Merislon

Merislon

betahistine

Manufacturer:

Eisai

Distributor:

DKSH
Full Prescribing Info
Contents
Betahistine mesilate.
Description
Each white plain tablet contains 6 mg of Betahistine mesilate.
Each white plain tablet contains 12 mg of Betahistine mesilate.
Betahistine mesilate occurs as white crystals or crystalline powder. It is odorless, or has a faint, characteristic odor, and has a bitter taste. It is very soluble in water, freely soluble in methanol and in acetic acid (100), sparingly soluble in ethanol (99.5), very slightly soluble in acetic anhydride, and in practically insoluble in diethyl ether.
It is hygroscopic.
Non-proprietary name: Betahistine mesilate (JAN), Betahistine (INN).
Chemical name: 6 mg: N
-Methyl-2-pyridin-2-ylethylamine dimethanesulfonate.
12 mg: N
-methyl-N[2-(pyridin-2-yl)ethyl ]aminedimethanesulfonate.
Molecular formula:
C8H12N2·2CH4O3S.
Molecular weight: 328.41.
Excipients/Inactive Ingredients: Hydrated silicon dioxide, microcrystalline cellulose, calcium stearate, talc and hydroxypropylcellulose.
Action
Merislon dilates pre-capillary sphincters, increasing the blood flow in the inner ear. It controls the permeability of capillaries in the inner ear, thereby removing endolymphatic hydrops. It also improves cerebral circulation, increasing blood flow in the internal carotid artery. Merislon is clinically useful for the relief of vertigo and dizziness.
Pharmacology: Pharmacodynamics: Improvement of Circulatory Disturbances in the Inner Ear: In the inner ear of the guinea pig with experimentally-induced microcirculation disturbances, the blood flow increases to 148% of the control level within 30 min after the intraperitoneal injection of betahistine mesilate. This effect was specific for pathological conditions.
Increase of Blood Flow in the Scala Media of Guinea Pigs with Endolymphatic Hydrops: When betahistine mesilate was administered to guinea pigs with endolymphatic hydrops, it produced a significant increase in blood flow in the scala media. The blood flow increased significantly from 5.5 mL/min/100 mg to 8.1 mL/min/100 g. It is considered that the increase in blood flow is due to relaxation of smooth muscle of the cochlear radial arteria.
Improvement of Intra-cerebral Blood Flow: In the experiment in rhesus monkeys, betahistine mesilate after intravenous administration increases blood flow in the cerebral and cerebellar tissues from 70.4 to 81.4 mL/min/100 g and 73.2 to 84 mL/min/100 g, respectively.
Clinical Studies: Clinical Efficacy: In clinical trials, including double-blind studies, treatment of a total of 875 patients has been demonstrated that Merislon is useful for relieving dizziness or feeling of dizziness associated with Meniere's disease, Meniere's syndrome or vertigo, etc.
Pharmacokinetics: Betahistine mesilate was administered orally to 20 healthy adult male volunteers at a single dose of 24 mg. The main metabolic product was 2-pyridylacetic acid and its plasma concentration was determined. The time to reach the peak plasma concentration (Tmax) was 0.98 ± 0.47 h, the peak plasma concentration (Cmax) was 339.4 ± 213.4 ng/ml, eliminated half-life (t1/2) was 5.17 ± 2.66 h and the area under the plasma concentration-time curve (AUC0-t) was 1153 ± 729 ng·h/ml.
Indications/Uses
Vertigo and dizziness associated with Meniere's disease(Note), Meniere's syndrome(Note) and peripheral vertigo.
Note: Meniere's disease/syndrome is a disorder of the inner ear which results in vertigo, hearing loss and tinnitus.
Dosage/Direction for Use
The usual adult dosage for oral use is 6-12 mg of betahistine mesilate, three times daily after meals. The dosage may be adjusted depending on the patient's age and symptoms.
Overdosage
There is no experience to date with deliberate overdose. No specific antidote is known.
Contraindications
Patients with a history of hypersensitivity to any ingredients of Merislon.
Special Precautions
Careful administration in the following patients: Patients with a history of peptic or active ulcer: Since Merislon has a histamine-like action, it may enhance gastric acid secretion through the intervention of H2-receptors.
Patients with bronchial asthma: Since Merislon has a histamine-like action, it may cause respiratory tract contraction through the intervention of H1-receptors.
Patients with pheochromocytoma: Since Merislon has a histamine-like action, it may cause an increase in blood pressure due to adrenaline hypersecretion.
Effects on Ability to Drive and Operate Machines: Based on the pharmacodynamic properties and the adverse events profile, it is unlikely that Merislon would cause an impairment of driving performance or compromise the ability to use machinery.
Use in Children: The safety in children has not been established (insufficient clinical experience).
Use in Elderly: Since the elderly often have a physiological hypofunction, it is advisable to take measures such as reduction in dosage under careful supervision.
Use In Pregnancy & Lactation
Use in Pregnancy and Lactation: Merislon should only be used in pregnant women or women suspected of being pregnant only if the expected therapeutic benefits are evaluated to outweigh the possible risk of treatment. (The safety of Merislon in pregnant women has not been established.)
It is not known whether betahistine is excreted in human milk so the therapeutic benefit of Merislon for lactating women should be evaluated to outweigh the possible risk to the child.
Adverse Reactions
Adverse reactions were reported in 26 of 2254 patients (1.15%). (Post-marketing clinical investigation.) See Table.

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Drug Interactions
Interaction between Merislon tab and other drugs has not been documented.
Theoretically, the effect of betahistine is antagonized by antihistamines.
Caution For Usage
Caution in Handling Over Drug: For drugs that are dispensed in a press-through package (PTP), the patient should be instructed to remove the drug from the package prior to use. (It has been reported that, if the PTP sheet is swallowed, the sharp corners of the sheet may puncture the esophageal mucosa, causing perforation and resulting in serious complications such as mediastinitis.)
Storage
Merislon tablets 12 mg should be stored at room temperature not exceeding 25°C and stored in a moisture-proof container after unsealing. Do not store above 30°C.
Shelf-Life: 36 months from manufacturing date.
MIMS Class
ATC Classification
N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.
Presentation/Packing
Tab 6 mg (white, round with beveled edge, plain on one side, engraved
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on the other side) x 3 x 10's. 12 mg (white, scored, plain on one side, engraved
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on the other side, with a diameter of 7.1 mm, weight of 120 mg and thickness of 2.7 mm) x 100 x 10's.
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