Betatin

Approved Indications:

• Management of Ménière’s disease characterized by vertigo, tinnitus, and hearing loss.
• Treatment of vestibular vertigo and balance disorders of various origins.

Clinically Accepted Off-Label Uses:

• Adjunct therapy for vertigo associated with labyrinthine disorders not classified as Ménière’s disease.
• Supportive treatment in tinnitus and auditory disturbances related to inner ear pathology.

Formulation and Route:

• Oral tablets.

Adults:

• Initial dose typically 8–16 mg three times daily (total 24–48 mg/day).
• Dose may be adjusted up to 48 mg three times daily based on response and tolerability.

Elderly:

• Start at lower doses and titrate cautiously; generally, same dosing range applies.

Pediatrics:

• Safety and efficacy not well established; generally not recommended.

Special Populations:

• No specific dose adjustment necessary in mild to moderate renal or hepatic impairment. Use caution in severe impairment.

Administration Notes:

• Take with meals to reduce gastrointestinal irritation.
• Consistency in dosing times improves therapeutic effect.

Betahistine is a histamine analogue that primarily acts as an H1 receptor agonist and a weak H3 receptor antagonist. By stimulating H1 receptors, it causes vasodilation of the inner ear microvasculature, improving blood flow and reducing endolymphatic pressure, thereby relieving vertigo symptoms. The antagonism of H3 receptors enhances histamine release and neurotransmitter modulation in the vestibular nuclei, stabilizing vestibular function and improving balance.

• Absorption: Well absorbed orally with peak plasma concentrations within 1–3 hours.
• Distribution: Widely distributed, including to the inner ear and central nervous system.
• Metabolism: Extensively metabolized in the liver mainly to 2-pyridylacetic acid and other metabolites.
• Elimination: Primarily excreted via the urine as metabolites.
• Half-life: Approximately 3–4 hours.
• Onset: Symptom improvement usually observed after several days to weeks of therapy.

• Pregnancy: Limited human data; use only if potential benefit justifies risk.
• Lactation: Unknown if excreted in breast milk; caution advised; avoid breastfeeding or use alternative therapy.

• Vestibular suppressant and antihistaminic agent.
• Histamine H1 receptor agonist with H3 antagonist properties.

• Known hypersensitivity to betahistine or excipients.
• Pheochromocytoma (due to potential stimulation of catecholamine release).
• Active peptic ulcer disease (use with caution or avoid).

• Use caution in patients with asthma due to potential histamine-related bronchospasm.
• Monitor for gastrointestinal side effects; avoid in active gastric ulcers.
• Patients with hypotension or hypertension should be monitored as vasodilation effects may alter blood pressure.
• No known black box warnings.

Common:

• Headache
• Nausea and gastrointestinal discomfort
• Dyspepsia
• Flushing

Less Common:

• Allergic skin reactions (rash, pruritus)
• Dizziness (paradoxical in some cases)

Rare / Serious:

• Severe hypersensitivity reactions (very rare)
• Exacerbation of asthma symptoms

• No major clinically significant interactions documented.
• Caution when combined with antihypertensive agents due to additive vasodilatory effects.
• Concomitant use with other histamine receptor modulators not recommended without medical supervision.

• Current guidelines recommend betahistine as first-line symptomatic treatment in Ménière’s disease and vestibular vertigo management.
• No major recent changes in dosing or safety profile.
• Ongoing research evaluates long-term efficacy and comparative effectiveness versus other vestibular suppressants.

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