More info
Active ingredients
Torasemide
Release form
Pills
Composition
Torsemide 10 mg; excipients: lactose monohydrate - 116.88 mg, corn starch - 29.12 mg, carboxymethyl starch sodium - 1.6 mg, anhydrous silicon colloidal dioxide - 1.2 mg, magnesium stearate - 1.2 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 longer .; The maximum diuretic effect develops within 2-3 hours after taking the drug inside .; Torsemide can be used 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 l .; 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. The general clearance makes 40 ml / min., Renal clearance - 10 ml / min .; On average, about 83% of the accepted dose 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, the T1 / 2 of M3 and M5 metabolites increases. Torsemide 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; - Allergy to sulfonamides (sulfanilamide antimicrobial agents or sulfonylurea preparations) .; Precautions should be used for arterial hypotension, cerebral arteries stenosing atherosclerosis, hypoproteinemia, susceptibility to hyperuricemia, violation of urine flow (benign prostatic hyperplasia, restriction of the urethra, or hydronephrosis), gastrointestinal obesity, adult aphroma, anesthesia, etc. , with diarrhea, pancreatitis, diabetes mellitus (decreased glucose tolerance), hepatorenal syndrome, gout, anemia, pregnancy.
Use during pregnancy and lactation
In pregnancy, Diuver can only be used when the potential benefit to the mother exceeds the possible risk to the fetus, only under the supervision of a physician, and only in minimal doses .; Torsemide does not have a teratogenic effect and fetotoxicity, penetrates the placental barrier, causing impaired water-electrolyte 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 once a day after breakfast with a small amount of water; Edematous syndrome of various genesis, incl. 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; Initial dose is 2.5 mg (1/2 tab. 5 mg) 1 time / day. If necessary, the dose can be increased to 5 mg 1 time per day; 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 (more often in elderly patients), which can lead to hemoconcentration with a tendency to develop thrombosis .; On the part of the cardiovascular system: excessive reduction of blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, reduced BCC .; Metabolism: 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 (possible manifestation of latent flowing diabetes mellitus) .; On the part of the urinary system: oliguria, acute urinary retention (for example, with prostatic hyperplasia, narrowing of the urethra, hydronephrosis); interstitial nephritis, hematuria, decreased potency .; On the part of the digestive system: nausea, vomiting, diarrhea, intrahepatic cholestasis, increased activity of liver enzymes, acute pancreatitis .; CNS and organ of hearing: hearing loss, usually reversible, and / or tinnitus,especially in patients with renal failure or hypoproteinemia (nephrotic syndrome), paresthesia .; On the part of the skin: itchy skin, urticaria, other types of rash or bullous skin lesions, erythema multiforme, exfoliative dermatitis, purpura, fever, vasculitis, eosinophilia, photosensitization; severe anaphylactic or anaphylactoid reactions up to shock, which have hitherto been described only after intravenous infusion; From the side 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 disturbances 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, allopurinol .; Pressor amines and Torsemide mutually reduce effectiveness .; Drugs that block tubular secretion, increase the concentration of Torsemide in serum .; With the simultaneous use of 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 elongation (for low polar) .; Torsemide reduces renal clearance of lithium drugs and increases the likelihood of intoxication .; NSAIDs, sucralfat reduce the diuretic effect due to inhibition of prostaglandin synthesis,impaired renin activity in the blood plasma and removal of aldosterone .; Torsemide enhances the hypotensive effect of antihypertensive agents, the neuromuscular blockade of depolarizing muscle relaxants (suksametoniy) and weakens the effect of non-depolarizing muscle relaxants (tubocurarine) .; At the same time taking high doses of salicylates during therapy with Torsemide, the risk of their toxicity increases (due to competitive elimination by the kidneys) .; Consistent or simultaneous use of Torsemide with ACE inhibitors or angiotensin II receptor antagonists can lead to a strong decrease in blood pressure. This can be avoided by lowering the dose of Torsemide or temporarily canceling it .; When applied simultaneously with probenecid or methotrexate, it is possible to reduce the effectiveness of Torsemide (the same secretion route). On the other hand, Torsemide may lead to a decrease in the renal elimination of these drugs .; With the simultaneous use of cyclosporine and Torsemide increases the risk of developing gouty arthritis due to the fact that cyclosporine can cause a violation of the excretion of urate by the kidneys, and Torsemide - hyperuricemia .; It was reported that patients with a high risk of nephropathy, receiving Torsemide orally, with the introduction of X-ray contrast agents, renal dysfunction was observed more often than patients with a high risk of developing nephropathy who underwent IV / IV 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 sulfonamides and sulfonylurea derivatives may have a cross-sensitivity to Diuver .; Patients receiving high doses of the drug Diuver for a long period, in order to avoid the development of hyponatremia, metabolic alkalosis and hypokalemia, it is recommended a diet with an adequate content of salt and potassium preparations .; 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 on the background of parenterally administered fluids) .; With the onset or increase of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended to suspend treatment .; The selection of a dosing regimen in patients with ascites on 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). This category of patients shows regular monitoring of plasma electrolytes .; Patients with diabetes mellitus or with reduced glucose tolerance require periodic monitoring of the concentration of glucose in the blood and urine .; In unconscious patients with hyperplasia of the prostate gland, narrowing of the ureters, control of diuresis is necessary due to the possibility of acute urinary retention .; Influence on the ability to drive motor vehicles and control mechanisms; During the treatment period, patients should refrain from driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.