Trigrim, tablets 5 mg 30 pcs

Diuretic drug. The main mechanism of action is due to the reversible binding of thoracemide to the Na⁺/2Cl^–/K⁺ transporter.located in the apical membrane of the thick segment of the ascending loop of Genle, resulting in a reduction or complete inhibition of sodium ion reabsorption, which leads to a decrease in the osmotic pressure of intracellular fluid and water reabsorption.

With this, due to its anti-aldosterone action, thorasemide causes hypokalemia to a lesser extent than furosemide, with greater activity and duration of action.

Pharmacokinetics

Intake

After oral administration, torasemide is rapidly and almost completely absorbed from the GI tract. C_max of torasemide in plasma is noted 1-2 h after ingestion. Bioavailability is about 80-91% or more in edema.

Eating has no effect on absorption of the drug.

Distribution

Binding to plasma proteins is 99%. V_d – 16 l.

Metabolism

Metabolized in the liver with the participation of cytochrome P450 system isoenzymes to form 3 metabolites M1, M3 and M5.

T_1/2 of torasemide and its metabolites in healthy volunteers is 3-4 hours. Total clearance of torasemide is 40 ml/min and renal clearance is about 10 ml/min. On average 80-83% of taken dose is excreted by kidneys through tubular secretion unchanged (24-25%) and as metabolites (M1 – 11-12%, M3 – 3%, M5 – 41-44%).

Pharmacokinetics in special clinical cases

In renal failure T_1/2 torasemide does not change.

Indications

Swelling, Heart failure, Hypertension (high blood pressure), Liver damage

• Oedema caused by heart failure, liver, kidney and lung diseases.
• Primary arterial hypertension (used as monotherapy or in combination with other hypotensive drugs).
  

Active ingredient

Torasemide

Composition

Excipients:

lactose,

corn starch,

colloidal silica,

magnesium stearate.

How to take, the dosage

The drug is administered in adults, orally, regardless of meals.

In case of edema

The drug is prescribed in a dose of 5 mg once daily. If necessary, the dose may be gradually increased to 20 mg once daily. In individual cases it is recommended to use up to 40 mg/day.

In edema associated with congestive heart failure

Prescribe in a dose of 5-20 mg once daily. If necessary, the daily dose may be gradually increased, doubling to a maximum of 200 mg.

In case of edema due to chronic renal insufficiency

The starting dose is 20 mg/day. If necessary, this dose may be gradually increased, doubling it, until optimal diuretic action is achieved. The maximum daily dose is 200 mg.

In case of edema associated with cirrhosis

The drug is indicated in a dose of 5-10 mg once daily. If necessary, this dose may be gradually increased by doubling until an adequate diuretic effect is achieved. There have been no appropriately controlled studies in patients with liver disease using doses greater than 40 mg/day.

In primary arterial hypertension

The dose is 2.5 mg once daily. If necessary, the dose can be gradually increased to 5 mg/day. According to studies, a dose of more than 5 mg/day does not lead to a further decrease in BP. Maximum effect is achieved after about 12 weeks of continuous treatment.

Patients of advanced age do not require dose adjustment.

Interaction

Trigrim^® increases myocardial sensitivity to cardiac glycosides in potassium or magnesium deficiency.

In concomitant administration with mineral and glucocorticoids, laxatives may increase potassium excretion.

Trigrim^® increases the effect of hypotensive drugs.

In high doses, Trigrim^® may increase the toxic effects of aminoglycosides, antibiotics, cisplatin; nephrotoxic effect of cephalosporins, and cardio- and neurotoxic effects of lithium.

Torasemide may increase the effects of curare-like myorelaxants and theophylline.

When using salicylates in high doses, their toxic effects may be increased, and the effect of antidiabetic agents, on the contrary, weakened.

The sequential or simultaneous use of thoracemide with ACE inhibitors may lead to a transient drop in BP. This can be avoided by reducing the starting dose of ACE, or by reducing the dose of thorasemide (or temporarily stopping it).

Torasemide reduces the effect of vasoconstrictors (epinephrine and norepinephrine).

NSAIDs and probenecid may decrease the diuretic and hypotensive effects of torasemide.

Colestyramine may decrease absorption of thoracemide from the gastrointestinal tract (in experimental animal studies).

Special Instructions

In long-term treatment it is recommended to monitor electrolyte balance, glucose, uric acid, creatinine and blood lipids.

If hypokalemia, hyponatremia, hypovolemia or urinary disorders occur, all of these conditions should be corrected before prescribing Trigrim.

In the presence of diabetes mellitus it is necessary to control carbohydrate metabolism.

In case of thrombocytopenia or inhibition of bone marrow function or skin rashes, the drug should be discontinued.

Pediatric use

There are no data on the use of Trigrim in children.

Impact on driving and operating machinery

In the initial phase of use, it is not recommended to drive vehicles and operate machinery because of the possibility of dizziness.

Contraindications

• Anuria.
• Hypatic coma and precoma.
• Cronic renal failure with increasing azotemia.
• Arrhythmia.
• Arterial hypotension.
• Pregnancy.
• Lactation period (no data on use during lactation).
• Age under 18 years of age (effectiveness and safety not established).
• High sensitivity to thoracemide and sulfonamides.

With caution, use the drug in patients with:

• Diabetes mellitus.
• Gout.
• Disorders of water-electrolyte balance.
• Disorders of liver function.
• Hepatic cirrhosis.
• Predisposition to hyperuricemia.

.

Side effects

Blood system disorders: in some cases – decrease of erythrocyte and leukocyte counts and thrombocytes.

Metabolism disorders: in some cases – hypovolemia, electrolyte imbalance, hypokalemia, increased serum levels of uric acid, glucose and lipids.

Cardiovascular system disorders: in single cases – circulatory disorders and thromboembolism (due to dehydration), BP decrease.

Digestive system disorders: symptoms of gastrointestinal dysfunction, loss of appetite, dry mouth; in individual cases – increased activity of liver enzymes (including GGT), pancreatitis.

Urinary system disorders: acute urinary retention, increased plasma levels of urea and creatinine.

CNS and peripheral nervous system disorders: headache, dizziness, weakness, drowsiness, confusion, convulsions, paresthesias in the extremities.

Sensory system disorders: visual disturbances, tinnitus, deafness.

Allergic reactions: skin itching, rashes and photosensitization.

Overdose

• Symptoms: there is no typical picture of poisoning; in overdose there is increased diuresis accompanied by hypovolemia, electrolyte imbalance, followed by a drop in BP, somnolence, confusion, collapse, gastrointestinal disorders are possible.
• Treatment: symptomatic therapy – dose reduction or drug withdrawal with simultaneous replenishment of fluid and electrolyte loss. A specific antidote is unknown.

.

Pregnancy use

Trigrim is contraindicated during pregnancy, lactation, under 18 years of age (efficacy and safety have not been established).

Similarities

Diuver, Trigrim, Torasemide-SZ, Lotonel, Torasemide