nepafenac ophthalmic

Action and Spectrum

Actions and Spectrum: 

Action: nepafenac is a prodrug, which means it is inactive when administered and must be converted into its active form within the eye. Once inside the eye, enzymes present in the eye tissue convert nepafenac into its active metabolite, amfenac. amfenac is a potent inhibitor of cyclooxygenase (COX) enzymes, particularly COX-1 and COX-2. 

The inhibition of COX enzymes reduces the production of prostaglandins, which are chemical messengers involved in the inflammatory process. By blocking prostaglandin production, nepafenac helps to decrease inflammation, pain, and swelling in the eye. This mechanism of action makes nepafenac particularly useful in the management of eye conditions characterized by inflammation, such as postoperative inflammation following cataract surgery. 

Spectrum: nepafenac ophthalmic is primarily used for the treatment of postoperative inflammation related with cataract surgery. Post-cataract surgery, it is a frequent occurrence for patients to undergo eye inflammation, leading to discomfort and potential impact on the recovery of their vision. nepafenac eye drops are prescribed in such cases to help control the inflammatory response, reduce pain, and promote healing. 

Drug Interaction

Adverse Reaction

Frequency not defined  

stuffy nose 

nausea, vomiting 

headache 

increased sensitivity to light 

itching or watering of the eye 

eye redness 

feeling like something is in your eye 

dry or sticky feeling in the eye 

Black Box Warning

Black Box Warning:  

None  

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Individuals with a known hypersensitivity or allergic reaction to nepafenac or any other components of the eye drop formulation should not use this medication. 

Allergic Reactions: Patients who have experienced allergic reactions to other NSAIDs or aspirin may also be at risk for allergic reactions to nepafenac ophthalmic. 

Asthma and Aspirin Sensitivity: Individuals with asthma or a history of aspirin sensitivity should avoid nepafenac ophthalmic, as it may exacerbate these conditions. 

Active Ocular Infections: nepafenac should not be used in the presence of active ocular infections, as it may delay healing or worsen the infection. 

Corneal Epithelial Defects: The use of nepafenac ophthalmic is contraindicated in patients with corneal epithelial defects, as it may delay corneal healing. 

Severe Allergic Reactions: There have been reports of severe allergic reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, associated with the use of NSAIDs, including nepafenac. Therefore, it should be avoided in patients with a history of these reactions. 

Children: Safety and efficacy in pediatric patients have not been established, so it is not recommended for use in children without proper medical supervision and evaluation. 

Pregnancy and Breastfeeding: The safety of nepafenac ophthalmic in pregnant and breastfeeding women has not been established. Therefore, it should be used with caution in these populations, and the potential benefits should outweigh the risks. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: AU TGA pregnancy category: C
US FDA pregnancy category: C 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

nepafenac ophthalmic is a nonsteroidal anti-inflammatory drug (NSAID) used as an ophthalmic solution to treat inflammation and pain associated with cataract surgery. 

Pharmacodynamics:  

nepafenac exerts its pharmacological actions by inhibiting the enzyme cyclooxygenase (COX), which plays a crucial role in the synthesis of prostaglandins. Prostaglandins are lipid mediators that promote inflammation, pain, and swelling in response to injury or trauma. By inhibiting COX, nepafenac reduces the production of prostaglandins, leading to decreased inflammation and pain in the eye. 

Pharmacokinetics: 

Absorption 

nepafenac ophthalmic is an ophthalmic prodrug of amfenac, which is a non-steroidal anti-inflammatory drug (NSAID). When applied as an ophthalmic solution, nepafenac is intended to be absorbed through the cornea into the intraocular tissues of the eye. The absorption rate may vary depending on factors such as the formulation of the ophthalmic solution, the health of the ocular surface, and the individual patient characteristics. 

Distribution 

After absorption, nepafenac and its active metabolite, amfenac, may distribute within the intraocular tissues, exerting their anti-inflammatory effects by inhibiting prostaglandin synthesis. The drug remains primarily localized within the eye and does not significantly enter systemic circulation in significant amounts. 

Metabolism 

Once absorbed into the intraocular tissues, nepafenac is rapidly metabolized by esterases to its active metabolite, amfenac. Amfenac is the pharmacologically active compound responsible for the therapeutic effects of nepafenac ophthalmic. The metabolism of nepafenac occurs locally within the eye, and the drug is not extensively metabolized in the systemic circulation. 

Excretion and Elimination 

 Since nepafenac ophthalmic primarily acts within the eye and does not significantly enter systemic circulation, the excretion of the drug and its metabolites mainly occurs through intraocular tissues and the tear film. The drug and its metabolites may be eliminated from the eye through normal physiological processes. 

Adminstartion

Administration:  

• Wash your hands thoroughly with soap and water before handling. 
• Tilt your head back or lie down and look up toward the ceiling. 
• Create a small pocket by gently pulling down your lower eyelid. 
• Position the dropper above your eye, ensuring the tip is facing downwards but not in contact with your eye or any other surface. 
• Squeeze the prescribed number of drops into the pocket formed by the lower eyelid.  
• Close your eyes gently and press on the inside corner of your eye (near the nose) with your finger for about 1-2 minutes. This helps prevent the medication from draining into the tear duct and ensures that it stays in the eye. 
• If you are using more than one type of eye drop, wait at least 5 minutes between administering each medication to allow enough time for the previous drop to be absorbed properly. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: nepafenac ophthalmic 

Why do we use nepafenac ophthalmic?  

Postoperative inflammation: nepafenac is often prescribed after cataract surgery to reduce inflammation in the eye.  

Ocular inflammation: nepafenac can be used to manage inflammation associated with other eye conditions, such as uveitis and keratitis.  

Pain relief: In addition to its anti-inflammatory properties, nepafenac can provide pain relief for certain eye conditions. It can reduce the discomfort and pain experienced by patients with various inflammatory eye disorders. 

Macular edema: nepafenac, when used in combination with other treatments, can help reduce macular edema associated with certain eye conditions, such as diabetic retinopathy.