Betahistine
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Clinical Pharmacology
Betahistine acts mainly on the histamine H1 and H3 receptors of the inner ear and the vestibular nuclei of the CNS. Through direct agonistic action on the H1 receptors of the vessels of the inner ear, as well as indirectly through the impact on the H3 receptors, improves microcirculation and capillary permeability, normalizes the endolymph pressure in the maze and cochlea. However, betahistine increases blood flow in the basilar artery. It has a pronounced central effect, being an inhibitor of the H3 receptors of the nuclei of the vestibular nerve. Improves conductivity in the neurons of the vestibular nuclei at the level of the brain stem. The clinical manifestation of these properties is to reduce the frequency and intensity of dizziness, reduce tinnitus, and improve hearing in case of its decrease.
Pharmacokinetics:
Absorbed quickly, the connection with plasma proteins is low. The maximum concentration in a blood plasma in 3 hours. The half-life in 3-4 hours. Almost completely excreted by the kidneys as a metabolite (2-peridylacetic acid) within 24 hours.
Indications
- treatment and prevention of vestibular vertigo of various origin;
- syndromes including dizziness and headache, tinnitus, progressive hearing loss, nausea and vomiting;
- Meniere's disease or syndrome.
Composition
active substance - betahistine dihydrochloride.
Excipients: microcrystalline cellulose; lactose (milk sugar); lemon acid; colloidal silicon dioxide (aerosil); talc; magnesium stearate; sodium lauryl sulfate; starch 1500 (pregelatinized starch).
Description: tablets 16 mg - white or almost white, flat-cylindrical in shape, with chamfer and risk.
Betahistine is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Vertran | pills | ||
Betahistine-SZ | North Star | Russia | pills |
Betahistine | Vertex | Russia | pills |
Vesticap | Ozon | Russia | capsules |
Tagista | Nizhpharm | Russia | pills |
Tagista | Hemofarm | Russia | pills |
Betahistine | Canonpharma | Russia | pills |
Betaver | Veropharm | Russia | pills |
Vestibo | Catalent Germani Schorndorf GmbH | Germany | pills |
Betaserc | Abbott | USA | pills |
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Dosage and Administration
Inside, while eating. 1 / 2-1 pills 3 times a day.
Improvement is usually noted already at the beginning of therapy. A stable therapeutic effect occurs after two weeks of treatment and may increase over several months of treatment. The treatment is long. The duration of the drug is selected individually.
Adverse reactions
Gastrointestinal disorders, allergic reactions of the skin (skin rash, itching, urticaria), angioedema.
Contraindications
Carefully:
- peptic ulcer and duodenal ulcer (in history);
- pheochromocytoma;
- bronchial asthma.
Drug interactions
Cases of interaction or incompatibility with other drugs are unknown.
Pregnancy and Lactation
Not enough data to assess the effects of the drug during pregnancy and lactation. In this regard, it is not recommended reception during pregnancy. At the time of treatment should stop breastfeeding.
Special instructions
Patients with gastric ulcer or duodenal ulcer history, pheochromocytoma or asthma should be prescribed the drug under regular medical supervision.
Influence on ability to drive motor transport and control mechanisms
Betahistine does not have a sedative effect and does not affect the ability to drive a car or engage in activities that require the speed of psychomotor reactions.
Overdosage
Symptoms:nausea, vomiting, convulsions.
Treatment:gastric lavage, reception of Activated charcoal, symptomatic therapy.
- Brand name: Versatis
- Active ingredient: Betahistine
- Manufacturer: Grünentalh GmbH
Studies and clinical trials of Betahistine (Click to expand)
- The influence of betahistine on the dynamics of the cutaneous hypersensitivity reaction in patients with grass pollen allergy
- Utilization of carbon disulphide for the analytical determination of betahistine hydrochloride and captopril in their pharmaceutical preparations
- Lack of substantial effect of the H3-antagonist thioperamide and of the non-selective mixed H3-antagonist/H1-agonist betahistine on amygdaloid kindled seizures
- Effects of histamine and betahistine on rat medial vestibular nucleus neurones: possible mechanism of action of anti-histaminergic drugs in vertigo and motion sickness
- Some studies of the action of betahistine at H1 and H2 receptors for histamine
- Effects of betahistine on locomotor activity and passive avoidance behavior in rats
- Liberation of histamine by compound 48/80, tolazoline, betahistine and burimamide from isolated spontaneously beating guinea pig and rabbit atrial pairs
- A clinical study on the effect of Yinxing Damo combined with Betahistine Hydrochloride Injection on vertebral basilar artery ischemic vertigo
- Management of acute vertigo with betahistine
- Betahistine
- Betahistine voor de ziekte van Menière
- Betahistine increases ACh release from the cortex, but not histamine release from the nucleus basalis magnocellularis of freely-moving rats.
- Does betahistine treatment have additional benefits to vestibular rehabilitation?
- High-dosage betahistine dihydrochloride between 288 and 480
- The vascular mechanism of action of betahistine in the inner ear of the guinea pig
- Stress degradation studies on betahistine and development of a validated stability-indicating assay method
- Prescribing practices for Betahistine
- Betahistine-induced bronchospasm
- Effect of standard-dose Betahistine on endolymphatic hydrops: an MRI pilot study
- Development of novel sustained release matrix pellets of betahistine dihydrochloride: effect of lipophilic surfactants and co-surfactants
- Topical application of betahistine improves eustachian tube function in an animal model
- What role for betahistine in the treatment of Méniére's disease?
- Inhibitory effect of betahistine on polysynaptic neurons in the lateral vestibular nucleus
- GLC determination of betahistine in serum