Torasemide - instructions, analogues, reviews
In this article, you can read the instructions for using the drug Torasemide. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Torasemide in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Torasemide in the presence of existing structural analogues. Use to treat hypertension and reduce pressure and get rid of swelling in adults, children, as well as during pregnancy and lactation. Composition of a diuretic.
Torasemide - loop diuretic.The main mechanism of action of the drug is due to the reversible binding of torasemide to the cotransporter of sodium / chlorine / potassium ions located in the apical membrane of the thick segment of the ascending loop of Henle, resulting in reduced or completely inhibited reabsorption of sodium ions and reduced osmotic pressure of the intracellular fluid and water reabsorption. Torasemide blocks aldosterone receptors of the myocardium, reduces fibrosis and improves diastolic function of the myocardium. Due to the antialdosteron effect, torasemide causes hypokalemia to a lesser degree than furosemide, while it exhibits greater activity and its action for a longer time.
The diuretic effect develops about an hour after ingestion, reaching a maximum in 2-3 hours, and lasts up to 18 hours, which facilitates the tolerability of therapy due to the lack of very frequent urination during the first hours after ingestion, limiting the activity of patients.
Torasemide reduces systolic and diastolic blood pressure in the "lying" and "standing" positions.
The use of torasemide is the most reasonable choice for long-term therapy.
Composition
Torasemide + auxiliary substances.
Pharmacokinetics
After oral administration, torasemide is rapidly and almost completely absorbed into the digestive tract. Eating does not have a significant effect on the absorption of the drug. Bioavailability is 80-90% with minor individual variations. Communication with plasma proteins is more than 99%. Metabolised in the liver with the help of 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. On average, about 83% of the dose is given by the kidneys: unchanged (24%) and mostly inactive metabolites (M1 - 12%, M3 - 3%, M5 - 41%). Torasemide and its metabolites are slightly excreted by hemodialysis and haemofiltration.
Indications
- edematous syndrome of various genesis, incl. with chronic heart failure;
- diseases of the liver, lungs and kidneys;
- arterial hypertension.
Forms of release
Tablets 5 mg and 10 mg.
Instructions for use and dosage
Inside, 1 time per day, without chewing, squeezed enough water. Tablets can be taken at any convenient constant time, regardless of food intake.
Edema Syndrome in Chronic Heart Failure
The usual initial dose is 10-20 mg once a day. If necessary, the dose can be doubled until the desired effect is achieved.
Edema syndrome with kidney disease
The usual initial dose is 20 mg once a day. If necessary, the dose can be doubled until the desired affect is obtained.
Edema syndrome with liver disease
The usual initial dose is 5-10 mg once a day. If necessary, the dose can be doubled until the desired effect is achieved.
The maximum single dose is 40 mg, it is not recommended to exceed it (no experience is available).
The drug is used for a long period or until the edema disappears.
Arterial hypertension
The initial dose is 2.5 mg (1/2 tablet 5 mg each) once a day. If there is no therapeutic effect for 4 weeks, the dose is increased to 5 mg once a day.
In the absence of an adequate reduction in blood pressure at a dose of 5 mg once a day for 4-6 weeks, the dose is increased to 10 mg once a day. If a dose of 10 mg does not give the desired effect, a hypotensive drug of another group should be added to the treatment regimen.
Older patients do not need a dose adjustment.
Side effect
- headache;
- dizziness;
- drowsiness;
- cramps in the muscles of the lower limbs;
- confusion of consciousness;
- fainting;
- paresthesia in the extremities (sensation of numbness, "crawling crawling" and tingling);
- impaired vision;
- hearing impairment;
- tinnitus and hearing loss (usually, reversible) usually in patients with renal insufficiency or hypoproteinemia (nephrotic syndrome);
- extrasystole;
- arrhythmia;
- tachycardia;
- excessive decrease in blood pressure;
- orthostatic hypotension;
- collapse;
- deep vein thrombosis;
- thromboembolism;
- a decrease in the volume of circulating blood;
- nose bleed;
- diarrhea;
- abdominal pain;
- flatulence;
- dry mouth;
- nausea, vomiting;
- loss of appetite;
- pancreatitis;
- dyspeptic disorders;
- itching;
- rash;
- hives;
- polymorphic erythema;
- exfoliative dermatitis;
- purpura;
- vasculitis;
- photosensitization;
- muscle weakness;
- increased frequency of urination;
- polyuria;
- nocturia;
- increased urge to urinate;
- oliguria;
- urinary retention (in patients with obstruction of the urinary tract);
- interstitial nephritis;
- hematuria (blood in the urine);
- decreased potency;
- hypokalemia, hyponatremia, hypomagnesemia, hypocalcemia, hypochloraemia;
- thrombocytopenia, leukopenia, agranulocytosis;
- hyperglycemia;
- a decrease in glucose tolerance (a manifestation of latent diabetes mellitus is possible);
- aplastic or hemolytic anemia.
Contraindications
- hypersensitivity to torasemide or to any of the components of the drug;
- allergy to sulfonamides (sulfanilamide antimicrobial agents or sulfonylureas);
- renal failure with anuria;
- hepatic coma and precoma;
- refractory hypokalemia;
- refractory hyponatremia;
- hypovolemia (with or without arterial hypotension) or dehydration;
- marked abnormalities of urine outflow from any etiology (including unilateral urinary tract damage);
- glycoside intoxication;
- acute glomerulonephritis;
- sinoatrial and AV-blockade of 2-3 degrees;
- decompensated aortic and mitral stenosis;
- hypertrophic obstructive cardiomyopathy;
- increased central venous pressure (more than 10 mm Hg);
- arrhythmia;
- chronic renal failure with increasing azotemia;
- hyperuricemia;
- age under 18 years (safety and efficacy not established);
- pregnancy;
- the period of breastfeeding;
- simultaneous use of aminoglycosides and cephalosporins;
- lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Carefully
- arterial hypotension:
- stenosing arteriosclerosis of cerebral arteries;
- hypoproteinemia;
- disorders of urinary outflow (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis);
- ventricular arrhythmia in the anamnesis;
- acute myocardial infarction (increased risk of developing cardiogenic shock);
- diarrhea;
- pancreatitis;
- hypokalemia;
- hyponatremia;
- impaired liver function, cirrhosis, renal failure, hepatorenal syndrome;
- diabetes mellitus (decreased glucose tolerance);
- gout, predisposition to hyperuricemia;
- anemia;
- simultaneous use of cardiac glycosides, corticosteroids and adrenocorticotropic hormone (ACTH).
Application in pregnancy and lactation
Torasemide does not have teratogenic affect and fetotoxicity, it penetrates the placental barrier, causing disturbances in water-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.
There is no data on the release of thorasemide into breast milk, so if thorasemide is needed during lactation, breastfeeding should be stopped.
Use in children
The use of the drug in children and adolescents under the age of 18 is contraindicated (safety and efficacy not established).
Application in elderly patients
Older patients do not need a dose adjustment.
special instructions
The drug Torasemide should be used strictly according to the doctor's prescription. Patients with hypersensitivity to sulfonamides and sulfonylureas may have cross-sensitivity to torasemide.
Patients receiving high doses of torasemide for a long period, in order to avoid the development of hyponatremia, hypokalemia and metabolic alkalosis, a diet with a sufficient content of common salt and the use of potassium preparations is recommended.
The risk of hypokalemia is greatest in patients with cirrhosis of the liver, with intensified diuresis, with insufficient intake of electrolytes with food, as well as with simultaneous use of corticosteroids or ACTH.
An increased risk of development of water-electrolyte imbalance is noted in patients with renal insufficiency. During the course of treatment with Torasemide, it is necessary to periodically monitor the content of electrolytes in the blood plasma (including sodium, calcium, potassium, magnesium), acid-base state, concentration of residual nitrogen, creatinine, uric acid and, if necessary, appropriate corrective therapy with a higher multiplicity in patients with frequent vomiting and against the background of parenterally injected fluids). In patients with developed water-electrolyte disorders, hypovolemia, or prerenal azotemia, laboratory analysis data may include: hyper- or hyponatremia, hyper- or hypochloraemia, hyper- or hypokalemia, acid-base balance disorders, and increased urea concentration in the blood plasma. If these disorders occur, stop taking the preparation of Torasemide until normal values are restored, then resume treatment with a smaller dose of Torasemide.
With the appearance or strengthening of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended to suspend treatment with Torasemide.
The choice of dosage regimen for patients with ascites on the background of cirrhosis of the liver should be carried out under stationary conditions (violations of the water-electrolyte balance may lead to the development of hepatic coma). This category of patients shows regular monitoring of plasma electrolytes.
The use of torasemide may exacerbate gout. Patients with diabetes mellitus or with reduced glucose tolerance require periodic monitoring of glucose concentrations in the blood and urine.
In patients in the unconscious state, with benign prostatic hyperplasia, narrowing of the ureters, diuretic control is necessary in connection with the possibility of acute urinary retention.
In patients with diseases of the cardiovascular system, especially those taking cardiac glycosides, diuretic-induced hypokalemia can cause arrhythmias.
Impact on the ability to drive vehicles and mechanisms
During the treatment period, patients should refrain from driving and other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions (risk of dizziness and drowsiness).
Drug Interactions
With the simultaneous use of torasemide with mineral- and glucocorticosteroids, amphotericin B increases the risk of hypokalemia; with cardiac glycosides - the risk of developing glycosidic intoxication due to hypokalemia (for high- and low-polar cardiac glycosides) increases and the half-life extends (for low-polar cardiac glycosides).
The administration of torasemide increases the concentration and risk of developing nephro- and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid, antibiotics, salicylates, cisplatin, platinum preparations, amphotericin B (due to competitive renal excretion).
Sequential or simultaneous use of torasemide with ACE inhibitors or angiotensin 2 receptor antagonists can lead to a dramatic decrease in blood pressure. This can be avoided by decreasing the initial dose of an ACE inhibitor or by lowering the dose of torasemide (or temporarily abolishing it).
Non-steroidal anti-inflammatory drugs, sucralfate reduce the diuretic effect of torasemide due to inhibition of prostaglandin synthesis, disruption of renin activity in plasma and aldosterone removal.
Torasemide enhances the antihypertensive effect of antihypertensive drugs, neuromuscular blockade of depolarizing muscle relaxants (suxamethonium), and weakens the effect of nondepolarizing muscle relaxants (tubocurarine).
Torasemide reduces the renal clearance of lithium preparations and increases the likelihood of intoxication.
Torasemide increases the effectiveness of diazoxide and theophylline, reduces the effectiveness of 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 blood plasma.
With the simultaneous use of cyclosporine and torasemide, the risk of gouty arthritis increases due to the fact that cyclosporine can cause impairment of urate excretion by the kidneys, and torasemide is hyperuricemia.
The simultaneous use of probenecid or Methotrexate may decrease the effectiveness of torasemide (the same pathway of secretion). On the other hand, torasemide can lead to a decrease in renal elimination of these drugs.
It was reported,that in patients with a high risk of developing nephropathy taking torasemide inside, with the introduction of radiopaque agents, renal dysfunction was observed more often than in patients at high risk of developing nephropathy who received intravenous hydration prior to the administration of radiocontrast agents.
Bioavailability and, as a consequence, the effectiveness of torasemide can be reduced by joint therapy with colestyramine.
Analogues of the drug Torasemide
Structural analogs for the active substance:
- Britomar;
- Diver;
- Torasemide Vertex;
- Torasemide Canon;
- Trigrim.
Analogues for the pharmacological group (diuretics):
- Aquaphor;
- Acrypamide;
- Aldactone;
- Arindap;
- Arifon;
- Arifon retard;
- Acetazolamide;
- Brinaldiks;
- Britomar;
- Brusniver;
- Bufenox;
- Verospilactone;
- Veroshpiron;
- Hydrochlorothiazide;
- Hydrochlorothiazide;
- Hypothiazide;
- Diakarb;
- Diver;
- Isobar;
- Indap;
- Indapamide;
- Indapamide Sandoz;
- Indapamid Teva;
- Inder;
- Inverse;
- Inspra;
- Ionik;
- Kanefron H;
- Clopamid;
- Lasix;
- Lespenefril;
- Lescopryl;
- Lauras;
- Mannitol;
- Mannitol;
- Moderetik;
- Urea;
- Pamid;
- Retapres;
- Spironolactone;
- Tenzar;
- Triompur compositum;
- Trigrim;
- Urakton;
- Urological (diuretic) collection;
- Uroflux;
- Phytolysin;
- Furosemide;
- Fursemide;
- Tsimalon;
- Espiro.