Torasemide-SZ pills 10mg 30pcs

Composition

Active ingredient:

torasemide – 10 mg

excipients:

lactose monohydrate (lactopress) (milk sugar) – 178.6 mg;

pregelatinized starch (starch 1500) – 49.0 mg;

colloidal silicon dioxide (aerosil) – 1.2 mg;

magnesium stearate-1.2 mg.

Description

Tablets are white or almost white in color, round, flat-cylindrical with a chamfer and a risk on one side.

Pharmacological action

Pharmacotherapeutic group of the medicinal product: Diuretic agent Code ATX: C 03 CA 04 Pharmacological Propertiespharmacodynamicatorasemide is a “loop” diuretic. The maximum diuretic effect develops 2-3 hours after ingestion of the drug. The main mechanism of action of the drug is due to the reversible binding of torasemide to the sodium / chlorine / potassium ion countertransporter located in the apical membrane of the thick segment of the ascending Henle loop, which reduces or completely inhibits the reabsorption of sodium ions and reduces the osmotic pressure of intracellular fluid and water reabsorption. Blocks aldosterone receptors of the myocardium; reduces fibrosis and improves diastolic function of the myocardium. Torasemide is less likely to cause hypokalemia than furosemide, but it is more active and has a longer duration of action. The use of torasemide is the most reasonable choice for long-term therapy. Pharmacokineticsafter oral use, torasemide is rapidly and almost completely absorbed in the gastrointestinal tract. Food intake does not significantly affect the absorption of the drug. The maximum concentration of torasemide in blood plasma is observed 1-2 hours after oral use. Bioavailability is 80-90% with minor individual variations. The diuretic effect persists for up to 18 hours, which makes it easier to tolerate therapy due to the lack of very frequent urination in the first hours after taking the drug inside, which limits the activity of patients. Binding to plasma proteins is more than 99%. The apparent volume of distribution is 16 liters. It is metabolized in the liver by cytochrome P450 isoenzymes. As a result of successive oxidation, hydroxylation, or ring hydroxylation reactions, three metabolites (M1, M3, and M5) are formed, which bind to plasma proteins by 86%,95%, and 97%, respectively. The half-life (T1/2) of torasemide and its metabolites is 3 to 4 hours and does not change in chronic renal failure. The total clearance of torasemide is 40 ml / min, the renal clearance is 10 ml/min. On average, about 83% of the dose taken is excreted by the kidneys: unchanged (24%) and in the form of mainly inactive metabolites (M1 – 12%, M3 – 3%, M5 – 41%). In renal insufficiency, T1 / 2 does not change, T1 / 2 of the metabolites M3 and M5 increases. Torasemide and its metabolites are slightly eliminated by hemodialysis and hemofiltration. In hepatic insufficiency, the concentration of torasemide 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 torasemide and the M5 metabolite is slightly increased, and accumulation of the drug is unlikely.

Indications

-edematous syndrome of various origins, including in chronic heart failure, liver, lung and kidney diseases—

– arterial hypertension.

Contraindications

— renal failure with anuria;

— hepatic coma and precoma;

refractory hypokalemia/refractory hyponatremia;

— hypovolemia (hypotension with or without it) or dehydration;

— pronounced violations of the outflow of urine of any etiology (including unilateral lesion of the urinary tract);

— glycoside intoxication;

acute glomerulonephritis;

— decompensated aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy;

— increase of Central venous pressure (over 10 mm Hg. St. )

— hyperuricemia;

— concomitant use of aminoglycosides and cephalosporins;

— pregnancy;

— the period of breastfeeding;

— age under 18 years;

— lactose intolerance, lactase deficiency or glucose-galactose malabsorci;

allergic reaction to sulfonamides (sulfa antimicrobial agent or a sulfonylurea);

— hypersensitivity to torasemid or to any component of the drug.

With caution should designate product hypotension, stenosing atherosclerosis of cerebral arteries, hypoproteinemia, predisposition to hyperuricemia, violation of the outflow of urine (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis), ventricular arrhythmia history, acute myocardial infarction (increased risk of developing cardiogenic shock), diarrhea, pancreatitis, diabetes (reduced tolerance to glucose), hepatorenal syndrome, gout, anemia; concomitant use of cardiac glycosides, corticosteroids and ACTH.

Side effects

the incidence of side effects is classified according to the recommendations of the world health organization: very often – ≥1/10 (>10%); often – from ≥1/100 to <1/10 (>1% and <10%); infrequently – from ≥1/1000 to <1/100 (>0.1% and <1%); rarely from ≥1/10,000 to <1/1000 (>0.01% and <0.1%); very rarely – <1/10 000 (<0.01%); frequency unknown – cannot be evaluated on the basis of available data.

Nervous system disorders: often – headache, dizziness, drowsiness; infrequently – muscle cramps of the lower extremities; frequency unknown-confusion, fainting, paresthesia in the extremities (numbness, “crawling” and tingling).

From the side of the senses: frequency unknown-visual impairment, hearing impairment, tinnitus, and hearing loss (usually reversible) usually in patients with renal insufficiency or hypoproteinemia (nephrotic syndrome).

From the cardiovascular system: infrequently-extrasystole, arrhythmia, tachycardia; frequency unknown-excessive decrease in blood pressure, orthostatic hypotension, collapse, deep vein thrombosis, thromboembolism, BCC decrease.

Respiratory system disorders: infrequently-nosebleeds.

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

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

From the side of the reproductive system: frequency unknown-decreased potency.

Skin and subcutaneous tissue disorders: frequency unknown – pruritus, rash, urticaria, erythema multiforme, exfoliative dermatitis, purpura, vasculitis, photosensitization.

Musculoskeletal disorders: frequency unknown-muscle weakness.

From the side of metabolism: the frequency is unknown-hypokalemia, hyponatremia, hypomagnesemia, hypocalcemia, hypochloremia, metabolic alkalosis, hypovolemia, dehydration (more often in elderly patients).

From the side of laboratory parameters: rarely, hypercholesterolemia, hypertriglyceridemia; frequency unknown – hyperuricemia, a small increase in the activity of alkaline phosphatase in blood plasma, increasing the concentration of creatinine and urea in blood plasma, increasing the activity of some liver enzymes in the blood plasma (e. g., GGT), thrombocytopenia, leukopenia, agranulocytosis, hyperglycemia, reduced tolerance to glucose (a possible manifestation of latent diabetes mellitus flowing).

Other services: the frequency is unknown-aplastic or hemolytic anemia.

Interaction

Increases the concentration and risk of developing nephrotoxic and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacric acid, cisplatin, amphotericin B (due to competitive renal excretion).

Increases the effectiveness of diazoxide and theophylline, reduces-hypoglycemic agents, allopurinol.

Pressor amines and torasemide mutually reduce the effectiveness of each other.

Drugs that block tubular secretion increase the concentration of torasemide in the blood serum.

With the simultaneous use of corticosteroids, 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 elongation of T 1/2(for low-polar).

Reduces the renal clearance of lithium preparations and increases the likelihood of intoxication.

NSAIDs, sucralfate reduce the diuretic effect due to inhibition of prostaglandin synthesis, impaired plasma renin activity and aldosterone excretion.

Increases the antihypertensive effect of antihypertensive agents, neuromuscular blockade of depolarizing muscle relaxants (suxamethonium) and weakens the effect of non-depolarizing muscle relaxants (tubocurarin).

Concomitant use of high-dose salicylates during torasemide therapy increases the risk of toxicity (due to competitive renal elimination).

Consistent or concomitant use of torasemide with ACE inhibitors or angiotensin II receptor antagonists can lead to a significant decrease in blood pressure. This can be avoided by reducing the dose of torasemide or temporarily discontinuing it.

Concomitant use of probenecid or methotrexate may reduce the effectiveness of torasemide (same secretion pathway). On the other hand, torasemide may reduce the renal elimination of these drugs.

Concomitant use of cyclosporine and torasemide increases the risk of gouty arthritis due to the fact that cyclosporine can cause impaired urate excretion by the kidneys, and torasemide-hyperuricemia.

It has been reported that patients at high risk of developing nephropathy, taking torasemide orally, with the introduction of radiopaque agents, impaired renal function was observed more often than in patients at high risk of developing nephropathy, who were given intravenous hydration before the introduction of radiopaque agents.

The bioavailability and, as a consequence, the effectiveness of torasemide may be reduced with co-therapy with colestyramine.

How to take, course of use and dosage

The drug is taken orally 1 time/day, at any convenient (but at the same time) time, regardless of food intake. Tablets should be swallowed without chewing and washed down with a sufficient amount of water.

Edematous syndrome in chronic heart failure

The recommended starting dose is 10-20 mg once a day. If necessary, the dose can be doubled until the desired effect is obtained.

Edematous syndrome in kidney disease

The recommended starting dose is 20 mg once a day. If necessary, the dose can be doubled until the desired effect is obtained.

Edematous syndrome in liver disease

The recommended starting dose is 5-10 mg once a day. If necessary, the dose can be doubled until the desired effect is obtained.

It is not recommended to exceed the maximum single dose, which is 40 mg (no experience of use).

The drug is used for a long period or until the edema disappears.

Arterial hypertension

The initial dose is 2.5 mg (1/2 tab. 5 mg) 1 time/day. In the absence of a therapeutic effect for 4 weeks, the dose is increased to 5 mg 1 time/day. If there is no adequate reduction in blood pressure when taking a dose of 5 mg 1 time/day for 4-6 weeks, the dose is increased to 10 mg 1 time/day. If the use of the drug at a dose of 10 mg / day does not give the desired effect, an antihypertensive drug of another group is added to the treatment.

No dose adjustment is required in elderly patients.

Overdose

Symptoms: increased diuresis, accompanied by a decrease in the volume of circulating blood and a violation of the water-electrolyte balance of the blood, followed by a pronounced decrease in blood pressure, drowsiness and confusion, collapse. Gastrointestinal disorders may occur. Treatment: there is no specific antidote. Provocation of vomiting, gastric lavage, activated charcoal.

Treatment is symptomatic, 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, symptomatic treatment. Hemodialysis is ineffective.

Special instructions

The drug should be used strictly as prescribed by a doctor.

Patients with hypersensitivity to sulfonamides and sulfonylurea derivatives may have cross-sensitivity to Torasemide-SZ.

Patients receiving Torasemide-SZ in high doses for a long period of time, in order to avoid the development of hyponatremia, metabolic alkalosis and hypokalemia, a diet with sufficient table salt and the use of potassium preparations is recommended.

An increased risk of developing water-electrolyte balance disorders is noted in patients with renal insufficiency. During the course of treatment, 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 corrective therapy (with greater frequency in patients with frequent vomiting and against the background of parenterally administered fluids).

If azotemia and oliguria appear or increase in patients with severe progressive kidney disease, it is recommended to suspend treatment.

Dose selection for patients with ascites and cirrhosis of the liver should be carried out in a hospital setting (violations of the water-electrolyte balance can lead to the development of hepatic coma). Regular monitoring of blood plasma electrolytes is indicated for this category of patients.

In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of blood and urine glucose concentrations is required.

In patients in an unconscious state, with prostatic hyperplasia, narrowing of the ureters, monitoring of diuresis is necessary due to the possibility of acute urinary retention.

Influence on the ability to drive motor vehicles and manage mechanisms

During treatment, patients should refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (risk of dizziness and drowsiness).

In case of kidney failure

The drug is contraindicated in patients with renal failure with anuria, acute glomerulonephritis, severe violations of the outflow of urine of any etiology (including unilateral urinary tract damage).

With caution, the drug should be prescribed in case of violation of the outflow of urine (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis), hepatorenal syndrome.

With impaired liver function

The drug is contraindicated in patients with hepatic coma and precoma.

With caution, the drug should be prescribed for hepatorenal syndrome.

For children

No dose adjustment is required in elderly patients.

Form of production

Tablets are white or almost white in color, round, flat-cylindrical, with a chamfer and a risk on one side.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Torasemide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Hypertension