Luxfen^® (Drops) Instructions for Use

Marketing Authorization Holder

Bausch Health, LLC (Russia)

Manufactured By

Pharma Stulln, GmbH (Germany)

ATC Code

S01EA05 (Brimonidine)

Active Substance

Brimonidine (Rec.INN registered by WHO)

Dosage Form

Luxfen®

Eye drops 0.2%: 5 ml bottle with dropper attachment

Dosage Form, Packaging, and Composition

Eye drops in the form of a transparent, slightly greenish-yellow solution.

Excipients: benzalkonium chloride, polyvinyl alcohol, sodium chloride, sodium citrate, citric acid monohydrate, 1M hydrochloric acid solution, 1M sodium hydroxide solution, water for injections.

5 ml – polyethylene bottles (1) with a dropper attachment – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug

Pharmacotherapeutic Group

Antiglaucoma agent – selective alpha₂-adrenergic agonist

Pharmacological Action

A selective α₂-adrenergic receptor agonist for topical use in ophthalmology. It has a dual mechanism of action: it lowers intraocular pressure by reducing the production of intraocular fluid and enhancing uveoscleral outflow.

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

Pharmacokinetics

When instilled in the form of eye drops, the C_max of brimonidine in plasma is reached within 0.5-2.5 hours. After twice-daily application for 10 days, the mean C_max in blood plasma remains low (on average 0.06 ng/ml). Protein binding with blood proteins upon topical application is 29%. Systemic absorption of brimonidine upon topical application is slowed. Brimonidine reversibly binds to melanin.

Concentrations of brimonidine in the iris, ciliary body, and retina after 2 weeks of eye instillation were 3-17 times higher than these indicators after a single dose instillation. It is metabolized mainly in the liver. Brimonidine and its metabolites are excreted by the kidneys. The T_1/2 after topical application averages 2 hours.

Indications

Open-angle glaucoma; ocular hypertension (as monotherapy and in combination with other intraocular pressure-lowering drugs).

ICD codes

Dosage Regimen

Instill one drop into the conjunctival sac of the affected eye(s) twice daily.

Maintain an approximate 12-hour interval between administrations.

If using other topical ophthalmic agents, administer them at least 5 minutes apart.

To minimize systemic absorption, apply gentle pressure to the lacrimal sac at the inner corner of the eye for one to two minutes after instillation.

Do not allow the dropper tip to contact the eye, eyelids, or any other surface.

Close the bottle tightly immediately after use.

The duration of therapy is determined by the physician based on intraocular pressure response.

Adverse Reactions

Eye disorders very common – conjunctival hyperemia, burning sensation, itching of the eyelid skin and ocular mucosa, foreign body sensation, blurred vision, allergic blepharitis, allergic blepharoconjunctivitis, allergic conjunctivitis, follicular conjunctivitis; common – hyperemia and swelling of the eyelids, blepharitis, conjunctival edema and mucous discharge from the eyes, conjunctival hemorrhage, conjunctivitis, lacrimation retention, epiphora, eye pain and lacrimation, conjunctival folliculosis, local allergic reactions of the ocular mucosa (including keratoconjunctivitis), cataract, keratitis, eyelid lesions, photosensitivity, superficial punctate keratopathy, visual field loss, vitreous body functional impairment, vitreous hemorrhage, vitreous floaters and decreased visual acuity, photophobia, corneal erosion and opacity, dryness and irritation of the ocular mucosal surface, conjunctival blanching; uncommon – stye; very rare – iritis, miosis.

Nervous system disorders very common – headache, drowsiness; common – dizziness, taste perversion; uncommon – depression; very rare – syncope, insomnia.

Cardiovascular system disorders uncommon – palpitations/arrhythmias (including bradycardia and tachycardia); very rare – increase or decrease in blood pressure.

Respiratory system disorders common – bronchitis, pharyngitis, cough, dyspnea; uncommon – dryness of the nasal mucosa; rare – dyspnea.

Gastrointestinal system disorders very common – dryness of the oral mucosa; common – gastrointestinal disorders, dyspepsia.

Skin and subcutaneous tissue disorders common – rash.

Infectious and parasitic diseases common – flu-like syndrome, infectious disease (chills and respiratory infection), rhinitis, sinusitis, including infectious.

Immune system disorders uncommon – systemic allergic reactions.

Investigations common – hypercholesterolemia.

General disorders very common – fatigue; common – asthenia.

In children: apnea, bradycardia, decreased blood pressure, hypothermia, muscle hypotonia, pallor, drowsiness, attention decrease.

Contraindications

Concomitant use with MAO inhibitors and tricyclic or tetracyclic antidepressants; children under 2 years of age (safety and efficacy of the drug for this age category have not been established); lactation period (breastfeeding); hypersensitivity to brimonidine.

Use in Pregnancy and Lactation

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

There are no precise data on the penetration of brimonidine into breast milk upon topical application. However, the risk cannot be completely excluded. Use during breastfeeding is contraindicated.

Pediatric Use

Brimonidine is contraindicated in children under 2 years of age. Use with caution in children aged 2 to 7 years.

Geriatric Use

The drug is approved for use in elderly patients.

Special Precautions

Use with caution in patients with renal failure (creatinine clearance below 40 ml/min) and hepatic failure; in patients with orthostatic hypotension, heart failure and cerebrovascular insufficiency, depression, Raynaud’s syndrome, thromboangiitis obliterans; in patients concurrently receiving antihypertensive drugs and/or cardiac glycosides; in children and adolescents from 2 to 18 years of age (safety and efficacy of use have not been established).

In elderly patients, no differences in safety or efficacy were noted compared to other adult patients. The C_max and T_1/2 of brimonidine were similar in elderly (65 years and older) and younger adult population patients, demonstrating no significant effect of age on the systemic absorption and elimination of brimonidine. Dose adjustment when treating elderly patients is not required.

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

If allergic reactions develop, it is necessary to discontinue use. An increase in intraocular pressure is possible in case of delayed hypersensitivity reactions.

Use in pediatrics

Brimonidine is contraindicated in children under 2 years of age. In children aged 2 to 7 years, the use of 0.2% brimonidine may cause drowsiness, which may be a reason for treatment discontinuation. Careful monitoring of the patient’s condition should be carried out due to the high frequency of drowsiness cases. The frequency of drowsiness may decrease with increasing age, but is largely determined by body weight: in children with a body weight ≤20 kg, drowsiness may be noted more often compared to children with a body weight >20 kg.

Effect on ability to drive vehicles and operate machinery

Brimonidine may cause fatigue or drowsiness, blurred vision, therefore, during treatment with the drug, one should refrain from driving vehicles and operating moving machinery.

Drug Interactions

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 may enhance the effect of substances affecting the CNS (ethanol, barbiturates, opioids, sedatives, or anesthetics).

Caution should be exercised when used concomitantly with drugs capable of affecting the absorption and metabolism of adrenaline, noradrenaline, and other so-called biogenic amines (chlorpromazine, methylphenidate, reserpine).

Some patients may experience a slight decrease in blood pressure after using a 2 mg/ml brimonidine solution. Caution should be exercised when used concomitantly with antihypertensive drugs and/or cardiac glycosides.

When systemic adrenergic receptor agonists or antagonists (e.g., isoprenaline or prazosin) are administered concomitantly for the first time, as well as when the dose of these concomitantly administered systemic drugs is changed (regardless of their route of administration), interaction with α-adrenergic receptor agonists or an effect on their actions may occur.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.