NAKVAN - instructions for use, doses, side effects, contraindications

Active substanceBromfenacBromfenac

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Broxinac®

drops d / eye

Sentiss Pharma Pvt. Ltd. India

NAKWAN®

drops d / eye

Senzu Pharmaceutical Co., Ltd. Japan

Dosage form: & nbspeye drops

Composition:

1 ml of the solution contains:

Active substance: bromfenac sodium sesquihydrate 1.035 mg, equivalent to bromfenac 0.9 mg.

Excipients: Boric acid 11 mg, sodium borate 11 mg, sodium sulfite 2 mg, disodium edetate dihydrate 0.2 mg, povidone (K30) 20 mg, polysorbate 80 1.5 mg, benzalkonium chloride 10% solution 0 , 1 μl, sodium hydroxide - to pH 8.0 - 8.6, purified water - up to 1 ml.

Description:

The clear solution is yellow.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

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

S.01.B.C.11 Bromfenac

Pharmacodynamics:

Bromfenac is a non-steroidal anti-inflammatory drug (NSAID) whose anti-inflammatory effect is realized by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase 1 and 2.

In studies in vitro bromfenac inhibited the synthesis of prostaglandins in the rabbit ciliary body. The concentration of half-maximal inhibition (IC50) for bromfenac (1.1 μmol) was lower than for indomethacin (4.2 μmol) and pranoprofen (11.9 μmol).

In the experimental model of uveitis in rabbits bromfenac in concentrations of 0.02%, 0.05%, 0.1% and 0.2% inhibited virtually all symptoms of ocular inflammation.

Pharmacokinetics:

Suction

Bromfenac effectively penetrates the cornea of patients suffering from cataracts: with a single injection, the mean peak the concentration in aqueous humor is 79 ± 68 ng / ml after 150-180 minutes after application. This concentration persists 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 applying eye drops of bromfenac two times a day, plasma concentrations were not quantifiable.

Distribution

Bromfenac actively binds to plasma proteins. According to the research in vitro, binding to proteins in human blood plasma was 99.8%.

Research in vitro did not reveal biologically significant binding to melanin.

According to a study in rabbits using radiolabeled bromfenac, the maximum concentration after topical application is observed in the cornea, high in the conjunctiva and watery eyes, low in the lens and vitreous body.

Metabolism

By the results of the study in vitro, the basic metabolism of bromfenac is carried out by the enzyme CYP2C9, which is absent in the iridociliary zone, retina and choroid. The level of this enzyme in the cornea is less than 1% compared with the corresponding hepatic level.

When administered orally to a person, the plasma in the main is found unchanged starting material. Several conjugated and unconjugated metabolites are isolated, the main one being cyclic amide, which is excreted in the urine.

Excretion

When instilled in the eye, the half-life of bromfenac from the aqueous humor of the eye is about 1.4 hours, which indicates rapid elimination.

After oral administration ¹⁴C-bromfenac by healthy volunteers found that the drug is mainly excreted in the urine (about 82% of the administered dose), while with feces about 13% of the administered dose is excreted.

Indications:

Treatment of noninfectious inflammatory diseases of the anterior part of the eye and postoperative inflammation.

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 intensified when taking acetylsalicylic acid and other NSAIDs.

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

Pregnancy and lactation:

Sufficient data on the use of bromfenac in pregnant women are absent. Animal studies have demonstrated reproductive toxicity. The potential risk to humans is unknown. Since the systemic effect after treatment with the drug in non-pregnant women is negligible, the risk during pregnancy can be considered low.

However, due to the known effects of drugs inhibiting the biosynthesis of prostaglandins on the fetal cardiovascular system (closure of the duct), 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 when the benefits exceed the potential risk.

Dosing and Administration:

For 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 drug dose is skipped for about 24 hours, the drug should be used at the next scheduled time, without doubling the dose to compensate for the missed dose.

Side effects:

Adverse reactions to the drug were noted in 72 of the 3,843 patients (1.87%) who were reported as part of clinical trials or 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%), pain in the eye [transient] in 8 cases (0.21%), superficial point keratitis in 6 cases (0.16%), itching in 6 cases (0.16%), epithelial detachment of the cornea in 1 case (0.03%) and burning sensation [of the eyelid] in 1 case (0.03%).

Undesirable reactions are classified according to the following gradation frequency:

Very often> 1/10

Often from ≥1 / 100 to <1/10

Rarely from ≥1 / 10000 to <1/100

Very muchcaustic <1/10000

In each group, adverse events are classified as the severity is reduced and grouped according tofrequency of occurrence and system-organ class.

The table below describes the undesirable reactions.

	Frequency of occurrence	Unwanted reaction
Disturbances on the part of the organ of sight	Infrequently	Corneal erosion, conjunctivitis, blepharitis, irritation, pain in the eye, transient,
	Rarely	Separation of the epithelium of the cornea (), burning sensation [eyelids] ()
	Unknown	Corneal ulcer () (), corneal perforation () (**)
Hypersensitivity	Unknown	Contact dermatitis (*)

^(*)If adverse reactions occur, discontinue drug treatment.

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

^(***) A serious undesirable reaction, single reports from the experience of post-marketing use of the drug.

Overdose:

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

According to foreign reports, serious violations of the liver function (including lethal cases) were observed in patients who took the sodium bromfenac drug inside at a total dose exceeding 1500 mg for a long period of time more than 1 month.In this regard, if abnormalities are detected that are believed to be associated with early symptoms of liver failure, discontinue treatment with this medication and take appropriate measures.

Interaction:

There have been no studies of interaction with other drugs.

Special instructions:This drug should be used in symptomatic treatment, and not for the purpose of etiotropic therapy.

This drug should be used only as eye drops.

This drug should be instilled with caution, making sure that the tip of the bottle does not touch the surface of the eye.

This drug contains sodium sulfite, which can cause allergic reactions, including symptoms of anaphylaxis and life-threatening or less severe asthmatic episodes in susceptible patients.

All local NSAIDs can slow or delay healing like local glucocorticosteroids. Joint use of NSAIDs and local steroids may increase the chance of healing problems.

Cross-sensitivity

There is a possibility of cross-sensitivity to acetylsalicylic acid, derivatives of phenylacetyl acid and other NSAIDs. Therefore, caution should be exercised in the treatment of people who have previously been susceptible to these medicines and should carefully evaluate the potential risks and benefits.

Special patient groups

In susceptible patients, prolonged use of local NSAIDs, including bromfenac, Can lead to tearing of the epithelium, thinning of the cornea, corneal erosion, corneal ulceration or perforation of the cornea. These events can threaten the loss of vision. Patients with signs of destruction of the corneal epithelium should immediately stop using local NSAIDs and carefully monitor the health of the cornea. Therefore, patients at risk, the simultaneous use of ophthalmic corticosteroids with NSAIDs may lead to an increased risk of undesirable effects from the cornea.

Post-registration application experience

Post-registration experience of using local NSAIDs indicates that in patients with complications after ophthalmic surgical interventions,with denervation of the cornea, defects in the corneal epithelium, diabetes mellitus and superficial eye diseases, rheumatoid arthritis or repeated Ophthalmic surgical procedures performed for a short period of time may have an increased risk of undesirable corneal events, which can become a threatening loss of vision. Local NSAIDs in such patients should be used with caution.

It has been reported that ophthalmic NSAIDs can cause increased bleeding in the eye tissues (including hyphema) in combination with ophthalmic surgery. Local NSAIDs 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.

Eye infections

The use of the drug should be closely monitored and cautioned to prescribe it to patients with inflammations caused by infections, since the drug can mask the symptoms of eye infections.

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 clear instructions are given by the attending physician.

Excipients

Because the composition of the drug is benzalkonium chloride, careful monitoring of patients in the case of frequent or prolonged use of the drug is necessary. It is known that benzalkonium chloride can discolour soft contact lenses. Avoid contact with soft contact lenses.

It is reported that benzalkonium chloride may cause eye irritation, spot keratopathy and / or toxic ulcer 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.

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

After instillation, there may be a transient fogging of vision. In the case of fogging of vision after instillation, it is necessary to refrain from driving the car or working with mechanisms until the vision is clear.

Form release / dosage:Eye drops, 0.09%.

Packaging:

5 ml in a polyethylene bottle, sealed with a plastic stopper with a dropper with a screwed polypropylene lid. A label of a heat-shrinkable film with a printed seal is glued onto the vial.

1 bottle is placed in a cardboard box together with instructions for medical use.

Storage conditions:

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

Shelf life:

2 years. Do not use after the expiry date printed on the package. After the first opening the bottle should be stored for no more than 30 days.

Terms of leave from pharmacies:On prescription

Registration number:LP-004224

Date of registration:03.04.2017

Expiration Date:03.04.2022

The owner of the registration certificate:Senzu Pharmaceutical Co., Ltd.Senzu Pharmaceutical Co., Ltd. Japan

Manufacturer: & nbsp

Senju Pharmaceutical Co., Ltd Japan

Representation: & nbspIskra Industry Co., Ltd.Iskra Industry Co., Ltd.Japan

Information update date: & nbsp23.04.2017

Illustrated instructions

Instructions

NAKWAN® (Nakvan®)