Betahistine dihydrochloride is widely used to reduce the severity and frequency of vertigo\nattacks associated with Ménièreâ??s disease. Betahistine is an analogue of histamine, and is a weak\nhistamine H1 receptor agonist and potent histamine H3 receptor antagonist. The recommended\ntherapeutic dose for adults ranges from 24 to 48 mg given in doses divided throughout the day.\nBetahistine undergoes extensive first-pass metabolism to the major inactive metabolite 2-pyridyl\nacetic acid (2PAA), which can be considered a surrogate index for quantitation of the parent drug\ndue to extremely low plasma levels of betahistine. The aim of the present investigation was to\nassess the pharmacokinetics and dose proportionality of betahistine in Arabic healthy adult male\nsubjects under fasting conditions. A single dose of betahistine in the form of a 8, 16, or 24 mg tablet\nwas administered to 36 subjects in randomized, cross-over, three-period, three-sequence design\nseparated by a one week washout period between dosing...................
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