Index of drugs

Reduction of elevated intraocular pressure in: ocular hypertension and open angle glaucoma. It is used as monotherapy in adult patients who do not respond to β-blockers or in adult patients in which β-blockers are contraindicated; and in combination with β-blocks or analogues of prostaglandins.

1 ml of suspension contains 10 mg brinzolamide. The preparation contains benzalkonium chloride.

Carbonic anhydrase II (CA-II) inhibitor, isoenzyme predominant in the eye. Inhibition of carbonic anhydrase in the ciliary processes of the eye reduces the secretion of aqueous humor, presumably by slowing the production of bicarbonate ions and, consequently, reducing the transport of sodium and liquids. The result is a reduction in intraocular pressure. After administration to the conjunctival sac, brinzolamide is absorbed into the systemic circulation. Due to its high affinity for CA-II, brinzolamide extensively extends into red blood cells and shows a long T_0,5 in whole blood (on average about 24 weeks). N-desmethylbrinzolamide, a brinzolamide metabolite formed in man, also binds to CA and accumulates in erythrocytes. In the presence of brinzolamide, this metabolite is mainly associated with CA-I. Plasma concentrations of both brinzolamide and N-desmethylbrinzolamide are low and generally remain below the limit of quantification. The binding of the drug to plasma proteins is not significant (about 60%). Brinzolamide is eliminated mainly by renal secretion (approximately 60%). Approx. 20% of the dose appears in the urine as metabolites.

Hypersensitivity to the active substance or to any of the excipients. Hypersensitivity to sulfonamides. Severe renal impairment (creatinine clearance <30 ml / min). Hyperlloric acidosis.

The drug is absorbed systemically - during the topical application may occur the same types of adverse reactions that are typical for sulfonamides. If signs of severe reactions or hypersensitivity develop, discontinue use. When used in patients at risk for renal dysfunction, caution should be exercised due to the possible risk of metabolic acidosis. Brinzolamide has not been studied in premature babies (in gestational age less than 36 weeks) and in less than 1 week of age. Patients with significant renal tubular immaturity or their abnormalities should only receive brinzolamide after careful consideration of the benefit / risk ratio, due to the possible risk of metabolic acidosis. The drug is not recommended in patients with impaired hepatic function (no studies). Oral carbonic anhydrase inhibitors may impair the ability to perform tasks requiring increased attention and / or motor coordination - the drug is absorbed systemically and therefore may also occur during topical administration. Due to the risk of an additive effect in the known systemic effects of carbonic anhydrase inhibition, co-administration of the preparation and oral carbonic anhydrase inhibitors has not been studied and is not recommended. There is limited experience in the use of the preparation in the treatment of pseudoexfoliative and pigmented glaucoma patients - care should be exercised and close monitoring of intraocular pressure is recommended. The drug has not been studied in patients with narrow-angle glaucoma and its use in these patients is not recommended. The possible effect of brinzolamide on corneal endothelial function in patients with damaged cornea (especially in patients with low endothelial cells) has not been studied. This particularly applies to patients wearing contact lenses that have not been tested and should be carefully monitored when using brinzolamide, as carbonic anhydrase inhibitors may affect the degree of corneal hydration and the use of contact lenses may increase the risk for the cornea. Careful monitoring of patients with corneal lesions, such as patients with diabetes or corneal disorder, is recommended.The benzalkonium chloride contained in the preparation may cause punctate keratopathy and / or toxic ulcerative keratopathy - careful monitoring of patients with dry eye or damaged cornea is required, and who frequently or long-term use the preparation. Benzalkonium chloride may cause eye irritation and discoloration of contact lenses. Avoid contact of the product with soft contact lenses. Patients should be advised of the need to remove soft contact lenses before instillation and to wait for at least 15 minutes after instillation of the preparation for contact lenses. The possible rebound effect after discontinuation of treatment with the preparation has not been studied; the effect of lowering the intraocular pressure should last for 5-7 days. The safety and efficacy of the preparation in infants, children and adolescents aged 0 to 17 years have not been established - use is not recommended.

The preparation is not recommended for use during pregnancy and in women of childbearing potential not using effective contraception. It is not known whether the drug and its metabolites are excreted in human milk. Based on available animal data, brinzolamide was excreted in milk. You should decide whether to stop breastfeeding or stop brinzolamide treatment, taking into account the benefits of breastfeeding for a child and the benefits of treatment for a woman.

Common: blurred vision, eye irritation, eye pain, feeling of a foreign body in the eye, congestion of the eye, disturbed taste. Uncommon: inflammation of the nose and throat, pharyngitis, sinusitis, decrease in the number of red blood cells, increase in blood chloride, apathy, depression, depressed mood, weakness of libido, nightmares, nervousness, dysfunction, amnesia, dizziness, paresthesia, headaches, corneal erosions, keratitis, punctate keratitis, corneal damage, eye deposits, corneal staining, corneal epithelial injury, corneal epithelial disorder, eyelid inflammation, ocular pruritus, conjunctivitis, eye edema, thyroid gland inflammation, blinding, photophobia , dry eye, allergic conjunctivitis, wingfly, scleral staining, poor vision, eye discomfort, impaired eye feeling, dry conjunctivitis and conjunctivitis, conjunctivitis, conjunctival hyperaemia, eyelid pruritus, presence of secretion in the eye, scabs on the eyelid edges, increased tearing, cardiovascular collapse a, bradycardia, palpitations, shortness of breath, nosebleeds, mouth and throat pain, laryngeal and pharyngeal pain, throat irritation, cough associated with upper respiratory tract, runny nose, sneezing, oesophagitis, diarrhea, nausea, vomiting, indigestion, pain in the epigastrium, epigastric discomfort, discomfort in the stomach, flatulence, frequent movements of the large intestine, stomach and intestinal disease, impaired sensation in the mouth, paresthesia in the mouth, dry mouth, rash, maculopapular rash, feeling of skin tightening, back pain, muscle cramps, muscle aches, kidney pain, erectile dysfunction, pain, chest discomfort, fatigue, unusual well-being, feeling of the presence of a foreign body in the eye. Rare: insomnia, memory impairment, drowsiness, corneal edema, double vision, reduced visual acuity, photopsy, impaired sensation in the eye, periorbital edema, increased intraocular pressure, increased proportion of the size of the cavity to the size of the optic disc, tinnitus, angina pectoris, irregular heart action, airway hyperresponsiveness, upper respiratory tract stasis, sinus congestion, rhinitis, cough, dry nose, urticaria, baldness, generalized pruritus, chest pain, nervousness, weakness, irritability. Not known: rhinitis, hypersensitivity, decreased appetite, tremor, impaired sensation, lack of taste, corneal disease, blurred vision, eye allergy, eyelash loss, eyelid disease, eyelid edema, dizziness, arrhythmias, tachycardia, hypertension, increased blood pressure , low blood pressure, increased heart rate, asthma, abnormal liver function tests, dermatitis, erythema, arthralgia, pain in the extremities, pollakiuria, peripheral edema, malaise.The use of systemic carbonic anhydrase inhibitors generally involves gastro-intestinal, nervous, hematopoietic, renal and metabolic disorders. Local adverse reactions of the same type may occur with topical carbonic anhydrase inhibitors, such as those involving oral carbonic anhydrase inhibitors. There were no unexpected adverse reactions when used in the adjunctive therapy of travoprost. Adverse reactions observed in such combination therapy were the same as when each of the active substances was used alone. In pediatric patients, the majority of adverse reactions were local, non-severe adverse reactions from the eye, such as conjunctival hyperemia, eye irritation, discharge from the eye, increased tearing.

Adults in monotherapy and in combination: 1 drop into the conjunctival sac of the affected eye (eyes) twice a day. In some patients, a better response is obtained by administering the formulation three times a day. Elderly, dose adjustment is not necessary. After instillation, it is recommended to compress the nasal-lacrimal canal or gentle closing of the eyelids. In case of the replacement of another anti-glaucoma drug with the preparation, the previously used medicine should be discontinued and the preparation should be started the Next day. If the patient uses more than one eye medicine, each of these medicines should be given at least 5 minutes apart. Eye Ointment should be used at the end. If a dose is missed, treatment should continue with the next dose as planned. The dose may not exceed 1 droplet administered to the affected eye (eyes) 3 times a day.