Torasemid - SZ 10mg, No. 60
Expiration Date: 05/2027
Russian Pharmacy name:
Торасемид - СЗ 10мг, №60
edematous syndrome of various origins, incl. with chronic heart failure, diseases of the liver, lungs and kidneys;
arterial hypertension.
The drug is taken orally 1 time / day, at any convenient (but at the same) time, regardless of the meal. The tablets should be swallowed without chewing and drinking plenty of water.
Edema syndrome in chronic heart failure
The recommended starting dose is 10-20 mg 1 time / day. If necessary, the dose can be doubled until the desired effect is obtained.
Edema syndrome in kidney disease
The recommended starting dose is 20 mg 1 time / day. If necessary, the dose can be doubled until the desired effect is obtained.
Edematous syndrome with liver disease
The recommended starting dose is 5-10 mg 1 time / 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 within 4 weeks, the dose is increased to 5 mg 1 time / day. In the absence of an adequate decrease in blood pressure when taken at 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.
In elderly patients, a dose adjustment is required.
Active substance: torasemide - 10 mg
Excipients : lactose monohydrate (lactopress) (milk sugar) - 178.6 mg, pregelatinized starch (starch 1500) - 49 mg, colloidal silicon dioxide (aerosil) - 1.2 mg, magnesium stearate - 1.2 mg.
renal failure with anuria;
hepatic coma and precoma;
refractory hypokalemia / refractory hyponatremia;
hypovolemia (with or without arterial hypotension) or dehydration;
pronounced violations of the outflow of urine of any etiology (including unilateral urinary tract damage);
glycosidic intoxication;
acute glomerulonephritis;
decompensated aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy;
increased central venous pressure (over 10 mm Hg);
hyperuricemia;
simultaneous use of aminoglycosides and cephalosporins;
pregnancy;
breastfeeding period;
age under 18;
lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
an allergic reaction to sulfonamides (sulfonamide antimicrobials or sulfonylureas);
hypersensitivity to torasemide or to any of the components of the drug.
The drug should be prescribed with caution in case of arterial hypotension, stenosing atherosclerosis of the cerebral arteries, hypoproteinemia, predisposition to hyperuricemia, impaired urine outflow (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis), ventricular arrhythmia in history, acute myocarcinoma ), diarrhea, pancreatitis, diabetes mellitus (decreased glucose tolerance), hepatorenal syndrome, gout, anemia; the simultaneous use of cardiac glycosides, corticosteroids and ACTH.
Clinical and pharmacological group: Diuretic
Pharmaco-therapeutic group: Diuretic
pharmachologic effect
Torasemide is a loop diuretic. The main mechanism of action of the drug is due to the reversible binding of torasemide to the sodium / chlorine / potassium ion 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 and the osmotic pressure of the intracellular fluid and water reabsorption decrease. Blocks myocardial aldosterone receptors; reduces fibrosis and improves diastolic myocardial function.
Torasemide, to a lesser extent than furosemide, causes hypokalemia, while it is more active and its effect is longer.
The maximum diuretic effect develops 2-3 hours after taking the drug inside. The diuretic effect lasts up to 18 hours, which facilitates the tolerance of therapy due to the absence of very frequent urination in the first hours after taking the drug inside, which limits the activity of patients.
The use of torasemide is the most reasonable choice for long-term therapy.
Pharmacokinetics
Suction
After oral administration, torasemide is rapidly and almost completely absorbed from the gastrointestinal tract. Food intake does not significantly affect the absorption of the drug. Cmax of torasemide in blood plasma is noted 1-2 hours after oral administration. Bioavailability is 80-90% with minor individual variations.
Distribution
Plasma protein binding is more than 99%. The apparent Vd is 16 liters.
Metabolism
It is metabolized in the liver using isoenzymes of the cytochrome P450 system. As a result of successive reactions of oxidation, hydroxylation or ring hydroxylation, three metabolites (M1, M3 and M5) are formed, which bind to blood plasma proteins by 86%, 95% and 97%, respectively.
Withdrawal
T1 / 2 of torasemide and its metabolites is 3-4 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 predominantly inactive metabolites (M1 - 12%, M3 - 3%, M5 - 41%).
Pharmacokinetics in special patient groups
In renal failure, T1 / 2 does not change, T1 / 2 of metabolites M3 and M5 increases. Torasemide and its metabolites are slightly excreted 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 heart or hepatic insufficiency, T1 / 2 of torasemide and the M5 metabolite is slightly increased, cumulation of the drug is unlikely.
Indications of the drug Torasemid-SZ
edematous syndrome of various origins, incl. with chronic heart failure, diseases of the liver, lungs and kidneys;
arterial hypertension.
Dosage regimen
The drug is taken orally 1 time / day, at any convenient (but at the same) time, regardless of the meal. The tablets should be swallowed without chewing and drinking plenty of water.
Edema syndrome in chronic heart failure
The recommended starting dose is 10-20 mg 1 time / day. If necessary, the dose can be doubled until the desired effect is obtained.
Edema syndrome in kidney disease
The recommended starting dose is 20 mg 1 time / day. If necessary, the dose can be doubled until the desired effect is obtained.
Edematous syndrome with liver disease
The recommended starting dose is 5-10 mg 1 time / 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 within 4 weeks, the dose is increased to 5 mg 1 time / day. In the absence of an adequate decrease in blood pressure when taken at 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.
In elderly patients, a dose adjustment is required.
Side effect
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? 1/10000 to <1/1000 (> 0.01% and <0.1%); very rarely - <1/10000 (<0.01%); frequency unknown - cannot be estimated from the available data.
From the nervous system: often - headache, dizziness, drowsiness; infrequently - muscle cramps of the lower extremities; the frequency is unknown - confusion, fainting, paresthesia in the extremities (feeling of numbness, 'creeping' and tingling sensation).
From the senses: the frequency is unknown - visual impairment, 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; frequency unknown - excessive decrease in blood pressure, orthostatic hypotension, collapse, deep vein thrombosis, thromboembolism, decreased BCC.
From the respiratory system: infrequently - epistaxis.
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 - 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.
On the part of the reproductive system: the frequency is unknown - a decrease in potency.
On the part of the skin and subcutaneous tissues: the frequency is unknown - itching, rash, urticaria, erythema polymorphism, exfoliative dermatitis, purpura, vasculitis, photosensitization.
From the musculoskeletal system: 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).
On the part of laboratory parameters: infrequently - hypercholesterolemia, hypertriglyceridemia; the frequency is unknown - hyperuricemia, a slight increase in the activity of alkaline phosphatase in the blood plasma, an increase in the concentration of creatinine and urea in the blood plasma, an increase in the activity of some liver enzymes in the blood plasma (for example, GGT), thrombocytopenia, leukopenia, agranulocytosis, hyperglycemia, decreased glucose tolerance (possible manifestation of latent diabetes mellitus).
Others: the frequency is unknown - aplastic or hemolytic anemia.
Contraindications for use
renal failure with anuria;
hepatic coma and precoma;
refractory hypokalemia / refractory hyponatremia;
hypovolemia (with or without arterial hypotension) or dehydration;
pronounced violations of the outflow of urine of any etiology (including unilateral urinary tract damage);
glycosidic intoxication;
acute glomerulonephritis;
decompensated aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy;
increased central venous pressure (over 10 mm Hg);
hyperuricemia;
simultaneous use of aminoglycosides and cephalosporins;
pregnancy;
breastfeeding period;
age under 18;
lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
an allergic reaction to sulfonamides (sulfonamide antimicrobials or sulfonylureas);
hypersensitivity to torasemide or to any of the components of the drug.
The drug should be prescribed with caution in case of arterial hypotension, stenosing atherosclerosis of the cerebral arteries, hypoproteinemia, predisposition to hyperuricemia, impaired urine outflow (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis), ventricular arrhythmia in history, acute myocarcinoma ), diarrhea, pancreatitis, diabetes mellitus (decreased glucose tolerance), hepatorenal syndrome, gout, anemia; the simultaneous use of cardiac glycosides, corticosteroids and ACTH.
Application during pregnancy and lactation
Torasemide does not have a teratogenic effect and fetotoxicity, penetrates the placental barrier, causing disturbances in water and electrolyte metabolism and thrombocytopenia in the fetus.
Controlled studies on the use of torasemide in pregnant women have not been conducted, the drug is not recommended for use during pregnancy.
It is not known whether torasemide is excreted in breast milk. If it is necessary to use the drug Torasemid-SZ during lactation, it is necessary to stop breastfeeding.
Application for violations of liver function
The use of the drug is contraindicated in hepatic coma and precoma.
With caution , the drug should be prescribed for hepatorenal syndrome.
Application for impaired renal function
The use of the drug is contraindicated in renal failure with anuria, acute glomerulonephritis, pronounced disorders of urine outflow 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.
Application in children
The use of the drug is contraindicated under the age of 18 years.
Use in elderly patients
In elderly patients, a dose adjustment is required.
special instructions
The drug should be used strictly according to the doctor's prescription.
Patients with hypersensitivity to sulfonamides and sulfonylurea derivatives may have cross-sensitivity to Torasemide-SZ.
In order to avoid the development of hyponatremia, metabolic alkalosis and hypokalemia, patients receiving the drug Torasemide-SZ in high doses for a long period are recommended to have a diet with a sufficient content of sodium chloride and the use of potassium preparations.
ѕовышенный риск развити¤ нарушений водно-электролитного баланса отмечаетс¤ у пациентов с почечной недостаточностью. ¬ ходе курсового лечени¤ необходимо периодически контролировать концентрацию электролитов плазмы крови (в т.ч. натрий, кальций, калий, магний), кислотно-основное состо¤ние, остаточный азот, креатинин, мочевую кислоту и проводить при необходимости соответствующую коррекционную терапию (с большей кратностью у больных с частой рвотой и на фоне парентерально вводимых жидкостей).
ѕри по¤влении или усилении азотемии и олигурии у пациентов с т¤желыми прогрессирующими заболевани¤ми почек, рекомендуетс¤ приостановить лечение.
ѕодбор дозы пациентам с асцитом на фоне цирроза печени нужно проводить в стационарных услови¤х (нарушени¤ водно-электролитного баланса могут повлечь развитие печеночной комы). ?анной категории пациентов показан регул¤рный контроль электролитов плазмы крови.
” больных сахарным диабетом или со сниженной толерантностью к глюкозе требуетс¤ периодический контроль концентрации глюкозы в крови и моче.
” больных в бессознательном состо¤нии, с гиперплазией предстательной железы, сужением мочеточников необходим контроль диуреза в св¤зи с возможностью острой задержки мочи.
¬ли¤ние на способность к вождению автотранспорта и управлению механизмами
¬ период лечени¤ пациенты должны воздерживатьс¤ от управлени¤ транспортными средствами и зан¤тий другими потенциально опасными видами де¤тельности, требующими повышенной концентрации внимани¤ и быстроты психомоторных реакций (риск развити¤ головокружени¤ и сонливости).
ѕередозировка
—имптомы: усиленный диурез, сопровождающийс¤ снижением ќ? и нарушением водно-электролитного баланса крови, с последующим чрезмерным снижением ј?, сонливостью и спутанностью сознани¤, коллапсом. ћогут наблюдатьс¤ желудочно-кишечные расстройства.
Ћечение: специфического антидота нет. ѕровокаци¤ рвоты, промывание желудка, активированный уголь. ѕроведение симптоматической терапии, снижение дозы или отмена препарата и одновременное восполнение ќ? и показателей водно-электролитного баланса и кислотно-основного состо¤ни¤ под контролем сывороточных концентраций электролитов, гематокрита. vемодиализ неэффективен.
Ћекарственное взаимодействие
ѕовышает концентрацию и риск развити¤ нефро- и ототоксического действи¤ цефалоспоринов, аминогликозидов, хлорамфеникола, этакриновой кислоты, цисплатина, амфотерицина ¬ (вследствие конкурентного почечного выведени¤).
ѕовышает эффективность диазоксида и теофиллина, снижает - гипогликемических средств, аллопуринола.
ѕрессорные амины и торасемид взаимно снижают эффективность друг друга.
Ћекарственные средства, блокирующие канальциевую секрецию, повышают концентрацию торасемида в сыворотке крови.
ѕри одновременном применении v —, амфотерицина ¬ повышаетс¤ риск развити¤ гипокалиемии, с сердечными гликозидами - возрастает риск развити¤ гликозидной интоксикации вследствие гипокалиемии (дл¤ высоко- и низкопол¤рных) и удлинени¤ “1/2 (дл¤ низкопол¤рных).
—нижает почечный клиренс препаратов лити¤ и повышает веро¤тность развити¤ интоксикации.
Ќѕ¬—, сукральфат снижают диуретический эффект вследствие ингибировани¤ синтеза простагландина, нарушени¤ активности ренина в плазме крови и выведени¤ альдостерона.
”силивает антигипертензивное действие гипотензивных средств, нервно-мышечную блокаду депол¤ризующих миорелаксантов (суксаметоний) и ослабл¤ет действие недепол¤ризующих миорелаксантов (тубокурарин).
ќдновременный прием салицилатов в высоких дозах на фоне терапии торасемидом увеличивает риск про¤влени¤ их токсичности (вследствие конкурентного почечного выведени¤).
ѕоследовательное или одновременное применение торасемида с ингибиторами јѕ‘ или антагонистами рецепторов ангиотензина II может привести к значительному снижению ј?. Ётого можно избежать, снизив дозу торасемида или временно отменив его.
ќдновременное применение пробенецида или метотрексата может уменьшать эффективность торасемида (одинаковый путь секреции). — другой стороны торасемид может приводить к снижению почечной элиминации этих лекарственных средств.
ѕри одновременном применении циклоспорина и торасемида увеличиваетс¤ риск развити¤ подагрического артрита вследствие того, что циклоспорин может вызвать нарушение экскреции уратов почками, а торасемид - гиперурикемию.
It was reported that in patients with a high risk of 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 nephropathy, who were hydrated intravenously before the introduction of X-ray contrast agents.
The bioavailability and, as a consequence, the effectiveness of torasemide can be reduced when combined therapy with cholestyramine.
Storage conditions of the drug Torasemid-SZ
The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25 ? C.
Shelf life of the drug Torasemid-SZ
Shelf life is 3 years.
Terms of sale
The drug is available with a prescription.
Contacts for inquiries
NORTH STAR NAO (Russia)