Azopt eye drops - is a preparation based on brenzolamide, intended to reduce intraocular pressure in open-angle glaucoma and ocular hypertension. The effect is achieved as a result of reduced production of intraocular fluid.
The antiglaucoma preparation is a local inhibitor of carbonic anhydrase. Carboangainase is an enzyme present in many tissues of the body, including the tissues of the eye. Catalyzes reversible reactions in which hydration of carbon dioxide and hydrolysis of carbonic acid occurs. In humans, carbonic anhydrase is present as a series of isoenzymes, the most active of them is carbonic anhydrase II (KA-II), found primarily in erythrocytes and other tissues. Inhibition of carbonic anhydrase II in the ciliary body of the eye reduces the production of intraocular fluid due to the slowing of the formation of bicarbonate ions, followed by a decrease in the transport of sodium and liquid. As a result, the intraocular pressure decreases.
Suction
With topical application, brenzolamide is absorbed into the systemic circulation.
The binding to plasma proteins is 60%.
Metabolism
Brinzolamide is absorbed in erythrocytes by selective binding to carbonic anhydrase II.
Metabolized with the formation of N-desethylbenzenamide, which binds to carbonic anhydrase (mainly with carbonic anhydrase-I) and also accumulates in erythrocytes.
Since Brinzolamide and its metabolite accumulate in erythrocytes, their concentration in the blood plasma is below the limit of quantitative determination (
Excretion
T1 / 2 is 111 days. Brinzolamide is excreted in urine in unchanged form and in the form of metabolites - the main (N-desethylbenzenamide) and small concentrations of other metabolites (N-demethoxypropyl and O-desmethyl).
Reduction of increased intraocular pressure with:
Hypersensitivity to the components of the preparation.
With caution should appoint Asopt with severe violations of the liver.
Since Azopt and its metabolites are excreted in the urine, the preparation is not recommended for patients with severe renal dysfunction (QC
It should be borne in mind that Brinzolamide is sulfonamide. Since with topical application, its systemic absorption occurs, it is possible the development of adverse reactions, including. severe allergic reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatonecrosis, agranulocytosis, aplastic anemia). Sensitization of the body with sulfonamides can develop if the preparation is administered repeatedly with violations of the instructions for its use. With the development of serious adverse reactions, the preparation should be discontinued.
It should be borne in mind that the benzoaconium chloride included in the preparation of Asopt can accumulate in contact lenses, therefore, the lenses should be removed before instillation and placed back no earlier than 15 minutes after application of the preparation.
When using several preparations, the interval between instillations should be at least 15 minutes.
Do not touch the eye with the tip of the dropper.
The effectiveness and safety of the preparation Asopt in children is not established.
Impact on the ability to drive vehicles and manage mechanisms
Immediately after applying Azopta, blurred vision may temporarily occur. Therefore, the patient should be careful when driving vehicles and when working with machinery.
In case of violations of kidney function
Since Azopt and its metabolites are excreted in the urine, the preparation is not recommended for patients with severe renal dysfunction (QC
With violations of liver function
With caution should appoint Asopt with severe violations of the liver.
Application in childhood
The effectiveness and safety of the preparation Asopt in children is not established.
The preparation is instilled in 1 drop in the conjunctival sac of the affected eye (or eyes) 2 times / day.
Before using the preparation, the vial should be shaken.
Important notice- the outer box design may vary before prior notice!
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