The instruction for use
of medicine for experts
the Trade name
the International unlicensed
name Brinzolamid Lekarstvennaya
the Drop form eye 1% 5 ml, suspension
of 1 ml contains
active agent – brinzolamid 10 mg
excipients: a benzalkoniya chloride (preservative), Mannitolum, carbomer 974P, tiloksapol, dinatrium edetat, sodium chloride, Acidum hydrochloricum and/or sodium hydroxide (for adjustment rn), purified water.
Suspension of white color.
Drugs for treatment of diseases of eyes. Antiglaukomny drugs and miotik, karboangidraza inhibitors.
The code of automatic telephone exchange S01EC04
Pharmacokinetics Later properties of instillation in an eye brinzolamid is soaked up in blood. Thanks to high affinity to KA ІІ, brinzolamid quickly and easily gets into erythrocytes and has long elimination half-life from blood — about 111 days. In a human body the metabolite (N-dezetil-brinzolamid) which also accumulates in erythrocytes is formed and in the presence of a brinzolamid it is active mainly concerning KA of I. In blood plasma brinzolamid and its metabolite are defined in the minimum concentration which are in most cases lower than a limit of test-sensitivity of quantitative definition (less than 7.5 ng/ml). Contacts proteins of blood plasma approximately for 60%. Brinzolamid is brought mainly with urine in not changed look (about 60%). About 20% are removed in the form of a metabolite. In urine are found also Ndezetil-brinzolamid and small amounts of N-dezmetoksipropila and O-dezmetilirovannogo of a metabolite.
Karboangidraz’s pharmacodynamics (coal anhydrase) the zinc-containing enzyme which is present at various body tissues including in kidneys and a ciliary body of an eye.
Enzyme has intracellular localization and participates in process of hydration and dehydration of carbonic acid. There are several types of coal anhydrase, however the karboangidraza of II has the greatest activity.
Both at local, and at system use, inhibitors of a karboangidraza cause decrease in intraocular pressure. The maximum hypotensive effect after Azopt’s burying begins in 2 hours and remains within 12 hours. The maximum decrease in intraocular tension is 14-24% of initial level.
Azopt (brinzolamid) it is characterized by good bioavailability, high selectivity and powerful inhibitory activity in relation to a karboangidraza of the II type.
Azopt has the best shipping in comparison with other inhibitors of a karboangidraza that is explained by its smaller concentration, optimum composition of suspension and physiological rn. At prolonged use of Azopt the decrease in its efficiency is not noted, besides Azopt, as a rule, does not make system impact on an organism.
– an open angle glaucoma
– the increased intraocular pressure
– preoperative preparation.
Azopt it is applied to treatment of the increased intraocular pressure as monotherapy at the patients who are not reacting to β-blockers sick to which β-blockers or in the accompanying therapy with β-blockers are contraindicated.
Route of administration and doses:
To stir up a bottle before the use!
At use as monotherapy or in the accompanying therapy of Azopt dig in on 1 drop twice a day in the lower conjunctival sac of the affected eye (eyes). To some patients 3 times a day recommend to dig in drug.
It is not necessary to touch with a pipette tip eyes or any other surface to avoid pollution of contents of a bottle.
After burying the pressing of the lacrimonasal channel or cover is recommended a century. It reduces system absorption and an adverse effect of the medicine which is applied locally through eye tissues.
When replacing other drug against glaucoma with eye drops of Azopt, it is necessary to stop intake of the replaced drug and to begin Azopt’s reception next day.
When using several ophthalmologic drugs of topical administration, it is necessary to observe an interval between burying at least 5 minutes.
– misting of sight, passing discomfort
– feeling of a foreign body in an eye
– the irritation of an eye, hyperaemia, blepharitis, konyyuktivit
– a keratitis, a keratopathy
– lachrymation, an itching
– decrease in visual acuity
– unusual smack in a mouth (acid or bitter) after burying.
At absorption in rare instances can be noted
– the paresthesias which are characterized as temporary numbness or feeling of pricking in extremities, a depression and dizziness, a headache
– a stethalgia, an allopecia, dryness in a mouth, nausea and dyspepsia.
– hypersensitivity to any component of drug
– the known hypersensitivity to streptocides
– serious violations of function of kidneys
– giperkhloremichesky atsidozirovanny
Metabolism of a brinzolamid happens with the participation of CYP3A4, CYP2A6, CYP2C8, CYP2C9 enzymes. CYP3A4 inhibitors, such as ketakonozol, intrakonozol, Clotrimazolum, ritonavir and trolenzhomitsin suppress metabolism of a brinzolamid.
Combinations to the following medicines are undesirable:
– methylxanthines (Euphyllinum) – potentiation of diuretic effect,
– ammonium chloride and other, acid-forming diuretics – reduction of diuretic effect.
Combinations to cholinergic drugs and β-adrenoblockers are favorable. At simultaneous use with them strengthening of hypotensive effect concerning VGD is possible.
of Azopt is streptocide and at topical administration there is its system absorption. There can be side reactions characteristic of streptocides. In case of serious reactions or hypersensitivity the drug phase-out is recommended.
At the patients accepting at the same time inhibitor karboangidraz and Azopt, the additional system effect which is shown at use of inhibitors karboangidraz can be observed.
Pregnant women should appoint pregnancy of Azopt only in case of emergency.
of Azopt is not recommended to accept to the women nursing.
Safety and efficiency of use for children are not established.
Is recommended constant observation of patients with risk of defeat of a cornea in case of diabetes.
The Patients using lenses need to apply contact lenses with care brinzolamid as inhibitors karboangidraz can affect humidity of a cornea, and use of lenses in this case increases risk of defeat of a cornea.
As Azopt contains chloride a benzalkoniya, it is necessary to refrain from carrying soft (hydrophilic) contact lenses, or to delete them during burying. Lenses can be carried in breaks between use of drug and to insert not earlier than in 15 minutes after burying. It is impossible to apply Azopt over contact lenses.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
As well as in a case with other eye drops, after burying the temporary ambiguity of sight or other visual concerns is possible that it can negatively affect ability to drive the car or other
potentially dangerous mechanisms. In this case it is necessary to wait some time before recovery of sight.
it is not known of overdose cases this drug.
At overdose by Azopt the treatment has to be symptomatic. At overdose there can be a disturbance of electrolytic balance, development of an atsidozny state and also disturbance from nervous system. It is necessary to watch the level of serumal electrolytes (especially potassium) and also to control size rn blood.
A form of release and packing
Eye drops of 1% 5 ml, suspension, in bottles from white opaque plastic with Drop-Tainer™ dropper doser. Each bottle together with the instruction for use is packed into a cardboard box.
To Store storage conditions in vertical position at a temperature from +40 to + 300C (390-860F).
To store in places inaccessible for children!
not to apply an expiration date after an expiration date.
An expiration date after the first opening – 4 weeks at a temperature from +40 to + 300C.
of Rijksweg 14, B-2870 Puurs, Belgium
prescription status According to the prescription