Reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Monotherapy in patients whose topical use of β-blockers is contraindicated. In combination with other drugs that lower the intraocular pressure, if the reduction in pressure with these medicines is insufficient.
Composition:
1 ml of solution contains 2 mg of brimonidine tartrate (equivalent to 1.3 mg of brimonidine). The preparation contains benzalkonium chloride.
Action:
A selective α receptor agonist2-adrenergic for topical use. Decreases intraocular pressure by reducing aqueous humor production and increasing choroidal scleral outflow. Affinity of the drug for α receptors1-adrenergic is 1000 times smaller compared to affinity for α receptors2, thanks to which the drug does not dilate pupils or shrinkage capillaries after human retinal xenografts. The product reduces intraocular pressure, minimally affecting the activity of the cardiovascular and respiratory system. The drug shows a rapid onset of action, and the maximum antihypertensive effect occurs 2 hours after administration. The degree of binding to plasma proteins is approximately 29%. After topical administration T0,5 in the systemic circulation it is about 3 hours. Brimonidine binds reversibly to the melanin of eye tissues without adverse effects. In the absence of melanin, there is no accumulation of the drug.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Newborns and infants. Concomitant treatment with MAO inhibitors or antidepressants that affect noradrenergic conduction (eg tricyclic antidepressants, mianserin).
Precautions:
In children aged 2 years or older, especially those aged 2-7 years and (or) with below 20 kg, the preparation should be used with caution and the patient's condition should be closely monitored due to the frequently observed pathological drowsiness. Caution should be exercised in patients with severe or unstable and uncontrolled cardiovascular disease. If allergic reactions occur, brimonidine should be discontinued. Bromonidine should be used with caution in patients with depression, cerebral or coronary circulation insufficiency, Raynaud's syndrome, orthostatic hypotension or thromboangiitis obliterans. Caution should be exercised when using brimonidin in patients with hepatic or renal impairment (no study). The benzalkonium chloride contained in the preparation may cause eye irritation. Avoid contact of the preparation with soft contact lenses. Remove contact lenses prior to instillation and wait at least 15 minutes before re-insertion. The substance may cause discoloration of soft contact lenses.
Pregnancy and lactation:
The safety of the preparation in pregnant women has not been established. The preparation can be used during pregnancy only if the benefit for the mother outweighs the potential risk to the fetus. Do not use during breast-feeding.
Side effects:
Very common: headache, drowsiness, eye irritation (including hypersensitivity reactions such as hyperemia, burning, pricking, pruritus, foreign body sensation, conjunctival papules), blurred vision, dry mouth, tiredness. Common: dizziness, taste disturbances, local irritation (swelling and congestion of the eyelids, blepharitis, conjunctival edema, presence of secretion in the conjunctival sac, eye pain, tearing), photophobia, damage and discoloration of the corneal epithelium, dry eyes, conjunctivitis, dysfunction vision, conjunctivitis, upper respiratory tract symptoms, gastrointestinal symptoms, weakness. Uncommon: palpitations / arrhythmias (including bradycardia and tachycardia), dryness of the nasal mucous membrane, depression, generalized allergic reactions. Rarely: shortness of breath. Very rare: syncope, iritis (anterior uveitis), miosis, hypertension, hypotension, insomnia.In newborns and infants whose part of congenital glaucoma therapy was the use of brimonidine, symptoms of overdose have been observed, such as loss of consciousness, drop in blood pressure, flaccidity, bradycardia, hypothermia, cyanosis and apnea. In a 3-month study of the third phase in children 2-7 years of age, in whom despite the administration of β-blockers, glaucoma control was not complete, brimonidine was found to be accompanied by a high incidence of somnolence (55%). In 8% of these patients, the severity of this symptom was significant, and in 13% of patients the treatment was discontinued. The incidence of somnolence diminished with age, the smallest was in the group of seven-year-olds (25%). However, body weight had a greater impact on its occurrence than age. This symptom was more common in patients with body weight <20 kg (63%) than in patients> 20 kg (25%).
Dosage:
Adults (including the elderly): 1 drop to the affected eye (eyes) 2 times a day, at intervals of about 12 hours. To reduce the possibility of absorption of brimonidine into the systemic circulation, immediately after instillation of the drug, it is recommended to compress the bag for one minute tear at the medial angle of the eye (compression of the tear point). The flow chart should be executed immediately with the administration of each drop. If you use more than one ophthalmic topical ophthalmologist, it is recommended that you keep at least a 5-15 min interval between administrations. There are no studies on the use of brimonidine in patients with impaired liver or kidney function. Clinical trials with adolescents (aged 12 to 17 years) have not been conducted. Brimonidine is not recommended for use in children below the age of 12. Use is contraindicated in newborns and infants (below the age of 2). The efficacy and safety of brimonidine in children has not been established.