Brinzolamid

When ATH:
S01EC04

Characteristic.

Carbonic anhydrase inhibitors. White powder, insoluble in water, soluble in methanol, soluble in ethanol. Molecular weight 383,5.

Pharmacological action.
Protivoglaukomnoe.

Application.

Increased intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Contraindications.

Hypersensitivity.

Restrictions apply.

Childhood (safety and effectiveness in children have not been established).

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of use in pregnant women were not conducted).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Teratogenic effects. In studies brinzolamide toxic effects during pregnancy in rabbits by oral route at doses 1, 3 and 6 mg / kg / day (in 20, 62 and 125 times the recommended human ophthalmic use in the) shows, at a dosage 6 mg/kg/day toxicity to females and an increase in the number of fetal changes is noted. In rats, body weight was reduced by female fetuses, treated during pregnancy brinzolamide inwardly doses 18 mg / kg / day (in 375 times the recommended human dose in the ophthalmic use). Weight loss of the embryos was proportional to the reduction of weight gain in female, thus it did not interfere with the development of organs or tissues. Displaying, that oral administration of the labeled carbon brinzolamide pregnant rats, ¹⁴C-brinzolamide passes through the placenta and is found in fetal tissues and blood.

When administered orally, brinzolamide dose 15 mg / kg / day (in 312 times the recommended human dose in the ophthalmic use) lactating rats observed no effects, In addition to reducing body weight in the offspring. However, the concentration ¹⁴C brinzolamide in milk were below, than the concentrations in the blood and plasma.

Unknown, whether brinzolamide gets into breast milk of nursing women. Considering, Many drugs into breast milk and then, brinzolamide that can cause serious side effects in children, breastfed, nursing mothers should stop breast-feeding or, or use of brinzolamide.

Side effects.

From the nervous system and sensory organs: 5–10% — blurred vision; 1–5% — blepharitis, dermatitis, dry eyes, foreign body sensation in the eye, headache, hyperemia, discharge from the eyes, discomfort in the eyes, keratit, pain and itching in the eyes; less 1% - Conjunctivitis, diplopia, dizziness, asthenopia, keratokonъyunktyvyt, keratopathy, the first signs of blepharitis (the feeling of the eyelids or sticking crust on the edges of eyelids), lacrimation.

From the respiratory system: 1-5% — rhinitis, breathlessness, pharyngitis.

From the digestive tract: 5-10% - bitter, sour or unusual taste in the mouth; less 1% - Diarrhea, dry mouth, dyspepsia, nausea.

Other: less 1% - Allergic reactions, hives, alopecia, chest pain, hypertension, kidney pain.

Cooperation.

There is a chance of increasing the known systemic effects, associated with the inhibition of carbonic anhydrase, patients, receiving carbonic anhydrase inhibitors interior and local (it is not recommended to use both brinzolamide as instillyatsionnoy forms and oral carbonic anhydrase inhibitors).

Overdose.

Data on overdose in humans when applied topically brinzolamide missing. If ingestion may occur following symptoms: electrolyte imbalance, Acidosis, disorders of the nervous system. Treatment: symptomatic, requires monitoring of electrolytes (especially potassium) levels and control the pH value of blood.

Dosing and Administration.

Instillyatsionno. Buried at 1 drop into the conjunctival sac of the affected eye (or eyes) 2 once a day. When using other local ophthalmic means the interval between the instillation should be at least 10-15 minutes.

Precautions.

Brinzolamide is sulfanilamide and though applied topically, subjected to systemic absorption. In this regard, when using brinzolamide eye drops may occur side reactions, characteristic of sulfonamides. Rarely, but there may be deaths due to severe reactions to sulfonamides, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, fulminant gepatonekroz, agranulocytosis, aplastic anemia, etc.. violation of hematopoiesis. Sensitization to sulfonamides may occur with repeated use, regardless of the route of administration. When serious adverse reactions or hypersensitivity manifestation of the use should be discontinued.

In rare cases with oral carbonic anhydrase inhibitors with high doses of salicylates have been reported changes in acid-base and electrolyte balance. Therefore, in the treatment of brinzolamide to consider the possibility of such drug interactions in patients.

The effect of prolonged exposure to brinzolamide on corneal epithelium is not fully appreciated. In patients with acute angle-closure glaucoma in addition to funds, applies when ocular, needed additional therapeutic measures. Application 1% brinzolamide ophthalmic suspension in patients with acute attack of angle-closure glaucoma has not been studied.

Features of use in patients with severe renal impairment (creatinine clearance less than 30 ml / min) not determined. Since brinzolamide (and its metabolite) excreted mainly by the kidney, it is not recommended in this pathology.

In patients with impaired liver function brinzolamide with caution (adequate clinical studies are not conducted).

Caution should be exercised when driving vehicles and operating machinery (due to the possibility of temporary blurred vision after instillation).

Before using the product should be removed contact lenses and wear them no earlier than 15 minutes after instillation.