Vertran, 24 mg tablets 30 pcs

Pharmacodynamics

An agonist of H1-histamine receptors of the inner ear vessels and an antagonist of H3-histamine receptors of the vestibular nuclei of the central nervous system (CNS).

Does not affect H2-histamine receptors, which improves blood flow in the vasculature of the inner ear through a relaxing effect on the pre-capillary sphincters of the cochlea and labyrinth. Relieves symptoms in Meniere’s syndrome and vertigo.

Pharmacokinetics

In oral administration, it is rapidly and completely absorbed in the gastrointestinal tract. Binding to plasma proteins is low (less than 5%). The maximum concentration in plasma (Cmax) is reached after 1 hour.

When the drug is taken with food the maximum concentration of the drug in blood 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 absorption of betahistine.

It is metabolized in the liver to form the inactive metabolite 2-pyridylacetic acid. Almost completely (90.7%) is excreted by the kidneys as a metabolite (2-pyridylacetic acid) within 24 hours. The elimination half-life is 3-4 hours. The elimination rate remains constant, indicating the linearity of the pharmacokinetics of betahistine.

Indications

Meniere’s syndrome, characterized by the following main symptoms:
dizziness (accompanied by nausea/vomiting)
hearing loss
tinnitus
Symptomatic treatment and prevention of vestibular dizziness (vertigo) of various etiologies.

Pharmacological effect

Pharmacodynamics

An agonist of H1-histamine receptors in the vessels of the inner ear and an antagonist of H3-histamine receptors of the vestibular nuclei of the central nervous system (CNS).

It does not affect H2-histamine receptors, which improves blood circulation in the vascular stria of the inner ear due to its relaxing effect on the precapillary sphincters of the cochlea and labyrinth. Relieves symptoms of Meniere’s syndrome and vertigo.

Pharmacokinetics

When taken orally, it is quickly and completely absorbed from the gastrointestinal tract. Plasma protein binding is low (less than 5%). The maximum concentration in blood plasma (Cmax) is achieved after 1 hour.

When taking the drug with food, the maximum concentration of the drug in the blood 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 down the absorption of betahistine.

Metabolized in the liver to form an inactive metabolite, 2-pyridylacetic acid. Almost completely (90.7%) is excreted by the kidneys in the form of a metabolite (2-pyridylacetic acid) within 24 hours. The half-life is 3-4 hours. The elimination rate remains constant, indicating the linearity of the pharmacokinetics of betahistine.

Special instructions

Impact on the ability to drive vehicles and machinery

Based on the results of clinical studies, it is believed that the effect of betahistine on the ability to drive a car and other mechanisms is absent or insignificant, since no effects potentially affecting this ability were detected.

Active ingredient

Betahistine

Composition

1 tablet contains:

active substance:
betahistine dihydrochloride 8 mg, 16 mg or 24 mg;
excipients:
microcrystalline cellulose – 151.810 / 303.619 / 455.430 mg,
mannitol – 54.040 / 108.081 / 162.120 mg,
citric acid monohydrate – 4.70 / 9.40 / 14.10 mg,
colloidal silicon dioxide – 4.70 / 9.40 / 14.10 mg,
talc – 11.75 / 23.50 / 35.25 mg.

Pregnancy

Taking betahistine during pregnancy and lactation is contraindicated, since there is insufficient data on its safety during pregnancy and breastfeeding.

Contraindications

Hypersensitivity to any of the components of the drug. Due to insufficient data on effectiveness and safety: pregnancy and lactation; age up to 18 years.

With caution

Betahistine should be prescribed with caution when treating patients with a history of gastric and duodenal ulcers. Patients with pheochromocytoma and bronchial asthma should be regularly monitored by a doctor during treatment.

Side Effects

From the gastrointestinal tract: often (from >1/100 to <1/10) - nausea and dyspepsia.From the nervous system: often (from >1/100 to <1/10) - headache.In addition to these effects identified in clinical studies, the following side effects have been reported during post-marketing use and in the scientific literature (the available data are insufficient to estimate their frequency):From the gastrointestinal tract: moderate disorders such as vomiting, pain in the gastrointestinal tract, bloating. As a rule, these effects disappear if the drug is taken simultaneously with food or after a dose reduction.From the skin and subcutaneous fat: angioedema, urticaria, itching and rash.On the part of the immune system: hypersensitivity reaction, including anaphylactic reactions have been reported.

Interaction

In vivo studies aimed at studying interactions with other drugs have not been conducted. Based on in vitro data, it can be assumed that there is no inhibition of the activity of cytochrome P450 isoenzymes.

When used simultaneously with H1-histamine receptor blockers, the therapeutic effect of betahistine may be reduced.

Overdose

Symptoms: after taking the drug in doses up to 640 mg, mild to moderate symptoms (nausea, drowsiness, abdominal pain) may be observed.

More serious complications (eg, seizures, cardiopulmonary complications) may occur when taking higher doses of betahistine, especially in combination with other drugs.

Treatment: symptomatic.

Patients with pheochromocytoma should use the drug under medical supervision.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

3 years.

Manufacturer

Belupo, medicines and cosmetics d.d., Croatia