Reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension: monotherapy in patients who are contraindicated in the topical use of beta-blockers; in combination with other drugs that lower the intraocular pressure, if the reduction in pressure with these drugs is insufficient.
Composition:
1 ml of solution contains 2 mg of brimonidine tartrate (equivalent to 1.3 mg of brimonidine); drops contain benzalkonium chloride.
Action:
A selective α receptor agonist2-adrenergic for topical use. It lowers intraocular pressure by reducing the production of aqueous humor and increasing its leakage by the scleral-scleral route. Affinity of brimonidin for α receptors1-adrenergic is 1000 times smaller compared to affinity for α receptors2thanks to which it does not dilate the pupils and does not cause capillary contraction after human retinal xenografts. In addition, it minimally affects the functioning of the cardiovascular and respiratory system. The drug is characterized by a rapid onset of action, and the maximum antihypertensive effect occurs 2 hours after administration. After topical administration of 0.2% solution twice daily for 10 days, the blood concentration is low. After local administration, apparent T0,5 in the general circulation is about 3 hours. Brimonidine binds reversibly to the melanin of the eye tissues, with no side effects. In the absence of melanin, no accumulation occurs.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Newborns, infants and children <2 years. Concomitant use of MAO inhibitors or antidepressants that affect noradrenergic prescription (eg tricyclic antidepressants and mianserin).
Precautions:
Brimonidine is not recommended for use in children aged 2-12. If brimonidine is required for children ≥ 2 years, especially those aged 2 to 7 years and / or those weighing ≤20 kg, care should be taken and patients should be closely monitored for frequent pathological this age group. Exercise caution in patients with severe or unstable and uncontrolled cardiovascular disease, depression, cerebral or coronary circulation disorders, Raynaud's syndrome, orthostatic hypotension, thromboangiitis obliterans, and in patients with impaired liver or kidney function. The preparation should be discontinued if hypersensitivity reactions occur. Drops contain benzalkonium chloride, which may cause eye irritation. Benzalkonium chloride discolor soft contact lenses - before using the medicine, contact lenses should be removed and replaced again after at least 15 minutes.
Pregnancy and lactation:
It can only be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus. Do not use when breastfeeding.
Side effects:
Very common: headache, drowsiness, irritation of the eye (hyperemia, burning, pruritus, pruritus, feeling of the presence of a foreign body, conjunctival vesicles), blurred vision, 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, corneal epithelium damage and discoloration, dry eye, conjunctivitis, visual disturbances, inflammation conjunctivitis, symptoms from the upper respiratory tract, gastrointestinal symptoms, asthenia. Uncommon: cardiac arrhythmias (including bradycardia and tachycardia), dry nasal mucous membrane, generalized allergic reactions, depression. Rarely: shortness of breath. Very rare: fainting, iritis, miosis, hypertension, hypotension, insomnia.In children aged 2-7 years, a large (55%) incidence of pathological somnolence was observed when administering brimonidine as a booster; the incidence of somnolence decreased with the increase in the age of treated children and with the increase of the child's body weight. Symptoms of brimonidine overdose (loss of consciousness, lethargy, drowsiness, hypotension, hypotonia, bradycardia, drop in body temperature, cyanosis, paleness, respiratory depression and apnea) have been observed in newborns and infants, therefore the medicine is contraindicated in this age group.
Dosage:
Adults (also elderly patients): 1 drop into the conjunctival sac of the affected eye (eyes) 2 times a day, every 12 hours. It is recommended after instillation of each drop to punctuate the tear sac at the medial angle of the eye (compression of the tear point) for approx. . 1 minute to reduce potential systemic absorption. When using several topical ophthalmic medications, a minimum of 5-15 minutes should be allowed between the instillation of subsequent medications.
(C)
