Acetazolamide

A diuretic from the group of carbonic anhydrase inhibitors . It causes diuresis by removing certain electrolytes , in quantitative terms not violating a significant degree of electrolyte balance in the body . The mechanism of this action is to inhibit the function of the carbonic anhydrase enzyme, which plays a serious role in the transport of ions and preserves the ionic balance of the organism. Inhibits carbonic anhydrase in the proximal convoluted nephron tubule, increases the excretion of Na ⁺ , K ⁺ , bicarbonate with urine , does not affect the excretion of Cl ^- , alkalizes urine . Violates acid-base balance (metabolic acidosis ). Inhibition of carbonic anhydrase ciliary body leads to a decrease in the secretion of aqueous humor and lower intraocular pressure . Suppression of carbonic anhydrase in the brain causes the anticonvulsant activity of the drug. Reduces the formation of cerebrospinal fluid and intracranial pressure . Duration of action - up to 12 hours.

Absorption - high, C _max in the blood - 2 hours after administration at a dose of 500 mg. It penetrates the placental barrier . Communication with plasma proteins is high. Excreted by the kidneys in unchanged form.

Edematous syndrome (mild and moderate severity, in combination with alkalosis ). Brain hypertension ; glaucoma (primary and secondary, acute attack), epilepsy (minor epileptic seizures in children, rare abscesses ), mountain sickness , Meniere's disease , tetany , premenstrual syndrome , gout .

Hypersensitivity , acute renal failure , liver failure , hypokalemia , acidosis , hypocorticism , Addison's disease , uremia , diabetes mellitus , pregnancy (I term).

Be careful

Swelling of the liver and kidney genesis .

Inside When edematous syndrome - 250 mg 1-2 times a day in courses for 5 days, followed by a two-day break. With epilepsy - 250-500 mg / day in one dose for 3 days, on the 4th day of a break. With an attack of glaucoma, the initial dose is 250-500 mg; then every 6 hours at 250 mg, after 1-2 days, the frequency of administration is first reduced to 3, then 2 times per day. Children 4-12 months - 50 mg / day in 1-2 doses; 3-5 years - 50-125 mg / day in 1-2 doses; 4-18 years old - 125-250 mg once in the morning. In chronic glaucoma, 125-250 mg 1-3 times every other day for 5 days. For glaucoma treatment, an ophthalmic solution containing acetazolamide, solubilized in an aqueous medium in the presence of hydroxypropyl-beta-cyclodextrin and a water-soluble stabilizing polymer, is proposed. For prolonged action using a 0.2-0.3% solution of hydroxyethylcellulose and methylcellulose. Beta-blockers are administered as an additional active substance. ^[2]

Hypokalemia , myasthenia gravis , convulsions , skin flushing , paresthesia , tinnitus, loss of appetite , metabolic acidosis , pruritus. With prolonged use - nephrourolithiasis , hematuria , glycosuria , hemolytic anemia , leukopenia , agranulocytosis , disorientation, violation of touch, drowsiness, nausea , vomiting , diarrhea , allergic reactions , paresthesia.

In case of appointment for more than 5 days, the risk of developing metabolic acidosis is high. With prolonged use should be monitored water and electrolyte balance, a picture of peripheral blood, acid-base state.

Strengthens manifestations of osteomalacia caused by taking antiepileptic drugs. Other diuretics and theophylline increase the severity of the diuretic action of acetazolamide, acid-forming diuretics weaken. GCS increases the risk of hypokalemia. Increases toxicity of salicylates, digitalis preparations, carbamazepine , ephedrine and non-polarizing muscle relaxants .

• Mashkovsky M. D. Medicinal products. - 15th ed. - M .: New Wave, 2005. - p. 505-506. - 1200 s. - ISBN 5-7864-0203-7 .