Abstract
Abstract: :
Purpose:Ocular toxicity studies were conducted in rabbits and monkeys with epinastine hydrochloride ophthalmic solution, a new-generation histamine H1 receptor antagonist being developed for the treatment of allergic conjunctivitis. Methods:Epinastine hydrochloride (HCl) ophthalmic solution 0.05%, 0.1%, 0.5%, or placebo was administered in the left eye of New Zealand White rabbits (n=96) and cynomolgus monkeys (n=32) 3 times daily for 6 months. Results:No drug-related effects were seen on clinical signs, gross ocular observation, biomicroscopy, IOP, pupillary reflex, ophthalmoscopy, body/organ weight, hematology, serum chemistry, or histopathology. Pharmacokinetic parameters measured at 6 months showed very low systemic exposure that was dose-dependent. Conclusion:Ophthalmic epinastine is well tolerated in rabbits and monkeys. Long term administration does not produce ocular or systemic toxicity. Pharmacokinetic Parameters For Ophthalmic Epinastine
Keywords: 390 drug toxicity/drug effects • 316 animal model