Nevanac, eye drops 0.1%, 5 ml

Composition

Eye drops 0.1% in the form of a suspension from light yellow to light orange color.

1 ml-nepafenac 1 mg

Auxiliary substances:

benzalkonium chloride (as a 50% solution) 0.05 mg,

carbomer 974 P 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,

purified water to 1 ml

. Pharmacological action

Nepafenac is a precursor to the active form of nonsteroidal anti-inflammatory drugs with analgesic and anti-inflammatory effects, it penetrates through the cornea of the eye, where it is converted to amphenac, the active form, by hydrolases. Amphenac inhibits the action of cyclooxygenase (prostaglandin-N-synthase), an enzyme necessary for the production of prostaglandins.

When applied topically, nepafenac reduces eye tissue edema and pain, but has no significant effect on intraocular pressure.

Pharmacokinetics

Suction

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

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

Distribution

Amphenac 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 radioactively labeled substances associated with the Active ingredient are widely distributed in the body after a single and repeated use of oral doses of 14C-nepafenac.

Metabolism

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

Further metabolism of amphenac proceeds by hydroxylation of the aromatic ring, which leads to the formation of conjugates with glucuronic acid. Radiochromatographic analysis performed before and after hydrolysis with 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 5-hydroxynepafenac with 9% total radioactivity at Cmax.

Deduction

Nepafenac is mainly excreted by the kidneys (about 85% of the radioactivity label for oral administration of 14C-nepafenac is detected in the urine, about 6% – in faeces), but the concentrations of nepafenac and amphenac in the urine are not quantifiable.

Indications

Prevention and treatment:

• Postoperative pain.
• Inflammatory phenomena during surgical interventions for cataract removal.

Use during pregnancy and lactation

It is not recommended for use during pregnancy and lactation. If it is necessary to prescribe during lactation, it is recommended to stop breastfeeding for the duration of treatment.

Animal testing revealed reproductive toxicity. When studying the effects of nepafenac 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 malformations of the offspring.

Use in children

Contraindicated in children under 18 years of age.

Contraindications

• Individual hypersensitivity to the components of the drug, as well as to other nonsteroidal anti-inflammatory drugs.
• Caused by taking acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs:
  • Bronchial asthma.
  • Urticaria.
  • Acute rhinitis.
• Age up to 18 years (safety and efficacy of the drug in children have not been studied).

Side effects

• Pinpoint keratitis, pain or itching in the eye, blurred vision, dry conjunctiva, crusting along the edge of the eyelids, iritis, keratitis, choroidal effusion, corneal deposits, eye discharge, eye irritation, photophobia.
• Allergic conjunctivitis, eye discomfort, lacrimation, conjunctival hyperemia.
• Headaches, dyspepsia, dry mouth, sinusitis, skin stretching (dermatochalasis), hypersensitivity.
• Ulcerative keratitis, pathologies of the corneal epithelium, corneal damage, inflammatory infiltrates of the anterior chamber of the eye, slowing of the corneal healing process, corneal scar, decreased visual acuity, corneal opacity.

At signs of corneal damage, the use of the drug is immediately canceled, and the cornea is carefully examined, since from the experience of using nonsteroidal anti-inflammatory drugs, it is known that patients with complications after ophthalmic surgical interventions, as well as with corneal epithelial defects, corneal denervation, diabetes mellitus, superficial eye diseases ( for example, dry eye syndrome), as well as rheumatoid arthritis or repeated surgical interventions, have a high risk of corneal side effects that they pose a threat of loss of visual functions.

Interaction

In in vitro studies, neither nepafenac nor amphenac inhibited the metabolic activity of human cytochrome P 450 (isoenzyme CYP1A2,2C9,2C19,2D6,2E1AND ZA4) at concentrations up to 300 ng / ml. Therefore, when used concomitantly with other medicinal products, interactions involving cytochrome P450 isoenzymes are unlikely. Interactions mediated by binding to plasma proteins are also unlikely.

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

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

How to take, course of administration and dosage

Locally. Shake the bottle before use.

1 drop into the conjunctival sac of the eye (eye) 3 times a day.

Treatment begins 1 day before cataract surgery and continues for the first 2 weeks of the postoperative period (including the day of surgery).30-120 minutes before the operation, an additional drop of the drug should be instilled.

Overdose

There are no data on overdose of the drug.

If an excessive amount of the drug gets into the eyes, it is recommended to rinse the eyes with warm water.

Special instructions

When using Nevanac, patients should avoid sun exposure.

The product contains the 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 cataract surgery. It is not recommended to use contact lenses during treatment with Nevanak.

Experience with topical NSAIDs suggests that patients with complications following surgical ophthalmic procedures, corneal denervation, corneal epithelial defects, diabetes mellitus, superficial eye diseases (such as dry eye syndrome), rheumatoid arthritis, or repeated surgical procedures performed within a short period of time may have an increased risk of corneal adverse reactions, which may pose a risk of vision loss. Topical NSAIDs should be used with caution in the treatment of such patients. Prolonged use may increase the risk and severity of corneal adverse reactions.

The use of the drug, as well as other topical NSAIDs, can cause keratitis. Prolonged use may increase the risk of corneal side effects or increase the severity of corneal side effects.

The use of the drug in combination with surgical intervention on the eyes can cause intense bleeding in the eye (including hyphema).

Nevanac should be used with caution in patients who have a history of a tendency to bleed, or when patients are receiving other medications that increase blood clotting time.

The drug contains benzalkonium chloride, which can cause eye irritation and discoloration in soft contact lenses, so they are not used. In addition, the use of contact lenses is prohibited during the recovery period after cataract surgery.

Do not touch the dropper bottle to any surface, in order to avoid contamination of the bottle and infection of its contents. The bottle must be tightly closed after each use.

Cross-sensitivity

When using nepafenac, there is a possibility of developing cross-sensitivity to acetylsalicylic acid, fennelacetic acid derivatives, as well as other NSAIDs.

Influence on the ability to drive motor vehicles and manage mechanisms

After applying Nevanak, there may be a temporary decrease in visual acuity, as well as clarity of visual perception, so driving a car or engaging in activities that require an adequate response and increased attention is prohibited until visual functions are fully restored.

Form of production

Eye drops

Storage conditions

At a temperature of 2-30 °C

Shelf life

2 years

Active ingredient

Nepafenac

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

For adults as directed by your doctor

Indications

Cataract

Weight

Weight: 17 gr.