Bepotastine besilate ophthalmic solution for the relief of nonocular symptoms provoked by conjunctival allergen challenge.

Abstract

BACKGROUND:

Bepotastine besilate is a selective histamine1-receptor antagonist and mast cell stabilizer with inhibitory effects on eosinophilic activity.

OBJECTIVE:

To evaluate the safety and efficacy of 1.5% bepotastine besilate ophthalmic solution in alleviating nonocular symptoms induced by a conjunctival allergen challenge (CAC), a clinical model of allergic conjunctivitis.

METHODS:

This was a single-center, double-masked, randomized, placebo-controlled clinical trial performed from March 1 to April 4, 2007. Patients 10 years or older with a history of allergic conjunctivitis and a reproducible, positive, clinical response to a CAC were eligible. Patients received either placebo or 1.5% bepotastine besilate, 1 drop in each eye. After 15 minutes, 8 hours, or 16 hours after dosing, a CAC was performed and patients evaluated nonocular symptoms using standardized grading scales.

RESULTS:

Seventy-one patients were enrolled in the study, and 66 comprised the per protocol population. A clinically meaningful reduction (> or = 1.0 unit) compared to placebo was achieved for rhinorrhea and nasal congestion at most time points after 1.5% bepotastine besilate instillation at 8 hours before a CAC test. Significant reductions (P < or = .05) in mean values were seen with 1.5% bepotastine besilate at 15 minutes and 8 hours after dosing for CAC-induced nasal congestion, rhinorrhea, ear or palate pruritus, nasal pruritus, and summed nonocular composite symptom (NOCS) scores and also at 16 hours after dosing for nasal congestion and rhinorrhea.

CONCLUSIONS:

The 1.5% bepotastine besilate formulation produced statistically significant reductions after a CAC in individual nonocular symptoms and NOCS scores at onset of allergic response and for at least 8 hours after instillation, with the greatest reduction seen for nasal congestion and rhinorrhea.

• Authors: Gail L Torkildsen, Jon I Williams, James A Gow, Paul J Gomes, Mark B Abelson, Timothy R McNamara, Bepotastine Besilate Ophthalmic Solutions Clinical Study Group
• Journal: Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology (Ann Allergy Asthma Immunol) Vol. 105 Issue 1 Pg. 57-64 (Jul 2010) ISSN: 1081-1206 [Print] United States
• PMID: 20642205 (Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial)

Chemical References

• Allergens
• Histamine Antagonists
• Ophthalmic Solutions
• Piperidines
• Pyridines
• bepotastine besilate

Topics

• Adult
• Allergens (immunology)
• Conjunctivitis, Allergic (diagnosis, drug therapy, physiopathology)
• Double-Blind Method
• Female
• Histamine Antagonists (administration & dosage, adverse effects)
• Humans
• Immunization
• Male
• Middle Aged
• Nasal Obstruction
• Ophthalmic Solutions (administration & dosage, adverse effects)
• Piperidines (administration & dosage, adverse effects)
• Pyridines (administration & dosage, adverse effects)