Tinnitus, dizziness, "special drug" betahistine how to use? The 4 tables are all summarized

*For medical professionals only

The article introduces the "anti-vertigo drug" betahistine

When you think of betalistine, as a clinician, you may immediately think of Meniere's disease. Yes, betalistine is an effective drug that is mainly used clinically to treat Meniere's disease.

In addition, betaxamide can also be used for the treatment of cerebral arteriosclerosis, acute ischemic vascular disease, orthostatic vertigo caused by hypertension, tinnitus and other symptoms.

So, do you really know anything about this drug? What are its clinical indications? By what mechanism does it work? Today, let the world small medicine take you to unveil the "true face of Lushan" of betastein.

First, clinical application

Betatastine was first officially approved in 1968 for the treatment of vertigo and dizziness symptoms associated with clinical Meniere's disease, Meniere syndrome, vertigo and other diseases. After half a century of clinical application, the efficacy and safety of betalistine have been widely recognized clinically.

1

Treatment of Meniere's disease

■ Indications: Meniere's disease is one of the most widely used diseases in the clinic, betahistine is mainly used for the treatment of vertigo, tinnitus, hearing loss related to Meniere's disease.

■Dosage

Note: This table is compiled from the betatastine drug instructions, there may be different manufacturers of instructions to use and dosage of different situations, for reference only

2

Treatment of acute ischemic vascular disease

■ Indications: Treatment of acute ischemic cerebrovascular diseases, such as cerebral thrombosis, cerebral embolism, transient cerebral insufficiency, etc.; orthostatic vertigo and tinnitus caused by ischemic cerebrovascular diseases.

3

Vertigo, tinnitus, and hearing loss due to cerebral arteriosclerosis

■Indications: Treatment of vertigo, tinnitus and hearing loss caused by cerebral arteriosclerosis.

4

Vertigo

5

Other clinical applications

While treating vertigo-based inner ear diseases and cerebral ischemia diseases, betatastine also has a therapeutic effect on the tinnitus symptoms of patients with subjective tinnitus, cervical tinnitus, refractory tinnitus, and persistent subjective tinnitus.

In addition, the combination of betaxalastine and olanzapine can be effective in reducing the incidence of weight gain and drowsiness [7].

Note that because betahistine can cause adverse reactions in the gastrointestinal tract such as nausea and vomiting, it is recommended to take it after meals.

2. Status of the Guide

At present, betaxestine is a vertigo treatment drug recommended by many authoritative guidelines at home and abroad, such as the Guidelines for Benign Paroxysmal Positional Vertigo (Updated Edition) of the American Society of Otolaryngology head and neck Surgery[8], the Guidelines for the Diagnosis and Treatment of Meniere's Disease of the Otolaryngology Head and Neck Surgery Branch of the Chinese Medical Association[9], and the Multidisciplinary Expert Consensus on the Diagnosis of Vertigo[10] of the Neurology Branch of the Chinese Medical Association.

In addition, the domestic Guidelines for the Diagnosis and Treatment of Sudden Deafness also recommend glucocorticoids combined with blood rheology (including betahistine mesylate) for the treatment of sudden deafness episodes (within three weeks) [11].

Third, the mechanism of action

The mechanism of action of betahistine is actually not complicated, it is a histamine analogue, its chemical structure and pharmacological properties are similar to histamine, is a weak agonist of histamine H1 receptor, a strong antagonist of H3 receptor, but has almost no effect on H2 receptor.

The effect of betahistine on H1 and H3 receptors has a synergistic effect to some extent: betastatin's antagonism of H3 receptors can promote an increase in the level of histamine released by histamine nerve endings; and an increase in histamine levels can enhance the effect of H1 receptors, which in turn enhances the stimulating effect of betahistine on H1 receptors.

Studies have shown that betahistine promotes vestibular compensation and anti-dizziness/vertigo in a variety of ways [7]:

Fig. 1 Betastatin promotes vestibular compensation and rehabilitation, and improves the mechanism of vertigo and dizziness symptoms

Fourth, pharmacokinetics

Adults are rapidly absorbed after oral administration, and the blood concentration reaches a peak within 3 hours. Most drugs are metabolized by the kidneys to 2-pyridineacetic acid, which is completely excreted through the urine within 24 hours [12].

Fifth, the safety of medication

According to the data [7], betahistine has been approved for marketing in more than 80 countries around the world, the marketing time > 35 years, and its post-marketing monitoring data shows that there are only 554 adverse drug reaction reports worldwide, about 1/100000.

Common adverse reactions occur in the nervous system, skin and subcutaneous tissues, and gastrointestinal tract.

6. Precautions

1. Betatastine binds to histamine H1 receptor, which can cause bronchial contraction, so patients with bronchitis should be used with caution.

2. Betaxalastine can bind to the H2 receptor of gastric parietal cells, which may increase gastric acid secretion, so patients with a history of peptic ulcer or active peptic ulcer should be used with caution.

3. Betahistine is a strong antagonist of histamine H3 receptors, when betahistine is combined with antihistamine drugs, antihistamine drugs can reduce the efficacy of betahistine, and should not be combined.

4. Medication for special groups: the safety and efficacy of betahistine in children has not been established and is not recommended; elderly patients should pay attention to reducing the amount of use due to physiological decline; whether betahistine is excreted by breast milk is not clear, and it is recommended that pregnant and lactating women use it with caution.

Q

Betastine hydrochloride and betaxalastine mesylate are different

The main components of betasteine hydrochloride and betahistine mesylate are both betahistine, both of which can be used to treat vertigo, but with the following differences:

The hydrochloride is different: one is hydrochloric acid, the other is methanesulfonic acid. Compared with hydrochloric acid, mesylate and betahistine are more stable after combining into salt, are not easily destroyed by gastric juice or intestinal fluid, and easily pass through the blood-brain barrier, enter the central nervous system, and exert histamine receptor stimulation.

Indications: Betaxalastine mesylate is mainly used for meniere disease, meniere syndrome and dizziness caused by dizziness, vertigo, and betahistine hydrochloride is not only suitable for Meniere syndrome, but also can be used for vascular headache, cerebral arteriosclerosis, cerebral thrombosis, transient cerebral ischemia, dizziness caused by hypertension, tinnitus and other cerebrovascular diseases.

Resources:

[1] Drug information: Betahistine mesylate tablets, Sinopharm ZH20040130;2007/11/14.

[2] Drug information: betahistine hydrochloride oral liquid, National Medicines ZH20066114.

[3] Drug information: Betahistine hydrochloride oral liquid, Sinopharm ZH20056604.

Zhuang Jianhua. Clinical research progress of central histamine receptor and betahistine[J].Chinese Journal of Clinical Neuroscience,2020,28(03):287-300.

[8] Bhattacharyya N, Gubbels SP, Schwartz SR, et al. Clinical Practice Guideline:Benign Paroxysmal Positional Vertigo (Update) Executive Summary[J]. Otolaryngol Head Neck Surg, 2017, 156(3): 403-416.

[9] Editorial Board of Chinese Journal of Otolaryngology Head and Neck Surgery, Chinese Medical Association Otolaryngology Head and Neck Surgery Branch. Guidelines for the diagnosis and treatment of Meniere's disease (2017)[J]. Chinese Journal of Otolaryngology Head and Neck Surgery, 2017, 52(03): 167-172.

[10] Chinese Medical Association Neurology Branch, Editorial Board of Chinese Journal of Neurology. Multidisciplinary expert consensus on the diagnosis and treatment of vertigo[J]. Chin J Neurology, 2017, 50(11):805-812.

[11] Editorial Board of Chinese Journal of Otolaryngology Head and Neck Surgery, Chinese Medical Association Otolaryngology Head and Neck Surgery Branch. Guidelines for the Diagnosis and Treatment of Sudden Deafness (2015)[J]. Chinese Journal of Otolaryngology Head and Neck Surgery,2015,50(6):443-447.

Chen Hua,Yu Qingsheng. Research progress of betahistine in the treatment of vertigo[J].Chinese Journal of New Drugs,1998(04):54-56.

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