Generic Name: Nepafenac
Class: Nonsteroidal Anti-inflammatory Agents
VA Class: CN104
Chemical Name: 2-amino-3-benzoylbenzeneacetamide
Molecular Formula: C15H14N2O2

Introduction

Prodrug of amfenac, a prototypical NSAIA.1 2 3 4 5 6 7 8

Uses for Nevanac

Postoperative Ocular Inflammation and Pain

Management of ocular inflammation and pain associated with cataract surgery.1 4 5

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Nevanac Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic suspension.1

Avoid contamination of the suspension container.9

Shake suspension container well prior to administration.1

Do not administer to an eye that has a contact lens.1 (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.1 9 If >1 topical ophthalmic drug is used, administer the drugs 10 minutes apart from nepafenac administration.9

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.1

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.1

Cautions for Nevanac

Contraindications

  • Known hypersensitivity to nepafenac or any ingredient in the formulation or to other NSAIAs.1

Warnings/Precautions

Warnings

Bleeding

May inhibit platelet aggregation and prolong bleeding time.1

May cause increased bleeding of ocular tissues (including hyphemas) when used in conjunction with ocular surgery.1

Use with caution in patients with underlying bleeding tendencies or in those receiving drugs known to prolong bleeding time.1

Sensitivity Reactions

Hypersensitivity Reactions

Possible cross-sensitivity with aspirin, phenylacetic acid derivatives, and other NSAIAs.1 Use with caution in patients with history of hypersensitivity to these drugs.1

General Precautions

Wound-healing Complications

May slow or delay wound healing.1 (See Specific Drugs under Interactions.)

Ocular Effects

Use may result in keratitis.1 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.1 If manifestations of corneal epithelial breakdown occur, discontinue therapy immediately and monitor for corneal health.1

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.1 Use with caution in these patients.1

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

No substantial effect on intraocular pressure reported; however, changes in intraocular pressure may occur following cataract surgery.1

Specific Populations

Pregnancy

Category C.1

Avoid use in late pregnancy because of known effects on fetal cardiovascular system (possible closure of the ductus arteriosus).1

Lactation

Distributed into milk in rats following oral administration of a single 3 mg/kg-dose;1 9 not known whether distributed into human milk following ophthalmic administration.1 Use with caution.1

Pediatric Use

Safety and efficacy not established in children <10 years of age.1

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.1

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.1

Interactions for Nevanac

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

Drugs Metabolized by Hepatic Microsomal Enzymes

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

Protein-bound Drugs

Pharmacokinetic interaction unlikely.1

Specific Drugs

Drug

Interaction

Corticosteroids, topical

Increased potential for wound-healing complications1

Nevanac Pharmacokinetics

Absorption

Bioavailability

Prodrug; penetrates the cornea following topical application to the eye and converted by ocular tissue hydrolases to amfenac.1

Following 3 times daily bilateral topical ophthalmic application, low, but quantifiable, plasma concentrations of nepafenac and amfenac observed 2 and 3 hours postdose, respectively.1

Distribution

Extent

Distributed into milk in rats following oral administration of a single 3 mg/kg-dose;1 9 not known whether distributed into human milk following ophthalmic administration.1

Elimination

Metabolism

Converted by ocular tissue hydrolases to amfenac.1 (See Bioavailability under Pharmacokinetics.)

Stability

Storage

Ophthalmic

Suspension

2–25°C.1

Actions

  • Prodrug of amfenac, a prototypical NSAIA.1 2 3 4 5 6 7 8

  • Amfenac inhibits the synthesis of prostaglandins by inhibiting cyclooxygenase (COX), including both COX-1 and COX-2 isoenzymes.1 2 3 6 8

  • Ocular effects appear to be associated principally with the inhibition of ocular prostaglandin synthesis.1 2 7

Advice to Patients

  • Risk of ocular bleeding.1 Risk of anaphylactoid and other sensitivity reactions.1

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the ophthalmic suspension with common bacteria that can cause ocular infections.9

  • Importance of removing contact lenses before administration.1 Importance of shaking suspension before administration.1

  • Importance of administering different topical ophthalmic preparations 10 minutes apart from nepafenac administration.9

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

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 Risk of use during late pregnancy.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

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

Nepafenac

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Suspension

0.1%

Nevanac (with benzalkonium chloride)

Alcon

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Nevanac 0.1% Suspension (ALCON VISION): 3/$144.00 or 9/$412.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions March 31, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Alcon Laboratories, Inc. Nevanac (nepafenac ophthalmic suspension) 0.1% prescribing information. Fort Worth, TX; 2005.

2. O’Brien TP. Emerging guidelines for use of NSAID therapy to optimize cataract surgery patient care. Curr Med Res Opin. 2005; 21:1131-37.

3. Takahashi K, Saishin Y, Saishin Y et al. Topical nepafenac inhibits ocular neovascularization. Invest Ophthalmol Vis Sci. 2003; 44:409-15. [PubMed 12506103]

4. Lane SS, Modi SS, Holland EJ et al. Pre- and post-operative nepafenac ophthalmic suspension, 0.1% for anterior segment inflammation after cataract surgery. Paper presented at the annual ASCRS/ASOA symposium and congress. Washington, DC: 2005 Apr 18.

5. Stewart WC, Stewart R, Maxwell WA et al. Pre- and post-operative clinical posology evaluation of nepafenac ophthalmic suspension, 0.1% for anterior segment inflammation after cataract surgery. Paper presented at the annual ASCRS/ASOA symposium and congress. Washington, DC: 2005 Apr 18.

6. Gamache DA, Graff G, Brady MT et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000; 24:357-70. [PubMed 10850857]

7. Ke TL, Graff G, Spellman JM et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000; 24:371-84. [PubMed 10850858]

8. Kapin MA, Yanni JM, Brady MT et al. Inflammation-mediated retinal edema in the rabbit is inhibited by topical nepafenac. Inflammation. 2003; 27:281-91. [PubMed 14635785]

9. Alcon Laboratories, Inc., Fort Worth, TX: Personal Communication.

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