Vestibo, tablets 16 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

Active ingredient

Composition

1 8 mg tablet contains:

the active ingredient: betahistine dihydrochloride 8.0 mg;

excipients: povidone K90 2.0 mg, microcrystalline cellulose (Vivapur 101) 33.0 mg, lactose monohydrate 70.0 mg, colloidal silicon dioxide 2.5 mg, crospovidone 6.0 mg, stearic acid 4.5 mg.

1 16 mg tablet contains:

the active ingredient: betahistine dihydrochloride 16.0 mg;

excipients: povidone K90 4.0 mg, microcrystalline cellulose (Vivapur 101) 66.0 mg, lactose monohydrate 140.0 mg, colloidal silicon dioxide 5.0 mg, crospovidone 12.0 mg, stearic acid 9.0 mg.

How to take, the dosage

Ingestion, with meals.

The dose of the drug for adults is 24 – 48 mg of betahistine per day.

Vestibo 8 mg

The 8 mg dosage should be taken 1 to 2 tablets 3 times daily.

Vestibo 16 mg

. The 16 mg dose should be taken in ⅟ 2 – 1 tablet 3 times a day. The 16 mg tablet can be divided into two equal parts.

The dose of the drug should be adjusted individually depending on the response to treatment.

Sometimes improvement is seen only after a few weeks of treatment. Sometimes the best results are seen after a few months of treatment. There is evidence that early treatment prevents progression and/or hearing loss in later stages of the disease.

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

Special clinical studies have not been performed in this patient group, but post-registration experience suggests that no dose adjustment is necessary in this patient group.

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

Interaction

Special Instructions

Synopsis

Contraindications

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, skin itching, and rash.

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

Overdose

Pregnancy use

Similarities