Spironolactone
Specification
Pharmaceutical form
Spironolactone 50 mg Tablets. There are 25 tablets in a blister. 4 blisters are packed in a cardboard box together with an enclosed leaflet.
Active ingredient
Spironolactone 50 mg
Pharmacotherapeutic group
Diuretic potassium-sparing agent.
Addison's disease, hyperkalemia, hypercalcemia, hyponatremia, chronic renal failure, anuria, hepatic failure, diabetes mellitus with confirmed or suspected chronic renal failure, diabetic nephropathy, I trimester of pregnancy, metabolic acidosis, menstrual irregularity or breast enlargement, hypersensitivity.
Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.
Structure
Active ingredient: Spironolactone 50 mg. Excipients: microcrystalline cellulose 102, calcium stearate, aerosil ® 200 (hydrophilic pyrogenic silicon dioxide).
Pharmacological properties
Spironolactone is a potassium-sparing diuretic, a specific long-acting aldosterone antagonist ( mineralocorticosteroid hormone of the adrenal cortex). In the distal nephron, Spironolactone prevents sodium and water retention by aldosterone and suppresses the potassium-excreting effect of aldosterone. By binding to aldosterone receptors, it increases the excretion of sodium, chlorine and water ions in the urine, reduces the excretion of potassium and urea ions, and reduces urine acidity.
The maximum effect is observed 7 hours after ingestion and lasts at least 24 hours. The hypotensive effect of the drug is due to the presence of a diuretic effect, which is variable: the diuretic effect appears on days 2-5 of treatment.
Spironolactone is well absorbed after oral administration and is mainly metabolized into active metabolites: sulfur-containing metabolites (80%) and partially canrenone (20%). The plasma half-life of Spironolactone is short (1.3 hours), the half-life of active metabolites is longer (from 2.8 to 11.2 hours). Excretion of metabolites occurs mainly through the urine, a small part is excreted in the feces. Spironolactone and its metabolites cross the placenta and ekskre tiruyutsya breast milk.
After administration of 100 mg of Spironolactone per day for 15 days on an non-fasting basis in healthy volunteers, Tmax was reached in 2.6 hours, Cmax was approximately 80ng / ml and Ti / 2 was approximately 1.4 hours. For 7-alpha- ( thiomethyl ) spironolactone and canrenone - Tmax 3.2 hours and 4.3 hours, Cmax was 391ng / ml and 181ng / ml and T1 / 213.8 hours aca and 16.5 hours, respectively. The effect on the kidneys of a single dose of Spironolactone reaches its peak after 7 hours and the activity persists for at least 24 hours.
Indications for use
Edema in chronic heart failure, cirrhosis of the liver (especially with the simultaneous presence of hypokalemia and hyperaldosteronism ), with nephrotic syndrome. Edema in the II and III trimesters of pregnancy. Arterial hypertension, incl. with aldosterone-producing adrenal adenoma (as part of combination therapy). Primary hyperaldosteronism. Aldosterone- producing adrenal adenoma (long-term maintenance therapy in case of contraindication to surgical treatment or in case of refusal). Di agnostic hyperaldosteronism. Hypokalemia and its prevention in the treatment of saluretics. Polycystic ovary syndrome, premenstrual syndrome.
Method of administration and dosage
Set individually depending on the severity of violations of water and electrolyte metabolism and hormonal status. With edematous syndrome - 100-200 mg / day (less often - 300 mg / day ) in 2-3 doses (usually in combination with a "loop" or / and thiazide diuretic) daily for 14-21 days. Dose adjustments should be made taking into account the values of the plasma potassium concentration. If necessary, courses are repeated every 10-14 days. With pronounced hyperaldosteronism and reduced potassium content in plasma - 300 mg / day in 2-3 doses.
Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.
Structure
Active ingredient: Spironolactone 50 mg.
Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.
Structure
Active ingredient: Spironolactone 50 mg.
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