Expiration date: 06/2025

Active substance: Torasemide

Description pharmaceutical form:

2.5 mg Tablets: round biconvex shape, white.

Tablets 5 mg and 10: flat round shape, white color.

Pharmacokinetics:

After oral torasemide is rapidly and almost completely absorbed in the digestive tract. Torasemide plasma Cmax observed 1-2 hours after administration. Bioavailability is approximately 80-91% and more swelling.

Contact with blood plasma proteins - 99%. Vd is 16 liters. It is metabolized in the liver by cytochrome P450 system to form a three metabolites M1, M3 and M5.

T1 / 2 of torasemide and its metabolites in healthy volunteers is 3-4 hr Total clearance torasemide -. 40 ml / min and renal clearance - about 10 ml / min. On average, 80-83% of the dose appears in the renal tubules: unchanged (24-25%) in the form of metabolites (Ml - 11-12%, the M3 - 3%, M5 - 41-44%).

In renal insufficiency, T1 / 2 of torasemide is unchanged.

Description of the pharmacological actions:

The main mechanism of action of the drug due to the reversible binding of torasemide cotransporter Na + / 2C1- / K +, situated in the apical membrane of the thick ascending loop of Henle segment, resulting in reduced or completely inhibited reabsorption of sodium ions, thus reducing manner intracellular osmotic pressure and fluid reabsorption of water.

Thus through the action of torasemide antialdosteronovy less than furosemide causes hypokalemia, with greater activity and duration of action.

Testimony:

• Swelling caused by heart failure, liver disease, kidney and lung;
  
• Primary hypertension (used alone or in combination with other antihypertensive agents).
  

Contraindications:

• Hypersensitivity to torasemide and sulfonamides;
  
• Anuria;
  
• Hepatic coma and prekomatosnoe state;
  
• Chronic renal failure with progressive azotemia;
  
• Arrhythmia;
  
• Hypotension;
  
• Pregnancy;
  
• Lactation (no data on the use during lactation);
  
• Age of 18 years (effectiveness and safety have been established).
  

Precautions: diabetes mellitus, gout, disorders of water and electrolyte balance, impaired liver function, cirrhosis, predisposed to hyperuricemia.

Side effect:

From the side of blood: in some cases may experience changes in blood indicators - reduction in the number of red blood cells, white blood cells and platelets also, hypovolemia, electrolyte imbalance, hypokalemia, increased uric acid, glucose and lipids in the blood serum.

Liver: increase in the activity of certain enzymes such as GGT.

From the CCC: in some cases, as a consequence of dehydration, having circulatory disorders, thrombosis, blood pressure reduction.

On the part of the digestive tract: various gastrointestinal dysfunction, loss of appetite, and in some cases may develop pancreatitis.

From the kidney and urinary tract: acute urinary retention, increased serum creatinine and urea in plasma.

CNS: headache, dizziness, weakness, sleepiness, confusion, seizures, and paresthesias of the limbs.

Allergic reactions: itching, rash and photosensitivity.

From the senses: visual disturbances, tinnitus, deafness.

Other: dry mouth.

Drug Interactions:

Increases myocardial sensitivity to cardiac glycosides with potassium or magnesium deficiency.

In simultaneous reception with mineral and glucocorticoids and laxatives may increase potassium excretion.

It enhances the effect of antihypertensive drugs.

In high doses, may potentiate the toxic effect of aminoglycoside antibiotics, cisplatin, nephrotoxic effects of cephalosporins and cardio- and neurotoxic effects of lithium.

Torasemide may increase the effects of muscle relaxants and of theophylline curariform.

When large doses of salicylates and their toxic effects may be enhanced, and the action of antidiabetic agents - weakened.

Consecutive or simultaneous reception of torasemide with ACE inhibitors may lead to a transient drop in blood pressure. This can be avoided by reducing the starting dose of the ACE inhibitor or lowering the dose of torasemide (or temporarily canceling it).

Torasemide reduces the effect of a vasoconstrictor (epinephrine and norepinephrine).

NSAIDs and probenicid can reduce the diuretic and hypotensive effect of torasemide.

Cholestyramine can reduce absorption from the digestive tract of torasemide (in animal studies).

Dosage and administration:

Inside.

Adults

Edema. 5 mg 1 time per day. If necessary, the dose can be gradually increased to 1 20 mg once a day. In some cases, it is recommended to 40 mg per day.

Congestive heart failure. 5-20 mg 1 time per day. If necessary, the daily dose can be gradually increased by doubling the maximum of 200 mg.

Chronic renal failure. The initial dose is 20 mg per day. If necessary, the dose can be gradually increased, doubling to achieve an appropriate diuretic effect. The maximum daily dose - 200 mg.

Cirrhosis of the liver. 5.10 mg 1 time per day. If necessary, the dose can be gradually increased, doubling to achieve an appropriate diuretic effect.

Not conducted properly controlled studies in patients with liver disease with doses of 40 mg per day.

Primary hypertension. 2.5 mg 1 time per day. If necessary, the dose can be gradually increased up to 5 mg per day. According to studies, a dose of more than 5 mg per day does not result in a further decrease in blood pressure. The maximum effect is achieved after about twelve weeks of continuous treatment.

Elderly patients

Elderly patients do not require a special dose adjustment.

Children

No data on the use of Trigrim children.

Food does not affect the absorption of Trigrim, and the drug can be taken regardless of meals.

Overdose:

Simtomy: typical picture of poisoning is not forced urination, accompanied by hypovolemia, electrolyte imbalance, followed by a fall in blood pressure, drowsiness, confusion, collapse may occur gastrointestinal disorders.

Treatment: the specific antidote is not known symptomatic treatment requires dose reduction or abolition of the drug and at the same time replenishing the loss of fluids and electrolytes.

Precautionary measures:

Prolonged treatment is recommended to monitor electrolyte balance, glucose, uric acid, creatinine and lipids in the blood.

When hypokalemia, hyponatremia, hypovolemia, or urinary disorders before prescribing the Trigrim carry out the removal of all the above conditions before prescribing this drug.

With care administered to treat gout or trends to increase uric acid levels.

If you have diabetes need to control carbohydrate metabolism.

When thrombocytopenia or suppression of bone marrow function, and the drug should be discontinued for skin rashes.

Effects on ability to drive or to perform work requiring higher rate of physical and mental reactions. At the initial stage it is not recommended to drive vehicles and mechanisms to serve because of the possibility of dizziness.