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Nepafenac
- indication:For the treatment of pain and inflammation associated with cataract surgery.
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.
- absorprion: Nepafenac rapidly cross the cornea (6 times faster than diclofenac in vitro).
- halflife:
- roouteelimination: After oral administration of 14C-nepafenac to healthy volunteers, urinary excretion was found to be the major route of radioactivity elimination, accounting for approximately 85% of the dose, while fecal excretion represented approximately 6% of the dose. Nepafenac (prodrug) and amfenac (active compound) were not quantifiable in the urine.
- volumedistribution:
- clearance: