Drug intelligence / Profile preview

betahistine

Development stage
Phase 4
Lead developer
Hubei Jiu'an Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

Betahistine is a histamine-like antivertigo drug primarily used to treat symptoms associated with Ménière's disease and other balance disorders. These symptoms include vertigo (spinning sensation), tinnitus (ringing in the ears), hearing loss, and nausea. Betahistine acts mainly as a weak partial agonist at histamine H1 receptors and as an antagonist or inverse agonist at histamine H3 receptors. Stimulation of H1 receptors in the inner ear leads to vasodilation and increased vascular permeability, reducing endolymphatic pressure and alleviating Ménière’s disease symptoms. Antagonism of H3 receptors increases the release of neurotransmitters such as histamine and serotonin in the brainstem vestibular nuclei, which helps restore balance function by modulating vestibular compensation[1][5][8]. Betahistine is rapidly absorbed when taken orally and is available by prescription in many countries but not approved for use in the United States[2][3].

Brand names
SercAuro-BetahistineM-BetahistineMINT-BetahistineNRA-BetahistinePMS-BetahistineTEVA-Betahistine
Other names
betahistine dihydrochloride
02

Targets

HRH3 (Histamine Receptor H3)HRH1 (Histamine H1 Receptor)

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