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

Spironolactone is a potassium-sparing diuretic, prolonged action, a competitive antagonist of 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 hypotensive effect of the drug is due to the presence of a diuretic effect; diuretic effect is manifested on the 2-5 day of treatment.

Pharmacokinetics:

When ingested quickly and completely absorbed from the gastrointestinal tract; bioavailability is almost 100%, and the food intake increases it to 100%; the bond with blood plasma proteins is about 98%. After a daily dose of 100 mg for 15 days, the maximum concentration (C max) is 80 ng / ml, the time to reach the maximum

concentration in the plasma (TSam) after the next morning reception - 2-6 h.

In the process of biotransformation, active sulfur-containing metabolites 7-alpha-thiomethylspinonolactone and canrenone form in the liver. Cannone reaches C max in 2-4 h, its association with plasma proteins is 90%.

Spironolactone poorly penetrates organs and tissues, while itself and its metabolites penetrate the placental barrier, and canrenone into breast milk. The volume of the distribution is 0.05 l / kg. Half-life (T_1/2) -13-24 h.

It is excreted by the kidneys: 50% - in the form of metabolites, 10% - in unchanged form and partially - through the intestine. 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 cirrhosis and heart failure, the duration T_1/2 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);

- an acute syndrome in chronic heart failure (can be used as a monotherapy and in combination with standard therapy);

-conditions at 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 auxiliary for its prevention during treatment with diuretics and when other methods of correction of potassium concentration are not possible);

- Primary hyperaldosteronism (Connes 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, lactose intolerance, lactase deficiency or glucose-galactose malabsorption, Addison's disease, hyperkalemia, hyponatremia, severe renal failure (creatinine clearance less than 10 ml / min), anuria, pregnancy, lactation period, age (up to 3 years) for this dosage form.

Carefully:

Hypercalcemia, metabolic acidosis, atrioventricular blockade (hyperkalaemia contributes to its enhancement); diabetes mellitus (with confirmed or suspected chronic renal failure); diabetic nephropathy; surgical interventions; the use of drugs that cause gynecomastia; local and general anesthesia; elderly age, menstrual irregularity, hepatic insufficiency, cirrhosis of the liver.

Pregnancy and lactation:

Veroshpiron is contraindicated in pregnancy and lactation.

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 must 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, with the improvement of the condition, 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 and treatment of primary hyperaldosteronism

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

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

After the diagnosis of hyperaldosteronism is established using more accurate diagnostic methods, Veroshpiron 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, Veroshpiron is used for prolonged maintenance therapy, while the lowest effective dose that is selected individually for each patient is used.

Edema on the background of nephrotic syndrome

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

With edematous syndrome against a background of chronic cardiac insufficiency daily, within 5 days of 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.

Children

The initial dose is 1-3.3 mg / kg body weight or 30-90 mg / m2 / day in 1-4 sessions.

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 hematopoietic system: agranulocytosis, thrombocytopenia, megaloblastosis.

From the laboratory indicators: hyperuricemia, hypercreatininaemia, increased urea concentration, disturbance of water-salt metabolism (hyperkalemia, hyponatremia) and acid-base balance (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 removal of Veroshpiron disappears, only in rare cases the breast remains slightly enlarged), a decrease in potency and erection; in women - menstrual irregularities, dysmenorrhea, amenorrhea, metrorrhagia in menopause, hirsutism, pain in the area of mammary glands, breast cancer (the presence of a connection with the drug is not established).

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, decreased blood pressure, 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 exchange with the help of potassium-withdrawing diuretics, rapid parenteral administration of a solution of dextrose (5-20% solutions) with insulin from the calculation 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, indanedione) and the toxicity of cardiac glycosides (as normalization of the level of potassium in the blood prevents the development of toxicity).

Enhances the metabolism of phenazol (antipyrine).

Reduces the sensitivity of vessels to norepinephrine (requires caution when conducting anesthesia), increasesT_1/2 digoxin - possible intoxication with digoxin. (

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

Accelerates the metabolism and excretion of carbenoksolona.

Carbenoxolone promotes sodium retention by spironolactone.

Glucocorticosteroids and diuretics (benzothiazine derivatives, furosemide, ethacrynic acid) intensify and accelerate diuretic and natriuretic effects.

Strengthens the action of diuretic and hypotensive drugs. Glucocorticosteroid preparations increase the diuretic and natauric effect in hypoalbuminemia and / or hyponatremia.

The risk of hyperkalemia increases with admission to potassium, potassium supplements and potassium-sparing diuretics, angiotensin-converting enzyme (acidosis) inhibitors, angiotensin II 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 the level of urea nitrogen in the blood serum, especially with reduced kidney function and hyperkalemia. Possible reversible hyperchloremic metabolic acidosis.

With kidney and liver diseases, as well as in old age, regular monitoring of 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 blood electrolyte indices 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:

The effect of the drug on the ability to drive a car and mechanisms, work on which is associated with an increased risk of injury

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

Form release / dosage:

Tablets, 25 mg.

Packaging:

For 20 tablets in a blister of A1 / PVC. 1 blister in a cardboard box with the attached instruction for medical use.

Storage conditions:

At a temperature of no higher than 30 ° C. Keep out of the reach of children!

Shelf life:5 years.

Terms of leave from pharmacies:On prescription

Registration number:П N012681 / 01

Date of registration:15.03.2010 / 30.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

GEDEON RICHTER OJSC Hungary

GEDEON RICHTER POLAND, Co. Ltd. Poland

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Veroshpiron (Verospiron)