Nepafenac (Monograph)

Brand name: Nevanac
Drug class: Nonsteroidal Anti-inflammatory Agents
- Nonsteroidal Anti-inflammatory Agents, Ophthalmic
- NSAIAs, EENT
- NSAIDs, EENT
VA class: CN104
Chemical name: 2-amino-3-benzoylbenzeneacetamide
Molecular formula: C₁₅H₁₄N₂O₂

Medically reviewed by Drugs.com on Mar 21, 2024. Written by ASHP.

Introduction

Prodrug of amfenac, a prototypical NSAIA.

Uses for Nepafenac

Postoperative Ocular Inflammation and Pain

Management of ocular inflammation and pain associated with cataract surgery.

Nepafenac Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic suspension.

Avoid contamination of the suspension container.

Shake suspension container well prior to administration.

Do not administer to an eye that has a contact lens. (See Advice to Patients.)

May be used in conjunction with other topical ophthalmic medications such as β-adrenergic blocking agents, carbonic anhydrase inhibitors, α-agonists, cycloplegics, and mydriatics. If >1 topical ophthalmic drug is used, administer the drugs 10 minutes apart from nepafenac administration.

Dosage

Pediatric Patients

Postoperative Ocular Inflammation and Pain

Ophthalmic

Patients ≥10 years of age: 1 drop of a 0.1% suspension in the affected eye(s) 3 times daily, beginning 1 day prior to cataract surgery and continuing on the day of the surgery and for 2 weeks after surgery.

Adults

Postoperative Ocular Inflammation and Pain

Ophthalmic

1 drop of a 0.1% suspension in the affected eye(s) 3 times daily, beginning 1 day prior to cataract surgery and continuing on the day of the surgery and for 2 weeks after surgery.

Related/similar drugs

diclofenac ophthalmic, dexamethasone ophthalmic, ketorolac ophthalmic, prednisolone ophthalmic, Lotemax, flurbiprofen ophthalmic, Nevanac

Cautions for Nepafenac

Contraindications

• Known hypersensitivity to nepafenac or any ingredient in the formulation or to other NSAIAs.

Warnings/Precautions

Warnings

Bleeding

May inhibit platelet aggregation and prolong bleeding time.

May cause increased bleeding of ocular tissues (including hyphemas) when used in conjunction with ocular surgery.

Use with caution in patients with underlying bleeding tendencies or in those receiving drugs known to prolong bleeding time.

Sensitivity Reactions

Hypersensitivity Reactions

Possible cross-sensitivity with aspirin, phenylacetic acid derivatives, and other NSAIAs. Use with caution in patients with history of hypersensitivity to these drugs.

General Precautions

Wound-healing Complications

May slow or delay wound healing. (See Specific Drugs under Interactions.)

Ocular Effects

Use may result in keratitis. In some susceptible patients, continued use may result in epithelial breakdown, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation; these events may be sight-threatening. If manifestations of corneal epithelial breakdown occur, discontinue therapy immediately and monitor for corneal health.

Patients with complicated ocular surgeries, corneal denervation, corneal epithelial defects, diabetes mellitus, ocular surface diseases (e.g., dry eye syndrome), rheumatoid arthritis, or repeat ocular surgeries within a short period of time may be at increased risk for developing adverse corneal effects that may become sight-threatening. Use with caution in these patients.

Use >1 day prior to surgery or use beyond 14 days postoperatively may precipitate or exacerbate adverse corneal effects.

No substantial effect on intraocular pressure reported; however, changes in intraocular pressure may occur following cataract surgery.

Specific Populations

Pregnancy

Category C.

Avoid use in late pregnancy because of known effects on fetal cardiovascular system (possible closure of the ductus arteriosus).

Lactation

Distributed into milk in rats following oral administration of a single 3 mg/kg-dose; not known whether distributed into human milk following ophthalmic administration. Use with caution.

Pediatric Use

Safety and efficacy not established in children <10 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.

Common Adverse Effects

Capsular opacity, decreased visual acuity, ocular foreign body sensation, increased intraocular pressure, ocular sticky sensation, conjunctival edema, corneal edema, dry eye, lid margin crusting, ocular discomfort, ocular hyperemia, ocular pain, ocular pruritus, photophobia, tearing, vitreous detachment, headache, hypertension, nausea, vomiting, sinusitis.

Drug Interactions

Does not inhibit CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4 in vitro.

Drugs Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions with drugs metabolized by CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4 unlikely.

Protein-bound Drugs

Pharmacokinetic interaction unlikely.

Specific Drugs

Nepafenac Pharmacokinetics

Absorption

Bioavailability

Prodrug; penetrates the cornea following topical application to the eye and converted by ocular tissue hydrolases to amfenac.

Following 3 times daily bilateral topical ophthalmic application, low, but quantifiable, plasma concentrations of nepafenac and amfenac observed 2 and 3 hours postdose, respectively.

Distribution

Extent

Distributed into milk in rats following oral administration of a single 3 mg/kg-dose; not known whether distributed into human milk following ophthalmic administration.

Elimination

Metabolism

Converted by ocular tissue hydrolases to amfenac. (See Bioavailability under Pharmacokinetics.)

Stability

Storage

Ophthalmic

Suspension

2–25°C.

Actions

• Prodrug of amfenac, a prototypical NSAIA.

• Amfenac inhibits the synthesis of prostaglandins by inhibiting cyclooxygenase (COX), including both COX-1 and COX-2 isoenzymes.

• Ocular effects appear to be associated principally with the inhibition of ocular prostaglandin synthesis.

Advice to Patients

• Risk of ocular bleeding. Risk of anaphylactoid and other sensitivity reactions.

• Importance of learning and adhering to proper administration techniques to avoid contamination of the ophthalmic suspension with common bacteria that can cause ocular infections.

• Importance of removing contact lenses before administration. Importance of shaking suspension before administration.

• Importance of administering different topical ophthalmic preparations 10 minutes apart from nepafenac administration.

• Importance of not using topical NSAIAs >1 day prior to surgery or beyond 14 days after surgery.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Risk of use during late pregnancy.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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