Ciclosporin (0.05% w/v) is a topical ophthalmic emulsion formulation of a potent calcineurin inhibitor and immunosuppressive agent. It is specifically indicated for increasing tear production in patients with keratoconjunctivitis sicca (severe dry eye disease) whose tear production is presumed to be suppressed due to ocular inflammation. In the Indian context, it is a critical treatment for moderate to severe dry eye disease, a condition prevalent due to environmental factors, high screen time, and underlying autoimmune conditions.
Adult: One drop (approximately 25-30 µL) instilled into each affected eye, twice daily, approximately 12 hours apart.
Note: 1. Wash hands. 2. Shake the vial well before each use to form a uniform, opaque, white emulsion. 3. Remove one vial from the protective pouch. 4. Twist off the tab. 5. Tilt head back, pull lower eyelid down to form a pouch, and instill one drop. 6. Close eyes gently for 1-2 minutes. Do not blink vigorously. 7. Press a finger against the inner corner of the eye (nasolacrimal occlusion) for 2 minutes to minimize systemic drainage. 8. Discard the single-use vial immediately after use. Do not store for later use. 9. Wait at least 15 minutes before instilling any other topical ophthalmic medication.
Ciclosporin is a calcineurin inhibitor. It forms a complex with cyclophilin (an intracellular immunophilin) in T-lymphocytes. This complex binds to and inhibits calcineurin, a calcium/calmodulin-dependent phosphatase. Inhibition of calcineurin prevents the dephosphorylation and nuclear translocation of the cytosolic component of the nuclear factor of activated T-cells (NF-AT). This subsequently inhibits the transcription and production of key inflammatory cytokines, particularly Interleukin-2 (IL-2). In the ocular surface, this action reduces T-cell mediated inflammation of the lacrimal gland and conjunctiva, which is a key pathophysiological factor in dry eye disease, thereby allowing the restoration of tear production.
Pregnancy: Pregnancy Category C. Animal studies have shown fetotoxicity at high systemic doses. No adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Topical administration minimizes systemic exposure.
Driving: May cause transient blurred vision immediately after instillation. Patients should be advised not to drive or operate machinery until their vision clears.
| Topical Ocular Corticosteroids (e.g., Loteprednol, Prednisolone) | Synergistic anti-inflammatory effect. However, concomitant use may mask signs of infection or increase risk of elevated IOP. Monitoring required. | Moderate |
| Systemic CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Diltiazem, Grapefruit juice) | Theoretically could increase systemic ciclosporin levels, but risk is minimal with topical use. Caution advised. | Low |
| Systemic CYP3A4 Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine, St. John's Wort) | Theoretically could decrease systemic ciclosporin levels, irrelevant for topical efficacy. No action needed. | Low |
Same composition (Ciclosporin (0.05% w/v)), different brands: