CYCLOSPORINE

Cyclosporine ophthalmic emulsion, 0.05% contains a topical calcineurin inhibitor immunosuppressant with anti-inflammatory effects. Cyclosporine’s chemical name is Cyclo[[( E )-(2 S ,3 R ,4 R )-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl]-L-2-aminobutyryl- N -methylglycyl- N -methyl-L-leucyl-L-valyl- N -methyl-L-leucyl-L-alanyl-D-alanyl- N -methyl-L-leucyl- N -methyl-L-leucyl- N -methyl-L-valyl] and it has the following structure: Structural Formula Formula: C 62 H 111 N 11 O 12 Mol. Wt.: 1202.6 Cyclosporine is a fine white powder. Cyclosporine ophthalmic emulsion appears as a white opaque to slightly translucent homogeneous emulsion. It has an osmolality of 230 to 320 mOsmol/kg and a pH of 6.5-8.0. Each mL of cyclosporine ophthalmic emulsion, 0.05% contains: Active: cyclosporine 0.05%. Inactives : glycerin; castor oil; polysorbate 80; carbomer copolymer type A; purified water; and sodium hydroxide to adjust pH. cyclosporine

Cyclosporine ophthalmic emulsion, 0.05% is indicated to increase tear production in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca. Increased tear production was not seen in patients currently taking topical anti-inflammatory drugs or using punctal plugs. Cyclosporine ophthalmic emulsion, 0.05% is a calcineurin inhibitor immunosuppressant indicated to increase tear production in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca. Increased tear production was not seen in patients currently taking topical anti-inflammatory drugs or using punctal plugs. ( 1 )

Invert the unit dose vial a few times to obtain a uniform, white, opaque emulsion before using. Instill one drop of cyclosporine ophthalmic emulsion, 0.05% twice a day in each eye approximately 12 hours apart. Cyclosporine ophthalmic emulsion can be used concomitantly with lubricant eye drops, allowing a 15-minute interval between products. Discard vial immediately after use. Instill one drop of cyclosporine ophthalmic emulsion, 0.05% twice a day in each eye approximately 12 hours apart. ( 2 )

Cyclosporine ophthalmic emulsion is contraindicated in patients with known or suspected hypersensitivity to any of the ingredients in the formulation. Hypersensitivity ( 4 )

The following serious adverse reactions are described elsewhere in the labeling: Potential for Eye Injury and Contamination [ see Warnings and Precautions ( 5.1 ) ] The most common adverse reaction following the use of -cyclosporine ophthalmic emulsion was ocular burning (17%). ( 6.1 ) To Report SUSPECTED ADVERSE REACTIONS, contact KVK-Tech, Inc. at 1-800-862-3895 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In clinical trials, the most common adverse reaction following the use of cyclosporine ophthalmic emulsion was ocular burning (17%). Other reactions reported in 1% to 5% of patients included conjunctival hyperemia, discharge, epiphora, eye pain, foreign body sensation, pruritus, stinging, and visual disturbance (most often blurring). 6.2 Post-marketing Experience The following adverse reactions have been identified during post approval use of cyclosporine ophthalmic emulsion. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Reported reactions have included: hypersensitivity (including eye swelling, urticaria, rare cases of severe angioedema, face swelling, tongue swelling, pharyngeal edema, and dyspnea); and superficial injury of the eye (from the vial tip touching the eye during administration).