An estimated 60 to 90 million individuals suffer from allergic conjunctivitis in the United States, and the prevalence may be increasing.1 While there are a number of topical and oral treatments available, 31% of patients taking an allergy medication are not fully satisfied with their current medication.2 Reports have indicated that nearly 73% of patients on allergy medication still suffer from itchy, red, watery eyes.1 This is why the more choices of medications we have access to, the better. Medications that target multiple mechanisms of action against inflammatory mediators may be more efficacious than single-mechanism medications, and this may make the difference for some of our patients.

Bepotastine is a topically active histamine H1 blocker that also inhibits the release of histamine from mast cells. It suppresses the migration of eosinophil into inflamed tissues. Bepotastine has been approved in Japan for systemic use in the treatment of allergic rhinitis since 2000 and for cases of urticaria/pruritus since 2002. Bepreve (bepotastine besilate ophthalmic solution 1.5%, ISTA Pharmaceuticals) was approved by the U.S. Food and Drug Administration in September 2009 for the treatment of ocular itching associated with allergic conjunctivitis. Bepreve is specifically indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.3 It’s supplied in a 10ml squeeze bottle and is designed for topical administration. The recommended dose of the drug is one drop into the affected eye(s) b.i.d.

The FDA approval of Bepreve was based on two conjunctival allergen challenge (CAC) studies in 237 patients. Bepreve was more effective than placebo in relieving ocular itching induced by an ocular allergen challenge, both at 15 minutes post-dosing and at eight hours post dosing. The drug was determined to be safe and well tolerated.3

Additional results from Phase 3 clinical studies demonstrated that Bepreve was as effective in suppressing ocular itching in patients with more severe itching as in patients with all grades of ocular itching.4

Results of other studies demonstrated that Bepreve was effective at reducing ocular itching for at least eight hours after dosing and noticeably improved ocular itching vs. placebo for up to 16 hours after dosing.5 In addition, evidence showed that Bepreve substantially reduces tearing caused by a conjunctival allergen challenge for at least eight hours after dosing.6 Bepreve, dosed twice daily for six weeks, was also found safe with minimal adverse events in a healthy pediatric population from 10 to 17 years of age.7 The most common reported adverse reaction, occurring in approximately 25% of subjects, was a mild aftertaste following instillation. Other adverse reactions occurring in 2% to 5% of subjects were ocular irritation, headache and nasopharyngitis.3

Advise patients to remove contact lenses prior to instillation of Bepreve; the preservative benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after waiting 10 minutes. Bepotastine plasma concentrations peaked at approximately one to two hours post-instillation. And, plasma concentration at 24 hours post-instillation were below the quantifiable limit (2ng/mL) in 11/12 subjects evaluated. The main route of elimination of bepotastine besilate is urinary excretion—approximately 75% to 90% is excreted unchanged in urine. It is not known if bepotastine besilate is excreted in human milk; therefore, caution should be exercised when Bepreve is used by nursing women.3 The medication is Pregnancy Category C, which means it should be used only if the benefit exceeds the risk.

Ocular allergy diagnosis and management is a large part of a medical optometric practice. With the addition of Bepreve, we have another weapon in our therapeutic arsenal. 

1. Tang EA, Matsui E, Wiesch DG, Samet JM. Epidemiology of asthma and allergic diseases. In: Middleton’s Allergy Principles and Practice, Vol. 2 (7th ed.). Adkinson et al, eds. St. Louis. CV Mosby, 2009.
2. Marple MA, Fornadley JA, Patel AA. Keys to successful management of patients with allergic rhinitis: focus on patience confidence, compliance, and satisfaction. Otolaryngol Head Neck Surg. 2007 Jun;136(6 Suppl):S107-24.
3. Bepreve. ISTA Pharmaceuticals. Package Insert.
4. Williams JI, Gow JA, Gomes PA, et al. Treatment of ocular itching with bepotastine besilate ophthalmic solution 1.5% for subjects with more severe itching response in a conjunctival allergen hallenge (CAC) clinical model of allergic conjunctivitis. Ann Allergy Asthma Immunol. 2009;103(5) Suppl 3.
5. Macejko TT, McLaurin EB, [third author please?], et al. Bepotastine Besilate Ophthalmic Solution 1.5% Reduces Ocular Itching Following Dosing in the Conjunctival Allergen Challenge (CAC) Model of Acute Allergic Conjunctivitis. ARVO Abstract D926; May 7,2009.
6. Kurata FK, Macejko TT, [third author please?], et al. Bepotastine Besilate Ophthalmic Solution 1.5% Reduces Tearing at 8 Hours Following Dosing in a Multi-Site Clinical Trial Using the Conjunctival Allergen Challenge (CAC) Model of Acute Allergic Conjunctivitis. ARVO Abstract D922; May 7, 2009.
7. Protzko EE, Williams JI, [ditto] et al. The Safety of the Anti-Histamine Bepotastine Besilate Ophthalmic Solution in a Healthy Pediatric Population From Ten to Seventeen Years of Age. ARVO Abstract D923; May 7, 2009.