Azopt, eye drops 10mg/ml, 5ml

Composition

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1 ml of eye drops contains:

Active ingredient:

10 mg brinzolamide;

excipients:

benzalkonium chloride,

mannitol,

carbomer 974 P,

tyloxapol,

disodium edetate,

sodium chloride,

sodium hydroxide and/or hydrochloric acid, concentrated (to maintain the pH level),

purified water.

Pharmacological action

Brinzolamide is an inhibitor of carbonic anhydrase P. Due to inhibition of carbonic anhydrase II, the formation of bicarbonate ions slows down, followed by a decrease in sodium and fluid transport, which leads to a decrease in the production of intraocular fluid in the ciliary body of the eye. As a result, there is a decrease in intraocular pressure (IOP).

Pharmacokinetics

When applied topically, brinzolamide penetrates the systemic circulation. Brinzolamide is adsorbed in red blood cells as a result of selective binding. A metabolite is formed – N-desethyl brinzolamide, which also binds to carbonic anhydrase and accumulates in red blood cells. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I.

Plasma concentrations of brinzolamide and its metabolite are below the limit of quantification (less than 10 ng / ml). The elimination half-life is 111 days. Binding to plasma proteins is about 60%. Brinzolamide is mainly excreted unchanged in the urine. The main metabolite (N-desethylbrinzolamide) and low concentrations of other metabolites (N-desmethoxypropyl and O-desmethyl) are also found in the urine.

Indications

Reduction of elevated intraocular pressure in: open-angle glaucoma; ocular hypertension.

Use during pregnancy and lactation

No adequate and well-controlled studies have been conducted in pregnant women. It is possible to use the drug for the treatment of pregnant women as prescribed by the attending physician, if the expected therapeutic effect exceeds the risk of developing potential side effects for the fetus.

Breast-feeding should be discontinued when using the drug.

Use in pediatrics it is recommended to use in children, since at the moment the safety and effectiveness of the drug for children have not been established.

Contraindications

Individual hypersensitivity to the components of the drug Azopt. Since Azopti and its metabolites are mainly excreted by the kidneys, it is not recommended for patients with severe renal impairment (creatinine clearance less than 30 ml / min).

Cautiously, the use of the drug has not been studied in patients with angle-closure glaucoma. The use of the drug has not been studied in patients with severe liver diseases, so such patients should be prescribed with caution.

Sensitization of the body with sulfonamides can develop if the drug is prescribed repeatedly in violation of the instructions for its use. If serious adverse reactions occur or if there are signs of hypersensitivity, the drug should be discontinued.

Side effects

In 5-10% of cases: blurred vision, bitter, sour, or unusual taste in the mouth.

In 1-5% of cases: blepharitis, dermatitis, dry eye, foreign body sensation, headache, conjunctival hyperemia, eye discharge, eye discomfort, keratitis, pain and itching in the eyes, rhinitis.

Less than 1% of cases: local reactions-conjunctivitis, keratoconjunctivitis, diplopia, keratopathy, lacrimation, asthenopia, crust on the edges of the eyelids; systemic reactions – dizziness, hypertension, shortness of breath, chest pain, dry mouth, dyspepsia, nausea, diarrhea, lower back pain, pharyngitis, alopecia, allergic reactions, urticaria.

Azopt is a sulfonamide. Since systemic absorption of the drug occurs when applied topically, side effects characteristic of sulfonamides may occur. Rarely, but there may be deaths caused by a severe reaction to sulfonamides, including Stevens-Johnson syndrome, toxic epidermal necrolysis, lightning-fast hepatonecrosis, agranulocytosis, aplastic anemia, and other hematopoietic disorders.

Interaction

Concomitant use with oral carbonic anhydrase inhibitors is not recommended, as there is a possibility of increased systemic adverse reactions.

High-dose salicylates increase the risk of systemic side effects.

If necessary, it can be used in combination with other topical ophthalmic medications. In this case, the interval between their use should be at least 10 minutes.

How to take, course of use and dosage

Locally. Shake the bottle before use.

Instill 1 drop into the conjunctival sac twice a day.

Overdose

There are no reports of overdose symptoms when applied topically.

When taking the drug orally, there may be a violation of the electrolyte balance, the development of acidosis, as well as disorders of the nervous system.

It is necessary to monitor the level of electrolytes (especially potassium) and the pH of the blood.

Special instructions

Shake the bottle before use. The bottle must be closed after each use. Do not touch any surfaces with the tip of the pipette.

If the patient’s vision is temporarily reduced after using the drug, it is not recommended to drive a car or engage in activities that require increased attention and reaction before it is restored. Azopt contains the preservative benzalkonium chloride, which can be absorbed by contact lenses. Before applying the drug, the lenses should be removed and replaced no earlier than 15-20 minutes after instillation of the drug.

Form of production

Eye drops.

Storage conditions

At a temperature of 4-30 °C

Shelf life

2 years

Active ingredient

Brinzolamide

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Description

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Glaucoma