Brizoton cap. eye. fl. 5 ml

Brizoton is appointed for decrease in intraocular pressure at adult patients with an open angle glaucoma or eye hypertensia at which application of monotherapy did not lead to sufficient decrease in intraocular pressure.

Structure

active ingredients: brinzolamid, Timololum maleate;

1 ml of suspension the brinzolamida of 10 mg, maleate Timololum (in terms of 100% substance) contains 6.84 mg that is equivalent to Timololum of 5 mg;

excipients: tiloksapol, carbomer, dinatrium edetat, a benzalkoniya chloride, a mannitol (E 421), sodium chloride, 1 M solution of sodium of hydroxide, 1 M acid solution hydrochloric, water for injections.

Eye drops Brizoton contain two active agents: brinzolamid and Timololum maleate. These two components reduce the increased intraocular pressure (VGD) by reduction of secretion of intraocular liquid, but do it by means of various mechanisms of action. The combined effect of these two active agents leads to additional reduction of VGD in comparison with effect which is reached at application of any of these components separately.

Brinzolamid – strong inhibitor of a karboangidraza II (KA of II) the person, the dominating eye isoenzyme. Oppression of a karboangidraza in tsiliarny shoots of an eye reduces discharge of intraocular liquid, mainly due to delay of formation of ions of bicarbonate with the subsequent reduction of transportation of sodium and liquid.

Timololum is a non-selective blocker of β-adrenoceptors which has no internal sympathomimetic and membrane stabilizing activity and also the direct oppressing action on a myocardium. Tonografiya and fluorofotometrichesky researches at people confirmed that his main action is connected with decrease in formation of intraocular liquid and small increase in its outflow.

Contraindication

• Hypersensitivity to active ingredients or to any excipients of medicine.
• Hypersensitivity to others of β-blockers.
• Hypersensitivity to sulfonamides.
• State, followed by hyperreactivity of airways, including bronchial asthma or bronchial asthma in the anamnesis, a serious chronic obstructive illness of lungs.
• Sinus bradycardia, a sick sinus syndrome, sinoauricular block, the atrioventricular block of II or III degree which is not controlled by a pacemaker. Profound heart failure, cardiogenic shock.
• Heavy allergic rhinitis.
• Giperkhloremichesky acidosis.
• Heavy renal failure.

Route of administration and doses

Use by the adult, including patients of advanced age

Dose makes 1 drop of eye drops Brizoton in a conjunctival sac of the affected eye (eyes) 2 times a day.

System absorption decreases if to press in the field of a lacrimonasal opening or to close eyelids. It reduces system side reactions and increases local activity (see the section "Features of Application").

If a dose it is passed, treatment should be continued, applying the following dose according to the scheme of application. The dose should not exceed 1 drop in the affected eye (eyes) 2 times a day.

When replacing other ophthalmologic antiglaukomny means with eye drops Brizoton of application of other means should be stopped, having begun application of eye drops Brizoton from the next day.

Patients with abnormal liver functions and kidneys

did not conduct any researches of the medicine Brizoton or eye drops of Timololum of 5 mg/ml at patients with abnormal liver functions and kidneys. There is no need for medicine dose adjustment to patients with abnormal liver functions or to patients with renal failures easy or moderate severity.

did not conduct a medicine Brizoton research at application to patients with heavy degree of a renal failure (clearance of creatinine <30 ml/min.) or to patients with giperkhloremichesky acidosis (see the section "Contraindications"). As brinzolamid and its main metabolite are removed mainly by kidneys, the medicine Brizoton is contraindicated for treatment of this category of patients (see the section "Contraindications").

should use the Drug Brizoton with care to patients with abnormal liver functions of heavy degree (see the section "Features of Application").

Route of administration

For ophthalmologic application.

to the Patient should recommend to shake up well a bottle before application.

After the first opening of a bottle should remove the protective ring intended for control of the first opening.

to prevent pollution of a tip of a dropper and contents of a bottle, it is necessary to be careful and not to concern a century, adjacent areas or other surfaces a bottle dropper tip. The patient should recommend to close densely a bottle after application of drops.

If locally to apply more than one ophthalmologic means, the interval between their application has to make not less than 5 minutes. To apply oculentums in the last turn.

Overdose

At accidental ingestion of contents of a bottle, overdose symptoms β-blockers can include bradycardia, hypotension, heart failure and a bronchospasm.

in case of overdose by eye drops Brizoton treatment has to be symptomatic and supporting. Because of the maintenance of a brinzolamid there can be an electrolytic imbalance, develop an atsidozny state and also potential impact on the central nervous system. It is necessary to control the level of electrolytes in blood serum (especially potassium) and level rn blood. Researches showed that Timololum is difficult removed from an organism by dialysis.

Side reactions

Short overview of data on safety

In clinical trials by the most frequent side reactions were misting of sight, irritation of an eye and eye pain which arose at approximately from 2% to 7% of patients.

Feature of application

Use during pregnancy or feeding by a breast

Pregnancy

Is not present the relevant data on application of a brinzolamid and Timololum to pregnant women. A research of a brinzolamid on animals showed existence of toxic impact on reproductive function (see the section "Preclinical Data on Safety"). Eye drops Brizoton should not be applied during pregnancy. To reduce system absorption, see the section "Route of Administration and Doses".

Epidemiological researches did not reveal negative impact on formation of a fruit, however at oral administration of β-blockers showed risk for pre-natal development. Besides, at application of β-blockers before childbirth at newborns signs and symptoms of β-blockade were observed (for example bradycardia, hypotension, a respiratory distress and a hypoglycemia). Newborns have to be under careful observation during the first days of life if mother Brizoton before childbirth applied eye drops.

that data on application of a brinzolamid to pregnant women are absent or their quantity is limited and researches on animals showed existence of toxic impact on reproductive function, it is not necessary to appoint this medicine during pregnancy and to the women of reproductive age who are not using contraceptive means.

feeding Period a breast

whether gets brinzolamid into breast milk of the person. Researches on animals showed excretion of a brinzolamid in breast milk at oral administration (see. section "Route of Administration and Doses").

β-blockers get into breast milk of the person. However at application of therapeutic doses of Timololum in an eye, it is improbable that its existence in breast milk is sufficient to cause clinical symptoms of β-blockade in newborns. To reduce system absorption see the section "Preclinical Data on Safety". However it is impossible to exclude risk for the child during breastfeeding. Brizoton has to accept the decision on the termination of breastfeeding or abstention from application of eye drops the doctor, considering advantage for women and risk for the child.

Reproductive function

Researches for assessment of the impact on reproductive function of the person at topical ophthalmologic administration Brizoton in the form of eye drops were not conducted.

any effects of a brinzolamid or Timololum on reproductive function at men or women after oral administration.

At application of eye drops Brizoton is not expected any effects on reproductive function of men or women.

Safety and efficiency of application of eye drops Brizoton are not established to children up to 18 years by

. Data on use of this category of patients are absent.

Ability to influence speed of response at control of motor transport or other mechanisms

Eye drops Brizoton have the minimum influence on ability to steer vehicles or to work with mechanisms.

Temporary turbidity of sight or violation from sight can affect ability to steer vehicles or to work with mechanisms. If turbidity of sight arises during burying, the patient needs to wait until the sight is restored before steering vehicles or to work with mechanisms.

Inhibitors of a karboangidraza can worsen ability to carry out the tasks demanding intellectual activity and/or physical coordination (see the section "Features of Application").

Interaction with other medicines and other types of interactions

Brizoton on their interaction with other medicines did not conduct Researches of eye drops.

Though the eye drops Brizoton containing brinzolamid, karboangidraza inhibitor, it is necessary to apply locally, medicine is absorbed systemically. At oral administration of inhibitors of a karboangidraza it was reported about violation of acid-base balance. At the patients applying eye drops Brizoton it is necessary to consider such manifestation of interaction.

probability of emergence of additive effect to already known system effects of inhibitors of a karboangidraza at the patients accepting karboangidraza inhibitors orally and eye drops of a brinzolamid Exists. Simultaneous application of the eye drops containing brinzolamid and oral inhibitors of a karboangidraza is not recommended.

P450 cytochrome Isoenzymes which are responsible for metabolism of a brinzolamid include CYP3A4 (main), CYP2A6, CYP2B6, CYP2S8 and CYP2S9. It is expected that CYP3A4 inhibitors, such as ketokonazol, itrakonazol, Clotrimazolum, ritonavir and troleandomitsin, will oppress the metabolism of a brinzolamid connected with CYP3A4 isoenzyme. It is necessary to be careful at the accompanying use of CYP3A4 inhibitors. However accumulation of a brinzolamid is improbable as he is generally brought by kidneys. Brinzolamid is not inhibitor of isoenzymes of P450 cytochrome.

probability of emergence of the additive effects leading to arterial hypotension and/or the expressed bradycardia at application of the eye drops containing β-blockers along with oral or intravenous blockers of calcium channels (diltiazem), β-blockers, antiarrhytmic means (including Amiodaronum), foxglove glycosides, parasympathomimetics, guanetidiny and reserpine Exists.

β-blockers can reduce sensitivity to adrenaline at treatment of anaphylactic reactions. Especially careful patients should be with an atopy or an anaphylaxis in the anamnesis.

At reception of β-blockers the hypertensive reaction in case of sudden phase-out of a clonidine can amplify. It is recommended to be careful at simultaneous application of eye drops Brizoton and a clonidine.

About strengthening of systemic action of β-blockers (for example decrease in heart rate, a depression) was reported during the combined treatment by CYP2D6 inhibitors (for example kvinidiny, fluoxetine, paroksetiny) and Timololum. It is recommended to apply combinations with care.

β-blockers can enhance hypoglycemic effect of antidiabetic means. β-blockers can mask signs and symptoms of a hypoglycemia.

was reported Sometimes about emergence of a mydriasis at simultaneous application of ophthalmologic β-blockers and adrenaline (epinephrine).

Storage conditions

Drug does not demand special storage conditions.

out of children's reach.

Expiration date - 2 years.

Expiration date after the first opening of a bottle – 28 days.

not to use medicine after the termination of the expiration date specified on packing.