Verospilactone pills 25mg, 20pcs

Composition

1 tablet contains

the Active ingredient:

spironolactone – 0.025 g

excipients:

magnesium stearate,

lactose (milk sugar),

potato starch,

colloidal silicon dioxide (aerosil),

talc

Pharmacological action

Pharmacodynamics

Spironolactone is a potassium-sparing diuretic, a specific antagonist of prolonged-acting aldosterone (mineralocorticosteroid hormone of the adrenal cortex). In the distal parts of the nephron, spironolactone prevents water retention by aldosterone sodium and suppresses the potassium-removing effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent region of the collecting tubules and distal tubules. 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 unstable: the diuretic effect is manifested on the 2-5 day of treatment.

Pharmacokinetics

When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract and converted to active metabolites: a metabolite containing sulfur (80%) and partially canrenone (20%). The maximum concentration (Cmax) of canrenone in blood plasma is reached in 2-4 hours, its binding to plasma proteins is 90%. Binding to plasma proteins is about 98% (canrenone-90%).

After a daily intake of 100 mg of spironolactone for 15 days, the Cmax reaches 80 mg / ml, the time to reach the Cmax after the next morning intake is 2-6 hours. Spironolactone penetrates poorly into organs and tissues, while itself and its metabolites penetrate the placental barrier, and canKreon – into breast milk. The volume of distribution is 0.05 l / kg. The half-life (half-life) of spironolactone is 13-24 hours, active metabolites-up to 15 hours.

It is excreted by the kidneys: 50% – in the form of metabolites,10% – unchanged and partially-in the feces. Excretion of canrenone (mainly by the kidneys) is biphasic, Half – life in the first phase is 2-3 hours, in the second – 12-96 hours.

In cirrhosis of the liver and heart failure, the elimination half-life is prolonged without signs of accumulation, which is more likely in chronic renal failure and hyperkalemia.

Indications

• Essential hypertension (as part of combination therapy);
• edematous syndrome in chronic heart failure (may be used as monotherapy and in combination with standard therapy);
• the condition under which it can occur secondary hyperaldosteronism, including liver cirrhosis accompanied by ascites and/or edema, nephrotic syndrome, and other conditions associated with edema;
• hypokalemia/hypomagnesemia (as subsidiary means For its prevention during treatment with diuretics and in case of impossibility of the use of other methods of correction of the potassium level);
• primary hyperaldosteronism (Conn’s syndrome) for a short preoperative course of treatment;
• for diagnosis of primary hyperaldosteronism.

Contraindications

• Hypersensitivity to any of the components
• of Verospilactone, 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), due to the solid dosage form.

With caution: hypercalcemia, metabolic acidosis, atrioventricular block (hyperkalemia increases it), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, surgical interventions, taking medications that cause gynecomastia, local and general anesthesia, old age, menstrual disorders, breast enlargement, liver failure.

Side effects

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

From the liver: impaired liver function.

From the central nervous system: ataxia, lethargy, 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 disorders; dysmenorrhea, amenorrhea, metrorrhagia in the menopausal period, hirsutism, pain in the mammary glands, breast carcinoma (the presence of a connection with taking the drug has not been established).

Metabolic disorders: hypercreatininemia, increased urea concentration, impaired water-salt metabolism (hyperkalemia, hyponatremia) and acid-base balance (metabolic hyperchloremic acidosis or alkalosis), hyperuricemia.

When using Verospilactone, gynecomastia may develop. The likelihood of gynecomastia depends on the dose of the drug and the duration of therapy. At the same time, gynecomastia is usually reversible, and after the drug is discontinued, it disappears, and only in rare cases the breast gland remains slightly enlarged.

Allergic reactions: urticaria, rarely maculopapular and erythematous rash, drug fever, pruritus.

From the skin: alopecia, hypertrichosis. From the urinary system: acute renal failure. From the musculoskeletal system: cramps of the calf muscles.

Interaction

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

Increases the metabolism of phenazole (antipyrine).

Reduces the sensitivity of blood vessels to noepinephrine (requires caution during anesthesia), increases the half-life of digoxin-possible intoxication-digoxin.

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

Accelerates the metabolism and elimination of carbenoxolone.

Carbenoxolone promotes sodium retention by spironolactone.

Glucocorticosteroid drugs and diuretics (benzothiadiazine derivatives, furosemide, etacric acid) enhance and accelerate the diuretic and natriuretic effects.

Increases the effect of diuretic and antihypertensive drugs. Nonsteroidal anti-inflammatory drugs reduce the diuretic and natriuretic effects, and increase the risk of hyperkalemia.

Glucocorticosteroid medications enhance the diuretic and natriuretic effects in patients with hypoalbuminemia and / or hyponatremia.

The risk of hyperkalemia increases when taken with potassium preparations, potassium supplements and potassium-sparing diuretics, angiotensin converting enzyme inhibitors( acidosis), angiotensin P antagonists, aldosterone blockers, Indometacin, cyclosporine. Salicylates, Indometacin reduce the diuretic effect.

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

Fludrocortisone causes a paradoxical increase in the tubular section of potassium. Reduces the effect of mitotan. Increases the effect of triptorelin, buserelin, gonadorelin.

How to take, course of use and dosage

Verospilactone is taken orally.

For 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,1 time in 2 weeks. To achieve an adequate response to therapy, the drug must be taken for at least 2 weeks. If necessary, adjust the dose.

For idiopathic hyperaldosteronism,100-400 mg / day.

With severe hyperaldosteronism and hypokalemia,300 mg / day (maximum 400 mg) in 2-3 doses, with improvement in the condition, the dose is gradually reduced to 25 mg/day.

Hypokalemia/hypomagnesemia

In case of hypokalemia and/or hypomagnesemia caused by diuretic therapy, the drug is prescribed at 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, distributed in several doses per day. With an increase in the concentration of potassium in the blood during taking the drug and a decrease after discontinuation of it, the presence of primary hyperaldosteronism can be assumed.

For a long-term diagnostic test: at 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, Verospilactone should be taken at 100-400 mg / day, divided into 1-4 doses per day during the entire period of preparation for surgery. If surgery is not indicated, Verospilactone is used for long-term maintenance therapy, 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. There was no effect of Verospilactone on the underlying pathological process, and therefore the use of this drug is recommended only in cases where other types of therapy are ineffective.

With edematous syndrome on the background of chronic heart failure,100-200 mg/day in 2-3 doses daily for 5 days, 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 on the background of cirrhosis of the liver

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

Edema in children

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

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 hypotension.

In case of hyperkalemia, it is necessary to normalize water and electrolyte metabolism with the help of potassium-removing diuretics, rapid parenteral use of 5-20% dextrose solution with insulin at the rate of 0.25-0.5 units per 1 g of dextrose; if necessary, it can be re-administered.

In severe cases, hemodialysis is performed.

Special instructions

It is possible to temporarily increase the level of urea nitrogen in the blood serum, especially with reduced renal function and hyperkalemia. Reversible hyperchloremic metabolic acidosis is possible.

In patients with kidney and liver diseases, as well as in the elderly, regular monitoring of serum electrolytes and kidney function is necessary.

The drug makes it difficult to detect digoxin, cortisol and epinephrine in the blood. Despite the lack of direct effects on carbohydrate metabolism, the presence of diabetes mellitus, especially with diabetic nephropathy, requires special caution due to the possibility of developing hyperkalemia. When treated with nonsteroidal anti-inflammatory drugs, kidney function and blood electrolyte levels should be monitored. Foods rich in potassium should be avoided.

Alcohol consumption is contraindicated during treatment.

The effect of the drug on the ability to drive a car and mechanisms that are associated with an increased risk of injury. During the initial period of treatment, it is forbidden to drive a car or engage in activities that require increased concentration of attention and speed of psychomotor reactions. The duration of restrictions is set individually.

Composition

Tablet Form of production

Storage conditions

In a dry place, protected from light

Shelf life

2 years

Active ingredient

Spironolactone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for children as prescribed by a doctor

Indications

Heart Failure, Hypertension