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

Excipients: Copovidone 5.2 mg, 10.4 mg, 15.6 mg; lactose monohydrate 41.6 mg, 83.2 mg, 124.8 mg; magnesium stearate 1 mg, 2 mg, 3 mg; cellulose microcrystalline 64.2 mg, 128.4 mg, 192.6 mg.

Description:Tablets are almost white or white with a creamy shade of color, round, flat-cylindrical with a bevel (dosage of 8 mg) or with chamfer and risk (dosages of 16 mg and 24 mg). Allowed a slight marbling.

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, confirmed by preclinical and clinical data:

Effect on the histaminergic system. Partial agonist H₁-gistaminovyh and antagonist H₃-gistaminovyh receptors of the vestibular nuclei of the central nervous system, has little activity in relation to H₂-gistaminovyh receptors. Betagistin increases histamine metabolism and its release by blocking presynaptic H₃-gistaminovyh receptors and reduce the number of H₃-gistaminovyh receptors.
Increased blood flow of the cochlear region, as well as the entire brain. According to pre-clinical 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 enhances cerebral blood flow in humans.
Facilitating the process of central vestibular compensation. Betagistin accelerates the restoration of vestibular function in animals after unilateral vestibular neurectomy, accelerating and facilitating neutral 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 pharmacological properties found on animals provide a positive therapeutic effect of betahistine in the vestibular system. The efficacy of betahistine was demonstrated in patients with vestibular dizziness and Menier's syndrome, which was manifested by a decrease in the severity and frequency of dizziness.

Pharmacokinetics:

Suction

When taken orally betagistin quickly and almost completely absorbed in the gastrointestinal tract. After absorption, the drug is rapidly and almost completely metabolized to form a metabolite of 2-pyridylacetic acid. The concentration of betagistin in the blood plasma is very low. Thus, pharmacokinetic analyzes are based on measuring the concentration of the metabolite of 2-pyridylacetic acid in plasma and urine. When taking the drug with food, the maximum concentration of C_mOh the drug in the blood is lower than when taken on an empty stomach. However, the total absorption of betahistin is the same in both cases, indicating that eating only slows the absorption of betahistine.

Distribution

Binding of betahistine to plasma proteins is less than 5%.

Biotransformation

After suction betagistin quickly and almost completely metabolized to form a metabolite of 2-pyridylacetic acid (which does not have pharmacological activity). The maximum concentration of 2-pyridylacetic acid in blood plasma (or urine) is reached in an hour after administration. The elimination half-life is approximately 3.5 hours.

Excretion

2-pyridylacetic acid is rapidly excreted in the urine. When taking the drug at a dose of 8-48 mg, about 85% of the initial dose is found in the urine. The excretion of betagistin by the kidneys or through the intestine is negligible.

Linearity

The elimination rate remains constant with 8-48 mg of oral ingestion, indicating the linearity of the pharmacokinetics of betahistin, and suggests that the involved metabolic pathway remains unsaturated.

Indications:Treatment for Meniere's syndrome, characterized by dizziness (accompanied by nausea and vomiting), hearing loss and noise in the ears.

Symptomatic treatment of vestibular vertigo.

Contraindications:

- Hypersensitivity to betahistine or to any of the components of the drug;

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- pheochromocytoma;

- Pregnancy;

- the period of breastfeeding;

- age under 18 years (efficiency and safety not established).

Carefully:

Stomach ulcer or 12 duodenal ulcer (in the anamnesis), bronchial asthma, patients with arterial hypotension.

Pregnancy and lactation:

The use of betagistin during pregnancy and during breastfeeding is contraindicated due to the lack of sufficient data on its safety during pregnancy and during breastfeeding. It is not known whether betagistin with breast milk; if the drug is needed during breastfeeding, breastfeeding should be discontinued.

Dosing and Administration:

Inside, with food.

Tablets 8 mg: 1-2 tablets 3 times a day.

Tablets 16 mg: ½-1 tablet 3 times a day.

Tablet 24 mg: 1 tablet 2 times a day.

The course of treatment is determined individually. Treatment is long.

There is no need for dose adjustment in elderly patients, as well as in patients with hepatic and / or renal insufficiency.

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

Side effects:

Classification of the incidence of side effects in accordance with the recommendations of the World Health Organization: very 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.

From the digestive system:

often - nausea, indigestion;

the frequency is unknown - vomiting, a feeling of heaviness in the epigastrium, abdominal pain, bloating.

From the skin:

frequency unknown - skin itching, rash, urticaria, angioedema.

Allergic reactions:

frequency is unknown - hypersensitivity reactions, incl. anaphylactic reactions.

From the central nervous system:

often a headache.

Overdose:

Symptoms: nausea, abdominal pain, drowsiness (when taken in a dose of up to 640 mg), convulsions, cardiopulmonary complications (when taken at a dose of more than 640 mg or in combination with other medicines).

Treatment: gastric lavage, intake of activated charcoal, symptomatic therapy.

Interaction:

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

Data in vitro showed inhibition of beta-histidine metabolism by drugs that inhibit monoamine oxidase (MAO), including MAO subtype B (eg seleginin). Caution should be exercised while concomitant administration of betagistin and MAO inhibitors (including MAO-B).

Betagistin is an analog of histamine, the interaction of betahistine with blockers H₁-gistaminovyh receptors can theoretically affect the effectiveness of one of these drugs.

Special instructions:

The therapeutic effect in a number of cases increases within a few months from the start of treatment.

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

In patients with peptic ulcer or duodenal ulcer (in the anamnesis), bronchial asthma,arterial hypotension, the drug should be used with caution and under the supervision of the attending physician.

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

Betagistin is indicated for the treatment of Ménière 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. According to the results of clinical studies it has been proved that the effect of betahistine on the ability to drive vehicles and work with mechanisms is absent or insignificant.

Form release / dosage:

Tablets, 8 mg, 16 mg and 24 mg.

Packaging:

For 10 or 30 tablets (doses of 8 mg and 16 mg), 10 or 15 tablets (24 mg dosage) in a contiguous cell pack of a PVC film or PVC / PVC film or PVC / PCTFE film and aluminum lacquered aluminum foil.

According to 1, 2, 3, 6 contour cell packs of 10 tablets or 2, 4 contour packs of 15 tablets each, or 1, 2 circuit packs of 30 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light 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 the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002330

Date of registration:15.09.2011 / 19.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betagistin Canon (Betahistine Canon)