Nevanak eye drops 0.1% 5ml
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Active ingredients
Nepafenak
Release form
Drops
Composition
On 1 ml: nepafenak 1 mg. Excipients: benzalkonium chloride (as a 50% solution) 0.05 mg, carbomer 974P 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 bring the pH, water purified to 1 ml.
Pharmacological effect
Nepafenac is a precursor of the active form of nonsteroidal anti-inflammatory drugs with anti-inflammatory and analgesic effects. When applied topically, nepafenak penetrates the cornea of the eye, where with the help of hydrolases it is transformed into amphenac, the active form. Amphenac inhibits the action of cyclooxygenase (prostaglandin H-synthase), an enzyme necessary for the production of prostaglandins. When applied topically, nepafenac reduces eye tissue swelling and pain, does not have a significant effect on intraocular pressure.
Pharmacokinetics
Suction Nevanak is rapidly absorbed through the cornea. With three times daily instillation of the drug Nevanak in both eyes in the blood plasma, low measured concentrations of nepafenac and amphenaca were detected after 2 and 3 hours, respectively. Cmax of nepafenac in plasma after topical administration is 0.310 ± 0.104 ng / ml; Cmax amphenac - 0.422 ± 0.121 ng / ml. Cmax nepafenac on average in aqueous humor is observed after 1 hour. Distribution Amfenac 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 showed that radioactively labeled substances associated with the active substance are widely distributed in the body after a single and repeated use of oral doses of 14C -naphavenaca.Metabolism. When applied locally by the action of intraocular hydrolases, nepafenac undergoes rapid hydrolysis to amphenac. The further metabolism of amfenac proceeds by hydroxylation. aromatic ring, which leads to the formation of conjugates with glucuronic acid. Radiochromatographic analysis performed 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 - the share of this substance accounted for about 13% of the total radioactivity detected in plasma.The second occurrence in plasma was the 5-hydroxynepaphenac metabolite with 9% of the total radioactivity at Cmax. Excretion of Nepafenak is excreted mainly by the kidneys (about 85% of the radioactive label when administered orally with 14C-nepafenac in the urine, about 6% in feces), however urinary amphenaca is not quantifiable.
Indications
Prevention and treatment of postoperative pain and inflammation during surgery for cataract removal.
Contraindications
- bronchial asthma, urticaria, acute rhinitis caused by taking acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs; - age up to 18 years (the safety and efficacy of the drug in children have not been studied); - hypersensitivity to the components of the drug and to other NSAIDs.
Use during pregnancy and lactation
Not recommended for use during pregnancy and lactation. If you need an appointment during lactation, breastfeeding is recommended to stop at the time of treatment. Animal tests revealed reproductive toxicity. When studying the effects of nepafenak on the reproductive organs of rats, taking toxic doses of> 10 mg / kg resulted in dystocia, an increase in the number of spontaneous abortions at the post-implantation stage, a decrease in body weight and embryo growth, a decrease in embryo survival. In pregnant rabbits, the administration of low-toxic doses of 30 mg / kg led to an increase in progeny developmental defects.
Dosage and administration
Locally. Shake the bottle before use. For 1 drop in the conjunctival sac of the eye (s) 3 times / 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). 30-120 minutes before the operation, you need to drop an extra drop of the drug.
Side effects
Local: in 1-10% of cases, there is observed keratitis, pain and itching in the eye, blurred vision, dry conjunctiva, foreign body sensation, formation of crusts at the edges of the eyelids. In 0.1-1% of cases - iritis, keratitis, deposits in the cornea, choroidal effusion, eye discharge, photophobia, eye irritation, allergic conjunctivitis, blemishes of the eyelids, discomfort in the eyes, increased tearing, conjunctival hyperemia. Systemic side effects: 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 elasticity (dermatochalasis), increased sensitivity, sensitivity. Postmarketing observations (frequency unknown): ulcerative keratitis, corneal epithelium defect / disease, corneal damage, formation of inflammatory infiltration in the anterior chamber of the eye, deterioration of the process corneal healing, reduced visual acuity, scar on the cornea, corneal clouding. Patients with signs of corneal damage should immediately discontinue use of the drug and carefully examine the condition cornea. Experience with nonsteroidal anti-inflammatory drugs for topical use suggests that patients with complications from surgical ophthalmologic interventions, corneal denervation, corneal epithelium defects, diabetes mellitus, superficial eye diseases (dry eye syndrome), rheumatoid arthritis or repeated surgical interventions performed during short period of time, there may be an increased risk of corneal adverse reactions that may create threat of vision loss.
Overdose
Data on drug overdose are not available. In case of contact with an excessive amount of the drug, it is recommended to wash the eyes with warm water.
Interaction with other drugs
In in vitro studies, neither nepafenak nor amphenac inhibits the metabolic activity of human cytochrome P450 (CYP1A2, 2C9, 2C19, 2D6, 2E1, and ZA4 isoenzymes) at concentrations up to 300 ng / ml. Therefore, with simultaneous use with other drugs, interaction with the involvement of cytochrome P450 isoenzymes is unlikely. Also, interactions mediated by binding to plasma proteins are unlikely. There are no data on the simultaneous use of the drug Nevanak and prostaglandin analogues. Given the mechanisms of their action, simultaneous use is not recommended. If necessary, it can be used in combination with other ophthalmologic preparations for topical use. In this case, the interval between their use should be at least 5 minutes.
special instructions
Patients should avoid exposure to sunlight. The use of NSAIDs for topical use may lead to the development of keratitis.In some susceptible patients, long-term use of nonsteroidal anti-inflammatory drugs for local use can cause epithelial cell rupture, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation. These side effects may create a risk of vision loss. Patients with signs of rupture of the corneal epithelium cells should immediately discontinue use of the drug, and be monitored to monitor the state of the cornea. The use of NSAIDs for topical administration can slow down or delay the healing process. It is also known that topical glucocorticosteroids slow down or delay healing. Simultaneous use of NSAIDs for local use and GCS for local use can slow down or delay the healing process. The experience of using NSAIDs for local use suggests that patients with complications from surgical ophthalmic interventions, cornea denervation, corneal epithelium defects, diabetes, superficial eye diseases (for example dry eye syndrome), rheumatoid arthritis or repeated surgical interventions carried out over a short period of time and may have an increased risk of adverse reactions on the part of the cornea that may pose a threat of loss. NSAIDs for topical use should be used with caution in treating such patients. Prolonged use may increase the risk and severity of adverse reactions from the cornea. The use of NSAIDs for local use in combination with surgery on the eyes can cause intense bleeding in the eye tissue (including hyphema). The drug Nevanak should be used with caution in patients with a history of a tendency to bleeding, or if patients receive other medications that can increase blood clotting time. There are no data on the simultaneous use of prostaglandin and Nevanak analogues. Given the mechanisms of their action, the simultaneous use is not recommended. The drug contains a preservative benzalkonium chloride, which can cause eye irritation and discoloration of soft contact lenses. In addition, the wearing of 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 Nevanak. Studies have shown that benzalkonium chloride, which is contained in the Nevanak preparation, can cause acne keratitis and / or toxic ulcerative keratitis. Therefore, with frequent or long-term use of the drug, careful medical monitoring of the patient's condition is necessary. The use of NSAIDs for topical use may impede the timely recognition of signs of an acute eye infection, because they do not possess any antimicrobial properties. In case of development of an eye infection, the use of nonsteroidal anti-inflammatory drugs for topical use simultaneously with antibacterial agents should be carried out with the observance of precautionary measures. dropper bottle to any surface to avoid contamination on and its contents. The bottle must be closed after each use. Effect on the ability to drive vehicles and control mechanisms After the drug is used, 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 requiring increased attention and reaction.