Ivinac-Solopharm eye drops 0.09%, 5ml

Composition

Active ingredient: Bromfenac sodium sesquihydrate 1.035 mg, based on bromfenac 0.9 mg

Auxiliary substances:

• Benzalkonium chloride 0.01 mg
• Hydroxypropyl Betadex 20.0 mg
• Boric acid 12.5 mg
• Sodium Tetraborate Decahydrate 12.5 mg
• Polysorbate 80 1.5 mg
• Disodium edetate dihydrate 0.2 mg
• Sodium hydroxide solution 10 M or hydrochloric acid solution 1 M to pH 8.3
• Water for injection up to 1 ml

Pharmacological action

Pharmacotherapy group

Nonsteroidal anti-inflammatory drug (NSAID).

ATX Code:

S01 SUN 11

Pharmacological properties

Pharmacodynamics

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

Suction

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 no biologically significant binding to melanin was detected.

According to a study in rabbits using radiolabeled bromfenac, the maximum concentration after topical application is observed in the cornea, while the highest concentration is observed in the conjunctiva and watery moisture of the eye. Low-in the lens and vitreous body.

Metabolism

Based on 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.

Deduction

When instilled into the eyes, the half-life of bromfenac from the watery moisture of the eye 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 (after cataract extraction, etc. ).

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

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

The 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%).

Interaction

Studies on the interaction of bromfenac with other drugs have not been conducted.

How to take, course of use and dosage

Instillation into the conjunctival sac.

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

If you miss a dose of the drug, it 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.

Treatment of postoperative inflammation: one drop once a day. Treatment begins 1 day before surgery and continues for the first 14 days of the postoperative period (including the day of surgery).

Treatment of non-infectious inflammatory diseases of the anterior segment of the eye: one drop twice a day. The course of treatment is determined by the doctor depending on the severity of the condition.

Procedure for working with the bottle (without a stop):

Procedure for working with a bottle equipped with a stop:

After opening the bottle, the drug can be used for 1 month. After this period, the drug should be discarded.

If the bottle is visibly damaged, the drug should not be used.

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.

Description

Transparent solution of greenish-yellow color.

Special instructions

The drug should be used as part of symptomatic treatment, and not for the purpose of etiotropic therapy.

The drug should only be used as an eye drop.

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-sensitivity

There is a potential for 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 groups

In susceptible 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-registration application experience

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 within 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

The use of the drug should be carefully monitored and prescribed with caution to patients with inflammation caused by infections, as the drug may mask the symptoms of infectious eye diseases.

Using contact lenses

In general, wearing contact lenses during treatment with the drug is not recommended. In this regard, patients are not recommended to wear contact lenses unless clearly instructed by the attending physician.

Auxiliary substances

Benzalkonium chloride, which is often used in ophthalmic preparations as a preservative, can cause spot keratopathy and / or toxic ulcerative keratopathy. Since the drug contains benzalkonium chloride, careful monitoring is necessary in the case of frequent or prolonged use in patients with dry eye syndrome or in cases of corneal damage. Benzalkonium chloride can change the color of soft contact lenses. It is necessary to remove soft contact lenses before applying the drug and put them back on 15 minutes after instillation.

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 vehicles and mechanisms until visual clarity is restored.

Form of production

Eye drops 0.09%.

2.5 ml or 5 ml in a bottle with a low-density polyethylene dropper and a lid with first opening control, or in a high-pressure polyethylene dropper bottle complete with a screw-on lid and a dropper stopper, or in a low-density polyethylene bottle complete with a dropper stopper and a lid with first opening control, or in a polyethylene terephthalate bottle with a plastic dropper and a lid with first opening control.

1 bottle in a foil bag or without a bag.

1 bottle or 1 bag of foil film together with the instructions for use, the stop device or without it in a pack of cardboard.

Storage conditions

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

Shelf

life is 3 years. After opening the bottle – 1 month. Do not use after the expiration date!

Active ingredient

Bromfenac

Conditions of release from pharmacies

By prescription

Dosage form

eye drops