Summary
Plasma levels of diphenhydramine were determined by gas chromatography up to 34 h after oral administration of 50 mg to 6 healthy men. The antihistaminic activity of diphenhydramine was assessed by reduction in the area of wheals induced by intradermal injection of 5 µg histamine hydrochloride. The plasma level of drug and reduction in size of wheal were related in 4 of the 6 subjects, but not in the other two although all six had similar concentrations of the drug in plasma. In two experiments designed to measure psychometric parameters (number facility and a time evaluation test), no relationship was found between plasma levels of diphenhydramine and the performances of the subjects.
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Bain, W. A.: The quantitative comparison of histamine antagonists in man. Proc. roy. Soc. Med.42, 615–623 (1948)
Bilzer, W., Gundert-Remy, U.: Determination of nanogram quantities of diphenhydramine and orphenadrine in human plasma using gas liquid chromatography. Europ. J. clin. Pharmacol.6, 268–270 (1973)
Drach, J. C., Howell, J. P.: Identification of diphenhydramine urinary metabolites in the rhesus monkey. Biochem. Pharmacol.17, 2155–2136 (1968)
Drach, J. C., Howell, J. P., Borondy, P. E., Glazko, A. J.: Species differences in the metabolism of diphenhydramine (Benadryl). Proc. Soc. exp. Biol. (N. Y.)135, 849–853 (1970)
Gundert-Remy, U., Bilzer, W., Weber, E.: Resorption von Diphenhydramin-HCl aus verschiedenen Darreichungsformen. Die Pharmazeutische Industrie36, 46–49 (1974)
Hollister, L. E., Clyde, D. J.: Blood levels of pentobarbital sodium, meprobamate, and tybamate in relation to clinical effect. Clin. Pharmacol. Ther.9, 204–208 (1968)
Sidell, F. R., Pless, J. E.: Ethyl alcohol: Blood levels and performance decrements after oral administration to man. Psychopharmacologia19, 246–261 (1971)
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Dedicated to Professor Dr. O. Eichler on the occasion of his 75th birthday.
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Bilzer, W., Gundert-Remy, U. & Weber, E. Relationship between antihistamic activity and plasma level of diphenhydramine. Eur J Clin Pharmacol 7, 393–395 (1974). https://doi.org/10.1007/BF00558213
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DOI: https://doi.org/10.1007/BF00558213