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Indications and Dosage
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.
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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.
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Food Interaction
Delayed absorption with food.
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Action
Description:
Mechanism of 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. Pharmacokinetics: 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). |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Betahistine, CID=2366, https://pubchem.ncbi.nlm.nih.gov/compound/Betahistine (accessed on Jan. 21, 2020) |
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Storage
Store between 15-30°C. Protect from moisture and light.
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MIMS Class
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ATC Classification
N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.
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References
Anon. Betahistine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 31/01/2022. Betahistine dihydrochloride 16 mg Tablets (Generics [UK] Limited t/a Mylan). MHRA. https://products.mhra.gov.uk. Accessed 31/01/2022. Betaserc 24 mg Tablet (Abbott Laboratories [M] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 31/01/2022. Buckingham R (ed). Betahistine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/01/2022. Joint Formulary Committee. Betahistine Dihydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/01/2022. Merislon Tablets (Eisai [Malaysia] Sdn Bhd). MIMS Malaysia. http://www.mims.com/malaysia. Accessed 31/01/2022. Serc 8 mg, 16 mg Tablet (Zuellig Pharma Corporation). MIMS Philippines. http://www.mims.com/philippines. Accessed 31/01/2022. Viatris Ltd. Serc 8 mg, 16 mg Tablet data sheet 11 January 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 02/02/2022.
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