Betagistin

General characteristics. Structure:

Active ingredient: 8 mg, 16 mg or 24 mg of a betagistin of dihydrochloride in 1 tablet.

Excipients: mannitol, citric acid monohydrate, silicon dioxide colloid anhydrous, croscarmellose sodium, talc, cellulose microcrystallic.

Means against dizziness.

Pharmacological properties:

Pharmacodynamics. The synthetic analog of a histamine, shows histamine-like action. Betagistin is a partial agonist of histamine N1-and the antagonist of H3-histamine receptors of an inner ear and vestibular nuclei of the central nervous system. Improves microcirculation and permeability of capillaries of an inner ear, increases a blood stream in basilar arteries, normalizes endolymph pressure in a labyrinth and a snail. Normalizes transmitterny transfer in neurons of medial kernels of a vestibular nerve at the level of the bridge of a trunk part of a brain. Disturbances of a vestibular mechanism and cochlear frustration are as a result normalized, the frequency and intensity of dizzinesses decrease, noise and a ring in ears decreases, hearing improves.

Improvement of a state at acute vestibular frustration is noted in the first days of treatment betagistiny. The stable therapeutic effect is reached within 2 weeks of administration of drug and can increase at reception of a betagistin within several months.

Being H3 receptors inhibitor of kernels of a vestibular nerve, shows the expressed central vasodilating effect.

Pharmacokinetics. Absorption and distribution. After intake it is quickly and almost completely adsorbed from digestive tract. The maximum concentration in plasma is reached in 3 hours. Linkng with proteins low. Gets through gistogematichesky barriers.

Metabolism and removal. It is metabolized in a liver to 2-pyridyl-acetic acid which is almost completely removed from an organism with urine within 24 hours. At administration of drug in a dose of 8 - 48 mg about 85% of an initial dose are found in urine in the form of 2-pyridyl-acetic acid. Removal of a betagistin kidneys or through intestines slightly.

Speed of removal remains to a constant at oral administration of 8-48 mg of drug, indicating linearity of pharmacokinetics of a betagistin, and allows to assume that the involved metabolic way remains saturated. At administration of drug with food the maximum concentration of drug in blood is lower, than at reception on an empty stomach. However total adsorption of a betagistin is identical in both cases that it indicates that reception only slows down absorption of a betagistin.

Indications to use:

Symptomatic treatment of recurrent dizziness with existence or without cochlear symptoms.

Route of administration and doses:

Inside, during food, tablets are swallowed, without chewing, washing down with a glass of water.

Dosage of 8 mg. The usual dosage makes 1 – 2 tablets 3 times a day, but no more than 6 tablets, i.e. 48 mg of a betagistin a day.

Dosage of 16 mg. The usual dosage makes ½ – 1 tablet 3 times a day.

Dosage of 24 mg. This form of release is intended for use at patients for whom the daily dose of 48 mg of a betagistin is necessary. In other cases it is necessary to apply lower doses. The usual dosage makes 1 tablet 2 times a day.

Children and teenagers. Betagistin is not recommended for use for children and teenagers aged up to 18 years in connection with insufficiency of data on efficiency and safety.

Elderly patients. Betagistin has to be applied at elderly patients with care as the available data on safety are limited.

Renal failure. There are no data on use for patients with a renal failure.

Liver failure. There are no data on use for patients with a liver failure.

Treatment duration. The recommended duration of treatment makes from 2 to 3 months, treatment can be prolonged depending on the course of a disease. Treatment by perhaps discontinuous or continuous courses.

Features of use:

Patients with bronchial asthma demand careful observation during therapy betagistiny (risk of a bronchospasm).

In case of pains in a stomach it is necessary to carry out administration of drug during food.

Betagistin is not recommended to apply to treatment of the following morbid conditions:

- benign paroxysmal dizziness;

- the dizziness connected with damage of the central nervous system.

Children. Drug is not recommended to children.

Pregnancy. Researches at animals did not show any teratogenic action. In view of lack of any teratogenic action at animals, the similar effect at the person is not expected. Now it is considered that the substances causing malformations in the person have the proved teratogenic effect at animals when carrying out well controlled researches on two animal species.

So far enough reliable data for evaluating a possibility of teratogenic or embriotoksichesky effect of a betagistin at use during pregnancy is not received. Therefore, as a precautionary measure, it is not recommended to accept бетагистин during pregnancy.

Breastfeeding period. As there are no data on allocation of a betagistin in breast milk, the risk is not known; therefore, breastfeeding is not recommended during use of a betagistin.

Influence on ability to manage motor transport and mechanisms. There are no data on influence of medicine on ability to manage motor transport or other mechanisms.

Side effects:

Gastrointestinal frustration: often (from ≥ 1/100 to <1/10) nausea and dyspepsia. With an unknown frequency moderate frustration, such as vomiting, gastrointestinal pains, abdominal distention. As a rule, these effects usually disappear after administration of drug along with food or after a dose decline. Increase in level of transaminases is possible.

From immune system and a hemopoiesis: hypersensitivity reaction, including it was reported about anaphylactic reaction. Thrombocytopenia.

From skin and hypodermic and fatty kletchatki:reaktion of hypersensitivity, such as Quincke's disease, small tortoiseshell, itch and rash.

Interaction with other medicines:

Researches of interaction invivo directed to studying of interaction with other medicines were not conducted.

Betagistin does not cause inhibition of activity of isoenzymes of cytochrome P 450 invivo.

Contraindications:

• Hypersensitivity to any of medicine components.
• Active form of a peptic ulcer.
• Pheochromocytoma.

Overdose:

Symptoms: after reception of medicine in doses to 640 mg – nausea, drowsiness, an abdominal pain. More serious complications (spasms, cardiopulmonary complications) are observed at deliberate reception of the raised doses of a betagistin, especially in combination with overdose of other medicines.

Treatment: symptomatic therapy, purpose of antihistamines.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Medicine cannot be used after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

10 tablets in a blister strip packaging. The 3 or 5 blister strip packagings together with a leaf insert place in a pack from a cardboard.