Peringatan Keamanan

Symptoms of an overdose with betahistine (< 640 mg) include dry mouth, nausea, dyspepsia, abdominal pain, and somnolence. Serious complications such as convulsions, pulmonary or cardiac effects may occur with higher doses (> 640 mg), especially during intentional overdoses and combination with other drugs. In the case of an overdose with betahistine, provide supportive therapy, and contact the local poison control center for further management.L16388

Betahistine

DB06698

small molecule approved investigational

Deskripsi

Ménière's disease is a progressive disease of the inner ear characterized by vertigo, tinnitus, and hearing loss. It has a significant impact on both the physical and social functioning of affected individuals.A220318,L16408

Betahistine is a histamine-like antivertigo drug used for treating symptoms associated with Ménière's disease. It is thought to reduce symptoms through its actions on histamine receptors.A220333,L16403 Betahistine was first approved by the FDA in the 1970s but withdrawn within approximately 5 years due to a lack of evidence supporting its efficacy. It is currently marketed in Canada by various companies, including Teva Pharmaceuticals.

Struktur Molekul 2D

Berat 136.1943
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of betahistine is 3-4 hours.[A220438,A220563,L16388]
Volume Distribusi In a pharmacokinetic study of rats, betahistine was found to be distributed throughout the body.[L16443] Human data for betahistine's volume of distribution is not readily available.[A220438,A220563,L16388,L16443]
Klirens (Clearance) -

Absorpsi

When given orally, betahistine is rapidly and almost completely absorbed from the gastrointestinal tract.A220438,L16388 In the fasted state, Cmax is achieved within 1 hour of administration; in the fed state, Cmax is delayed, but the total drug absorption is similar. Food, therefore, has little effect on the absorption of betahistine.A220563,16388

Metabolisme

Betahistine is metabolized primarily into the inactive metabolite 2-pyridylacetic acid. There is both clinical and in vitro evidence that monoamine oxidase enzymes are responsible for the metabolism of betahistine.A220443,A36211,A36212,L16388

Rute Eliminasi

Betahistine is mainly excreted in the urine; with approximately 85-91% being detected in urine samples within 24 hours of administration.A220438,A220563,L16388

Interaksi Makanan

1 Data
  • 1. Take with food. This may reduce or prevent gastrointestinal upset.

Interaksi Obat

203 Data
Benzylpenicilloyl polylysine Betahistine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Benzatropine The therapeutic efficacy of Betahistine can be decreased when used in combination with Benzatropine.
Ziprasidone The therapeutic efficacy of Betahistine can be decreased when used in combination with Ziprasidone.
Clemastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Clemastine.
Amitriptyline The therapeutic efficacy of Betahistine can be decreased when used in combination with Amitriptyline.
Olanzapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Olanzapine.
Cetirizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cetirizine.
Terfenadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Terfenadine.
Buclizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Buclizine.
Clozapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Clozapine.
Doxylamine The therapeutic efficacy of Betahistine can be decreased when used in combination with Doxylamine.
Mirtazapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Mirtazapine.
Dexbrompheniramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Dexbrompheniramine.
Promazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Promazine.
Triprolidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Triprolidine.
Cyproheptadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cyproheptadine.
Loratadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Loratadine.
Imipramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Imipramine.
Chlorpromazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Chlorpromazine.
Cimetidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cimetidine.
Nortriptyline The therapeutic efficacy of Betahistine can be decreased when used in combination with Nortriptyline.
Amoxapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Amoxapine.
Hydroxyzine The therapeutic efficacy of Betahistine can be decreased when used in combination with Hydroxyzine.
Cinnarizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cinnarizine.
Nizatidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Nizatidine.
Astemizole The therapeutic efficacy of Betahistine can be decreased when used in combination with Astemizole.
Trazodone The therapeutic efficacy of Betahistine can be decreased when used in combination with Trazodone.
Azatadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Azatadine.
Trimipramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Trimipramine.
Risperidone The therapeutic efficacy of Betahistine can be decreased when used in combination with Risperidone.
Meclizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Meclizine.
Carbinoxamine The therapeutic efficacy of Betahistine can be decreased when used in combination with Carbinoxamine.
Benzquinamide The therapeutic efficacy of Betahistine can be decreased when used in combination with Benzquinamide.
Propiomazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Propiomazine.
Tripelennamine The therapeutic efficacy of Betahistine can be decreased when used in combination with Tripelennamine.
Brompheniramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Brompheniramine.
Ranitidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Ranitidine.
Methdilazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Methdilazine.
Ketotifen The therapeutic efficacy of Betahistine can be decreased when used in combination with Ketotifen.
Famotidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Famotidine.
Maprotiline The therapeutic efficacy of Betahistine can be decreased when used in combination with Maprotiline.
Methantheline The therapeutic efficacy of Betahistine can be decreased when used in combination with Methantheline.
Fexofenadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Fexofenadine.
Desloratadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Desloratadine.
Azelastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Azelastine.
Dimenhydrinate The therapeutic efficacy of Betahistine can be decreased when used in combination with Dimenhydrinate.
Promethazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Promethazine.
Mequitazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Mequitazine.
Diphenhydramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Diphenhydramine.
Levocabastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Levocabastine.
Chlorpheniramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Chlorpheniramine.
Doxepin The therapeutic efficacy of Betahistine can be decreased when used in combination with Doxepin.
Diphenylpyraline The therapeutic efficacy of Betahistine can be decreased when used in combination with Diphenylpyraline.
Desipramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Desipramine.
Orphenadrine The therapeutic efficacy of Betahistine can be decreased when used in combination with Orphenadrine.
Cyclizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Cyclizine.
Quetiapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Betahistine can be decreased when used in combination with Aripiprazole.
Chlorprothixene The therapeutic efficacy of Betahistine can be decreased when used in combination with Chlorprothixene.
Alimemazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Alimemazine.
Methotrimeprazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Methotrimeprazine.
Aceprometazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Aceprometazine.
Phenindamine The therapeutic efficacy of Betahistine can be decreased when used in combination with Phenindamine.
Pheniramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Pheniramine.
Zuclopenthixol The therapeutic efficacy of Betahistine can be decreased when used in combination with Zuclopenthixol.
Methapyrilene The therapeutic efficacy of Betahistine can be decreased when used in combination with Methapyrilene.
Clofedanol The therapeutic efficacy of Betahistine can be decreased when used in combination with Clofedanol.
Flunarizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Flunarizine.
Iloperidone The therapeutic efficacy of Betahistine can be decreased when used in combination with Iloperidone.
Mianserin The therapeutic efficacy of Betahistine can be decreased when used in combination with Mianserin.
Pizotifen The therapeutic efficacy of Betahistine can be decreased when used in combination with Pizotifen.
Asenapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Asenapine.
Levocetirizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Levocetirizine.
Esmirtazapine The therapeutic efficacy of Betahistine can be decreased when used in combination with Esmirtazapine.
Mepyramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Mepyramine.
Antazoline The therapeutic efficacy of Betahistine can be decreased when used in combination with Antazoline.
Chloropyramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Chloropyramine.
Dimetindene The therapeutic efficacy of Betahistine can be decreased when used in combination with Dimetindene.
Isothipendyl The therapeutic efficacy of Betahistine can be decreased when used in combination with Isothipendyl.
Metiamide The therapeutic efficacy of Betahistine can be decreased when used in combination with Metiamide.
Roxatidine acetate The therapeutic efficacy of Betahistine can be decreased when used in combination with Roxatidine acetate.
Chlorcyclizine The therapeutic efficacy of Betahistine can be decreased when used in combination with Chlorcyclizine.
Dimetotiazine The therapeutic efficacy of Betahistine can be decreased when used in combination with Dimetotiazine.
Butriptyline The therapeutic efficacy of Betahistine can be decreased when used in combination with Butriptyline.
Dosulepin The therapeutic efficacy of Betahistine can be decreased when used in combination with Dosulepin.
Acrivastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Acrivastine.
Dexchlorpheniramine maleate The therapeutic efficacy of Betahistine can be decreased when used in combination with Dexchlorpheniramine maleate.
Thonzylamine The therapeutic efficacy of Betahistine can be decreased when used in combination with Thonzylamine.
Bilastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Bilastine.
Rupatadine The therapeutic efficacy of Betahistine can be decreased when used in combination with Rupatadine.
Pitolisant The therapeutic efficacy of Betahistine can be decreased when used in combination with Pitolisant.
Ebastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Ebastine.
Mizolastine The therapeutic efficacy of Betahistine can be decreased when used in combination with Mizolastine.
Lafutidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Lafutidine.
GSK-1004723 The therapeutic efficacy of Betahistine can be decreased when used in combination with GSK-1004723.
Oxatomide The therapeutic efficacy of Betahistine can be decreased when used in combination with Oxatomide.
Lavoltidine The therapeutic efficacy of Betahistine can be decreased when used in combination with Lavoltidine.
Deptropine The therapeutic efficacy of Betahistine can be decreased when used in combination with Deptropine.
Dexchlorpheniramine The therapeutic efficacy of Betahistine can be decreased when used in combination with Dexchlorpheniramine.
Tritoqualine The therapeutic efficacy of Betahistine can be decreased when used in combination with Tritoqualine.

Target Protein

Histamine H1 receptor HRH1
Histamine H3 receptor HRH3

Referensi & Sumber

Synthesis reference: Jean S. Cherqui, Alain C. Djiane, "New galenical form of administration of betahistine and its derivatives and the preparation thereof." U.S. Patent US4264574, issued February, 1979.
Artikel (PubMed)
  • PMID: 27327415
    Murdin L, Hussain K, Schilder AG: Betahistine for symptoms of vertigo. Cochrane Database Syst Rev. 2016 Jun 21;(6):CD010696. doi: 10.1002/14651858.CD010696.pub2.
  • PMID: 24669323
    Orji F: The Influence of Psychological Factors in Meniere's Disease. Ann Med Health Sci Res. 2014 Jan;4(1):3-7. doi: 10.4103/2141-9248.126601.
  • PMID: 18236637
    Della Pepa C, Guidetti G, Eandi M: Betahistine in the treatment of vertiginous syndromes: a meta-analysis. Acta Otorhinolaryngol Ital. 2006 Aug;26(4):208-15.
  • PMID: 28358888
    Parfenov VA, Golyk VA, Matsnev EI, Morozova SV, Melnikov OA, Antonenko LM, Sigaleva EE, Situkho MI, Asaulenko OI, Popovych VI, Zamergrad MV: Effectiveness of betahistine (48 mg/day) in patients with vestibular vertigo during routine practice: The VIRTUOSO study. PLoS One. 2017 Mar 30;12(3):e0174114. doi: 10.1371/journal.pone.0174114. eCollection 2017.
  • PMID: 19300572
    Lacour M, van de Heyning PH, Novotny M, Tighilet B: Betahistine in the treatment of Meniere's disease. Neuropsychiatr Dis Treat. 2007 Aug;3(4):429-40.
  • PMID: -
    Duaa J. Al-Tamimi, Afaq M. Ammoo , Mays E. Alani, Jaafar J. Ibraheem, Duaa J. Al-Tamimi , Afaq M. Ammoo , Mays E. Alani and Jaafar J. Ibraheem: Pharmacokinetics and dose proportionality of betahistine in healthy individuals Scientia Pharmaceutica.
  • PMID: 29532287
    Strupp M, Kraus L, Schautzer F, Rujescu D: Meniere's disease: combined pharmacotherapy with betahistine and the MAO-B inhibitor selegiline-an observational study. J Neurol. 2018 Mar 12. pii: 10.1007/s00415-018-8809-8. doi: 10.1007/s00415-018-8809-8.
  • PMID: 4150992
    Sternson LA, Tobia AJ, Walsh GM, Sternson AW: The metabolism of betahistine in the rat. Drug Metab Dispos. 1974 Mar-Apr;2(2):123-8.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 33 • International brands: 0
Produk
  • Act Betahistine
    Tablet • 16 mg • Oral • Canada • Approved
  • Act Betahistine
    Tablet • 24 mg • Oral • Canada • Approved
  • Apo-betahistine
    Tablet • 8 mg • Oral • Canada • Generic • Approved
  • Apo-betahistine
    Tablet • 16 mg • Oral • Canada • Generic • Approved
  • Apo-betahistine
    Tablet • 24 mg • Oral • Canada • Generic • Approved
  • Auro-betahistine
    Tablet • 8 mg • Oral • Canada • Generic • Approved
  • Auro-betahistine
    Tablet • 16 mg • Oral • Canada • Generic • Approved
  • Auro-betahistine
    Tablet • 24 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 33 produk.

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