Betaserk, tablets 24 mg 60 pcs

Pharmgroup:

The drug improving microcirculation of the labyrinth, used for pathology of the vestibular system.

Pharmic action:

Betaserk is a synthetic analog of histamine. It is an agonist of histamine H1 receptors of the inner ear vessels and an antagonist of histamine H3 receptors of the vestibular nuclei of the CNS. According to preclinical studies through relaxation of precapillary sphincters of the vessels of the inner ear improves blood flow in the vascular shelf of the inner ear.

Dose-dependently reduces the generation of action potentials in the neurons of the lateral and medial vestibular nuclei. It accelerates recovery of vestibular function after unilateral vestibular neurectomy, accelerating and facilitating central vestibular compensation (due to antagonism with histamine H3-receptors). Relieves symptoms in Meniere’s syndrome and vertigo.

Pharmacokinetics:

Betahistine is quickly and almost completely absorbed from the gastrointestinal tract when ingested. After absorption, the drug is rapidly and almost completely metabolized to form the inactive metabolite 2-pyridylacetic acid.

If the drug is taken at a dose of 8-48 mg, about 85% of the initial dose is detected in the urine as 2-pyridylacetic acid. Excretion of betahistine by the kidneys or through the intestine is insignificant. The excretion rate remains constant with oral administration of 8-48 mg of the drug, indicating linearity in the pharmacokinetics of betahistine, and suggesting that the metabolic pathway involved remains unsaturated.

When the drug is taken with food, the maximum blood concentration of the drug is lower than when taken on an empty stomach. However, the total absorption of betahistine is the same in both cases, indicating that food intake only slows the absorption of betahistine.

Indications

Active ingredient

Betahistine

Composition

1 tablet:

– betahistine dihydrochloride 24 mg

Supplementary substances:

Microcrystalline cellulose,

Mannitol (E421),

citric acid monohydrate,

silicon dioxide colloid,

talk.

How to take, the dosage

The drug is prescribed orally with meals. The dose should be adjusted individually depending on the response to treatment.

The dose for adults is 24-48 mg/day.

Betaserk® 8 mg: 1-2 tablets 3 times daily.

Betaserk® 16 mg: 1/2 to 1 tablet 3 times/day.

Betaserk® 24 mg: 1 tablet 2 times/day.

The 16 mg tablet and the 24 mg tablet can be divided into 2 equal parts. This is done by placing the tablet on a hard surface with the ridges facing upward and pressing it down with the thumb.

Sometimes improvement is seen only after a few weeks of treatment, and a sustained therapeutic effect is seen after several months of treatment. There is evidence that prescribing the drug at the beginning of the disease prevents progression and/or hearing loss in later stages.

While data from clinical studies are limited, extensive post-registration experience suggests that dose adjustments

Betaserk in elderly patients are not necessary.

Special clinical studies have not been performed in patients with renal and/or hepatic impairment, but post-registration experience suggests that no dose adjustment is required in this group of patients.

Interaction

In vivo studies to study the interaction with other drugs have not been conducted.

Based on in vitro data, it can be assumed that there is no inhibition of cytochrome P450 isoenzyme activity in vivo.

In vitro data showed inhibition of betahistine metabolism by drugs that inhibit MAOIs, including MAO subtype B (e.g., selegiline). Caution should be exercised when concomitant administration of betahistine and MAO inhibitors (including MAO-B).

Betahistine is a histamine analog, an interaction of betahistine with H₁-histamine receptor blockers could theoretically affect the effectiveness of one of these drugs.

The patient must tell the physician if he or she is currently or has recently taken any medications.

Special Instructions

Caution should be exercised in patients with a history of gastric or duodenal ulcer disease, in the second and third trimesters of pregnancy, and in children.

It should be taken into account that the desired clinical effect is achieved after several months of treatment.

In case of dyspeptic symptoms, betahistine is recommended to be taken with or after meals.

Synopsis

Tablets white or almost white, round, biconvex, with beveled edges, with a rib on one side and engraved “289” on both sides of the rib.

Contraindications

• Pheochromocytoma;
• High sensitivity to any of the ingredients of the drug.
• Betaserk® is not recommended for use in children under 18 years of age due to insufficient data on efficacy and safety.

Side effects

Frequent: nausea and dyspepsia; headache;

Frequent unknown: hypersensitivity reactions, including anaphylactic reaction, vomiting, gastrointestinal pain, bloating, angioedema, urticaria, itching, rash

Overdose

There have been several known cases of overdose of Betaserc.

Symptoms: mild to moderate nausea, drowsiness, abdominal pain have been observed in some patients after taking the drug in doses up to 640 mg.

More serious complications (seizures, cardiopulmonary complications) have been observed when betahistine is intentionally taken at higher doses, especially in combination with overdose of other medications.

Treatment: conduct symptomatic therapy.

Pregnancy use

Pregnancy.

The data available on the use of betahistine in pregnant women are insufficient. Animal studies have shown no direct or indirect reproductive toxicity. Betahistine should not be used during pregnancy unless clearly necessary.

Breastfeeding.

It is not known whether betahistine is excreted with breast milk in humans. Betahistine is excreted with breast milk in rats. Animal studies have been limited to the use of the drug at very high doses. Administration of the drug to the mother should be decided only after weighing the benefits of breastfeeding against the potential risks to the infant.

Fertility.

There has been no effect on fertility in animal studies (rats).

Similarities

Betaserk, Vestibo, Betahistine, Betahistine NW, Tagista, Vertran