Restasis
Restasis
Generic Name
Restasis
Mechanism
- Cyclosporine A blocks the protease calcium‑dependent phosphatase calcineurin, preventing the transcription of pro‑inflammatory cytokines from T‑lymphocytes.
- This reduction in IL‑2, IL‑5, and IFN‑γ lowers ocular surface inflammation, restores tear‑film stability, and increases aqueous tear secretion.
- The effect is dose‑related and slow‑onset, typically appearing after 3–6 weeks of consistent use.
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Pharmacokinetics
| Parameter | Detail |
| Absorption | Primarily via tear film; limited systemic exposure (<0.001 % of applied dose). |
| Distribution | Local ocular tissues: conjunctiva, cornea, and lacrimal glands. |
| Metabolism | Predominantly cytochrome P450 3A4 in conjunctival cells; minimal first‑pass metabolism. |
| Elimination | Tear drainage; negligible systemic clearance. |
| Half‑life | Ocular half‑life ≈12 h; systemic half‑life ~7 days (but <1 % absorbed). |
Clinical relevance: Systemic cyclosporine‑related toxicity (renal, hepatic) is negligible with topical use.
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Indications
- Dry eye disease (keratoconjunctivitis sicca) secondary to ocular surface inflammation, including:
- Sjögren’s syndrome
- Non‑Sjögren’s dry eye
- Improves corneal staining, visual acuity, and patient‑reported comfort.
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Contraindications
| Contraindications | Warnings |
| Infections of the eye (e.g., herpetic keratitis) | Uncontrolled systemic hypertension |
| Known hypersensitivity to cyclosporine or any emulsion component | Pregnancy: Category B (limited data); avoid if possible |
| Use of other topical immunosuppressants (e.g., tacrolimus) without physician approval | Children <12 y: clinical studies limited |
| Active ocular inflammation requiring corticosteroids | Potential for ocular irritation; monitor for worsening inflammation |
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Dosing
- Standard regimen:
- Instill 1 drop in the affected eye twice daily (morning & evening).
- Use after washing hands and before bedtime to allow tear film residence.
- Continue for ≥12 weeks; can be extended for chronic disease.
- Loading protocol (optional):
- 3 times daily for 2 weeks → 2 times daily thereafter.
Tip: Do not remove the cap when dispensing; keep the bottle on the eye to pre‑load the drop for quick use.
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Adverse Effects
- Common (≤10 %):
- Ocular burning or irritation
- Blurred vision (transient)
- Conjunctival injection
- Hypopyon, if severe inflammation develops
- Serious (≤1 %):
- Herpes simplex keratitis (rare)
- Ocular surface ulceration or perforation (rare)
- Severe conjunctival inflammation → require discontinuation
Mitigation: Use warm compresses, lubricating drops; monitor for signs of infection.
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Monitoring
| Parameter | Frequency | Rationale |
| Ocular exam (visual acuity, slit‑lamp) | Every 4 weeks | Detect early keratitis or stromal changes |
| Dry eye scoring (Ocular Surface Disease Index) | Every 8 weeks | Gauge symptom improvement |
| Tear breakup time | Every 2 months | Evaluate tear film stability |
| Serum renal/hepatic function (as needed) | Only if systemic immunosuppressants added | Prevent cumulative toxicity |
| Infectious signs | Immediate | Prompt treatment of herpes or bacterial keratitis |
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Clinical Pearls
- Start low, go slow: Many patients need 8–12 weeks to feel benefit; a short trial (≤4 weeks) does not predict response.
- No “wash‑out” needed: If treatment is stopped for 2 weeks, effectiveness returns only after re‑initiation, so steady use is critical.
- Pediatric use: Short‑term (≤8 weeks) has been used successfully under close supervision; data for long‑term safety remain limited.
- Combination therapy: Can be safely combined with lubricating gels, cyclosporine‐free artificial tears, and oral antihistamines for allergic conjunctivitis.
- Eye patching and contact lenses: Do not remove the cap when a patient needs to use drop immediately; it helps avoid wastage and contamination.
- Cosmetic considerations: Some patients report mild blue discoloration of the bulbar conjunctiva after prolonged use; reassure that it is benign and reversible.
- Adherence boosters: Provide a drop‑card or smartphone reminder; 2‑dose regimen is more likely to be followed than 3‑dose.
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