Azopt eye drops 1%, 5 ml

Decrease in increased IOP in diseases such as:

• open-angle glaucoma;

• ocular hypertension.

Shake the bottle topically before use.

1 drop into the conjunctival sac 2 times a day.

Eye drops in the form of a homogeneous suspension of white or almost white color.

1 ml

brinzolamide 10 mg

Excipients: benzalkonium chloride solution, equivalent to benzalkonium chloride - 0.1 mg, disodium edetate - 0.1 mg, sodium chloride - 2.5 mg, tyloxapol - 0.25 mg, mannitol - 33 mg, carbomer (974R) - 4 mg, sodium hydroxide and / or hydrochloric acid concentrated acid - to adjust the pH, purified water - to 1 ml.

Individual hypersensitivity to drug components;

pharmachologic effect

Antiglaucoma drug is a local carbonic anhydrase inhibitor. Carbonic anhydrase is an enzyme found in many tissues of the body, including the tissues of the eye. Catalyzes reversible reactions in which carbon dioxide hydration and carbonic acid hydrolysis take place. In humans, carbonic anhydrase is present in the form of a number of isoenzymes, the most active of which is carbonic anhydrase II (CA-II), which is 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 a slowdown in the formation of bicarbonate ions with a subsequent decrease in sodium and fluid transport. The result is a decrease in intraocular pressure.

Pharmacokinetics

Suction

When applied topically, brinzolamide is absorbed into the systemic circulation.

Distribution

Plasma protein binding is 60%.

Metabolism

Brinzolamide is absorbed in erythrocytes due to selective binding to carbonic anhydrase II.

It is metabolized to form N-desethylbrinzolamide, which binds to carbonic anhydrase (mainly carbonic anhydrase-I) and also accumulates in erythrocytes.

Since brinzolamide and its metabolite accumulate in erythrocytes, their plasma concentration is below the limit of quantitation (<10 ng / ml).

Withdrawal

T1 / 2 is 111 days. Brinzolamide is excreted in the urine unchanged and in the form of metabolites - the main one (N-desethylbrinzolamide) and small concentrations of other metabolites (N-desmethoxypropyl and O-desmethyl).

Side effect

From the side of the organ of vision: 5-10% - blurred vision; 1-5% - blepharitis, keratitis, dry eyes, flushing, sensation of a foreign body in the eye, discharge from the eyes, discomfort, pain, itching of the eyes; <1% - conjunctivitis, keratoconjunctivitis, keratopathy, initial symptoms of blepharitis (sticking of the eyelids or crust 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.

From the respiratory system: 1-5% - rhinitis; <1% - shortness of breath, pharyngitis.

From the side of the cardiovascular system: <1% - chest pain, hypertension.

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

Allergic reactions: <1% - urticaria.

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

Application during pregnancy and lactation

Adequate and strictly controlled clinical studies of the safety of using Azopt in pregnant women have not been conducted. 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 is excreted in breast milk. Therefore, if it is necessary to prescribe Azopt during lactation, the issue of stopping breastfeeding should be resolved.

Application for violations of liver function

Azopt should be prescribed with caution in severe liver dysfunction.

Application for impaired renal function

Since Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe renal impairment (CC <30 ml / min).

Application in children

The efficacy and safety of using Azopt in children has not been established.

special instructions

Azopt should be prescribed with caution in severe liver dysfunction.

Since Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe renal impairment (CC <30 ml / min).

It should be borne in mind that brinzolamide is a sulfonamide. Since when applied topically, its systemic absorption occurs, the development of adverse reactions is possible, incl. 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 instructions for its use. With the development of severe adverse reactions, the use of the drug should be discontinued.

It should be borne in mind that benzalkonium chloride, which is part of the drug Azopt, can accumulate in contact lenses, so the lenses should be removed before instillation and installed back no earlier than 15 minutes after using the drug.

When using several drugs, the interval between instillation should be at least 15 minutes.
Do not touch the eye with the tip of the dropper bottle.

Use in pediatrics

The efficacy and safety of using Azopt in children has not been established.

Influence on the ability to drive vehicles and mechanisms

Immediately after using Azopt, blurred vision may temporarily occur. Therefore, the patient should be careful when driving vehicles and when working with equipment.

Overdose

There are no data on overdose with local application of Azopt.

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

Treatment: if necessary, carry out symptomatic therapy; it is also necessary to control the pH of the blood, the level of electrolytes (especially potassium).

Drug interactions

With the simultaneous use of Azopt and carbonic anhydrase inhibitors for systemic use, it is possible to increase systemic reactions associated with inhibition of the enzyme. Therefore, it is not recommended to prescribe such a combination.

With the simultaneous use of Azopt and salicylates in high doses, violations of the acid-base and electrolyte balance are possible.