Brinzolamide, Timolol | Azarga eye drops, 5 ml

Latin name

AZARGA

Release form

Azarga eye drops. Eye drops.

Packing

5 ml - dropper bottle (1) drop-container made of low density polyethylene - cardboard packs.

Pharmacological action of

Brinzolamide is an inhibitor of carbonic anhydrase II. Due to the inhibition of carbonic anhydrase II, there is a slowdown in the formation of bicarbonate ions, 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).

Timolol is a non-selective beta-adrenergic receptor blocker without sympathomimetic activity, does not have a direct depressive effect on the myocardium, and does not have membrane-stabilizing activity. When applied topically, it reduces intraocular pressure by reducing the formation of aqueous humor and a slight increase in its outflow.

The combined effect of brinzolamide and timolol exceeds the action of each substance separately.

Pharmacokinetics

When applied topically, brinzolamide and timolol penetrate into the systemic circulation. Brinzolamide is absorbed in red blood cells as a result of selective binding mainly with carbonic anhydrase II. Cmax of brinzolamide in red blood cells is about 18.4 M. Plasma protein binding is about 60%.

Brinzolamide metabolism occurs by N-dealkylation, O-dealkylation and oxidation of the N-propyl side chain. The main metabolite is N-deethylbrinzolamide, in the presence of brinzolamide it binds predominantly to carbonic anhydrase I and also accumulates in red blood cells. In vitro studies show that the metabolism of brinzolamide is mainly responsible for the isoenzyme CYP3A4, as well as the isoenzymes CYP2A6, CYP2B6, CYP2C8 and CYP2C9. Brinzolamide is excreted mainly by the kidneys unchanged - about 60%. About 20% is excreted in the form of metabolites: the main metabolite (N-desethylbrinzolamide) and trace concentrations of other metabolites (N-desmethoxypropyl and O-desmethyl).

Cmax of timolol in the blood plasma is about 0.824 ng / ml and remains until the detection threshold for 12 hours. T1 / 2 of timolol is 4.8 hours after topical application of Azarga. Timolol metabolism occurs in two ways: with the formation of an ethanolamine side chain on the thiadiazole ring and with the formation of an ethanol side chain for morpholine nitrogen and a similar side chain with a carbonyl group connected to nitrogen. Timolol metabolism is carried out mainly by the CYP2D6 isoenzyme. Timolol and the resulting metabolites are mainly excreted by the kidneys. About 20% of timolol is excreted unchanged, the rest - in the form of metabolites.

Indications

Decreased elevated intraocular pressure in open-angle glaucoma and intraocular hypertension in patients in whom monotherapy was insufficient to reduce intraocular pressure.

Contraindications

bronchial asthma (including history)

chronic obstructive pulmonary disease of severe severity

bronchial hyperresponsiveness

sinus bradycardia

AV block II-III degree

severe heart failure

cardiogenic shock

allergic rhinitis mild severe angle-closure glaucoma

simultaneous use with oral carbonic anhydrase inhibitors

pregnancy

lactation period

children under 18

hypersensitivity to group of beta-blockers, hyperchloremic acidosis

hypersensitivity to sulfonamides

hypersensitivity to the components of the drug.

Caution: patients with hyperthyroidism, Prinzmetal angina, violation of peripheral and central blood circulation and arterial hypotension.

Experience in using Azarga to treat patients with pseudoexfoliation glaucoma, pigmented glaucoma is limited: in these cases, use the drug with caution and constantly monitor intraocular pressure.

Anaphylactic reactions. Patients with atopy or with severe anaphylactic reactions to various history of allergens receiving beta-blockers may be resistant to normal doses of adrenaline in the treatment of anaphylactic reactions.

System effects. Brinzolamide and timolol may undergo systemic absorption. When used locally, timolol can cause the same side effects from the cardiovascular and respiratory systems as systemic beta-blockers. The condition of the patient should be monitored before and during timolol therapy. Cases of severe respiratory and cardiovascular disorders, including death from bronchospasm in patients with bronchial asthma and death from heart failure using timolol, are described.

Beta-blockers should be used with caution in patients with a tendency to hypoglycemia or diabetes (especially labile diabetes), since these drugs can mask the symptoms of acute hypoglycemia.

Before the planned operation, beta-blockers should be gradually (not simultaneously) canceled 48 hours before general anesthesia, because during general anesthesia, they can reduce the sensitivity of the myocardium to sympathetic stimulation, the necessary day of the heart.

Azarga contains brinzolamide, which is a sulfonamide. Because when applied topically, a systemic absorption of the drug occurs, adverse reactions characteristic of sulfonamides may occur. The development of acid-base imbalance with the use of oral forms of carbonic anhydrase inhibitors is described.

Use during pregnancy and lactation

Azarga is contraindicated in pregnancy and lactation.

Composition

Eye drops 1 ml

brinzolamide 10 mg

timolol (in the form of maleate) 5 mg

Excipients: mannitol, disodium edetate, sodium chloride, purified water, benzalkonium chloride 50% sodium hydroxide.

Dosage and Administration

Locally. Shake the bottle before use.

1 drop in the conjunctival sac of the eye 2 times / day.

After using the drug to reduce the risk of developing systemic side effects, it is recommended to lightly press a finger on the projection area of ​​the lacrimal sacs at the inner corner of the eye for 1-2 minutes after the installation of the drug - this reduces the systemic absorption of the drug.

If a dose has been missed, then treatment should be continued with the next dose as scheduled. The dose should not exceed 1 drop in the conjunctival sac of the eye 2 times / day.

If you replace any anti-glaucoma drug with Azarga, you should start using Azarga the day after the previous drug is canceled.

Side effects

Local reactions: 1-10% of cases - blurred vision, eye pain, eye irritation, foreign body sensation 0.1-1% of cases - corneal erosion, acne keratitis, dry eye syndrome, eye discharge, itching in the eye , blepharitis, allergic conjunctivitis, effusion in the anterior chamber of the eye, conjunctival hyperemia, crusting on the edges of the eyelids, asthenopia, sensation of 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 disease, pain in the oropharynx, rhinorrhea, cough, impaired hair growth, lichen planus.

Brinzolamide

Local reactions: keratitis, keratopathy, increased excavation of the optic disc, defect in the corneal epithelium, increased intraocular pressure, deposits on the cornea, formation of corneal defects, corneal edema, conjunctivitis, meibomian gland inflammation, diplopia, photophobia, photopsia, decreased visual acuity, pterygium, dry keratoconjunctivitis, eye hypesthesia, scleral pigmentation, subjunctival imbalance, subconjuncture , swelling of the eye, allergic reactions of the eye, mydriasis, swelling of the eyelids.

Systemic side effects: apathy, depression, decreased libido, nightmares, nervousness, drowsiness, motor dysfunctions, amnesia, memory impairment, disorders of the central nervous system.

Treatment: Flush eyes immediately with water. Symptomatic and supportive therapy. Electrolyte levels and blood pH should be monitored. Hemodialysis is ineffective.

Storage Conditions

Store at 2 РC to 30 РC, out of the reach of children. Use within 4 weeks of opening the vial.

Shelf life

2 years.

Deystvuyushtee substance

Brinzolamide, Timolol

Terms and conditions

prescription

dosage form

eye drops

Appointment

Appointment

Adults doctor's prescription

Alcon, USA