Cyclosporine Eye Drops for Dry Eye Syndrome
Topical cyclosporine 0.05% eye drops should be administered twice daily, approximately 12 hours apart, for the treatment of moderate to severe dry eye syndrome. 1, 2
Mechanism of Action and Indications
Cyclosporine is an immunomodulatory agent that:
- Acts as a partial immunomodulator in patients with tear production suppressed due to ocular inflammation
- Prevents activation and nuclear translocation of cytoplasmic transcription factors required for T-cell activation
- Inhibits inflammatory cytokine production and mitochondrial pathways of apoptosis 1
Cyclosporine 0.05% ophthalmic emulsion (Restasis) is FDA-approved for:
- Moderate to severe dry eye syndrome where tear production is presumed to be suppressed due to ocular inflammation
- Patients who have not responded adequately to artificial tears 1, 2
Standard Treatment Regimen
Dosing:
- Apply one drop in each affected eye twice daily, approximately 12 hours apart 2
- Invert the vial before using
- Use immediately after opening and then discard the single-use vial 2
Duration:
- Long-term therapy is typically required
- Clinical trials demonstrated significant improvement after 6 months of treatment 1, 2
- The dose can be decreased to once daily in some patients after 1 full year of twice-daily therapy without decreased efficacy 1
Efficacy and Expected Outcomes
- Increases Schirmer wetting test results by 10 mm compared to vehicle at 6 months in approximately 15% of treated patients (vs. 5% with vehicle) 1, 2
- Demonstrates success rates of 74%, 72%, and 67% in mild, moderate, and severe dry eye patients, respectively 1
- May provide prolonged improvement of dry eye signs even after discontinuation, with benefits lasting a median of 20 months in some patients 1
- May act as a disease-modifying agent for dry eye disease 1
Treatment Algorithm
First-line therapy: Preservative-free artificial tears containing methylcellulose or hyaluronate, applied at least twice daily and increased as needed based on symptom severity 3
For moderate dry eye (when artificial tears provide insufficient relief):
For severe or refractory cases:
- Some patients with severe dry eye may require more frequent dosing (3-4 times daily) 4
- Consider short-term topical corticosteroids (2-4 weeks) to rapidly reduce inflammation before or alongside cyclosporine 1, 3
- Consider punctal occlusion in addition to cyclosporine for patients with inadequate response 1, 3
Common Side Effects and Management
- Ocular burning reported in 17% of patients 1
- Other potential side effects include redness, irritation, and eyelid swelling 5
- Side effects are typically transient and diminish with continued use
- No increase in bacterial or fungal ocular infections has been reported 2
- No detectable drug accumulation in blood during 12 months of treatment 2
Special Considerations
- Cyclosporine eye drops are licensed for severe keratitis in dry eye disease that has not responded to treatment with tear substitutes 1
- Blood concentrations remain below quantitation limit (0.1 ng/mL) with topical administration 2
- Increased efficacy is not seen in patients currently taking topical anti-inflammatory drugs or using punctal plugs 2
- Store at 15-25°C (59-77°F) and keep vials in the thermoformed tray until use 2
Monitoring and Follow-up
- Evaluate response after 3-6 months of continuous therapy
- Monitor for improvement in:
Cyclosporine eye drops represent an important second-line therapy for moderate to severe dry eye syndrome, particularly when artificial tears alone are insufficient to control symptoms and signs of ocular surface inflammation.