Ilevro®
Nepafenac 0.3% · ophthalmic suspension
NSAID
Approved uses
Pain and inflammation associated with cataract surgery
One drop QD to the affected eye from 1 day before surgery through the first 2 weeks postoperatively, with an additional drop 30 to 120 minutes preoperatively.
Once-daily dosing is noninferior to TID nepafenac 0.1%, with 91% pain free at day 14.
OFF-LABELNot in the FDA label for this product
Prevention of macular edema after cataract surgery in diabetic retinopathy
One drop QD starting the day before surgery and continued for 90 days after surgery, the regimen used in both trials.
2 RCTs · n=1220 · BCVA mixed
Two prospective, randomized, multicenter, double-masked, vehicle-controlled phase 3 studies in patients with diabetes (615 and 605 patients). Macular edema, defined as a 30% or greater rise in central subfield macular thickness from preoperative baseline, occurred within 90 days in 2.3% versus 17.3% (P < 0.001) and 5.9% versus 14.3% (P = 0.001), pooled 4.1% versus 15.9% (P < 0.001); the endpoint of a 15-letter or greater BCVA improvement, gained through day 14 and maintained through day 90, separated from vehicle in study 1 (61.7% versus 43.0%, P < 0.001) but not in study 2 (48.8% versus 50.5%, P = 0.671).
Contraindications
Hypersensitivity to any ingredient in the formulation or to other NSAIDs.
Available Forms0.3% ophthalmic suspension, 1.7 mL in a 4 mL bottle, 3 mL in a 4 mL bottle
Mechanism of ActionNonsteroidal anti-inflammatory prodrug: after topical ocular dosing it penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, an NSAID. Parent drug and amfenac are thought to inhibit prostaglandin H synthase (cyclooxygenase), the enzyme required for prostaglandin production.
Warnings & Precautions
- Corneal effects: Topical NSAIDs may cause keratitis, and continued use in susceptible patients may progress to epithelial breakdown, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation, any of which may be sight threatening. Discontinue immediately on evidence of corneal epithelial breakdown and monitor corneal health closely.
- Higher-risk corneas: Postmarketing experience with topical NSAIDs suggests complicated ocular surgery, corneal denervation, corneal epithelial defects, diabetes mellitus, ocular surface disease such as dry eye, rheumatoid arthritis, and repeat ocular surgery within a short period may raise the risk of sight-threatening corneal events; use with caution in these patients.
- Extended perioperative use: Postmarketing experience with topical NSAIDs also suggests use more than 1 day before surgery, or beyond 14 days after surgery, may increase the risk and severity of corneal adverse events.
- Increased bleeding time: Interference with thrombocyte aggregation; ocularly applied NSAIDs have been reported to increase bleeding of ocular tissues, including hyphema, in conjunction with ocular surgery. Use caution with known bleeding tendencies or with drugs that prolong bleeding time.
- Delayed healing: Topical NSAIDs may slow or delay healing, and concomitant topical corticosteroids, which also delay healing, may increase the potential for healing problems.
- Contact lens wear: Not to be administered while using contact lenses.
Common Side Effects
- Ocular, 5% to 10%: Capsular opacity, decreased visual acuity, foreign body sensation, increased IOP, sticky sensation.
- Ocular, 1% to 5%: Conjunctival edema, corneal edema, dry eye, lid margin crusting, ocular discomfort, ocular hyperemia, ocular pain, ocular pruritus, photophobia, tearing, vitreous detachment; some may be a consequence of the surgery itself.
- Systemic, 1% to 4%: Headache, hypertension, nausea and vomiting, sinusitis.
Pregnancy & LactationPregnancy: Category C on this label, with no adequate and well-controlled studies in pregnant women; avoid during late pregnancy because prostaglandin synthesis inhibitors close the fetal ductus arteriosus. Oral reproduction studies in rats and rabbits showed no teratogenicity, but maternally toxic doses of 10 mg/kg or more in rats caused dystocia, increased postimplantation loss, reduced fetal weight and growth, and reduced fetal survival, and the drug crosses the rat placenta.
Lactation: Excreted in the milk of lactating rats; excretion in human milk is not known, so use caution in a nursing woman.
Pediatric UseSafety and effectiveness below age 10 not established.