Eysuvis®

GoodRx

Loteprednol 0.25% · ophthalmic suspension

Dry Eye/OSD, Steroid

Approved uses

Dry eye disease flare, short course

1 to 2 drops into each eye QID for up to 2 weeks

Korenfeld M, Nichols KK, Goldberg D, Evans D, Sall K, Foulks G, Coultas S, Brazzell K. Safety of KPI-121 ophthalmic suspension 0.25% in patients with dry eye disease: a pooled analysis of 4 multicenter, randomized, vehicle-controlled studies. Cornea. 2021;40(5):564-570 (safety figures). Approval basis from Paton DM. Loteprednol etabonate: a formulation for short-term use in inflammatory flares in dry eye disease. Drugs Today (Barc). 2022;58(2):77-84. Regimen from the FDA label, Dosage and Administration.

Contraindications

Most viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella.
Mycobacterial infection of the eye.
Fungal diseases of ocular structures.

Available Forms

0.25% suspension (loteprednol etabonate 2.5 mg/mL), 8.3 mL in a 10 mL bottle

Mechanism of Action

Corticosteroid: binds and activates the glucocorticoid receptor and is thought to inhibit prostaglandin production, suppressing the edema, fibrin deposition, capillary dilation, leukocyte migration, fibroblast proliferation, and collagen deposition of ocular surface inflammation, while also delaying healing. Lipid soluble and structurally engineered from prednisolone-related compounds for predictable breakdown to the inactive carboxylic acid metabolites PJ-90 and PJ-91, and formulated as mucus-penetrating nanoparticles to cross the tear film mucin barrier; plasma levels stayed below the 1 ng/mL limit of quantitation after 2 drops QID for 14 days in 20 healthy adults.

Warnings & Precautions

Delayed healing and corneal perforation: Topical corticosteroids delay healing and cause corneal and scleral thinning; use over already thin corneal or scleral tissue may lead to perforation.
IOP elevation and glaucoma: Prolonged corticosteroid use may produce glaucoma with optic nerve damage and defects in visual acuity and visual fields; use with caution in the presence of glaucoma.
Posterior subcapsular cataract: Corticosteroid use may produce it.
Prescription renewal: The initial prescription and every renewal only after examination with magnification such as slit lamp biomicroscopy, with fluorescein staining where appropriate, and evaluation of IOP. This label sets no day count, so the gate applies to every refill of a 2-week course.
Secondary ocular infection: Corticosteroids may suppress host response and increase the hazard of secondary ocular infection; in acute purulent conditions of the eye they may mask infection or enhance existing infection.
Viral infection exacerbation: Ocular corticosteroids may prolong the course and worsen the severity of many ocular viral infections including herpes simplex; a history of herpes simplex requires great caution.
Fungal keratitis: Fungal corneal infection is particularly prone to develop coincidentally with long-term local corticosteroid use; consider fungal invasion in any persistent corneal ulceration where a corticosteroid has been used or is in use, and culture when appropriate.
Soft contact lenses: Remove lenses before instillation; the benzalkonium chloride 0.01% preservative may be absorbed by soft lenses, which may be reinserted 15 minutes after administration.

Common Side Effects

Instillation site pain, 5%: The most common adverse reaction in the clinical trials after 2 weeks of use, and the only one the label quantifies.
Pooled trial safety, 4 trials: Across 1 phase 2 and 3 phase 3 vehicle-controlled trials dosed QID for 2 to 4 weeks (1430 on drug, 1438 on vehicle), instillation site pain occurred in 5.2% versus 4.4% and every other adverse event in 0.8% or fewer; an IOP rise of more than 5 mmHg from baseline reaching 21 mmHg or higher occurred in 0.6% versus 0.2%, in trials that excluded patients with current or prior glaucoma.
Corticosteroid class effects: Elevated IOP with infrequent optic nerve damage and visual acuity and field defects, posterior subcapsular cataract formation, delayed wound healing, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where the cornea or sclera is thinned.

Pregnancy & Lactation

Pregnancy: No adequate and well controlled studies in pregnant women, and teratogenicity occurred at clinically relevant doses in rabbits and rats given the drug orally during pregnancy. Oral dosing in pregnant rabbits produced fetal malformations at 1.4 times the recommended human ophthalmic dose (spina bifida including meningocele), exencephaly and craniofacial malformations at 5.6 times, and abortion and embryofetal lethality at 83 times, with no developmental no-adverse-effect level established. Oral dosing in pregnant rats produced malformations at 34 times and embryofetal lethality at 695 times, with a developmental no-adverse-effect level of 3.4 times; in rats dosed from late gestation through lactation, survival of live-born offspring was reduced at 3.4 times. Background U.S. population risk is 2% to 4% for major birth defects and 15% to 20% for miscarriage.

Lactation: No data on presence in human milk, effects on the breastfed infant, or effects on milk production; weigh the developmental and health benefits of breastfeeding against the clinical need for treatment.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.