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Cyclosporine ophthalmic

RESTASIS

Pronunciation: SYE-kloe-spor-een

Cyclosporine ophthalmic ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Cyclosporine ophthalmic ballicule

What it isOphthalmic calcineurin inhibitor that reduces ocular-surface inflammation; chronic dry-eye disease.

Why this oneModifies inflammatory dry eye rather than merely lubricating and avoids steroid-related glaucoma and cataracts.

What limits itBurning and stinging commonly derail adherence, especially because meaningful benefit develops slowly.

Cyclosporine ophthalmic molecular structure (skeletal formula)
Molecular structure: Cyclosporine ophthalmic

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityOcular burning (17 %) and stinging; keep the bottle tip off the eye; remove contact lenses before use. Not detected in blood after ocular use.

FDA label

NO BOXED WARNINGS

FDA dosingPopulationStartTargetMax
Increase tear production in keratoconjunctivitis sicca (ocular inflammation)Adults1 drop each eye BID1 drop each eye BID (~12 h apart)1 drop each eye BID

Renal Undefined

Hepatic Undefined

Instill the two eye doses approximately 12 hours apart

Instructions

Available strengths

Cautions

Adverse reactions

Pregnancy Not detected systemically after topical ocular use; maternal use not expected to result in fetal exposure

Lactation Blood concentrations undetectable after topical use; exercise caution when administered to a nursing woman

Cost

Cyclosporine ophthalmic (RESTASIS)
Strength#/mogeneric $/unitCostPlus
0.05 %emulsionper unitnot offered
0.1 %emulsionper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Cyclosporine ophthalmic is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Other forms: Cyclosporine (NEORAL)

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