Class: Anti-inflammatory Agents, Miscellaneous
VA Class: IM600
Chemical Name: Cyclo[[(E)-(2S,3R,4R)-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]
CAS Number: 59865-13-3
Medically reviewed by Drugs.com. Last updated on March 23, 2020.
Uses for cycloSPORINE (EENT)
Used to increase tear production in adults whose tear production presumably is suppressed secondary to ocular inflammation related to keratoconjunctivitis sicca.1
Increased tear production not observed in patients already receiving topical anti-inflammatory agents or using punctal plugs.1
cycloSPORINE (EENT) Dosage and Administration
Apply topically to the eye as an ophthalmic emulsion.1
Avoid contamination of emulsion container.1
Invert unit-dose vial a few times before use to obtain a uniform, opaque, white emulsion.1
Preservative-free emulsion is for single use only in one or both eyes; discard any unused portion immediately after administration.1
Remove contact lenses prior to administration; may reinsert lenses 15 minutes after dose.1
When used concomitantly with artificial tears, administer ophthalmic preparations at least 15 minutes apart.1
1 drop of a 0.05% emulsion into each eye twice daily, approximately 12 hours apart.1
Cautions for cycloSPORINE (EENT)
Known hypersensitivity to cyclosporine or any ingredient in the formulation.1
Active ocular infections.1
Safety and efficacy not established in patients with history of herpes keratitis.1
Safety and efficacy not established in children <16 years of age.1
No substantial differences in safety and efficacy relative to younger adults.1
Common Adverse Effects
Ocular burning, conjunctival hyperemia, discharge, epiphora, ocular pain, foreign body sensation, pruritus, stinging, visual disturbance (e.g., blurring).1
Interactions for cycloSPORINE (EENT)
No formal drug interaction studies to date.9
cycloSPORINE (EENT) Pharmacokinetics
Blood cyclosporin A concentrations were below quantitation limit (0.1 ng/mL) after topical application of cyclosporine 0.05% emulsion to the eye twice daily for up to 12 months.1 7 No detectable drug accumulation in blood during 12 months of treatment.1 7
Not known whether distributed into milk after topical application to the eye.1
Exhibits immunosuppressive activity when administered systemically.1
Advice to Patients
Importance of learning and adhering to proper administration techniques to avoid contamination of the product.1
Importance of administering ophthalmic emulsion immediately after opening single-use vial and discarding any unused portion immediately after administration.1
Importance of not wearing contact lenses in presence of decreased tear production.1 If contact lenses are worn, importance of removing lenses prior to administration and delaying reinsertion of lenses for 15 minutes after instillation.1
Importance of women informing clinicians if they are or plan to become pregnant or to breast-feed.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
If using artificial tears and ophthalmic cyclosporine, importance of allowing at least 15 minutes to elapse between administration.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
AHFS DI Essentials™. © Copyright 2021, Selected Revisions April 1, 2010. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Allergan, Inc. Restasis (cyclosporine) ophthalmic emulsion 0.05% prescribing information. Irvine, CA; 2002 Dec.
2. Sall K, Stevenson OD, Mundorf TK et al. Two multicenter, randomized studies of the efficacy and safety of cyclosporine ophthalmic emulsion in moderate to severe dry eye disease. Ophthalmology. 2000; 107:631-9. http://www.ncbi.nlm.nih.gov/pubmed/10768324?dopt=AbstractPlus
3. Stevenson D, Tauber J, Reis BL et al. Efficacy and safety of cyclosporin A ophthalmic emulsion in the treatment of moderate-to-severe dry eye disease. A dose-ranging randomized trial. Ophthalmology. 2000; 107:967-74. http://www.ncbi.nlm.nih.gov/pubmed/10811092?dopt=AbstractPlus
4. Allergan, Inc, Irvine, CA: Personal communication.
5. Laibovitz R, Solch S, Andriano K et al. Pilot trial of cyclosporine 1% ophthalmic ointment in the treatment of keratoconjunctivitis sicca. Cornea. 1993; 12:315-23. http://www.ncbi.nlm.nih.gov/pubmed/8339560?dopt=AbstractPlus
6. Tauber J, for the Cyclosporine Study Group. A dose-ranging clinical trial to assess the safety and efficacy of cyclosporine ophthalmic emulsion in patients with keratoconjunctivitis sicca. Adv Exp Med Biol. 1998; 438:969-72. http://www.ncbi.nlm.nih.gov/pubmed/9634996?dopt=AbstractPlus
7. Small DS, Acheampong A, Reis B et al. Blood cyclosporin A during long-term treatment with cyclosporin A ophthalmic emulsions in patients with moderate to severe dry eye disease. J Ocul Pharmacol Ther. 2002; 18:411-8. http://www.ncbi.nlm.nih.gov/pubmed/12419092?dopt=AbstractPlus
8. Kunert KS, Tisdale AS, Gipson IK. Goblet cell numbers and epithelial proliferation in the conjunctiva of patients with dry eye syndrome treated with cyclosporine. Arch Ophthalmol. 2002; 120:330-7. http://www.ncbi.nlm.nih.gov/pubmed/11879137?dopt=AbstractPlus
9. Allergan, Inc. Restasis (cyclosporine ophthalmic emulsion) 0.05% formulary kit. Irvine, CA; 2003.
10. Anon. Ophthalmic cyclosporine (Restasis) for dry eye disease. Med Lett Drugs Ther. 2003; 45:42-3. http://www.ncbi.nlm.nih.gov/pubmed/12766701?dopt=AbstractPlus
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- Drug class: ophthalmic anti-inflammatory agents