Dosage/Direction for Use
Oral Meniere's disease Adult: For the treatment of vertigo, tinnitus, hearing loss, and nausea associated with Meniere's disease: As betahistine dihydrochloride: Initially, 8-16 mg tid. Maintenance: 24-48 mg daily in divided doses. As betahistine mesilate: 6-12 mg tid. Adjust doses according to patient needs. |
Administration
May be taken with or without food.
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Contraindications
Phaeochromocytoma, active or history of peptic ulcer.
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Special Precautions
Patient with bronchial asthma, CV disease, urticaria, rashes, allergic rhinitis. Patient taking antihistamines. Hepatic impairment. Pregnancy and lactation.
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Adverse Reactions
Significant: Rarely, ventricular extrasystoles, hypotension, tachycardia.
Gastrointestinal disorders: Diarrhoea, dry mouth, dyspepsia, nausea. Rarely, mild gastric complaints (e.g. vomiting, gastrointestinal pain, abdominal distension, bloating).
Immune system disorders: Hypersensitivity reactions (e.g. anaphylaxis).
Nervous system disorders: Headache.
Skin and subcutaneous tissue disorders: Rarely, rash, pruritus, urticaria, angioneurotic oedema.
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Overdosage
Symptoms: Nausea, somnolence, abdominal pain; convulsions, pulmonary or cardiac complications. Management: Supportive and symptomatic treatment. Perform gastric lavage.
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Drug Interactions
Metabolism may be inhibited by MAOIs (e.g. selegiline). May diminish efficacy with antihistamines.
Potentially Fatal: |
Food Interaction
Delayed absorption with food.
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Action
Betahistine is a histamine analogue that is claimed to improve the microcirculation of the labyrinth resulting in decreased endolymphatic pressure. The exact mechanism is not yet fully determined; however, it is known to act as both a partial histamine H1-receptor agonist and histamine H3-receptor antagonist in neuronal tissue, with negligible histamine H2-receptor activity. It inhibits presynaptic histamine H3-receptors and induces H3-receptor downregulation, thus increasing the histamine turnover and release.
Absorption: Readily and almost completely absorbed from the gastrointestinal tract. Delayed absorption with food. Time to peak plasma concentration: 1 hour (inactive metabolite). Distribution: Plasma protein binding: <5%. Metabolism: Rapidly and almost completely metabolised into 2-pyridylacetic acid (inactive metabolite). Excretion: Via urine (approx 91%; mainly as inactive metabolite). Elimination half-life: Approx 3.5 hours (inactive metabolite). |
Storage
Oral: Store between 15-30°C. Protect from moisture and light.
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CIMS Class
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ATC Classification
N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.
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