Torasemid Canon

1 tablet contains:

Active substance: 

torasemide 10 mg;

Excipients:

pregelatinized corn starch,

colloidal silicon dioxide, 

croscarmellose sodium, 

mannitol,

magnesium stearate,

microcrystalline cellulose.

Torasemide is a loop diuretic; in low doses used for antihypertensive treatment, it has a weak diuretic and saluretic effect. At higher doses, torasemide increases urine output in a dose-dependent manner.

Torasemide exhibits maximum diuretic activity 2-3 hours after oral administration.

After oral administration, torasemide is rapidly and almost completely absorbed; Cmax in serum is reached within 1-2 hours after administration. Systemic bioavailability is 80–90%. Binding of torasemide to blood plasma proteins is> 99%, metabolites M1, M3 and M5 - 86; 95 and 97%, respectively.

The estimated volume of distribution is 16 liters. Torasemide is metabolized by oxidation and hydroxylation to form three metabolites: M1, M3 and M5. M5 is pharmacologically inactive, while metabolites M1 and M3 account for approximately 10% of the pharmacological action of the drug. 

T1 / 2 of torasemide and its metabolites in healthy volunteers is 3-4 hours. The total clearance of torasemide is 40 ml / min, renal clearance is about 10 ml / min. About 80% of the dose is excreted in the form of unchanged torasemide (24%) and its metabolites: M1 (12%), M3 (3%), M5 (41%). 

In renal failure, T1 / 2 of torasemide does not change, and T1 / 2 of metabolites M3 and M5 is lengthened. Torasemide and its metabolites are practically not excreted by hemodialysis or hemofiltration. 

In patients with impaired liver function or heart failure, T1 / 2 of torasemide and the M5 metabolite are slightly lengthened, but the cumulation of torasemide and its metabolites is unlikely. 

• Edema syndrome of various origins, incl. with chronic heart failure, liver and kidney diseases.
• Arterial hypertension.

Torasemide does not have a teratogenic effect and fetotoxicity, penetrates the placental barrier, causing disturbances in water-electrolyte metabolism and thrombocytopenia in the fetus.

The drug Torasemide Canon can be used during pregnancy only if the intended benefit to the mother outweighs the potential risk to the fetus, under close medical supervision and only in minimal doses.

There is no data on the excretion of torasemide in breast milk, therefore, if it is necessary to use the drug Torasemide Canon during lactation, breastfeeding should be stopped.

• Anuria; 
• hepatic coma and precoma; 
• refractory hypokalemia; 
• refractory hyponatremia; 
• dehydration; 
• pronounced violations of the outflow of urine of any etiology (including unilateral urinary tract damage); 
• glycosidic intoxication; 
• acute glomerulonephritis; 
• sinoatrial and AV block II and III degree; 
• children and adolescents up to 18 years old; 
• pregnancy; 
• hypersensitivity to torasemide; 
• allergy to sulfonamides (sulfonamide antimicrobials or sulfonylureas).

WHO classification of the incidence of side effects: very often - ≥1 / 10 appointments (> 10%), often - from ≥1 / 100 to <1/10 appointments (> 1% and <10%), infrequently - from ≥1 / 1000 to <1/100 appointments (> 0.1% and <1%), rarely ≥1 / 10,000 to <1/1000 appointments (> 0.01% and <0.1%), very rarely <1/10 000 appointments ( <0.01%), frequency unknown - cannot be estimated from the available data.

From the hematopoietic system: the frequency is unknown - thrombocytopenia, leukopenia, agranulocytosis, aplastic or hemolytic anemia.

From the side of metabolism and nutrition: infrequently - polydipsia, hypercholesterolemia, hypertriglyceridemia; the frequency is unknown - a decrease in glucose tolerance (possible manifestation of latent diabetes mellitus).

From the water-electrolyte and acid-base balance: the frequency is unknown - hypokalemia, hyponatremia, hypomagnesemia, hypocalcemia, hypochloremia, metabolic alkalosis, hypovolemia, dehydration (more often in elderly patients), which can lead to hemoconcentration with a tendency to develop blood clots.

From the nervous system: often - dizziness, headache, drowsiness; the frequency is unknown - confusion, fainting, paresthesia in the extremities (feeling of numbness, "crawling" and tingling sensation).

From the side of the organ of vision: the frequency is unknown - visual impairment.

On the part of the organ of hearing: the frequency is unknown - hearing impairment, tinnitus and hearing loss (usually reversible), usually in patients with renal failure or hypoproteinemia (nephrotic syndrome).

From the side of the cardiovascular system: infrequently - extrasystole, arrhythmia, tachycardia.

Vascular disorders: frequency unknown - excessive decrease in blood pressure, orthostatic hypotension, collapse, deep vein thrombosis, thromboembolism.

From the respiratory system: infrequently - nosebleeds.

From the digestive system: often - diarrhea; infrequently - abdominal pain, flatulence; frequency unknown - dry mouth, nausea, vomiting, loss of appetite, pancreatitis, dyspeptic disorders, intrahepatic cholestasis.

From the urinary system: often - an increase in the frequency of urination, polyuria, nocturia; infrequently - an increased urge to urinate; frequency unknown - oliguria, urinary retention (in patients with urinary tract obstruction), interstitial nephritis, hematuria.

From the genitals and mammary gland: the frequency is unknown - a decrease in potency.

Skin and subcutaneous tissue disorders: frequency unknown - exfoliative dermatitis, purpura, vasculitis, photosensitization.

From the musculoskeletal system: infrequently - muscle cramps of the lower extremities; frequency unknown - muscle weakness.

Allergic reactions: infrequently - severe anaphylactic reactions up to shock, which until now have been described only after intravenous administration; frequency unknown - pruritus, rash, urticaria, erythema multiforme.

On the part of laboratory and instrumental data: the frequency is unknown - hypercholesterolemia, hypertriglyceridemia, hyperuricemia, a slight increase in the concentration of alkaline phosphatase in the blood, a transient increase in the concentration of creatinine and urea in the blood, an increase in the activity of some liver enzymes (for example, gamma-glutamyltransferase).

Others: infrequently - fever, asthenia, weakness, fatigue, hyperactivity, nervousness.

If any of the side effects indicated in the instructions are aggravated or any other side effects not indicated in the instructions are noted, the patient should inform the doctor about it.

With the simultaneous use of mineral and glucocorticosteroids, amphotericin B, the risk of hypokalemia increases; with cardiac glycosides - the risk of glycosidic intoxication due to hypokalemia (for high and low polarity) and T1 / 2 lengthening (for low polarity) increases.

The drug Torasemide Canon increases the concentration and risk of developing the nephrotoxic and ototoxic effects of chloramphenicol, ethacrynic acid, antibiotics, salicylates, platinum (Pt) preparations, amphotericin B (due to competitive renal excretion).

Sequential or simultaneous administration of the drug Torasemide Canon with ACE inhibitors or angiotensin II receptor antagonists can lead to a sharp drop in blood pressure. This can be avoided by reducing the initial dose of an ACE inhibitor or by reducing the dose of Torasemide Canon (or temporarily canceling it).

NSAIDs, sucralfate, methotrexate and probenecid reduce the diuretic effect due to inhibition of prostaglandin synthesis, impaired renin activity in blood plasma and elimination of aldosterone.

Torasemide enhances the antihypertensive effect of antihypertensive agents, neuromuscular blockade of depolarizing muscle relaxants (suxamethonium) and weakens the effect of non-depolarizing muscle relaxants (tubocurarine).

Torasemide may increase the toxicity of lithium preparations and the ototoxicity of ethacrynic acid.

Torasemide increases the effectiveness of diazoxide and theophylline, reduces the effectiveness of hypoglycemic agents, allopurinol.

Pressor amines and the drug Torasemide Canon mutually reduce the effectiveness.

Drugs that block tubular secretion increase the serum concentration of Torasemide Canon.

With the simultaneous use of cyclosporine and the drug Torasemide Canon, the risk of developing gouty arthritis increases due to the fact that cyclosporine can cause impaired excretion of urate by the kidneys, and torasemide - hyperuricemia.

It was reported that in patients with a high risk of developing nephropathy taking oral torasemide, with the introduction of X-ray contrast agents, renal dysfunction was observed more often than in patients with a high risk of developing nephropathy, who were hydrated intravenously before the administration of X-ray contrast agents.

The bioavailability and, as a consequence, the effectiveness of torasemide can be reduced when combined therapy with cholestyramine.

The drug is taken orally, at any convenient time, regardless of the meal, preferably at the same time. The tablets should be taken without chewing and with water.

In case of edematous syndrome in chronic heart failure, the initial dose is 10-20 mg 1 time / day. If necessary, the dose can be doubled to obtain the desired effect.

For edematous syndrome with kidney disease, the initial dose is 20 mg 1 time / day. If necessary, the dose can be doubled to obtain the desired effect.

With edematous syndrome in liver disease, the initial dose is 5-10 mg 1 time / day. If necessary, the dose can be doubled to obtain the desired effect.

A single dose of more than 40 mg is not recommended, because its action has not been studied.

The drug Torasemid Canon is prescribed for a long period or until the edema disappears.

In hypertension, the initial dose is 5 mg 1 time / day. In the absence of an adequate decrease in blood pressure within 4-6 weeks, the dose is increased to 10 mg 1 time / day. If this dose does not give the desired effect, an antihypertensive drug of another group should be added to the treatment regimen.

Elderly patients do not need dose adjustment.

Symptoms: increased urine output, accompanied by a decrease in BCC and electrolyte imbalance, followed by an excessive decrease in blood pressure, drowsiness and confusion, collapse. Gastrointestinal upset may occur.

Treatment: there is no specific antidote; provocation of vomiting, gastric lavage, activated carbon. Conducting symptomatic therapy, reducing the dose or discontinuing the drug and simultaneously replenishing the BCC and indicators of water-electrolyte balance and acid-base state under the control of serum electrolyte concentrations, hematocrit. 

Hemodialysis is not effective because excretion of torasemide and its metabolites is not accelerated.

The drug Torasemid Canon should be used strictly according to the doctor's prescription.

Patients with hypersensitivity to sulfonamides and sulfonylurea derivatives may have cross-sensitivity to the drug Torasemide Canon.

For patients receiving the drug Torasemide Canon in high doses, in order to avoid the development of hyponatremia, hypokalemia and metabolic alkalosis, it is inappropriate to limit the consumption of table salt and the use of potassium preparations.

The risk of hypokalemia is greatest in patients with cirrhosis of the liver, severe diuresis, inadequate intake of electrolytes from food, and also with simultaneous treatment with corticosteroids or ACTH.

An increased risk of developing disorders of water and electrolyte balance is observed in patients with renal failure. During the course of treatment with Torasemide Canon, it is necessary to periodically monitor the concentration of blood plasma electrolytes (including sodium, calcium, potassium, magnesium), acid-base state, residual nitrogen, creatinine, uric acid and, if necessary, carry out appropriate therapy (with greater frequency in patients with frequent vomiting and against the background of parenterally administered fluids).

In patients with developed water-electrolyte disorders, hypovolemia or prerenal azotemia, laboratory test data may include: hyper- or hyponatremia, hyper- or hypochloremia, hyper- or hypokalemia, acid-base balance disorders and increased blood urea concentration. 

If these disorders occur, it is necessary to stop taking the drug Torasemide Canon until normal values ​​are restored, and then resume treatment at a lower dose.

When azotemia and oliguria appear or intensify in patients with severe progressive kidney disease, it is recommended to suspend treatment with Torasemide Canon.

The selection of the dosing regimen for patients with ascites against the background of liver cirrhosis should be carried out in stationary conditions (disturbances in the water-electrolyte balance can lead to the development of hepatic coma). This category of patients is shown regular monitoring of blood plasma electrolytes.

The use of the drug Torasemide Canon can exacerbate gout.

Patients with diabetes mellitus or with impaired glucose tolerance require periodic monitoring of the concentration of glucose in the blood and urine.

In patients with prostatic hyperplasia, narrowing of the ureters, diuresis control is necessary due to the possibility of acute urinary retention.

In patients with diseases of the cardiovascular system, especially those taking cardiac glycosides, hypokalemia caused by diuretics can cause the development of arrhythmias.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment with the drug Torasemide Canon, patients should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Pills