4mg Betahistine Hydrochloride Tablets, 12 tablets
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4mg Betahistine Hydrochloride Tablets, 12 tablets
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Product Details
Date of approval: 15 November 2021
Betahistine Hydrochloride Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician.
[Drug Name]
Generic name: Betahistine Hydrochloride Tablets
English name: Betahistine Hydrochloride Tablets
Pinyin: Yansuan Beitasiting Pian
[Element]
The active ingredient of this product is betahistine hydrochloride.
Chemical name: N-methyl-2-pyridineethylenediamine dihydrochloride
chemical structural formula ：
Molecular formula: C8H12N2·2HCl
Molecular weight: 209.12
[Shape and Properties]
This product is a white or off-white tablet.
[Indication]
For the treatment of vertigo, tinnitus, and hearing loss associated with Ménière's syndrome.
[Specifications]
（1）4mg （2）8mg
[Usage and Dosage]
The initial dose is 4mg per administration, three times daily, preferably taken with meals. The dose should be adjusted according to age and symptoms, with a maximum daily dose of 48 mg.
[Untoward Effect]
In placebo-controlled clinical trials, the following adverse reactions were observed in patients treated with betahistine: very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1000 to <1/100); rare (≥ 1/10000 to <1/1000); and very rare (<1/10000).
Gastrointestinal dysfunction
Common: nausea and dyspepsia
Neurological abnormalities
Common: headache
In addition to the adverse reactions reported in clinical trials, the following adverse reactions have been reported following post-marketing surveillance and in the literature. (The frequency cannot be estimated from available data and is therefore classified as 'unknown').
Abnormal immune system: allergic reaction
Gastrointestinal system abnormalities: Mild gastric discomfort (e.g., vomiting, gastrointestinal pain, bloating). These symptoms can be alleviated by taking the medication with meals or reducing the dosage.
Abnormalities of the skin and subcutaneous tissue: angioedema, urticaria, rash, and pruritus.
[Taboo]
Pheochromocytoma. Contraindicated in patients with hypersensitivity to any component of this product.
[Matters Need Attention]
Use with caution in patients with a history of peptic ulcer disease or bronchial asthma, and close monitoring should be performed.
[Medication Use in Pregnant and Lactating Women]
Gravida
Pregnancy: There is insufficient data on the use of betahistine in pregnant women. Animal studies are inadequate regarding the effects of this product on pregnancy, embryonic/fetal development, delivery, and postpartum development. The potential risks to humans are unknown unless the benefits outweigh the risks. Betahistine should not be used during pregnancy.
feed a baby at the breast
It is currently unclear whether betahistine is secreted in breast milk. No studies have been conducted to determine whether this product is secreted in the milk of animals. The use of this medication in lactating women should be carefully considered after weighing the maternal benefits against potential risks to infants.
Pediatric Medication
The safety and efficacy of this product in children have not been established.
Geriatric Medication
Monitor and adjust the dose as needed.
[Drug Interaction]
No in vivo studies on drug interactions have been conducted. According to in vitro study data, there is no inhibitory effect on cytochrome P450 enzymes.
In vitro studies have demonstrated that drugs inhibiting monoamine oxidase (MAO), including MAO subtype B (e.g., selegiline), can suppress the metabolism of betahistine. Caution should be exercised when combining betahistine with MAO inhibitors.
Since betahistine is a histamine analogue, there may theoretically be an interaction between betahistine and antihistamines, which could affect the efficacy of one drug.
[Overdose]
There have been a few reports of overdoses. Some patients experienced mild to moderate symptoms (e.g., nausea, drowsiness, abdominal pain) at doses as high as 640 mg. More severe cases (e.g., convulsions, pulmonary or cardiac complications) occurred with intentional overdose of betahistine, particularly when used in combination with other overdosed medications. Treatment measures for drug overdoses should include standard supportive care.
[Pharmacology and Toxicology]
Pharmacological Action
The mechanism of action of betahistine remains unclear. Based on animal and human data, it is hypothesized to be potentially related to the following:
Affects the histamine system:
Betahistine acts as both a partial agonist of histamine H1 receptors and an antagonist of histamine H3 receptors in neural tissues, with negligible H2 receptor activity. It enhances the conversion and release of histamine by blocking presynaptic H3 receptors and inducing H3 receptor downregulation.
may increase blood flow to the cochlear region and the entire brain:
Pharmacological studies in animals have demonstrated improved blood circulation in the vascular pattern of the inner ear, which may be achieved by relaxing the precapillary sphincter of the inner ear microcirculation. Betahistine also enhances cerebral blood flow in humans.
Promote vestibular compensation:
Betahistine accelerates vestibular recovery after unilateral nerve resection in animals by promoting central vestibular compensation, which is achieved through inhibition of histamine conversion and release mediated by H3 receptors. In human subjects, patients undergoing vestibular nerve resection exhibited shortened recovery time with betahistine administration.
Betahistine alters neuronal firing in the vestibular nuclei:
Betahistine exerts dose-dependent inhibitory effects on the firing of neurons in the lateral and medial vestibular nuclei. The pharmacodynamic properties demonstrated in animals support the therapeutic role of betahistine in the vestibular system. In studies involving patients with vestibular vertigo and Ménière's syndrome, betahistine has shown therapeutic efficacy, improving the severity and frequency of vertigo episodes.
Toxicology Studies
Genetoxic
Betahistine was negative in routine in vitro and in vivo genotoxicity tests.
Genotoxicity
The effects of the animal reproductive toxicity test were only observed at exposures exceeding the maximum human exposure, suggesting no significant correlation with clinical use. In limited studies on reproductive toxicity in rats and rabbits, betasidine showed no teratogenic effects.
Carcinogenicity
Histopathological examination in the rat 18-month repeated administration toxicity study showed no carcinogenic effect, but betasidine was not specifically tested for carcinogenicity.
[Pharmacokinetics]
Absorb ：
Betahistine is rapidly and almost completely absorbed throughout the gastrointestinal tract after oral administration. Following absorption, the drug is quickly and almost entirely metabolized into 2-pyridylacetic acid. The plasma concentration of betahistine is very low. Therefore, pharmacokinetic analysis is primarily based on the detection of 2-pyridylacetic acid in plasma and urine.
Compared to fasting conditions, the Cmax is reduced under postprandial conditions. However, the total absorption is similar under both fasting and postprandial conditions. Therefore, it can be concluded that food intake only slows the absorption rate of betasidine.
Distribution ：
The plasma protein binding of betalystine is less than 5%.
Bioconversion ：
After absorption, betahistine is rapidly and almost completely metabolized into 2-pyridylacetic acid (non-pharmacologically active). The peak plasma and urinary concentrations of 2-pyridylacetic acid are reached 1 hour after oral administration of betahistine, with a half-life of 3.5 hours.
Drain ：
2-Pyridylacetic acid is rapidly excreted in urine. Within the dose range of 8mg to 48 mg, approximately 85% of the original dose can be recovered in urine. The levels of betahistine prodrug in urine and feces are extremely low.
Linear ：
The recovery was constant in the range of 8mg-48mg, indicating that the pharmacokinetics of betahistine was linear in this range and the metabolic pathway involved was not saturated.
[Store Up]
Seal and store in a dry place below 25°C.
[Pack]
Pharmaceutical aluminum foil, PVC/PVDC solid pharmaceutical composite hard sheet packaging, 12 sheets/plate × 1 plate/box; 12 sheets/plate × 2 plates/box; 12 sheets/plate × 3 plates/box.
[Term of Validity]
24 months
[Operative Norm]
(1) 4mg: National Medical Products Administration Drug Registration Standard YBH14872021
(2) 8mg: National Medical Products Administration Drug Registration Standard YBH14872021
[License number]
(1) 4 mg: National Drug Approval Number H41023380
(2) 8 mg: National Drug Approval Number H20217112
[Marketing Authorization Holder]
Name: Henan Zhongjie Pharmaceutical Co., Ltd.
Registered address: South Railway Station, Xinxiang City, Henan Province
[Manufacturing Enterprise]
Company Name: Henan Zhongjie Pharmaceutical Co., Ltd.
Production address: South Railway Station, Xinxiang City, Henan Province
Postal Code: 453003
Phone Number: +86-373-5071333
Fax: +86-373-5071222
Website: http://www.xxzjyy.com.cn
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