Betagistin - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline - 199.20 mg; lactose monohydrate - 120.00 mg; silicon dioxide colloidal - 11.25 mg; talc - 9.30 mg; citric acid monohydrate 7.50 mg; calcium stearate - 3.75 mg.

Description:

Round flat-cylindrical tablets of white or almost white color with a facet and a risk.

Pharmacotherapeutic group:Histamine drug

ATX: & nbsp

N.07.C.A.01 Betagistin

Pharmacodynamics:

The mechanism of action of betagistin is known only in part. There are several possible hypotheses presented below, confirmed by preclinical and clinical data.

Effect on the histaminergic system

Partial agonist H1-histamine and antagonist of H3-histamine receptors of the vestibular nuclei of the central nervous system, has little activity against Hg-histamine receptors. Betagistin increases histamine metabolism and its release by blocking presynaptic H3-histamine receptors and reducing the amount of H3 histamine receptors.

Increased blood flow of the cochlear region, as well as the entire brain According to preclinical studies betagistin improves blood circulation in the vascular stria of the inner ear by relaxing precapillary sphincters of the vessels of the inner ear. It is also shown that betagistin increases the blood flow of the brain in humans.

Facilitating the process of central vestibular compensation

Betagistin accelerates the recovery of vestibular function in animals after unilateral vestibular neurectomy, speeding up and facilitating central vestibular compensation due to antagonism with H3-histamine receptors. The recovery time after vestibular neurectomy in humans in the treatment with betahistine is also reduced.

Excitation of neurons in the vestibular nuclei

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

The phtrmacodynamic properties found on animals provide a positive therapeutic effect of betagistip in the vestibular system.

The efficacy of betagistip was demonstrated in patients with vestibular dizziness and Meniere's syndrome, which was manifested by a decrease in the severity and frequency of dizziness.

Pharmacokinetics:

Suction

When ingested quickly and completely absorbed in the gastrointestinal tract. The intake of food slows the absorption of betagistin, but the total absorption is the same when administered on an empty stomach and with food.

Distribution

Communication with blood plasma proteins is low - less than 5%. Time to reach the maximum concentration in blood plasma - 1 hour.

Metabolism
Fast and almost completely metabolized in the liver with the formation of inactive metabolites: 2-pyridylacetic acid (the main metabolite) and dimethylbetahistine.

Excretion

85-90% is excreted by the kidneys in the form of 2-pyridylacetic acid for 24 hours. The excretion of betahistine and dimethylbetahistine by the kidneys is insignificant. Only a small part of betagistin and its metabolites are excreted by the intestine. The half-life is 3-4 hours. The rate of inoculation with oral administration of 8-48 mg of begagistin remains constant, indicating the linearity of the pharmacokinetics of betahistine.

Indications:

- treatment for Meniere's syndrome characterized by dizziness (accompanied by nausea and vomiting), hearing loss and tinnitus;

- symptomatic treatment and prevention of vestibular vertigo of various etiologies.

Contraindications:

- increased sensitivity to betagistin and other components of the drug;

- pheochromocytoma;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- pregnancy;

- the period of breastfeeding;

- age to 18 years (safety and efficacy not established).

Carefully:

- peptic ulcer of stomach or duodenum (in the anamnesis);

- bronchial asthma.

Pregnancy and lactation:

Contraindicated use of the drug in connection with the lack of sufficient data on the safety of its use during pregnancy and during breastfeeding.

It is not known whether betagistin with breast milk.

If taking the drug is necessary during breastfeeding, breastfeeding should be stopped.

If pregnancy is detected during drug treatment Betagistin, the drug should be discarded.

Dosing and Administration:

Inside, with food, not liquid, squeezed a little water.

1 tablet 2 times a day.

The maximum daily dose is 48 mg.

Dose and duration of treatment should be selected individually, depending on the patient's response to treatment. Treatment is long.

Improvement is sometimes observed after several weeks of treatment. The best results are sometimes achieved after several months of treatment.

In patients with renal or hepatic insufficiency, as well as in elderly patients, dose adjustment is not required.

Side effects:

Classification of the incidence of adverse events according to the recommendations of the World Health Organization (WHO):

Often ≥ 1/10;

often from ≥ 1/100 to <1/10;

infrequently from ≥ 1/1000 to <1/100;

rarely from ≥ 1/10000 to <1/1000;

very rarely <1/10000, including individual messages;

the frequency is unknown - it is not possible to establish the frequency of occurrence from the available data.

Co side of the digestive system: often - nausea, indigestion; frequency unknown - vomiting, pain in the area of the gastrointestinal tract, bloating.

From the central nervous system: often a headache.

From the skin: frequency unknown - redness, hives, skin rash, itchy skin.

Alpergic reactions: frequency is unknown - hypersensitivity reactions, including anaphylactic reactions, angioedema.

Overdose:

CиMpts: Abdominal pain, nausea, snotty (after taking betagistin in doses up to 640 mg); convulsions, cardiopulmonary complications (after taking betagistin in doses over 640 mg or in combination with other drugs).

Treatment: Gastric lavage, intake of adsorbents (activated charcoal), symptomatic therapy.

Interaction:

Research in vivo, aimed at studying the interaction of betahistine with other drugs, have not been conducted. Based on the data in vitro, it can be assumed that there is no inhibition of the activity of cytochrome P450 isoenzymes.

When used simultaneously with blockers H1-histamine receptors, the therapeutic effect of betahistine may decrease.

According to research in vitro, monoamine oxidase (MAO) inhibitors, including selective inhibitors of MAO subtype B, inhibit beta-histidine metabolism.When used simultaneously with MAO inhibitors, including selective MAO inhibitors of subtype B, an increase in the concentration of betahistine in the blood plasma is possible.

Special instructions:

The therapeutic effect is usually noted already at the beginning of therapy, but can be gradual and manifest within a few weeks of treatment. A stable therapeutic effect in some cases is achieved after several months of treatment.

Patients with arterial hypotension should be administered with caution and under the supervision of the treating physician.

Effect on the ability to drive transp. cf. and fur:

According to the results of clinical studies, it is considered that the effect of betahistine on the ability to control vehicles and mechanisms is absent or insignificant, since no effects potentially affecting this ability have been detected.

Begagistin is indicated for the treatment of Meniere's syndrome, which is characterized by a triad of major symptoms: dizziness, hearing loss, tinnitus, and symptomatic treatment of vestibular vertigo. Both states can adversely affect the ability to drive and operate machinery.

Form release / dosage:

Tablets 24 mg.

Packaging:

10 or 15 tablets in a contour cell box made of a polyvinylchloride film and aluminum foil.

1. 2. 3, 5 or 6 contour cell packs of 10 tablets, 2 or 4 contour packs of 15 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000593

Date of registration:21.09.2011 / 22.09.2016

Expiration Date:Unlimited

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

GRUNENTHAL, GmbH Germany

Representation: & nbspVERTEKS CJSC VERTEKS CJSC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betagistin (Betahistine)