Tablets white or white with Valium a color shade, round, Valium forms with Valium on one side and a facet, almost odorless or with a faint characteristic odor.

Pharmacotherapeutic group : potassium-sparing diuretic agent ATX Code C03DA01

Pharmacological properties : Pharmacodynamics: anadrol cycle is a potassium-sparing diuretic, a specific antagonist of aldosterone long-acting (mineralokortikosteroidny hormone of the adrenal cortex). In the distal nephron anadrol cycle prevents water retention of sodium and aldosterone suppresses kaliyvyvodyaschy aldosterone effect, reduces the synthesis permeases in aldosterone-sensitive area of the collecting ducts and distal tubules. By binding to the receptors of aldosterone, increases the excretion of sodium, chloride and water excretion, reduces the excretion of potassium ion and urea reduces the acidity of urine. The maximum effect is observed after 7 hours after oral administration and lasts for at least 24 hours. The antihypertensive effect of the drug caused by the presence diuretic effect who endures the diuretic effect is seen on the 2-5 day of treatment.

Pharmacokinetics
When administered rapidly and completely absorbed from the gastrointestinal tract and converted to active metabolites: metabolite containing sulfur (80%) and partially canrenone (20%). The maximum concentration (Cmax) of canrenone in the blood plasma is reached in 2-4 hours, its relation to plasma proteins 90%.Contact with blood plasma proteins for about 98% (canrenone – 90%).
After daily administration of 100 mg of anadrol cycle for 15 days, C max is 80 mg / ml, the time to reach Cmax after a morning reception -. 2-6 hours anadrol cycle bad into the organs and fabric, with himself and its metabolites cross the placental barrier and kankreon – in breast milk. The volume of distribution – 0.05 L / kg. The half-life (the T ½ .) anadrol cycle 13-24 hours, active metabolites – up to 15 hours
excreted by the kidneys: 50% – in the form of metabolites, 10% – unchanged and partly -kalovymi masses. Withdrawal of canrenone (mainly kidneys) biphasic T ½in the first phase – 2-3 hours, in the second -. 12-96 hours
in liver cirrhosis and heart failure duration of half-life is increased with no signs of accumulation, the probability is higher in patients with chronic renal failure and hyperkalemia.

INDICATIONS

  • Essential hypertension (as part of combination therapy);
  • edema syndrome in patients with chronic heart failure (can be used as monotherapy and in combination with standard therapy);
  • conditions that can be detected secondary hyperaldosteronism, including cirrhosis of the liver, accompanied by ascites and / or edema, nephrotic syndrome, and other conditions involving swelling;
  • hypokalemia / hypomagnesemia (as an aid for its prevention during treatment with diuretics and inability to use other methods of potassium level correction);
  • Primary hyperaldosteronism (Conn’s syndrome) – for a short pre-operative treatment;
  • for the diagnosis of primary hyperaldosteronism.

CONTRAINDICATIONS
Hypersensitivity to any component of the drug, Addison’s disease, hyperkalemia, hyponatremia, severe renal insufficiency (creatinine clearance less than 10 ml / min), anuria, pregnancy, lactation. Children’s age (up to 3 years), due to the solid dosage form. Precautions : hypercalcemia, metabolic acidosis, atrioventricular block (hyperkalemia enhances it), diabetes (with confirmed or suspected renal insufficiency), diabetic nephropathy, surgery, taking medicines that cause gynecomastia, local and general anesthesia, advanced age, menstrual disorders, breast enlargement, liver failure.

DOSAGE AND ADMINISTRATION
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In essential hypertension
daily dose for adults is usually 50-100 mg once daily and may be increased to 200 mg, and the dose should be increased gradually, one every 2 weeks. To achieve an adequate response to therapy, the drug must be taken for at least 2 weeks. If necessary, a dose adjustment.

When idiopathic hyperaldosteronism 100-400 mg / day.

In marked hypokalemia and hyperaldosteronism 300 mg / day (maximum 400 mg) for 2-3 hours, while improving the state gradually reduce the dose to 25 mg / day.

Hypokalemia / hypomagnesemia
When hypokalemia and / or hypomagnesemia caused by diuretic therapy, prescribe a drug at a dose of 25-100 mg / day, once or in several stages. The maximum daily dose of 400 mg if oral potassium supplements or other methods of filling the deficit ineffective.

Diagnosis treatment of primary hyperaldosteronism
as a diagnostic tool for short diagnostic assay: for 4 days at 400 mg / day, spreading to several doses per day. By increasing the concentration of potassium in the blood during treatment and after the cancellation of his reduction can assume the presence of primary hyperaldosteronism.
When prolonged diagnostic test : at the same dose for 3-4 weeks. Upon reaching the correction of hypokalemia and hypertension can assume the presence of primary hyperaldosteronism.

Preoperative course of therapy Short primary hyperaldosteronism
After diagnosis hyperaldosteronism set with more accurate diagnostic methods should take Veroshpilakton 100-400 mg / day, divided into 1-4 daily reception during the period of preparation for surgery. If surgery is not indicated, then Veroshpilakton used for long-term maintenance therapy, using the lowest effective dose, which is chosen individually for each patient.

Swelling on the background of nephrotic syndrome
daily dose for adults is usually 100-200 mg / day. Veroshpilaktona revealed no effect on the primary disease process, and therefore the use of this drug is recommended only when other therapies are ineffective.

When the edematous syndrome, chronic heart failure to background daily for 5 days at 100-200 mg / day for 2-3 hours, in combination with the “loop” or thiazide diuretic. Depending on the effect to reduce the daily dose of 25 mg. The maintenance dose is adjusted individually. The maximum dose of 200 mg / day.

Edema amid cirrhosis
If the ratio of urine sodium and potassium ions (Na + / K +) exceeds 1.0, the daily intake for adults normally being 100 mg. If the ratio is less than 1.0, the daily dose for adults is usually 200-400 mg. The maintenance dose is adjusted individually.

Edema in children
initial dose of 1-3,3 mg / kg body weight, or 30-90 mg / m2 / day. The reception 1-4. After 5 days, and the dose is adjusted as necessary to increase three-fold over the original.

ADVERSE EFFECTS From the digestive tract : nausea, vomiting, diarrhea, ulceration and bleeding from the gastrointestinal tract, gastritis, intestinal colic, abdominal pain, constipation. Liver : abnormal liver function. On the part of the central nervous system : ataxia , confusion, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm. From the hematopoietic system: leucopenia (including agranulocytosis), thrombocytopenia. Endocrine system : brutalization vote, men – gynecomastia (development of probability depends on the dose, duration of treatment and usually is reversible); lower potency and erection; for women – the menstrual cycle; dysmenorrhea, amenorrhea, metrorrhagia, menopause, hirsutism, pain in the breast, breast carcinoma (a connection with the drug intake is not installed). Metabolic disorders : hypercreatininemia, increasing concentrations of urea, a violation of water-salt metabolism (hyperkalemia, hyponatremia) and acid-base balance (metabolic acidosis or alkalosis hyperchloraemic), hyperuricemia. In applying Veroshpilaktona may develop gynecomastia. The likelihood of gynecomastia depends on the dose and duration of therapy. Thus gynecomastia usually is reversible, and after discontinuation of the drug disappears, and only in rare cases, breast remains somewhat increased. Allergic reactions : urticaria, rarely maculopapular and erythematous rash, drug fever, itching. With the Skin : alopecia, hypertrichosis. From the urinary system : acute renal failure. From the musculoskeletal system : leg cramps.

Overdose Symptoms : nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesia, muscle weakness, arrhythmia), hyponatremia (dry mouth, thirst, drowsiness), hypercalcemia, dehydration, increase in urea concentration. Treatment : gastric lavage, symptomatic treatment of dehydration and hypotension. When hyperkalemia is necessary to normalize the water-electrolyte metabolism via kaliyvyvodyaschih diuretics, rapid parenteral administration of 5-20% dextrose with insulin at the rate of 0.25-0.5 units per 1 g of dextrose; you can enter, if necessary repeatedly. In severe cases, hemodialysis. 

 

INTERACTION WITH OTHER DRUGS
Reduces the effect of anticoagulants, anticoagulants (heparin, coumarin derivatives, indandinona) and the toxicity of cardiac glycosides (ie. To the. Normalization of potassium level in the blood interferes with toxicity).
Increases metabolism fenazola (antipyrine).
Reduces the sensitivity of vessels to noepinefrinu ( requires compliance with caution during anesthesia), increases the half-life of digoxin – possible intoxication -. digoxin
increase the toxic effect of lithium due to the decrease in clearance.
It accelerates the metabolism and excretion of carbenoxolone.
carbenoxolone contributes to the delay of sodium anadrol cycle.
glucocorticosteroids and diuretics (derivatives benzotiadiazina, furosemide, ethacrynic acid) increase and accelerate the diuretic and natriuretic effects.
Enhances the effect of diuretics and antihypertensive drugs. Nonsteroidal anti-inflammatory drugs reduce the diuretic and natriuretic effects, increases the risk of hyperkalemia.
Glucocorticosteroids enhance the diuretic and natriuretic effect in hypoalbuminemia and / or hyponatremia.
The risk of hyperkalemia when taken with potassium supplements, potassium supplements and potassium-sparing diuretics, inhibitors of angiotensin converting enzyme (acidosis) , angiotensin II antagonists, aldosterone blockers, indomethacin, cyclosporin. Salicylates, indomethacin reduces the diuretic effect.
Ammonium chloride, cholestyramine giperkaliemicheskogo contribute to the development of metabolic acidosis.
Fludrocortisone is a paradoxical increase in potassium tubular section. It reduces the effect of mitotane.
Do effect of triptorelin, buserelin, gonadorelin.

Cautions
possible temporary increase in the level of urea nitrogen in serum, especially with reduced kidney function and hyperkalemia. Hyperchloraemic possible reversible metabolic acidosis.
In diseases of the kidneys and liver, as well as in the elderly requires regular monitoring of serum electrolytes and renal function. The drug is difficult to determine digoxin, cortisol and adrenaline in the blood.Although there is no direct effect on carbohydrate metabolism, presence of diabetes, especially diabetic nephropathy, it requires special caution because of the possibility of hyperkalemia.
In the treatment of non-steroidal anti-inflammatory drugs should
monitor kidney function and electrolytes in the blood.
You should avoid foods rich in potassium.
during treatment contraindicated use of alcohol.
The effect of the drug on the ability to drive and mechanisms, work on which is associated with an increased risk of injury.
In the initial period of treatment is prohibited to drive and engage in activities that require high concentration and psychomotor speed reactions. Time limits set individually.

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