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

Tablets white or white with a creamy shade of color, round, flat-cylindrical shape with a risk on one side and chamfer, almost odorless or with a weak specific odor.

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 water retention by aldosterone 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 maximum effect is observed 7 hours after ingestion and lasts at least 24 hours. The hypotensive effect of the drug is due to the presence of a diuretic effect, which is unstable: the diuretic effect is manifested on the 2-5 day of treatment.

Pharmacokinetics:

When ingested quickly and completely absorbed from the gastrointestinal tract and converted into active metabolites: a metabolite containing sulfur (80%) and partly canrenone (20%). The maximum concentration (Сmах) of canrenone in blood plasma is reached in 2-4 h, its connection with blood plasma proteins is 90%.

The connection with blood plasma proteins is about 98% (canrenone - 90%).

After daily intake of 100 mg of spironolactone for 15 days, C max reaches 80 mg / ml, the time of reaching C max after the next morning intake is 2-6 h. Spironolactone poorly penetrates into organs and tissues, while himself and his metabolites penetrate the placental barrier, and canreon - into breast milk. The volume of distribution is 0.05 l / kg. Half-life (T_1/2) spironolactone 13-24 h, active metabolites - up to 15 h.

It is excreted by the kidneys: 50% - in the form of metabolites, 10% - in an unchanged form and partly - in calories. The excretion of canrenone (mainly by the kidneys) is biphasic,T_1/2 in the first phase - 2-3 hours, in the second - 12-96 hours.

With liver cirrhosis and heart failure, the half-life period increases without signs of cumulation, the probability of which is higher for 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 adjuvant For its prevention during treatment with diuretics and when other methods of correction of the potassium level are not possible);

. - Primary typeraldosteronism (Conn's syndrome). - 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 failure (creatinine clearance less than 10 ml / min), anuria, pregnancy, lactation. Children's age (up to 3 years), in connection with a solid dosage form.

Carefully:

Hypercalcaemia, metabolic acidosis, atrioventricular blockade (hyperkalaemia contributes to its strengthening), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, surgical interventions, drugs causing gynecomastia, local and general anesthesia, elderly age, menstrual irregularity , breast enlargement,liver failure.

Dosing and Administration:

Inside.

With 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 300 mg / day (maximum 400 mg) for 2-3 doses, when the condition is improved, the dose is gradually reduced to 25 mg / day.

Hypokalemia / 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 oral potassium preparations or other methods of replenishing its deficiency are ineffective.

Diagnosis treatment of primary hyperaldosteronism

As a diagnostic tool for short diagnostic test: for 4 days at 400 mg / day, divided into 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.

When long-term 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, Veroshpilakton should be taken at 100-400 mg / day, dividing by 1-4 doses per day during the entire period of preparation for a surgical operation. If the operation is not indicated, then Veroshpilakton is used to conduct long-term maintenance therapy, while using the lowest effective dose, which is selected individually for each patient.

Edema on the background of nephrotic syndrome

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

With edematous syndrome in the 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 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, retardation, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm.

From the hematopoietic system: leukopenia (including agranulocytosis), thrombocytopenia.

From the endocrine system: coarsening of the voice, in men - gynecomastia (the probability of development depends on the dose, duration of treatment and, usually, is reversible); 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).

Metabolic disorders: hyperkreatininemia, increased urea concentration, violation of water-salt metabolism (hyperkalemia, hyponatremia) and acid-base equilibrium (metabolic hyperchloremic acidosis or alkalosis), hyperuricemia. When using Veroshpilaktona gynecomastia may develop. The likelihood of gynecomastia depends on the dose of the drug and on the duration of therapy. In this case, gynecomastia is usually reversible, and after discontinuation of the drug disappears, and only in rare cases the breast remains slightly enlarged. Allergic reactions: urticaria, rarely maculopapular and erythematous rash, drug fever, itching.

From the skin: alopecia, hypertrichosis.

From the urinary system: acute renal failure.

From the musculoskeletal system: cramps calf muscles.

Overdose:

Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesia, muscle weakness, arrhythmias), hyponatremia (dry mouth, thirst, drowsiness) hypercalcemia, dehydration, increased urea concentration.

Treatment: gastric lavage, symptomatic treatment 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 5-20% dextrose solution with insulin at the rate of 0.25-0.5 units per 1 g of dextrose; If necessary, you can re-enter it. In severe cases, hemodialysis is performed.

Interaction:

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

Enhances the metabolism of phenazol (antipyrine).

Reduces vascular sensitivity to noepinefrinu (requires care in compliance anesthesia) that increases the half-life of digoxin - possible intoxication - 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 (benzothiadiazine derivatives, 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. 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, angiotensin-converting enzyme (acidosis), angiotensin II antagonists, aldoeterona blockers,indomethacin, cyclosporine.

Salicylates, indomethacin reduce the diuretic effect.

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

Fludrocortisone causes a paradoxical enhancement of the tubular section of potassium.

Reduces the effect of mitotane.

Strengthens the effect of tryptorelin, buserelin, gonadorelin.

Special instructions:

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

In diseases of the kidney 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.

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 a car and engage in activities that require an increased concentration of attention and speed of psychomotor reactions. The duration of restrictions is set individually.

Form release / dosage:

Tablets of 25 mg.

Packaging:

For 10, 15, 20 or 30 tablets in a contour cell pack of film polyvinylchloride and foil aluminum printed varnished.

By 1, 2, 3 contour cell packings with instructions for use are a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:4 years. Do not use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001560 / 01

Date of registration:18.07.2008

Expiration Date:Unlimited

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

Veroshpilakton® (Verospilactone)