Naquan eye drops 0.09% 5ml, 1pc

Composition

>1 ml of the solution contains: Active ingredient: bromfenac sodium sesquihydrate – 1.035 mg, equivalent to bromfenac-0.9 mg. Auxiliary substances: boric acid 11 mg, sodium borate – 11 mg, sodium sulfite,2 mg of disodium edetate dihydrate – 0.2 mg, povidone (K 30),20 mg, Polysorbate 80 1.5 mg benzalkonium chloride solution 10%, and 0.1 µl of sodium hydroxide to a pH of 8.0 and 8.6, purified water to 1 ml.

Pharmacological action

Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) whose anti-inflammatory effect is realized by blocking prostaglandin synthesis when cyclooxygenase 1 and 2 are inhibited. In vitro studies, bromfenac inhibited prostaglandin synthesis in the rabbit ciliary body. The concentration of semi-maximal inhibition (IC50) for bromfenac (1.1 mmol) was lower than for Indometacin (4.2 mmol) and pranoprofen (11.9 mmol). In an experimental model of uveitis in rabbits, bromfenac at concentrations of 0.02%,0.05%,0.1% and 0.2% inhibited almost all symptoms of ocular inflammation. Pharmacokinetics: Absorption Bromfenac effectively penetrates the cornea of patients suffering from cataracts: with a single use, the average peak concentration in aqueous humor is 79±68 ng / ml 150-180 minutes after application. This concentration is maintained for 12 hours in aqueous humor, while maintaining measurable levels of concentration in the main tissues of the eye, including the retina, for up to 24 hours. When bromfenac eye drops were administered twice daily, plasma concentrations were not quantifiable. Distribution Bromfenac actively binds to plasma proteins. According to an in vitro study, protein binding in human plasma was 99.8%. In vitro studies showed no biologically significant binding to melanin. According to a study in rabbits using radioactively labeled bromfenac, the maximum concentration after topical application is observed in the cornea, high – in the conjunctiva and watery moisture of the eye, low-in the lens and vitreous body. According to the results of an in vitro study, the main metabolism of bromfenac is carried out by the enzyme CYP2C9, which is absent in the iridociliary zone, retina and vascular membrane. The level of this enzyme in the cornea is less than 1% compared to the corresponding liver level. When taken orally in humans, the plasma is mainly found unchanged starting substance. Several conjugated and unconjugated metabolites have been isolated, the main one being cyclic amide, which is excreted in the urine. Elimination When instilled in the eyes, the half-life of bromfenac from the watery eye moisture is about 1.4 hours, which indicates rapid elimination. After oral use of 14C-bromfenac to healthy volunteers, it was found that the drug is mainly excreted in the urine (about 82% of the administered dose), while about 13% of the administered dose is excreted in the faeces.

Indications

Treatment of non-infectious inflammatory diseases of the anterior segment of the eye and postoperative inflammation.

Use during pregnancy and lactation

There are no sufficient data on the use of bromfenac in pregnant women. Animal studies have demonstrated the presence of reproductive toxicity. The potential risk to humans is unknown. Since systemic exposure after treatment with the drug in non-pregnant women is insignificant, the risk during pregnancy can be considered low.

However, due to the known effects of drugs that inhibit prostaglandin biosynthesis on the fetal cardiovascular system (duct closure), the use of this drug in the third trimester of pregnancy should be avoided. In general, the use of this drug during pregnancy is not recommended, except in cases where the benefit outweighs the potential risk.

Contraindications

This drug is contraindicated in patients who have a history of hypersensitivity to any component of the drug.

This drug is contraindicated in patients who have attacks of bronchial asthma, urticaria and symptoms of acute rhinitis are aggravated by taking acetylsalicylic acid and other NSAIDs.

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

Side effects

Adverse reactions to the drug were observed in 72 of 3,843 patients (1.87%), data on which were obtained in clinical studies or with post-marketing use. Serious adverse reactions included corneal erosion in 16 cases (0.42%), conjunctivitis (including conjunctival injection and conjunctival follicles) in 11 cases (0.29%), blepharitis in 9 cases (0.23%), irritation in 8 cases (0.21%), eye pain [transient] in 8 cases (0.21%), superficial punctate keratitis in 6 cases (0.16%), pruritus in 6 cases (0.16%), epithelial detachment cornea in 1 case (0.03%) and burning sensation [eyelids] in 1 case (0.03%).

Adverse reactions are classified according to the following frequency gradation: :

Very common >1/10>

Common ≥1/100 to <1/10

Rarely ≥1/10000 to <1/100

Very rare <1/10000

In each group, adverse events are classified according to decreasing severity and grouped according to frequency of occurrence and organ-system class.

The table below describes the adverse reactions.

(*)If any adverse reactions occur, discontinue treatment with the drug.

(**) If clinically significant adverse reactions occur, such as the development of corneal epithelial diseases, etc., it is necessary to stop treatment with this drug and take appropriate measures.

(***) Serious adverse reaction, isolated reports from the experience of post-marketing use of the drug.

Interaction

Interaction studies with other drugs have not been conducted.

How to take, course of use and dosage

1-2 drops of the drug in the conjunctival sac twice a day for no more than 15 days.

In case of missing a dose of the drug, the drug should be used as soon as possible in the dosage indicated in the instructions for use. If the missed dose of the drug is about 24 hours, the drug should be used at the next scheduled time, without doubling the dose to compensate for the missed dose.

Overdose

At the moment, there is no information about overdose with topical application in humans.

According to foreign reports, patients who took the drug bromfenac sodium orally in a total dose exceeding 1500 mg for a long period of time more than 1 month, serious liver function disorders (including deaths) were observed. In this regard, if abnormalities are detected that are suspected to be associated with early symptoms of liver failure, it is necessary to stop treatment with this drug and take appropriate measures.

Special instructions

This drug should be used as part of symptomatic treatment, and not for the purpose of etiotropic therapy. This medicine should only be used as an eye drop. This medicine should be instilled with caution, making sure that the tip of the bottle does not touch the surface of the eye. This medicine contains sodium sulfite, which can cause allergic reactions, including anaphylaxis symptoms and life-threatening or less severe asthmatic episodes in susceptible patients. All topical NSAIDs can slow or delay healing, similar to topical corticosteroids. Concomitant use of NSAIDs and topical steroids may increase the likelihood of healing problems. Cross-sensitivitythere is a possibility of cross-sensitivity to acetylsalicylic acid, phenylacetylic acid derivatives, and other NSAIDs. Therefore, caution should be exercised when treating individuals who have previously experienced sensitivity to these drugs, and the potential risks and benefits should be carefully evaluated. Special patient groupssusceptible patients Prolonged use of topical NSAIDs, including bromfenac, may result in epithelial rupture, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation. These events may threaten vision loss. Patients with signs of corneal epithelial damage should immediately stop using topical NSAIDs and carefully monitor the health of the cornea. Therefore, in patients at risk, concomitant use of ophthalmic corticosteroids with NSAIDs may lead to an increased risk of corneal adverse events.Post-marketing experience with topical NSAIDs Post-marketing experience with topical NSAIDs indicates that patients with complications after ophthalmic surgery, corneal denervation, corneal epithelial defects, diabetes mellitus and superficial eye diseases, rheumatoid arthritis, or repeated ophthalmic surgery performed over a short period of time may have an increased risk of corneal adverse events that may threaten vision loss. Topical NSAIDs should be used with caution in these patients. It has been reported that ophthalmic NSAIDs can cause increased bleeding in the eye tissues (including hyphema) in combination with ophthalmic surgery. Topical NSAIDs should be used with caution in patients who have a history of bleeding, or if patients are receiving other medications that may increase blood clotting time. Eye infections It is necessary to carefully monitor the use of the drug and prescribe it with caution to patients with inflammation caused by infections, as the drug can mask the symptoms of infectious eye diseases. The use of contact lenses in general, wearing contact lenses during treatment with this drug is not recommended. In this regard, patients are not recommended to wear contact lenses unless clearly instructed by the attending physician. Excipients: Since benzalkonium chloride is part of the drug, patients should be carefully monitored for frequent or prolonged use of the drug. Benzalkonium chloride is known to discolor soft contact lenses. Avoid contact with soft contact lenses. Benzalkonium chloride has been reported to cause eye irritation, pinpoint keratopathy, and / or toxic ulcerative keratopathy. Use in patients with hepatic and renal insufficiency The effect of the drug in patients with renal and hepatic insufficiency has not been studied. Influence on the ability to drive vehicles and mechanisms:After instillation, temporary blurred vision may occur. If blurred vision develops after instillation, it is necessary to refrain from driving a car or working with mechanisms until visual clarity is restored.

Storage conditions

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years. Do not use after the expiration date indicated on the package. After the first opening of the bottle, it should be stored for no more than 30 days.

Active ingredient

Bromfenac

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

For adults as directed by your doctor

Indications

Inflammatory eye diseases