Betahistine
(Synonyms: 倍他司汀；培他啶) 目录号 : GC60072
A histamine H3 receptor antagonist and histamine H1 receptor agonist
Cas No.:5638-76-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Betahistine is a histamine H3 receptor antagonist and histamine H1 receptor agonist.1 In vivo, betahistine dilates pre-capillary arterioles and increases blood flow to the stria vascularis in guinea pigs.2,3 Betahistine (8 mg/kg) reduces weight gain and increased feeding behavior induced by olanzapine in female rats.4 Formulations containing betahistine have been used in the treatment of balance disorders and vertigo symptoms associated with Meniere's disease.
1.Timmerman, H.Histamine agonists and antagonistsActa Otolaryngol. Suppl.4795-11(1991) 2.Bertlich, M., Ihler, F., Sharaf, K., et al.Betahistine metabolites, aminoethylpyridine, and hydroxyethylpyridine increase cochlear blood flow in guinea pigs in vivoInt. J. Audiol.53(10)753-759(2014) 3.Bertlich, M., Ihler, F., Weiss, B.G., et al.Role of capillary pericytes and precapillary arterioles in the vascular mechanism of betahistine in a guinea pig inner ear modelLife Sci.18717-21(2017) 4.Lian, J., Huang, X.-F., Pai, N., et al.Ameliorating antipsychotic-induced weight gain by betahistine: Mechanisms and clinical implicationsPharmacol. Res.10651-63(2016)
| Cas No. | 5638-76-6 | SDF | |
| 别名 | 倍他司汀；培他啶 | ||
| Canonical SMILES | CNCCC1=NC=CC=C1 | ||
| 分子式 | C8H12N2 | 分子量 | 136.19 |
| 溶解度 | DMSO : 100mg/mL | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 7.3427 mL | 36.7134 mL | 73.4268 mL |
| 5 mM | 1.4685 mL | 7.3427 mL | 14.6854 mL |
| 10 mM | 0.7343 mL | 3.6713 mL | 7.3427 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Betahistine for symptoms of vertigo
Cochrane Database Syst Rev 2016 Jun 21;2016(6):CD010696.PMID:27327415DOI:10.1002/14651858.CD010696.pub2.
Background: Vertigo is a symptom in which individuals experience a false sensation of movement. This type of dizziness is thought to originate in the inner ear labyrinth or its neural connections. It is a commonly experienced symptom and can cause significant problems with carrying out normal activities. Betahistine is a drug that may work by improving blood flow to the inner ear. This review examines whether Betahistine is more effective than a placebo at treating symptoms of vertigo from different causes. Objectives: To assess the effects of Betahistine in patients with symptoms of vertigo from different causes. Search methods: The Cochrane ENT Information Specialist searched the Cochrane ENT Trials Register; Central Register of Controlled Trials (CENTRAL 2015, Issue 8); PubMed; EMBASE; CINAHL; Web of Science; ClinicalTrials.gov; ICTRP and additional sources for published and unpublished trials. We also contacted manufacturers and researchers in the field. The date of the search was 21 September 2015. Selection criteria: We included randomised controlled trials of Betahistine versus placebo in patients of any age with vertigo from any neurotological diagnosis in any settings. Data collection and analysis: We used the standard methodological procedures expected by Cochrane. Our primary outcome was the proportion of patients with reduction in vertigo symptoms (considering together the intensity, frequency and duration those symptoms). Main results: We included 17 studies, with a total of 1025 participants; 12 studies were published (567 patients) and five were unpublished (458 patients). Sixteen studies including 953 people compared Betahistine with placebo. All studies with analysable data lasted three months or less. The majority were at high risk of bias, but in some the risk of bias was unclear. One study, at high risk of bias, included 72 people with benign paroxysmal positional vertigo (BPPV) and compared Betahistine with placebo; all patients also had particle repositioning manoeuvres. The studies varied considerably in terms of types of participants, their diagnoses, the dose of Betahistine and the length of time it was taken for, the study methods and the way any improvement in vertigo symptoms was measured. Using the GRADE system, we judged the quality of evidence overall to be low for two outcomes (proportion of patients with improvement and proportion with adverse events).Pooled data showed that the proportion of patients reporting an overall reduction in their vertigo symptoms was higher in the group treated with Betahistine than the placebo group: risk ratio (RR) 1.30, 95% confidence interval (CI) 1.05 to 1.60; 606 participants; 11 studies). This result should be interpreted with caution as the test for statistical heterogeneity as measured by the I(2) value was high.Adverse effects (mostly gastrointestinal symptoms and headache) were common but medically serious events in the study were rare and isolated: there was no difference in the frequency of adverse effects between the Betahistine and placebo groups, where the rates were 16% and 15% respectively (weighted values, RR 1.03, 95% CI 0.76 to 1.40; 819 participants; 12 studies).Sixteen per cent of patients from both the Betahistine and the placebo groups withdrew (dropped out) from the studies (RR 0.96, 95% CI 0.65 to 1.42; 481 participants; eight studies).Three studies looked at objective vestibular function tests as an outcome; the numbers of participants were small, techniques of measurement very diverse and reporting details sparse, so analysis of this outcome was inconclusive.We looked for information on generic quality of life and falls, but none of the studies reported on these outcomes. Authors' conclusions: Low quality evidence suggests that in patients suffering from vertigo from different causes there may be a positive effect of Betahistine in terms of reduction in vertigo symptoms. Betahistine is generally well tolerated with a low risk of adverse events. Future research into the management of vertigo symptoms needs to use more rigorous methodology and include outcomes that matter to patients and their families.
Betahistine in Ménière's Disease or Syndrome: A Systematic Review
Audiol Neurootol 2022;27(1):1-33.PMID:34233329DOI:10.1159/000515821.
Background: Ménière's disease is characterized by recurrent episodes of vertigo, hearing loss, and tinnitus, often with a feeling of fullness in the ear. Although Betahistine is thought to be specifically effective for Ménière's disease, no evidence for a benefit from the use of Betahistine exists, despite its widespread use. Reassessment of the effect of Betahistine for Ménière's disease is now warranted. Search methods: We searched for randomized controlled trials (RCTs) in the Central Register of Controlled Trials (CENTRAL), Ovid Medline, Ovid Embase, CINAHL, Web of Science, Clinicaltrials.gov, ICTRP, and additional sources for published and unpublished trials, in which Betahistine was compared to placebo. Data collection and analysis: Our outcomes involved vertigo, significant adverse effect (upper gastrointestinal discomfort), hearing loss, tinnitus, aural fullness, other adverse effects, and disease-specific health-related quality of life. We used GRADE to assess the quality of the evidence. Main results: We included 10 studies: 5 studies used a crossover design and the remaining 5 were parallel-group RCTs. One study with a low risk of bias found no significant difference between the Betahistine groups and placebo with respect to vertigo after a long-term follow-up period. No significant difference in the incidence of upper gastrointestinal discomfort was found in 2 studies (low-certainty evidence). No differences in hearing loss, tinnitus, or well-being and disease-specific health-related quality of life were found (low- to very low-certainty of evidence). Data on aural fullness could not be extracted. No significant difference between the Betahistine and the placebo groups (low-certainty evidence) could be demonstrated in the other adverse effect outcome with respect to dull headache. The pooled risk ratio for other adverse effect in the long term demonstrated a lower risk in favor of placebo over Betahistine. Conclusions: High-quality studies evaluating the effect of Betahistine on patients with Ménière's disease are lacking. However, one study with low risk of bias found no evidence of a difference in the effect of Betahistine on the primary outcome, vertigo, in patients with Ménière's disease when compared to placebo. The main focus of future research should be on the use of comparable outcome measures by means of patient-reported outcome measures.
[Betahistine in vestibular disorders: current concepts and perspectives]
Vestn Otorinolaringol 2021;86(2):73-81.PMID:33929156DOI:10.17116/otorino20218602173.
The goal of this paper is to review the pharmacological profile of Betahistine and evidence for using it in the treatment of common vestibular disorders. Betahistine is a weak agonist for histamine H1 receptors and strong antagonist for histamine H3 receptors. It demonstrates the maximum benefit in different types of peripheral vertigo, especially in Meniere's disease. The best results in decreasing intensity of vertigo, frequency of attacks and stimulation of vestibular compensation were obtained in daily dose 48 mg during 3 months. In benign paroxysmal positional vertigo Betahistine is used to treat residual dizziness after successful treatment of otolithiasis and to reduce the severity of vertigo during repositioning maneuvers. In vestibular neuritis Betahistine stimulates central compensation during vestibular rehabilitation. A new once-daily drug formulation of modified-release Betahistine is non-inferior to traditional and has a comparable safety profile, and could improve patient adherence. The implication of Betahistine in the treatment of central vestibular disorders is under-researched. The efficacy of Betahistine in increasing of vestibular compensation in post-stroke central vestibular disorders, persistent postural-perceptual dizziness and its role in vestibular migraine need further investigation.
Use of Betahistine in the treatment of peripheral vertigo
Acta Otolaryngol 2015;135(12):1205-11.PMID:26245698DOI:10.3109/00016489.2015.1072873.
Conclusion: Clinical studies and meta-analyses demonstrated that Betahistine is effective and safe in the treatment of Ménière's disease, BPPV (benign paroxysmal positional vertigo), vestibular neuronitis, and other types of peripheral vertigo. Objectives: The goal of this paper is to review the pharmacological profile of Betahistine and the evidence for its effectiveness and safety in the treatment of peripheral vertigo. Methods: Selection criteria for the publications on Betahistine included randomized clinical trials that evaluated the effectiveness and safety of Betahistine vs placebo or active control in the treatment of peripheral vertigo. Recent meta-analyses were also included. Databases searched included PubMed, the Cochrane Ear, Nose and Throat Disorders Group Trials Register, and ICTRP. The review also presents an update on the mechanisms of action, pharmacodynamics, and pharmacokinetics of Betahistine. Results: Efficacy and safety of Betahistine has been demonstrated in numerous clinical trials. The precise mechanism of action of Betahistine is still not completely understood, but the clinical experience demonstrated the benefit of Betahistine in different types of peripheral vertigo. In more than 40 years of clinical use, Betahistine has shown an excellent safety profile with the usual dose range from 8-48 mg daily. According to clinical studies, Betahistine 48 mg daily during 3 months is an effective and safe option for the treatment of peripheral vertigo.
Efficacy and safety of Betahistine treatment in patients with Meniere's disease: primary results of a long term, multicentre, double blind, randomised, placebo controlled, dose defining trial (BEMED trial)
BMJ 2016 Jan 21;352:h6816.PMID:26797774DOI:10.1136/bmj.h6816.
Study question: What is the long term efficacy of Betahistine dihydrochloride on the incidence of vertigo attacks in patients with Meniere's disease, compared with placebo? Methods: The BEMED trial is a multicentre, double blind, randomised, placebo controlled, three arm, parallel group, phase III, dose defining superiority trial conducted in 14 German tertiary referral centres (for neurology or ear, nose, and throat). Adults aged 21-80 years (mean age 56 years) with definite unilateral or bilateral Meniere's disease were recruited from March 2008 to November 2012. Participants received placebo (n=74), low dose Betahistine (2 × 24 mg daily, (n=73)), or high dose Betahistine (3 × 48 mg daily, (n=74)) over nine months. The primary outcome was the number of attacks per 30 days, based on patients' diaries during a three month assessment period at months seven to nine. An internet based randomisation schedule performed a concealed 1:1:1 allocation, stratified by study site. Secondary outcomes included the duration and severity of attacks, change in quality of life scores, and several observer-reported parameters to assess changes in audiological and vestibular function. Study answer and limitations: Incidence of attacks related to Meniere's disease did not differ between the three treatment groups (P=0.759). Compared with placebo, attack rate ratios were 1.036 (95% confidence interval 0.942 to 1.140) and 1.012 (0.919 to 1.114) for low dose and high dose Betahistine, respectively. The overall monthly attack rate fell significantly by the factor 0.758 (0.705 to 0.816; P<0.001). The population based, mean monthly incidence averaged over the assessment period was 2.722 (1.304 to 6.309), 3.204 (1.345 to 7.929), and 3.258 (1.685 to 7.266) for the placebo, low dose Betahistine, and high dose Betahistine groups, respectively. Results were consistent for all secondary outcomes. Treatment was well tolerated with no unexpected safety findings. Without a control group of patients who did not receive any intervention to follow the natural course of the disease, the placebo effect could not be accurately assessed and differentiated from spontaneous remission and fluctuation of symptoms. What this study adds: Current evidence is limited as to whether Betahistine prevents vertigo attacks caused by Meniere's disease, compared with placebo. The trial provides information on symptom relief on placebo intervention which is relevant for the design of future studies on potential disease modifying treatments in patients with Meniere's disease. Funding, competing interests, data sharing: Support from the German Federal Ministry of Education and Research (BMBF support code 01KG0708). Potential competing interests have been reported in full at the end of the paper on thebmj.com. Data are available from the corresponding author (Michael.Strupp@med.uni-muenchen.de) or biostatistician (mansmann@ibe.med.uni-muenchen.de). Study registration EudraCT no 2005-000752-32; ISRCTN no ISRCTN44359668.