Nevanak - instructions for use, dose, side effects, contraindications

Active substanceNepafenacNepafenac

Similar drugsTo uncover

Nevanac®

drops d / eye

ALKON PHARMACEUTICS, LLC Russia

Dosage form: & nbspeye drops

Composition:

Composition 1 ml of the preparation.

Active substance: Nepafenac 1.0 mg.

Excipients: benzalkonium chloride (as 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 until the pH is adjusted, water purified to 1 ml.

Description:homogeneous suspension from light yellow to light orange color.

Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug.

ATX: & nbsp

S.01.B.C Non-steroidal anti-inflammatory drugs (NSAIDs)

S.01.B.C.10 Nepafenac

Pharmacodynamics:

Nepaphenac is a precursor of the active form of non-steroidal anti-inflammatory drugs with anti-inflammatory and analgesic action. At the local application of nepafenac penetrates through the cornea of the eye, where with the help of hydrolases it is converted into amfenac, 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 edema of the eye tissues and pain, does not have a significant effect on intraocular pressure.

Pharmacokinetics:

Absorption. Nevanak® is rapidly absorbed through the cornea of the eye. With a threefold 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. The maximum value of the average concentration of napafenac (C_max) in plasma after topical application is 0.310 ± 0.104 ng / ml; amfenac (C_max) -

0.422 ± 0.121 ng / ml.

The maximum concentration of napafenac on average in aqueous humor is observed after 1 hour.

Distribution. Amfenac has a high affinity for serum albumins. In vitro the 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 ¹⁴C-Nepafenac.

Metabolism. With topical application under the influence of intraocular hydrolases nepafenac undergoes rapid hydrolysis to amfenac.

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.

Excretion. Nepafenac is excreted mainly by the kidneys (about 85% of the radioactive label when administered orally ¹⁴C-napafenac is found in urine, about 6% in feces), but the concentrations of nepafenac and amfenac in urine are not quantifiable.

Indications:

Preventive maintenance and treatment of postoperative pain and inflammatory phenomena during surgical interventions for the removal of cataracts.

Contraindications:

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

Bronchial asthma, urticaria, acute rhinitis caused by the intake of aspirin or other nonsteroidal antiinflammatory drugs.

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

Pregnancy and lactation:

Not recommended for use in 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 in 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.

Dosing and Administration:

Locally. Shake the bottle before use!

1 drop in the conjunctival sac of the eye (eye) 3 times a 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 to 120 minutes before the operation, it is necessary to drip an additional drop of the drug.

Side effects:

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 % cases - iritis, keratitis, corneal deposits, choroidal effusion, discharge from the eyes, photophobia, eye irritation, allergic conjunctivitis, disorders of the eyelids, discomfort in the eyes, increased tearing, conjunctival hyperemia.

Systemic side effects. In 1-10% of cases - a headache. In 1-4% of cases - increased blood pressure, nausea, vomiting, sinusitis. In 0.1-1 % cases - dry mouth, skin stretchiness (dermatochalasis), hypersensitivity.

Post-marketing observations (frequency unknown): ulcerative keratitis,

defect / disease of the corneal epithelium, damage to the cornea, the formation of an inflammatory infiltrate in the anterior chamber of the eye, deterioration of the healing process of the cornea, reduced visual acuity, a 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!

Experience with non-steroidal anti-inflammatory drugs for topical application 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 procedures performed for a short period of time, may have an increased risk of developing side effects from the cornea, which can create a threat of vision loss.

Overdose:

Data on drug overdose are absent.

If eye contact is excessive, it is recommended to wash eyes with warm water.

Interaction:

In studies in vitro nor nepafenac, nor amphenac does not inhibit the metabolic activity of human cytochrome P450 (isoenzyme CYP1A2, 2C9, 2C19, 2D6, 2E1 and 3A4) at a concentration of 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.

Special instructions:

Patients should avoid exposure to sunlight.

The use of non-steroidal anti-inflammatory drugs 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 non-steroidal anti-inflammatory drugs for topical application can slow or delay the healing process. It is also known that glucocorticosteroids for topical application slow or delay healing.The simultaneous use of non-steroidal anti-inflammatory drugs for topical application and glucocorticosteroids for topical application may slow or delay the healing process.

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 It is a threat to vision loss. Non-steroidal anti-inflammatory drugs 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 non-steroidal anti-inflammatory drugs for topical use in combination with a surgical procedure on the eyes can cause intense bleeding in the eye tissues (including hyphema).The drug Nevanac® should be used with caution in patients who have a history of bleeding tendency, or if patients receive other medications that may increase clotting time.

Data on the simultaneous use of prostaglandin analogues and the drug Nevanak® are not available. Given the mechanisms of their action, 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, 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 preparation 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 non-steroidal anti-inflammatory drugs for topical use may prevent timelyrecognition of signs of acute eye infection, t. 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.

Cross-sensitivity

With the use of nepafenac, it is possible to develop cross-sensitivity to acetylsalicylic acid, phenylacetic acid derivatives, as well as other non-steroidal anti-inflammatory drugs!

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.

Effect on the ability to drive transp. cf. and fur:

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.

Form release / dosage:

Eye drops 0.1%.

5 ml per bottle-dropper "Droptainer™" from low density polyethylene. By

1 A bottle with instructions for use in a pack of cardboard.

Packaging:eye drops 0.1% (bottle-dropper "Droptainer ™") 5 ml x 1

Storage conditions:

Store at temperatures between 2 and 30 ° C out of the reach of children.

Shelf life:

2 of the year.

Use within 4 weeks after opening the vial.

Do not use after the expiry date printed on the package!

Terms of leave from pharmacies:On prescription

Registration number:LP-001118

Date of registration:03.11.2011

The owner of the registration certificate:ALKON PHARMACEUTICS, LLC ALKON PHARMACEUTICS, LLC Russia

Manufacturer: & nbsp

ALCON-COUVREUR, n.v. s.a. Belgium

Representation: & nbspALKON PHARMACEUTICS LLCALKON PHARMACEUTICS LLCRussia

Information update date: & nbsp07.08.2015

Illustrated instructions

Instructions

Nevanac® (Nevanac®)