Azarga, eye drops, 5ml

Composition

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1 ml of eye drops contains:

active ingredients:

brinzolamide 10 mg,

timolol (in the form of maleate) 5 mg,

excipients:

mannitol,

disodium edetate,

sodium chloride,

purified water,

benzalkonium chloride 50%,

sodium hydroxide,

tyloxapol

Pharmacological action

Azarga eye drops contain two main active ingredients-brinzolamide and timolol. Brinzolamide reduces the production of intraocular fluid in the ciliary body of the eye, which leads to a decrease in intraocular pressure.

Timolol is a beta-blocker that does not irritate the sympathetic nervous system and does not depress the heart muscle. When applied topically, it reduces the formation of watery moisture and slightly increases its outflow.

Brinzolamide and timolol when used topically penetrate the systemic circulation. Both the substances themselves and their metabolites are excreted mainly by the kidneys. The combined effect of two active substances is more pronounced than when they are used separately.

Indications

Azarga eye drops are prescribed for elevated intraocular pressure associated with open-angle glaucoma or intraocular hypertension in cases where therapy with drugs with one active component was insufficient to permanently reduce intraocular pressure.

Use during pregnancy and lactation

Azarga is contraindicated in children under 18 years of age, pregnant women and during lactation.

Contraindications

The drug is not recommended for use in bronchial asthma and other severe chronic obstructive pulmonary diseases, bronchial hyperreactivity, severe heart failure, sinus bradycardia, cardiogenic shock, AV block II-III degree.

Contraindications include severe allergic rhinitis, severe renal insufficiency (creatinine clearance less than 30 ml / min), hypersensitivity to beta-blockers, sulfonamides, to the components of the drug as a whole or separately, and when used simultaneously with oral carbonic anhydrase inhibitors. Do not use the drug for angle-closure glaucoma.

Azarga eye drops are contraindicated during pregnancy, lactation and under the age of 18 years.

With caution, Azargu is prescribed for hyperthyroidism, central and peripheral circulatory disorders, arterial hypotension, Prinzmetal angina, diabetes mellitus, a tendency to hypoglycemia, pseudoexfoliative or pigmented glaucoma (with constant monitoring of intraocular pressure).

Patients with a history of severe anaphylactic reactions to various allergens, as well as atopy, while receiving beta-blockers may experience resistance to the usual doses of epinephrine in the treatment of anaphylactic reactions.

Before elective surgery under general anesthesia, the dosage of the drug is gradually reduced and canceled 48 hours before the application of anesthesia.

Side effects

Local reactions:  1-10% of cases – blurred vision, eye pain, eye irritation, foreign body sensation; 0.1-1% of cases – corneal erosion, pinpoint keratitis, dry eye syndrome, eye discharge, itching in the eye, blepharitis, allergic reactions, effusion into the anterior chamber of the eye, conjunctival hyperemia, crusting on the edges of the eyelids, asthenopia, discomfort in the eyes, itching, erythema of the eyelids, allergic blepharitis.

Systemic side effects:  1-10% of cases – dysgeusia; 0.1-1% of cases-insomnia, decreased blood pressure, chronic obstructive pulmonary diseases, oropharyngeal pain, rhinorrhea, cough, hair growth disorders, lichen planus.

Brinzolamide

Local reactions:  keratitis, keratopathy, increased excavation of the optic disc, corneal epithelial defect, increased intraocular pressure, corneal deposits, corneal defects, corneal edema, conjunctivitis, inflammation of the Meibomian glands, diplopia, photophobia, photopsia, decreased visual acuity, pterygium, dry keratoconjunctivitis, eye hypesthesia, scleral pigmentation, subconjunctival cyst, increased lacrimation, visual impairment, edema of the eye, allergic reactions of the eye, mydriasis, edema of the eyelids.

Systemic side effects:  apathy, depression, decreased libido, nightmares, nervousness, drowsiness, motor dysfunction, amnesia, memory loss, CNS disorders.

Treatment:  immediately flush eyes with water.

Symptomatic and supportive care. You should monitor the level of electrolytes and blood pH. Hemodialysis is ineffective.

Interaction

In the case of use with other topical ophthalmic medications, the interval between their use should be at least 15 minutes. Cytochrome P 450 isoenzymes are responsible for the metabolism of brinzolamide: CYP3A4 (mainly), CYP2A6, CYP2B6, CYP2C8 and CYP2C9. Caution should be exercised when prescribing drugs that inhibit the CYP3A4 isoenzyme, such as ketoconazole, itraconazole, clotrimazole, ritonavir and troleandomycin, due to possible inhibition of brinzolamide metabolism. Caution should be exercised when co-prescribing inhibitors of the CYP3A4 isoenzyme. However, the accumulation of brinzolamide is unlikely, since it is excreted by the kidneys. Brinzolamide is not an inhibitor of cytochrome P450 isoenzymes. Interaction studies with other drugs have not been conducted. Concomitant use with oral carbonic anhydrase inhibitors is not recommended, as there is a potential for increased systemic adverse reactions. There is a possibility of increasing the hypotensive effect and/or the development of severe bradycardia when timolol is co-administered with oral calcium channel blockers, guanethidine, beta-blockers, antiarrhythmic drugs, cardiac glycosides and parasympathomimetics. The development of hypertension after abrupt withdrawal of clonidine may increase with simultaneous use of beta-blockers. An increase in the systemic effect of beta-blockers (a decrease in heart rate) can develop with the simultaneous use of CYP2D6 inhibitors (quinidine and cimetidine) timolol. Beta-blockers may enhance the hypoglycemic effect of antidiabetic agents. Beta-blockers can mask the symptoms of hypoglycemia.

How to take, course of use and dosage

The bottle should be shaken before use.

The drug is instilled 2 times a day,1 drop in the conjunctival sac of the eye (the space between the eye and the eyelid).

Immediately after instillation, it is recommended to lightly press your finger on the area under the inner corner of the eye for 1-2 minutes, this reduces the risk of side effects.

If a dose has been missed, the next dose is continued as usual. Do not instill in the eye more than 1 drop 2 times a day.

If Azarga eye drops are prescribed instead of another anti-glaucoma drug, the drops begin to be used the next day after the previous remedy is discontinued.

Special instructions

In elderly patients, oral carbonic anhydrase inhibitors may affect the ability to engage in activities that require increased attention or coordination. This effect should be taken into account when prescribing Azarga, because when applied topically, the drug penetrates the systemic circulation.

When using brinzolamide in patients wearing contact lenses, the condition of the cornea should be monitored, since carbonic anhydrase inhibitors can lead to a violation of its hydration. Careful monitoring of patients with corneal abnormalities, diabetes mellitus, or corneal dystrophy is recommended.

Benzalkonium chloride, which is part of Azarga, can cause pinpoint keratopathy and / or toxic ulcerative keratopathy. With prolonged use of the drug, careful monitoring of patients is recommended. Benzalkonium chloride can be absorbed by contact lenses. Before applying the drug, the lenses should be removed and replaced no earlier than 15 minutes after applying the drug.

Do not touch the tip of the dropper bottle to any surface to avoid contamination of the dropper bottle and its contents. The bottle must be closed after each use.

Influence on the ability to drive motor vehicles and manage mechanisms

After using the drug, visual clarity may temporarily decrease, and until it is restored, it is not recommended to drive a car or engage in activities that require increased attention.

With impaired renal function

The drug is contraindicated in severe renal insufficiency (creatinine clearance less than 30 ml / min).

Use in the elderly

In elderly patients, oral carbonic anhydrase inhibitors may affect the ability to engage in activities that require increased attention or coordination. This effect should be taken into account when prescribing Azarga, because when applied topically, the drug penetrates the systemic circulation.

Form of production

Azarga eye drops. Eye drops.

Storage conditions

At a temperature of 2-30 °C

Shelf life

2 years

Active ingredient

Brinzolamide, Timolol

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

Adults as prescribed by a doctor

Indications

Glaucoma