Description
Latin name
AZOPT
Release form
Azopt eye drops. Eye drops.
Packaging
In a dropper bottle 5 ml of suspension. In a cardboard box 1 bottle.
Pharmacological action
Antiglaucoma is a local carbonic anhydrase inhibitor. Carbonic anhydrase is an enzyme that is present in many body tissues, including the eye tissue. Catalyzes reversible reactions in which hydration of carbon dioxide and hydrolysis of carbonic acid occur. In humans, carbonic anhydrase is present in the form of a series of isoenzymes, the most active of them is carbonic anhydrase II (KA-II), which is found primarily in red blood cells and other tissues. Inhibition of carbonic anhydrase II in the ciliary body of the eye reduces the production of intraocular fluid due to a slowdown in the formation of bicarbonate ions, followed by a decrease in sodium and fluid transport. As a result, there is a decrease in intraocular pressure.
Pharmacokinetics
Absorption
When applied topically, brinzolamide is absorbed into the systemic circulation.
Distribution of
Plasma Protein Binding is 60%.
Metabolism
Brinzolamide is absorbed in red blood cells through selective binding to carbonic anhydrase II.
Metabolized with the formation of N-deethylbrinzolamide, which binds to carbonic anhydrase (mainly carbonic anhydrase-I) and also accumulates in red blood cells.
Since brinzolamide and its metabolite accumulate in red blood cells, their plasma concentration is below the limit of quantification (
Excretion of
T1 / 2 is 111 days. Brinzolamide is excreted unchanged in the urine and in the form of metabolites – the main one (small N-desethylbrinzolamide) concentrations of other metabolites (N-desmethoxypropyl and O-desmethyl)
Indications
Decreased increased intraocular pressure with: Open-angle glaucoma,
Ocular hypertension.
Contraindications
Hypersensitivity to the components of the drug.
Pregnancy and lactation
There have been no adequate and strictly controlled clinical trials of the safety of Azopt in pregnant women. Therefore, the use of the drug Azopt during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
It is not known whether brinzolamide with breast milk is excreted. Therefore, if necessary, the appointment of Azopt during lactation should decide on the termination of breastfeeding.
Composition
Ophthalmic suspension 1% 1 ml
brinzolamide 10 mg
Excipients: mannitol, carbomer 974P, tyloxapol, disodium edetate, sodium chloride, hydrochloric acid and / or sodium hydroxide solution (to maintain the pH level), purified water, benzalkonium chloride 0.01% (as a preservative).
Dosage and administration
The drug is instilled 1 drop in the conjunctival sac of the affected eye (or eyes) 2 times / day.
Shake the vial before using the drug.
Side effects
From the side of the organ of vision: 5-10% – blurred vision 1-5% – blepharitis, keratitis, dry eyes, hyperemia, foreign body sensation in the eye, discharge from the eyes, discomfort, pain, pruritus
From the side digestive system: 5-10% – bitter, sour or unusual taste in the mouth
From the respiratory system: 1-5% – rhinitis
From the cardiovascular system:
From the urinary system:
Allergic reactions:
Other: 1 -5% – headache, dermatitis
Drug Interaction
With the simultaneous use of Azopt and carbonic anhydrase inhibitors for systemic administration, systemic reactions associated with enzyme inhibition may be enhanced. Therefore, it is not recommended to assign such a combination.
Salicylates in high doses
With the simultaneous use of Azopt and salicylates in high doses disturbances of acid-base and electrolyte balance are possible.
Overdose
There is no data on overdose with topical Azopt.
Symptoms: an overdose caused by the accidental ingestion of the drug may occur: electrolyte balance disturbance, acidosis, nervous system disorders.
Treatment: if necessary, conduct symptomatic therapy. It is also necessary to control the pH of the blood, the level of electrolytes (especially potassium).
Storage conditions
The drug should be stored at a temperature of 4 ° to 30 ° C. After opening the bottle, the drug should be used within 4 weeks.
Expiration
2 Year
Deystvuyuschee substances
Brynzolamyd
Pharmacy leave conditions
Prescription
Dosage Form A dosage form of eye drops
Alcon, USA
