NEVANAC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NEVANAC (NEVANAC).
Nepafenac is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, primarily COX-2, reducing prostaglandin synthesis and thereby suppressing ocular inflammation and pain.
| Metabolism | Nepafenac is metabolized via ocular tissues to amfenac, the active metabolite. Systemic metabolism primarily involves hepatic conjugation and oxidation. |
| Excretion | Nepafenac is extensively metabolized, primarily via hydrolysis to amfenac. Renal excretion accounts for approximately 85% of the administered dose, with about 13% excreted as unchanged nepafenac and amfenac in urine. Fecal elimination is minimal. |
| Half-life | The terminal elimination half-life of nepafenac is approximately 12.5 hours in plasma, while its active metabolite amfenac has a half-life of about 24 hours. This supports twice-daily dosing. |
| Protein binding | Nepafenac is approximately 98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | The apparent volume of distribution (Vd/F) is approximately 0.6 L/kg (range 0.5-0.7 L/kg), suggesting distribution into total body water and some tissue binding. |
| Bioavailability | Ophthalmic: Systemic bioavailability after topical ocular administration is very low (approximately 0.1-1% of the dose), but sufficient for local ocular effects. Oral bioavailability is not clinically relevant as drug is only used ophthalmically. |
| Onset of Action | Ophthalmic: Analgesic effect and reduction of inflammation occur within 1-2 hours post-instillation. |
| Duration of Action | The clinical effect lasts approximately 12-16 hours, supporting twice-daily dosing. Duration may be extended with continued use. |
| Molecular Weight | 254.28 |
One drop of 0.1% ophthalmic suspension instilled into the affected eye(s) three times daily.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dose adjustment required in renal impairment; systemic exposure is minimal due to topical administration. |
| Liver impairment | No dose adjustment required in hepatic impairment; systemic exposure is minimal. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; use is not recommended. |
| Geriatric use | No specific dose adjustment; dosing is identical to standard adult dosing. |
| 1st trimester | Avoid use during first trimester due to potential NSAID-related risks; studies suggest possible increased risk of miscarriage and congenital malformations. |
| 2nd trimester | Use only if clearly needed; avoid during second trimester due to risk of premature ductus arteriosus closure and oligohydramnios. |
| 3rd trimester | Contraindicated during third trimester due to risk of premature closure of the ductus arteriosus and fetal renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for NEVANAC (NEVANAC).
| Placental transfer | Nepafenac is known to cross the placenta; data indicate significant transfer in animal studies, and human data suggest placental passage is likely, especially in late pregnancy. |
| Breastfeeding | Nepafenac is excreted into breast milk in low amounts; however, due to potential adverse effects in the infant (e.g., platelet dysfunction, renal impairment), caution is advised. Use only if clearly needed and monitor infant for any signs of gastrointestinal bleeding or renal impairment. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Decreased vision Foreign body sensation in eyes Increased intraocular pressure Stickiness |
| Serious Effects |
Hypersensitivity to nepafenac or any component of the formulationHistory of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDsThird trimester of pregnancy (risk of premature ductus arteriosus closure)Active gastrointestinal bleeding or perforationSevere renal impairment (CrCl < 30 mL/min)Severe hepatic impairment
| Precautions | Increased bleeding time due to antiplatelet effect, Delayed healing or corneal adverse events including keratitis and corneal perforation, Cross-sensitivity with aspirin or other NSAIDs, Use with caution in patients with bleeding diatheses or concurrent anticoagulants |
| Food/Dietary |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Nepafenac is an NSAID. First trimester: limited human data, but NSAIDs as a class are associated with increased risk of spontaneous abortion and cardiac defects. Second trimester: generally considered lower risk for teratogenicity, but avoid if possible. Third trimester: increased risk of premature closure of the ductus arteriosus, oligohydramnios, and fetal renal impairment. Ophthalmic use results in minimal systemic absorption, but theoretical risks remain. Use only if clearly needed. |
| Fetal Monitoring | Monitor for maternal signs of NSAID-related adverse effects (gastrointestinal bleeding, renal impairment, hypertension) if used systemically. Fetal monitoring in third trimester: assess amniotic fluid volume, ductus arteriosus patency via ultrasound if prolonged use or exposure near term. |
| Fertility Effects | NSAIDs may impair female fertility by inhibiting prostaglandin synthesis, potentially delaying or preventing ovulation. Reversible upon discontinuation. No specific data for nepafenac. |
| No clinically significant food interactions have been identified with ophthalmic nevanac. Systemic absorption is minimal, so dietary restrictions are not required. |
| Clinical Pearls | Nevanac (nepafenac) is a nonsteroidal anti-inflammatory drug (NSAID) ophthalmic suspension indicated for pain and inflammation associated with cataract surgery. Its prodrug formulation enhances corneal penetration, with active metabolite amfenac inhibiting COX-1 and COX-2. Administer one drop three times daily starting 1 day prior to surgery, continuing on day of surgery and for 2 weeks postoperatively. Avoid concurrent use of other NSAIDs or corticosteroids to mitigate risk of corneal adverse events. Monitor for signs of corneal epithelial breakdown, especially in patients with compromised corneal innervation (e.g., diabetes, prior ocular surgery). |
| Patient Advice | Wash hands before and after instilling the drop. · Remove contact lenses before use and wait 10 minutes after administering before reinserting. · Do not touch the dropper tip to any surface to avoid contamination. · Apply one drop to the affected eye three times daily as directed, starting one day before cataract surgery. · Temporary blurred vision may occur; avoid driving or operating machinery until vision clears. · Notify your doctor if you experience eye pain, redness, sensitivity to light, or changes in vision. · Do not use other eye drops without consulting your doctor, especially other anti-inflammatory medications. · Store the bottle upright at room temperature, away from heat and light, and discard any unused suspension after the treatment period. |