Azarga

Azarga – the combined protivoglaukomny means containing inhibitor of a karboangidraza II and a non-selective blocker of beta adrenoceptors.

Form of release and structure

Dosage form – drops eye: homogeneous suspension of almost white or white color (on 5 ml in plastic bottles droppers of "Droptainer™", in a pack a cardboard 1 bottle).

Contain in 1 ml of drops:

• Active ingredients: бринзоламид – 10 mg; Timololum (in the form of a maleate) – 5 mg;
• Auxiliary components: a benzalkoniya chloride (50% solution), sodium chloride, sodium hydroxide, dinatrium эдетат, тилоксапол, Mannitolum, the water purified.

Indications to use

The Azarga is applied to decrease in the increased intraocular pressure at intraocular hypertensia and an open angle glaucoma in case of inefficiency of monotherapy.

Contraindications

Absolute:

• Closed-angle glaucoma;
• Allergic rhinitis of a heavy current;
• Hyperreactivity of bronchial tubes;
• Chronic obstructive diseases of lungs of a heavy current;
• Bronchial asthma (in the anamnesis including);
• Cardiogenic shock;
• The expressed heart failure;
• Atrioventricular block of the II-III degree;
• Sinus bradycardia;
• Heavy renal failure (clearance of creatinine less than 30 ml/minute);
• Giperkhloremichesky acidosis;
• Age up to 18 years;
• Period of pregnancy and lactation;
• Simultaneous use of peroral inhibitors of a karboangidraza;
• Hypersensitivity to components of Azargi, sulfonamides or beta adrenoblockers.

Relative (drops apply with care):

• Hyperthyroidism;
• Printsmetal's stenocardia;
• Arterial hypotension and cardiovascular diseases;
• Disturbances of the central and peripheric circulation;
• Pseudo-exfoliative glaucoma;
• Pigmental glaucoma;
• Tendency to a hypoglycemia;
• Diabetes mellitus, especially labile current;
• Myasthenia;
• Disturbances of acid-base balance;
• Liver failure;
• Atopy or heavy anaphylactic reactions to various allergens in the anamnesis.

Route of administration and dosage

The Azarga is applied locally. Before use it is necessary to stir up a bottle.

Drug is appointed on 1 drop in a conjunctival sac of an eye by 2 times a day.

For decrease in risk of development of system side effects after instillation it is recommended to press accurately for 1-2 minutes a finger on area of a projection of dacryocysts at an internal corner of an eye (it allows to reduce system absorption of drug).

In case of the admission of the next instillation it is necessary to continue use of medicine from the following dose according to the schedule. It is not necessary to exceed the recommended daily dose.

In case of the previous use of other protivoglaukomny drug to begin to apply Azargu it is necessary next day after cancellation of the previous means.

Side effects

Gradation of side effects from bodies and systems for the following scale: often – from> 1/100 to <1/10; infrequently – from> 1/1000 to <1/100; frequency is unknown – it is not possible to estimate frequency reliably or to establish a direct connection with administration of drug:

• From a nervous system and mentality: often – ^disgevziya1, infrequently – ^bessonnitsa1, frequency is unknown – head ^bol1, ^depressiya1, ^{golovokruzheniye1,2}, cerebrovascular ^narusheniye2, cerebral ^ishemiya2, ^obmorok2, loss ^pamyati2, strengthening of signs and symptoms of a myasthenia ^{of gravis2}, ^koshmary2,3, ^{parestezii2,3}, night ^nervoznost3, ^apatiya3, deterioration ^pamyati3, ^amneziya3, ^sonlivost3, depressive ^{nastroyeniye3}, ^gipesteziya3, ^tremor3, ^agevziya3, motor ^disfunktsii3, decrease ^libido3;
• From an organ of sight: often – pain in ^glazu1, misting ^zreniya1, irritation ^glaz1; infrequently – a syndrome of "a dry eye" ¹, ^fotofobiya1, dot ^keratit1, a hyperemia ^glaz1, a hyperemia ^{konjyunktivy1}, a hyperemia ^sklery1, raised ^{slezotecheniye1}, allocations from ^glaza1, feeling of a foreign body in ^glazakh1, an erythema ^vek1, an exudate in an anterior chamber ^glaza1, an erosion ^rogovitsy1, an itch in ^glazu1,3; frequency is unknown – disturbance ^zreniya1, swelled ^vek1, decrease in sensitivity ^rogovitsy2, ^ptoz2, choroid amotio after filtering ^operatsii2, ^keratit2,3, decrease in sharpness ^zreniya2,3, ^diplopiya2,3, frustration ^zreniya3, deposits in ^glazu3, defect of an epithelium ^rogovitsy3, the increase in excavation of a disk visual ^nerva3, ^madaroz3 increased ^{slezotecheniye3}, allergic reactions ^glaza3, ^pterigium3, increase intraocular ^davleniya3, a swelling ^glaz3, a sensation of discomfort in ^glazu3, disturbance of an epithelium ^rogovitsy3, ^{konjyunktivit3}, ^{keratopatiya3}, an inflammation meibomian ^zhelez3, pigmentation ^sklery3, a contrast decrease ^zreniya3, coloring ^rogovitsy3, Sukhoi ^{keratokonjyunktivit3}, ^fotopsiya3, a hypesthesia ^glaza3, disturbances ^vek3, ^astenopiya3 swelled ^rogovitsy3, formation of crusts at edges ^vek3, ^blefarit3, subconjunctival ^kista3;
• Infectious and parasitic diseases: frequency is unknown – ^rinit3, ^faringit3, ^{nazofaringit3}, ^sinusit3;
• From blood and lymphatic system: frequency is unknown – increase in content of chlorides in ^krovi3, reduction of quantity ^{eritrotsitov3};
• From immune system: frequency is unknown – ^{giperchuvstvitelnost1}, system allergic ^reaktsii2 (including a Quincke's disease), ^krapivnitsa2, ^zud2, local and generalized ^syp2, system red ^volchanka2, ^{anafilaksiya3};
• From an acoustic organ: frequency is unknown – a ring in ^ushakh3, ^vertigo3;
• From cardiovascular system: infrequently – decrease arterial ^davleniya1; frequency is unknown – increase arterial ^davleniya1, cold brushes and ^stopy2, ^oteki2, ^gipotenziya2, pain in ^grudi2, ^AV-blokada2, a phenomenon ^{of Reyno2}, cordial ^{nedostatochnost2}, chronic cordial ^{nedostatochnost2}, a stop ^serdtsa2, ^{bradikardiya2,3}, feeling ^{serdtsebiyeniya2,3}, ^aritmiya2,3, ^{gipertenziya3}, ^{takhikardiya3}, ^{stenokardiya3}, increase in frequency cordial ^{sokrashcheniy3}, irregular frequency cordial ^{sokrashcheniy3}, a cardiorespiratory ^{distress-sindrom3};
• From respiratory system, bodies of a thorax and a mediastinum: infrequently – ^kashel1; frequency is unknown – ^odyshka1, nasal ^{krovotecheniye1}, ^astma1, ^{bronkhospazm2} (it is preferential at patients with a bronkhospastichesky disease in the anamnesis), a congestion ^nosa3, feeling of dryness ^nosa3, ^chikhaniye3, ^rinoreya3, irritation ^gortani3, faringolaringitny ^bol3, a congestion upper respiratory ^putey3, hyperreactivity ^bronkhov3, a syndrome post-nasal ^zateka3;
• From digestive tract: often – a dysgeusia after ^{instillyatsii1,3} (bitter or unusual taste in a mouth); frequency is unknown – dryness in ^rtu1, pain in an upper part belly ^polosti1,3, ^toshnota1,3, ^diareya1,3, pain in ^zhivote2, ^{dispepsiya2,3}, vomiting ^2,3, a sensation of discomfort in an abdominal cavity and ^zheludke3, ^ezofagit3, gastrointestinal ^{rasstroystvo3}, strengthening ^{peristaltiki3}, ^meteorizm3, a hypesthesia and paresthesia of a cavity ^rta3;
• From skin and hypodermic fabrics: frequency is unknown – ^syp1, ^alopetsiya1, ^eritema1,3, psoriazoformny rash or an aggravation ^psoriaza2, makulo-papular ^syp2,3, consolidation ^kozhi3, ^krapivnitsa3, ^dermatit3, generalized ^zud3;
• From skeletal and muscular and connecting fabric: frequency is unknown – ^mialgiya1, pain in ^{konechnostyakh3}, pain in ^spine3, ^artralgiya3, muscular ^spazmy3;
• From kidneys and urinary tract: frequency is unknown – ^{pollakiuriya3}, pain in the area ^pochek3;
• From generative organs and a mammary gland: frequency is unknown – decrease ^libido2, sexual ^{disfunktsiya2}, erectile ^{disfunktsiya3};
• Others: frequency is unknown – pain in ^grudi1, ^{utomlyaemost1,2}, ^asteniya2,3, ^bol3, ^{razdrazhitelnost3}, abnormal ^{oshchushcheniya3}, a sensation of discomfort in ^grudi3, ^{nedomoganiye3}, feeling ^{trevozhnosti3}, peripheral ^otek3;
• Laboratory and tool data: frequency is unknown – increase in maintenance of a lactate dehydrogenase and potassium in ^krovi1.

Notes:

¹ The side reactions observed at use of Azargi.

² Side reactions which arose at monotherapy by Timololum.

³ Side reactions which were noted at monotherapy brinzolamidy.

Special instructions

Even at local use Timololum can cause the same side effects from respiratory and cardiovascular systems, as well as system beta adrenoblockers. For this reason before purpose of drug and during its use it is necessary to control a condition of the patient. Cases of heavy cardiovascular and respiratory frustration, including lethal outcomes, owing to a bronchospasm at patients with bronchial asthma and death from heart failure are known.

Before planned operation using the general anesthesia in 48 hours it is necessary to stop use of Azargi since Timololum, as well as all beta adrenoblockers, can reduce sensitivity of a myocardium to the sympathetic stimulation necessary for cardiac performance.

Being a part of drug (as preservative) the benzalkoniya chloride can cause irritation of eyes and change color of soft contact lenses. It is necessary to remove lenses before an instillation and to be established back not earlier than in 15 minutes.

Benzalkoniya chloride can cause a dot keratopathy and/or a toxic ulcer keratopathy, and бринзоламид – to break hydration of a cornea therefore at prolonged treatment it is necessary to control overall health of the patient, including a condition of its cornea. Special observation is required to patients with a diabetes mellitus, anomalies and dystrophy of a cornea.

It is necessary to be careful at an instillation: not to concern a dropper of an eye and other surfaces to avoid drug pollution. After each use it is necessary to close a bottle.

Due to the possible decrease in clearness of sight directly after an instillation it is recommended to refrain from driving and performance of potentially dangerous types of the works requiring special attention.

Peroral inhibitors of a karboangidraza can influence the speed of reactions and ability to concentration of attention at elderly people. This effect needs to be considered also at purpose of Azargi as its components (including karboangidraza inhibitor бринзоламид) get into a system blood stream.

Medicinal interaction

Researches on an occasion of interaction of Azargi with other drugs were not conducted.

It is impossible to appoint at the same time peroral inhibitors of a karboangidraza since there is a risk of strengthening of system side reactions.

With care it is necessary to use at the same time the drugs inhibiting CYP3A4 isoenzyme such as ритонавир, Clotrimazolum, тролеандомицин, итраконазол and кетоконазол.

At simultaneous use of CYP2D6 inhibitors (for example, quinidine or Cimetidinum) strengthening of systemic action of Timololum (decrease in heart rate) is possible.

There is a probability of strengthening of hypotensive action and/or development of the expressed bradycardia at the combined use of Azargi with peroral blockers of calcium channels, antiarrhytmic drugs, beta adrenoblockers, cardiac glycosides, parasympathomimetics, guanetidiny.

Timololum can mask symptoms of a hypoglycemia and strengthen hypoglycemic action of antidiabetic means.

After sharp cancellation of a clonidine Timololum can promote strengthening of hypertensia.

In need of use of other local ophthalmologic means between instillations it is necessary to observe at least 15-minute intervals.

Terms and storage conditions

To store in the place, unavailable to children, with observance of temperature condition 2-30 ºС.

Period of validity – 2 years, after the first opening of a bottle – 4 weeks.