Drug information of Nepafenac Ophthalmic

Nepafenac Ophthalmic

Drug group: Anti-Inflammatory Agents

NEVANAC® (nepafenac ophthalmic suspension) 0.1% is a sterile, topical, nonsteroidal anti-inflammatory (NSAID) prodrug for ophthalmic use

Nepafenac Ophthalmic

Mechanism of effect

Non-steroidal anti-inflammatory prodrug, converted to amfenac which putatively inhibits prostaglandin biosynthesis

Pharmacodynamic

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

Pharmacokinetics

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

Protein binding: Amfenac has high affinity toward serum albumin proteins. In vitro, the percent bound to human albumin and human serum was 95.4% and 99.1% respectively.

Metabolism: 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.

Drug indications

NEVANAC® ophthalmic suspension is indicated for the treatment of pain and inflammation associated with cataract surgery.

Dosage

One drop of NEVANAC should be applied to the affected eye three-times-daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period.

Drug contraindications

Hypersensitivity

Hypersensitivity to NSAIDs or any ingredients

Side effects

Capsular opacity (5-10%)
Decreased visual acuity (5-10%)
Foreign body sensation (5-10%)
Increased IOP (5-10%)
Sticky sensation (5-10%)
Conjunctival edema (1-5%)
Corneal edema (1-5%)
Dry eye (1-5%)
Headache (1-4%)
HTN (1-4%)
Lid margin crusting (1-5%)
N/V (1-4%)
Ocular discomfort (1-5%)
Ocular hyperemia (1-5%)
Ocular pain (1-5%)
Ocular pruritus (1-5%)
Photophobia (1-5%)
Tearing (1-5%)
Vitreous detachment (1-5%

Interactions

Acetylcholine , Loteprednol , Travoprost , Ramucirumab , Bromfenac

Alerts

Sensitivity to aspirin or phenylacetic acid deivatives

 

May cause increased bleeding in ocular tissues

 

May cause keratitis & corneal damage (risk increased if applied earlier than 1 day presurgery or longer than 2 wk postsurgery)

 

Use caution in patients with bleeding predisposition, ocular disease states, diabetes ( corneal adverse effects may result in loss of vision), rheumatoid arthritis

 

Do not wear contact lenses while on the medication

 

Risk of corneal adverse effects increases with use 1 day before surgery or >14 days following surgery

Pregnancy level

Pregnancy Category: C
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

Breast feeding warning

Lactation: Unknown if excreted in breast milk; use caution

Drug forms

Nevanac, Ilevro

Ask a Pharmacist


User's questions
    No comments yet.