Betahistine


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
May be taken with or without food.
Chống chỉ định
Phaeochromocytoma, active or history of peptic ulcer.
Thận trọng
Patient with bronchial asthma, CV disease, urticaria, rashes, allergic rhinitis. Patient taking antihistamines. Hepatic impairment. Pregnancy and lactation.
Tác dụng không mong muốn
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.
Quá liều
Symptoms: Nausea, somnolence, abdominal pain; convulsions, pulmonary or cardiac complications. Management: Supportive and symptomatic treatment. Perform gastric lavage.
Tương tác
Metabolism may be inhibited by MAOIs (e.g. selegiline). May diminish efficacy with antihistamines.
Tương tác với thức ăn
Delayed absorption with food.
Tác dụng
Description: 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).
Đặc tính

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)

Bảo quản
Store between 15-30°C. Protect from moisture and light.
Phân loại MIMS
Thuốc trị chóng mặt
Phân loại ATC
N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.
Tài liệu tham khảo
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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  • Agihistine
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  • Kernhistine
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  • Serc
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  • Verist
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