Structure Verospiron:
Composition per 1 tablet
Active ingredient Verospiron:
spironolactone 25 mg.
Excipients Verospiron:
colloidal silicon dioxide - 1.2 mg; magnesium stearate - 2 mg; talcum powder - 5.8 mg; corn starch - 70 mg; lactose monohydrate - 146 mg.
general description Verospiron:
Potassium-sparing diuretic
Special conditions Verospiron:
A temporary increase in serum urea nitrogen level is possible, especially with decreased renal function and hyperkalemia. Possible reversible hyperchloremic metabolic acidosis.
In diseases of the kidneys and liver, as well as in old age, regular monitoring of serum electrolytes and kidney function is necessary. Verospiron
The drug Verospiron makes it difficult to determine digoxin, cortisol and adrenaline in the blood. Despite the absence of a direct effect on carbohydrate metabolism, the presence of diabetes mellitus, especially with diabetic nephropathy, requires special care because of the possibility of developing hyperkalemia.
In the treatment of non-steroidal anti-inflammatory drugs Verospiron, kidney function and blood electrolyte counts should be monitored. Avoid eating potassium-rich foods. During treatment, alcohol is contraindicated.
Impact on the ability to drive vehicles and other mechanisms:
The effect of the drug Verospiron on the ability to drive a car and mechanisms that work with an increased risk of injury
In the initial period of treatment, it is forbidden to drive a car and engage in activities that require an increased concentration of attention and speed of psychomotor reactions. The duration of the restrictions is set individually.
Drug Interactions Verospiron:
Reduces the effect of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indandion) and toxicity of cardiac glycosides (since normalization of potassium levels in the blood prevents the development of toxicity).
Enhances the metabolism of phenazole (antipyrine).
Reduces vascular sensitivity to norepinephrine (requires caution when conducting anesthesia), increases T1 / 2 of digoxin - digoxin intoxication is possible. (
Enhances the toxic effect of lithium due to a decrease in its clearance.
Accelerates the metabolism and excretion of carbenoxolone.
Carbenoxolone promotes sodium retention with spironolactone/Verospiron.
Glucocorticosteroid drugs and diuretics (benzothiazine derivatives, furosemide, ethacrylic acid) enhance and accelerate the diuretic and natriuretic effects.
Enhances the effect of diuretic and antihypertensive drugs Verospiron. Glucocorticosteroid drugs enhance the diuretic and natriuric effects of hypoalbuminemia and / or hyponatremia.
The risk of developing hyperkalemia increases when taken with potassium preparations, potassium supplements and potassium-sparing diuretics, angiotensin-converting enzyme inhibitors (acidosis), angiotensin II antagonists, aldosterone blockers, indomethacin, cyclosporine.
Salicylates, indomethacin reduce the diuretic effect.
Ammonium chloride, colestyramine contribute to the development of hyperkalemic metabolic acidosis.
Fludrocortisone causes a paradoxical increase in tubular secretion of potassium.
Reduces the effect of mitotan.
Enhances the effect of triptorelin, buserelin, gonadorelin.
Pharmacodynamics Verospiron:
Spironolactone is a potassium-sparing diuretic Verospiron, prolonged action, a competitive antagonist of aldosterone (mineralocorticosteroid hormone of the adrenal cortex). In the distal nephron, spironolactone prevents the aldosterone from retaining sodium and water and inhibits the potassium-excreting effect of aldosterone, reduces the synthesis of permeases in the aldosterone-dependent portion of the collecting tubules and distal tubules. By 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.
The hypotensive effect of the drug Verospiron is due to the presence of a diuretic effect; diuretic effect is manifested on 2-5 days of treatment.
Pharmacokinetics Verospiron:
When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract; bioavailability of almost 100%, and food intake increases it to 100%; communication with plasma proteins about 98%. After a daily dose of 100 mg for 15 days, the maximum concentration (Cmax) is 80 ng / ml, the time to reach the maximum
concentration in plasma (TCmax) after the next morning intake - 2-6 hours.
During biotransformation, active sulfur-containing metabolites of 7-alpha-thiomethylspironolactone and canrenone are formed in the liver. Canrenone reaches Cmax after 2-4 hours, its connection with blood plasma proteins is 90%.
Spironolactone penetrates poorly into organs and tissues, while itself and its metabolites penetrate through the placental barrier, and canrenone into breast milk. Distribution volume - 0,05 l / kg.
The half-life (T1 / 2) is 13-24 hours.
It is excreted by the kidneys: 50% - in the form of metabolites, 10% - unchanged and partially through the intestines. Excretion of canrenone (mainly by the kidneys) is two-phase, T1 / 2 in the first phase - 2-3 hours, in the second -12-96 hours.
With cirrhosis of the liver and heart failure, the duration of T1 / 2 increases without signs of cumulation, the probability of which is higher in chronic renal failure and hyperkalemia.
Indications Verospiron:
- essential hypertension (as part of combination therapy);
- edema syndrome in chronic heart failure (can be used as monotherapy and 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, as well as other conditions accompanied by edema;
- hypokalemia / hypomagnesemia (as an aid to its prevention during treatment with diuretics and when it is impossible to use other methods of correction of potassium concentration);
- primary hyperaldosteronism (Conn syndrome) - for a short preoperative course of treatment;
- to establish a diagnosis of primary hyperaldosteronism.
- Verospiron
Contraindications Verospiron:
Hypersensitivity to any of the components of the drug Verospiron, 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, children age (up to 3 years) for this dosage form.
Carefully:
Hypercalcemia, metabolic acidosis, atrioventricular block (hyperkalemia contributes to its strengthening); diabetes mellitus (with confirmed or suspected chronic renal failure); diabetic nephropathy; surgical interventions; taking medicines that cause gynecomastia; local and general anesthesia; elderly age, menstrual irregularities, liver failure, cirrhosis.
Pregnancy and lactation:
Veroshpiron is contraindicated in pregnancy and lactation.
Verospiron
Overdose Verospiron:
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 metabolism using potassium-releasing diuretics Verospiron, rapid parenteral administration of a dextrose solution (5-20% solutions) with insulin at the rate of 0.25-0.5 PIECES per 1 g of dextrose; if necessary, you can re-enter. In severe cases, hemodialysis is performed.
Side effects Verospiron:
From the gastrointestinal tract: nausea, vomiting, diarrhea, ulceration and bleeding from the gastrointestinal tract, gastritis, intestinal colic, abdominal pain, constipation.
From the liver: impaired liver function.
From the central nervous system: ataxia, lethargy, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm.
From the hematopoietic system: agranulocytosis, thrombocytopenia, megaloblastosis.
On the part of laboratory parameters: hyperuricemia, hypercreatininemia, increased urea concentration, impaired water-salt metabolism (hyperkalemia, hyponatremia) and acid-base balance (metabolic hyperchloremic acidosis or alkalosis). Verospiron
From the endocrine system: coarsening of the voice, in men - gynecomastia (the likelihood of development depends on the dose, duration of treatment and, usually, is reversible and after discontinuation of Veroshpiron disappears, only in rare cases the mammary gland remains slightly increased), decreased potency and erection; in women - menstrual irregularities, dysmenorrhea, amenorrhea, menorrhagia in the menopause, hirsutism, pain in the area of the mammary glands, breast cancer (no connection with the drug Verospiron has been established).
Allergic reactions: urticaria, rarely maculopapular and erythematous rash, drug fever, pruritus.
From the skin: alopecia, hypertrichosis.
From the urinary system: acute renal failure.
From the musculoskeletal system: spasms of the calf muscles.
Ways of application Verospiron:
Inside.
With essential hypertension
The daily dose for adults is usually 50-100 mg once and can be increased to 200 mg, and the dose should be increased gradually, once every 2 weeks.
To achieve an adequate response to therapy, the drug Verospiron must be taken for at least 2 weeks. If necessary, adjust the dose.
With idiopathic hyperaldosteronism: 100-400 mg / day.
With severe hyperaldosteronism and hypokalemia: 300 mg / day (maximum 400 mg) in 2-3 doses, with improvement, the dose is gradually reduced to 25 mg / day.
Hypokalemia / hypomagnesemia
With hypokalemia and / or hypomagnesemia caused by diuretic therapy, a drug 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.
Diagnosis and treatment of primary hyperaldosteronism
As a diagnostic tool for a short diagnostic test: 400 mg / day for 4 days, distributed into several doses per day. With an increase in the concentration of potassium in the blood while taking the drug Verospiron and a decrease after cancellation, it can be assumed that there is primary hyperaldosteronism.
With a long diagnostic test: in the same dose for 3-4 weeks. When correction of hypokalemia and arterial hypertension is achieved, primary hyperaldosteronism can be assumed.
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, divided into 1-4 doses per day during the entire period of preparation for a surgical operation. If the operation is not indicated, then Veroshpiron is used for long-term maintenance therapy, while the lowest effective dose is used, which is selected individually for each patient.
Edema on the background of nephrotic syndrome
The daily dose for adults is usually 100-200 mg / day. No effect of spironolactone on the main pathological process was detected, and therefore the use of this drug Verospiron is recommended only in cases where other types of therapy are ineffective.
With edematous syndrome against the background of chronic heart failure, daily, for 5 days, 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 is 200 mg / day.
Swelling against cirrhosis
If in urine the ratio of sodium and potassium ions (Na + / K +) exceeds 1.0, then the daily dose for adults is usually 100 mg. If the ratio is less than 1.0, then the daily dose for adults is usually 200-400 mg. The maintenance dose is selected individually.
In children
The initial dose Verospiron is 1-3.3 mg / kg body weight or 30-90 mg / m2 / day in 1-4 doses.
After 5 days, the dose is adjusted and, if necessary, increased by 3 times compared to the original
