Aldactone (Tablets) Instructions for Use

ATC Code

C03DA01 (Spironolactone)

Active Substance

Spironolactone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Potassium-sparing diuretic

Pharmacotherapeutic Group

Potassium-sparing diuretic agent

Pharmacological Action

Potassium- and magnesium-sparing diuretic. It is a competitive antagonist of aldosterone in its effect on the distal parts of the nephron (competes for binding sites on cytoplasmic protein receptors, reduces the synthesis of permeases in the aldosterone-dependent section of the collecting tubules and distal tubules), increases the excretion of Na⁺, Cl^– and water and reduces the excretion of K⁺ and urea, reduces the titratable acidity of urine.

Enhancement of diuresis causes a hypotensive effect, which is inconsistent. The hypotensive effect does not depend on the plasma renin level and does not manifest at normal blood pressure.

The diuretic effect appears on the 2nd-5th day of treatment.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract, absorption is 90%. Metabolized in the liver, the main active metabolite is canrenone.

T_1/2 is 13-24 hours. Excreted mainly by the kidneys, some amount is excreted with bile.

Indications

Edema in chronic heart failure, liver cirrhosis (especially with simultaneous hypokalemia and hyperaldosteronism), in nephrotic syndrome.

Edema in the II and III trimesters of pregnancy.

Arterial hypertension, including in aldosterone-producing adrenal adenoma (as part of combination therapy).

Primary hyperaldosteronism. Aldosterone-producing adrenal adenoma (long-term maintenance therapy when surgical treatment is contraindicated or in case of refusal of it). Diagnosis of hyperaldosteronism.

Hypokalemia and its prevention during treatment with saluretics.

Polycystic ovary syndrome, premenstrual syndrome.

ICD codes

Dosage Regimen

Tablets

The dosage is set individually depending on the severity of water-electrolyte balance disorders and hormonal status.

For edematous syndrome – 100-200 mg/day (less often – 300 mg/day) in 2-3 doses (usually in combination with a “loop” and/or thiazide diuretic) daily for 14-21 days. Dose adjustment should be carried out taking into account plasma potassium concentration values. If necessary, courses are repeated every 10-14 days. For severe hyperaldosteronism and reduced plasma potassium content – 300 mg/day in 2-3 doses.

Adverse Reactions

From the digestive system nausea, vomiting, abdominal pain, gastritis, ulcerations and bleeding in the gastrointestinal tract, intestinal colic, diarrhea or constipation.

From the central nervous system dizziness, drowsiness, lethargy, headache, lethargy, ataxia.

From metabolism increased urea concentration, hypercreatininemia, hyperuricemia, disturbance of water-electrolyte balance and acid-base balance (metabolic hypochloremic acidosis or alkalosis).

From the hematopoietic system megaloblastosis, agranulocytosis, thrombocytopenia.

From the endocrine system with long-term use – gynecomastia, erectile dysfunction in men; in women – dysmenorrhea, amenorrhea, metrorrhagia in the climacteric period, hirsutism, voice coarsening, breast tenderness, breast carcinoma.

Allergic reactions urticaria, maculopapular and erythematous rashes, drug fever, itching.

Other muscle cramps, decreased potency.

Contraindications

Addison’s disease, hyperkalemia, hypercalcemia, hyponatremia, chronic renal failure, anuria, hepatic failure, diabetes mellitus with confirmed or suspected chronic renal failure, diabetic nephropathy, first trimester of pregnancy, metabolic acidosis, menstrual cycle disorders or breast enlargement, hypersensitivity to spironolactone.

Use in Pregnancy and Lactation

There are no data on the negative impact of spironolactone on the course of pregnancy and fetal development. However, use in the first trimester of pregnancy is contraindicated; in the second and third trimesters, use is possible according to indications.

If it is necessary to use during lactation, it should be taken into account that the spironolactone metabolite canrenone is excreted in breast milk in small amounts.

Use in Hepatic Impairment

Contraindicated in hepatic failure. Use with caution in decompensated liver cirrhosis.

Use in Renal Impairment

Contraindicated in chronic renal failure, anuria, diabetic nephropathy.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Use with caution in AV block (possibility of enhancement due to the development of hyperkalemia), decompensated liver cirrhosis, surgical interventions, use of drugs causing gynecomastia, when using local and general anesthetics, in elderly patients.

Against the background of spironolactone use, potassium-containing preparations, as well as other diuretic agents that cause potassium retention in the body, should not be prescribed. The use of spironolactone with carbenoxolone, which causes sodium retention, should be avoided.

During treatment, periodic determination of the content of electrolytes and urea in the blood should be carried out.

When using spironolactone in combination with other diuretic or antihypertensive agents, it is recommended to reduce the dose of the latter. When using spironolactone simultaneously with digoxin, it may be necessary to reduce both the loading and maintenance doses of the latter.

Drug Interactions

With simultaneous use with antihypertensive drugs, the hypotensive effect of spironolactone is potentiated.

With simultaneous use with ACE inhibitors, the development of hyperkalemia is possible (especially in patients with impaired renal function), because ACE inhibitors reduce aldosterone content, which leads to potassium retention in the body against the background of limited potassium excretion.

With simultaneous use with potassium preparations, other potassium-sparing diuretics, salt substitutes and dietary supplements containing potassium, the development of hyperkalemia is possible.

With simultaneous use with salicylates, the diuretic effect of spironolactone is reduced due to blockade of canrenone excretion by the kidneys.

Indomethacin and mefenamic acid inhibit the excretion of canrenone by the kidneys.

With simultaneous use, the hypoprothrombinemic effect of oral anticoagulants is reduced.

With simultaneous use with digitoxin, both enhancement and reduction of digitoxin effects are possible.

With simultaneous use, Spironolactone inhibits the excretion of digoxin by the kidneys and probably reduces its volume of distribution. This can cause an increase in the plasma concentration of digoxin.

With simultaneous use with candesartan, losartan, eprosartan, there is a risk of developing hyperkalemia.

Cases of hypochloremic alkalosis have been described with simultaneous use with cholestyramine.

With simultaneous use with lithium carbonate, an increase in the plasma concentration of lithium is possible.

With simultaneous use with norepinephrine, a decrease in vascular sensitivity to norepinephrine is possible.

With simultaneous use, the action of triptorelin, buserelin, gonadorelin is enhanced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.