APFECTO

Nepafenac is a non-steroidal anti-inflammatory prodrug (NSAID) usually sold as a prescription eye drop.

It is used to treat pain and inflammation associated with cataract surgery.

For the treatment of pain and inflammation associated with cataract surgery.

Low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects and 3 hours postdose, respectively, following bilateral topical ocular TID dosing of nepafenac ophthalmic suspension, 0.1%.

The mean steady-state

Cmax for nepafenac and for amfenac were 0.310 ± 0.104 ng/ml and 0.422 ± 0.121 ng/ml, respectively, following ocular administration.

G/H synthase 1 Inhibitor Prostaglandin G/H synthase 2 Inhibitor.

Nepafenac rapidly cross the cornea (6 times faster than diclofenac in vitro).

Nepafenac (prodrug) is deaminated to amfenac (active compound) in the ciliary body epithelium, retina, and choroid by intraocular hydrolases.

Subsequently, amfenac undergoes extensive metabolism to more polar metabolites involving hydroxylation of the aromatic ring leading to glucuronide conjugate formation.

After oral administration of 14C-nepafenac to healthy volunteers, urinary excretion was found to be the major route of radioactivity elimination, accounting for approximately 85% of the dose, while fecal excretion represented approximately 6% of the dose.

Nepafenac (prodrug) and amfenac (active compound) were not quantifiable in the urine.

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Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.

® 0.3% is contraindicated in patients with previously demonstrated hypersensitivity to any of the ingredients in the formula or to other nonsteroidal anti-inflammatory drugs (NSAIDs).

Hypersensitivity to any of the ingredients in the formula or to other non-steroidal anti-inflammatory drugs (NSAIDS).

One drop of

ILEVRO ® 0.3% should be applied to the affected eye one-time-daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period.

An additional drop should be administered to 120 minutes prior to surgery. 2.1 Recommended Dosing One drop of ILEVRO ® 0.3% should be applied to the affected eye one time daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period.

An additional drop should be administered to 120 minutes prior to surgery. 2.2 Use with Other Topical Ophthalmic Medications ILEVRO ® 0.3% may be administered in conjunction with other topical ophthalmic medications such as beta-blockers, carbonic anhydrase inhibitors, alpha-agonists, cycloplegics, and mydriatics.

If more than one topical ophthalmic medication is being used, the medicines must be administered at least 5 minutes apart.

® 0.3% is supplied in a white, oval, low density polyethylene dispenser with a natural low density polyethylene dispensing plug and gray polypropylene cap. 3 mL in 4 mL bottle NDC 82667-400-03 Storage: Store at 2°C to 25°C (36°F to 77°F).

Protect from light.

Reproduction studies performed with nepafenac in rabbits and rats at oral doses up to 10 mg/kg/day have revealed no evidence of teratogenicity due to nepafenac, despite the induction of maternal toxicity.

At this dose, the animal plasma exposure to nepafenac and amfenac was approximately and 630 times human plasma exposure at the recommended human topical ophthalmic dose for rats and and 180 times human plasma exposure for rabbits, respectively.

In rats, maternally toxic doses greater than or equal to 10 mg/kg were associated with dystocia, increased postimplantation loss, reduced fetal weights and growth, and reduced fetal survival.

Nepafenac has been shown to cross the placental barrier in rats.

There are no adequate and well-controlled studies in pregnant women.

Because animal reproduction studies are not always predictive of human response, ILEVRO ® 0.3% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Because of the known effects of prostaglandin biosynthesis inhibiting drugs on the fetal cardiovascular system (closure of the ductus arteriosus), the use of ILEVRO ® 0.3% during late pregnancy should be avoided.

Nepafenac is excreted in the milk of lactating rats.

It is not known whether this drug is excreted in human milk.

Because many drugs are excreted in human milk, caution should be exercised when ILEVRO ® 0.3% is administered to a nursing woman.

The safety and effectiveness of

ILEVRO ® 0.3% in pediatric patients below the age of 10 years have not been established.

No overall differences in safety and effectiveness have been observed between elderly and younger patients.