Azarga eye drops 10mg + 5mg dropper bottle 5ml
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Active ingredients
Brinzolamide + Timolol
Release form
Drops
Composition
Eye drops 1 ml: Brinzolamide 10 mg, timolol (in the form of maleate) 5 mg. Adjuvants: mannitol, disodium edetate, sodium chloride, purified water, benzalkonium chloride 50%, sodium hydroxide, tyloxapol.
Pharmacological effect
Brinzolamide is a carbonic anhydrase II inhibitor. Due to the inhibition of carbonic anhydrase II, the formation of bicarbonate ions is slowed 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). Timolol is a non-selective beta-adrenoreceptor blocker without sympathomimetic activity, does not have a direct depressive effect on the myocardium, and does not have membrane stabilizing activity. When applied topically reduces intraocular pressure by reducing the formation of aqueous humor and a small increase in its outflow. The combined effect of brinzolamide and timolol exceeds the effect of each substance separately.
Pharmacokinetics
When applied topically, brinzolamide and timolol penetrate the systemic circulation. Brinzolamide is absorbed in erythrocytes as a result of selective binding predominantly with carbonic anhydrase II. Сmax of brinzolamide in erythrocytes is about 18.4 μM. 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 mainly to carbonic anhydrase I and also accumulates in erythrocytes. In vitro studies show that the metabolism of brinzolamide is primarily 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-deethylbrinzolamide) and trace concentrations of other metabolites (N-dezethoxypropyl and O-desmethyl). Cmax timolol in plasma is about 0.824 ng / ml and persists to the detection threshold for 12 h .T1 / 2 timolol is 4.8 hours after topical administration 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 in morpholine nitrogen and a similar side chain with a carbonyl group connected to nitrogen. Timolol metabolism is mainly carried out by the CYP2D6 isoenzyme. Timolol and formed metabolites are mainly excreted by the kidneys. About 20% of timolol is excreted unchanged, the rest in the form of metabolites.
Indications
- reduction of increased intraocular pressure in open-angle glaucoma and intraocular hypertension in patients in whom monotherapy was not sufficient to reduce intraocular pressure.
Contraindications
- bronchial asthma (including in history); - chronic obstructive pulmonary disease of a severe course; - hyperreactivity of the bronchi; - sinus bradycardia; - AV-block II-III degree; - severe heart failure; - cardiogenic shock; - allergic rhinitis severe course; severe renal insufficiency (creatinine clearance <30 ml / min); angle-closure glaucoma; simultaneous use with oral carbonic anhydrase inhibitors; pregnancy; lactation period; children under 18; hypersensitivity to the beta group adrenergic blockers, hyperchloremic acidosis; hypersensitivity to sulfonamides; hypersensitivity to drugs; with caution: patients with hyperthyroidism, Prinzmetal angina, disturbed peripheral and central blood circulation and arterial hypotension. limited: in these cases, you should use the drug with caution and constantly monitor the intraocular pressure. Anafilak tic reactions. Patients with atopy or severe anaphylactic reactions to various allergens in history, receiving beta-blockers, may be resistant to the usual doses of adrenaline in the treatment of anaphylactic reactions. Systemic effects. Brinzolamide and timolol may undergo systemic absorption. When used locally, timolol can cause the same side effects of the cardiovascular and respiratory systems as systemic beta-blockers.The patient’s condition 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 when using timolol are described. Beta-adrenergic blockers should be used with caution in patients with a tendency to hypoglycemia or diabetes (especially with labile diabetes), since these drugs can mask the symptoms of acute hypoglycemia. Before a planned operation, beta-blockers should be gradually (not simultaneously) canceled 48 hours before general anesthesia sion, as during general anesthesia, they can reduce the sensitivity of the myocardium to the sympathetic stimulation required by the day of the heart. Azarga contains brinzolamide, which is a sulfonamide. Since when applied topically, systemic absorption of the drug occurs, and side reactions characteristic of sulfonamides may occur. The development of acid-base imbalance in the use of oral forms of carbonic anhydrase inhibitors is described.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
Locally. Shake the bottle before use. For 1 drop in the conjunctival pouch of the eye 2 times / day. After using the drug to reduce the risk of systemic side effects, it is recommended that a finger lightly press on the projection area of the lacrimal sacks at the inner corner of the eye for 1-2 minutes after the drug is installed - this reduces systemic absorption of the drug. If the dose has been missed, treatment should be continued with the next dose on a schedule. The dose should not exceed 1 drop in the conjunctival sac of the eye 2 times / day. In case of replacement of any antiglaucoma drug with the drug Azarga, you should start using Azarga on the next day after the previous drug is discontinued.
Side effects
Local reactions: 1-10% of cases - blurred vision, pain in the eye, eye irritation, foreign body sensation; 0.1-1% of cases - corneal erosion, punctate keratitis, dry eye syndrome, eye discharge, itching in the eye, blepharitis, allergic conjunctivitis,effusion in the anterior chamber of the eye, conjunctival hyperemia, the formation of crusts 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 disease, pain in the oropharynx, rhinorrhea, cough, impaired hair growth, lichen planus. Brinzolamide Local reactions: keratitis, keratopathy, increased excavation of the optic nerve head, defect of the cornea epithelium, increased intraocular pressure, deposits on the cornea, the formation of corneal defects, corneal edema, conjunctivitis, inflammation of the meibomian glands, diplopia, photophobia, photopsia, reduced visual acuity, pterygium, dry keratoconjunctivitis, hypesthesia manhole, sclera pigmentation, subconjunctival cyst, increased tearing, impaired vision, eye swelling, allergic reactions of the eye, mydriasis, eyelid edema. Systemic side effects: apathy, depression, decreased libido, nightmares, nervousness, drowsiness, motor dysfunctions, amnesia, memory, violations of the central nervous system. Treatment: immediately flush eyes with water. Symptomatic and supportive therapy. Electrolyte levels and blood pH should be monitored. Hemodialysis is ineffective.
Overdose
Cases of overdose were reported. When they occur, symptomatic therapy is performed. It is necessary to control the level of electrolytes (especially potassium) and blood pH.
Interaction with other drugs
Research on the interaction with other drugs was not conducted. Concurrent use with oral carbonic anhydrase inhibitors is not recommended, since There is a possibility of increased systemic adverse reactions. Cytochrome P450 isoenzymes: CYP3A4 (mostly), CYP2A6, CYP2B6, CYP2C8 and CYP2C9 are responsible for the metabolism of brinzolamide. It is necessary to prescribe with caution drugs inhibiting CYP3A4 isoenzyme, such as ketoconazole, itraconazole, clotrimazole, ritonavir and troleandomycin, due to the possible inhibition of the metabolism of brinzolamide. Care should be taken when co-prescribing inhibitors of the isoenzyme CYP3A4. However, accumulation of brinzolamide is unlikely, since it is excreted by the kidneys.Brinzolamide not an inhibitor of cytochrome isoenzymes R450.Suschestvuet probability amplification hypotensive action and / or develop severe bradycardia with simultaneous application of timolol with calcium channel blocker for oral, guanethidine, beta-blockers, antiarrhythmics, cardiac glycosides and parasympathomimetics .Razvitie hypertension following abrupt withdrawal Clonidine may be enhanced while taking beta-blockers. Strengthening the systemic action of beta-blockers (decrease in heart rate) may develop with simultaneous use of inhibitors of CYP2D6 (quinidine, cimetidine) and timolol. Beta-blockers may enhance the hypoglycemic effect of antidiabetic agents. Beta-blockers may mask the symptoms of hypoglycemia. In case of use with other local ophthalmologic drugs, the interval between their use should be at least 15 minutes.
special instructions
In elderly patients, carbonic anhydrase inhibitors, administered orally, may affect the ability to engage in activities requiring increased attention or coordination. This effect should be considered when prescribing Azarga, since when applied topically, the drug penetrates the systemic circulation. When using brinzolamide in patients wearing contact lenses, the state of the cornea should be monitored, since carbonic anhydrase inhibitors can lead to impaired hydration. It is recommended to carefully monitor patients with corneal abnormalities, diabetes mellitus or corneal dystrophy. Benzalkonium chloride, which is part of the drug Asarga, can cause acne keratopathy and / or toxic ulcerative keratopathy. With prolonged use of the drug is recommended to carefully monitor patients. Benzalkoniya chloride can be absorbed by contact lenses. Before using the drug, the lenses should be removed and installed back 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. The effect on the ability to drive vehicles and control mechanisms. After using the drug, the clarity of vision may temporarily decrease and it is not recommended to drive a car and engage in activities requiring increased attention until it is restored.