Veroshpilakton

General characteristics. Structure:

Active ingredient: 25 mg, 50 mg or 100 mg of Spironolactonum in 1 capsule.

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

Gelatinous solid capsules: the case and a lid of the capsule - titanium dioxide, gelatin; or the capsule case - titanium dioxide, gelatin, a capsule lid - titanium dioxide, dye blue patent, dye diamond black, gelatin; or the case and a lid of the capsule - titanium dioxide; dye blue patent, gelatin.

Pharmacological properties:

Pharmacodynamics. Spironolactonum is kaliysberegayushchy diuretic, the specific antagonist of Aldosteronum of the prolonged action (a mineralokortikosteroidny adrenal hormone). In distal departments of nephron Spironolactonum interferes with a delay of aldosteronomas of sodium and water and suppresses kaliyvyvodyagtsy effect of Aldosteronum, reduces synthesis пермеаз in Aldosteronum - the dependent site of collective tubules and distal tubules. Contacting Aldosteronum receptors, increases excretion of ions of sodium, chlorine and water with urine, reduces removal of potassium ions and urea, reduces acidity of urine.

Strengthening of a diuresis is caused by existence of diuretic effect which is changeable. The diuretic effect is shown for 2-5 day of treatment.

Pharmacokinetics. Absorption and distribution. At intake it is quickly and completely soaked up from digestive tract. Contacts proteins of a blood plasma approximately for 98% (канренон - 90%). The maximum concentration (Cmax) of a kanrenon in a blood plasma is reached in 2-4 h after reception. After daily reception of 100 mg of Spironolactonum within 15 days of Cmax reaches 80 ng/ml, time of achievement of Cmax after the next morning reception - 2-6 h. Distribution volume - 0,05 l/kg.

Metabolism. Spironolactonum turns into active metabolity:metabolit,
containing sulfur (80%), and partially канренон (20%). Spironolactonum badly gets into bodies and fabrics, at the same time itself and its metabolites get through a placental barrier, and канренон - into breast milk.

Removal. It is removed by kidneys (50% - in the form of metabolites, 10% - in not changed look) and partially through intestines. The elimination half-life (Is hard) Spironolactonum of 13-24 h, active metabolites - to 15 h. Removal of a kanrenon (mainly kidneys) two-phase, It is hard in the first phase - 2-3 h, in the second - 12-96 h.

Pharmacokinetics at separate groups of patients. At cirrhosis and heart failure duration of an elimination half-life increases without signs of cumulation which probability is higher at a chronic renal failure and a hyperpotassemia.

Indications to use:

- essential hypertensia (as a part of a combination therapy).

- an edematous syndrome at chronic heart failure (it can be applied in monotherapy and in a combination with standard therapy).

- states at which the secondary hyper aldosteronism, including the cirrhosis which is followed by ascites and/or hypostases, a nephrotic syndrome, and also other states which are followed by hypostases can be found.

- a hypopotassemia/hypomagnesiemia (as supportive application for its prevention during treatment by diuretics and at impossibility of use of other ways of correction of content of potassium).

- primary hyper aldosteronism (Conn's syndrome) - for a short preoperative course of treatment.

- for establishment of the diagnosis of primary hyper aldosteronism.

Route of administration and doses:

Inside.

Essential hypertensia. The daily dose for adults usually makes 50-100 mg once and can be increased to 200 mg, at the same time it is necessary to increase a dose gradually, 1 time in 2 weeks. To achieve the adequate response to therapy, drug it is necessary to accept not less than 2 weeks. If necessary carry out correction of a dose.

Idiopathic hyper aldosteronism. Appoint 100-400 mg/days.

The expressed hyper aldosteronism and hypopotassemia. Appoint 300 mg/days (at most 400 mg/days) for 2-3 receptions, at improvement of a state gradually reduce a dose to 25 mg/days.

Hypopotassemia and/or hypomagnesiemia. At the hypopotassemia and/or a hypomagnesiemia caused by therapy by diuretics appoint drug in a dose of 25-100 mg/days, once or in stages. The maximum daily dose of 400 mg if potassium drugs for intake or other methods of completion of its deficit are inefficient.

Diagnosis and treatment of primary hyper aldosteronism. As diagnostic means at short diagnostic test: within 4 days on 400 mg/days, having distributed on several receptions in day. At increase in content of potassium in blood during administration of drug and decrease after cancellation it is possible to assume it existence of primary hyper aldosteronism.

At long diagnostic test: in the same dose within 3-4 weeks. At achievement of correction of a hypopotassemia and arterial hypertension it is possible to assume existence of primary hyper aldosteronism.

Short course of preoperative therapy of primary hyper aldosteronism. After the diagnosis of a hyper aldosteronism is established by means of more exact diagnostic methods, Veroshpilakton it is necessary to accept drug on 100-400 mg/days, having divided into 1-4 receptions a day during the entire period of preparation for surgical intervention. If surgical intervention is not shown, then drug Veroshpilakton is used for carrying out a long maintenance therapy, at the same time the smallest effective dose which is selected individually for each patient is applied.

Hypostases against the background of a nephrotic syndrome. The daily dose for adults usually makes 100-200 mg/days. Influence of Spironolactonum on the main pathological process and therefore use of this drug is recommended only when other types of therapy are inefficient is not revealed.

Edematous syndrome against the background of chronic heart failure. Daily, within 5 days on 100-200 mg/days in 2-3 receptions, in a combination with "loopback" or thiazide diuretic. Depending on effect, the daily dose is reduced to 25 mg. The maintenance dose is selected individually. Maximum dose of 200 mg/days.

Hypostases against the background of cirrhosis. If in urine the ratio of ions of sodium and potassium (Na+/K+) is exceeded 1,0, then the daily dose for adults usually makes 100 mg. If a ratio less than 1,0, then a daily dose for adults it is usually equal to 200-400 mg. The maintenance dose is selected individually.

Hypostases at children. The initial dose at children is more senior than 3 years makes 1-3,3 mg/kg of body weight or 30 - 90 mg/sq.m/days in 1-4 receptions. In 5 days the dose is adjusted and if necessary increased by 3 times in comparison with initial.

Features of use:

Pregnancy and lactation. Drug use Veroshpilakton is contraindicated at pregnancy and during feeding by a breast. Spironolactonum and its metabolites can get through a placental barrier. Metabolites of Spironolactonum are found in breast milk. In need of use of drug during breastfeeding, feeding by a breast should be stopped.

Perhaps temporary increase in maintenance of an urea nitrogen in blood serum, especially at reduced function of kidneys and a hyperpotassemia. The reversible giperkhloremichesky metabolic acidosis is possible.

At renal failures and a liver, and also at advanced age regular control of electrolytes of blood serum and function of kidneys is necessary.

Drug complicates definition of digoxin, cortisol and adrenaline in blood.
Despite the lack of direct impact on carbohydrate metabolism, existence of a diabetes mellitus, especially with a diabetic nephropathy, demands extra care because of a possibility of development of a hyperpotassemia.

At simultaneous treatment by non-steroidal anti-inflammatory drugs it is necessary to control function of kidneys and content of electrolytes in blood. It is necessary to avoid the use of the food rich with potassium.
During treatment alcohol intake is contraindicated.

Influence on ability to manage vehicles and mechanisms. It is necessary to be careful at control of vehicles and work with the mechanisms demanding the increased concentration of attention and speed of reactions (risk of development of dizziness and drowsiness).

Side effects:

From digestive tract: nausea, vomiting, diarrhea, ulcerations and bleedings from digestive tract, gastritis, intestinal colic, an abdominal pain, a lock.

From a liver: abnormal liver function.

From the central nervous system: ataxy, block, dizziness, headache, drowsiness, lethargy, confusion of consciousness, muscular spasm.

From blood and lymphatic system: agranulocytosis, thrombocytopenia, мегалобластоз.

From laboratory indicators: hyperuricemia, giperkreatininemiya, increase in concentration of urea, disturbance of water and electrolytic balance (hyperpotassemia, hyponatremia) and acid-base state (metabolic giperkhloremichesky acidosis or alkalosis).

From endocrine system: voice coarsening, men have a gynecomastia (the probability of development depends on a dose, duration of treatment and, usually, has reversible character, and after drug withdrawal disappears, and only in rare instances chest gland remains a little increased); decrease in a potentiality and erection; women have a disturbance of a menstrual cycle; a dysmenorrhea, an amenorrhea, a metrorrhagia in a climacteric, a hirsutism, pains in mammary glands, a carcinoma of a mammary gland (existence of communication with administration of drug is not established).

Allergic reactions: urticaria, makulopapulezny and erythematic rash,
medicinal fever, skin itch, eosinophilia, Stephen-Johnson's syndrome, toxic epidermal necrolysis.

From skin and hypodermic fabrics: alopecia, hypertrichosis.

From kidneys and urinary tract: acute renal failure.

From skeletal and muscular and connecting fabric: spasms of gastrocnemius muscles, osteomalacy.

From respiratory system, bodies of a thorax and a mediastinum: asthma.

If any of the undesirable reactions specified in the instruction are aggravated, or you noticed other undesirable phenomena which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Reduces effect of anticoagulants, indirect anticoagulants (heparin, derivative coumarin, an indandion) and toxicity of cardiac glycosides (since normalization of content of potassium in blood interferes with toxicity development).
Strengthens metabolism of phenazone (antipyrine).

Reduces sensitivity of vessels to Norepinephrinum (demands respect for care when carrying out anesthesia), increases a digoxin elimination half-life - intoxication digoxin is possible.

Strengthens toxic effect of lithium because of decrease in clearance.

Perhaps strengthens action of not depolarizing muscle relaxants (for example, tubocurarine).

Accelerates metabolism and removal of a karbenoksolon.

Karbenoksolon promotes a sodium delay Spironolactonum.

Glucocorticosteroid drugs and diuretics (tiazida and tiazidopodobny, furosemide, Acidum etacrynicum) strengthen and accelerate diuretic and natriuretic effects.

Strengthens effect of diuretic and hypotensive medicines. Non-steroidal anti-inflammatory drugs reduce diuretic and natriuretic effects, the risk of development of a hyperpotassemia increases.

Alcohol (ethanol), barbiturates, narcotic substances strengthen orthostatic hypotension.

Glucocorticosteroid drugs strengthen diuretic and natriuretic effect at a hypoalbuminemia and/or a hyponatremia.

The risk of development of a hyperpotassemia at reception with potassium drugs, potassium additives and kaliysberegayushchy diuretics, inhibitors of an angiotensin-converting enzyme increases (acidosis), antagonists of receptors of angiotensin II, blockers of Aldosteronum, indometacin, cyclosporine.

Salicylates, indometacin reduce diuretic effect.

Ammonium chloride, Colestyraminum promote development of a giperkaliyemichesky metabolic acidosis.

Fludrokortizon causes paradoxical strengthening of canalicular secretion of potassium. Reduces effect of Mitotanum.

Strengthens effect of a triptorelin, buserelin, gonadorelin.

Contraindications:

- hypersensitivity to any of drug components.
- Addison's disease.
- hyperpotassemia.
- hyponatremia.
- heavy renal failure (clearance of creatinine less than 10 ml/min.).
- anury.
- simultaneous use of an eplerenon and other kaliysberegayushchy diuretics, potassium drugs.
- a diabetes mellitus with the confirmed renal failure.
- pregnancy, feeding period breast.
- children's age up to 3 years (in connection with a firm dosage form).
- deficit of lactase, a lactose intolerance, a syndrome of glyukozo-galaktozny malabsorption (as monohydrate is a part of drug lactoses).

With care. A hypercalcemia, a metabolic acidosis, an atrioventricular block (the hyperpotassemia promotes its strengthening); a diabetes mellitus (at the confirmed or estimated chronic renal failure); diabetic nephropathy; surgical interventions, when carrying out anesthesia; reception of the medicines causing a gynecomastia; local and general anesthesia; advanced age; disturbance of a menstrual cycle, increase in mammary glands; liver failure, cirrhosis.

Overdose:

Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperpotassemia (paresthesias, muscular weakness, arrhythmias), hyponatremia (dryness of a mucous membrane of an oral cavity, thirst, drowsiness) hypercalcemia, dehydration, increase in concentration of urea.

Treatment: gastric lavage, symptomatic treatment of dehydration. At a hyperpotassemia it is necessary to normalize water and electrolytic balance by means of kaliyvyvodyashchy diuretics, bystry parenteral administration of 5-20% of solution of a dextrose (glucose) with insulin at the rate of 0,25-0,5 PIECES on 1 g of a dextrose (glucose); if necessary it is possible to enter repeatedly. In hard cases carry out a hemodialysis.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules of 25 mg, 50 mg and 100 mg. On 10, 14, 15 or 20 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2 or 3 blister strip packagings together with the application instruction in a pack from a cardboard.