Betahistine


Generic Medicine Info
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.
Administration
May be taken with or without food.
Contraindications
Phaeochromocytoma, active or history of peptic ulcer.
Special Precautions
Patient with bronchial asthma, CV disease, urticaria, rashes, allergic rhinitis. Patient taking antihistamines. Hepatic impairment. Pregnancy and lactation.
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.
Overdosage
Symptoms: Nausea, somnolence, abdominal pain; convulsions, pulmonary or cardiac complications. Management: Supportive and symptomatic treatment. Perform gastric lavage.
Drug Interactions
Metabolism may be inhibited by MAOIs (e.g. selegiline). May diminish efficacy with antihistamines.
Food Interaction
Delayed absorption with food.
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).
Chemical Structure

Chemical Structure Image
Betahistine

Source: National Center for Biotechnology Information. PubChem Database. Betahistine, CID=2366, https://pubchem.ncbi.nlm.nih.gov/compound/Betahistine (accessed on Jan. 21, 2020)

Storage
Store between 15-30°C. Protect from moisture and light.
MIMS Class
Antivertigo Drugs
ATC Classification
N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.
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.

Disclaimer: This information is independently developed by MIMS based on Betahistine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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