Cyclosporine
Cyclosporine Prescribing Information
Cyclosporine ophthalmic emulsion 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.
Invert the unit dose vial a few times to obtain a uniform, white, opaque emulsion before using. Instill one drop of cyclosporine ophthalmic emulsion 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.
Ophthalmic emulsion containing cyclosporine 0.5 mg/mL
Clinical administration of cyclosporine ophthalmic emulsion 0.05% is not detected systemically following topical ocular administration [
Blood cyclosporine A concentrations were measured using a specific high pressure liquid chromatography-mass spectrometry assay. Blood concentrations of cyclosporine, in all the samples collected, after topical administration of cyclosporine ophthalmic emulsion 0.05%, twice daily, in humans for up to 12 months, were below the quantitation limit of 0.1 ng/mL. There was no detectable drug accumulation in blood during 12 months of treatment with cyclosporine ophthalmic emulsion.
At maternally toxic doses (30 mg/kg/day in rats and 100 mg/kg/day in rabbits), cyclosporine oral solution (USP) was teratogenic as indicated by increased pre- and postnatal mortality, reduced fetal weight and skeletal retardations. These doses (normalized to body surface area) are 5,000 and 32,000 times greater, respectively, than the daily recommended human dose of one drop (approximately 28 mcL) of cyclosporine ophthalmic emulsion 0.05% twice daily into each eye of a 60 kg person (0.001 mg/kg/day), assuming that the entire dose is absorbed. No evidence of embryofetal toxicity was observed in rats or rabbits receiving cyclosporine during organogenesis at oral doses up to 17 mg/kg/day or 30 mg/kg/day, respectively. These doses in rats and rabbits are approximately 3,000 and 10,000 times greater, respectively, than the daily recommended human dose.
An oral dose of 45 mg/kg/day cyclosporine administered to rats from Day 15 of pregnancy until Day 21 postpartum produced maternal toxicity and an increase in postnatal mortality in offspring.
This dose is 7,000 times greater than the daily recommended human dose. No adverse effects in dams or offspring were observed at oral doses up to 15 mg/kg/day (2,000 times greater than the daily recommended human dose).
Cyclosporine ophthalmic emulsion is contraindicated in patients with known or suspected hypersensitivity to any of the ingredients in the formulation.
• To avoid the potential for eye injury and contamination, be careful not to touch the vial tip to your eye or other surfaces. ()5.1 Potential for Eye Injury and ContaminationBe careful not to touch the vial tip to your eye or other surfaces to avoid potential for eye injury and contamination.