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Active ingredients
Spironolactone
Release form
Pills
Composition
Active ingredient: Spironolactone (Spironolactone). Concentration of active ingredient (mg): 25
Pharmacological effect
In the instructions to Verospiron the drug is described as a potassium-sparing diuretic. The main active ingredient competes with aldosterone (the hormone of the adrenal cortex) and inhibits its action. Na +, Cl- and water are not absorbed back into the renal tubules, and K + and urea, on the contrary, penetrate the endothelium of the glomerulus into the blood. Increased urination causes a decrease in blood pressure and the disappearance of edema. The diuretic effect is manifested only 3-5 days after the first day of taking the drug. Verospiron does not significantly affect the function of the renal tubules and does not lead to acid-base imbalance of the body.
Pharmacokinetics
When ingestion is quickly and completely absorbed from the gastrointestinal tract; bioavailability of almost 100%, and prim food increases it to 100%; communication with plasma proteins is about 98%. After a daily dose of 100 mg for 15 days, the maximum concentration (Cax) is 80 ng / ml, the time to reach the maximum plasma concentration (TCmax) after the next morning dose is 2-6 hours. During the biotransformation process, active sulfur-containing metabolites are formed in the liver 7 -alpha-thiomethylspironolactone and canrenone. Canrenone reaches Cmax after 2–4 h, its association with plasma proteins is 90%. Spironolactone penetrates poorly into organs and tissues, while itself and its metabolites penetrate the placental barrier, and canrenone - into breast milk. Distribution volume - 0.05 l / kg. The elimination half-life is (T1 / 2) -13-24 h. Excreted by the kidneys: 50% - in the form of metabolites, 10% - in unchanged form and partially through the intestines. Cranrenon excretion (mainly by the kidneys) is biphasic, T1 / 2 in the first phase - 2-3 hours, in the second - 12-96 hours. With liver cirrhosis and heart failure, the duration of T1 / 2 increases without signs of cumulation, the probability of which is higher in chronic renal deficiency and hyperkalemia.
Indications
Edematous syndrome in chronic heart failure, cirrhosis of the liver, nephrotic syndrome, essential hypertension (in adults), primary hyperaldosteronism (to clarify the diagnosis and short-term preoperative treatment), prevention of hypokalemia in the treatment with saluretics, ascites.
Contraindications
Addison's Disease.Acute renal failure, chronic renal failure with a significant decrease in excretory function (CK less than 10 ml min), anuria, hyperkalemia, hyponatremia, pregnancy, lactation (breastfeeding), hypersensitivity to spironolactone and other components of the drug.
Precautionary measures
In case of intolerance of milk sugar (lactose), it should be taken into account that each tablet of Verospiron 25 mg contains 146 mg of milk sugar (lactose monohydrate), each capsule of Verospiron 50 mg contains 127.5 mg of milk sugar, each capsule of Verospiron 100 mg contains 255 mg of milk sugar.
Use during pregnancy and lactation
Before you start taking any drug, talk with your doctor or pharmacist. Verospiron is contraindicated during pregnancy and during breastfeeding.
Dosage and administration
When edematous syndrome in chronic heart failure, the drug is prescribed to adults in the initial daily dose of 25 mg. The maximum dose is 100 mg days. Maintenance dose is determined individually. In case of edema syndrome in case of liver cirrhosis, the drug is prescribed in a dose of 100-400 mg / day (depending on the ratio of potassium and sodium). Maintenance dose is determined individually. When edematous syndrome in nephrotic syndrome, the drug is prescribed in a dose of 100-200 mg / day. With essential hypertension, the initial daily dose is 50-100 mg (divided into several doses). If necessary, the daily dose is gradually increased to 200 mg over 2 weeks. Duration of treatment for at least 2 weeks. For the prevention of hypokalemia caused by taking saluretiki, Verospiron is used in a daily dose of 25-100 mg. Verospiron can be used for initial diagnosis as an indirect indicator of primary aldosteronism in patients on a normal diet. To do this, conduct tests. Long test: adults Verospiron prescribed in a daily dose of 400 mg for 3-4 weeks. The elimination of hypokalemia and hypertension indirectly indicates primary hyperaldosteronism. Short test: Verospiron prescribed in a daily dose of 400 mg for 4 days. If, during the period of taking the drug, the concentration of potassium in the blood serum increases and decreases with the cancellation of Verospiron, the result may indirectly indicate primary hyperaldosteronism.After the diagnosis of hyper aldosteronism is made using more informative diagnostic tests, Verospiron can be prescribed in preparation for surgery at a dose of 100-400 mg / day. In patients not subject to surgery, Verospiron can be used as a long-term maintenance therapy in the lowest effective doses, which are set individually. Children are prescribed the drug in a daily dose at the rate of 3 mgkg. Dose picked individually. Reception frequency - 1-2 times a day.
Side effects
On the part of the endocrine system: gynecomastia (usually disappears after drug withdrawal, but in rare cases it may persist), pain in the mammary glands, decreased libido, menstrual disorders. On the part of the digestive system: dyspeptic phenomena (including nausea), abnormal liver function. From the side of the central nervous system: dizziness, weakness, confusion. From the side of water and electrolyte balance: hyperkalemia, electrolyte imbalance. On the part of the hematopoietic system: leukopenia, agranulocytosis, thrombocytopenia Dermatological reactions: alopecia, hypertrichosis, urticaria, pruritus, rash. Other: cramps of the calf muscles.
Overdose
According to reviews of Verospiron patients, drug overdose occurs extremely rarely. In case of its occurrence, all side effects of the drug are exacerbated. An urgent need to flush the stomach, consume a large amount of liquid and caffeine to increase blood pressure. For hyperkalemia, the doctor prescribes dextrose and insulin.
Interaction with other drugs
Please inform your doctor or pharmacist if you are taking or have recently taken any other drugs, including over-the-counter drugs. While taking the drug Verospiron with the following drugs, it is possible to change the effects of drugs: for example, other diuretics (diuretics), cholestyramine, ammonium chloride, hypnotics, some vasoconstrictor drugs (vasoconstrictors), some steroidal anti-inflammatory drugs (glucocorticosteroids), drugs to reduce blood pressure (antihypertensives), potassium, lithium, carbamazepine, some nonsteroidal anti-inflammatory drugs - NSAIDs (for example, acetylsalicylic acid, indomethacin, mefenamic acid), digoxin, carbenoxolone, drugs that prevent the formation of blood clots (anticoagulants), some anticancer drugs (triptorelin, buserelin, gonadorelin, cyclosporine, tacrolimus).
special instructions
Management of motor transport and other mechanisms. At the beginning of treatment, you should abandon driving and working with dangerous machinery for a period of time, the duration of which is determined individually. In the future, the doctor will decide on this restriction.