Betaserk - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 242.0 mg, mannitol (E421) 75.0 mg, citric acid monohydrate 7.5 mg, silicon dioxide colloid 7.5 mg, talc 19.0 mg.

Description:

Round, biconvex tablets, white or almost white, with bevelled edges, with a risk on one side of the tablet and engraved "289" on both sides of the risks.

Pharmacotherapeutic group:Histamine drug

ATX: & nbsp

N.07.C.A.01 Betagistin

Pharmacodynamics:

The mechanism of action of betagistin is known only in part. There are several possible hypotheses, confirmed by preclinical and clinical data:

- Influence on the histaminergic system.

Partial agonist H₁-gistaminovyh and antagonist H₃-gistaminovyh receptors of vestibular nuclei of the central nervous system, has insignificant activity in relation to H₂receptors. Betagistin increases histamine metabolism and its release by blocking presynaptic H₃-receptors and decrease in the number of H₃receptors.

- Increased blood flow of the cochlear region, as well as the entire brain.

According to preclinical studies betagistin improves blood circulation in the vascular stria of the inner ear by relaxing precapillary sphincters of the vessels of the inner ear. It is also shown that betagistin increases the blood flow of the brain in humans.

- Facilitating the process of central vestibular compensation. Betagistin accelerates the restoration of vestibular function in animals after a one-sided vestibular neurrectomy, accelerating and facilitating central vestibular compensation due to antagonism with H₃-histamine receptors.

The recovery time after vestibular neurectomy in humans in the treatment with betahistine is also reduced.

- Excitation of neurons in the vestibular nuclei.

It dose-dependently reduces the generation of action potentials in the neurons of the lateral and medial vestibular nuclei.

Pharmacodynamic properties found on animals provide a positive therapeutic effect of betahistine in the vestibular system.

The efficacy of betahistine was demonstrated in patients with vestibular dizziness and Menier's syndrome, which was manifested by a decrease in severity and frequency dizziness.

Pharmacokinetics:

Suction

When taken orally betagistin quickly and almost completely absorbed in the gastrointestinal tract. After absorption, the drug is quickly and almost completely metabolized with oby metabolizing the metabolite of 2-pyridylacetic acid. The concentration of betagistin in the blood plasma is very low. Thus, pharmacokinetic analyzes are based on measuring the concentration of the metabolite of 2-pyridylacetic acid in plasma and urine.

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

Distribution

Binding of betahistine to plasma proteins is less than 5%.

Biotransformation

After suction betagistin quickly and almost completely metabolized to form a metabolite of 2-pyridylacetic acid (which does not have pharmacological activity).The maximum concentration of 2-pyridylacetic acid in blood plasma (or urine) is reached in an hour after administration. Period half-life approximately 3.5 hours.

Excretion

2-pyridylacetic acid is rapidly excreted in the urine. When taking the drug at a dose of 8-48 mg, about 85% of the initial dose is found in the urine. The excretion of betagistin by the kidneys or through the intestine is negligible.

Linearity

The rate of excretion remains constant with oral intake of 8-48 mg of the drug, indicating the linearity of the pharmacokinetics of betahistine, and suggests that the involved.

Indications:

Meniere's syndrome, characterized by the following main symptoms:

- dizziness (accompanied by nausea / vomiting);

- Hearing loss (hearing loss);

- noise in ears.

Symptomatic treatment of vestibular vertigo.

Contraindications:

- Feochromocytoma;

- hypersensitivity to any of the components of the drug.

- Betaserk® is not recommended for use in children under the age of 18 due to inadequate data on efficacy and safety.

Carefully:

Patients with bronchial asthma, peptic ulcer and / or The duodenum requires careful observation during the treatment period.

Pregnancy and lactation:

Pregnancy

There are not enough available data on the use of betagistin by pregnant women.

The potential risk to humans is unknown. The use of betagistin during pregnancy is allowed if the benefit from the use for the mother exceeds the potential risk to the fetus.

Lactation

It is not known whether betagistin with breast milk. Do not take the drug during breastfeeding. The question of prescribing a medicinal product of the mother should be taken only after comparing the benefits of breastfeeding with the potential risk for an infant.

Dosing and Administration:

Inside, with food.

The dose of the drug for adults is 48 mg of betahistine per day.

Betaserk® 24 mg should be taken 1 tablet 2 times a day.

The tablet can be divided into two equal parts, as shown in Figure 1. Place the tablet on a hard surface with a risk upward and press it down with your thumb.

The dose should be selected individually depending on the response to treatment. Improvement is sometimes observed only after several weeks of treatment.The best results are sometimes achieved after several months of treatment. There is evidence that the appointment of treatment at the onset of the disease prevents its progression and / or hearing loss at later stages.

Elderly age

Despite the limited data from clinical studies, extensive post-registration experience suggests that dose adjustment in this group of patients is not required.

Patients with renal / hepatic insufficiency

Special clinical studies in this group, patients were not carried out, however, post-registration experience gives grounds to assume that dose adjustment in this group of patients is not required.

Side effects:

If you notice any side effects not mentioned in this manual, or if any side effect has taken a serious nature, please notify your health care provider.

Disorders from the gastrointestinal tract:

Often (from ≥1 / 100 to <1/10): nausea and indigestion.

Disturbances from the nervous system:

Often (from ≥1 / 100 to <1/10): headache.

In addition to these effects, identified during clinical trials, in the process of post-registration and in the scientific literature, the following undesirable effects. The available data are insufficient to estimate their frequency.

Immune system disorders: hypersensitivity reaction, including anaphylactic reaction.

Disorders from the gastrointestinal tract: moderate disorders such as vomiting, gastrointestinal pain, bloating. These effects usually disappear after taking the drug at the same time as food or after lowering the dose.

Disturbances from the skin and subcutaneous tissues: hypersensitivity reactions, especially angioedema, urticaria, pruritus and rash.

Overdose:

There are several cases of drug overdose. Some patients experienced mild to moderate symptoms (nausea, drowsiness, abdominal pain) after taking the drug at doses up to 640 mg. More serious complications (convulsions, cardiopulmonary complications) were observed with the deliberate use of elevated doses of betagistin, especially in combination with overdose of other drugs.

Symptomatic treatment is recommended.

Interaction:

If you have taken other medicines at this time or in the recent past, including without a doctor's prescription, please inform your doctor.

Research in vivo, aimed at studying the interaction with other medicinal products, were not conducted. Based on the data in vitro, it can be assumed that there is no inhibition of the activity of cytochrome P450 isoenzymes in vivo.

Data in vitro showed inhibition of beta-histidine metabolism by drugs that inhibit monoamine oxidase (MAO), including MAO subtype B (for example, selegiline). Caution should be exercised while concomitant administration of betagistin and MAO inhibitors (including MAO-B).

Betagistin is an analog of histamine, the interaction of betahistine with blockers H₁-gistaminovyh receptors theoretically can affect the effectiveness of one of the of these medicines.

Special instructions:The risk on the pill is intended to break the tablet in order to facilitate its swallowing and is not intended to be divided into two equal doses.

Effect on the ability to drive transp. cf. and fur:

Betagistin does not influence or slightly affect the ability to drive vehicles and work with mechanisms, in clinical studies, undesirable reactions that could affect this ability are not identified.

Form release / dosage:

Tablets, 24 mg.

Packaging:

For 10 tablets in PVC / PVDC / Al blister, 5 blisters each, along with instructions for use in a pack of cardboard.

For 15 tablets in PVC / PVDC / Al blister, 2 blisters together with instructions for use in a pack of cardboard.

For 20 tablets in PVC / PVDC / Al blister, 1, 2, 3 or 5 blisters together with instructions for use in a cardboard box.

For 25 tablets in PVC / PVDC / Al blister, 1, 2 or 4 blisters together with instructions for use in a cardboard pack.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000268

Date of registration:27.02.2008 / 08.07.2016

Expiration Date:Unlimited

The owner of the registration certificate:Abbott Helskea Products BVAbbott Helskea Products BV Netherlands

Manufacturer: & nbsp

ABBOTT HEALTHCARE, SAS Netherlands

VEROPHARM SA Russia

Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betaserc® (Betaserc®)