metabolism in isolated rat hepatocytes. Pharmacol Biochem Behav 18 [Suppl 1]: 301–304
Sellers EM, Holloway MR (1978) Drug kinetics and alcohol ingestion. Clin Exp Biol Med 156: 440–452
Sellers EM, Hamilton CA, Kaplan HL, Degani NC, Foltz RL (1985) Pharmacokinetic interaction of propoxyphene with ethanol. Br J Clin Pharmacol 19: 398–401
Stein SW, Lieber CS, Leevy CM, Cherrick GR, Abelmann WH (1963) The effect of ethanol upon systemic and hepatic blood flow in man. Am J Clin Nutr 13: 509–513
Wolen RI, Gruber CM, Kiplinger GF, Scholz NE (1971) Concentration of propoxyphene in human plasma following oral, intramuscular and intravenous administration. Toxicol Appl Pharmacol 19: 480–492
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Girre, C., Hirschhorn, M., Bertaux, L. et al. Enhancement of propoxyphene bioavailability by ethanol. Eur J Clin Pharmacol 41, 147–152 (1991). https://doi.org/10.1007/BF00265908
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DOI: https://doi.org/10.1007/BF00265908