Vestibo, tablets 24 mg 30 pcs

Pharmacotherapeutic group: Histamine drug

ATX code: N07CA01

Pharmacological properties

.Pharmacodynamics

The mechanism of action of betahistine is only partially known. There are several possible hypotheses supported by preclinical and clinical data:

Influence on the histaminergic system

Partial agonist of H1-histamine and antagonist of H3-histamine receptors of the vestibular nuclei of the central nervous system (CNS), with little activity against H2 receptors. Betahistine increases histamine metabolism and release by blocking presynaptic H3 receptors and decreasing H3 receptors.

Augment blood flow to the cochlear region as well as the entire brain

According to preclinical studies, betahistine improves blood flow in the inner ear vasculature by relaxing the precapillary sphincters of the inner ear vessels. Betahistine has also been shown to increase cerebral blood flow in humans.

Easing central vestibular compensation

Betahistine accelerates the recovery of vestibular function in animals after unilateral vestibular neurectomy by accelerating and facilitating central vestibular compensation through antagonism with H3-histamine receptors.

The recovery time after vestibular neurectomy in humans is also reduced with treatment with betahistine.

Anxiety of neurons in the vestibular nuclei

Dose-dependently reduces the generation of action potentials in neurons of the lateral and medial vestibular nuclei.

Pharmacodynamic properties found in animals provide a positive therapeutic effect of betahistine in the vestibular system.

The efficacy of betahistine has been demonstrated in patients with vestibular vertigo and Meniere’s syndrome, as evidenced by a reduction in the severity and frequency of dizziness.

Pharmacokinetics

absorption

. When taken orally, betahistine is rapidly and almost completely absorbed in the gastrointestinal (GI) tract. After absorption, betahistine is rapidly and almost completely metabolized to form the metabolite 2-pyridylacetic acid. The plasma concentration of betahistine is very low. Thus, pharmacokinetic assays are based on measuring the concentration of the metabolite 2-pyridylacetic acid in plasma and urine.

When the drug is taken with food, the maximum concentration (Cmax) of betahistine in the blood is lower than when taken on an empty stomach. However, the total absorption of betahistine is the same in both cases, indicating that food intake only slows the absorption of betahistine.

Distribution

The binding of betahistine to plasma proteins is less than 5%.

Biotransformation

After absorption, betahistine is rapidly and almost completely metabolized to form the metabolite 2-pyridylacetic acid (which has no pharmacological activity). The maximum concentration (Cmax) of 2-pyridylacetic acid in blood plasma (or urine) is reached one hour after taking the drug. The elimination half-life (T_1/2) is approximately 3.5 h.

Elimation

2-pyridylacetic acid is rapidly excreted in the urine. When the drug is taken at a dose of 8 to 48 mg, about 85% of the initial dose is detected in the urine. Excretion of betahistine by the kidneys or through the intestine is insignificant.

Linearity

The rate of excretion remains constant with oral administration of 8 – 48 mg of the drug, indicating linearity in the pharmacokinetics of betahistine, and suggesting that the metabolic pathway involved remains unsaturated.

Indications

Hearing impairment, Meniere’s disease, Headache, Tinnitus, Impaired cerebral circulation, Dizziness

Meniere’s syndrome, characterized by the following main symptoms:

– dizziness (accompanied by nausea/vomiting);

– hearing loss (hearing loss);

– tinnitus;

Symptomatic treatment for vestibular vertigo (vertigo).

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Active ingredient

Betahistine

Composition

1 tablet contains:

active ingredient: betahistine dihydrochloride 24.0 mg;

excipients: povidone K90 6.0 mg, microcrystalline cellulose (Vivapur 101) 99.0 mg, lactose monohydrate 210.0 mg, colloidal silicon dioxide 7.5 mg, crospovidone 18.0 mg, stearic acid 13.5 mg.

How to take, the dosage

Orally, with meals.
The drug dose for adults is 48 mg of betahistine per day.
The drug should be taken 1 tablet 2 times a day. The tablet can be divided into two equal parts.
The dose should be adjusted individually, depending on the response to treatment. Improvement is sometimes only seen after a few weeks of treatment. The best results are sometimes achieved after several months of treatment. There is evidence that prescribing treatment early in the disease prevents progression and/or hearing loss in later stages.

Elderly age
Despite limited clinical trial data, extensive post-registration experience suggests that dose adjustment in this patient group is not necessary.

Patients with renal/hepatic impairment
No specific clinical studies have been conducted in this patient group, but post-registration experience suggests that no dose adjustment is required in this patient group.

Always take the drug as prescribed by your physician. If you have any questions, you should consult your doctor.

Interaction

If at present or in the recent past you have taken other medicinal products, including without a prescription, please inform the attending physician.

There have been no in vivo studies to study the interaction with other medicinal products. Based on in vitro data, it can be assumed that there is no inhibition of cytochrome P450 isoenzyme activity in vivo.

The in vitro data showed inhibition of betahistine metabolism by drugs that inhibit MAOIs, including MAO subtype B (e.g., selegiline). Caution should be exercised when concomitant administration of betahistine and MAOI inhibitors (including MAO subtype B).

Betahistine is a histamine analog, and an interaction of betahistine with H1-histamine receptor blockers could theoretically affect the effectiveness of one of these drugs.

Special Instructions

The rasp on the tablet is designed to break the tablet in order to facilitate its swallowing and is not intended to divide it into two equal doses.

Influence on the ability to drive vehicles, mechanisms
Betahistine has no or negligible effect on the ability to drive vehicles and operate mechanisms, in clinical trials adverse reactions that could affect such ability have not been identified.

Synopsis

Round biconvex tablets from white to almost white in color, with a rib on one side.

Contraindications

– hypersensitivity to any of the drug components;
– pheochromocytoma;

Betahistine is not recommended for use in children under 18 years of age due to insufficient data on efficacy and safety.

The drug contains an adjuvant – lactose. Patients with rare hereditary problems of galactose intolerance, lactase deficiency (Lapp type) or glucose-galactose malabsorption should not use it.

With caution
Patients with bronchial asthma, peptic ulcer disease and/or duodenal disease require close monitoring during treatment.

Side effects

According to the World Health Organization (WHO) classification, all reactions are categorized by organ system and frequency of occurrence: Very frequent (> 1/10); frequent (> 1/100, < 1/10); infrequent (> 1/1000, < 1/100); rare (> 1/10000, < 1/1000); very rare (< 1/10000); frequency unknown (cannot be determined from available data).

Nervous system disorders:

frequent: headache.

Gastrointestinal (GI) disorders:

frequent: nausea and dyspepsia.

In addition to the above adverse effects identified in clinical studies, the following adverse effects have been reported during post-registration use and in the scientific literature. There is insufficient data available to estimate their frequency.

Immune system disorders:hypersensitivity reactions, including anaphylactic reactions.

Gastrointestinal (GI) disorders:moderate disorders such as vomiting, gastrointestinal pain, bloating. These effects usually disappear after taking the drug simultaneously with food or after reducing the dose.

Skin and subcutaneous tissue disorders:

Hypersensitivity reactions, especially angioedema, urticaria, itching, and rash.

If you notice any side effects not mentioned in these instructions, or if any side effect is serious, please tell your doctor.