Betahistine Mesilate CEO

Uses

Betahistine Mesilate CEO Mesilate dilates precapiilary sphincters, increasing the blood flow in the inner ear. It controls the permeability of capillaries in the inner ear, thereby removes endolymphatic hydrops. It also improves cerebral circulation, increasing blood flow in the internal carotid artery. Thus, Betahistine Mesilate CEO Mesylate is clinically useful for the relief of vertigo and dizziness.

Betahistine Mesilate CEO is also used to associated treatment for these conditions: Menière's Disease

How Betahistine Mesilate CEO works

Vertigo is a disturbing sensation of movement caused by dysfunction of the labyrinth (inner ear), vestibular nerve, cerebellum, brainstem, or Central Nervous System (CNS). Vestibular forms of vertigo are often accompanied by auditory dysfunctions such as hyperacusis, hearing loss, and tinnitus. In most cases, adaptive mechanisms of the CNS lead to functional recovery after episodes of vertigo, however, syndromes such as Ménière's disease tend to cause the recurrence of vertigo symptoms. This significantly impacts the quality of life and the ability to carry out daily activities.

H1-receptor activity

The mechanism of action of betahistine is multifactorial. Ménière's disease is thought to result from a disruption of endolymphatic fluid homeostasis in the ear. Betahistine Mesilate CEO mainly acts as a histamine H1-receptor agonist. The stimulation of H1-receptors in the inner ear causes a vasodilatory effect leading to increased permeability of blood vessels and a reduction in endolymphatic pressure; this action prevents the rupture of the labyrinth, which can contribute to the hearing loss associated with Ménière's disease. Betahistine Mesilate CEO is also purported to act by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, relieving symptoms of vertigo.

H3-receptor activity

In addition to the above mechanisms, betahistine also acts as a histamine H3-receptor antagonist, increasing the turnover of histamine from postsynaptic histaminergic nerve receptors, subsequently leading to an increase in H1-agonist activity. H3-receptor antagonism elevates levels of neurotransmitters including serotonin in the brainstem, inhibiting the activity of vestibular nuclei, thus restoring proper balance and decreasing vertigo symptoms.

Dosage

Betahistine Mesilate CEO dosage

Usually for adults, administer orally 6 mg to 12 mg three times per day after meals. The dose may be adjusted according to the age of patient and severity of symptoms.

Side Effects

Nausea or vomiting may rarely occur. Hypersensitivity reactions, such as skin rash, may rarely occur.

Toxicity

Symptoms of an overdose with betahistine (< 640 mg) include dry mouth, nausea, dyspepsia, abdominal pain, and somnolence. Serious complications such as convulsions, pulmonary or cardiac effects may occur with higher doses (> 640 mg), especially during intentional overdoses and combination with other drugs. In the case of an overdose with betahistine, provide supportive therapy, and contact the local poison control center for further management.

Precaution

Patients with a history of digestive ulcer or an active digestive ulcer, Patients with bronchial asthma, Patients with pheochromocytoma.

Food Interaction

• Take with food. This may reduce or prevent gastrointestinal upset.

Volume of Distribution

In a pharmacokinetic study of rats, betahistine was found to be distributed throughout the body. Human data for betahistine's volume of distribution is not readily available.

Elimination Route

When given orally, betahistine is rapidly and almost completely absorbed from the gastrointestinal tract. In the fasted state, Cmax is achieved within 1 hour of administration; in the fed state, Cmax is delayed, but the total drug absorption is similar. Food, therefore, has little effect on the absorption of betahistine.

Half Life

The half-life of betahistine is 3-4 hours.

Elimination Route

Betahistine Mesilate CEO is mainly excreted in the urine; with approximately 85-91% being detected in urine samples within 24 hours of administration.

Pregnancy & Breastfeeding use

Safety of Betahistine Mesilate CEO during pregnancy has not been established. This drug should be administered to pregnant patients or women suspected of being pregnant, only if the expected therapeutic benefit is thought to outweigh any possible risk.

Contraindication

Hypersensitivity to betahistine mesylate, pheochromocytoma, peptic ulcer, acute bronchial asthma.

Storage Condition

Store in cool and dry place. Protect from light & moisture.

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