Luxfen eye drops 0.2%, 5ml

• Open-angle glaucoma;

• ophthalmic hypertension (as monotherapy and in combination with other drugs that reduce intraocular pressure).

The drug is used topically. In the conjunctival sac of the affected eye, 1 drop is instilled 2 times / day with an interval between injections of 12 hours.

The duration of treatment is determined by the doctor.

In order to reduce the possible systemic absorption of the drug, it is recommended to squeeze the lacrimal sac at the inner corner of the eye (closing the lacrimal opening) for 1 min. This technique should be performed immediately after each drop is instilled.

If it is necessary to use two or more ophthalmic agents, different drugs should be instilled with an interval of 5-15 minutes.

The use of the drug in patients with impaired liver or kidney function has not been studied, and care must be taken when treating such patients.

In elderly patients, there were no differences in safety or efficacy compared with other adult patients. Cmax and T1 / 2 of brimonidine were similar in the elderly (65 years and older) and younger patients of the adult population, which demonstrates the absence of a significant effect of age on the systemic absorption and elimination of brimonidine. No dose adjustment is required when treating elderly patients.

Brimonidine is contraindicated in children under 2 years of age. In children aged 2 to 7 years, when using 0.2% brimonidine, drowsiness may occur, which may cause discontinuation of treatment. Careful monitoring of the patient's condition should be carried out, due to the high frequency of cases of drowsiness. The frequency of drowsiness may decrease with increasing age, but to a greater extent is determined by body weight: in children with a body weight of? 20 kg, drowsiness may be observed more often than in children with a body weight> 20 kg.

Eye drops in the form of a clear solution of greenish-yellow color.

1 ml brimonidine tartrate 2 mg

Excipients: benzalkonium chloride - 0.052 mg, polyvinyl alcohol - 14 mg, sodium chloride - 6.9 mg, sodium citrate dihydrate - 4.7 mg, citric acid monohydrate - 0.48 mg, 1M hydrochloric acid solution or 1M sodium hydroxide solution - up to pH 6.45, water purified - up to 1 ml.

• Hypersensitivity to brimonidine or to any of the excipients;

• simultaneous administration with MAO inhibitors and tricyclic or tetracyclic antidepressants (including mianserin);

• children under 2 years of age (the safety and efficacy of the drug for this age category have not been established);

• lactation period.

pharmachologic effect

Brimonidine is a selective agonist of ?2-adrenergic receptors. It has a dual mechanism of action: it lowers intraocular pressure by reducing the synthesis of intraocular fluid and increasing uveoscleral outflow.

With instillation of a 0.2% brimonidine solution, the decrease in intraocular pressure is 10-12 mm Hg. Art., the maximum effect is noted after 2 hours, the duration of action is 12 hours.

Pharmacokinetics

Absorption and distribution

With instillation of eye drops, Cmax of the drug in blood plasma is achieved after 0.5-2.5 hours. After using the drug 2 times / day for 10 days, the average value of Cmax in blood plasma remains low (on average 0.06 ng / ml). Binding to blood proteins when applied topically is 29%. Systemic absorption of brimonidine when applied topically is slowed down.

Brimonidine binds reversibly to melanin. The concentration of brimonidine in the iris, ciliary body and retina after 2 weeks of instillation into the eye was 3-17 times higher than these values ??after instillation of one dose of the drug.

Metabolism and distribution

The drug is metabolized mainly in the liver. Brimonidine and its metabolites are excreted by the kidneys. T1 / 2 after topical application averages 2 hours.

Side effect

From the side of the organ of vision: very often - conjunctival hyperemia, burning sensation, itching of the eyelids and mucous membranes of the eyes, foreign body sensation, impaired clarity of visual perception, allergic blepharitis, allergic blepharoconjunctivitis, allergic conjunctivitis, follicular conjunctivitis; often - hyperemia and edema of the eyelids, blepharitis, edema of the conjunctiva and mucous discharge from the eyes, hemorrhage into the conjunctiva, conjunctivitis, retention lacrimation, epiphora, eye pain and lacrimation, conjunctival folliculosis, local allergic reactions of the mucous membrane of the eyes (including ), cataract, keratitis, eyelid lesions, photosensitivity, superficial spotty keratopathy, loss of visual field, functional lesion of the vitreous body, vitreous hemorrhage,floating opacities in the vitreous and decreased visual acuity, photophobia, erosion and opacity of the cornea, dryness and irritation of the mucous membrane of the surface of the eye, blanching of the conjunctiva; infrequently - barley; very rarely - iritis, miosis.

From the nervous system: very often - headache, drowsiness; often - dizziness, violation of taste; infrequently - depression; very rarely - fainting, insomnia.

From the side of the cardiovascular system: infrequently - palpitations / arrhythmias (including bradycardia and tachycardia); very rarely - an increase or decrease in blood pressure.

From the respiratory system: often - bronchitis, pharyngitis, cough, shortness of breath; infrequently - dryness of the nasal mucosa; rarely - shortness of breath.

On the part of the digestive system: very often - dryness of the oral mucosa; often - gastrointestinal disorders (dyspepsia).

On the part of the skin and subcutaneous fat: often - a rash.

Infectious and parasitic diseases: often - flu-like syndrome, infectious disease (chills and respiratory infection), rhinitis, sinusitis, incl. infectious.

From the immune system: infrequently - systemic allergic reactions.

On the part of laboratory parameters: often - hypercholesterolemia.

Others: very often - fatigue; often asthenia.

In children, the following were noted: apnea, bradycardia, decreased blood pressure, hypothermia, muscle hypotension, pallor, drowsiness, decreased attention.

Post-registration use of brimonidine in the form of eye drops (2 mg / ml) revealed adverse reactions, the source of which were spontaneous messages with an unknown population size, therefore, it is not possible to indicate the frequency of their occurrence: on the part of the organ of vision - iridocyclitis (anterior uveitis); on the part of the skin and subcutaneous fat - allergic reactions from the skin, including erythema, facial edema, itching, rash and vasodilation of the eyelid skin vessels; from the digestive system - nausea.

Application during pregnancy and lactation

The safety of using the drug during pregnancy in humans has not been determined. In animal studies, topical application of brimonidine did not lead to impaired intrauterine development. The use of brimonidine during pregnancy is allowed only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

There is no exact data on the penetration of brimonidine into breast milk when applied topically. However, the risk cannot be completely ruled out. The use of the drug during breastfeeding is contraindicated.

Application for violations of liver function

With caution: in patients with hepatic impairment.

Application for impaired renal function

With caution: in patients with renal insufficiency (CC below 40 ml / min).

Application in children

The use of the drug in children under 2 years of age is contraindicated.

The drug should be used with caution in children and adolescents from 2 to 18 years of age.

Use in elderly patients

No dose adjustment is required when treating elderly patients.

special instructions

The drug should be used with caution in patients with renal impairment (CC below 40 ml / min) and hepatic impairment.

In patients with orthostatic hypotension, heart failure and cerebrovascular accident, depression, Raynaud's syndrome, thromboangiitis obliterans, the drug may increase the severity of the course of diseases caused by vascular insufficiency.

The drug should be used with caution in patients simultaneously receiving therapy with antihypertensive drugs and (or) cardiac glycosides.

Avoid getting the drug on soft contact lenses, since discoloration of the latter is possible. Remove contact lenses before using the drug. The time interval between using the drug and reinstalling contact lenses should be at least 15 minutes.

With the development of allergic reactions to the drug, the patient must stop treatment and consult a doctor.

An increase in intraocular pressure is possible in the event of delayed hypersensitivity reactions.

The preservative contained in the preparation (benzalkonium chloride) may irritate the eyes.

Use in pediatrics

The drug should be used with caution in children aged 2 to 18 years (safety and efficacy have not been established).

During the treatment period, careful monitoring of the condition of patients aged 2 to 7 years (especially with a body weight of up to 20 kg) is required due to the high frequency and severity of drowsiness.

The use of the drug in children under 12 years of age is not recommended.

Influence on the ability to drive vehicles and use mechanisms

The drug can cause a state of fatigue or drowsiness, a decrease in vision clarity, therefore, during the period of drug treatment, one should refrain from driving vehicles and servicing moving mechanisms.

Overdose

Overdose when applied topically

Overdose symptoms with topical application of the drug are represented by previously noted adverse reactions.

Overdose in case of accidental ingestion of the drug inside (adult patients)

There are few reports of overdose in adults.

The following symptoms are possible: depression of the central nervous system, drowsiness, depression and loss of consciousness, hypotension, bradycardia, decreased body temperature, cyanosis of the skin, apnea, asthenia, vomiting, convulsions, arrhythmia, miosis.

Treatment: supportive and symptomatic therapy; it is necessary to maintain patency of the airway.

Overdose in children

An overdose of brimonidine (as adjunctive therapy for congenital glaucoma or accidental ingestion) has been observed in young children (2-7 years).

Symptoms: loss of consciousness, lethargy, drowsiness, hypotension, hypotension, bradycardia, hypothermia, cyanosis, pallor, respiratory depression and apnea.

Treatment: carrying out supportive and symptomatic therapy, control of airway patency, intensive therapy with intubation may be necessary.

Drug interactions

Studies to study the interaction of the drug with other drugs have not been conducted.

Brimonidine is contraindicated in patients taking MAO inhibitors and in patients taking tricyclic or tetracyclic antidepressants (including mianserin).

Brimonidine at a concentration of 2 mg / ml can enhance the effect of substances that affect the central nervous system (ethanol, barbiturates, opioids, sedatives or anesthetics).

Caution should be exercised when used simultaneously with drugs that can affect the absorption and metabolism of adrenaline, norepinephrine and other so-called biogenic amines (chlorpromazine, methylphenidate, reserpine).

In some patients, after using a solution of brimonidine at a concentration of 2 mg / ml, there is a slight decrease in blood pressure. Caution should be exercised when used simultaneously with antihypertensive drugs and / or cardiac glycosides.

With the simultaneous systemic administration of agonists or antagonists of adrenergic receptors (for example, isoprenaline or prazosin) for the first time, as well as when the dose of these simultaneously administered systemic drugs (regardless of the method of administration) is changed, interactions with ?-adrenergic receptor agonists or an effect on their effects may occur. ...