Vergostin

Vergostin is a medicine for the treatment of NS; used in vestibular disorders.

Indications Vergostina

It is used in people with Meniere's syndrome, manifested by such signs:

• dizziness, with which sometimes vomiting occurs along with nausea;
• hearing impairment ( hearing loss );
• ear noise

Also assigned to eliminate the manifestations of dizziness associated with the vestibular apparatus and having different etiologies.

Release form

The release of a therapeutic agent is implemented in tablet form, 10 pieces per cell package; in a pack - 3 packs.

Pharmacodynamics

The principle of the therapeutic effect of betahistine has not been fully investigated. The substance potentiates the vascular blood circulation in the region of the inner ear - mainly by relaxing the strained precapillary sphincters inside the microcirculation of the inner-ear system.

It was revealed that betahistine has a slight agonistic effect on the H1-terminations and a powerful antagonistic effect on histamine H3-terminations within the autonomous NA and CNS. At the same time, betahistine has a moderating effect, depending on the size of the dosage, relative to the generation of maximum potentials associated with neurons located inside the vestibular nuclei (among them medial, and at the same time lateral).

The drug increases the speed of recovery of the ongoing vestibular activity after performing 1-sided neurectomy, simplifying and accelerating the developing vestibular compensation, which has a central character. This effect is developed by the potentiation of the processes of regulation of histamine release along with the exchange, and then realized through the antagonism of H3-terminations.

When all these effects are combined, a positive medical effect of the drug develops in the case of Meniere's syndrome, as well as dizziness associated with the vestibular apparatus, which has a different etiology.

The drug potentiates the release and metabolism of histamine, blocking the activity of presynaptic H3-endings, due to which their sensitivity is weakened. This effect in relation to the histaminergic system explains the high efficacy of drugs in the treatment of vestibular disorders and dizziness.

Pharmacokinetics

Betahistine at high speed is fully absorbed when taken orally. Excretion occurs together with the urine (90%) in the form of 2-pyridylacetic acid 24 hours after taking the pill. The substance is not determined in unchanged condition.

Tests using the radioactively labeled component have demonstrated that its half-life is 3-4 hours, and urine half-life is 3-5 hours.

Dosing and administration

During the day, the use of 24-48 mg of a substance is prescribed, which should be distributed into several uniform techniques:

• volume 8 mg - 1-2 tablets 3 times a day;
• 16 mg - 0.5-1 tablet 3 times a day;
• 24 mg - 1 tablet 2 times a day.

The portion size is selected for each patient separately, taking into account the impact on him.

The weakening of the signs of pathology is sometimes noted only after 2-3 weeks of therapy.

The maximum effect from the use of Vergostin can be achieved after its reception in a period of several months. There is information confirming that at the beginning of therapy in the early stages of the disease, its deterioration or complete loss of hearing in the later stages is prevented.

[2]

Use Vergostina during pregnancy

You can not prescribe medication during lactation or pregnancy.

Contraindications

Among the contraindications:

• the presence of strong sensitivity to any of the elements of the drug;
• pheochromocytoma.

Side effects Vergostina

The introduction of the drug can lead to some side effects:

• Disorders in the digestive tract: dyspepsia or nausea often appear. Mild abnormalities in gastric activity (for example, flatulence, vomiting and pain in the gastrointestinal region), which usually disappear, can be noted if the dosage of the drug is reduced or taken with food;
• NS dysfunction: often develop headaches;
• immune lesions: manifestations of intolerance, such as anaphylaxis; 
• problems with the subcutaneous layer and the epidermis: symptoms of hypersensitivity, including urticaria with rashes, angioedema, and itching.

[1]

Overdose

In the case of drug poisoning (use of a portion up to 0.64 g), the development of light or moderate symptoms (pain in the abdominal area, nausea and drowsiness) was noted. In case of intentional use of higher dosages, more severe disorders (complications affecting cardiopulmonary function and convulsions) developed, especially when combined with intoxication with other drugs.

Conventional maintenance procedures are performed to treat the disorders.

Interactions with other drugs

In vivo testing, in which interactions with other drugs were investigated, were not performed. Information from in vitro tests suggests that the drug does not slow down the activity of cytochrome P450 enzymes in the in vivo state.

Information obtained in vitro demonstrates that metabolic processes of betahistine are suppressed by substances slowing down the activity of the MAO element (this also includes the subtype B-MAO, such as selegilin). Vergostin should be very carefully combined with IMAO preparations.

Based on the fact that betahistine is included in the group of analogs of the histamine component, when a drug is combined with antihistamine drugs, in theory, the effect on the therapeutic efficacy of any of these drugs can develop.

[3], [4]

Storage conditions

Vergostin must be kept in a place that is closed to the penetration of small children. Temperature values are in the range of 25 ° С.

Shelf life

Vergostin can be administered for a 24-month period from the time the therapeutic substance is manufactured.

Application for children

Vergostin is not used in pediatrics (persons under the age of 18), because for this group of patients there is little information regarding drug efficacy and safety.

[5]

Analogs

Antagonists of drugs are considered drugs Betaserk, Betaver, Tagista with Vestikapom and Vestibo.