Betahistine Mesylate

• Approved Indications:
• Treatment of Ménière’s disease to reduce vertigo, tinnitus, and hearing loss symptoms.
• Management of vestibular vertigo and balance disorders related to inner ear dysfunction.
• Clinically Accepted Off-Label Uses:
• Symptomatic relief in vestibular disorders such as labyrinthitis and vestibular neuritis.
• Adjunct therapy for tinnitus associated with inner ear disease.

• Formulation and Route:
• Oral tablets.
• Adults:
• Typical dose: 8 mg to 16 mg taken three times daily (total 24–48 mg/day).
• Dosage may be adjusted up to 48 mg three times daily depending on clinical response and tolerability.
• Elderly:
• Start at lower doses; titrate carefully due to potential sensitivity.
• Pediatrics:
• Safety and efficacy not established; use generally not recommended.
• Special Populations:
• No established dose adjustment for renal or hepatic impairment; use cautiously in severe organ dysfunction.
• Administration Notes:
• Take with food to reduce gastrointestinal side effects.
• Maintain consistent dosing intervals for optimal effect.

Betahistine is a structural analogue of histamine that acts primarily as an H1 receptor agonist and a weak H3 receptor antagonist. Its action on H1 receptors induces vasodilation in the inner ear’s microvasculature, improving blood flow and reducing endolymphatic pressure responsible for vertigo. The H3 antagonism enhances histamine release and neurotransmitter modulation in central vestibular pathways, stabilizing vestibular function and alleviating symptoms of dizziness and imbalance.

• Absorption: Rapid and almost complete after oral administration; peak plasma levels reached within 1 to 3 hours.
• Distribution: Widely distributed including central nervous system and inner ear structures.
• Metabolism: Extensively metabolized in the liver to inactive metabolites such as 2-pyridylacetic acid.
• Elimination: Metabolites excreted primarily via the kidneys.
• Half-Life: Approximately 3 to 4 hours.
• Onset of Action: Clinical benefits typically appear after several days to weeks of continuous treatment.

• Pregnancy: Limited data on safety; use only if clearly needed and benefits outweigh risks.
• Lactation: Unknown if excreted in human milk; caution advised, and breastfeeding should be avoided or alternative therapy considered.

• Vestibular suppressant and histamine receptor modulator.

• Known hypersensitivity to betahistine or any component of the formulation.
• Pheochromocytoma due to risk of hypertensive crisis.
• Active peptic ulcer disease or severe gastrointestinal disorders.

• Use with caution in patients with bronchial asthma due to potential histamine-related bronchospasm.
• Monitor for gastrointestinal discomfort; discontinue if severe symptoms develop.
• Use cautiously in patients with hypotension or hypertension.
• No black box warnings reported.

• Common:
• Headache
• Nausea, dyspepsia, and gastrointestinal discomfort
• Flushing
• Less Common:
• Allergic skin reactions (rash, pruritus)
• Dizziness (rare paradoxical effect)
• Rare / Serious:
• Severe hypersensitivity reactions (anaphylaxis very rare)
• Asthma exacerbation

• No significant drug interactions widely reported.
• Possible additive hypotensive effects when combined with antihypertensive agents.
• Avoid concurrent use with other histamine receptor modulators without medical supervision.

• Maintained as a first-line treatment for Ménière’s disease in clinical guidelines.
• No recent major changes in dosing or safety profile.
• Ongoing studies continue to evaluate long-term efficacy and comparative effectiveness.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and direct light.
• Keep container tightly closed and out of reach of children.