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

Ingredient	amount
Active substance:
Betahistine dihydrochloride	8 mg	16 mg	24 mg
Auxiliary substances:
lactose monohydrate	122.7 mg	245.4 mg	368.1 mg
microcrystalline cellulose	5.37 mg	10.74 mg	16.11 mg
magnesium stearate	1.38 mg	2.76 mg	4.14 mg
Silica colloidal dioxide	0.7 mg	1.4 mg	2.1 mg
corn starch	1.85 mg	3.7 mg	5.55 mg

Description:

Tablets are white or white with a yellowish tint of color. Light marble is allowed. Tablets 8 mg - round, biconcave, without risks, 16 mg - round, biconcave, with a risk. Tablets of 24 mg are round, flat-cylindrical, with a risk and a facet.

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 antagonist of the H1-histamine antagonist of the H3-histamine receptors of the vestibular nuclei of the central nervous system (CNS), has little activity with respect to H2 receptors. Betagistin increases histamine metabolism and its release by blocking presynaptic H3-retenters and reducing the number of H3 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 the impapillary sphincters of the vessels of the inner ear. It is also shown that betagistin increases the blood flow of the brain in humans.

Facilitation of central vestibular compensation Betagistin accelerates the restoration of vestibular function in animals after unilateral vestibular neurectomy, accelerating and facilitating central vestibular compensation due to antagonism with H3-histamine receptors.

The recovery time after vestibular neurrectomy in humans also decreases.

Excitation of neurons in the vestibular nuclei

Dose-dependent, reduces the generation of action potentials in neurons of the lateral and medial vestibular nuclei.

Pharmacodynamic 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

With oral intake betagistin quickly and almost completely absorbed in the gastrointestinal tract (GIT). After absorption, the drug is rapidly and almost completely megabolized to form a metabolite of 2-pyridylacetic acid in blood plasma and urine. 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. When taking the drug with food, the maximum concentration (Cmax) of the drug in the blood is lower than when taken on an empty stomach. However, the total absorption of betagistin is the same in both cases, which indicates that eating 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 half-life period is approximately 3.5 hours.

Excretion

2-peridylacetic acid is quickly 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 Ménière's syndrome, characterized by dizziness (accompanied by nausea and vomiting), hearing loss and noise in the ears.

Symptomatic treatment of vestibular vertigo.

Contraindications:

Hypersensitivity, pregnancy, the period of breastfeeding, children's age.

Hypersensitivity to any of the components of the drug.

Children under 18 years (due to lack of data).

The drug should not be taken in patients with lactose intolerance. Deficiency of lactase, glucose-galactose malabsorption syndrome (the preparation contains lactose).

Pheochromocytoma.

Carefully:Peptic ulcer of stomach or duodenum (in the anamnesis), bronchial asthma, urticaria, exanthema, allergic rhinitis, arterial hypotension, when taking antihistamines.

Pregnancy and lactation:

There is insufficient data to assess the effects of the drug during pregnancy and breastfeeding. In this regard, it is not recommended reception during pregnancy. For the duration of treatment it is necessary to stop breastfeeding.

Dosing and Administration:

Inside, with food.

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

Tablets 16 mg: 1/2 tablet 3 times a day.

Tablets 24 mg: 1 tablet 2 times a day.

The maximum daily dose is 48 mg.

The dose and duration of treatment should be selected individually, depending on the patient's response to treatment.

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

Correction of dose in elderly patients, as well as in patients with renal and / or liver failure is not required.

Side effects:

Impaired nervous system: often (from ≥1/100 to <1/10)

headache, weakness, fatigue, dizziness, lethargy, drowsiness, insomnia.

From the digestive system: often (from ≥1/100 to <1/10)

nausea, dyspepsia (vomiting, abdominal pain, bloating, diarrhea). how Normally, these effects disappear if you take the drug at the same time as a beggar or after a dose reduction.

In addition to these effects identified during clinical trials, post-marketing and scientific literature reported the following side effects (available data are not sufficient to estimate their frequency).

Allergic reactions: hypersensitivity, incl. anaphylactic reactions, angioedema.

From the skin: urticaria, itching, skin rash, redness.

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

Treatment: symptomatic.

Interaction:

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

Cases of interaction or incompatibility with other medicinal products are unknown.

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 betahistin metabolism under the Action of drugs that inhibit monoamine oxidase (MAO), including MAO of subtype B (for example, selegiline). Caution should be exercised while concomitant administration of betagistin and MAO inhibitors (including MAO-B).

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

Has no sedative effect and does not affect the ability to drive vehicles or work on machines and mechanisms.

Form release / dosage:

Tablets of 8 mg, 16 mg, 24 mg.

Packaging:

7 tablets per contour cell package. 2, 3, 4 contour mesh packages together with instructions for use are placed in a pack of cardboard.

10 tablets per contour cell pack. 1, 2, 3, 4, 5 contour mesh packages together with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark place at a temperature not higher than

25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003159

Date of registration:31.08.2015

Expiration Date:31.08.2020

The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia

Manufacturer: & nbsp

PRANAFARM, LLC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betagistin (Betahistine)