Spironolactone (Spironolactone)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSpironolactoneSpironolactone
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    • Dosage form: & nbspTabletki.
    Composition:For one tablet:

    Active substance: spironolactone

    25.0 mg

    Excipients:


    Lactose monohydrate (milk sugar)

    117.0 mg

    Corn starch

    50.0 mg

    Povidone-K25

    5.0 mg

    Silica colloidal dioxide

    1.0 mg

    Magnesium stearate

    2.0 mg
    Description:

    Round, flat-cylindrical tablets white or white with a yellowish shade of color, with a risk on one side and a facet on both sides, with a characteristic odor.

    Pharmacotherapeutic group:diuretic potassium-sparing agent
    ATX: & nbsp

    C.03.D.A   Aldosterone antagonists

    C.03.D.A.01   Spironolactone

    Pharmacodynamics:

    A potassium-sparing diuretic, whose action is due to the antagonism of aldosterone (mineralocorticosteroid hormone of the adrenal cortex). Aldosterone promotes the inverse absorption of sodium ions in the renal tubules and enhances the excretion of potassium ions. Spironolactone - Competitive antagonist of aldosterone on the effect on the distal nephron (competes for binding sites on cytoplasmic protein receptors, reduces the synthesis of permeases in the aldosterone-dependent region of collecting ducts and distal tubules), increases the excretion of sodium, chlorine and water ions and reduces the elimination of potassium and urea ions, reduces acidity of urine. Strengthening diuresis causes an antihypertensive effect, which is unstable.

    Diuretic effect is manifested on the 2nd-5th day of treatment.

    Pharmacokinetics:

    When ingested quickly and completely absorbed from the gastrointestinal tract. Bioavailability is 100%. The maximum concentration for daily intake of 100 mg for 15 days is 80 ng / mg, the time required to reach the maximum concentration after the next morning intake is 2.6 hours. After absorption, it is metabolized in the liver to several activesulfur-containing metabolites (80%), including canrenone (20%), the maximum concentration of which is determined 2-4 hours after ingestion. Communication with blood plasma proteins - 98% (canrenone - 90%). Poor penetration of organs and tissues, but penetrates the placental barrier, and canrenone - into breast milk. The volume of distribution is 0.05 l / kg.

    It is excreted by the kidneys (50% - in the form of metabolites, 10% - unchanged), in part - through the intestine. The excretion of canrenone (mainly by the kidneys) is biphasic, the half-life in the first phase is 2-3 hours, in the second - 12-96 hours.

    With cirrhosis of the liver and chronic heart failure, the elimination half-life increases without signs of cumulation (its probability increases with chronic renal failure and hyperkalemia). The half-life is 13-24 hours.

    Indications:

    - Essential hypertension (as part of combination therapy);

    - edematous syndrome with chronic heart failure (can be used in monotherapy and as part of combination therapy);

    - conditions in which secondary hyperaldosteronism can be detected, including cirrhosis accompanied by ascites and / or edema, nephrotic syndrome, and other conditions accompanied by edema;

    - hypokalemia / hypomagnesemia (as an aid for its prevention during treatment with diuretics if other methods of correction of potassium content are not possible);

    - primary hyperaldosteronism (Conn's syndrome) - for a short preoperative course of treatment;

    - to establish the diagnosis of primary hyperaldosteronism;

    - severe chronic heart failure (III-IV functional class on classification of NYHA) on the background of standard therapy.

    Contraindications:

    - Hypersensitivity to spironolactone and any of the components of the drug.

    - Addison's disease;

    - hyperkalemia;

    - hyponatremia;

    - severe renal failure (creatinine clearance less than 10 ml / min);

    - anuria;

    - lactose deficiency, lactase intolerance, glucose-galactose malabsorption syndrome;

    - pregnancy;

    - lactation period (breastfeeding);

    - Children under 3 years of age (solid dosage form);

    - simultaneous use of eplerenone and other potassium-sparing diuretics, potassium preparations (risk of hyperkalemia).

    Carefully:

    Atrioventricular block (possibility of amplification due to the development of hyperkalemia); diabetes(with confirmed or suspected chronic renal failure); diabetic nephropathy; dysmenorrhea; hypercalcemia; metabolic acidosis; hepatic failure, cirrhosis; surgical interventions; gynecomastia and simultaneous use of drugs that cause gynecomastia; local and general anesthesia; elderly age.

    Pregnancy and lactation:

    The use of the drug during pregnancy and during breastfeeding is contraindicated.

    If it is necessary to use lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Inside. Simultaneously with the reception of food.

    With essential hypertension:

    The daily dose for adults is usually 50-100 mg once and may be increased to 200 mg, while increasing the dose should be gradual, 1 time in 2 weeks. To achieve an adequate response to therapy, the drug should be taken at least 2 weeks. If necessary, adjust the dose.

    With idiopathic hyperaldosteronism:

    100-400 mg / day.

    With pronounced hyperaldosteronism and hypokalemia:

    The daily dose is 300 mg / day (maximum 400 mg) for 2-3 doses, with the improvement of the condition, the dose is gradually reduced to 25 mg / day.

    With hypokalemia and / or hypomagnesemia caused by diuretic therapy:

    Assign the drug in a dose of 25-100 mg / day once or in several ways. The maximum daily dose of 400 mg, if potassium preparations for oral administration or other methods of replenishing its deficiency are ineffective.

    In the diagnosis and treatment of primary hyperaldosteronism as a diagnostic tool in a short diagnostic test:

    The drug is prescribed for 4 days at 400 mg / day, distributing the daily dose for several doses per day. With an increase in the potassium content in the blood at the time of taking the drug and decreasing after its withdrawal, it can be assumed that there is a primary hyperaldosteronism.

    With a long diagnostic test:

    The drug is given in the same dose for 3-4 weeks. When the correction of hypokalemia and arterial hypertension is achieved, it is possible to assume the presence of primary hyperaldosteronism.

    Short course of preoperative therapy of primary hyperaldosteronism:

    After the diagnosis of hyperaldosteronism is established using more accurate diagnostic methods, Spironolactone should be taken at 100-400 mg / day.dividing by 1-4 doses per day during the entire period of preparation for surgery. If the operation is not shown, then Spironolactone is used for long-term maintenance therapy, with the lowest effective dose that is selected individually for each patient.

    Edema on the background of nephrotic syndrome:

    The daily dose for adults is usually 100-200 mg. The effect of spironolactone on the main pathological process was not revealed, and therefore the use of this drug is recommended only in cases when other types of therapy are ineffective.

    With edematous syndrome in the background of chronic heart failure:

    The drug is prescribed daily, for 5 days to 100-200 mg / day in 2-3 doses.

    Depending on the effect, the daily dose is reduced to 25 mg. The maintenance dose is selected individually. The maximum dose of 200 mg / day.

    Edema on the background of liver cirrhosis:

    If in urine the ratio of sodium and potassium ions (Na+/K+) exceed 1.0, the daily dose for adults is usually 100 mg. If the ratio is less than 1.0, the daily dose for adults is usually 200-400 mg.The maintenance dose is selected individually.

    When swelling in children:

    The initial dose is 1-3.3 mg / kg body weight or 30-90 mg / m2/ day. in 1-4 reception. After 5 days, the dose is adjusted and, if necessary, increased 3 times as compared with the original dose.

    Application in elderly patients:

    It is recommended to start treatment with a minimal dose and titrate it until the maximum dose necessary under the control of liver / kidney function.

    Severe chronic heart failure (III-IV functional class by classification NYHA) on the background of standard therapy:

    Treatment begins with 25 mg once a day, if serum potassium is less than 5.0 meq / L and blood creatinine is less than 2.5 mg / L. Patients who tolerate a dose of 25 mg once a day / day may increase the dose to 50 mg once a day. Treatment is carried out under the control of the content of potassium and blood creatinine one week after the start of therapy or increasing the dose, then monthly for the first 3 months, then quarterly for a year, and then every 6 months.

    Side effects:

    From the digestive system: nausea, vomiting, diarrhea, ulceration and bleeding of the gastrointestinal tract, gastritis, intestinal colic, abdominal pain, diarrhea or constipation, impaired liver function.

    From the nervous system: ataxia, retardation, dizziness, headache pain, drowsiness, lethargy, confusion, muscle spasm.

    From the endocrine system: with prolonged use - gynecomastia, erectile dysfunction in men, decreased potency; in women - dysmenorrhea, amenorrhea, metrorrhagia in the climacteric period, hirsutism, hypertrichosis, coarsening of the voice, pains in the region of the mammary glands, breast carcinoma.

    From the urinary system: acute renal failure.

    On the part of the organs of hematopoiesis: agranulocytosis, thrombocytopenia, megaloblastosis.

    Allergic reactions: drug fever, urticaria, maculopapular and erythematous rash, Stevens-Johnson syndrome, toxic epidermal necrolysis.

    From the skin: alopecia, itchy skin.

    From the laboratory indicators: increased urea concentration, Hypercreatinemia, hyperuricemia, disturbance of water-electrolyte metabolism and acid-base state (metabolic hypochloraemic acidosis or alkalosis).

    Other: spasms of the calf muscles, muscle spasm.

    Overdose:

    Symptoms: nausea, vomiting, dizziness, lowering of arterial pressure, diarrhea, skin rash, hyperkalemia (paresthesia, myasthenia gravis, arrhythmias, weakness), hyponatremia (dry mouth, thirst, drowsiness), hypercalcemia, dehydration, increased urea concentration.

    Treatment: gastric lavage, symptomatic therapy of dehydration and arterial hypotension.

    With hyperkalemia it is necessary to normalize water-electrolyte metabolism with the help of potassium-releasing diuretics, rapid parenteral administration of a solution of dextrose (glucose) (5-20% solutions) with insulin from 0.25-0.5 units per 1 g of dextrose (glucose); if necessary, repeated administration of dextrose (glucose). In severe cases, hemodialysis is performed.

    Interaction:

    Reduces the effect of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indanedione) and toxicity of cardiac glycosides (as normalization of the potassium content in the blood prevents the development of toxicity).

    Enhances the metabolism of phenazol (antipyrine).

    Reduces the sensitivity of blood vessels to norepinephrine (requires caution when conducting anesthesia).

    Increases the half-life of digoxin - possible intoxication with digoxin.

    Increases the toxic effect of lithium due to a decrease in its clearance.

    Accelerates the metabolism and excretion of carbenoksolona. Carbenoksolon promotes sodium retention by spironolactone.

    Glucocorticosteroids and diuretics (benzothiazine derivatives, furosemide, ethacrynic acid) intensify and accelerate the diuretic and natriuretic effect.

    Strengthens the action of diuretic and hypotensive drugs.

    Nonsteroidal anti-inflammatory drugs reduce diuretic and natriuretic effects, increases the risk of hyperkalemia.

    Glucocorticosteroid preparations increase the diuretic and natriouric effect in hypoalbuminemia and / or hyponatremia.

    The risk of hyperkalemia increases with admission to potassium, potassium supplements and potassium-sparing diuretics, angiotensin-converting enzyme (acidosis) inhibitors, angiotensin II receptor antagonists, aldosterone blockers, indomethacin, cyclosporine.

    Salicylates, indomethacin reduce the diuretic effect.

    Ammonium chloride, colestramine promote the development of hyperkalemic metabolic acidosis.

    Fludrocortisone causes a paradoxical increase in tubular secretion of potassium. Reduces the effect of mitotane.

    Strengthens the effect of tryptorelin, buserelin, gonadorelin.

    Ethanol, barbiturates, narcotic substances strengthen orthostatic hypotension.
    Special instructions:

    There may be a temporary increase in the concentration of urea nitrogen in the blood serum, especially with reduced kidney function and hyperkalemia. Possible reversible hyperchloremic metabolic acidosis.

    In case of violations of kidney and liver function, as well as in old age, regular monitoring of serum electrolytes and kidney function is necessary.

    The drug makes it difficult to determine digoxin, cortisol and adrenaline in the blood.

    Despite the absence of direct effects on carbohydrate metabolism, the presence of diabetes mellitus, especially with diabetic nephropathy, requires extreme caution because of the possibility of developing hyperkalemia.

    In the treatment of non-steroidal anti-inflammatory drugs, kidney function and blood electrolyte indices should be monitored. Avoid eating foods rich in potassium.

    During treatment, alcohol consumption is contraindicated.

    Effect on the ability to drive transp. cf. and fur:

    In the initial period of treatment it is forbidden to drive vehicles and engage in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions. The duration of restrictions is set individually.

    Form release / dosage:

    Tablets, 25 mg.

    Packaging:

    For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    10, 20, 30, 40, 50 or 100 tablets in cans of polyethylene terephthalate for medicinal products sealed with caps screwed with a first opening control or a "push-turn" system made of polypropylene or polyethylene, or cans of polypropylene for medicinal products sealed with lids with the control of the first opening of high pressure polyethylene.

    One jar or 1, 2, 3, 4 or 5 contour squares, together with the instruction for use, is placed in a cardboard package (bundle).

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003702
    Date of registration:23.06.2016
    Expiration Date:23.06.2021
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspOZONE LLC OZONE LLC Russia
    Information update date: & nbsp16.08.2016
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