Betahistin-VERTEX
Latin name: Betahistine-VERTEX
ATX code: N07CA01
Active ingredient: betahistine (Betahistine)
Manufacturer: JSC "VERTEX" (Russia)
Description and photo update: 2020-11-06
Betahistin-VERTEX is a drug with a histamine-like effect, prescribed for the treatment of diseases of the vestibular apparatus.
Release form and composition
The drug is produced in the form of tablets: almost white or white, flat-cylindrical, round; 8 mg tablets - chamfered, 16 and 24 mg tablets - chamfered and scored (dosage 8 and 16 mg: in a blister strip of 10, 15, 20 or 30 pcs., in a cardboard box 1, 2, 3, 5 or 6 packs of 10 pcs., 2 or 4 packs of 15 pcs., 1, 2 or 3 packs of 20 pcs., 1 or 2 packs of 30 pcs.; Dosage 24 mg: in a blister strip of 10 or 15 pcs., in a cardboard box 1, 2, 3, 5 or 6 packs of 10 pcs., 2 or 4 packs of 15 pcs. Each cardboard box contains instructions for the use of Betahistin-VERTEX).
1 tablet contains:
- active substance: betahistine dihydrochloride - 8, 16 or 24 mg;
- additional components: colloidal silicon dioxide, microcrystalline cellulose, citric acid monohydrate, lactose monohydrate, calcium stearate, talc.
Pharmacological properties
Pharmacodynamics
The mechanism of action of betahistine is not fully understood. There are several scientific hypotheses presented below, which have been confirmed in the process of preclinical and clinical studies:
- Effects on the histaminergic system: betahistine is one of the partial agonists of H 1 -histamine and antagonists of H 3 -histamine receptors (H 3 -receptors) of the vestibular nuclei of the central nervous system (CNS) and exhibits insignificant activity towards H 2 -histamine receptors (H 2 -receptors). The drug promotes an increase in the metabolism of histamine and its release as a result of inhibition of presynaptic H 3 receptors and a decrease in the number of H 3 receptors.
- Increased blood flow in the cochlear area and throughout the brain: in animal studies, an improvement in blood circulation in the vascular stria within the cochlear duct has been recorded, due to a relaxing effect on the precapillary sphincters of the inner ear vessels. It has also been found that the drug increases cerebral blood flow in humans.
- Facilitating the process of central vestibular compensation: in animals after unilateral vestibular neuroectomy, the drug activated the restoration of vestibular function, facilitating, as a result of antagonism with H 3 receptors, acceleration and facilitation of central vestibular compensation. In humans, after neuroectomy, the use of betahistine also leads to a decrease in the recovery period of vestibular function.
- Excitation of neurons in the vestibular nuclei: the drug dose-dependently suppresses the generation of action potentials in the neurons of the vestibular nuclei, both in the medial and lateral ones. According to the data of preclinical studies, betahistine, due to its pharmacodynamic properties, demonstrated a positive therapeutic effect on the functions of the vestibular system of animals. The effectiveness of the remedy was established in patients with Meniere's syndrome and vestibular dizziness, which was manifested by a decrease in the frequency and severity of dizziness.
Pharmacokinetics
After oral administration, betahistine is fully absorbed in the gastrointestinal tract (GIT). Simultaneous intake with food reduces the absorption of the active substance, but at the same time its total absorption is the same when taken on an empty stomach and with food.
The agent binds to blood plasma proteins by less than 5%, the peak plasma concentration is recorded 1 hour after administration. The metabolic transformation of the drug quite quickly and almost completely proceeds in the liver with the formation of dimethylbetahistine and 2-pyridylacetic acid (the main derivative), both metabolites are pharmacologically inactive.
For 24 hours in the form of 2-pyridylacetic acid, 85–90% of the substance is eliminated by the kidneys. Betahistine and dimethylbetahistine are insignificantly subject to renal elimination. Only a small proportion of the basic substance and its derivatives are excreted by the intestines. The half-life is 3-4 hours. With oral administration of betahistine at a dose of 8-48 mg, the rate of excretion remains constant, which indicates the linearity of the drug's pharmacokinetics.
Indications for use
- vestibular dizziness (vertigo) of various origins - symptomatic therapy and prevention;
- Meniere's syndrome, characterized by dizziness (with nausea and vomiting), tinnitus and hearing loss - therapy.
Contraindications
Absolute:
- lactase deficiency, glucose-galactose malabsorption, lactose intolerance;
- pheochromocytoma;
- pregnancy and lactation;
- age up to 18 years;
- hypersensitivity to any component of Betahistin-VERTEX tablets.
Relative (therapy should be performed with great care):
- bronchial asthma;
- peptic ulcer and 12 duodenal ulcer (including history).
Betahistin-VERTEX, instructions for use: method and dosage
Betahistine-VERTEX is taken orally. The tablets should be swallowed whole, without chewing, and washed down with a little water.
The daily doses of the drug can vary from 24 to 48 mg and depend on the dosage:
- 8 mg: 3 times / day, 1-2 pcs.;
- 16 mg: 3 times / day, ½ – 1 pc.;
- 24 mg: 2 times / day, 1 pc.
The maximum daily dose should not exceed 48 mg. The doctor sets the dose of the drug and the course individually, taking into account the patient's response to therapy. The course of treatment is long.
In some cases, improvement is noted a few weeks after the start of Betahistine-VERTEX. Sometimes the best results are observed after several months of continuous therapy.
Elderly persons, as well as patients with impaired renal and / or liver function, do not need to adjust the dose of Betahistine-VERTEX.
Side effects
- skin: the frequency has not been established - itching, redness, skin rash, urticaria;
- CNS: often - headache;
- immune system: frequency not established - hypersensitivity reactions, including angioedema, anaphylactic reactions;
- digestive system: often - dyspepsia, nausea; frequency not established - bloating, pain in the gastrointestinal tract, vomiting.
Overdose
The main symptoms of Betahistine-VERTEX overdose, depending on the dose taken, include:
- doses below 640 mg: drowsiness, nausea, abdominal pain;
- doses above 640 mg (or in combination with other drugs): convulsions, complications from the heart and lungs.
If intoxication is suspected, gastric lavage is performed, activated carbon is prescribed and symptomatic treatment is prescribed.
special instructions
Basically, the therapeutic effect of betahistine is recorded already at the beginning of the course, but sometimes it can be observed gradually over several weeks of admission. In some cases, a stable effect can be achieved after several months of therapy.
In the presence of arterial hypotension, the use of Betahistin-VERTEX tablets is required with caution and under medical supervision.
Influence on the ability to drive vehicles and complex mechanisms
According to the results of clinical studies, betahistine has no or insignificant effect on the ability to drive vehicles or work with complex equipment. However, the drug is recommended for the symptomatic treatment of vestibular dizziness and the treatment of Meniere's syndrome, characterized by the presence of tinnitus, hearing loss and dizziness. These conditions can negatively affect the ability to concentrate and the speed of psychomotor reactions.
Application during pregnancy and lactation
Breastfeeding and pregnant women are not prescribed Betahistin-VERTEX due to insufficient data on the safety of its administration during pregnancy and lactation. If pregnancy occurs during the period of therapy, the drug must be discontinued.
It is unknown whether the agent is excreted in breast milk. In the case when the use of betahistine is necessary during lactation, the child should be transferred to artificial feeding.
Pediatric use
For children and adolescents under 18 years of age, drug therapy is contraindicated, since the safety and effectiveness of its use in this category of patients have not been established.
Drug interactions
Studies of the interaction of betahistine with other drugs / drugs in vivo have not been conducted. Considering the in vitro data, the drug presumably lacks the ability to inhibit the activity of cytochrome P 450 isoenzymes.
In the case of combined use with blockers of H 1 -histamine receptors, a decrease in the therapeutic effect of betahistine may be observed.
In vitro studies have shown that monoamine oxidase inhibitors (MAOIs), including selective MAOIs of subtype B, suppress the metabolism of the drug, which can lead to an increase in its plasma concentration.
Analogs
Betagistin-VERTEX analogs are Betagistin, Betaver, Betagistin Medisorb, Betagistin Canon, Betaserk, Betagistin-Akrikhin, Vestikap, Betacsentrin, Westinorm-NEO, Tagista.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a place protected from light and out of reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Betagistine-VERTEX
Reviews about Betahistine-VERTEX are mostly positive. Patients note that the drug relieves dizziness, and also prevents their development, relieves tinnitus, and improves general condition. However, in order to achieve the desired result, many advise to carry out a long course of therapy, since Betahistine-VERTEX has a cumulative effect and its effect manifests itself in everyone in different ways.
In some cases, they indicate the absence of a stable positive result after treatment, since only temporary improvement is recorded. Sometimes there are complaints about the development of side effects from the gastrointestinal tract.
Price for Betagistin-VERTEX in pharmacies
The average price for Betagistin-VERTEX, in tablet form, is:
- dosage of 8 mg - 140 rubles. for 30 pcs.;
- dosage 16 mg - 240 rubles. for 30 pcs.;
- dosage 24 mg - 270 rubles. for 20 pcs. and 550 rubles. for 60 pcs.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
