Universal reference book for medicines
Product name: AZOPT в„ў (AZOPTВ®)

Active substance: brinzolamide

Type: Anti-glaucoma preparation is a local inhibitor of carbonic anhydrase

Manufacturer: ALCON LABORATORIES (USA)
Composition, form of production and packaging
Eye suspension 1%
1 ml

Brenzolamide 10 mg

Auxiliary substances: 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).

5 ml - a bottle of dropper plastic "Drop Tainer" (1) with a dispenser - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the print edition of 2007.

PHARMACHOLOGIC EFFECT

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.
PHARMACOKINETICS

Suction

With topical application, brenzolamide is absorbed into the systemic circulation.

Distribution

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 (<10 ng / ml).

Excretion

T 1/2 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).
INDICATIONS

To reduce increased intraocular pressure with:

- open-angle glaucoma;

ocular hypertension.

DOSING MODE

The drug 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.

SIDE EFFECT

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, itching of the eyes; <1% - conjunctivitis, keratoconjunctivitis, keratopathy, initial symptoms of blepharitis (clumping of eyelids or crusts on the edges of the eyelids), lacrimation, diplopia, asthenopia.
On the part of the digestive system: 5-10% - bitter, sour or unusual taste in the mouth;
<1% - dry mouth, dyspepsia, nausea, diarrhea.
On the part of the respiratory system: 1-5% - rhinitis;
<1% - shortness of breath, pharyngitis.
From the cardiovascular system: <1% - chest pain, hypertension.

From the side of the urinary system: <1% - pain in the kidneys.

Allergic reactions: <1% - urticaria.

Other: 1-5% - headache, dermatitis;
<1% - alopecia, dizziness.
CONTRAINDICATIONS

- Hypersensitivity to the components of the drug.

PREGNANCY AND LACTATION

Adequate and strictly controlled clinical trials of safety of use of Asopt in pregnant women have not been conducted.
Therefore, the use of Asopt during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
It is not known whether brinzolamide is excreted in breast milk.
Therefore, if you need to appoint Azopt in the lactation period, you should decide whether to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

Because Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe renal dysfunction (CK <30 mL / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should appoint Asopt with severe violations of the liver.

APPLICATION FOR CHILDREN

The effectiveness and safety of the drug Asopt in children is not established.

SPECIAL INSTRUCTIONS

With caution should appoint Asopt with severe violations of the liver.

Because Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe renal dysfunction (CK <30 mL / min).

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 drug is administered repeatedly with violations of the guidelines for its use. With the development of serious adverse reactions, the drug 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 drug.

When using several drugs, the interval between instillations should be at least 15 minutes.

Do not touch the eye with the tip of the dropper.

Use in Pediatrics

The effectiveness and safety of the drug 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.
OVERDOSE

Data on overdose with topical application of Azopta is not available.

In case of an overdose caused by accidental ingestion of the drug inside, the following symptoms may occur : violation of electrolyte balance, acidosis, disorders of the nervous system.

Treatment: if necessary, conduct symptomatic therapy;
it is also necessary to monitor the pH of the blood, the level of electrolytes (especially potassium).
DRUG INTERACTION

With the simultaneous use of Azopt and inhibitors of carbonic anhydrase for systemic use, it is possible to strengthen systemic reactions associated with inhibition of the enzyme.
Therefore, it is not recommended to assign such a combination.
With simultaneous use of Azopt and salicylates in high doses, acid-base and electrolyte balance can be violated.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored at a temperature of 4 В° to 30 В° C in places inaccessible to children.
Shelf life - 2 years.
After opening the vial, the drug should be used within 4 weeks.


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