Chemical Properties
White or almost white, crystalline powder, very hygroscopic.
Uses
Vasodilatator;H1 agonist
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).
Definition
Betahistine mesylate is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
Indications
Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
Safety Profile
Poison by subcutaneous route.Moderately toxic by ingestion and other routes. Whenheated to decomposition it emits toxic fumes of NOx andSOx.
in vitro
In Vitro: Betahistine mesylate (0-10 μM) inhibits [125I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. Lead to Ki values of 1.4 μM and 2.5 μM, respectively.
Betahistine mesylate (0-10 μM) has a regulating function on cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. At low concentrations, Betahistine mesylate behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC50 values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, Betahistine mesylate inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity.
Mode of action
Betahistine is indicated for the treatment of Meniere's disease and other audiovestibular disorders like vertigo and tinnitus. Betahistine is an analogue of histamine and an H1-receptor agonist. Stimulating the H1- receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels, resulting in reduced endolymphatic pressure. Betahistine acts by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, decreasing symptoms of vertigo, tinnitus, balance disorders, and hearing loss associated with Meniere's disease. Betahistine also acts as a histamine H3- receptor antagonist which causes an increased output of histamine, increase in the direct H1-agonist activity, and inhibition of the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms.
