Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Emulsion, Ophthalmic [preservative free]:
Restasis: 0.05% (30 ea, 60 ea) [contains polysorbate 80]
Restasis MultiDose: 0.05% (1.5 mL, 5.5 mL) [contains polysorbate 80]
Solution, Ophthalmic [preservative free]:
Cequa: 0.09% (60 ea)
Pharmacokinetics/Pharmacodynamics
Absorption
Serum concentrations were below the quantitation limit of 0.1 ng/mL
Use: Labeled Indications
Keratoconjunctivitis sicca: Increase tear production when suppressed tear production is presumed to be due to keratoconjunctivitis sicca-associated ocular inflammation (in patients not already using topical anti-inflammatory drugs or punctal plugs)
Contraindications
Hypersensitivity to cyclosporine or any component of the formulation.
Dosage and Administration
Dosing: Adult
Keratoconjunctivitis sicca: Ophthalmic: Instill 1 drop in each eye twice daily (approximately 12 hours apart).
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Keratoconjunctivitis sicca: Adolescents ≥16 years: Ophthalmic: Instill 1 drop in each eye every 12 hours
Vernal keratoconjunctivitis (VKC), severe: Limited data available:
Treatment: Children and Adolescents 5 to 14 years: Ophthalmic: Instill 1 drop (0.05%) in affected eye(s) 4 times daily. Dosing based on experience from a prospective trial of 54 pediatric patients (mean age: 9.6 years; range: 5 to 14 years); after 3 months of therapy, improved symptoms were observed, no adverse effects were reported (Keklikci 2008). A case series in six patients (6 to 14 years) treated with 1 drop twice daily or 4 times daily was also shown to improve symptoms; in four patients cyclosporine was weaned after 6 months (n=1) or 12 months (n=3) of therapy; in three other patients, therapy was still ongoing at the time of publication (Ozcan 2007). Higher concentrations of cyclosporine have also shown efficacy in clinical trials (1% and 2%); however, those formulations have a different vehicle and are not commercially available in the US (Vichyanond 2013).
Prevention: Children ≥6 years and Adolescents: Ophthalmic: Instill 1 drop (0.05%) in affected eye(s) twice daily; dosing based on a blinded, comparative (ketotifen) crossover trial in 34 pediatric patients (mean age: 14 ± 7 years) with severe but stable VKC; over a 2-year period, cyclosporine showed a statistically significant reduction in number of recurrences or flare-up compared to ketotifen; both drugs were considered to be well-tolerated (Lambiase 2011)
Administration
Ophthalmic: Administer immediately after opening single-use vial; discard remaining contents after use. Remove contact lenses prior to instillation of drops; may be reinserted 15 minutes after administration. May be used with lubricant eye drops; allow 15-minute interval between products. To avoid contamination, do not touch bottle tip or vial tip to eyelids or other surfaces.
Emulsion 0.05%: Prior to use, invert bottle or vial several times to obtain a uniform emulsion. Prime multidose bottle for first-time use by squeezing 2 drops onto a tissue (do not let bottle tip touch tissue).
Storage
Store at 20°C to 25°C (68°F to 77°F).
Drug Interactions
There are no known significant interactions.
Adverse Reactions
>10%: Ophthalmic: Eye pain (1% to 22%), burning sensation of eyes (17%)
1% to 10%:
Central nervous system: Foreign body sensation of eye (1% to 5%), headache (1% to 5%)
Genitourinary: Urinary tract infection (1% to 5%)
Ophthalmic: Conjunctival hyperemia (1% to 6%), blepharitis (1% to 5%), blurred vision (1% to 5%), epiphora (1% to 5%), eye discharge (1% to 5%), eye irritation (1% to 5%), eye pruritus (1% to 5%), stinging of eyes (1% to 5%), visual disturbance (1% to 5%)
<1%, postmarketing and/or case reports: Hypersensitivity reaction
Warnings/Precautions
Special populations:
- Contact lens wearers: Remove contact lens prior to administration and wait 15 minutes before reinserting.
Dosage form specific issues:
- Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.
Other warnings/precautions:
- Appropriate use: To avoid contamination, do not touch vial tip to eyelids or other surfaces.
Pregnancy
Pregnancy Considerations
Adverse events were not observed following the use of oral cyclosporine in animal reproduction studies. Serum concentrations are below the limit of detection (<0.1 ng/mL) following ophthalmic use; fetal exposure following ophthalmic administration is not expected.
Patient Education
What is this drug used for?
- It is used to help some patients make more tears.
Frequently reported side effects of this drug
- Eye pain
- Eye redness
- Burning
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Vision changes
- Severe eye irritation
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
