Veroshpilakton-OBL pills 25mg N20
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Active ingredients
Spironolactone
Release form
Pills
Composition
Spironolactone 25 mg. Adjuvants: Povidone - 5 mg, lactose monohydrate - 70 mg, potato starch - 52 mg, colloidal silicon dioxide (aerosil) - 2 mg, sodium lauryl sulfate - 2.6 mg, talc - 1.6 mg, magnesium stearate - 1.6 mg. Composition capsule body and caps: titanium dioxide - 2%, gelatin - up to 100%.
Pharmacological effect
Potassium-sparing diuretic, a specific antagonist of aldosterone (mineralocorticosteroid hormone of the adrenal cortex) prolonged action. In the distal parts of the nephron, spironolactone prevents 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 increased urine output is due to the presence of a diuretic effect, which is not constant. The diuretic effect is manifested at 2-5 days of treatment.
Pharmacokinetics
Absorption and distributionIf ingestion is quickly and completely absorbed from the gastrointestinal tract. Plasma protein binding is approximately 98% (canrenon 90%). Cmax of plasma cannonone is achieved 2–4 hours after exposure. After daily intake of spironolactone at a dose of 100 mg for 15 days, Cmax is 80 ng / ml, the time to reach Cmax after the next morning dose is 2–6 hours. Vd - 0, 05 l / kg. MetabolismSpyronolactone is converted into active metabolites: a metabolite containing sulfur (80%), and partly canrenone (20%). Spironolactone penetrates poorly into organs and tissues, while itself and its metabolites penetrate the placental barrier and canrenone into breast milk. Excretion is excreted by the kidneys: 50% in the form of metabolites, 10% in unchanged form and partially through the intestines. T1 / 2 spironolactone is 13-24 h, active metabolites - up to 15 h. Cannarone excretion (mainly by the kidneys) is two-phase, T1 / 2 in the first phase - 2-3 h, in the second - 12-96 h. Pharmacokinetics in special clinical In cases of liver cirrhosis and heart failure, the duration of T1 / 2 increases without signs of cumulation, the likelihood 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 in monotherapy and in combination with standard therapy); conditions in which secondary hyper aldosteronism can be detected, including cirrhosis of the liver, accompanied by ascites and / or edema , nephrotic syndrome, as well as other conditions associated with edema; - hypokalemia / hypomagnesia (as an aid to its prevention during treatment with diuretics and when not POSSIBILITY use other methods of potassium correction) - primary hyperaldosteronism (Conn syndrome) - short for preoperative treatment - for the diagnosis of primary hyperaldosteronism.
Contraindications
- hypersensitivity to the components of the drug; - Addison's disease; - hyperkalemia; - hyponatremia; - severe renal failure (CK <10 ml / min); - anuria; - diabetes mellitus with confirmed renal insufficiency; - simultaneous use of eplerenone and other potassium-sparing diuretics , potassium preparations; - pregnancy; - lactation period (breastfeeding); - children's age up to 3 years (for solid dosage form); - lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome (tons . Of the drug is included lactose monohydrate) .With caution: hypercalcemia, metabolic acidosis, AV-block (hyperkalemia promotes its strengthening); diabetes mellitus (with confirmed or suspected chronic renal failure); diabetic nephropathy; surgical interventions during anesthesia; medication that causes gynecomastia; local and general anesthesia; violation of the menstrual cycle, breast enlargement; liver failure, liver cirrhosis; elderly age.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects.The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
The use of the drug Veroshpilakton contraindicated during pregnancy and during breastfeeding. Spironolactone and its metabolites can penetrate the placental barrier. Spironolactone metabolites are found in breast milk. If necessary, the use of the drug during lactation breastfeeding should be discontinued.
Dosage and administration
The drug is taken orally. Tablets are taken after a meal. Essential hypertension The daily dose for adults is usually 50-100 mg 1 time / day and can be increased to 200 mg, while increasing the dose gradually, 1 time in 2 weeks. To achieve an adequate response to therapy, the drug must be taken at least 2 weeks. If necessary, adjust the dose. Idiopathic hyperaldosteronism Assign a dose of 100-400 mg / day. Severe hyper aldosteronism and hypokalemia Appoint a dose of 300 mg / day (maximum 400 mg / day) for 2-3 doses, while improving the state, the dose is gradually reduced to 25 mg / sut. Hypopotassemia and / or hypomagnesemia In case of hypokalemia and / or hypomagnesemia caused by diuretic therapy, the drug is prescribed in a dose of 25-100 mg / day, once or in several doses. The maximum daily dose of 400 mg, if potassium preparations for oral administration or other methods to fill its deficiency are ineffective. Diagnosis and treatment of primary hyperaldosteronism As a diagnostic tool with a short diagnostic test: 400 mg / day in several doses per day, for 4 days. With an increase in the content of potassium in the blood while taking the drug and a decrease after its cancellation, we can assume the presence of primary hyperaldosteronism. With a long diagnostic test: at the same dose for 3-4 weeks. When attaining correction of hypokalemia and arterial hypertension, it is possible to assume the presence of primary hyper aldosteronism. A short course of preoperative therapy of primary hyper aldosteronism preparation for surgery.If surgery is not shown, the drug Veroshpilakton is used for long-term maintenance therapy, and the smallest effective dose should be applied, which is selected individually for each patient. Edema against nephrotic syndrome The daily dose for adults is usually 100-200 mg / day. No effect of spironolactone on the main pathological process has been identified, and therefore the use of this drug is recommended only in cases when other therapies are ineffective. Discharge syndrome against the background of chronic heart failure Assign 100-200 mg / day in 2-3 doses, daily for 5 days, in combination with a loop or thiazide diuretic. Depending on the effect, the daily dose is reduced to 25 mg. Maintenance dose is selected individually. The maximum dose is 200 mg / day. Edema against cirrhosis of the liver If the ratio of sodium and potassium ions (Na + / K +) in urine 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. Children With edema in children over 3 years old, the initial dose is 1-3.3 mg / kg of 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 with the original.
Side effects
On the part of the digestive system: nausea, vomiting, diarrhea, ulceration and bleeding from the gastrointestinal tract, gastritis, intestinal colic, abdominal pain, constipation. On the liver: impaired liver function. On the nervous system: ataxia, lethargy, dizziness, headache, drowsiness, lethargy, confusion, muscle spasm. From the hematopoietic system: agranulocytosis, thrombocytopenia, megaloblastosis. From the laboratory indicators: hyperuricemia, hypercreatininemia, increased urea concentration, impaired water-electrolyte balance (hyperkalemia, hyponatremia) and acid-base status (metabolic hyperchloremic acidosis or alkalosis). From the endocrine system: coarsening of the voice, in men - gynecomastia (the likelihood of development depends on the dose, duration of treatment and is usually reversible, and drug disappears,and only in rare cases, the mammary gland remains somewhat enlarged), reducing potency and erection; in women - menstrual disorders, dysmenorrhea, amenorrhea, metrorrhagia during menopause, hirsutism, pain in the mammary gland, breast carcinoma (connection with the drug is not installed). fever, pruritus, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis. On the side of the skin and subcutaneous tissues: alopecia, hypertrichosis. On the part of the kidneys and urinary tract: acute renal failure. on the part of the musculoskeletal system: leg cramps, osteomalyatsiya.So the respiratory system: odyshka.Esli any of the adverse reactions listed above are compounded, or any other undesirable effects, the patient should inform the doctor.
Overdose
Symptoms: nausea, vomiting, dizziness, diarrhea, skin rash, hyperkalemia (paresthesias, muscle weakness, arrhythmias), hyponatremia (dryness of the oral mucosa, thirst, drowsiness) hypercalcemia, dehydration, increase in urea concentration. dehydration. In case of hyperkalemia, it is necessary to normalize the water-electrolyte balance with the help of potassium-withdrawing diuretics, rapid parenteral administration of a 5-20% dextrose solution (glucose) with insulin at the rate of 0.25-0.5 IU per 1 g of dextrose (glucose); if necessary, you can re-enter. In severe cases, hemodialysis is performed.
Interaction with other drugs
Spironolactone reduces the effects of anticoagulants, indirect anticoagulants (heparin, coumarin derivatives, indandion) and cardiac glycosides toxicity (because normalization of potassium in the blood prevents the development of toxicity). Strengthens phenazone (antipyrin) metabolism. anesthesia), increases T1 / 2 digoxin - possible digoxin intoxication. Strengthens the toxic effect of lithium due to a decrease in clearance. Possibly enhances the effect of non-depolarium muscle relaxants (for example,tubocurarine). Accelerates metabolism and excretion of carbenoxolone. Carbenoxolone contributes to the retention of sodium by spironolactone. GCS and diuretics (thiazides and thiazide-like, furosemide, ethacrynic acid) strengthen and accelerate diuretic and natriuretic effects. , increases the risk of hyperkalemia. Alcohol (ethanol), barbiturates, narcotic substances increase orthostatic hypotension. t-diuretic and natriuretic reduce the diuretic effect of spironolactone. Ammonium chloride, colestyramine promote the development of hyperkalemic metabolic acidosis. Fludrocortisone causes paradoxical enhancement of tubular secretion of potassium. Spironolactone reduces the effect of mitotane. Enhances the effects of triptorelin, buserelin, gonadorelin.
special instructions
Perhaps a temporary increase in the urea nitrogen content in the blood serum, especially with reduced kidney function and hyperkalemia. Reversible hyperchloremic metabolic acidosis is possible. Regular monitoring of electrolytes in the blood serum and kidney function is necessary in cases of impaired renal and liver function, as well as in elderly patients. The preparation makes it difficult to determine digoxin, cortisol and adrenaline in the blood. Despite the lack of a direct effect on carbohydrate metabolism, the presence of diabetes, especially diabetic nephropic Attire, it requires special care because of the possibility of developing hyperkalemia. With simultaneous treatment of NSAIDs, kidney function and electrolyte levels in the blood should be monitored. Eating foods rich in potassium should be avoided. Alcohol consumption is contraindicated during treatment. Impact on the ability to drive vehicles and control mechanisms Patients should be careful when driving and working with mechanisms that require increased concentration of attention and responsiveness (risk of dizziness and drowsiness) .