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Cyclosporine inhibits calcineurin in T-lymphocytes, suppressing IL-2 production and T-cell proliferation. In the eye, this reduces immune-mediated inflammation of lacrimal gland tissue, increasing natural tear production and reducing corneal cell apoptosis.
Commercial cyclosporine eye drops (Restasis 0.05%, Cequa 0.09%) are available only at fixed concentrations. Compounded cyclosporine allows higher concentrations (0.1–0.2%) for refractory cases not adequately managed on commercial formulations, as well as preservative-free unit-dose vials for patients with preservative sensitivity.
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Cyclosporine ophthalmic emulsion targets the underlying inflammatory cause of dry eye disease rather than just providing lubrication. By suppressing T-cell mediated inflammation in the lacrimal gland and ocular surface, it helps restore normal tear production over time.
Restasis (0.05%) and Cequa (0.09%) are FDA-approved but extremely expensive. Compounded cyclosporine offers identical active ingredients at a fraction of the cost and allows higher concentrations for patients with severe or refractory disease.
T-Cell Calcineurin Inhibition
Cyclosporine binds to cyclophilin (an intracellular immunophilin), and the cyclosporine-cyclophilin complex inhibits calcineurin. This blocks dephosphorylation of NFAT transcription factors, suppressing T-cell production of IL-2 and other pro-inflammatory cytokines.
Lacrimal Gland Protection
In dry eye disease, T-lymphocyte-mediated inflammation damages lacrimal gland acinar cells, reducing tear production. Cyclosporine suppresses this immune attack, allowing lacrimal gland function to recover — increasing natural aqueous tear production over time.
Apoptosis Reduction
Cyclosporine also reduces apoptosis (programmed cell death) of conjunctival and corneal epithelial cells induced by pro-inflammatory cytokines, improving ocular surface integrity.
Chronic dry eye disease (keratoconjunctivitis sicca), Sjögren's syndrome, graft-versus-host disease (GVHD) ocular involvement, post-LASIK dry eye, vernal keratoconjunctivitis, ocular rosacea, refractory meibomian gland dysfunction
Vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC), graft-versus-host disease (GVHD) ocular surface involvement, superior limbic keratoconjunctivitis, post-LASIK or post-refractive surgery dry eye, ocular rosacea-associated dry eye
Standard (0.05%): 1 drop per eye twice daily (12 hours apart)
Refractory disease (0.1%): Per physician protocol
Onset: Improvement seen at 3–6 months; full benefit at 6–12 months
Bridging: Artificial tears may be used between doses
Begin with 1 drop per eye twice daily, 12 hours apart. No dose titration is needed. Consistency is critical — missed doses reduce efficacy. Use artificial tears 15 minutes after cyclosporine drops if needed for comfort. If using corticosteroid drops initially (as a bridge for rapid onset), taper per prescriber guidance after 1–3 months once cyclosporine takes effect.
Ophthalmic Solution 0.05% — equivalent to Restasis; FDA-approved concentration; standard starting dose for most patients
Ophthalmic Solution 0.1% — double the commercial concentration; used for moderate-to-severe disease or partial non-responders to 0.05%
Ophthalmic Solution 0.2% — highest concentration; reserved for refractory cases or GVHD-associated severe dry eye
Preservative-free Vials — unit-dose preservative-free preparations for patients with preservative sensitivity or intolerance
Transient burning and stinging on instillation (most common, typically improves over weeks). No significant systemic absorption at ophthalmic doses. No steroid-related side effects. Safe for long-term use.
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