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Diphenhydramine kinetics following intravenous, oral, and sublingual dimenhydrinate administration
Author(s) -
Scavone Joseph M.,
Luna Becki G.,
Harmatz Jerold S.,
von Moltke Lisa,
Greenblatt David J.
Publication year - 1990
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510110302
Subject(s) - diphenhydramine , medicine , anesthesia , pharmacology , histamine
Eight healthy volunteers received 50 mg of dimenhydrinate, a theoclate salt of diphenhydramine, orally, sublingually, and intravenously on three separate occasions in random sequence. Plasma diphenhydramine concentrations during 12 h after each dose were measured by gas‐liquid chromatography with nitrogen‐phosphorous detection. Mean peak plasma concentrations after sublingual administration were slightly lower than after oral dosage (38·3 vs 47·8 ng ml −1 ), and the time of peak concentration was similar (2·6 vs 2·3 h after dose). These differences did not reach statistical significance. The mean total area under the plasma concentration‐time curve (AUC) for sublingual administration was slightly but not significantly smaller than after oral dosage (221 vs 270 h ng ml −1 ). Systemic availability of diphenhydramine after sublingual dimenhydrinate, measured by the ratio of oral AUC to intravenous AUC, was slightly less than after oral dimenhydrinate (0·58 vs 0·69, NS), and both were significantly less than 1·0. Thus sublingual and oral administration of dimenhydrinate result in comparable, but incomplete, systemic availability of diphenhydramine.