Bepotastine Besilate

Bepotastine Besilate tablet is indicated for treatment of allergic rhinitis and urticaria.

Antagonistic action on histamine H1 receptor: Bepotastine besilate is a highly selective antagonist of histamine H1 receptor. In vitro receptor binding studies have shown no measurable affinity for 5-HT2, α1, α2 or muscarinic receptors. Orally administered bepotastine besilate inhibited the histamine–induced cutaneous vascular hyperpermeability in rats and guinea pigs. In vitro, bepotastine besilate showed dose-dependent inhibition of histamine-induced contraction of tracheal and ileal smooth muscles isolated from guinea pigs.

Inhibitory actions on type I allergic reaction: Orally administered bepotastine besilate inhibited passive cutaneous anaphylaxis (PCA) reaction in rats and guinea pigs, as well as anaphylactic shock and antigen-induced airway constriction in guinea pigs. Orally administered bepotastine besilate inhibited increase in nasal cavity-resistance in experimental allergic rhinitis model guinea pigs and antigen-induced vascular hyperpermeability in the nasal mucosa in rats.

Effects on eosinophils: Orally administered bepotastine besilate inhibited platelet activating factor (PAF)-induced eosinophil infiltration in rats and guinea pigs, and antigen-induced eosinophil infiltration in mice. Orally administered bepotastine besilate inhibited antigen-induced peripheral blood eosinophilia in mice.

Effects on cytokine production: In vitro, bepotastine besilate suppressed interleukin-5 production in human peripheral blood mononuclear cells.

Usually, for adults, 10 mg of bepotastine besilate as a single dose is orally administered twice daily. The dosage may be adjusted depending on the patient’s age and symptoms.

Patients with renal impairment: The blood concentration of bepotastine may be increased and remain persistently high. This product should be administered with care such as starting from lower dosage (e.g. 5 mg per dose).

Elderly patients: This product is primarily excreted by the kidneys as intact form. Since elderly patients often have reduced renal function, pay appropriate attention to possible persistence of the elevated blood concentration.

Pediatric patients: Usually, for children (≥7 years old), 10 mg of bepotastine besilate as a single dose is orally administered twice daily. The safety of bepotastine besilate in children under 7 years of age has not been established (little
clinical experience).

Bepotastine Besilate is contraindicated in the patients with a history of hypersensitivity to any of the ingredients of this product.

This product is not recommended to be administered to pregnant women or women who may possibly be pregnant. It should be used only if the expected therapeutic benefits outweigh the possible risks associated with treatment. Use of this product in lactating woman is not recommended. If administration of this product is judged to be essential, lactation should be discontinued during treatment.

This product could possibly cause somnolence in some patients. Whoever aims to be riding, driving, operating machine or working at height with a potential risk to fall from height, should test and ensure, in advance, that this product would not cause him/her somnolence. This product should not be taken concomitantly with alcohol-containing beverages. This product should not be used during the first trimester of pregnancy, during the period of lactation, and in children under 2 years of age.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.