Ocufenac

• Approved Indications:
• Treatment of pain and inflammation associated with cataract surgery.
• Prevention and management of postoperative inflammation following ocular surgery.
• Relief of ocular inflammation due to non-infectious anterior segment diseases.
• Clinically Accepted Off-Label Uses:
• Management of ocular pain and inflammation related to other anterior segment surgeries.
• Adjunctive treatment for diabetic macular edema in some cases (off-label).

• Route: Topical ophthalmic suspension (eye drops).
• Adults:
• Post-cataract surgery:
  • Instill 1 drop into the affected eye(s) 3 times daily, starting 1 day before surgery, continued on the day of surgery, and for 2 weeks after surgery.
• For other inflammatory conditions, dosing may vary per physician’s guidance, typically 3 times daily.
• Pediatrics:
  Safety and efficacy not established; use only if clearly needed under specialist supervision.
• Elderly:
  No dose adjustment required; monitor for tolerance.
• Renal/Hepatic Impairment:
  No systemic absorption of clinical significance; no dose adjustment required.
• Administration Instructions:
• Shake well before use.
• Avoid contact of the dropper tip with the eye or other surfaces to prevent contamination.
• Wait at least 5 minutes before instilling other ophthalmic medications.

Nepafenac is a prodrug that penetrates the cornea and is converted by ocular tissue hydrolases into amfenac, a potent nonsteroidal anti-inflammatory drug (NSAID). Amfenac inhibits cyclooxygenase enzymes COX-1 and COX-2, leading to reduced synthesis of prostaglandins which mediate inflammation, pain, and vasodilation in ocular tissues. By inhibiting prostaglandin production, nepafenac decreases inflammation and pain associated with surgery or ocular conditions.

• Absorption:
  Rapidly absorbed into ocular tissues after topical administration; systemic absorption is minimal.
• Distribution:
  Distributes primarily within the anterior segment of the eye (cornea, aqueous humor).
• Metabolism:
  Converted enzymatically in ocular tissues from nepafenac (prodrug) to active metabolite amfenac.
• Elimination:
  Metabolized by ocular and systemic enzymes; systemic exposure is negligible.
• Half-life:
  Ocular half-life not precisely defined; systemic half-life is not clinically relevant due to minimal systemic exposure.

• Pregnancy:
  Classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use only if potential benefits justify potential risks.
• Lactation:
  Unknown if excreted in human milk. Use with caution; risk to infant is considered low due to minimal systemic absorption.

• Primary Class: Nonsteroidal Anti-Inflammatory Drug (NSAID) — Ophthalmic
• Subclass: Prodrug NSAID

• Known hypersensitivity to nepafenac, amfenac, other NSAIDs, or any component of the formulation.
• Active corneal epithelial defects or corneal infections.
• History of bronchial asthma, urticaria, or allergic-type reactions to aspirin or other NSAIDs.

• Use with caution in patients with bleeding disorders or those on anticoagulants due to increased risk of ocular bleeding.
• Delayed wound healing: NSAIDs may slow corneal healing; monitor patients with corneal epithelial defects.
• Corneal adverse events: Rare reports of corneal thinning, ulceration, or perforation, particularly in patients with compromised corneas or prolonged use.
• Avoid use in ocular infections unless concurrently treated with appropriate antimicrobial therapy.
• Monitor for signs of ocular irritation, burning, or allergic reactions.

Common:

• Eye pain or discomfort
• Eye irritation or redness
• Blurred vision
• Dry eyes
• Photophobia

Less Common:

• Headache
• Increased intraocular pressure (rare)
• Foreign body sensation

Rare but Serious:

• Corneal thinning or perforation (especially with prolonged use)
• Hypersensitivity reactions (rash, swelling, itching)
• Severe ocular inflammation or worsening infection

• No significant systemic drug interactions due to minimal systemic absorption.
• Caution advised when used concomitantly with other ophthalmic NSAIDs or corticosteroids to avoid additive adverse effects.
• No known significant interactions with CYP450 enzymes.

• Continued endorsement by ophthalmologic societies for post-cataract surgery inflammation control.
• Newer formulations have improved ocular penetration and patient tolerability.
• Safety warnings updated to emphasize rare but serious corneal adverse effects, especially with prolonged use beyond recommended duration.
• No recent major changes in dosing or indications from FDA, EMA, or WHO.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from light and excessive moisture.
• Do not freeze.
• Keep bottle tightly closed when not in use.
• Discard opened bottles after the recommended usage period (typically 4 weeks).