Instructions Betahistine-KV tablets 16 mg No. 30
Composition
active ingredient: betahistine dihydrochloride;
1 tablet contains betahistine dihydrochloride in terms of 100% substance 16 mg;
Excipients: microcrystalline cellulose, mannitol (E 421), colloidal anhydrous silicon dioxide, talc, citric acid monohydrate, stearic acid.
Dosage form
Pills.
Main physicochemical properties:
16 mg or 24 mg tablets: flat-cylindrical tablets, with a bevel and a score, white or almost white in color. The presence of marbling on the surface of the tablets is allowed.
Pharmacotherapeutic group
Treatments for vestibular disorders.
ATX code N07C A01.
Pharmacological properties
Pharmacodynamics
The mechanism of action of betahistine is only partially understood. It is known that there are several plausible hypotheses that have been confirmed by studies conducted on animals and with the participation of humans.
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.
There is evidence of improved blood flow in the stria 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.
It is known that the pharmacodynamic properties of betahistine can 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 complete 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 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 drug administration and decreases with a half-life of about 3.5 hours.
Excretion. 2-pyridylacetic acid is rapidly excreted in the urine. When taking the drug in a dosage of 8-48 mg, about 85% of the initial dose is found in the urine. The excretion of betahistine by the kidneys or with feces is insignificant.
Linearity. The recovery rate remains constant over the oral administration of 8-48 mg of the drug, indicating linearity of the 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:
dizziness, sometimes accompanied by nausea and vomiting; hearing loss (hearing loss); tinnitus.
Symptomatic treatment of vestibular vertigo of various origins.
Contraindication
Hypersensitivity to any of the components of the drug. Pheochromocytoma.
Interaction with other medicinal products and other types of interactions
In vitro data indicate that betahistine metabolism is inhibited 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 selective MAO subtype B).
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.
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 core 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. Betahistine is known to have no or negligible influence on the ability to drive and use machines.
Use during pregnancy or breastfeeding
Pregnancy: There are no adequate data from the use of betahistine in pregnant women.
Animal studies are insufficient to assess the effects on pregnancy, embryonal/fetal development, parturition and postnatal development. The potential risk to humans is unknown. Betahistine should not be used during pregnancy unless clearly necessary.
Breastfeeding. It is not known whether betahistine is excreted in human milk. Animal studies on the excretion of betahistine in milk have not been conducted. The benefit of the drug to the mother should be weighed against the benefits of breastfeeding and the potential risk to the child.
Method of administration and doses
The daily dose for adults is 24-48 mg, evenly distributed throughout the day.
| 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 two to three weeks of treatment. The best results are sometimes achieved when taking the drug for several months. There is evidence that prescribing treatment early in the disease prevents its progression and/or hearing loss in the later stages.
Elderly patients
Post-marketing experience suggests that dose adjustment is not necessary for this patient population.
Kidney failure
Post-marketing experience suggests that no dose adjustment is necessary.
Liver failure
Post-marketing experience suggests that no dose adjustment is necessary.
Children
Due to insufficient data on the safety and efficacy of this medicinal product, 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 administration of increased doses of betahistine, especially in combination with overdose of other drugs.
Treatment of overdose should include standard supportive measures.
Adverse reactions
Gastrointestinal: nausea and dyspepsia, 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.
From the nervous system: headache.
Immune system disorders: Hypersensitivity reactions, e.g. anaphylaxis.
Skin and subcutaneous tissue disorders: Hypersensitivity reactions of the skin and subcutaneous tissue, including angioedema, rash, pruritus and urticaria, have been observed.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Vacation category
According to the recipe.
Producer
JSC "KYIV VITAMIN FACTORY".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
