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Pharmacological action of Diamox
A diuretic with a mild diuretic effect. Inhibits the enzyme carbonic anhydrase in the proximal convoluted tubule of the nephron. Increases urinary excretion of sodium, potassium, bicarbonate ions, does not affect the excretion of chlorine ions; causes an increase in urine pH. With prolonged and / or frequent use, it can cause metabolic acidosis. Reduces intraocular pressure. Reduces the production of cerebrospinal fluid.
After oral administration, acetazolamide is well absorbed from the gastrointestinal tract. After taking in a dose of 500 mg, Cmax of the active substance is 12-27 μg / ml and is reached after 1-3 hours. The determined concentration of acetazolamide in plasma is maintained for 24 hours after administration. It is distributed mainly in erythrocytes, kidneys, muscles, tissues of the eyeball and the central nervous system. Binds to plasma proteins to a high degree. Penetrates the placental barrier.
Acetazolamide is not biotransformed in the body. It is excreted by the kidneys unchanged. About 90% of the dose is excreted in the urine within 24 hours.
Indications of the active substances of the drug Acetazolamide
Edema syndrome, especially in combination with alkalosis, with chronic heart and cardiopulmonary failure (as part of complex therapy); increased intracranial pressure; primary and secondary glaucoma, acute attack of glaucoma; minor epileptic seizures.
Dosing regimen of Diamox
For edematous syndrome - 250 mg 1-2 times / day in courses of 2-4 days, with intervals of several days. With epilepsy - 250 mg 3-4 times / day. With an attack of glaucoma - the initial dose is 250-500 mg; then every 6 hours, 250 mg. Then the dose is gradually reduced. In children, the dose is adjusted according to age.
Contraindications for use
Acute renal failure, severe liver dysfunction, hypokalemia, metabolic acidosis, hypocorticism, diabetes mellitus, I trimester of pregnancy.
Application during pregnancy and lactation
Acetazolamide is contraindicated in the first trimester, in the second and third trimesters, it is used with caution and only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Acetazolamide in a small amount is excreted in breast milk, therefore, if necessary, use during lactation, breastfeeding should be discontinued.
Application for violations of liver function
Contraindicated: severe violations of liver function,
Application for impaired renal function
Contraindicated: acute renal failure. Use with caution in patients with impaired renal function.
Use in elderly patients
Use with caution in elderly patients.
Acetazolamide should not be used for more than 5 days in a row because of the increased risk of metabolic acidosis.
Use with caution in elderly patients and / or patients with impaired renal function due to an increased risk of metabolic acidosis. Acetazolamide can increase the manifestations of osteomalacia caused by anticonvulsants, increase the risk of toxic effects of salicylates, digitalis drugs, carbamazepine, ephedrine, non-depolarizing muscle relaxants. At the same time, acetazolamide increases the clinical efficacy of insulin and oral hypoglycemic agents.
When used simultaneously with anticholinesterase drugs, muscle weakness increases in patients with myasthenia gravis.
With simultaneous use, the risk of developing the toxic effects of salicylates, digitalis drugs, carbamazepine, ephedrine, non-depolarizing muscle relaxants increases.
With simultaneous use with diuretics, theophylline potentiates the diuretic effect.
With simultaneous use with lithium preparations, it is possible to increase the excretion of lithium in the urine. A case of the development of lithium intoxication (with a significant increase in its concentration in the blood plasma) after acetazolamide therapy for 1 month is described.
Ammonium chloride causes acidosis and weakens the action of acetazolamide (should not be used simultaneously).
With simultaneous use with acetazolamide, the clinical efficacy of insulin, oral hypoglycemic agents, increases.
With simultaneous use with primidone, a decrease in the concentration of primidone in the blood serum, a decrease in its anticonvulsant effect, severe osteomalacia is possible; with phenytoin, phenobarbital - severe osteomalacia.
There are reports that with the simultaneous use of a significant and rapid increase in the concentration of cyclosporine in the blood plasma, which may be accompanied by toxic effects on the kidneys.
Possible: hypokalemia, muscle weakness, convulsions, redness of the skin, lack of appetite, metabolic acidosis, itching.
With long-term administration , cases of nephrolithiasis, transient hematuria and glucosuria, hemolytic anemia, leukopenia, agranulocytosis, paresthesias, and disorientation have been described.