Nepafenac
Nepafenac Uses, Dosage, Side Effects, Food Interaction and all others data.
Nepafenac is a nonsteroidal anti-inflammatory prodrug (NSAID). After instillation in the eye, it penetrates the cornea and is converted by ocular tissue hydrolase to Amfenac, a potent nonsteroidal anti-inflammatory drug. Amfenac is thought to inhibit the action of cyclooxygenase enzyme. This enzyme is required for prostaglandin synthesis.
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.
| Trade Name | Nepafenac |
| Generic | Nepafenac |
| Nepafenac Other Names | Nepafenac, Népafénac, Nepafenaco, Nepafenacum |
| Weight | 0.1%w/w |
| Type | Ophthalmic, Eye Drops |
| Formula | C15H14N2O2 |
| Weight | Average: 254.2839 Monoisotopic: 254.105527702 |
| 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. |
| Groups | Approved, Investigational |
| Therapeutic Class | Ophthalmic Non-Steroid drugs |
| Manufacturer | Stallion Laboratories Pvt Ltd |
| Available Country | United States, India, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nepafenac 0.1% Sterile Ophthalmic Suspension: The treatment of post-operative ocular pain and inflammation including cataract surgery Inhibition of surgery induced miosis and Prevention of post-operative cystoid macular edema (CME).
Nepafenac 0.3% Sterile Ophthalmic Suspension: Post-operative pain and inflammation associated with cataract surgery.
Nepafenac is also used to associated treatment for these conditions: Inflammation, Pain
How Nepafenac works
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.
Dosage
Nepafenac dosage
Nepafenac 0.1% Sterile Ophthalmic Suspension-
- For post-operative pain & inflammation: Instill 1 drop 3 times daily 1 day prior to cataract surgery and continued on the day of surgery and through the first 2 weeks of the post-operative period.
- For surgery induced miosis: Instill 1 drop 3 times daily 1 day before surgery & on the day of surgery.
- For prevention of post-operative CME: Instill 1 drop 3 times daily 1 day before surgery and continued on the day of surgery and through the first 6 weeks of the post-operative period.
Nepafenac 0.3% Sterile Ophthalmic Suspension-
- For post-operative pain & inflammation: Instill 1 drop once daily 1 day prior to cataract surgery and continued on the day of surgery and through the first 2 weeks of the post-operative period. An additional drop should be administered 30 to 120 minutes prior to surgery.
Side Effects
Reported side effects are foreign body sensation, lid margin crusting, ocular discomfort, ocular hyperemia etc.
Toxicity
Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.
Precaution
Nepafenac should be used with caution in patients with known bleeding tendencies or who are receiving medications which may prolong bleeding time.
Food Interaction
No interactions found.Elimination Route
Nepafenac rapidly cross the cornea (6 times faster than diclofenac in vitro).
Elimination Route
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.
Pregnancy & Breastfeeding use
Use in pregnancy: There are no adequate and well-controlled studies in pregnant women. Nepafenac should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in lactation: It is not known whether this drug is excreted in human milk. So, caution should be exercised when Nepafenac ophthalmic suspension is administered to a nursing mother.
Contraindication
Contraindicated in patients with previously demonstrated hypersensitivity to any of the ingredients in the formulation or to other NSAIDs.
Special Warning
Use in children: Safety and effectiveness in pediatric patients below 18 years of age have not been established.
Use in elderly patients: No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Innovators Monograph
You find simplified version here Nepafenac
Nepafenac contains Nepafenac see full prescribing information from innovator Nepafenac Monograph, Nepafenac MSDS, Nepafenac FDA label
FAQ
What is Nepafenac used for?
Ophthalmic Nepafenac is used to treat eye pain, redness, and swelling in patients who are recovering from cataract surgery (procedure to treat clouding of the lens in the eye). Nepafenac is in a class of medications called nonsteroidal anti-inflammatory drugs.
How safe is Nepafenac?
Do not start using this medication early, use it more often than prescribed, or continue using it for longer than directed by your doctor. Prolonged use of Nepafenac eye drops (more than 2 weeks) may increase the risk of very serious side effects of the eye. Inform your doctor if your condition persists or worsens.
How does Nepafenac work?
Nepafenac works by stopping the production of certain natural substances that cause pain and swelling.
What are the common side effects of Nepafenac?
Common side effect of Nepafenac are include:
- headache.
- runny nose.
- pain or pressure in the face.
- nausea.
- vomiting.
- dry, itchy, or sticky eyes.
Is Nepafenac safe during pregnancy?
During pregnancy, Nepafenac should be used only when prescribed during the first 6 months.
Is Nepafenac safe during breastfeeding?
Maternal use of Nepafenac eye drops would not be expected to cause any adverse effects in breastfed infants.
When should be taken of Nepafenac?
Nepafenac is usually instilled three times a day beginning one day before cataract surgery, on the day of the surgery, and for 14 days after the surgery. Use Nepafenac eye drops at around the same times every day.
How many time can I take Nepafenac daily?
Nepafenac is usually instilled three times a day beginning one day before cataract surgery, on the day of the.
How long should I use Nepafenac?
This Nepafenac is usually used for up to 14 days after eye surgery or as directed by your doctor
Who should not take Nepafenac?
You should not use Nepafenac ophthalmic if you are allergic to it. Before using Nepafenac ophthalmic, tell your doctor if you are allergic to any other eye drops, or if you have diabetes, dry eye syndrome, arthritis, or a bleeding or blood-clotting disorder such as hemophilia.
What happens if I miss a dose?
Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.
What happens if I overdose?
An overdose of Nepafenac ophthalmic is not expected to be dangerous. Seek emergency medical attention.If anyone has accidentally swallowed the medication. Do not use other eye medications unless your doctor tells you to, especially steroid eye drops.
Is Nepafenac a steroid?
Nepafenac belongs to a group of medicines known as non-steroidal anti-inflammatory drugs (NSAIDs).
Can I use Nepafenac for dry eyes?
No, you should not use the Nepafenac for dry eyes. It is used to prevent and relieve eye pain, irritation and redness associated with cataract eye surgery.
Can Nepafenac affect my diabetes ?
People with diabetes are at an increased risk of side effects that can cause the loss of sight. If you have diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
What happen If I stop taking Nepafenac?
Stop taking the medication and seek immediate medical attention if any of the following occur:
eyes become redder or more painful while using the drops,reduced vision,signs of a serious allergic reaction (i.e., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat).
