Bepreve (Bepotastine Besilate Ophthalmic Solution 1.5%) Drug Information: Clinical Pharmacology

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May 25, 2012

Bepreve

Allergy »

Allergy facts

Allergy involves an exaggerated response of the immune system.
The immune system is the body's organized defense mechanism against foreign invaders, particularly infections.
Allergens are substances that are foreign to the body and can cause an allergic reaction.
IgE is the allergy antibody.
Allergies can develop at any age.
Your risk of developing allergies is related to your parents' allergy history.

Introduction

In this review you will learn how allergy relates to the immune system. You will begin understanding how and why certain people become allergic. The most common allergic diseases are discussed briefly in this article.

What does an allergy mean?

An allergy refers to an exaggerated reaction by our immune system in response to bodily contact with certain foreign substances. It is exaggerated because these f...

Read the Allergy article »

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CLINICAL PHARMACOLOGY

Mechanism of Action

Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

Pharmacokinetics

Absorption: The extent of systemic exposure to bepotastine following topical ophthalmic administration of bepotastine besilate 1% and 1.5% ophthalmic solutions was evaluated in 12 healthy adults. Following one drop of 1% or 1.5% bepotastine besilate ophthalmic solution to both eyes four times daily (QID) for seven days, bepotastine plasma concentrations peaked at approximately one to two hours post-instillation. Maximum plasma concentration for the 1% and 1.5% strengths were 5.1 ± 2.5 ng/mL and 7.3 ± 1.9 ng/mL, respectively. Plasma concentration at 24 hours post-instillation were below the quantifiable limit (2 ng/mL) in 11/12 subjects in the two dose groups.

Distribution: The extent of protein binding of bepotastine is approximately 55% and independent of bepotastine concentration.

Metabolism: In vitro metabolism studies with human liver microsomes demonstrated that bepotastine is minimally metabolized by CYP450 isozymes.

In vitro studies demonstrated that bepotastine besilate does not inhibit the metabolism of various cytochrome P450 substrate via inhibition of CYP3A4, CYP2C9, and CYP2C19. The effect of bepotastine besilate on the metabolism of substrates of CYP1A2, CYP2C8, CYP2D6 was not studied. Bepotastine besilate has a low potential for drug interaction via inhibition of CYP3A4, CYP2C9, and CYP2C19.

Excretion: The main route of elimination of bepotastine besilate is urinary excretion (with approximately 75-90% excreted unchanged in urine).

Clinical Studies

Clinical efficacy was evaluated in 2 conjunctival allergen challenge (CAC) studies (237 patients). BEPREVE™ (bepotastine besilate ophthalmic solution) 1.5% was more effective than its vehicle for relieving ocular itching induced by an ocular allergen challenge, both at a CAC 15 minutes post-dosing and a CAC 8 hours post dosing of BEPREVE™ (bepotastine besilate ophthalmic solution 1.5%) .

The safety of BEPREVE™ (bepotastine besilate ophthalmic solution 1.5%) was evaluated in a randomized clinical study of 861 subjects over a period of 6 weeks.

Last reviewed on RxList: 9/17/2009
This monograph has been modified to include the generic and brand name in many instances.