Betaserk

General characteristics. Structure:

Active agent: a betagistina dihydrochloride of 8 mg (for a dosage of 8 mg), 16 mg (for a dosage of 16 mg).

Excipients: cellulose microcrystallic — 80,8 mg (161,5 mg), Mannitolum (E421) — 25,0 mg (50,0 mg), citric acid monohydrate — 2,5 mg (5,0 mg), silicon dioxide colloid — 2,5 mg (5,0 mg), talc — 6,3 mg (12,5 mg).

Description

For a dosage of 8 mg:

Round flat tablets of white or almost white color with slanted edges with an engraving "256" on one party of a tablet.

For a dosage of 16 mg:

Round biconvex tablets of white or almost white color with slanted edges from a tablet, risky on one party, and an engraving "267" on both sides from risks.

Pharmacological properties:

The mechanism of action of a betagistin is known only partially. There are several possible hypotheses confirmed with preclinical and clinical data:
Influence on gistaminergichesky system
The partial agonist of H1-histamine and the antagonist of H3-histamine receptors of vestibular nuclei of TsNS, has insignificant activity concerning H2 receptors. Betagistin increases exchange of a histamine and its release by blocking presynaptic H3 receptors and decrease in quantity of H3 receptors.
Strengthening of a blood-groove of cochlear area, and also all brain
According to preclinical trials бетагистин improves blood circulation in a vascular stripe of an inner ear due to relaxation of precapillary sphincters of vessels of an inner ear. It is also shown what бетагистин strengthens a brain blood stream at the person.
Simplification of process of the central vestibular compensation
Betagistin accelerates recovery of vestibular function at animals after a unilateral vestibular neurectomy, accelerating and facilitating the central vestibular compensation for the account of antagonism with H3-histamine receptors.
Recovery time after a vestibular neurectomy at the person at treatment betagistiny also decreases.
Excitement of neurons in vestibular nuclei
Dozozavisimo reduces generation of action potentials in neurons of lateral and medial vestibular nuclei.
The Pharmakodinamichesky properties revealed on animals provide positive therapeutic effect of a betagistin in vestibular system.
Efficiency of a betagistin was shown at patients with vestibular dizziness and Menyer's syndrome that was shown by reduction of expressiveness and frequency of dizzinesses.

Pharmacokinetics. Absorption

At oral administration бетагистин it is quickly and almost completely soaked up in digestive tract. After absorption drug quickly and almost is completely metabolized with formation of a metabolite of 2-pyridylacetic acid. Concentration of a betagistin in a blood plasma very low. Thus, pharmacokinetic analyses are based on measurement of concentration of a metabolite of 2-pyridylacetic acid in plasma and urine.

At administration of drug with food the maximum concentration (Cmax) of drug in blood is lower, than at reception on an empty stomach. However total absorption of a betagistin is identical in both cases that it indicates that meal only slows down absorption of a betagistin.

Distribution

Linkng of a betagistin with proteins of a blood plasma makes less than 5%.

Biotransformation

After absorption бетагистин quickly and almost it is completely metabolized with formation of a metabolite of 2-pyridylacetic acid (which has no pharmacological activity). The maximum concentration of 2-pyridylacetic acid in a blood plasma (or urine) is reached in an hour after reception. Elimination half-life about 3,5 hours.

Removal

2-pyridylacetic acid is quickly removed with urine. At administration of drug in a dose of 8-48 mg about 85% of an initial dose are found in urine. Removal of a betagistin kidneys or through intestines slightly.

Linearity

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 unsaturated.

Indications to use:

Menyer's syndrome which is characterized by the following main symptoms:

— the dizziness (which is followed by nausea/vomiting)

— decrease in hearing (relative deafness)

— sonitus

Symptomatic treatment of vestibular dizziness (вертиго).

Route of administration and doses:

Always accept Betaserk® precisely as your attending physician registered. If you have any questions, consult with your attending physician.

Inside, during food.

The drug dose for adults makes 24-48 mg of a betagistin a day.

It is necessary to accept Бетасерк® 8 mg on 1-2 tablets 3 times a day.

ÜÑÔáßÑÓ¬® 16 mg should be accepted on ½ - 1 tablet 3 times a day. The tablet can be divided into two equal parts. Place a tablet on a firm surface risky up and pressure her a thumb.

The dose should be selected individually depending on reaction to treatment. Improvement is sometimes observed only in several weeks of treatment. The best results are sometimes achieved after several months of treatment. There are data that purpose of treatment at the beginning of a disease prevents its progressing and/or a hearing loss at later stages.

Advanced age

Despite limitation of these clinical trials, extensive post-registration experience assumes that dose adjustment is not required from this group of patients.

Patients with a renal/liver failure

Special clinical trials in this group of patients were not conducted, however post-registration experience gives the grounds to assume that dose adjustment is not required from this group of patients.

Side effects:

If you noticed any side effects which are not mentioned in this instruction, or any side effect accepted serious character, notify, please, your attending physician.

Disturbances from digestive tract: Often (from ≥1/100 to <1/10): nausea and dyspepsia.

Disturbances from a nervous system: Often (from ≥1/100 to <1/10): headache.

Except these effects revealed at conduct of clinical trials in the course of post-registration use and in scientific literature it was reported about the following undesirable effects. The available data are not enough to estimate their frequency.

Disturbances from immune system: hypersensitivity reaction, including anaphylactic reaction.

Disturbances from digestive tract: moderate frustration, such as vomiting, gastrointestinal pains, abdominal distention. These effects usually disappear after administration of drug along with food or after a dose decline.

Disturbances from skin and hypodermic fabrics: hypersensitivity reactions, in particular Quincke's disease, small tortoiseshell, itch and rash.

Interaction with other medicines:

If now or in the recent past you accepted other medicines, including without appointment of the doctor, report about it, please, to the attending physician.

The researches in vivo directed to studying of interaction with other medicines were not conducted. Based on these in vitro, it is possible to assume lack of inhibition of activity of isoenzymes of in vivo P450 cytochrome.

These in vitro showed inhibition of metabolism of a betagistin under the influence of drugs which inhibit monoamine an oxidase (MAO), including MAO of a subtype B (for example, селегилин). It is necessary to be careful at co-administration of a betagistin and MAO inhibitors (including MAO-B).

Betagistin is a histamine analog, interaction of a betagistin with blockers of H1-histamine of receptors can theoretically influence efficiency of one of these medicines.

Influence on ability to driving and other mechanisms

Betagistin does not influence or slightly influences ability to manage vehicles and to work with mechanisms, in clinical trials undesirable reactions which could affect such ability are not revealed.

Contraindications:

— pheochromocytoma;

— hypersensitivity to any of drug components.

Бетасерк® it is not recommended for use for children aged up to 18 years in connection with insufficiency of data on efficiency and safety.

With care

Patients with bronchial asthma, a peptic ulcer of a stomach and/or duodenum demand careful observation during treatment.

Use at pregnancy and during breastfeeding

Pregnancy

The available data on use of a betagistin by pregnant women are not enough.

The potential risk for the person is unknown. Betagistin should not be used during pregnancy except for cases of absolute necessity.

Lactation

It is unknown whether it is allocated бетагистин with breast milk. It is not necessary to accept drug during breastfeeding. The issue of purpose of medicine of mother has to be resolved only after comparison of advantage of breastfeeding to potential risk for the baby.

Overdose:

Several cases of overdose of drug are known. At some patients easy and moderate symptoms (nausea, drowsiness, an abdominal pain) after administration of drug in doses to 640 mg were observed. More serious complications (spasms, cardiopulmonary complications) were observed at deliberate reception of the raised doses of a betagistin, especially in combination with overdose of other medicines.

The symptomatic treatment is recommended.

Storage conditions:

List B. In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity of 5 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 8 mg; 16 mg.

On 15 tablets in PVC/PVDH / the blister, on 2 blisters together with the application instruction in a cardboard pack Is scarlet.

On 20 tablets in PVC/PVDH / the blister, on 3 blisters together with the application instruction in a cardboard pack Is scarlet.

On 30 tablets in PVC/PVDH / the blister, on 1 or 2 blisters together with the application instruction in a cardboard pack Is scarlet.