Index of drugs

Treatment of chronic systolic heart failure (group III-IV NYHA) as a supplement to standard treatment. Treatment of oedemas caused by nephrotic syndrome, when other treatments for edema have failed, especially in the case of suspected hyperaldosteronism. Treatment of ascites and edema associated with decompensated liver cirrhosis or portal hypertension and other liver diseases when other treatments for edema have failed, especially if hyperaldosteronism is suspected. In the treatment of hypertension as an add-on to patients not responding adequately to other antihypertensive agents. Primary hyperaldosteronism.

1 tabl powl. contains 25 mg, 50 mg or 100 mg spironolactone. The drug contains lactose.

Spironolactone is a competitive aldosterone receptor blocker; it binds competitively to the receptors in the distal kidney channels, preventing the synthesis of the key protein for the transport of K ions⁺ and Na⁺. Spironolactone exerts a diuretic and potassium-sparing effect, increases the excretion of sodium and water, while retaining potassium and magnesium. Spironolactone also inhibits the adrenal cortex of aldosterone biosynthesis in patients with primary aldosteronism. The effect of spironolactone depends on aldosterone: the higher the concentration of aldosterone in the body, the more effective the response to spironolactone. Spironolactone is well absorbed (70-80%) from the digestive tract. Its bioavailability is higher after a meal than on an empty stomach, ranging from 25 to 70%. The maximum concentration is reached on average within 1-2 h after administration. The volume of distribution of spironolactone is 14.4 l / kg, the degree of binding to proteins exceeds 90% and the clearance is 100 ml / kg / min. T_0,5 in the elimination phase, spironolactone is 1.3-2 h. Spironolactone is largely a first-pass effect. Spironolactone is metabolised to canrenone, 7-α-thiomethyl-spironolactone and other, partially active metabolites. T_0,5 in the phase of elimination it is approximately 15 h for these metabolites, which significantly extends the duration of action of the drug. Spironolactone is mainly excreted in the urine and also to some extent in the faeces (in the bile), mainly in the form of metabolites. The full diuretic effect of spironolactone is usually obtained within 2-3 days of starting treatment. The diuretic effect lasts for 2-3 days after the end of treatment. In the elderly, the clearance of spironolactone may decrease and T_0,5 it may be prolonged.

Hypersensitivity to spironolactone or to any of the excipients. Hyperkalemia. Hyponatremia. Adrenal crisis. acute and chronic renal failure, creatinine clearance less than 30 ml / min. Anuria. Porphyria.

Particular care should be taken when treating patients with diabetes with renal impairment. Caution is advised during the treatment of ascites and the patient's weight should not be reduced by more than 1 kg per day (due to increased diuresis). In patients with peptic ulcers, spironolactone may delay ulcer healing, so it should only be used after careful consideration. In experimental animals, spironolactone caused or stimulated tumor growth, hence this should be taken into account; this effect may be due to hormonal changes that spironolactone also causes in humans. In patients with cirrhosis, hypochloremic metabolic acidosis with hyperkalemia has been reported during treatment with spironolactone, despite normal renal function. Patients with cirrhosis and other patients at risk of acidosis should be closely monitored. The risk of hyperkalemia is higher in the elderly and in patients with renal or hepatic impairment, as well as in the combined use of spironolactone and ACE inhibitors or angiotensin II receptor antagonists or potassium-sparing diuretics; these patients should be carefully monitored for serum potassium.Hyperkalemia may lead to death - monitoring of serum potassium in patients with chronic heart failure receiving spironolactone is essential. The use of other potassium-sparing diuretics should be avoided. The use of oral potassium supplements should be avoided in patients with serum potassium> 3.5 mmol / l. It is recommended to determine potassium and creatinine concentrations one week after the start of treatment or to increase the dose of spironolactone, every month for the first three months, every three months for one year and then every six months. Treatment with serum potassium> 5 mmol / l or creatinine> 220 micromol / l should be discontinued or discontinued. It is not recommended to use potassium supplements, potassium substitutes containing potassium or a potassium-rich diet because of the risk of hyperkalemia. When using the drug, serum electrolytes and renal function should be monitored regularly. The drug contains lactose - patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose should not use this drug.

Avoid using the drug during pregnancy. In studies in rats, spironolactone caused males to acquire female features. The active metabolite of spironolactone, canrenone, passes into breast milk in small amounts. A decision should be made whether to stop breastfeeding or to interrupt and / or suspend treatment, taking into account the benefits of breastfeeding for the child and the benefits of therapy for the mother.

Common: headache, gastrointestinal disturbances, nausea, diarrhea, vomiting, dry skin, gynecomastia, breast tenderness, menstrual disorders, impotence, drowsiness. Uncommon: electrolyte imbalance (hyperkalemia, hyponatremia), confusion, paresthesia, rash, pruritus, urticaria, muscle cramps, increased serum creatinine, increased renin concentration. Rare: thrombocytopenia, leukopenia, agranulocytosis, dehydration, apathy, changes in libido, dizziness, acute renal failure. Very rare: benign breast tumors, liver dysfunction, alopecia, hypertrichosis.

Orally.Adults. Chronic heart failure (NYHA class III to IV): the initial dose in patients with severe heart failure (NYHA III to IV) and potassium ≤5 mmol / l and serum creatinine ≤220 μmol / l is usually 25 mg / day, in combination with standard treatment. If fluid retention builds up or persists for 8 weeks after starting treatment and potassium levels continue to be <5 mmol / L, the dose of spironolactone may be increased to 50 mg once a day. Potassium and creatinine levels must be tested after one week of this dose. If the potassium level rises to 5.5 mmol / l or the creatinine concentration rises to 220 μmol / l, the dose of spironolactone must be reduced to 25 mg every other day or the drug should be discontinued.edemaThe usual dose is 25 mg to 100 mg a day. In severe cases, the dose can be increased to 200 mg a day. In the case of significant edema, e.g. in the course of liver cirrhosis, short-term administration of 200 to 400 mg per day may be indicated.Treatment of hypertensionThe usual dose is 50 to 100 mg a day. The full therapeutic effect is usually achieved within approximately 2 weeks, which should be taken into consideration when changing the dose.Treatment of primary hyperaldosteronism: 100 to 400 mg a day before surgery. If the surgery is not performed, the dose should be reduced to the lowest effective dose.Children: the starting dose is 3 mg / kg / day; long-term treatment in combination with other diuretics: 1 to 2 mg / kg / day. Caution should be exercised when using spironolactone in patients with moderate renal insufficiency (creatinine clearance 30 to 50 ml / min) and the drug should not be used in patients with severe renal impairment.
Table. should be taken with a meal (for better absorption).