Betaserc® Combi

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

An artificial analogue of histamine . The effect of betahistine has not been fully studied. There are only a number of hypotheses confirmed by clinical data:

• active substance – partial stimulator of H1-histamine receptors and blocker of H3-histamine receptors of the vestibular centers of the nervous system; improves histamine metabolism and its release due to the above properties;
• betahistine increases blood circulation in the inner ear, relaxing vascular sphincters in this area, and also enhances microcirculation in the brain;
• betahistine stimulates restoration of vestibular function after vestibular neurectomy in animals and humans;
• dose-dependently reduces the generation of impulses in neurons of the vestibular nuclei.

The therapeutic effect of betahistine was demonstrated in patients with Meniere's syndrome and vestibular vertigo , which was expressed by a decrease in the severity and frequency of dizziness .

Pharmacokinetics

When taken orally, the active substance is actively absorbed from the intestine and is almost completely transformed to form a derivative of 2-pyridylacetic acid. The content of betahistine in the blood is low.

Concomitant food intake may slow down the absorption of betahistine. Reaction with blood proteins does not reach the 5% barrier. The maximum concentration of 2-pyridylacetic acid in the blood occurs 1 hour after consumption. The half-life is approximately 3 and a half hours.

The metabolite is actively evacuated in the urine. Excretion of betahistine itself through the kidneys or intestines is negligible.

Pharmacological properties of the drug Betaserc

Pharmacodynamics. The mechanism of action of betahistine is not fully understood. It increases blood circulation in the stria vascularis of the inner ear, by relaxing the precapillary sphincters in the microcirculation system of the inner ear. It has been established that betahistine has a weak agonistic effect on H1 receptors and a pronounced antagonistic effect on histamine H3 receptors in the central and autonomic nervous system. In addition, it was found that betahistine has a dose-dependent inhibitory effect on the generation of peak potentials in neurons of the lateral and medial vestibular nuclei. Betahistine accelerates the process of restoration of vestibular function after unilateral neurectomy, accelerating and facilitating 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 combination, all these properties provide a positive therapeutic effect of betahistine in the treatment of Meniere's disease and vestibular vertigo of various origins. Betahistine enhances the metabolism and release of histamine by blocking presynaptic H3 receptors, which leads to a decrease in their sensitivity. This effect on the histaminergic system explains the effectiveness of betahistine in the treatment of dizziness and vestibular disorders. Pharmacokinetics. After oral administration, betahistine is quickly and completely absorbed from the gastrointestinal tract. It is quickly and completely metabolized to form 2-pyridylacetic acid (a pharmacologically inactive metabolite). The concentration of betahistine in the blood plasma is low (below the detection limit ≤100pg/ml). In this regard, pharmacokinetic analyzes are carried out by measuring the metabolite 2-pyridylacetic acid in plasma and urine. The maximum concentration of the metabolite in the blood plasma is achieved 1 hour after administration. The half-life of 2-pyridylacetic acid is approximately 3.5 hours. 2-pyridylacetic acid is rapidly excreted from the body in the urine. When taking the drug in a dosage of 8-48 mg, about 85% of the initial dose is determined in the urine. Excretion of betahistine by the kidneys or feces is insignificant.

Indications for use of Betaserc

Indications for use of Betaserc:

• Meniere's disease;
• vertebrobasilar insufficiency , atherosclerosis of the cerebral arteries , post-traumatic encephalopathy (as a component of complex therapy);
• syndromes characterized by tinnitus, increasing hearing loss, dizziness , including hydrops of the inner ear , labyrinthine and vestibular disorders, labyrinthitis , vestibular neuritis, benign positional vertigo.

Betaserc tablets, instructions for use (Method and dosage)

The medicine is prescribed to be taken orally with meals. The dosage is selected individually, taking into account the response to therapy.

The daily dose for adults is usually 24-48 mg, divided into 2-3 doses. The 16 mg or 24 mg tablet is easy to split. To do this, place the dosage form on a hard surface with the notch facing up and press firmly on it with your finger.

Sometimes the drug shows its effect only after 2-3 weeks of treatment, and a confident therapeutic effect develops after several months of constant use. No dosage adjustment is required in elderly patients.

Betaserc tablets 16 mg No. 15x2

Name

Betaserc tablet 16 mg in bl. in pack No. 15x2

Description

Round biconvex tablets of white or almost white color with beveled edges, with a score on one side of the tablet and engraving “267” on both sides of the score. The tablet is divided into two equal halves.

Main active ingredient

Betagistine

Release form

Pills

Dosage

16mg

pharmachologic effect

Pharmacodynamics

Mechanism of action The mechanism of action of betahistine is partially known. There are several reliable hypotheses, confirmed by studies conducted with animals and humans: Betahistine affects the histamine system Betahistine is simultaneously a partial agonist of H1-histamine receptors, as well as an antagonist of 3-histamine receptors in nervous tissue. It also has a minor effect on H2 receptor activity. Betahistine accelerates the metabolism and release of histamine by blocking presynaptic NS receptors and the feedback system. Betahistine may improve cochlear circulation as well as cerebral circulation. Pharmacological studies in animals indicate an improvement in blood supply to the stria vascularis of the inner ear, probably as a result of dilation of the precapillary sphincters in the microvasculature of the inner ear. Betahistine also increases cerebral circulation in humans. Betahistine increases compensation of the vestibular apparatus Betahistine accelerates the restoration of normal vestibular function after unilateral neurectomy in animals by stimulating and improving compensation from the central vestibular apparatus. This effect occurs due to an increase in the metabolism and release of histamine as a result of an antagonistic effect on NZ receptors. In patients treated with betahistine, the time to recovery of vestibular root function after injury was also reduced. Betahistine modifies the formation of impulses in the vestibular nuclei. A dose-dependent inhibitory effect of betahistine on the formation of action potentials in neurons of the lateral and medial vestibular nuclei has also been established. Betahistine does not have sedative properties. Animal studies have shown that the pharmacodynamic properties of betahistine may have a beneficial therapeutic effect on the vestibular system. Efficacy and clinical safety The effectiveness of betahistine has been proven in studies involving patients with dizziness of vestibular origin and Meniere's syndrome, who experienced improvement associated with a decrease in the intensity and frequency of dizziness.

Pharmacokinetics

Absorption After oral administration, betahistine is rapidly and almost completely absorbed from all parts of the gastrointestinal tract. After absorption, it is quickly and almost completely biotransformed to 2-pyridylacetic acid (2-PAA). The concentration of betahistine in blood plasma is very low. For this reason, pharmacokinetic assays are based on measuring 2-PAA concentrations in plasma and urine. Cmax when taking the drug with food is lower than when taken on an empty stomach. However, complete absorption of betahistine is similar in both conditions, indicating that food slows the absorption of betahistine. Distribution The level of betahistine bound to plasma proteins is less than 5%. Biotransformation After absorption, betahistine is quickly and almost completely biotransformed to 2-PAA acid, which has no pharmacological activity. Following oral administration of betahistine, plasma (and urine) concentrations of 2-PAA reach a maximum after 1 hour and decline with a half-life of approximately 3.5 hours. Excretion 2-PAA is rapidly excreted in the urine. When taking the drug at a dose of 8 - 48 mg, about 85% of the initial dose is excreted in the urine. Excretion of betahistine itself in feces or urine is negligible. The elimination rate is constant over the dose range from 8 mg to 48 mg, indicating linear pharmacokinetics of betahistine and indicating that the metabolic pathway remains unsaturated.

Indications for use

Symptomatic treatment of recurrent dizziness with or without cochlear symptoms.

Directions for use and doses

Dosage Betaserc 8 mg The usual dosage for adults is 1-2 tablets 3 times a day, but not more than 6 tablets, i.e. 48 mg betahistine per day. Betaserc 16 mg The usual dosage for adults is 1/2-1 tablet 3 times a day. Betaserc 24 mg This dosage form is intended for use in patients who require a daily dose of 48 mg of betahistine. In other cases, lower doses should be used. The usual dosage for adults is 1 tablet 2 times a day. Children and adolescents Betaserc is not recommended for use in children and adolescents under 18 years of age due to insufficient data on efficacy and safety. Elderly patients Betahistine should be used with caution in elderly patients as available safety data are limited. Renal failure There are no data on use in patients with renal failure. Hepatic insufficiency There are no data on use in patients with hepatic insufficiency. Duration of treatment The recommended duration of treatment is from 2 to 3 months, treatment can be extended depending on the course of the disease, in intermittent or continuous courses. Directions for use: Orally, during meals, swallow the tablets without chewing with a glass of water.

Use during pregnancy and lactation

Pregnancy Studies in animals have not shown any teratogenic effects. Because reproductive toxicity studies in animals do not always assess the potential for toxic effects on pregnancy, embryonic/fetal development, childbirth and postnatal development in humans, it is not recommended to take betahistine during pregnancy. Breastfeeding It is not known whether betahistine is excreted in breast milk. Betahistine is excreted into rat milk. Postpartum effects in animal studies were observed only at very high doses. The benefit of using the drug for the mother should be weighed against the benefits of breastfeeding and the potential risk to the child. Fertility Animal studies have shown no effect on fertility in rats.

Precautionary measures

Patients with bronchial asthma require careful monitoring during betahistine therapy (risk of bronchospasm). Taking the drug with meals can prevent the occurrence of pain in the stomach. Betahistine is not recommended for the treatment of the following pathological conditions: benign paroxysmal vertigo; dizziness associated with damage to the central nervous system.

Interaction with other drugs

No in vivo studies regarding drug interactions have been conducted. Data obtained from in vitro studies do not provide evidence to suggest inhibition of the activity of cytochrome P45O enzymes under in vivo conditions. In vitro laboratory data indicate that the biotransformation of betahistine may be inhibited by monoamine oxidase inhibitors (MAOIs), including MAO subtype B (for example, selegiline). Caution is recommended when taking betahistine and MAO inhibitors (including selective MAO-B inhibitors) concomitantly. Due to the fact that betahistine is a histamine analog, the interaction of betahistine with antihistamine drugs could theoretically affect the effectiveness of one of them.

Contraindications

Hypersensitivity to any component of the drug; Active phase of peptic ulcer; Pheochromocytoma.

Compound

1 16 mg tablet contains: 16 mg betahistine dihydrochloride, which corresponds to 10.42 mg betahistine; Excipients: microcrystalline cellulose, mannitol (E421), citric acid monohydrate, anhydrous colloidal silicon dioxide, talc.

Overdose

There have been reports of several cases of drug overdose. Some patients experienced mild or moderate symptoms after taking the drug at a dose of up to 640 mg (for example, nausea, drowsiness, abdominal pain). More serious symptoms of overdose (eg, seizures, pulmonary or cardiovascular events) have been observed when increased doses of betahistine were intentionally taken in combination with overdose of other drugs. Symptoms of overdose are treated with usual corrective measures.

Side effect

The following adverse reactions were observed in patients taking betahistine during clinical placebo-controlled studies, with the following frequencies: very common (≥1/10); often (≥1/100 to

Storage conditions

Store in original packaging at a temperature not exceeding 25°C. Keep out of the reach of children.

Buy Betaserc tablets 16 mg No. 15x2 in the pharmacy

Price for Betaserc tablets 16 mg No. 15x2

Instructions for use for Betaserc tablets 16 mg No. 15x2

Betaserc's analogs

Level 4 ATX code matches:
Betagis

Stugeron

Betaver

Westinorm

Westicap

Betagistine

Tagista

Vestibo

Cinnarizine

• Betagistine
• Alfaserk
• Microzer
• Asniton
• Betaver
• Betacentrin
• Vertran
• Vestibo
• Westinorm
• Westicap
• Denoise
• Vazoserk
• Tagista (Russian equivalent)

The price of Betaserc analogues is noticeably lower than the price of the described drug.

Betaserc and its analogues (the vast majority) contain betahistine as an active substance, so their indications and contraindications will be identical.

Which is better: Betaserc or Betahistine?

Betahistine and the described drug are analogues with an identical active component. Their indications and contraindications are also the same. The choice should be made based on economic feasibility.

Betaserk or Vestibo – which is better?

Vestibo is a cheaper analogue of Betaserc with almost the same composition. The choice between these drugs should be made for reasons of economic feasibility.

Tagista or Betaserk – which is better?

Tagista is the Russian analogue of Betaserk. The main difference is the price: Tagista rightfully takes the place of the most affordable medicine containing betahistine.

Betaserk

Betaserc (active ingredient - betahistine) is a drug that improves microcirculation in the inner ear and is used for disorders of the vestibular apparatus, incl. with Meniere's syndrome and vertigo. It is a synthetic analogue of the biogenic amine histamine. The mechanism of action of the drug has only been partially studied. Currently, scientists continue to work on several hypotheses, supported by the results of preclinical and clinical studies. Thus, as one of the mechanisms of pharmacological action of betaserc, its effect on the histaminergic system is considered. The drug stimulates the metabolism and release of histamine due to the blockade of presynaptic H3 receptors and a decrease in the number of H3 receptors. In addition, as was established at the preclinical stage of studying betaserc, the drug is able to activate blood circulation in the cochlea of ​​the inner ear and throughout the brain. This occurs due to a decrease in the tone of the precapillary sphincters in the blood vessels of the inner ear. Preclinical studies have also found that betaserc provides faster recovery of vestibular function in laboratory animals after unilateral vestibular nerve ablation. This property of the drug was later confirmed in clinical trials on humans. Another clinically significant effect of betaserc is the suppression of the generation of action potentials in nerve cells of the lateral and medial nuclei of the vestibular nuclear complex. The effectiveness of the drug was confirmed in patients with vestibular dizziness (vertigo) and Meniere's syndrome, which was reflected in a decrease in the frequency and severity of dizziness. When betaserc is taken orally, it is quickly and completely absorbed from the gastrointestinal tract. Almost immediately after this, it undergoes systemic metabolism to form 2-pyridylacetic acid. When taking betaserc simultaneously with food, the maximum concentration of the active substance in the blood plasma will be lower than on an empty stomach.

However, the total degree of absorption of betahistine in both cases will be approximately the same. In other words, food intake only slows down the absorption of the drug to some extent, without significantly affecting other pharmacokinetic characteristics. Betaserc is quickly excreted from the body through the urine and only to a small extent through the intestines. The rate of elimination of the drug remains unchanged when taken orally from 8 to 48 mg, which indicates the linearity of its pharmacokinetics.

Betaserc is taken with food. The specific dose of the drug is selected individually depending on the severity of the therapeutic response and the patient’s tolerability of treatment. Adults take betaserc 24-48 mg per day. It is possible to divide the tablet into two parts, for which it is placed on a hard, smooth surface in the upward position and pressed from above with the thumb. You should not expect instant relief of symptoms from betaserc: in some cases, visible improvement occurs only after several weeks of regular pharmacotherapy, and a lasting therapeutic effect can develop only after several months. There is clinical evidence that taking betaserc in the initial phase of the disease prevents its further progression or hearing loss at a later stage. As the practice of using the drug shows, dose adjustment is not required in elderly patients. Clinical studies covering the interaction of betaserc with other drugs have not been conducted to date. Based on data from laboratory studies, it can be assumed that in a living organism, the activity of the cytochrome P450 enzyme system will remain at the same level. Being a histamine analogue, betaserc may have an effect on drugs that block histamine H1 receptors. In any case, before starting a course of medication, the patient must inform the doctor about the current or recent use of any medications.

Betaserk price, where to buy

The price of Betaserc 24 mg No. 20 on average in Russia is about 500 rubles, and the drug with a dosage of 16 mg No. 30 is 600 rubles.

In Ukraine, the price range is wide: a package of medicine with a dosage of 16 mg No. 30 can be bought for about 400 hryvnia.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

LuxPharma* special offer

• Betaserc tablet.
  24 mg 20 pcs 950 rub. order

ZdravCity

• Betaserc tab. 24 mg No. 60 JSC Veropharm

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• Betaserc tab. 16mg No. 30AO Veropharm

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• Betaserc tab. 24mg No. 20AO Veropharm

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• Betaserc Long tablets 48 mg 28 pcs. JSC Veropharm

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Pharmacy Dialogue

• Betaserc (8 mg tablet No. 30) Abbot/Veropharm

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• Betaserc Long tablets 48 mg No. 28 Veropharm

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• Betaserc tablets 24 mg No. 60Abbot/Veropharm

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Pharmacy24

• Betaserc 8 mg N30 tablets Abbott Healthcare SAS., France
  376 UAH order
• Betaserc 16mg N30 tablets Mylan Laboratories SAS, France

  423 UAH. order

PaniPharmacy

• Betaserc tablets Betaserc tablets 24 mg No. 20 France, Mylan Lab.

  418 UAH. order

• Betaserc tablets Betaserc tablets 16 mg No. 30 France, Mylan Lab.

  429 UAH. order

• Betaserc tablets Betaserc tablets 8 mg No. 30 France, Mylan Lab.

  432 UAH. order

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