Verospiron, capsules 50mg, 30pcs

Composition

1 capsule contains:

Active ingredients:

spironolactone – 50 mg.

Auxiliary substances:

sodium lauryl sulfate-2.5 mg,

magnesium stearate-2.5 mg,

corn starch-42.5 mg,

lactose monohydrate-127.5 mg.

Composition of solid gelatin capsule:

cap – dye quinoline yellow (E 104) – 0.48%,

titanium dioxide (E 171) – 2%,

gelatin – up to 100%;

body – titanium dioxide (E 171) – 2%,

gelatin-up to 100%.

Pharmacological action

Pharmacodynamics

Verospiron – potassium-sparing, diuretic. Spironolactone is a potassium-sparing diuretic, a specific antagonist of long-acting aldosterone (mineralocorticosteroid hormone of the adrenal cortex).

In the distal parts of the nephron, spironolactone prevents the retention of sodium and water by aldosterone and suppresses the potassium-removing effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent area 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. Increased diuresis is due to the presence of a diuretic effect, which is unstable; the diuretic effect is manifested on the 2nd-5th day of treatment.

Pharmacokinetics

Suction and distribution

When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract. It binds to plasma proteins by approximately 98% (canrenone-90%). Tmax of canrenone in blood plasma is 2-4 hours. After a daily intake of 100 mg of spironolactone for 15 days, Cmax reaches 80 ng / ml, Tmax after the next morning intake is 2-6 hours. Vd — 0.05 l/kg.

Metabolism

Spironolactone is converted to active metabolites: a metabolite containing sulfur (80%) and partially — to canrenone (20%). Spironolactone does not penetrate well into organs and tissues, while it and its metabolites penetrate the placental barrier, and canrenone – into breast milk.

Deduction

It is excreted by the kidneys: 50% – in the form of metabolites,10% – unchanged and partially through the intestines. T1 / 2 of spironolactone — 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.

In cirrhosis of the liver and heart failure: the duration of T1 / 2 increases without signs of accumulation, the probability of which is higher in chronic renal failure and hyperkalemia.

Indications

Primary hyperaldosteronism (Conn’s syndrome) – for a short preoperative course of treatment.

To establish the diagnosis of primary hyperaldosteronism. Essential hypertension (as part of combination therapy). Edematous syndrome in chronic heart failure (can be used as monotherapy or 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, and other conditions accompanied by edema.

Hypokalemia/hypomagnesemia (as an adjunct for its prevention during treatment with diuretics and if it is impossible to use other methods of correcting potassium levels).

Use during pregnancy and lactation

Contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Contraindications

Pregnancy. Lactation period (breastfeeding). Children under 3 years of age. Addison’s disease. Hyperkalemia. Hyponatremia. Severe renal insufficiency (creatinine clearance less than 10 ml / min). Anuria.

Lactose intolerance, lactase deficiency, glucose / galactose malabsorption syndrome. Hypersensitivity to the components of the drug.

With caution: the drug should be prescribed for hypercalcemia, metabolic acidosis, AV block (hyperkalemia contributes to its strengthening), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, surgical interventions, taking medications that cause gynecomastia, local and general anesthesia, menstrual disorders, breast enlargement, liver failure, cirrhosis of the liver, as well as elderly patients.

Side effects

Allergic reactions: urticaria; rarely-maculopapular and erythematous rash, drug fever, pruritus. Dermatological reactions: alopecia, hypertrichosis.

From the urinary system: acute renal failure.

Musculoskeletal disorders: muscle spasm, calf muscle cramps.

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

From the central nervous system and peripheral nervous system: ataxia, lethargy, dizziness, headache, drowsiness, lethargy, confusion.

From the hematopoietic system: agranulocytosis, thrombocytopenia, megaloblastosis.

From the side of metabolism: hyperuricemia, hypercreatininemia, increased urea concentration, hyperkalemia, hyponatremia, metabolic hyperchloremic acidosis or alkalosis.

From the endocrine system: coarsening of the voice, in men – gynecomastia (the probability of development depends on the dose, duration of treatment and usually has a reversible character and after the withdrawal of Verospiron disappears, only in rare cases the breast gland remains slightly enlarged), 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 is not established).

Composition

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

Verospiron reduces the effect of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indanedione) and toxicity of cardiac glycosides (since normalization of blood potassium levels prevents the development of toxicity). Increases the metabolism of phenazole. Reduces the sensitivity of blood vessels to norepinephrine (requires caution during anesthesia). Increases T1 / 2 of digoxin, so possible intoxication with digoxin.

Increases the toxic effect of lithium due to a decrease in its clearance. Accelerates the metabolism and elimination of carbenoxolone. Carbenoxolone promotes sodium retention by spironolactone. Corticosteroids and diuretics (benzothiazine derivatives, furosemide, etacric acid) enhance and accelerate the diuretic and natriuretic effects.

Increases the effect of diuretic and antihypertensive drugs. CORTICOSTEROIDS enhance the diuretic and natriuric effects of hypoalbuminemia and / or hyponatremia. The risk of hyperkalemia increases when taking Verospiron with potassium preparations, potassium supplements and potassium-sparing diuretics, ACE inhibitors( acidosis), angiotensin II antagonists, aldosterone blockers, Indometacin, cyclosporine.

Salicylates, Indometacin reduce the diuretic effect. Ammonium chloride, colestyramine contribute to the development of hyperkalemic metabolic acidosis.

How to take, course of use and dosage

With 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. In idiopathic hyperaldosteronism, the drug is prescribed at a dose of 100-400 mg / day. With severe hyperaldosteronism and hypokalemia, the daily dose is 300 mg (maximum 400 mg) in 2-3 doses, with improvement in the condition, the dose is gradually reduced to 25 mg / day.

With hypokalemia and/or hypomagnesemia caused by diuretic therapy, Verospiron 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.

In the diagnosis and treatment of primary hyperaldosteronism as a diagnostic tool for a short diagnostic test, Verospiron 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 during taking the drug and a decrease after discontinuation of it, the presence of primary hyperaldosteronism can be assumed. With a long-term diagnostic test, the drug is prescribed 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. After the diagnosis of hyperaldosteronism is established using more accurate diagnostic methods, as a short course of preoperative therapy for primary hyperaldosteronism, Verospiron should be taken in a daily dose of 100-400 mg, divided into 1-4 doses during the entire period of preparation for surgery.

If surgery is not indicated, Verospiron is used for long-term maintenance therapy, using the lowest effective dose, which is selected individually for each patient. In the treatment of edema on the background of nephrotic syndrome, the daily dose for adults is usually 100-200 mg. No effect of spironolactone on the underlying pathological process was found, 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, 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. For edema associated with cirrhosis of the liver, the daily dose of Verospiron for adults is usually 100 mg if the ratio of sodium and potassium ions (Na+/K+) in the 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. For edema in children, the initial dose 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, it is increased by 3 times compared to the original one.

Overdose

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

Treatment: gastric lavage, symptomatic treatment of dehydration, 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 dextrose solution (5-20% solutions) with insulin at the rate of 0.25-0.5 units per 1 g of dextrose; if necessary, repeated use of dextrose is possible. In severe cases, hemodialysis is performed.

Special instructions

Influence on the ability to drive motor vehicles and manage mechanisms

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.

When using Verospiron, 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 may also occur.

When prescribing Verospiron to patients with impaired renal and hepatic function, elderly patients need regular monitoring of serum electrolytes and renal function.

Taking Verospiron makes it difficult to determine the concentration of 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 when prescribing Verospiron due to the possibility of hyperkalemia.

When treating NSAIDs while taking Verospiron, renal function and blood electrolyte levels should be monitored. During treatment with Verospiron, you should avoid eating foods rich in potassium.

Alcohol consumption is contraindicated during treatment.

Form of production

Capsules.

Storage conditions

Keep out of reach of children at a temperature not exceeding 30°C.

Shelf life

5 years

Active ingredient

Spironolactone

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

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

Indications

Heart Failure, Cirrhosis of the liver, Hypertension