ILEVRO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ILEVRO (ILEVRO).
Nepafenac is a prodrug that is metabolized to amfenac, a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) activity, reducing prostaglandin synthesis.
| Metabolism | Nepafenac is hydrolyzed to amfenac by ocular tissue hydrolases. Amfenac undergoes further metabolism via CYP450 enzymes, primarily CYP2C9. |
| Excretion | Nepafenac is extensively metabolized, and its active metabolite amfenac is primarily excreted renally (approximately 80% as metabolites, including amfenac glucuronide, and 20% as unchanged drug in urine). Biliary/fecal excretion accounts for less than 10%. |
| Half-life | Terminal elimination half-life of amfenac is approximately 0.7 hours in plasma, but due to prolonged residence in ocular tissues, the clinical effect lasts up to 24 hours with once-daily dosing. |
| Protein binding | Amfenac is approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.16 L/kg, indicating distribution mainly in extracellular fluid. |
| Bioavailability | Ocular bioavailability is low due to limited systemic absorption; plasma concentrations are undetectable after topical administration in most patients. |
| Onset of Action | Onset of analgesic effect following ophthalmic administration occurs within 1 hour; anti-inflammatory effect begins within 2 hours. |
| Duration of Action | Duration of action is approximately 24 hours after a single ophthalmic dose, allowing once-daily dosing for inflammation and pain associated with cataract surgery. |
1 drop of the 0.3% ophthalmic solution administered to the affected eye(s) four times daily.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No overall differences in safety or efficacy observed between elderly and younger patients; no specific dose adjustment recommended. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ILEVRO (ILEVRO).
| Breastfeeding | No human data available; M/P ratio unknown. Nepafenac and its active metabolite amfenac are excreted in rat milk. Due to potential adverse effects in nursing infants, caution advised. Consider temporary discontinuation during breastfeeding. |
| Teratogenic Risk | Nepafenac is an NSAID; risk of premature closure of ductus arteriosus and oligohydramnios starting at 20 weeks gestation. Avoid in third trimester. No adequate studies in first trimester; animal studies show no teratogenicity at clinically relevant doses. |
■ FDA Black Box Warning
None
| Common Effects | Decreased vision Foreign body sensation in eyes Increased intraocular pressure Stickiness |
| Serious Effects |
["Hypersensitivity to nepafenac or any component of the formulation","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs"]
| Precautions | ["Increased bleeding time due to antiplatelet effect","Risk of corneal adverse events including keratitis and corneal perforation","Potential for cross-sensitivity to aspirin or other NSAIDs","May mask signs of infection","Use with caution in patients with prior ocular surgery or epithelial defects"] |
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| Fetal Monitoring |
| Monitor for signs of premature ductus arteriosus closure and oligohydramnios if used after 20 weeks; perform fetal echocardiography and amniotic fluid index assessments if exposure occurs. Also monitor maternal renal function. |
| Fertility Effects | NSAIDs may impair female fertility via inhibition of prostaglandin synthesis affecting ovulation and implantation; reversible upon discontinuation. No direct data for nepafenac, but class effect applies. |