Spironolactone - instructions for use, dose, side effects, contraindications

Auxiliary substances: potato starch - 13.2 mg, copovidone (kollidon VA-64) 3.7 mg, calcium stearate (calcium stearic acid) 1.2 mg, talc 3.6 mg, crospovidone (clolidon CL-M) - 5.4 mg, microcrystalline cellulose - up to 120 mg

Description:Tablets from white to white with a cream shade of color, flat-cylindrical shape with a bevel, almost odorless or with a specific odor

Pharmacotherapeutic group:diuretic potassium-sparing agent

ATX: & nbsp

C.03.D.A Aldosterone antagonists

C.03.D.A.01 Spironolactone

Pharmacodynamics:

Potassium-sparing diuretic, whose action is due to antagonism with 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, a competitive antagonist of aldosterone, influences distal nephron sections (competes for binding sites on cytoplasmic protein receptors, reduces 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 excretion of potassium ions and urea, reduces the acidity of urine. Strengthening diuresis causes an antihypertensive effect, which is unstable. Diuretic effect is manifested on the 2nd-5th day of treatment.

Pharmacokinetics:

Absorption is complete. Bioavailability is 100%. The maximum concentration at a daily intake of 100 mg for 15 days is 80 ng / ml, 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 active sulfur-containing metabolites,including canrenone, the maximum concentration of which is determined after 2-4 hours. The connection with plasma proteins is 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. The half-life is 13-24 hours.

It is excreted by the kidneys (50% - in the form of metabolites, 10% - unchanged), in part - through the intestine. Excretion of canrenone (mainly by the kidneys) is biphasic, the half-life in the first phase is 3-2 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). '

Indications:

essential hypertension (as part of combination therapy);

edematous syndrome with chronic heart failure (can be used in the form of monotherapy and in combination with standard 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 auxiliary for its prevention during treatment with diuretics, if other methods of correction of the potassium level can not be used);

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

to establish the diagnosis of primary hyperaldosteronism.

Contraindications:

Addison's disease;

hyperkalemia; -

hyponatremia;

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

anuria;

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

pregnancy;

lactation period (breastfeeding);

children under 3 years;

hypersensitivity to any of the components of the drug.

Carefully:

Atrioventricular blockade (the possibility of amplification due to the development of hyperkalemia), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, dysmenorrhea, hypercalcemia, metabolic acidosis, hepatic insufficiency, surgical interventions, gynecomastia and simultaneous administration of medications,causing gynecomastia, conducting local and general anesthesia, elderly age.

Pregnancy and lactation:

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

Dosing and Administration:

Inside.

In essential hypertension, the daily dose for adults is usually 50-100 mg once and can be increased to 200 mg, while increasing the dose should be gradual, 1 every 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 (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 hypomagnesemia caused by diuretic therapy, the drug is prescribed in a dose of 25-100 mg / day once or in several doses. The maximum daily dose of 400 mg, if oral potassium preparations 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 in several doses per day.With an increase in the concentration of potassium in the blood at the time of taking the drug and lowering it after cancellation it can be assumed that there is a primary hyperaldosteronism.

With a long diagnostic test, the drug is prescribed 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.

After the diagnosis of hyperaldosteronism is established with the help of more accurate diagnostic methods, as a short course of preoperative therapy of primary, hyperaldosteronism, the drug should be taken at a daily dose of 100 to 400 mg, dividing by 1 to 4 doses during the entire period of preparation for a surgical operation. If the operation is not indicated, then the drug is used to conduct long-term maintenance therapy, while using the lowest effective dose, which is selected individually for each patient.

In the treatment of edema against the background of nephrotic syndrome, the daily dose for adults is 100-200 mg. No effect of spironolactone on the main pathological process was found, and therefore the use of this drug is recommended only in cases when * other types of therapy are ineffective.

With edematic syndrome against a background of chronic heart failure, the drug is prescribed daily for 5 days at 100-200 mg / day in 2-3 doses, in combination with a "loop" or thiazide diuretic. Depending on the effect, the daily dose is reduced to 25 mg. The maintenance dose is selected individually. The maximum daily dose is 200 mg.

"With swelling on the background of cirrhosis of the liver, the daily dose for adults is usually 100 mg if the ratio of sodium and potassium ions (Na + / K +) in urine exceeds 1.0. If the ratio is less than 1.0, the daily dose is usually 200-400 mg The maintenance dose is selected individually.

With edema in children, the initial dose is 1-3.3 mg / kg body weight or 30-90 mg / m2 / day in 1-4 doses. After 5 days, dose adjustment is performed and, if necessary, it is increased 3 times as compared with the original dose.

Side effects:

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

From the nervous system: dizziness; drowsiness, lethargy, headache, inhibition, ataxia, muscle spasms, confusion.

On the part of the endocrine system: with prolonged use - gynecomastia, erectile dysfunction in men, decreased potency; in women - dysmenorrhea, amenorrhea, metrorrhagia in menopause, hirsutism, hypertrichosis, voice coarsening, breast tenderness, breast carcinoma.

From the urinary system: increased urea concentration, hyper-creatininemia, hyperuricemia, acute renal failure. -

From the side of metabolism: violation of water-electrolyte metabolism and acid-base state (metabolic hypochloraemic acidosis or alkalosis).

On the part of the organs of hematopoiesis: megaloblasticosis, agranulocytosis, thrombocytopenia. Allergic reactions: urticaria, maculopapular and erythematous rash, drug fever, pruritus.

Dermatological reactions: alopecia.

Other: spasms of gastrocnemius muscles, muscle spasm.

Overdose:

Symptoms: nausea, vomiting, dizziness, lowering blood pressure, diarrhea, skin rash, hyperkalemia (paresthesia, myasthenia gravis, arrhythmias), 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-withdrawing diuretics, rapid parenteral administration of a solution of dextrose (5-20% solutions) with insulin at a rate of 0.25-0.5 U per gram of dextrose; if necessary, repeated dextrose administration. In severe cases, hemodialysis is performed

Interaction:

Reduces the effect of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indanedione) and the toxicity of cardiac glycosides (as the normalization of the level of potassium 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, so it is possible to intoxicate with digoxin.

Increases the toxic effect of lithium due to reduced clearance.

Accelerates the metabolism and excretion of carbenoksolona.

Carbenoxolone promotes sodium retention by spironolactone.

Glucocorticosteroid preparations and diuretics (derivatives of benzothiazine, furosimide, ethacrynic acid) intensify and accelerate diuretic and natriuretic effects.

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

Glucocorticosteroid drugs increase the diuretic and natriuretic effect in hypoalbuminemia and / or hyponatremia.

The risk of hyperkalemia when taken with potassium preparations, potassium supplements and potassium-sparing diuretics, enzyme inhibitors antiotenzinprevraschayuschego (acidosis), angiotensin II antagonists, aldosterone blockers, indometa- tsinom cyclosporin.

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.

Enhances the effect of triptorelin, buserelin, ganadorelin.

Special instructions:

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

In diseases of the kidneys and liver, as well as in old age, regular monitoring of blood 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 the level of electrolytes in the blood should be monitored.

You should avoid 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.

On 20 tablets in cans polymeric.

10 tablets per contour cell pack. ' '

Each jar or 1, 2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Packaging:

Tablets 25 mg.

On 20 tablets in cans polymeric.

10 tablets per contour cell pack. ' '

Each jar or 1, 2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no more than 25 ° C.

Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002410

Date of registration:28.09.2011

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp19.08.2015

Illustrated instructions

Instructions

Spironolactone (Spironolactone)