NEVANAC EYE SUSPENSION

Indications

• Postoperative pain and inflammation associated with cataract surgery
• Reduction in the risk of postoperative macular oedema in diabetic patients undergoing cataract surgery

Dosage

Children: Child 4–17 years: Apply 4 times a day, with treatment duration sometimes extending up to 4 weeks, depending on the clinical response.

Adults: Apply 4 times a day, with treatment duration sometimes extending up to 4 weeks, depending on the clinical response.

Mechanism of action

Nepafenac is a prodrug that is rapidly bioactivated to amfenac after penetrating the cornea. Amfenac inhibits both COX-1 and COX-2 enzymes, leading to a reduction in the synthesis of prostaglandins, which are mediators of inflammation and pain.

Pharmacodynamics

Following topical ocular administration, low but measurable plasma concentrations of nepafenac and amfenac are observed. The mean steady-state peak plasma concentrations (Cmax) for nepafenac and amfenac are approximately 0.310 ng/ml and 0.422 ng/ml, respectively, indicating effective local action with minimal systemic absorption.

Pharmacokinetics

Nepafenac is applied topically to the eye, where it is rapidly converted to its active form, amfenac. The pharmacokinetics involve minimal systemic absorption, allowing for targeted action at the site of inflammation with low plasma levels. The exact half-life and clearance rates are not well defined due to the localized use, but the rapid action suggests a quick onset of therapeutic effects.

Adverse effects

• Dry eye
• Eye discomfort
• Dizziness
• Headache
• Nausea
• Vision disorders
• Corneal deposits
• Allergic dermatitis
• Rash
• Taste altered
• Nasal complaints

Precautions

• Avoid sunlight exposure
• Discontinue if evidence of corneal epithelial breakdown or symptoms of infection occur

Pregnancy

Use in pregnancy should be assessed based on the benefit-risk balance, as safety data is limited.

Breast-feeding

Limited data available; caution is advised as it is not known if nepafenac is excreted in breast milk.

Storage

Store at room temperature, protect from light, and keep out of reach of children.

Formulations

• Nepafenac 3 mg/mL eye drops (Nevanac)

Mechanism of action

Nepafenac is a prodrug. After penetrating the cornea, nepafenac undergoes rapid bioactivation to amfenac, which is a potent NSAID that uniformly inhibits the COX1 and COX2 activity.

Pharmacodynamics

Low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects 2 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.