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Active ingredients
Brimonidine
Release form
Drops
Composition
Brimonidine tartrate 2 mg Auxiliary substances: 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, hydrochloric acid - to pH 6.45, sodium hydroxide - to pH 6.45, water - up to 1 ml.
Pharmacological effect
Antiglaucoma drug. Brimonidine is a selective α2-adrenoreceptor agonist. When instilating a 0.2% solution of brimonidine, the reduction in intraocular pressure is 10-12 mmHg. Art., the maximum effect is noted after 2 hours, the duration of action is 12 hours. Brimonidine has a double mechanism of action: lowers intraocular pressure by reducing the synthesis of intraocular fluid and enhancing uveoscleral outflow.
Pharmacokinetics
Absorption and distribution When instillation of the eye drops of the drug Cmax in the blood plasma is achieved in 0.5-2.5 hours. The binding to blood proteins when applied topically is 29%. Systemic absorption of brimonidine slowed down. After using the drug 2 times / day for 10 days, plasma concentration of brimonidine remains low (on average, 0.06 ng / ml). Metabolism and distribution The drug is metabolized mainly in the liver. Brimonidine and its metabolites are excreted by the kidneys. T1 / 2 is about 2 hours.
Indications
Open-angle glaucoma, ophthalmic hypertension (as monotherapy and in combination with other drugs that reduce intraocular pressure).
Contraindications
Simultaneous therapy with MAO inhibitors and tricyclic antidepressants; children's age up to 2 years; lactation period (breastfeeding); hypersensitivity to the drug components. With caution, the drug should be prescribed to patients with severe, unstable and uncontrolled cardiovascular diseases, with cerebral or coronary insufficiency , depression, orthostatic hypotension, Raynaud's disease, thromboangiitis obliterans, with impaired liver or kidney function, as well as in children and adolescents Cove age from 2 to 18 years.
Precautionary measures
Use for violations of liver functionWith caution should be prescribed the drug for violations of the liver.Application for violations of renal functionWith caution should be prescribed the drug for violations of the kidneys.Application in childrenThe drug is contraindicated in children under 2 years of age.With caution, use the drug in children and adolescents from 2 to 18 years.
Use during pregnancy and lactation
Studies on the safety and efficacy of brimonidine in pregnant and lactating women have not been conducted. In experimental animal studies, local application of brimonidine did not lead to disruption of fetal development. There is no accurate data on the allocation of brimonidine with breast milk when applied topically. However, the risk cannot be completely eliminated. Use of the drug during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus. If you need to use the drug during lactation, breastfeeding should be stopped for the duration of treatment.
Dosage and administration
Locally. Instill 1 drop of the drug 2 times / day. The duration of treatment is determined by the doctor.
Side effects
The frequency of side effects is classified as follows: very often (> 1/10), often (from> 1/100 to less than 1/10), sometimes (from> 1/1000 to less than 1/100), rarely (from> 1 / 10 000 to less than 1/1000), very rarely (less than 1/10 000), the frequency is unknown. On the part of the organ of vision: very often - conjunctival hyperemia, itching of the eyelids and eye mucosa; often - burning sensation; conjunctiva follicle and follicular disease bodies in the eyes, keratitis, eyelids, photosensitivity, superficial spotted keratopathy, lacrimation, loss of visual fields, functional damage to the vitreous body, violence in the vitreous, floating opacities in the vitreous and reduced visual acuity; infrequently - erosion of the cornea, barley. On the side of the CNS: often - headache, drowsiness, insomnia, dizziness. On the part of the cardiovascular system: often - increase in blood pressure; infrequently - decrease in blood pressure. From the side of the respiratory system: often - bronchitis, cough, shortness of breath; infrequently - dry nasal mucosa, apnea. From the digestive system: often - gastrointestinal disorders (dyspepsia), dryness of the oral mucosa. From the skin and subcutaneous fat: often - rashes. Infectious and parasitic diseases: often - flu-like syndrome, infectious disease (chills and respiratory infection), rhinitis, sinusitis, incl.infectious. For laboratory parameters: often - hypercholesterolemia. Allergic reactions: very often - allergic conjunctivitis; often - local allergic reactions of the mucous membrane of the eyes (including keratoconjunctivitis), general allergic reactions. Others: often - asthenia, fatigue; Infrequently - changing taste sensations. In children: apnea, bradycardia, lowering blood pressure, hypothermia, muscle hypotonia. In addition, data on the following effects are obtained. On the part of the organ of vision: the frequency is unknown - iritis, miosis. On the side of the CNS: depression. cardiovascular system: bradycardia, tachycardia. From the digestive system: nausea. From the skin and subcutaneous fat: local skin reactions (erythema, itching, swelling of the face, rash and vasodilation of the eyelid skin vessels).
Overdose
Overdosing is extremely rare. When accidentally taking the drug inside, the following symptoms are possible: CNS depression, drowsiness, depression and loss of consciousness, decreased blood pressure, bradycardia, decrease in body temperature, skin cyanosis, apnea. Treatment: maintenance symptomatic therapy, control of airway patency .
Interaction with other drugs
Brimonidine at a concentration of 2 mg / ml may enhance the effect of substances affecting the central nervous system (ethanol, barbiturates, opioids, sedatives and anesthetics). Care should be taken with simultaneous use with drugs that can affect the absorption and metabolism of adrenaline, noradrenaline and others, so called biogenic amines (chlorpromazine, methylphenidate, reserpine). In some patients, after applying the brimonidine solution 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 (digitalis preparations). With simultaneous systemic administration of adrenoceptor agonists or antagonists (eg, isoprenaline or prazosin) for the first time, as well as changing the dose of these simultaneously administered systemic drugs ( on the mode of their administration), there may be interaction with α-adrenoreceptor agonists or effects on their effects.
special instructions
Remove contact lenses before use. The time interval between the use of the drug and the re-installation of contact lenses should be at least 15 minutes. Impact on the ability to drive vehicles and control machinery moving mechanisms.