Active material: Torasemide
When ATH: C03CA04
CCF: Diuretic
ICD-10 codes (testimony): I10, I50.0, K74, N18
When CSF: 01.08.01.01
Manufacturer: Pharmaceutical Works POLPHARMA S.A. (Poland)
Pills white, round, lenticular.
| 1 tab. | |
| Torasemide | 2.5 mg |
Excipients: lactose, corn starch, colloidal silicon dioxide, magnesium stearate.
10 PC. – блистеры (3) – пачки картонные.
Pills white, round, flat, with Valium.
| 1 tab. | |
| Torasemide | 5 mg |
Excipients: lactose, corn starch, colloidal silicon dioxide, magnesium stearate.
10 PC. – блистеры (3) – пачки картонные.
Pills white, round, flat, with Valium.
| 1 tab. | |
| Torasemide | 10 mg |
Excipients: lactose, corn starch, colloidal silicon dioxide, magnesium stearate.
10 PC. – блистеры (3) – пачки картонные.
Diruetichesky drug. The main mechanism of action is due to the reversible binding of torasemide with kontransporterom Na+/2Cl–/K+, located in the apical membrane of the thick ascending loop of Henle segment, The resulting reduced or completely inhibited reabsorption of sodium ions, which leads to a decrease in the osmotic pressure of the intracellular fluid and water reabsorption.
At the same time, due to the antialdosterone action of torasemide, to a lesser extent, than furosemide causes hypokalemia, with greater activity and duration of action.
Absorption
After oral torasemide is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax torasemide in plasma is noted through 1-2 h after administration. Bioavailability is about 80-91 % and more with edema.
Eating does not affect the absorption of the drug.
Distribution
Linking blood plasma proteins- 99%. Vd – 16 l.
Metabolism
It is metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system with the formation 3 metabolites M1, M3 and M5.
Deduction
T1/2 torasemide and its metabolites in healthy volunteers is 3-4 no. The total clearance of torasemide is 40 мл/мин и почечный клиренс – около 10 ml / min. Average 80-83 % from the dose taken is excreted by the kidneys by tubular secretion unchanged (24-25%) and as metabolites (M1 – 11-12%, М3 – 3%, M5 – 41-44%).
Pharmacokinetics in special clinical situations
In renal insufficiency T1/2 torasemide unchanged.
- Swelling, caused by heart failure, liver disease, kidneys and lungs;
- primary arterial hypertension (used as monotherapy or in combination with other antihypertensive drugs).
The drug is prescribed for adults, inside, regardless of the meal.
At edema the drug is prescribed in a dose 5 mg 1 time / day. If necessary, the dose can be gradually increased to 20 mg 1 time / day. In some cases, it is recommended to apply before 40 mg / day.
At edema, associated with congestive heart failure administered at a dose of 5-20 mg 1 time / day. When necessary, the daily dose can be gradually increased, doubling its, maximum 200 mg.
At edema, associated with chronic renal failure starting dose is 20 mg / day. If necessary, the dose can be gradually increased, doubling its, to achieve an optimal diuretic effect. The maximum daily dose - 200 mg.
At edema, associated with liver cirrhosis the drug is prescribed in a dose 5-10 mg 1 time / day. If necessary, the dose can be gradually increased, doubling its, until an appropriate diuretic effect is achieved. There have been no appropriately controlled studies in patients with liver disease using doses greater than 40 mg / day.
At primary arterial hypertension dose of 2.5 mg 1 time / day. If necessary, the dose can be gradually increased to 5 mg / day. According to research, dose more 5 mg / day does not lead to a further decrease in blood pressure. The maximum effect is achieved after about 12 weeks of continuous treatment.
Elderly patients do not require dose adjustment.
From the hematopoietic system: в отдельных случаях – снижение числа эритроцитов и лейкоцитов, and platelet.
Metabolism: в отдельных случаях – гиповолемия, electrolyte imbalance, kaliopenia, an increase in serum uric acid blood, glucose and lipid.
Cardio-vascular system: в отдельных случаях – нарушения кровообращения и тромбоэмболии (due to dehydration), decrease in blood pressure.
From the digestive system: Gastrointestinal dysfunction symptoms, loss of appetite, dry mouth; в отдельных случаях – повышение активности печеночных ферментов (incl. GGT), pancreatitis.
From the urinary system: acute urinary retention, increased levels of urea and creatinine in plasma.
From the central and peripheral nervous system: headache, dizziness, weakness, drowsiness, confusion, convulsions, paresthesias in extremities.
From the senses : visual disturbances, noise in ears, deafness.
Allergic reactions: itching, rashes and photosensitivity.
- Anurija;
- Hepatic coma and prekomatosnoe state;
- chronic renal failure with increasing azotemia;
- Arrhythmia;
- Hypotension;
- Pregnancy;
- Lactation (no data on use during lactation);
- Up to 18 years (efficacy and safety have not been established);
- Hypersensitivity to torasemide and sulfonamides.
FROM caution the drug should be used in patients with diabetes mellitus, gout, disorders of water and electrolyte balance, impaired liver function, cirrhosis of the liver, predisposition to hyperuricemia.
The drug is contraindicated in pregnancy and lactation (breast-feeding).
With prolonged treatment is recommended to monitor the electrolytic balance, Glucose, Uric acid, creatinine and blood lipids.
when hypokalemia, giponatriemii, hypovolemia or urination disorders before prescribing Trigrima® carry out the elimination of all the listed conditions.
In the presence of diabetes mellitus, it is necessary to control carbohydrate metabolism.
For thrombocytopenia or bone marrow suppression, and should stop the drug for skin rashes.
Use in Pediatrics
No information regarding the application Trigrima® children.
Effects on ability to drive vehicles and management mechanisms
At the initial stage of reception it is not suitable for driving vehicles and service mechanisms because of the possibility of dizziness.
Symptoms: No typical picture of poisoning; in case of an overdose, an increase in diuresis is observed, accompanied by hypovolemia, electrolyte imbalance, followed by a drop in blood pressure, sleepiness, confusion, collapse, possible gastrointestinal disturbances.
Treatment: проведение симптоматической терапии – снижение дозы или отмена препарата с одновременным восполнением потери жидкости и электролитов. Spetsificheskiy antidote unknown.
Trigrama® improves myocardial sensitivity to cardiac glycosides when potassium or magnesium deficiency.
While admission to mineralogical- and glucocorticoids, laxatives may increase the excretion of potassium.
Trigrama® enhances the effect of antihypertensive drugs.
In high doses of Trigrim® able to enhance the toxic effect of aminoglycosides, antibiotics, cisplatin; nephrotoxic effect of cephalosporins, as well as cardio- and the neurotoxic effect of lithium.
Torasemide may enhance the effects of curariform muscle relaxants and theophylline.
When using salicylates in high doses, their toxic effect may increase, and the effect of antidiabetic agents, opposite, loosen.
Sequential or concomitant use of torasemide with ACE inhibitors can lead to a transient fall in blood pressure. This can be avoided, by reducing the initial dose of ACE, or by reducing the dose of torasemide (or by temporarily canceling it).
Torasemide reduces the effect of vasoconstrictors (epinephrine and norepinephrine).
NSAIDs and probenecid may reduce diuretic and hypotensive effect of torasemide.
Cholestyramine is capable of reducing absorption from the gastrointestinal tract of torasemide (in animal studies).
The drug is released under the prescription.
The drug should be stored out of reach of children, dry, protected from light, at a temperature no higher than 25 ° C. Shelf life - 3 year.
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