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

active substance: spironolactone 25 mg / 50 mg / 100 mg; Excipients: povidone 5 mg / 5 mg / 10 mg, lactose monohydrate 70 mg / 56 mg / 112 mg, potato starch 52.0 mg / 41.2 mg / 82.4 mg, silicon dioxide colloid (aerosil) 2 mg / 2 mg / 4 mg, sodium lauryl sulfate 2.6 mg / 2.6 mg / 5.2 mg, talc 1.6 mg / 1.6 mg / 3.2 mg, magnesium stearate 1.6 mg / 1.6 mg / 3, 2 mg;

hard gelatine capsules:

body and cap capsule - titanium dioxide 2%, gelatin - up to 100%;

or capsule casing - titanium dioxide 2%, gelatin - up to 100%, cap of capsule - titanium dioxide 2%, dye blue patented 0.0176%, dye diamond black 0.0051%, gelatin - up to 100%;

or body and cap capsule - titanium dioxide 2%; dye blue patented 0.0158%, gelatin - up to 100%.

Description:

Dosage of 25 mg: capsule number 3 with a body and a lid of white color.

Dosage 50 mg: capsule No. 3 with a white body and a blue lid.

Dosage of 100 mg: capsule number 1 with a body and a lid of a blue color.

The contents of capsules are white or white powder with a yellowish tinge.

Pharmacotherapeutic group:Diuretic potassium-sparing agent

ATX: & nbsp

C.03.D.A Aldosterone antagonists

C.03.D.A.01 Spironolactone

Pharmacodynamics:

Spironolactone is a potassium-sparing diuretic, a specific antagonist of prolonged-action aldosterone (mineralocorticosteroid hormone of the adrenal cortex). In the distal sections of the nephron spironolactone prevents the delay of aldosterone sodium and water and suppresses the potassium-releasing effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent region of the collecting tubules and distal tubules. By binding to aldosterone receptors, increases the excretion of sodium, chlorine and water ions in the urine, reduces the excretion of potassium and urea ions, reduces the acidity of urine.

The increase in diuresis is due to the presence of a diuretic effect, which is unstable.Diuretic effect is manifested on the 2nd-5th day of treatment.

Pharmacokinetics:

Absorption and distribution. When ingested quickly and completely absorbed from the gastrointestinal tract. It binds to blood plasma proteins by about 98% (canrenone - 90%). The maximum concentration (C_max) canrenone in the blood plasma is achieved in 2-4 hours after admission. After a daily intake of 100 mg of spironolactone for 15 days C_max reaches 80 ng / ml, time to reach C_max after the next morning reception - 2-6 hours. The volume of distribution is 0,05 l / kg.

Metabolism. Spironolactone is converted into active metabolites: metabolite,

containing sulfur (80%), and partly canrenone (20%). Spironolactone poorly penetrates into organs and tissues, while himself and his metabolites penetrate the placental barrier, and canrenone - into breast milk.

Excretion. It is excreted by the kidneys (50% - in the form of metabolites, 10% - unchanged) and partially through the intestine. Half-life (T_1/2) spironolactone 13-24 h, active metabolites - up to 15 h. Excretion of canrenone (mainly by the kidneys) biphasic, T_1/2 in the first phase - 2-3 hours, in the second - 12-96 hours.

Pharmacokinetics in selected patient groups. With cirrhosis and heart failure, the half-lifeincreases without signs of cumulation, the probability of which is higher for chronic renal failure and hyperkalemia.

Indications:

Essential hypertension (as part of combination therapy).

Edema syndrome with chronic heart failure (can be used in monotherapy and in combination with standard therapy).

Conditions in which secondary hyperaldosteronism may 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 and when other methods of correction of potassium content are not possible).

Primary hyperaldosteronism (Conn's syndrome) is for a short preoperative course of treatment.

To establish the diagnosis of primary hyperaldosteronism.

Contraindications:

Hypersensitivity to any of the components of the drug.

Addison's disease.

Hyperkalemia.

Hyponatremia.

Severe renal insufficiency (creatinine clearance less than 10 ml / min).

Anuria.

Simultaneous use of eplerenone and other potassium-sparing diuretics, potassium preparations.

Diabetes mellitus with confirmed renal failure.

Pregnancy, the period of breastfeeding.

Children up to 3 years of age (due to solid dosage form).

Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome (since lactose monohydrate is included in the formulation).

Carefully:

Hypercalcemia, metabolic acidosis, atrioventricular blockade (hyperkalaemia contributes to its enhancement); diabetes mellitus (with confirmed or suspected chronic renal failure); diabetic nephropathy; surgical interventions, during anesthesia; taking medicines that cause gynecomastia; local and general anesthesia; elderly age; violation of the menstrual cycle, enlargement of the mammary glands; hepatic failure, cirrhosis.

Pregnancy and lactation:

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

Spironolactone and its metabolites can penetrate the placental barrier.Metabolites of spironolactone are found in breast milk. If it is necessary to use the drug during breastfeeding, breastfeeding should be stopped

Dosing and Administration:

Inside.

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.

Idiopathic hyperaldosteronism

Assign 100-400 mg / day.

Pronounced hyperaldosteronism and hypokalemia

Assign 300 mg / day (maximum 400 mg / day) for 2-3 doses, as the condition improves, the dose is gradually reduced to 25 mg / day.

Hypokalemia and / or hypomagnesemia

With hypokalemia and / or 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 potassium preparations for oral administration or other methods of replenishing its deficiency are ineffective.

Diagnosis and treatment of primary hyperaldosteronism

As a diagnostic tool for a short diagnostic test: for 4 days at 400 mg / day, divided into several doses per day. With an increase in the potassium content 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: 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

Once the diagnosis of hyperaldosteronism is established with more accurate diagnostic methods, the drug Veroshpilakton should be taken at 100-400 mg / day, dividing by 1-4 doses per day during the entire period of preparation for surgery. If surgery is not indicated, the drug Veroshpilakton is used to provide 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 / day. 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.

Edema on a background of chronic heart failure

Daily, for 5 days to 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 dose of 200 mg / day. Edema on the background of liver cirrhosis

If the ratio of sodium and potassium ions (Na + / K +) in urine exceeds 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.

Swelling in children

The initial dose in children older than 3 years 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.

Side effects:

From the gastrointestinal tract: nausea, vomiting, diarrhea, ulceration and bleeding from the gastrointestinal tract, gastritis, intestinal colic, abdominal pain, constipation.

From the side of the liver: abnormal liver function.

From the central nervous system: ataxia, inhibition, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm.

From the side of the blood and lymphatic system: agranulocytosis, thrombocytopenia, megaloblastosis.

From the laboratory indicators: hyperuricemia, hypercreatininaemia,

increase in urea concentration, disturbance of water-electrolyte balance (hyperkalemia, hyponatremia) and acid-base state (metabolic hyperchloremic acidosis or alkalosis).

From the endocrine system: coarsening of the voice, in men - gynecomastia (the probability of development depends on the dose, the duration of treatment and, usually, is reversible, and after the drug is discontinued, and only in rare cases the breast remains slightly enlarged); decreased potency and erection; in women, menstrual cycle disorders; dysmenorrhea, amenorrhea, metrorrhagia in menopause, hirsutism, pain in the mammary gland, breast carcinoma (the presence of a connection with the drug is not established).

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

From the skin and subcutaneous tissues: alopecia, hypertrichosis.

From the side of the kidneys and urinary tract: acute renal failure.

From the side of the musculoskeletal and connective tissue: cramps of the calf muscles, osteomalacia.

From the respiratory system, chest and mediastinum: dyspnea.

If any of the unwanted reactions listed in the manual is aggravated, or if you notice other undesirable phenomena not listed in the manual, inform the doctor about it.

Overdose:

Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesia, muscle weakness, arrhythmias), hyponatremia (dryness of the oral mucosa, thirst, drowsiness) hypercalcemia, dehydration, increased urea concentration.

Treatment: gastric lavage, symptomatic treatment of dehydration. With hyperkalemia, it is necessary to normalize the water-electrolyte balance with the help of potassium-releasing diuretics,rapid parenteral administration of 5-20% dextrose (glucose) solution with insulin at the rate of 0.25-0.5 ED per 1 g of dextrose (glucose); If necessary, you can re-enter it. 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 phenazone (antipyrine).

Reduces the sensitivity of the 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 reduced clearance.

It probably enhances the effect of nondepolarizing muscle relaxants (eg, tubocurarine).

Accelerates the metabolism and excretion of carbenoksolona.

Carbenoxolone promotes sodium retention by spironolactone.

Glucocorticosteroid preparations and diuretics (thiazides and thiazide-like, furosemide, ethacrynic acid) intensify and accelerate diuretic and natriuretic effects.

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

Alcohol (ethanol), barbiturates, narcotic substances strengthen orthostatic hypotension.

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

The risk of hyperkalemia increases with admission with potassium preparations, potassium supplements and potassium-sparing diuretics, inhibitors

angiotensin-converting enzyme (acidosis), 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.

Special instructions:

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

With violations of the kidneys and liver, as well as in the elderly, 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.

With simultaneous treatment with nonsteroidal anti-inflammatory drugs, kidney function and electrolyte content in the blood 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:

Care must be taken when driving vehicles and working with mechanisms that require high concentration and rapid reaction (risk of dizziness and drowsiness).

Form release / dosage:

Capsules 25 mg, 50 mg and 100 mg.

Packaging:

By 10, 14, 15 or 20 capsules in a planar cell pack of film

polyvinylchloride and aluminum foil printed lacquered.

For 1, 2 or 3 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002347

Date of registration:15.01.2014

Expiration Date:15.01.2019

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Verospilactone (Verospilactone)