Spironolactone
Spironolactone: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Spironolactone
ATX code: C03DA01
Active ingredient: spironolactone (Spironolactone)
Manufacturer: Ozone LLC (Russia); Synthesis JSC (Russia); CJSC Pharmaceutical Firm Darnitsa (Ukraine)
Description and photo update: 2019-26-08
Prices in pharmacies: from 43 rubles.
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Spironolactone is a potassium-sparing diuretic drug.
Release form and composition
Dosage form - tablets: flat-cylindrical, from white to white with a cream shade, with a bevel, with a weak specific odor or almost odorless (10 pcs. In blisters, in a cardboard box 1 or 2 packs; 20 pcs. In polymer cans, in a pack of cardboard 1 can).
Composition of 1 tablet:
- active substance: spironolactone - 25 mg;
- additional components: crospovidone (Kollidon CL-M), copovidone (Kollidon VA-64), talc, potato starch, calcium stearate (calcium stearic acid), microcrystalline cellulose.
Pharmacological properties
Pharmacodynamics
Spironolactone is a potassium-sparing diuretic. Its mechanism of action is due to the antagonism of aldosterone, a mineralocorticosteroid hormone of the adrenal cortex, which promotes the reabsorption of sodium ions in the renal tubules and enhances the excretion of potassium ions.
Spironolactone is a competitive antagonist of aldosterone in relation to the effect on the distal parts of the nephron (competes for binding sites on cytoplasmic protein receptors; in the aldosterone-dependent part of the collecting ducts and distal tubules it reduces the synthesis of permeases). Reduces the excretion of urea and potassium ions, reduces the acidity of urine, increases the excretion of water, chlorine and sodium ions. Increased diuresis contributes to the development of a hypotensive effect, which is not permanent.
The diuretic effect of spironolactone develops after 2–5 days of treatment.
Pharmacokinetics
After entering the gastrointestinal tract, spironolactone is rapidly and completely absorbed. The bioavailability of the drug is 100%.
With a daily dose of 100 mg for 15 days, the maximum concentration of the substance (C max) is 80 ng / mg. C max after the next morning intake reaches within 2.6 hours.
It is metabolized in the liver. As a result of biotransformation, several active sulfur-containing metabolites (80%) are formed, including canrenone (20%) - its C max is determined 2–4 hours after taking Spironolactone.
Plasma proteins bind 98% (canrenone - 90%). Poorly penetrates tissues and organs. The volume of distribution is 0.05 l / kg. Spironolactone crosses the placental barrier, canrenone - into breast milk.
It is excreted from the body mainly by the kidneys (in the form of metabolites - 50%, unchanged - 10%), partly through the intestines. The half-life (T 1/2) is 13-24 hours. Canrenon is excreted in two phases, T 1/2 in the first - 2-3 hours, in the second - 12-96 hours.
T 1/2 increases with chronic heart failure and liver cirrhosis. There are no signs of cumulation of the drug, but the risk increases with chronic renal failure and hyperkalemia.
Indications for use
- edematous syndrome in chronic heart failure;
- essential hypertension (as part of combination therapy);
- hypokalemia / hypomagnesemia (for prophylaxis as an adjuvant while taking diuretics if it is impossible to use other methods of correcting potassium levels);
- primary hyperaldosteronism (Connes syndrome) - for diagnosis, as well as for a short preoperative course of treatment;
- nephrotic syndrome, cirrhosis of the liver, accompanied by edema and / or ascites, as well as other conditions accompanied by edema, in which secondary hyperaldosteronism can be detected.
Contraindications
- severe chronic renal failure (creatinine clearance less than 10 ml / minute);
- hyponatremia;
- hyperkalemia;
- anuria;
- Addison's disease;
- lactase intolerance, lactose deficiency, glucose-galactose malabsorption syndrome;
- pregnancy;
- children under 3 years old;
- lactation period;
- hypersensitivity to the components of Spironolactone.
Carefully:
- metabolic acidosis;
- hypercalcemia;
- liver failure;
- diabetes mellitus with confirmed or suspected chronic renal failure;
- diabetic nephropathy;
- atrioventricular block;
- gynecomastia or the simultaneous use of drugs that cause gynecomastia;
- dysmenorrhea;
- local and general anesthesia;
- surgical interventions;
- elderly age.
Instructions for the use of Spironolactone: method and dosage
Spironolactone tablets should be taken orally.
Recommended dosing regimens for adults:
- edematous syndrome due to chronic heart failure: 100-200 mg per day for 2-3 doses for 5 days in combination with thiazide or loop diuretics. The maintenance daily dose is selected individually: minimum - 25 mg, maximum - 200 mg;
- Essential hypertension: 50-100 mg 1 time per day, if necessary, the dose is gradually increased (1 time in 2 weeks) to 200 mg. An adequate response to therapy is usually noted after 2 weeks;
- hypokalemia and hypomagnesemia caused by the use of diuretics: 25-100 mg per day in one or more doses. If oral potassium preparations or other methods of making up for its deficiency are ineffective, the daily dose can be increased to the maximum allowable - 400 mg;
- edema due to nephrotic syndrome (in case of ineffectiveness of other types of therapy): 100-200 mg;
- edema due to liver cirrhosis: if the ratio of sodium and potassium ions in urine exceeds 1 - 100 mg per day, if less than 1 - 200-400 mg. The maintenance dose is selected individually;
- idiopathic hyperaldosteronism: 100-400 mg per day;
- severe hyperaldosteronism and hypokalemia: 300-400 mg per day for 2-3 doses. After improving the condition, the daily dose is gradually reduced to a maintenance dose of 25 mg.
Children with edema are prescribed 1–3.3 mg / kg of body weight (30–90 mg / m 2) per day for 1–4 doses. After 5 days, the dose is adjusted. If necessary, it can be increased by 3 times compared to the initial one.
The use of Spironolactone for the diagnosis of hyperaldosteronism:
- short diagnostic test: 400 mg per day (in several doses) for 4 days. If the concentration of potassium increased while taking the drug, and then decreased after its withdrawal, we can assume the presence of primary hyperaldosteronism;
- long-term diagnostic test: 400 mg per day (in several doses) for 3-4 weeks. If during this period it is possible to correct hypokalemia and arterial hypertension, one can assume the presence of primary hyperaldosteronism.
After establishing the diagnosis "primary hyperaldosteronism" with the help of more accurate diagnostic methods, Spironolactone is prescribed for a short course of preoperative therapy - 100-400 mg per day (for 1-4 doses) during the entire preparatory period. If the operation is not indicated, then the drug is used for long-term maintenance therapy in the lowest effective dose, which the doctor selects individually for each patient.
Side effects
- digestive system: diarrhea or constipation, abdominal pain, intestinal colic, gastritis, nausea, vomiting, liver dysfunction, ulceration and bleeding in the gastrointestinal tract;
- endocrine system: with prolonged use in men - erectile dysfunction, decreased potency, gynecomastia; in women - coarsening of the voice, hirsutism, hypertrichosis, breast tenderness, amenorrhea, dysmenorrhea, metrorrhagia in the climacteric period, breast carcinoma;
- urinary system: hyperuricemia, hypercreatininemia, increased urea concentration, acute renal failure;
- nervous system: headache, ataxia, drowsiness, lethargy, dizziness, confusion, muscle spasms, lethargy;
- hematopoietic organs: agranulocytosis, megaloblastosis, thrombocytopenia;
- metabolism: violation of the acid-base state and water-electrolyte metabolism (metabolic hypochloremic acidosis or alkalosis);
- dermatological and allergic reactions: alopecia, urticaria, pruritus, drug fever, erythematous and maculopapular rash;
- others: muscle spasms, cramps of the calf muscles.
Overdose
Symptoms: diarrhea, nausea, vomiting, dehydration, hypercalcemia, hyponatremia (thirst, dry mouth, drowsiness), hyperkalemia (weakness, myasthenia gravis, paresthesia, arrhythmias), increased urea concentration, decreased blood pressure, dizziness, skin rash.
Gastric lavage is recommended. Therapy for arterial hypotension and dehydration is symptomatic. In the case of hyperkalemia, the normalization of water-electrolyte metabolism with potassium-excreting diuretics, rapid parenteral administration of a 5–20% dextrose solution (glucose) with insulin at the rate of 0.25–0.5 U per 1 g of dextrose (glucose) is shown. If necessary, dextrose (glucose) is re-injected. In cases of severe intoxication, hemodialysis is performed.
special instructions
Although Spironolactone has no direct effect on carbohydrate metabolism, due to the risk of hyperkalemia, it should be used with caution in diabetes mellitus, especially when accompanied by diabetic nephropathy.
Elderly people, patients with liver and kidney disease, as well as patients who simultaneously receive nonsteroidal anti-inflammatory drugs, require regular monitoring of kidney function and serum electrolytes.
During treatment, it is recommended to exclude foods rich in potassium from the diet; alcohol is prohibited.
Spironolactone makes it difficult to detect adrenaline, digoxin and cortisol in the blood.
Influence on the ability to drive vehicles and complex mechanisms
At the beginning of treatment, one should refrain from driving and performing potentially hazardous types of work that require high concentration of attention and reaction speed. Further, the degree of restrictions is determined individually.
Application during pregnancy and lactation
There are no data confirming the negative effect of Spironolactone on fetal development. Nevertheless, in the first trimester of pregnancy, the drug is contraindicated, in the second and third trimesters it can be used as directed by a doctor, under his close supervision.
The metabolite of spironolactone (canrenone) is excreted in the mother's milk, so breastfeeding should be discontinued if therapy during lactation is clinically justified.
Pediatric use
According to the instructions, Spironolactone is prohibited for the treatment of children under the age of 3 years (due to the solid dosage form).
With impaired renal function
Spironolactone is contraindicated in severe chronic renal failure (creatinine clearance <10 ml / min).
Patients with renal insufficiency, diabetic nephropathy and anuria should take Spironolactone with caution.
For violations of liver function
In liver failure and liver cirrhosis, Spironolactone should be used with caution.
Use in the elderly
Elderly patients should be treated with caution. At the beginning of therapy, it is recommended to take the minimum dose with its further titration until the required one is reached. In the course of therapy, it is required to monitor the functions of the kidneys and liver.
Drug interactions
The effect of spironolactone on concurrently taken substances / drugs:
- enhances the metabolism of phenazole (antipyrine);
- reduces the effectiveness of indirect anticoagulants (coumarin derivatives, heparin, indandione) and anticoagulants;
- reduces the toxicity of cardiac glycosides (due to the normalization of potassium levels in the blood);
- enhances the effect of buserelin, triptorelin, gonadorelin;
- reduces the sensitivity of blood vessels to norepinephrine (care must be taken when carrying out anesthesia);
- accelerates metabolism and excretion of carbenoxolone;
- increases the half-life of digoxin, as a result of which intoxication is possible;
- reduces the action of mitotane;
- reduces clearance and enhances the toxic effect of lithium;
- enhances the effect of diuretics and antihypertensive drugs.
The effect of other substances / drugs on the action of spironolactone:
- cholestyramine and ammonium chloride: promote the development of hyperkalemic metabolic acidosis;
- glucocorticosteroids: enhance the diuretic and natriuretic effect in hyponatremia and / or hypoalbuminemia;
- indomethacin and salicylates: reduce the diuretic effect;
- fludrocortisone: causes a paradoxical increase in tubular potassium secretion;
- carbenoxolone: promotes sodium retention;
- non-steroidal anti-inflammatory drugs: reduce diuretic and natriuretic effects, increasing the risk of hyperkalemia;
- diuretics (ethacrynic acid, furosemide, benzothiazine derivatives): enhance and accelerate the diuretic and natriuretic effects of Spironolactone;
- cyclosporine, indomethacin, aldosterone blockers, angiotensin II antagonists, potassium preparations, angiotensin-converting enzyme inhibitors, potassium supplements and potassium-sparing diuretics: increase the risk of hyperkalemia.
Analogs
Spironolactone analogs are Veroshpilacton, Veroshpiron, Inspra, Espiro, Eplenor, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry, dark place and out of reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Spironolactone
According to reviews, Spironolactone is an effective and inexpensive diuretic drug. However, it has many contraindications and can cause side effects, so it should be used only as directed by a doctor and under his close supervision.
The price of Spironolactone in pharmacies
Depending on the pharmacy chain, the price of Spironolactone varies from 37 to 76 rubles. per pack of 20 tablets of 25 mg.
Spironolactone: prices in online pharmacies
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Drug name Price Pharmacy |
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Spironolactone 25 mg tablets 20 pcs. 43 rbl. Buy |
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Spironolactone 25 mg tablets 20 pcs. 43 rbl. Buy |
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Spironolactone 25 mg tablets 20 pcs. RUB 70 Buy |
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Spironolactone 50 mg capsule 30 pcs. 144 RUB Buy |
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Spironolactone 100 mg capsules 30 pcs. 204 RUB Buy |
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Spironolactone capsules 100mg 30 pcs. 236 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
