Introduction
Eysuvis (loteprednol etabonate ophthalmic suspension 0.25%) is a topical corticosteroid specifically formulated for short-term treatment of ocular inflammation and pain associated with dry eye disease. Approved by the FDA in October 2020, it represents the first corticosteroid indicated specifically for dry eye disease, offering a targeted approach to managing inflammatory components of this common condition.
Mechanism of Action
Loteprednol etabonate is a site-active corticosteroid that undergoes rapid metabolic deactivation. It binds to glucocorticoid receptors in ocular tissues, modulating the expression of genes involved in inflammatory processes. The drug inhibits the migration of polymorphonuclear leukocytes and reverses increased capillary permeability, thereby reducing edema, fibrin deposition, capillary dilation, and phagocytic migration. Its unique ester-based structure allows for effective anti-inflammatory activity while minimizing systemic absorption and side effects due to rapid hydrolysis to inactive metabolites.
Indications
- FDA-approved for the short-term (up to 2 weeks) treatment of ocular inflammation and pain associated with dry eye disease
- Off-label uses may include treatment of other ocular inflammatory conditions, though specific approval for these uses is lacking
Dosage and Administration
Standard dosing: Instill one drop into the affected eye(s) four times daily Duration: Treatment should not exceed 2 weeks Administration technique:- Shake well before use
- Wash hands before administration
- Avoid touching dropper tip to any surface to prevent contamination
- Wait at least 10 minutes between instilling multiple ophthalmic medications
- Pediatric patients: Safety and effectiveness not established
- Geriatric patients: No dosage adjustment required
- Hepatic impairment: No specific recommendations
- Renal impairment: No specific recommendations
Pharmacokinetics
Absorption: Limited systemic absorption following ocular administration. Peak plasma concentrations are low and transient. Distribution: Primarily localized to ocular tissues with minimal systemic distribution. Metabolism: Undergoes rapid hydrolysis to inactive metabolites (PJ-91 and PJ-90) primarily in the cornea and aqueous humor. Elimination: Systemic elimination follows pathways typical of corticosteroids. Half-life in ocular tissues is approximately 2-3 hours. Protein binding: Extensive binding to glucocorticoid receptors in target tissues.Contraindications
- Hypersensitivity to loteprednol etabonate or any component of the formulation
- Active ocular infections including most viral diseases of the cornea and conjunctiva
- Ocular mycobacterial infections
- Fungal diseases of the ocular structures
Warnings and Precautions
Prolonged use: May result in glaucoma, optic nerve damage, visual acuity defects, cataract formation, or secondary ocular infections Steroid response: May increase intraocular pressure (IOP) in susceptible individuals; monitor IOP regularly Infection risk: May mask or enhance existing infection; if infections do not respond promptly, discontinue use Perforation risk: Use with caution in patients with corneal thinning or history of corneal perforation Contact lens wear: Should not be used while wearing contact lenses Surgical patients: May delay healing after ocular surgery Pregnancy: Category C - Use only if potential benefit justifies potential risk to fetus Lactation: Exercise caution when administering to nursing womenDrug Interactions
- No formal drug interaction studies conducted
- Theoretical interactions with other corticosteroids may result in additive effects
- Patients receiving other immunosuppressive agents may have increased risk of infection
- May affect glucose control in diabetic patients
Adverse Effects
Most common (>5%):- Eye pain (12%)
- conjunctival hyperemia (10%)
- visual acuity reduced (7%)
- foreign body sensation (6%)
- Eye irritation
- itching
- discharge
- dry eye
- headache
- increased lacrimation
- photophobia
- conjunctival edema
- corneal staining
- blepharitis
- dysgeusia
- Elevated intraocular pressure
- Cataract formation
- Corneal perforation
- Secondary ocular infections
- Optic nerve damage
Monitoring Parameters
- Intraocular pressure at baseline and during treatment
- Visual acuity assessment
- Slit-lamp examination for signs of infection
- Corneal integrity evaluation
- Signs of steroid response (increased IOP, posterior subcapsular cataract formation)
- Resolution of inflammatory signs and symptoms
- Patient-reported symptom improvement
Patient Education
- Use exactly as prescribed; do not exceed recommended duration
- Shake bottle well before each use
- Do not touch dropper tip to any surface
- Wait at least 10 minutes between different eye medications
- Do not wear contact lenses during treatment
- Report any worsening symptoms, eye pain, vision changes, or signs of infection immediately
- Attend all follow-up appointments for pressure checks
- Store at room temperature (15-25°C); do not freeze
- Discard bottle 28 days after opening
- Inform all healthcare providers about Eysuvis use, especially before eye surgery
References
1. FDA prescribing information: Eysuvis (loteprednol etabonate ophthalmic suspension) 0.25% 2. Holland EJ, et al. Loteprednol Etabonate 0.25% for the Treatment of Dry Eye Disease: A Phase 3, Randomized, Double-Masked, Placebo-Controlled Study. Cornea. 2020;39(10):1234-1240. 3. Sheppard JD, et al. Loteprednol Etabonate 0.25% for the Treatment of Signs and Symptoms of Dry Eye Disease: A Systematic Review. Clin Ophthalmol. 2021;15:3189-3200. 4. American Academy of Ophthalmology. Dry Eye Syndrome Preferred Practice Pattern. 2018. 5. Novack GD, et al. Ophthalmic corticosteroids and their use in dry eye disease. Surv Ophthalmol. 2022;67(2):301-331. 6. ClinicalTrials.gov: Phase 3 Study of Loteprednol Etabonate Ophthalmic Suspension 0.25% in Dry Eye Disease (NCT03527277)