Veroshpiron

General characteristics. Structure:

Capsules of 50 mg
Active ingredient: Spironolactonum - 50,00 mg
Excipients in the capsule: sodium lauryl sulfate - 2,50 mg; magnesium stearate - 2,50 mg; starch corn - 42,50 mg; lactoses monohydrate - 127,50 mg.
Solid gelatin capsule:
Size No. 3.
Lid: dye of quinolinic yellow E 104 - 0,48%; titanium dioxide of E 171 - 2,0%; gelatin - to 100%.
Case: titanium dioxide of E 171 - 2,00%; gelatin - to 100%.

Capsules of 100 mg
Active ingredient: Spironolactonum - 100,00 mg.
Excipients in the capsule: sodium lauryl sulfate - 5,00 mg; magnesium stearate - 5,0 mg; starch corn - 85,00 mg; lactoses monohydrate - 255,00 mg.
Solid gelatin capsule:
Size No. 0.
Lid: dye sunset of yellow E 110 - 0,04%; titanium dioxide of E 171 - 2,0%; gelatin - to 100%.
Case: dye sunset of yellow E 110 - 0,04%; titanium dioxide of E 171 - 2,0%, dye of quinolinic yellow E 104 - 0,50%; gelatin - to 100%.

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 kaliyvyvodyashchy 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 metabolites: the metabolite 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. An elimination half-life (T1/2) of Spironolactonum of 13-24 h, active metabolites - to 15 h. Removal of a kanrenon (mainly kidneys) two-phase, T1/2 in the first phase is 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 arterial hypertension (as a part of a combination therapy).
- An edematous syndrome at chronic heart failure (it can be applied in the form of 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.
- At 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.
- At an idiopathic hyper aldosteronism of 100-400 mg/days.
- At the expressed hyper aldosteronism and a hypopotassemia of 300 mg/days (at most 400 mg) for 2-3 receptions, at improvement of a state the dose is gradually reduced to 25 mg/days in other dosage form.
- Hypopotassemia/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 peroral drugs of potassium 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, Veroshpiron it is necessary to accept 100-400 mg/days, having divided into 1-4 receptions a day during the entire period of preparation for surgery. If operation is not shown, then Veroshpiron is applied to carrying out a long maintenance therapy, at the same time the smallest effective dose which is selected individually for each patient is used.
- 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.
- At an 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+) exceeds 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:

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

Influence of drug on ability to manage the vehicle and mechanisms on which work is connected with the increased risk of traumatism
In an initial stage of treatment the control of vehicles is forbidden and to be engaged in the types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Duration of restrictions is established in an individual order.

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 the hemopoietic 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 balance (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); decrease in a potentiality and erection; women have disturbances of a menstrual cycle; dysmenorrhea; amenorrhea; a metrorrhagia in a climacteric; hirsutism; pains in mammary glands; a carcinoma of a mammary gland (existence of communication with administration of drug it is not established).

At drug use Veroshpiron can develop a gynecomastia. The probability of emergence of a gynecomastia depends both on a drug dose, and on therapy duration. At the same time the gynecomastia usually has reversible character, and after drug withdrawal Veroshpiron disappears, and only in rare instances chest gland remains a little increased.
- Allergic reactions: urticaria, seldom makulopapulyozny and erythematic rash, medicinal fever, itch, eosinophilia, Stephen-Johnson's syndrome, toxic epidermal necrolysis.
- From integuments: alopecia, hypertrichosis.
- From an urinary system: acute renal failure.
- From a musculoskeletal system: spasms of gastrocnemius muscles.

Interaction with other medicines:

Reduces effect of anticoagulants, indirect anticoagulants (heparin, derivative coumarin, an idandion) and toxicity of cardiac glycosides (since normalization of content of potassium in blood interferes with toxicity development).
Strengthens metabolism of a fenazol (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 its 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 (derivative a benzotiazina, furosemide, Acidum etacrynicum) strengthen and accelerate diuretic and natriuretic effects.
Strengthens effect of diuretic and anti-hypertensive 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 angiotensin II, blockers of Aldosteronum, indometacin, cyclosporine.
Salicylates, indometacin reduce diuretic effect.
Ammonium chloride, холестирамин promote development of a giperkaliyemichesky metabolic acidosis.
Fludrokortizon causes paradoxical strengthening of canalicular secretion of potassium.
Reduces effect of Mitotanum.
Strengthens action of a triptorelin, buzerelin, 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;
- Pregnancy, feeding period breast;
- Children's age up to 3 years (a firm dosage form);
- Deficit of lactase, lactose intolerance, glyukozo-galaktozny malabsorption.

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.

Use at pregnancy and in the period of a lactation
At pregnancy:
Drug is contraindicated at pregnancy.
In the period of a lactation
Drug is contraindicated in the period of a lactation. Breastfeeding should be stopped in case of impossibility of cancellation of Spironolactonum.

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

Storage conditions:

At a temperature not above 30 °C.
To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Capsules on 50 and 100 mg.
10 capsules in the blister from AL/PVH. 3 blisters in a cardboard pack with the enclosed application instruction.