Instructions Betaserc tablets 16 mg blister No. 30
Composition
active ingredient: betahistine dihydrochloride;
1 tablet contains betahistine dihydrochloride 8 mg, 16 mg or 24 mg;
excipients: microcrystalline cellulose, mannitol (E 421), citric acid monohydrate, colloidal anhydrous silicon dioxide, talc.
Dosage form
Pills.
Main physicochemical properties:
8 mg tablets: round, flat, white or almost white tablets with beveled edges, marked "256" on one side of the tablet; diameter approximately 7 mm and tablet weight approximately 125 mg.
16 mg tablets: round, biconvex, scored, white or almost white tablets with beveled edges, scored on one side and marked "267" on both sides of the score; diameter approximately 8.5 mm and weight approximately 250 mg; the tablet can be divided into two equal doses.
24 mg tablets: round, biconvex, scored, white or almost white tablets with beveled edges, scored on one side and marked "289" on both sides of the score; diameter approximately 10 mm and tablet weight approximately 375 mg; the score is intended only to facilitate breaking the tablet for easier swallowing and is not intended to divide the tablet into two equal doses.
Pharmacotherapeutic group
Agents for the treatment of vestibular disorders. Betahistine. ATX code N07C A01.
Pharmacological properties
Pharmacodynamics
The mechanism of action of betahistine is only partially understood. There are several plausible hypotheses that have been supported by animal and human studies.
The effect of betahistine on the histaminergic system.
Betahistine has been shown to have partial agonist activity at H1 receptors and antagonist activity at histamine H3 receptors in nervous tissue, with little activity at histamine H2 receptors. Betahistine increases histamine metabolism and release by blocking presynaptic H3 receptors and inducing a process of downregulation of the corresponding H3 receptors.
Betahistine can increase blood flow in the cochlear area, as well as throughout the brain.
Pharmacological studies in animals have shown an improvement in blood flow in the striae vascularis of the inner ear, possibly by relaxing precapillary sphincters in the inner ear microcirculation system. Betahistine has also been shown to increase cerebral blood flow in humans.
Betahistine promotes vestibular compensation.
Betahistine accelerates the recovery of vestibular function after unilateral neurectomy in animals by stimulating and promoting the process of central vestibular compensation. This effect is characterized by increased regulation of histamine metabolism and release and is realized as a result of H3-receptor antagonism. In humans, treatment with betahistine also reduced the time to recovery of vestibular function after neurectomy.
Betahistine alters the activity of neurons in the vestibular nuclei.
It was also found that betahistine has a dose-dependent inhibitory effect on the generation of spike potentials in neurons of the lateral and medial vestibular nuclei.
The pharmacodynamic properties of betahistine, as shown in animals, may provide a positive therapeutic effect of the drug in the vestibular system.
The effectiveness of betahistine has been shown in studies in patients with vestibular vertigo and Ménière's disease, as demonstrated by a reduction in the severity and frequency of vertigo attacks.
Pharmacokinetics
Absorption.
When administered orally, betahistine is rapidly and almost completely absorbed from all parts of the gastrointestinal tract. After absorption, the drug is rapidly and almost completely metabolized to form the metabolite 2-pyridylacetic acid. The concentration of betahistine in blood plasma is very low. Therefore, all pharmacokinetic analyses are carried out by measuring the concentration of the metabolite 2-pyridylacetic acid in plasma and urine.
When the drug is taken with food, the maximum concentration (Cmax) of the drug is lower than when taken on an empty stomach. At the same time, the total absorption of betahistine is identical in both cases, which indicates that food intake only slows down the absorption process of the drug.
Distribution.
The percentage of betahistine bound to blood plasma proteins is less than 5%.
Biotransformation.
After absorption, betahistine is rapidly and almost completely metabolized to 2-pyridylacetic acid (which has no pharmacological activity).
After oral administration of betahistine, the concentration of 2-pyridylacetic acid in blood plasma (and urine) reaches its maximum 1 hour after administration and decreases with a half-life of about 3.5 hours.
Breeding.
2-Pyridylacetic acid is rapidly excreted in the urine. When taking the drug in a dose of 8-48 mg, about 85% of the initial dose is found in the urine. Excretion of betahistine by the kidneys or with feces is insignificant.
Linearity.
The recovery rate remains constant over the oral dose range of 8–48 mg, indicating linear pharmacokinetics of betahistine and suggesting that the metabolic pathway involved is non-saturable.
Indication
Meniere's disease and syndrome, which are characterized by three main symptoms:
– hearing loss (hearing loss);
– tinnitus.
Symptomatic treatment of vestibular vertigo of various origins.
Contraindication
Hypersensitivity to the active substance or to any of the excipients of the drug.
Pheochromocytoma.
Interaction with other medicinal products and other types of interactions
In vivo studies to investigate interactions with other medicinal products have not been conducted. Based on in vitro data, inhibition of cytochrome P450 enzyme activity in vivo is not expected.
In vitro data indicate inhibition of betahistine metabolism by drugs that inhibit monoamine oxidase (MAO) activity, including MAO subtype B (e.g. selegiline). Caution is recommended when betahistine is used concomitantly with MAO inhibitors (including B-selective MAO inhibitors).
Since betahistine is a histamine analogue, the interaction of betahistine with antihistamines could theoretically affect the effectiveness of one of these drugs.
Application features
During treatment with the drug, it is necessary to carefully monitor the condition of patients with bronchial asthma and/or a history of gastric and duodenal ulcers.
Use during pregnancy or breastfeeding
Pregnancy: There are no adequate data from the use of betahistine in pregnant women.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity at doses similar to those used in clinical practice. Betahistine should not be used during pregnancy unless clearly necessary.
Breastfeeding. It is not known whether betahistine is excreted in human milk. Betahistine is excreted in rat milk. Effects observed after delivery in animal studies were only observed at very high doses. The benefit of the drug to the mother should be weighed against the benefits of breastfeeding and the potential risk to the child.
Fertility: Studies in rats have shown no effect on fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
Betahistine is indicated for the treatment of Ménière's syndrome, characterized by a triad of main symptoms: dizziness, hearing loss, tinnitus, and for the symptomatic treatment of vestibular vertigo. Both conditions may adversely affect the ability to drive and use machines. According to clinical studies investigating the effect of the drug on the ability to drive and use machines, betahistine had no or negligible influence on this ability.
Method of administration and doses
The daily dose for adults is 24–48 mg, which is evenly distributed throughout the day. The tablets should be swallowed with water.
| 8 mg tablets | 16 mg tablets | 24 mg tablets |
1–2 tablets 3 times a day | ½–1 tablet 3 times a day | 1 tablet 2 times a day |
The dose should be adjusted individually, depending on the effect. A reduction in symptoms is sometimes observed only after several weeks of treatment. The best results are sometimes achieved when the drug is taken for several months. According to some reports, prescribing treatment early in the disease prevents its progression or hearing loss in the later stages.
Betaserc® can be used regardless of meals. Minor gastrointestinal disturbances may occur during administration of the drug (listed in the section "Adverse reactions"), which can be eliminated by taking the drug with food.
Elderly patients
Although clinical trial data in this patient group are currently limited, extensive post-marketing experience suggests that dose adjustment is not necessary for elderly patients.
Kidney failure
No specific clinical trials have been conducted in this patient group, but based on post-marketing experience, no dose adjustment is required.
Liver failure
No specific clinical trials have been conducted in this patient group, but based on post-marketing experience, no dose adjustment is required.
Children
Due to insufficient data on the safety and efficacy of Betaserc®, it is not recommended for use in children (under 18 years of age).
Overdose
Several cases of overdose of the drug are known. Some patients experienced mild to moderate symptoms (nausea, drowsiness, abdominal pain) after taking the drug in doses up to 640 mg. More serious complications (convulsions, cardiopulmonary complications) were observed with intentional intake of increased doses of betahistine, especially in combination with overdose of other drugs.
Overdose treatment
Treatment of overdose should include standard supportive measures.
Adverse reactions
The following adverse reactions were observed in patients taking Betaserc® during placebo-controlled studies with the following frequencies: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000).
Gastrointestinal tract
Common: nausea and dyspepsia.
From the nervous system
Common: headache.
In addition to cases reported during clinical trials, the following adverse reactions have been reported spontaneously during post-marketing use and from the scientific literature. The frequency cannot be estimated from the available data and is therefore classified as unknown.
On the part of the immune system
Hypersensitivity reactions, such as anaphylaxis.
Gastrointestinal tract
Complaints of minor stomach upset (vomiting, gastrointestinal pain, bloating and flatulence). These side effects usually disappear when the drug is taken with food or after reducing the dose.
Skin and subcutaneous tissue disorders
Hypersensitivity reactions of the skin and subcutaneous tissue, including angioedema, urticaria, rash and pruritus, have been observed.
Expiration date
3 years.
Storage conditions
Does not require any special storage conditions. Keep out of the reach of children.
Packaging
8 mg tablets: 15 tablets in a blister, 2 blisters in a cardboard box; 30 tablets in a blister, 1 blister in a cardboard box; 25 tablets in a blister, 4 blisters in a cardboard box;
16 mg tablets: 15 or 21 tablets in a blister, 2 blisters in a cardboard box; 20 tablets in a blister, 3 blisters in a cardboard box;
24 mg tablets: 10 tablets in a blister, 1 or 5 blisters in a cardboard box; 20 tablets in a blister, 1, 3 or 5 blisters in a cardboard box; 25 tablets in a blister, 2 or 4 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Mylan Laboratories SAS, France.
Location of the manufacturer and address of its place of business
Route de Belleville, Lieu dit Maillard, 01400, Chatillon-sur-Chalaronne, France.
