Diclofenac Sodium Ophthalmic Solution, 0.1%

Prostaglandins have been shown in many animal models to be mediators of certain kinds of intraocular inflammation. In studies performed in animal eyes, prostaglandins have been shown to produce disruption of the blood-aqueous humor barrier, vasodilation, increased vascular permeability, leukocytosis, and increased intraocular pressure.

Diclofenac sodium is one of a series of phenylacetic acids that have demonstrated anti-inflammatory and analgesic properties in pharmacological studies. It is thought to inhibit the enzyme cyclooxygenase, which is essential in the biosynthesis of prostaglandins.

Results from a bioavailability study of another formulation of diclofenac sodium ophthalmic solution established that plasma levels of diclofenac following ocular instillation of two drops of diclofenac sodium ophthalmic solution, 0.1% to each eye were below the limit of quantitation (10 ng/mL) over a 4-hour period. This study suggests that limited, if any, systemic absorption occurs with diclofenac sodium ophthalmic solution, 0.1%.

It is recommended that Diclofenac Sodium Ophthalmic Solution, 0.1%, like other NSAIDs, be used with caution in surgical patients with known bleeding tendencies or who are receiving other medications that may prolong bleeding time.

Diclofenac Sodium Ophthalmic Solution, 0.1% may slow or delay healing.

Results from clinical studies indicate that Diclofenac Sodium Ophthalmic Solution, 0.1% has no significant effect upon intraocular pressure, however, elevations in intraocular pressure may occur following cataract surgery.

Long term carcinogenicity studies in rats given oral diclofenac sodium up to 2 mg/kg/day (approximately the human oral dose) have revealed no significant increases in tumor incidence. There was a slight increase in benign rat mammary fibroadenomas in mid-dose females (high dose females had excessive mortality) but the increase was not significant for this common rat tumor. A 2-year carcinogenicity study conducted in mice employing oral diclofenac sodium up to 2 mg/kg/day did not reveal any oncogenic potential. Diclofenac sodium did not show mutagenic potential in various mutagenicity studies including the Ames test. Diclofenac sodium administered to male and female rats at 4 mg/kg/day did not affect fertility.

Safety and effectiveness in pediatric patients have not been established.

Transient burning and stinging was reported in 15% of patients with the use of topical diclofenac sodium ophthalmic solution, 0.1%. In cataract studies, keratitis occurred in 28% of patients receiving diclofenac sodium ophthalmic solution, 0.1%; however, most of the cases of keratitis occurred prior to drug therapy. Elevated intraocular pressure was reported in 15% of patients receiving diclofenac sodium ophthalmic solution, 0.1%. The following adverse reactions were reported in approximately 5% or less of the patients: abnormal vision, anterior chamber reaction, blurred vision, conjunctivitis, corneal deposits, corneal edema, corneal lesions, corneal opacity, discharge, injection, iritis, irritation, itching and ocular allergy.

The following adverse reactions were reported in 3% or less of the patients: abdominal pain, asthenia, chills, dizziness, facial edema, fever, headache, insomnia, nausea, pain, rhinitis, viral infection, and vomiting.