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

Excipients: cellulose microcrystalline 66.40 mg, lactose monohydrate 40.00 mg, silicon dioxide colloid 3.75 mg, talc 3.10 mg, citric acid monohydrate 2.50 mg, calcium stearate 1.25 mg.

D16 mg solution

active substance: betahistine dihydrochloride 16.00 mg;

Excipients: cellulose microcrystalline 132,80 mg, lactose monohydrate 80.00 mg, silicon colloidal dioxide 7.50 mg, talc 6.20 mg, citric acid monohydrate 5.00 mg, calcium stearate 2.50 mg.

Description:

Round, flat-cylindrical tablets white or almost white, with a bevel (for a dosage of 8 mg) or with a facet and a risk (for a dosage of 16 mg).

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.

- Influence on gistaminergic 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 preclinical studies betagistin improves blood circulation in Vascular stria of the inner ear due to relaxation of precapillary sphincters vessels of the inner ear. It is also shown that betagistin enhances the flow of the head of the brain in humans.

- Facilitating the process of central vestibular compensation

Betagistin accelerates the recovery of vestibular function in animals after from extraneous 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.

Pharmacodynamic properties revealed in 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 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%. The time to reach the maximum concentration in the blood plasma - 1 h.

Metabolism

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

Excretion

85-90% is excreted by the kidneys in the form of 2-pyridylacetic acid for 24 hours. The excretion of betahistine and demethylbetahistine by the kidneys is negligible. Only a small part of betagistin and its metabolites are excreted by the intestine. The elimination half-life is 3-4 hours. The rate of induction of 8-48 mg of betahistine intake remains constant, indicating the linearity of the pharmacokinetics of betahistine.

Indications:

- LTreatment of Meniere's syndrome, characterized by dizziness (accompanied by nausea and vomiting), hearing loss and noise in the ears;

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

Contraindications:

- PAn 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:

- Iulcerous disease of the 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 useduring 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.

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

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

The minimum 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 correction of the dose is not required.

Side effects:

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

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; frequency unknown - vomiting, pain in the area of the gastrointestinal tract, bloating.

Co the central nervous system: often a headache.

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

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

Overdose:

Symptoms

Abdominal pain, nausea, drowsiness (after taking betagistin in doses up to 640 mg), seizures, cardiopulmonary complications (after taking betagistin in doses over 640 mg or in combination with other medicines).

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 inhibitors of monoamine oxidase (MAO), including selective inhibitors of MAO subtype B, inhibit the metabolism of betahistine. When applied simultaneously with MAO inhibitors, including selective inhibitors of MAO subtype B, betahistine may increase the concentration in plasma.

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 trials it is considered that the effect of betahistine on ability to drive and use machines is absent or negligible, since the effects of potentially influencing this ability were found.

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.

Form release / dosage:

Tablets, 8 mg and 16 mg.

Packaging:

10, 15 or 30 tablets in a planar cell packaging 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, 1 or 2 contour packs of 30 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:LSR-004681/07

Date of registration:11.12.2007 / 31.08.2015

Expiration Date:Unlimited

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

Manufacturer: & nbsp

VERTEKS, AO Russia

Representation: & nbspVERTEKS CJSC VERTEKS CJSC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betagistin (Betahistine)