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Active ingredients
Torasemide
Release form
Pills
Composition
1 tablet contains: Active substances: Torsemide - 5 mg.; Excipients: lactose monohydrate - 58.44 mg, corn starch - 14.56 mg, carboxymethyl starch sodium - 0.8 mg, anhydrous colloidal silicon dioxide - 0.6 mg, magnesium stearate - 0.6 mg.
Pharmacological effect
"Loopback" diuretic. The main mechanism of the drug's action is due to the reversible binding of Torsemide to the Na + / 2Cl- / K + co-transporter located in the apical membrane of the thick segment of the ascending part of the loop of Henle. As a result, the reabsorption of sodium ions is reduced or completely inhibited and the osmotic pressure of the intracellular fluid and water reabsorption are reduced. Blocks aldosterone receptors in the myocardium, reduces fibrosis and improves the diastolic function of the myocardium. Torsemide, to a lesser extent than furosemide, causes hypokalemia, while showing greater activity and its action is more prolonged. inside.; Torsemide can be applied for a long time.
Pharmacokinetics
After ingestion, Torsemide is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax of Torsemide in plasma is achieved within 1-2 hours after taking the drug inside after eating. Bioavailability - 80-90% with minor individual variations.; Distribution; Plasma protein binding - more than 99%. Visible Vd is 16 liters.; Metabolism and excretion; Metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system. As a result of successive reactions of oxidation, hydroxylation or ring hydroxylation, 3 metabolites are formed (M1, M3 and M5), the binding of which to plasma proteins is 86%, 95% and 97%, respectively. T1 / 2 of Torsemide and its metabolites is 3-4 hours and does not change in case of chronic renal failure. Total clearance is 40 ml / min, renal clearance is 10 ml / min. On average, about 83% of the dose taken is excreted by the kidneys: unchanged (24%) and predominantly inactive metabolites (M1 - 12%, M3 - 3 %, M5 - 41%); Pharmacokinetics in special clinical situations; In renal failure, T1 / 2 of Torsemide does not change, T1 / 2 of the metabolites M3 and M5 increases.Torasemide and its metabolites are slightly excreted by hemodialysis and hemofiltration. In liver failure, the concentration of Torsemide in the blood plasma increases due to a decrease in the metabolism of the drug in the liver. In patients with cardiac or hepatic insufficiency, the T1 / 2 of Torsemide and the metabolite M5 are slightly increased, the drug is unlikely to accumulate.
Indications
- edematous syndrome of various genesis, including in chronic heart failure, liver, kidney and lung diseases; - arterial hypertension.
Contraindications
- hypersensitivity to Torsemide; - renal failure with anuria; - hepatic coma and precoma; - severe hypokalemia; - severe hyponatremia; - hypovolemia (with or without arterial hypotension) or dehydration; - pronounced violations of the outflow of urine of any etiology (including unilateral damage to the urinary tract); - glycoside intoxication; - acute glomerulonephritis; - decompensated aortic and mitral stenosis; - hypertrophic obstructive cardiomyopathy; - increase in central venous pressure (more than 10 mm Hg); - hyperuricemia; - age up to 18 years; - lactation period; - lactose intolerance, lactase deficiency, glucose-galactose malabsorption; - hypersensitivity to the drug; Apt to treat sulphonamides (sulphonamide) or to treat sulphonic history of arrhythmias, acute myocardial infarction (increased risk of cardiogenic shock), diarrhea, pancreatitis, sa Chronic diabetes (decreased glucose tolerance), hepatorenal syndrome, gout, anemia, pregnancy.
Use during pregnancy and lactation
In pregnancy, Diuver can be used only when the potential benefit to the mother outweighs the possible risk to the fetus, only under the supervision of a physician and only in minimal doses.; metabolism and thrombocytopenia in the fetus. It is not known whether Torsemide is excreted in breast milk.If necessary, the use of the drug Diuver during lactation should stop breastfeeding.
Dosage and administration
The drug is taken orally 1 time / day after breakfast, with a small amount of water.; Edema syndrome of various origins, including with chronic heart failure, liver, lung and kidney diseases; The therapeutic dose is 5 mg 1 time / day. If necessary, the dose should be gradually increased to 20-40 mg 1 time / day, in some cases - up to 200 mg / day. The drug is prescribed for a long period or until the edema disappears; Arterial hypertension; The initial dose is 2.5 mg (1/2 tab. 5 mg) 1 time / day. If necessary, the dose can be increased up to 5 mg 1 time / day; For elderly patients, dose adjustment is not required.
Side effects
From the side of water-electrolyte and acid-base balance: hyponatremia, hypochloremia, hypokalemia, hypomagnesemia, hypocalcemia, metabolic alkalosis. Symptoms that indicate the development of electrolyte and acid-base disorders can be headache, confusion, convulsions, tetany, muscle weakness, heart rhythm disturbances, and dyspepsia disorders; hypovolemia and dehydration (often in elderly patients), which can lead to hemoconcentration with a tendency to develop thrombosis. From the side of the cardiovascular system: excessive blood pressure reduction, orthostatic hypotension, collapse, tachycardia, arrhythmias, reduced BCC. substances: hypercholesterolemia, hypertriglyceridemia; a transient increase in the concentration of creatinine and urea in the blood; increasing the concentration of uric acid in the blood, which can cause or increase the manifestations of gout; decrease in glucose tolerance (latent diabetes mellitus may manifest itself); From the urinary system: oliguria, acute urinary retention (for example, with prostatic hyperplasia, narrowing of the urethra, hydronephrosis); interstitial nephritis, hematuria, reduced potency. On the part of the digestive system: nausea, vomiting, diarrhea, intrahepatic cholestasis, increased liver enzymes, acute pancreatitis. earsespecially in patients with renal insufficiency or hypoproteinaemia (nephrotic syndrome), paresthesia; For the skin:. pruritus, urticaria, other rashes or bullous skin lesions, erythema multiforme, exfoliative dermatitis, purpura, fever, vasculitis, eosinophilia, photosensitivity; severe anaphylactic or anaphylactoid reactions up to shock, which until now have been described only after IV injection; On the part of peripheral blood: thrombocytopenia, leukopenia, agranulocytosis, aplastic or hemolytic anemia.
Overdose
Symptoms: excessively increased diuresis, accompanied by a decrease in BCC and impaired electrolyte balance in the blood, followed by a pronounced decrease in blood pressure, drowsiness, confusion, collapse; gastrointestinal disorders are possible.; Treatment: there is no specific antidote. It should induce vomiting, gastric lavage, appoint activated charcoal. Dose reduction or withdrawal of the drug and at the same time replenishment of the BCC and indicators of water and electrolyte balance and acid-base balance under the control of serum electrolyte concentrations, hematocrit, symptomatic treatment. Hemodialysis is ineffective.
Interaction with other drugs
Torsemide increases the concentration and risk of nephrotoxic and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid, cisplatin, amphotericin B (due to competitive renal excretion); Torsemide increases the effectiveness of diazoxide and theophylline, reduces the effectiveness of hypoglycemic agents, allopurin-iuropurin. Torsemide mutually reduce the effectiveness.; Drugs that block tubular secretion, increase the concentration of Torsemide in the blood serum.; With simultaneous With GCS, amphotericin B increases the risk of hypokalemia, with cardiac glycosides - increases the risk of glycoside intoxication due to hypokalemia (for high and low polar) and T1 / 2 lengthening (for low polar); Torsemide reduces renal clearance of lithium and increases the likelihood of intoxication .; NSAIDs, sucralfat reduce the diuretic effect due to inhibition of prostaglandin synthesis,impaired renin activity in blood plasma and aldosterone elimination.; Torsemide enhances the hypotensive effect of antihypertensive agents, neuromuscular blockade of depolarizing muscle relaxants (suxametonium) and weakens the effect of non-depolarizing muscle relaxants (tubocurarine); manifestations of their toxicity (due to competitive renal excretion); Sequential or simultaneous use of Torsemide with ACE inhibitors or anta angiotensin II receptor receptors can lead to a strong decrease in blood pressure. This can be avoided by reducing the dose of Torsemide or by temporarily canceling it. If used simultaneously with probenecid or methotrexate, the effectiveness of Torsemide may decrease (the same secretion route). On the other hand, Torsemide can reduce the renal elimination of these drugs. With the simultaneous use of cyclosporine and Torsemide, the risk of developing gouty arthritis is increased due to the fact that cyclosporine can cause a violation of urate excretion by the kidneys and Torsemide - hyperuricemia high risk of nephropathy, receiving Torsemide orally, with the introduction of radiopaque means of renal dysfunction were observed more often than in patients with high risk of developed Nephropathy, which prior to the introduction of radiopaque agents was carried out in / in hydration.
special instructions
Apply strictly on doctor's prescription.; The diuretic effect lasts up to 18 hours, it facilitates tolerability of therapy due to the lack of very frequent urination in the first hours after taking the drug inside, which limits the activity of patients.; Patients with hypersensitivity to sulfonylureas can have a cross sensitivity to the drug Diuver.; Patients receiving high doses of the drug Diuver for a long period, in order to avoid the development of hyponatremia, metabolic alk sham and hypokalemia, a diet with a sufficient content of sodium chloride and the use of potassium preparations are recommended.; An increased risk of developing disorders of water and electrolyte balance is observed in patients with renal insufficiency.During the course of treatment, it is necessary to periodically monitor the concentration of electrolytes in the blood plasma (including sodium, calcium, potassium, magnesium), acid-base state, residual nitrogen, creatinine, uric acid, and, if necessary, carry out appropriate corrective therapy (with a higher frequency in patients with frequent vomiting and parenterally administered fluids); With the onset or increase of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended that treatment be suspended. dosing in patients with ascites against the background of cirrhosis should be carried out in a hospital setting (disruption of water and electrolyte balance may lead to the development of hepatic coma). Regular monitoring of plasma electrolytes is shown in this category of patients. In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of glucose in the blood and urine is required. In unconscious patients with prostatic hyperplasia, urethral contraction is necessary to control diuresis due to with the possibility of acute urinary retention.; Impact on the ability to drive vehicles and control mechanisms; During treatment, patients should refrain from driving REMEDIES and busy with other potentially hazardous activities that require high concentration and psychomotor speed reactions.