Composition, form of production and packaging
Eye drops 0.1% in the form of a suspension from light yellow to light orange.
Nepafenac 1 mg
Excipients: benzalkonium chloride (as a 50% solution) 0.05 mg, carbomer 974R 5.0 mg, tyloxapol 0.1 mg, disodium edetate 0.1 mg, mannitol 24.0 mg, sodium chloride 4.0 mg, sodium hydroxide and / or hydrochloric acid to adjust pH, water purified to 1 ml.
5 ml - a dropper bottle (1) "Droptainer" from low density polyethylene - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Nepaphenac is a precursor of the active form of non-steroidal anti-inflammatory drugs with anti-inflammatory and analgesic action. With topical application, nepafenac penetrates through the cornea of вЂ‹вЂ‹the eye, where hydrolases convert it into amphenac, an active form. Amfenac inhibits the action of cyclooxygenase (prostaglandin-H-synthase), an enzyme necessary for the production of prostaglandins.
With topical application, nepafenac reduces the swelling of the eye tissues and pain, has no significant effect on intraocular pressure.
Nevanak is rapidly absorbed through the cornea of вЂ‹вЂ‹the eye. Three times daily instillation of the drug Nevanak in both eyes in the blood plasma revealed low measured concentrations of napafenac and amfenac after 2 and 3 hours, respectively. C max of napafenac in plasma after topical application is 0.310 В± 0.104 ng / ml; C maxamphenac - 0.422 В± 0.121 ng / ml.
C max of non-pafenac on average in watery moisture is observed after 1 h.
Amfenac has a high affinity for serum albumins. 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 radiolabeled substances associated with the active substance are widely distributed in the body after a single and repeated use of oral doses of 14 C-napafenac.
With topical application under the influence of intraocular hydrolases, napafenac undergoes rapid hydrolysis to amphenac.
Further metabolism of amfenac proceeds by hydroxylation of the aromatic ring, which leads to the formation of conjugates with glucuronic acid. Radiographic chromatographic analysis performed before and after hydrolysis involving P-glucuronidase showed that all metabolites were presented in the form of conjugates with glucuronic acid, with the exception of amfenac. Amphenac was the main metabolite in plasma - this substance accounted for about 13% of the total radioactivity detected in the plasma. The second on the occurrence in the plasma was a metabolite of 5-hydroxynapaphenac with 9% of the total radioactivity at C max .
Nepaphenac is excreted mainly by the kidneys (about 85% of the radioactive label when oral administration of 14 C-napafenac is found in the urine, about 6% in the feces), but the concentrations of nepafenac and amfenac in the urine are not quantifiable.
- prevention and treatment of postoperative pain and inflammatory phenomena during surgical interventions for cataract removal.
Locally. Shake the bottle before use.
1 drop in the conjunctival sac of the eye (eye) 3 times / day. Treatment is started 1 day before surgery for cataract removal and continues for the first 2 weeks of the postoperative period (including the day of the operation). For 30-120 minutes before the operation it is necessary to drip an additional drop of the drug.
Local: in 1-10% of cases, there is spot keratitis, pain and itching in the eye, blurred vision, dry conjunctiva, sensation of foreign body, crust formation on the edges of the eyelids. In 0.1-1% of cases - iritis, keratitis, corneal deposits, choroidal effusion, discharge from the eyes, photophobia, eye irritation, allergic conjunctivitis, eyelid disorders, discomfort in the eyes, increased tearing, conjunctival hyperemia.
Systemic side effects: in 1-10% of cases - headache. In 1-4% of cases - increased blood pressure, nausea, vomiting, sinusitis. In 0.1-1% of cases - dry mouth, skin stretch (dermatochalasis), increased sensitivity sensitivity.
Postmarketing observations (frequency unknown): ulcerative keratitis, corneal epithelial defect / disease, corneal damage, formation of an inflammatory infiltrate in the anterior chamber of the eye, deterioration of the corneal healing process, decreased visual acuity, scar on the cornea, corneal opacity.
Patients with signs of corneal damage should immediately discontinue the use of the drug and carefully examine the condition of the cornea. The experience with non-steroidal anti-inflammatory drugs for topical application suggests that patients with complications after surgical ophthalmic interventions, corneal denervation, corneal epithelial defects, diabetes mellitus, superficial eye diseases (eg, dry eye syndrome), rheumatoid arthritis or repeated surgical interventions for a short period of time, may have an increased risk of developing side effects from the cornea, which can create threat of loss of sight.
- bronchial asthma, urticaria, acute rhinitis caused by the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs;
- age to 18 years (safety and efficacy of the drug in children have not been studied);
- Hypersensitivity to the components of the drug and to other NSAIDs.
PREGNANCY AND LACTATION
It is not recommended to use during pregnancy and lactation. If it is necessary to appoint during lactation, breastfeeding should be stopped for the duration of treatment.
Animal testing revealed reproductive toxicity. When studying the effects of napafenac on the reproductive organs of rats, taking toxic doses> 10 mg / kg led to dystocia, an increase in the number of spontaneous abortions at the post-implantation stage, a decrease in body weight and embryo growth, and a decrease in embryo survival. In pregnant rabbits, taking low-toxic doses of 30 mg / kg led to an increase in the developmental defects of the offspring.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
Patients should avoid exposure to sunlight.
The use of NSAIDs for topical application can lead to the development of keratitis. In some susceptible patients, prolonged use of non-steroidal anti-inflammatory drugs for topical use can cause a rupture of epithelial cells, thinning of the cornea, erosion of the cornea, the formation of an ulcer on the cornea, or perforation of the cornea. These side effects can create a risk of vision loss. Patients with signs of rupturing the corneal epithelium should immediately stop using the drug, and be monitored to monitor the condition of the cornea.
The use of NSAIDs for topical application may slow or delay the healing process. It is also known that glucocorticosteroids for topical application slow or delay healing. Simultaneous application of NSAIDs for topical application and SCS for local administration may slow or delay the healing process.
The experience with topical application of NSAIDs suggests that patients with complications after surgical ophthalmic interventions, denervation of the cornea, defects in the corneal epithelium, diabetes mellitus, superficial eye diseases (eg, dry eye syndrome), rheumatoid arthritis or repeated surgical interventions for a short period time, may have an increased risk of developing side effects from the cornea, which can create a threat of vision loss. NSAIDs for topical use should be used with caution in the treatment of such patients. Long-term use may increase the risk of occurrence and severity of adverse reactions from the cornea.
The use of NSAIDs for topical use in combination with a surgical procedure on the eyes can cause intense bleeding in the eye tissues (including hyphema). The drug Nevanak should be used with caution in patients who have a history of bleeding tendency, or if patients receive other medications that can increase clotting time.
Data on the simultaneous use of prostaglandin analogs and the drug Nevanak are absent. Given the mechanisms of their action, simultaneous use is not recommended.
The drug contains a preservative of benzalkonium chloride, which can cause eye irritation and discoloration of soft contact lenses. In addition, wearing contact lenses is not recommended during the postoperative period after surgery for cataracts. It is not recommended to use contact lenses in the treatment with the drug Nevanak.
Studies have shown that benzalkonium chloride, which is contained in the drug Nevanak, can cause point keratitis and / or toxic ulcer keratitis. Therefore, with frequent or prolonged use of the drug, careful medical supervision of the patients' condition is necessary.
The use of NSAIDs for topical application may interfere with the timely recognition of signs of acute eye infection. they do not possess any antimicrobial properties. In the case of ocular infection, the use of non-steroidal anti-inflammatory drugs for topical administration concomitantly with antibacterial agents should be carried out with precautionary measures.
With the use of nepafenac, it is possible to develop cross-sensitivity to acetylsalicylic acid, derivatives of fennulfacetic acid, as well as other NSAIDs.
Do not touch the tip of the dropper bottle to any surface to avoid contamination of the vial and its contents.
The bottle must be closed after each use.
Impact on the ability to drive vehicles and manage mechanisms
After application of the drug, a temporary decrease in the clarity of visual perception is possible, and before its restoration it is not recommended to drive and engage in activities requiring increased attention and reaction.
Data on drug overdose are absent.
If eye contact is excessive, it is recommended to wash eyes with warm water.
In in vitro studies neither napafenac nor amfenac inhibits the metabolic activity of human cytochrome P450 (isozyme CYP1A2, 2C9, 2C19, 2D6, 2E1 and 3A4) at concentrations up to 300 ng / ml. Therefore, with simultaneous use with other drugs, interaction with the involvement of cytochrome P450 isoenzymes is unlikely.Interactions mediated by binding to plasma proteins are also unlikely.
Data on the simultaneous use of the drug Nevanak and analogues of prostaglandin are absent. Given the mechanisms of their action, simultaneous use is not recommended.
If necessary, can be used in combination with other ophthalmic drugs for topical use. In this case, the interval between their use should be at least 5 minutes.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Keep the drug at a temperature of 2 В° to 30 В° C out of the reach of children.
Shelf life - 2 years.
Use within 4 weeks after opening the vial.
Do not use after the expiry date printed on the package.