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Pharmacology: Pharmacodynamics: Mechanism of Action: Betahistine has a direct stimulating (agonistic) effect on H1 receptors located on blood vessels in the inner ear. Betahistine dilates the blood vessels within the middle ear which can relieve pressure from excess fluid and act on the smooth muscle. This would give rise to local vasodilation and increased permeability, which would help reverse the underlying problem of endolymphatic hydrops (the main pathological feature is an excess of endolymph fluid producing an increase in pressure in the membranous labyrinth).
Pharmacokinetics: Absorption is rapid and complete. It undergoes hepatic metabolism, and its elimination half-life is 3.4 hours via urine as inactive metabolites.
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