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CycloSPORINE (Ophthalmic)

Medically reviewed by Drugs.com. Last updated on Oct 15, 2020.

Pronunciation

(SYE kloe spor een)

Index Terms

  • Cequa
  • Ciclosporin
  • CsA
  • CyA
  • Cyclosporin A

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) [contains cremophor el]

Brand Names: U.S.

  • Cequa
  • Restasis
  • Restasis MultiDose

Pharmacologic Category

  • Calcineurin Inhibitor
  • Immunosuppressant Agent

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.

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:

Emulsion 0.05% (eg, Restasis): Adolescents ≥16 years: Ophthalmic: Instill 1 drop in each eye every 12 hours.

Solution 0.09% (eg, Cequa): Adolescents ≥18 years: Ophthalmic: Instill 1 drop in each eye every 12 hours.

Vernal keratoconjunctivitis, severe:

Treatment:

Ophthalmic emulsion 0.05% (Restasis): Limited data available: Children ≥5 years and ≤14 years: Ophthalmic: Instill 1 drop 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 6 patients (6 to 14 years) treated with 1 drop twice daily or 4 times daily was also shown to improve symptoms; in 4 patients cyclosporine was weaned after 6 months (n=1) or 12 months (n=3) of therapy; in 3 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).

Ophthalmic emulsion 0.1% (Verkazia [Canadian product]): Children ≥4 years and Adolescents: Ophthalmic: Instill 1 drop 4 times daily; after clinical response established, may consider reduced daily dose to 1 drop twice daily; discontinue treatment after resolution of signs and symptoms; safety and efficacy has not been evaluated past 12 months of therapy (Leonardi 2019).

Prevention: Limited data available:

Ophthalmic emulsion 0.05% (eg, Restasis): Children ≥6 years and Adolescents: Ophthalmic: Instill 1 drop 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 vernal keratoconjunctivitis; 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

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>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 Considerations

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.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Eye pain

• Eye redness

• Burning

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Vision changes

• Severe eye irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, 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 limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.