Nevanak eye drops 0.1%, 5 ml

Prevention and treatment of postoperative pain and inflammation during surgery for cataract removal.

Topically. Shake the bottle before use. 1 drop into the conjunctival sac of the eye (s) 3 times a day. Treatment begins 1 day before surgery for cataract removal and continues for the first 2 weeks of the postoperative period (including the day of surgery). An additional drop of the drug should be instilled 30-120 minutes before the operation.

Eye drops in the form of a homogeneous suspension from light yellow to light orange.

1 ml

nepafenac 1 mg

Excipients: benzalkonium chloride (in the form of a 50% solution) - 0.05 mg, carbomer (974R) - 5 mg, tyloxapol - 0.1 mg, disodium edetate - 0.1 mg, mannitol - 24 mg, sodium chloride - 4 mg, sodium hydroxide and / or hydrochloric acid - to adjust the pH, purified water - to 1 ml.

• Individual hypersensitivity to the components of the drug, as well as to other non-steroidal anti-inflammatory drugs.

• Bronchial asthma.

• Hives.

• Acute rhinitis.

• Age up to 18 years (the safety and efficacy of the drug in children have not been studied).

pharmachologic effect

Nepafenac is a precursor of the active form of non-steroidal anti-inflammatory drugs with analgesic and anti-inflammatory effects; it penetrates the cornea of ??the eye, where it is converted into amfenac, the active form, with the help of hydrolases. Amphenac inhibits the action of cyclooxygenase (prostaglandin H synthase), an enzyme required for the production of prostaglandins.

When applied topically, nepafenac reduces eye tissue edema and pain, does not have a significant effect on intraocular pressure.

Pharmacokinetics

Suction

Nevanak is rapidly absorbed through the cornea of ??the eye. Three times daily instillation of the drug Nevanak in both eyes in the blood plasma revealed low measurable concentrations of nepafenac and amfenac after 2 and 3 hours, respectively. Cmax of nepafenac in plasma after topical application is 0.310 ± 0.104 ng / ml; Cmax of amphenac - 0.422 ± 0.121 ng / ml.

Cmax of nepafenac on average in aqueous humor is observed after 1 hour.

Distribution

Amphenac has a high affinity for serum albumin. In vitro binding to rat albumin, human albumin and human serum was 98.4%, 95.4% and 99.1%, respectively.

Studies in rats have shown that radioactively labeled substances associated with the active substance are widely distributed in the body after single and multiple oral doses of 14 C-nepafenac.

Metabolism

When applied topically, under the action of intraocular hydrolases, nepafenac undergoes rapid hydrolysis to amfenac.

Further metabolism of amphenac proceeds by hydroxylation of the aromatic ring, which leads to the formation of conjugates with glucuronic acid. Radiochromatographic analysis carried out before and after hydrolysis with the participation of P-glucuronidase showed that all metabolites were presented in the form of conjugates with glucuronic acid, with the exception of amphenac. Amphenac was the main metabolite in plasma, accounting for about 13% of the total radioactivity detected in plasma. The second most common metabolite in plasma was the metabolite 5-hydroxynepafenac with 9% of the total radioactivity at Cmax.

Withdrawal

Nepafenac is excreted mainly by the kidneys (about 85% of the radioactive label after oral administration of 14 C-nepafenac is found in urine, about 6% in feces), however, the concentrations of nepafenac and amphenac in urine cannot be quantified.

Interaction

In in vitro studies, neither; neither nepafenac nor amfenac inhibit the metabolic activity of human cytochrome P450 (isoenzyme CYP1A2, 2C9, 2C19, 2D6, 2E1 and ZA4) at concentrations up to 300 ng / ml. Therefore, with simultaneous use with other drugs, interaction with the involvement of cytochrome P450 isoenzymes is unlikely. Plasma protein binding interactions are also unlikely.

There are no data on the simultaneous use of Nevanak and prostaglandin analogues. Given their mechanisms of action, simultaneous use is not recommended.

If necessary, it can be used in combination with other ophthalmic preparations for topical use. In this case, the interval between their application should be at least 5 minutes.

Overdose

There are no data on drug overdose. In case of contact with the eyes of an excessive amount of the drug, it is recommended to rinse the eyes with warm water.

special instructions

Patients should avoid exposure to sunlight.

The use of topical NSAIDs can lead to the development of keratitis. In some susceptible patients, long-term use of topical nonsteroidal anti-inflammatory drugs can cause rupture of epithelial cells, thinning of the cornea, corneal erosion, corneal ulceration, or corneal perforation. These side effects can create a risk of loss of vision. Patients with signs of rupture of corneal epithelial cells should immediately stop using the drug, and be monitored to monitor the condition of the cornea.

Topical NSAIDs can slow or delay the healing process. Topical glucocorticosteroids are also known to slow or delay healing. The simultaneous use of NSAIDs for topical use and GCS for topical use can slow down or delay the healing process.

Experience with topical NSAIDs suggests that patients with complications from ophthalmic surgery, corneal denervation, corneal epithelial defects, diabetes mellitus, superficial eye diseases (such as dry eye syndrome), rheumatoid arthritis, or repeated short-term surgical interventions time, may have an increased risk of developing adverse reactions from the cornea, which may pose a threat of loss of vision. Topical NSAIDs should be used with caution when treating these patients. Long-term use may increase the risk and severity of corneal adverse reactions.

The use of topical NSAIDs in combination with eye surgery can cause intense bleeding in the tissues of the eye (including hyphema). The drug Nevanak should be used with caution in patients with a history of bleeding tendencies, or if patients are receiving other drugs that can increase the blood clotting time.

There are no data on the simultaneous use of prostaglandin analogues and Nevanak. Given their mechanisms of action, simultaneous use is not recommended.

The preparation contains a preservative benzalkonium chloride, which may cause eye irritation and discoloration of soft contact lenses. In addition, contact lens wear is not recommended during the postoperative period after cataract surgery. It is not recommended to use contact lenses when treating with Nevanak.

Studies have shown that benzalkonium chloride, which is contained in Nevanak, can cause punctate keratitis and / or toxic ulcerative keratitis. Therefore, with frequent or prolonged use of the drug, careful medical monitoring of the patient's condition is necessary.

The use of NSAIDs for topical application may interfere with the timely recognition of signs of acute ocular infection, because they do not have any antimicrobial properties. In the case of an ocular infection, the use of non-steroidal anti-inflammatory drugs for topical use simultaneously with antibacterial agents should be carried out with precautions.

Cross sensitivity

With the use of nepafenac, there is the possibility of developing cross-sensitivity to acetylsalicylic acid, phenylacetic acid derivatives, and other NSAIDs.

Do not touch the tip of the dropper bottle to any surface to avoid contamination of the bottle and its contents.

The bottle must be closed after each use.

Influence on the ability to drive vehicles and use mechanisms

After using the drug, a temporary decrease in the clarity of visual perception is possible, and until it is restored, it is not recommended to drive a car and engage in activities that require increased attention and reaction.