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Active ingredients
Torasemide
Release form
Pills
Composition
Torsemide 5 mg; Excipients: lactose, corn starch, colloidal silicon dioxide, magnesium stearate.
Pharmacological effect
Diuretic drug. The main mechanism of action is due to the reversible binding of Torsemide to the Na + / 2Cl- / K + cotransporter, located in the apical membrane of the thick segment of the ascending loop of Henle, as a result of which the reabsorption of sodium ions is reduced or completely inhibited, which reduces the osmotic pressure of the intracellular fluid and reabsorption of water .; Moreover, due to the anti-aldosterone action, Torsemide to a lesser extent than furosemide causes hypokalemia, with greater activity and duration of action.
Pharmacokinetics
After ingestion, Torsemide is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax of Torsemide in plasma is noted 1-2 h after administration. Bioavailability is about 80-91% or more with edema.; Eating does not affect the absorption of the drug.; Distribution; Binding to plasma proteins - 99%. Vd - 16 l.; Metabolism; Metabolized in the liver with the participation of cytochrome P450 isoenzymes with the formation of 3 metabolites M1, M3 and M5.; Elimination; T1 / 2 of Torsemide and its metabolites in healthy volunteers is 3-4 hours. The total clearance of the Torsemide is 40 ml / min and renal clearance is about 10 ml / min. On average, 80-83% of the accepted dose is excreted by the kidneys by tubular secretion unchanged (24-25%) and as metabolites (M1 - 11-12%, M3 - 3%, M5 - 41-44%) .; Pharmacokinetics in special clinical situations; In renal failure, T1 / 2 Torsemide does not change.
Indications
- swelling caused by heart failure, diseases of the liver, kidneys and lungs; - primary hypertension (used as monotherapy or in combination with other antihypertensive drugs).
Contraindications
- anuria; - hepatic coma and precomatose state; - chronic renal failure with increasing azotemia; - arrhythmia; - arterial hypotension; - pregnancy; - lactation period (no data on the use during lactation); - age up to 18 years (efficacy and safety have not been established); - hypersensitivity to Torsemide and sulfonamides. With caution it is necessary to use the drug in patients with diabetes mellitus, gout, impaired water and electrolyte balance, impaired liver function, liver cirrhosis, susceptibility to hyperuricemia.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is prescribed for adults, by mouth, regardless of the meal.; For edema, the drug is prescribed in a dose of 5 mg 1 time / day. If necessary, the dose can be gradually increased to 20 mg 1 time / day. In some cases, it is recommended to use up to 40 mg / day; In case of congestive heart failure, it is prescribed in a dose of 5-20 mg 1 time / day. If necessary, the daily dose can be gradually increased, doubling it, up to a maximum of 200 mg. In chronic renal failure, the initial dose is 20 mg / day. If necessary, this dose can be gradually increased, doubling it, until optimal diuretic action is achieved. The maximum daily dose is 200 mg. In case of liver cirrhosis, the drug is prescribed in a dose of 5-10 mg 1 time / day. If necessary, this dose can be gradually increased, doubling it, until a corresponding diuretic effect is achieved. No properly controlled studies have been conducted in patients with liver diseases using doses of more than 40 mg / day. In case of primary hypertension, the dose is 2.5 mg 1 time / day. If necessary, the dose can be gradually increased to 5 mg / day. According to research, a dose of more than 5 mg / day does not lead to a further reduction in blood pressure. The maximum effect is achieved after approximately 12 weeks of continuous treatment.; Elderly patients do not require dose adjustment.
Side effects
On the part of the hematopoietic system: in some cases, a decrease in the number of erythrocytes and leukocytes, as well as platelets. On the part of the metabolism: in some cases, hypovolemia, electrolyte imbalance, hypokalemia, increased serum uric acid, glucose and lipids .; Since the cardiovascular system: in some cases - circulatory disorders and thromboembolism (due to dehydration), a decrease in blood pressure.; From the digestive system: symptoms of dysfunction of the gastrointestinal tract, loss of appetite, dry mouth y in some cases - increased activity of liver enzymes (including GGT), pancreatitis. From the urinary system: acute urinary retention,increased urea and creatinine levels in plasma.; From the side of the central nervous system and peripheral nervous system: headache, dizziness, weakness, drowsiness, confusion, convulsions, paresthesias of the limbs; From the sense organs: visual disturbances, tinnitus, deafness .; Allergic reactions: pruritus, rash and photosensitivity.
Overdose
Symptoms: There is no typical pattern of poisoning; in case of overdose, forced urination is observed, accompanied by hypovolemia, electrolyte imbalance, followed by a fall in blood pressure, drowsiness, confusion, collapse, and gastrointestinal disturbances are possible. . The specific antidote is unknown.
Interaction with other drugs
Trigrim increases the sensitivity of the myocardium to cardiac glycosides with potassium or magnesium deficiency. When taken simultaneously with mineral and glucocorticoids, laxatives, an increase in potassium excretion is possible. Trigrim enhances the action of antihypertensive drugs. cisplatin; the nephrotoxic effect of cephalosporins, as well as the cardio-and neurotoxic effect of lithium.; Torsemide may enhance the effect of curare-like muscle relaxants and theophylline. Torsemide with ACE inhibitors can lead to a transient drop in blood pressure. This can be avoided by reducing the initial dose of ACE, or by lowering the dose of Torsemide (or temporarily canceling it); Torsemide reduces the effect of vasoconstrictor agents (epinephrine and norepinephrine); Torsemide from the gastrointestinal tract (in experimental animal studies).
special instructions
With prolonged treatment, it is recommended to monitor the electrolyte balance, glucose, uric acid, creatinine and lipids in the blood. With hypokalemia,Hyponatremia, hypovolemia, or urination disorders before prescribing the drug Trigrim, the above conditions are eliminated. In the presence of diabetes mellitus, it is necessary to control carbohydrate metabolism. skin rashes should stop the drug.; Use in Pediatrics; There is no data on the use of the drug Trigrim in children.; Effect on the ability to drive motor transport and control mechanisms; At the initial stage of reception it is not recommended to drive vehicles and maintain mechanisms because of the possibility of dizziness.