Restasis 0.05% Ophthalmic Emulsion

Key Features

How does Restasis 0.05% Ophthalmic Emulsion Work?

• Bind to cyclophilin-binding-protein complex that inhibits calcineurin phosphatase
• Inhibition of dephosphorylation and subsequent nuclear translocation of Nuclear factor of activated T-cells (NFAT).
• Blocking the transcription of genes that code for IL-2 and other inflammatory cytokines
• Suppressed proliferation and activity of T-helper cells and cytotoxic T-cells

Uses

• Increased tear production: Restores natural tear production in many patients with inflammation-related dry eye.
• Reduced ocular surface inflammation: Diminishes the inflammatory milieu that impairs lacrimal gland and ocular surface function.
• Improved comfort and visual stability: With better tear quality and volume, patients frequently report reduced irritation and more stable vision for sustained visual tasks.

Dosage

• Usually taken as a drop in each eye, twice a day and can be taken approx. 12 hours apart.
• It can be used only after consulting a medical professional or healthcare professional.

Side effects

• Nephrotoxicity
• Hypertension
• Tremor
• Headache
• Hyperlipidemia
• Hyperglycemia
• Ghirsutism excess hair growth
• Gum Hyperplasia

Interactions

• Strong CYP3A4 inhibitors ketoconazole, erythromycin, diltiazem increases the cyclosporine level.
• CYP3A4 inducers rifampin, phenytoin may lead to decrease cyclosporine levels
• Other immunosuppressants may show addictive effect, increased infection/cancer risk.

Pharmacokinetics

• It may show variable absorption approx. 30%
• It is highly lipophilic and may distributes widely into tissue, including fat, liver, pancreas and kidney.
• Hepatic via CYP3A4 extensive first-pass metabolism.
• It is excreted through primarily biliary approx. 90% and less than 1% through urine.

Precautions

• Avoid use in patients with known hypersensitivity to cyclosporine or any excipient.
• Treat active ocular infections before initiating an immunomodulatory topical therapy.
• Use caution in patients with significant ocular surface disease or prior ocular surgery discuss with your ophthalmologist.
• Pregnancy & breastfeeding: limited controlled data exist; weigh risks and benefits with your clinician.

Conclusion

Restasis 0.05% Ophthalmic Emulsion is a safe and effective formulation for the patients with inflammation-related chronic dry eye (keratoconjunctivitis sicca) and Sjogren’s syndrome. It works by reducing ocular surface inflammation to allow increased natural tear production over time. The safety profile is dominated by local ocular effects such as transient burning or irritation; serious adverse events are uncommon when the product is used as directed. Always use under prescription and follow up with your eye care provider for monitoring and combined dry-eye management. Restasis treats underlying inflammation to improve natural tear production and is not a simple lubricating artificial tear.

References

• https://pmc.ncbi.nlm.nih.gov/articles/PMC4420022/
• https://pubchem.ncbi.nlm.nih.gov/patent/US-2010016219-A1

FAQ’s