Dosage form:
Capsules 100 mg: Content of the capsule: fine-grained granular powder mixture of white color.
Capsule: hard gelatin, size No.0; Cap: opaque, orange; Case: opaque, yellow.
Structure:
100 mg capsules
Active ingredient: spironolactone - 100.00 mg.
Excipients in the capsule: sodium lauryl sulfate - 5.00 mg; magnesium stearate -5.00 mg; corn starch - 85.00 mg; lactose monohydrate - 255.00 mg.
Hard gelatin capsule:
Size No. 0.
Cap: sunset yellow dye E110 - 0.04%; titanium dioxide E 171 - 2.00%; gelatin - up to 100%.
Case: dye sunny sunset yellow E 110 - 0.04%; titanium dioxide E 171 -2.00%, dye quinoline yellow E 104 - 0.50%; gelatin - up to 100%.
general description
Potassium-sparing diuretic
Special conditions:
When using Veroshpiron, a temporary increase in the level of urea nitrogen in the blood serum is possible, especially with reduced renal function and hyperkalemia. The development of reversible hyperchloremic metabolic acidosis is also possible.
When prescribing Veroshpiron to patients with impaired renal and hepatic function, elderly patients require regular monitoring of serum electrolytes and renal function.
Reception of Veroshpiron makes it difficult to determine the concentration of digoxin, cortisol and adrenaline in the blood.
Despite the lack of a direct effect on carbohydrate metabolism, the presence of diabetes mellitus, especially with diabetic nephropathy, requires special care when prescribing Veroshpiron because of the possibility of developing hyperkalemia.
In the treatment of NSAIDs while taking Veroshpiron, kidney function and blood electrolyte levels should be monitored.
During treatment with Veroshpiron, alcohol is contraindicated, and potassium-rich foods should be avoided.
During treatment, alcohol is contraindicated.
Influence on the ability to drive vehicles and control mechanisms
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:
Veroshpiron 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.
Reduces vascular sensitivity to norepinephrine (requires caution when conducting anesthesia).
Increases T1 / 2 of digoxin, therefore 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.
GCS and diuretics (benzothiazine derivatives, furosemide, ethacrylic acid) enhance and accelerate the diuretic and natriuretic effects.
Enhances the effect of diuretic and antihypertensive drugs.
GCS enhance the diuretic and natriuric effect in case of hypoalbuminemia and / or hyponatremia.
Pharmacodynamics:
Potassium-sparing diuretic, a competitive aldosterone antagonist.
In the distal nephron, spironolactone prevents the aldosterone retention of sodium and water and suppresses the potassium-eliminating 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 antihypertensive effect is due to the diuretic effect. The diuretic effect is manifested on 2-5 days of treatment.
Pharmacokinetics:
Suction
After oral administration, it is rapidly and completely absorbed from the digestive tract. Bioavailability is about 100%, and food intake increases it to 100%. After a daily dose of 100 mg of spironolactone for 15 days, Cmax is 80 ng / ml, the time to reach Cmax after the next morning dose is 2-6 hours.
Distribution
Plasma protein binding is 98%.
Spironolactone penetrates poorly into organs and tissues, while spironolactone and its metabolites penetrate the placental barrier, and canrenone - into breast milk. Vd - 0.05 l / kg.
Metabolism
During biotransformation, active sulfur-containing metabolites of 7-alpha-thiomethylspironolactone and canrenone are formed in the liver. Canrenone reaches its Cmax after 2-4 hours, its binding to plasma proteins is 90%.
Breeding
T1 / 2 - 13-24 hours. It is excreted mainly 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.
Pharmacokinetics in special clinical cases
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:
- 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 and 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 levels);
- primary hyperaldosteronism (Conn's syndrome) - for a short preoperative course of treatment;
- to establish a diagnosis of primary hyperaldosteronism.
Contraindications:
- Addison's disease;
- hyperkalemia;
- hyponatremia;
- severe renal failure (CC less than 10 ml / min);
- anuria;
- lactose intolerance, lactase deficiency, glucose / galactose malabsorption syndrome;
- pregnancy;
- lactation (breastfeeding);
- children's age up to 3 years;
- Hypersensitivity to the components of the drug.
With caution, the drug should be prescribed for hypercalcemia, metabolic acidosis, AV block (hyperkalemia enhances it), diabetes mellitus (with confirmed or suspected chronic renal failure), diabetic nephropathy, surgical interventions, taking medications that cause gynecomastia, local and general anesthesia, menstrual irregularities, liver failure, cirrhosis, as well as elderly patients.
Overdose:
nausea, vomiting, dizziness, decreased blood pressure, diarrhea, skin rash, hyperkalemia (paresthesia, muscle weakness, arrhythmias), hyponatremia (dry mouth, thirst, drowsiness), hypercalcemia, dehydration, increased urea concentration
Side effects:
From the digestive system: nausea, vomiting, diarrhea, ulceration and bleeding from the digestive tract, gastritis, intestinal colic, abdominal pain, constipation, impaired liver function
From the side of the central nervous system and peripheral nervous system: ataxia, lethargy, dizziness, headache, drowsiness, lethargy, confusion.
From the side of the hematopoietic system: agranulocytosis, thrombocytopenia, megaloblastosis.
From the side of metabolism: hyperuricemia, hypercreatininemia, increased urea concentration, hyperkalemia, hyponatremia, metabolic hyperchloremic acidosis or alkalosis.
On the part of the endocrine system: coarsening of the voice, in men - gynecomastia (the probability of development depends on the dose, duration of treatment and usually is reversible and after discontinuation of Veroshpiron disappears, only in rare cases the breast remains slightly increased), decreased potency and erection; in women - menstrual irregularities, dysmenorrhea, amenorrhea, menorrhagia in the menopause, hirsutism, pain in the mammary gland, breast carcinoma (no connection with the drug has been established).
Allergic reactions: urticaria; rarely, maculopapular and erythematous rash, drug fever, pruritus.
Dermatological reactions: alopecia, hypertrichosis.
From the urinary system: acute renal failure.
From the musculoskeletal system: muscle spasm, spasms of the calf muscles.
Ways of application:
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 must be taken for at least 2 weeks. If necessary, carry out dose adjustment.
With idiopathic hyperaldosteronism, the drug is prescribed in a dose of 100-400 mg /
With severe hyperaldosteronism and hypokalemia, the daily dose is 300 mg (maximum 400 mg) in 2-3 doses, with improvement, the dose is gradually reduced to 25 mg /
With hypokalemia and / or hypomagnesemia caused by diuretic therapy, Veroshpiron is prescribed at a dose of 25-100 mg /, 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.
In the diagnosis and treatment of primary hyperaldosteronism as a diagnostic tool with a short diagnostic test, Veroshpiron is prescribed for 4 days at 400 mg /, distributing the daily dose in several doses per day. With an increase in the concentration of potassium in the blood while taking the drug and a decrease after cancellation it can be assumed the presence of primary hyperaldosteronism. With a long diagnostic test, the drug is prescribed in the same dose for 3-4 weeks. When correction of hypokalemia and arterial hypertension is achieved, primary hyperaldosteronism can be assumed.
After the diagnosis of hyperaldosteronism is established using more accurate diagnostic methods, Veroshpiron should be taken in a daily dose of 100-400 mg as a short course of preoperative treatment of primary hyperaldosteronism, dividing it into 1-4 doses throughout the preparation period 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.
In the treatment of edema against the background of nephrotic syndrome, the daily dose for adults is usually 100-200 mg. The effect of spironolactone on the main pathological process has not been identified and therefore the use of this drug is recommended only in cases where other types of therapy are ineffective.
In case of edematous syndrome against the background of chronic heart failure, the drug is prescribed daily for 5 days at 100-200 mg / 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 daily dose is 200 mg.
For edema with cirrhosis of the liver, the daily dose of Veroshpiron for adults is usually 100 mg if the ratio of sodium and potassium ions (Na + / K +) in the urine exceeds 1.0. If the ratio is less than 1.0, then the daily dose is usually 200-400 mg. The maintenance dose is selected individually.
