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 when using these drugs alone is not enough.
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. It lowers 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 local administration, apparent 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, infants and children under 2 years old. It is contraindicated in patients treated with MAO inhibitors and antidepressants that affect noradrenergic conduction (eg tricyclic antidepressants and mianserin).
Precautions:
For children 2 years of age or older, especially those aged 2-7 years and (or) with a body weight below 20 kg, the drug should be used with caution and the patient's condition should be closely monitored due to the frequent pathological sleepiness. There were no clinical trials in adolescents (12 to 17 years of age). Brimonidine is not recommended for children under 12 years of age. Caution should be exercised in patients with severe, unstable and untreatable cardiovascular disease. If allergic reactions occur, brimonidine should be discontinued. Delayed eye hypersensitivity reactions have been reported with the use of brimonidine, some of which have been reported as associated with an increase in intraocular pressure. Bromonidine should be used with caution in patients with depression, cerebral and coronary circulation insufficiency, Raynaud's syndrome, orthostatic hypotension or thromboangiitis obliterans. Caution is advised when using brimonidin in patients with hepatic and / or renal failure (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 changes the color of soft contact lenses.
Pregnancy and lactation:
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 (congestion, burning and prickling, pruritus, foreign body sensation, conjunctival vesicles), blurred vision, allergic blepharitis, allergic blepharitis and conjunctivitis, allergic conjunctivitis, ocular allergic reactions, follicular conjunctivitis, dry mouth, fatigue. Common: dizziness, taste disturbances, local irritation (swelling and eyelid hyperemia, blepharitis with the presence of discharge in the conjunctival sac, eye pain, tearing), photophobia, damage and discoloration of the corneal epithelium, dry eyes, conjunctivitis, blurred vision, inflammation conjunctivitis, symptoms from the upper respiratory tract, gastrointestinal symptoms, weakness (asthenia). Uncommon: Arrhythmia (including bradycardia and tachycardia), dry nose, depression, generalized allergic reactions. Rarely: shortness of breath. Very rare: syncope, iritis, miosis, hypertension, hypotension, insomnia.Not known: Iritis and ciliary body (anterior uveitis), eyelid pruritus, skin reactions (including erythema, face edema, pruritus, rash, vasodilation). In neonates and infants, in whom brimonidin was used in congenital glaucoma therapy, symptoms of overdose have been observed, such as loss of consciousness, lethargy, drowsiness, hypotension, laxity, bradycardia, hypothermia, cyanosis, paleness, respiratory depression and apnea. In a three-month study of the third phase in children aged 2 to 7 years who were not fully controlled for glaucoma despite beta-blockers, brimonidine was reported to be accompanied by high incidence of somnolence (55%). In 8% of children, the severity of this symptom was significant, and in 13% of patients the treatment was discontinued. The incidence of drowsiness decreased 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 found more frequently in children with mc. <20 kg (63%) than patients with a > 20 kg (25%).
Dosage:
Adults (including elderly patients): 1 drop to the affected eye (eyes) 2 times a day, at intervals of about 12 hours. Immediately after instillation of the drug, it is recommended to compress the lacrimal sac in the area of the medial angle of the eye for 1 lacrimal). If you use more than one eye medicine, it is recommended that you keep at least 5-15 minutes between each administration.