Active substanceBrinzolamideBrinzolamide
Similar drugsTo uncover
  • Asopt®
    drops d / eye 
    Novartis Pharma AG     Switzerland
  • Brinzopt
    drops d / eye 
  • Dosage form: & nbspeye drops
    Composition:

    Composition per 1 ml of the preparation:
    Active ingredient: Brenzolamide 10.00 mg; auxiliary components: tyloxapol 0.25 mg, carbomer 974 P 4.00 mg, mannitol (E 421) 33.00 mg, sodium chloride 2.50 mg, disodium edetate dihydrate 0.10 mg, benzalkonium chloride 0.15 mg , sodium hydroxide or hydrochloric acid - to a pH of 7.5 ± 0.1, purified water to 1.0 ml.

    Description:White or almost white suspension.
    Pharmacotherapeutic group:The antiglaucoma agent is a carbonic anhydrase inhibitor
    ATX: & nbsp

    S.01.E.C   Inhibitors of carbonic anhydrase

    S.01.E.C.04   Brinzolamide

    Pharmacodynamics:

    Brinzolamide is an inhibitor of carbonic anhydrase II (KA-II). Carboangihydra - an enzyme, which is determined in many tissues of the body, including in the tissues of the eye. Catalyzes reversible reactions in which hydration of carbon dioxide and hydrolysis of carbonic acid occurs. Inhibition of carbonic anhydrase at the level of the ciliary body reduces the secretion of aqueous humor by slowing the formation of bicarbonate ions, followed by a decrease in the transport of sodium and water, which leads to a decrease in intraocular pressure. Increase in intraocular pressure is the main risk factor for damage to the optic nerve and narrowing the boundaries of fieldsview.

    Pharmacokinetics:

    After instillation brenzolamide enters the systemic circulation. Due to the high affinity for KA-II brenzolamide is adsorbed in erythrocytes. There is a large half-life of Brinzolamide from whole blood (an average of 24 weeks). A person develops a metabolite N-desethyl-brinzolamide, which binds to the CA and accumulates in the erythrocytes. This metabolite is mainly associated with KA-I in the presence of brenzolamide. In plasma, the concentration of Brinzolamide and N-desethyl-brinzolamide below the limit of quantitation (<7.5 ng / ml). Binding to plasma proteins is about 60%.

    Brinzolamide is excreted mainly by the kidneys in an unchanged form (approximately 60%). N- Desethyl-Brinzolamide is also present in urine along with trace amounts of metabolites N-desmethoxypropyl and O-desmethyl.

    Indications:

    Brinzopt is designed to reduce increased intraocular pressure in ophthalmic hypertension and open-angle glaucoma:

    - as a monotherapy in adult patients who do not respond to beta-blockers;

    - in adult patients who are contraindicated with beta-blockers;

    - as an additional therapy to beta-blockers or analogues prostaglandins.

    Contraindications:

    - Hypersensitivity to the active ingredient or to any of the auxiliary substances;

    - Known hypersensitivity to sulfonamides;

    - Severe renal insufficiency;

    - Hyperchloremic acidosis.

    Carefully:

    Care should be taken when using Brinzopt in patients at risk of developing renal failure because of the possible development of metabolic acidosis.

    Brinzolamide has not been studied in preterm infants (gestational age less than 36 weeks) or in children under one week of age. Patients with anomalies or significant immaturity of the renal tubules can receive treatment with brenzolamide only after a thorough assessment of the risk / benefit ratio, as there is a risk of developing metabolic acidosis.

    Carbonic anhydrase inhibitors used orally may affect the ability to perform actions requiring attention concentration and / or high coordination of movements. Brinzopt enters the systemic circulation and, thus, these phenomena can occur after topical application.

    The experience of using Brinzolamide in the treatment of patients with pseudoexfoliation or pigment glaucoma is limited.It is advisable to use caution when applying Brinzopt in the treatment of such patients and to perform careful monitoring of intraocular pressure (IOP).

    The use of brenzolamide in patients whoDo not wear contact lenses. was studied. A careful observation is recommended when using brinzolamide in such patients, since carbonic anhydrase inhibitors can influence the degree of moistening of the cornea, which can increase the risk of corneal injury when wearing contact lenses. Careful monitoring of patients with a high risk of corneal damage, such as patients with diabetes mellitus and corneal dystrophy, is required. Benzalkonium chloride, which is often used in ophthalmic preparations as a preservative, can cause point keratopathy and / or toxic ulcer keratopathy. Since Brinzopt contains benzalkonium chloride, careful monitoring is necessary in case of frequent or prolonged use in patients with dry eye syndrome or in cases of corneal damage. Benzalkonium chloride can change the color of soft contact lenses.Patients should be instructed to remove soft contact lenses before using Brinzopt and reinstall them again 15 minutes after instillation.

    Pregnancy and lactation:

    Fertility

    According to the results of animal studies, no information has been obtained on the effect of brinzolamide on fertility. There have been no studies to evaluate the effect of a solution of Brinzolamide for local ophthalmic use on human fertility.

    Pregnancy

    There is no reliable data on the use of brinzolamide in pregnant women. In animal studies, data on reproductive toxicity have been obtained after systemic use. Brinzolamide is not recommended for use during pregnancy and women of childbearing age who do not use contraceptives.

    Breastfeeding period

    It is not known whether brenzolamide / its metabolites into breast milk after instillation into the conjunctival cavity. In animal studies, excretion of the minimum levels of brenzolamide in breast milk after oral administration has been demonstrated.

    Due to the potential for side effects in the infant during the treatment of the mother with Brinzopt drops, 10 mg / ml, a decision must be made to stop breastfeeding or to stop treatment, taking into account the importance of treatment for the mother and the importance of breastfeeding for the baby.

    Dosing and Administration:

    Doses

    When used as a monotherapy or in combination, the dose is one drop of the Brinzopt drug in the conjunctival sac of the affected eye (affected eyes) twice a day. Some patients can better respond to treatment in the case of the drug one drop three times a day.

    When switching from therapy to another ophthalmologic antiglaucoma drug for treatment with Brinzopt, the use of the Brinzopt preparation should be started the next day.

    If more than one medicinal product is used for topical application, the remaining preparations should be instillated at intervals of not less than 5 minutes, ophthalmic ointments should be used last.

    If a single dose is missed, treatment should be continued with the next dose.The dose should not exceed one drop in the affected eye (affected eyes) three times a day.

    Mode of application

    Locally. After instillation, nasolacrimal occlusion or easy closure of the eyelid is recommended. This can reduce the ingestion of the drug into the systemic bloodstream, which leads to a reduction in systemic side effects.

    The patient should be instructed to shake the bottle well before use. To prevent infection tip of the dropper and suspension should avoid contact with the surface of the eye and other surfaces. The patient should be instructed to keep the bottle tightly closed between applications.

    Elderly

    There is no need for dose adjustment in elderly patients.

    Renal and hepatic impairment

    The use of Brinzolamide has not been studied in patients with hepatic impairment and therefore, for this pathology its use is not recommended.

    The use of Brinzolamide has not been studied in patients with severe renal insufficiency (creatinine clearance <30 mL / min) or in patients with hyperchloremic acidosis. Because the brenzolamide and its main metabolite is excreted mainly by the kidneys, Brinzopt is contraindicated for patients with these conditions.

    Children and teens

    The efficacy and safety of Brinzopt in patients aged 0 to 17 years have not been established. It is not recommended to use the drug in this group of patients.

    Side effects:

    In clinical trials involving more than 2,732 patients who received brenzolamide as monotherapy or additional therapy with timolol maleate 5 mg / ml, the most frequently reported adverse reactions were: dysgeusia (6.0%) (bitter or unusual taste) and temporary blurring of vision (5.4%) after instillation over several seconds to several minutes.

    The frequency of adverse reactions given below is determined by the following frequency categories: very often (≥1 / 10); often (≥1 / 100 and <1/10); infrequently (≥1 / 1000 and <1/100); rarely (≥1 / 10000 and <1/1000); rarely (<1/10000); with an unknown frequency (which can not be estimated on the basis of available data). In each group of frequencies, adverse reactions are presented in order of frequency of occurrence. Adverse reactions were obtained from clinical studies and from post-marketing spontaneous reports.

    Infections and infections:

    Infrequently: nasopharyngitis, pharyngitis, sinusitis.

    With unknown frequency: rhinitis.

    On the part of the hematopoiesis system:

    Infrequently: Reducing the number of red blood cells, increasing the chlorine content in the plasma.

    From the immune system:

    With unknown frequency: hypersensitivity.

    From the side of metabolism and nutrition:

    With unknown frequency: decreased appetite.

    Mental disorders:

    Infrequently: apathy, depression, depressed mood, decreased libido, nightmares, nervousness;

    Rarely: Insomnia.

    From the nervous system:

    Infrequently: motor dysfunction, amnesia, dizziness, paresthesia, headache;

    Rarely: memory impairment, drowsiness;

    With unknown frequency: tremor, hypoesthesia, agevia.

    From the side of the organ of vision:

    Often: blurred vision, eye irritation, eye pain, foreign body sensation in the eyes, eye hyperemia.

    Infrequently: corneal erosion, keratitis, spot keratitis, keratopathy, accumulation in the eye, staining the cornea, defective corneal epithelium, breach of the integrity of the corneal epithelium, blepharitis, itching of the eyes, conjunctivitis, conjunctival edema, meibomite, photophobia, allergic conjunctivitis, pigment accumulation in the cornea during diagnostic tests to confirm corneal epithelial integrity disorder, pterygium, scleral pigmentation, asthenopia, discomfort in the eyes, unusual sensation in the eye,dry eye syndrome, subconjunctival cysts, conjunctival injection, itchy eyelids, discharge from the eyes, crust on the edges of the eyelids, lacrimation.

    Rarely: corneal edema, diplopia, decreased visual acuity, photopsy, hypoesthesia, periorbital edema, increased intraocular pressure, changes in the ratio of excavation diameters to the diameter of the optic disc;

    With unknown frequency: violations of the cornea, visual impairment, allergic manifestations of the eyes, madarose, violations of the eyelids, erythema century.

    From the side of the organ of hearing and labyrinth:

    Rarely: ringing in the ears.

    With unknown frequency: dizziness.

    From the side of the cardiovascular system:

    Infrequently: cardiorespiratory distress syndrome, bradycardia, heart palpitations.

    Rarely: stenocardia, a violation of the rhythm of heartbeats.

    With unknown frequency: arrhythmia, tachycardia, hypertension, increased blood pressure, lower blood pressure, increased heart rate.

    Disorders from the respiratory, thoracic and mediastinal organs:

    Infrequently: shortness of breath, nosebleeds, oropharyngeal pain, pharyngeal pain, irritation in the throat, cough syndrome of the upper respiratory tract, runny nose, sneezing.

    Rarely: bronchial hyperactivity, a feeling of congestion in the upper respiratory tract, edema of the mucous membrane of the paranasal sinuses, congestion of the nose, coughing, dryness in the nose.

    With unknown frequency: bronchial asthma.

    From the gastrointestinal tract:

    Often: dysgeusia.

    Infrequently: esophagitis, diarrhea, nausea, vomiting, dyspepsia, pain in the upper abdomen, abdominal discomfort, stomach discomfort, flatulence, frequent bowel movement, gastrointestinal disorders, decreased sensitivity in the mouth, paresthesia in the mouth, dry mouth .

    From the hepatobiliary system:

    With unknown frequency: change in the results of analysis of the functional state of the liver.

    From the skin and subcutaneous fat:

    Infrequently: a rash, maculopapular rash, a feeling of tightness of the skin.

    Rarely: urticaria, hair loss, generalized itching.

    With unknown frequency: dermatitis, erythema.

    From the musculoskeletal system and connective tissue:

    Infrequently: back pain, muscle spasms, myalgia.

    With unknown frequency: arthralgia, pain in the extremities.

    On the part of the kidneys and urinary tract:

    Infrequently: pain in the kidney area.

    With unknown frequency: pollakiuria.

    On the part of the reproductive system:

    Infrequently: erectile disfunction.

    Common violations:

    Infrequently: pain, discomfort in the chest, increased fatigue, unusual sensations.

    Rarely: pain in the chest, a sense of anxiety, asthenia, irritability.

    With unknown frequency: peripheral edema, malaise.

    Injuries, poisoning and complications during instillation

    Infrequently: the sensation of a foreign body in the eye.

    Description of individual adverse reactions

    Dysgeusia (a bitter or unusual taste in the mouth after instillation) is the most common systemic adverse reaction noted during clinical studies of brenzolamide. Most likely, it is associated with the passage of eye drops into the nasopharynx through the nasolacrimal canal. Nasolacrimal occlusion or easy eyelid closure after instillation can help in reducing the frequency of this effect.

    Brinzopt is an inhibitor of carbonic anhydrase with a sulfonamide structure, its excretion into the systemic circulation is noted. Side effects with regard to the gastrointestinal tract, nervous system, hematologic indices, kidneys, as well as metabolic abnormalities were mainly noted in systemic use of carbonic anhydrase inhibitors.Side effects noted with oral administration of carbonic anhydrase inhibitors may also occur after topical application in ophthalmology.

    No unexpected side effects were observed with the use of Brinzolamide as an additional therapy for travoprost. The observed adverse reactions with additional therapy were seen after each active ingredient alone.

    Pediatric Use

    In small-scale short-term clinical trials, about 12.5% ​​of pediatric patients experienced adverse reactions, most of which were local, non-serious eye reactions, such as conjunctival injection, eye irritation, discharge from the eyes and lacrimation.

    Overdose:

    There were no cases of overdose with topical application.

    Treatment should be symptomatic and supportive. When overdose may lead to electrolyte imbalance, acidosis, possible disorders of the nervous system. It is necessary to monitor plasma concentrations of electrolytes (especially potassium) and blood pH.
    Interaction:

    Special studies regarding the interaction of Brinzopt with other drugs have not been conducted. In clinical trials, where brenzolamide was used concomitantly with ophthalmic preparations - analogues of prostaglandin and with timolol, there were no adverse interactions. Studies of the joint use of Brinzolamide with miotics or adrenergic drugs have not been conducted.

    Isozymes of cytochrome P-450, responsible for the metabolism of Brinzolamide, include CYP3A4 (basically), CYP2A6, CYP2C8 and CYP2C9. It is expected that inhibitors CYP3A4, such as ketoconazole, itraconazole, clotrimazole, ritonavir and troleandomycin, will inhibit the metabolism of brenzolamide by CYP3A4. It is advisable to use caution while using inhibitors CYP3A4. Nevertheless, the accumulation of Brinzolamide is unlikely, since the secretion is mainly through the kidneys. Brinzolamide is not an inhibitor of cytochrome P-450 isoenzyme.
    Special instructions:

    Brinzopt is an inhibitor of carbonic anhydrase, with a sulfamide structure and although it is applied topically, it can enter the systemic circulation.The same types of adverse reactions that are related to sulfonamides may occur in the case of topical application of Brinzolamide. If signs of severe hypersensitivity reactions appear, it is recommended to stop using this medication.

    Violations of the acid-base balance with oral use of carbonic anhydrase inhibitors have been reported. Should use with caution in patients at risk of developing renal disease. deficiency due to the possible development of metabolic acidosis.

    Brinzolamide has not been studied in preterm infants (gestational age less than 36 weeks) or in children under one week of age. Patients with anomalies or significant immaturity of the renal tubules can receive treatment with brenzolamide only after a thorough assessment of the risk / benefit ratio, as there is a risk of developing metabolic acidosis.

    Carbonic anhydrase inhibitors used orally may affect the ability to perform actions requiring attention concentration and / or high coordination of movements. Brinzopt is absorbed systemically and, thus, these phenomena can occur after topical application.There is a potential additive effect of known systemic effects of inhibiting carbonic anhydrase in patients receiving both oral and topical inhibitors of carbonic anhydrase. Simultaneous use of brinzolamide and oral inhibitors of carbonic anhydrase has not been studied and is not recommended.

    Brinzolamide was evaluated initially with simultaneous use with timolol as an additional therapy for glaucoma. In addition, the effect of reducing intraocular pressure (IOP) of brenzolamide, used as an adjunctive therapy to prostaglandin analog, and travoprost was studied. There is no available long-term data on the use of Brinzolamide as an adjunct to travoprost.

    The experience of using brinzolamide in the treatment of patients with pseudoexfoliation or pigment glaucoma is limited. It is advisable to use caution when applying Brinzopt in the treatment of such patients and to perform careful monitoring of intraocular pressure (IOP). Brinzolamide It has not been studied in patients with narrow-angle glaucoma and its use is not recommended in patients with this pathology.

    The possible effect of Brinzolamide on the endothelium of the cornea was not was studied in patients with a damaged cornea (in particular, patients with a decrease in the number of endothelial cells).

    The use of Brinzolamide in patients who wear contact lenses has not been studied. A careful observation is recommended when using brinzolamide in such patients, since carbonic anhydrase inhibitors can influence the degree of moistening of the cornea, which can increase the risk of corneal injury when wearing contact lenses. Careful monitoring of patients with a high risk of corneal damage, such as patients with diabetes mellitus and corneal dystrophy, is required. Benzalkonium chloride, which is often used in ophthalmic preparations as a preservative, can cause point keratopathy and / or toxic ulcer keratopathy. Since Brinzopt contains benzalkonium chloride, careful monitoring is necessary in case of frequent or prolonged use in patients with dry eye syndrome or in cases of corneal damage. Benzalkonium chloride can change the color of soft contact lenses. Patients should be instructed to remove soft contact lenses before using Brinzopt and reinstall them again 15 minutes after instillation.

    The possible effects of withdrawal syndrome after discontinuing treatment with Brinzopt have not been studied; it is expected that the effect of reducing intraocular pressure will last 5-7 days.

    The efficacy and safety of Brinzopt in patients aged 0 to 17 years have not been established. It is not recommended to use the drug in this group of patients.

    Effect on the ability to drive transp. cf. and fur:

    Brinzopt has an insignificant effect on the ability to drive vehicles and control mechanisms.

    Temporary blurring of vision or other visual impairments may affect the ability to drive. If after instillation blurred vision is noted, the patient should wait until vision is restored, before driving or working with machinery.

    Oral inhibitors of carbonic anhydrase may affect the ability to perform tasks requiring attention and / or physical coordination.
    Form release / dosage:Eye drops 10 mg / ml.
    Packaging:

    For 5 ml of the drug is placed in a 5 ml polyethylene bottle, closed with a drop applicator (stopper with dropper and lid with a safety ring made of polyethylene). A label is applied to the bottle.One bottle together with the instruction for use is placed in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25aboutC, in the original packaging.

    Keep out of the reach of children!

    Shelf life:

    2 years.

    The bottle after opening should be used within 4 weeks.

    Do not use after the expiration date!

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003866
    Date of registration:28.09.2016
    Expiration Date:28.09.2021
    The owner of the registration certificate:K.O. Ромфарм Компани С.Р.Л.K.O. Ромфарм Компани С.Р.Л. Romania
    Manufacturer: & nbsp
    Representation: & nbspРомфарма ОООРомфарма ООО
    Information update date: & nbsp21.03.2017
    Illustrated instructions
      Instructions
      Up