Veroshpilactone tablets 100mg, No. 30

• Essential hypertension (as part of combination therapy);

• edematous syndrome in chronic heart failure (can be used in monotherapy and in combination with standard therapy);

• conditions in which secondary hyperaldosteronism can be detected, including cirrhosis of the liver, accompanied by ascites and / or edema, nephrotic syndrome, as well as other conditions accompanied by edema;

• hypokalemia / hypomagnesemia (as an adjuvant for its prevention during treatment with diuretics and when it is impossible to use other methods of correcting potassium content);

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

• for the diagnosis of primary hyperaldosteronism.

Inside.

Essential hypertension

The daily dose for adults is usually 50-100 mg once and can be increased to 200 mg, while the dose should be increased gradually, once every 2 weeks. To achieve an adequate response to therapy, the drug must be taken for at least 2 weeks. Dose adjustments are made if necessary.

Idiopathic hyperaldosteronism

Assign in a dose of 100-400 mg / day.

Severe hyperaldosteronism and hypokalemia

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

Hypokalemia and / or hypomagnesemia

In case of 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 is 400 mg if oral potassium preparations 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, 400 mg / day, divided into several doses per day. With an increase in the concentration of potassium in the blood while taking the drug and a decrease after its cancellation, one can assume the presence of primary hyperaldosteronism.

With a long-term diagnostic test: in the same dose for 3-4 weeks. When the correction of hypokalemia and arterial hypertension is achieved, the presence of primary hyperaldosteronism can be assumed.

Short course of preoperative therapy for primary hyperaldosteronism

After the diagnosis of hyperaldosteronism is established using more accurate diagnostic methods, Veroshpilactone should be taken at 100-400 mg / day, divided into 1-4 doses during the entire period of preparation for surgery. If the operation is not indicated, then the drug Veroshpilactone is used for long-term maintenance therapy, while the lowest effective dose is used, which is selected individually for each patient.

Edema against the background of nephrotic syndrome

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

Edematous syndrome against the background of chronic heart failure

Daily, for 5 days, 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 is 200 mg / day.

Edema against the background of liver cirrhosis

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

Swelling in children

The initial dose in children over 3 years of age is 1-3.3 mg / kg of body weight or 30-90 mg / m2 / day in 1-4 doses. After 5 days, the dose is adjusted and, if necessary, increased by 3 times compared to the initial one.

1 caps.

Spironolactone

Excipients: povidone, lactose monohydrate, potato starch, colloidal silicon dioxide (aerosil), sodium lauryl sulfate, talc, magnesium stearate.

• Hypersensitivity to any of the components of the drug;

• Addison's disease;

• hyperkalemia;

• hyponatremia;

• severe renal failure (CC less than 10 ml / min);

• anuria;

• pregnancy;

• lactation period (breastfeeding);

• children under 3 years of age (for solid dosage form);

• lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome (since the drug contains lactose monohydrate).

• With care: hypercalcemia, metabolic acidosis, AV blockade (hyperkalemia contributes to its strengthening); diabetes mellitus (with confirmed or suspected chronic renal failure); diabetic nephropathy; surgical interventions during anesthesia; taking medications that cause gynecomastia; local and general anesthesia; elderly age; violation of the menstrual cycle, enlargement of the mammary glands; liver failure, liver cirrhosis.

pharmachologic effect

Spironolactone is a potassium-sparing diuretic, a specific antagonist of aldosterone (mineralocorticosteroid hormone of the adrenal cortex) with prolonged action. In the distal nephron, spironolactone prevents the retention of sodium and water by aldosterone and inhibits the potassium-excreting effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent section of the collecting ducts and distal tubules. By binding to aldosterone receptors, it increases the excretion of sodium, chlorine and water ions in the urine, reduces the excretion of potassium and urea ions, and reduces the acidity of urine.

The maximum effect is observed 7 hours after ingestion and lasts at least 24 hours. The antihypertensive effect of the drug is due to the presence of a diuretic effect, which is variable: the diuretic effect appears on days 2-5 of treatment.

Pharmacokinetics

Absorption and distribution

When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract. The maximum concentration of Cmax canrenone in blood plasma is reached 2-4 hours after administration. Binds to blood plasma proteins by about 98% (canrenone - 90%). The volume of distribution (Vd) is 0.05 l / kg.

After daily intake of spironolactone at a dose of 100 mg for 15 days, Cmax is 80 ng / ml, the time to reach Cmax after the next morning intake is 2-6 hours.

Spironolactone poorly penetrates organs and tissues, while itself and its metabolites penetrate the placental barrier, and canrenone - into breast milk.

Metabolism

Spironolactone is converted into active metabolites: a metabolite containing sulfur (80%), and partially canrenone (20%).

Withdrawal

It is excreted by the kidneys: 50% - in the form of metabolites, 10% - unchanged and partially through the intestines. The half-life (T1 / 2) of spironolactone is 13-24 hours, active metabolites - up to 15 hours. Excretion of canrenone (mainly by the kidneys) is biphasic, T1 / 2 in the first phase - 2-3 hours, in the second - 12-96 hours.

Pharmacokinetics in selected patient groups

With cirrhosis of the liver and heart failure, the duration of T1 / 2 increases without signs of cumulation, the likelihood of which is higher in chronic renal failure and hyperkalemia.

Side effect

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

From the liver: abnormal liver function.

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

On the part of the blood and lymphatic system: agranulocytosis, thrombocytopenia, megaloblastosis.

On the part of laboratory parameters: hyperuricemia, hypercreatininemia, increased urea concentration, impaired water and electrolyte balance (hyperkalemia, hyponatremia) and acid-base state (metabolic hyperchloremic acidosis or alkalosis).

On the part of the endocrine system: coarsening of the voice, in men - gynecomastia (the likelihood of development depends on the dose, duration of treatment and is usually reversible, and after discontinuation of the drug disappears, and only in rare cases the mammary gland remains somewhat enlarged), decreased potency and erection; in women - menstrual irregularities, dysmenorrhea, amenorrhea, metrorrhagia in the climacteric period, hirsutism, pain in the mammary glands, breast carcinoma (no connection with the drug has been established).

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

On the part of the skin and subcutaneous tissues: alopecia, hypertrichosis.

From the kidneys and urinary tract: acute renal failure.

Musculoskeletal and connective tissue disorders: cramps of the calf muscles.

From the respiratory system: shortness of breath.

If any of the above adverse reactions are aggravated or other undesirable phenomena not specified in the instructions occur, the patient should be informed about this by the doctor.

Application during pregnancy and lactation

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

Spironolactone and its metabolites can cross the placental barrier.

Spironolactone metabolites are found in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Application for violations of liver function

With care: liver failure, liver cirrhosis.

Application for impaired renal function

Contraindication: severe renal failure (CC less than 10 ml / min).

Application in children

Contraindication: children under 3 years of age (for solid dosage form).

Use in elderly patients

With care: old age.

special instructions

A temporary increase in serum urea nitrogen is possible, especially with reduced renal function and hyperkalemia.

Reversible hyperchloremic metabolic acidosis is possible.

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

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

Despite the absence of a direct effect on carbohydrate metabolism, the presence of diabetes mellitus, especially with diabetic nephropathy, requires special care due to the possibility of developing hyperkalemia.

With the simultaneous treatment of NSAIDs, renal function and the content of electrolytes in the blood should be monitored.

Avoid eating foods rich in potassium.

Drinking alcohol is contraindicated during treatment.

Influence on the ability to drive vehicles and use mechanisms

In the initial period of treatment, it is forbidden to drive a vehicle and engage in activities that require an increased concentration of attention and speed of psychomotor reactions. The duration of the restrictions is set individually.

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 the water-electrolyte balance with the help of potassium-excreting diuretics, rapid parenteral administration of 5-20% dextrose (glucose) solution with insulin at the rate of 0.25-0.5 U per 1 g of dextrose (glucose); you can enter it again if necessary In severe cases, hemodialysis is performed.

Drug interactions

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

Strengthens the metabolism of phenazone (antipyrine).

Reduces the sensitivity of blood vessels to norepinephrine (caution is required during anesthesia), increases T1 / 2 of digoxin - intoxication with digoxin is possible.

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

Possibly enhances the effect of non-depolarizing muscle relaxants (for example, tubocurarine).

Accelerates the metabolism and excretion of carbenoxolone.

Carbenoxolone promotes sodium retention by spironolactone.

GCS and diuretics (thiazides and thiazide-like, furosemide, ethacrynic acid) enhance and accelerate the diuretic and natriuretic effects.

Strengthens the effect of diuretic and antihypertensive drugs.

NSAIDs reduce diuretic and natriuretic effects, increasing the risk of hyperkalemia.

Alcohol (ethanol), barbiturates, drugs increase orthostatic hypotension.

GCS enhance the diuretic and natriuretic effect in hypoalbuminemia and / or hyponatremia.

The risk of developing hyperkalemia increases when taken with potassium supplements, potassium supplements and potassium-sparing diuretics, ACE inhibitors (acidosis), angiotensin II receptor antagonists, blockers of aldosterone, indomethacin, cyclosporine.

Salicylates, indomethacin reduce the diuretic effect of spironolactone.

Ammonium chloride, cholestyramine contribute to the development of hyperkalemic metabolic acidosis.

Fludrocortisone causes a paradoxical increase in tubular potassium secretion.

Spironolactone reduces the effect of mitotane.

Enhances the effects of triptorelin, buserelin, gonadorelin.