Torasemide pills 5mg, 20pcs

Composition

For 1 tablet of 5.0 mg:

Active ingredient:

torasemide – 5.0 mg.

Auxiliary substances:

lactose monohydrate ( milk sugar) – 90.4 mg,

sodium carboxymethyl starch-3.0 mg,

magnesium stearate-0.8 mg,

colloidal silicon dioxide-0.8 mg

Pharmacological action

Pharmacotherapy group: Diuretic ATX code: C03saPharmacodynamics :

Torasemide 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.

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.

Torasemide causes hypokalemia to a lesser extent than furosemide, while it is more active and its effect is longer.

The use of torasemide is the most reasonable choice for long-term therapy.

Pharmacokinetics:

After 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.

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 reactions of hydroxylation or ring hydroxylation, three metabolites are formed (M1m3 and M5), which bind to plasma proteins by 86%,95% and 97%, respectively.

The half-life (T 1/2) 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 and 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%).

With renal insufficiency, T 1/2 does not change, and T 1/2 of the M3 and M5 metabolites 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 T 1/2 of torasemide and the M5 metabolite is slightly increased, accumulation of the drug is unlikely.

Elderly patients

The pharmacokinetic profile of torasemide in elderly patients is similar to that in young patients, except that there is a decrease in the renal clearance of torasemide due to the characteristic age-related renal dysfunction in elderly patients. The total clearance and half-life do not change.

Indications

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

– arterial hypertension.

Use during pregnancy and lactation

Pregnancy

Torasemide does not have a teratogenic effect and fetotoxicity penetrates the placental barrier causing disorders of water and electrolyte metabolism and thrombocytopenia in the fetus. Controlled studies on the use of torasemide in pregnant women have not been conducted, and therefore the drug is not recommended for use during pregnancy.

Breast-feeding period

It is not known whether torasemide passes into breast milk. If it is necessary to use the drug Torasemide during lactation, it is necessary to stop breastfeeding.

Contraindications

– Hypersensitivity to torasemid or to any component of the drug; patients allergic to sulfonamides (sulfa antibiotics or sulfonylureas) may be cross-allergic to torasemid;

– 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;

– sinoatrial and atrioventricular block degree II-III arrhythmia;

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

– hyperuricemia;

– age under 18 years;

– pregnancy period of breastfeeding;

– concomitant use of aminoglycosides and cephalosporins;

– lactose intolerance lactase deficiency or glucose – galactose malabsorci.

With caution:

– Arterial hypotension;

– stenosing atherosclerosis of cerebral arteries;

– hypoproteinemia;

– violation of the outflow of urine (benign prostatic hyperplasia narrowing of the urethra or hydronephrosis);

– ventricular arrhythmia in history;

acute myocardial infarction (increased risk of developing cardiogenic shock);

diarrhea;

– pancreatitis;

diabetes mellitus (impaired glucose tolerance);

– hepatorenal syndrome;

the liver cirrhosis;

renal failure;

– gout;

– predisposed to hyperuricemia;

– anemia;

– concomitant use of cardiac glycosides, corticosteroids and adrenocorticotropic hormone (ACTH);

– hypokalemia;

– hyponatremia.

Side effects

the incidence of side effects is classified according to the recommendations of the world health organization: very common: ≥ 1/10 (> 10%); often: from ≥ 1/100 to < 1/10 (> 1% and < 10%); uncommon: from ≥ 1/1000 to < 1/100 (> 01% and < 1%); rare: from ≥ 1/10000 to < 1/1000 (> 001% and < 01%); very rare: < 1/10000 (< 001%); frequency not known: frequency cannot be estimated based on available data.

Nervous system disorders:

often – headache dizziness drowsiness;

infrequently – muscle cramps of the lower extremities hyperactivity nervousness;

frequency unknown-confusion syncope paresthesia in the extremities (feeling of numbness “crawling” and tingling).

Visual disturbances:

frequency unknown-visual impairment

Hearing disorders and labyrinth disorders:

frequency unknown-hearing impairment tinnitus and hearing loss (usually reversible) usually in patients with renal insufficiency or hypoproteinemia (nephrotic syndrome).

Disorders of the cardiovascular system:

infrequently-extrasystole arrhythmia tachycardia;

frequency unknown-excessive decrease in blood pressure orthostatic hypotension collapse deep vein thrombosis thromboembolism hypovolemia (decrease in the volume of circulating blood).

Respiratory system disorders:

infrequently-nosebleeds.

Disorders of the digestive system:

common – diarrhea;

uncommon-abdominal pain flatulence polydipsia;

frequency unknown-dry mouth nausea vomiting loss of appetite pancreatitis dyspeptic disorders intrahepatic cholestasis.

Skin and subcutaneous tissue disorders:

frequency unknown-pruritus skin rash urticaria erythema multiforme exfoliative dermatitis purpura vasculitis photosensitization.

Musculoskeletal disorders:

frequency unknown-muscle weakness.

Urinary system disorders:

often-increased frequency of urination polyuria nocturia;

infrequently-frequent urge to urinate;

frequency unknown-polyuria urinary retention (in patients with urinary tract obstruction) interstitial nephritis hematuria.

Reproductive system disorders:

frequency unknown-decreased potency.

Metabolic disorders:

infrequently-polydipsia

frequency unknown-hypokalemia hyponatremia hypomagnesemia hypocalcemia hypochloremia metabolic alkalosis hypovolemia dehydration (more often in elderly patients) impaired glucose tolerance (possible manifestation of latent diabetes mellitus)

Violations of laboratory parameters:

infrequently-hypercholesterolemia hypertriglyceridemia thrombocytosis;

frequency unknown-hyperglycemia hyperuricemia slight increase in the activity of alkaline phosphatase in blood plasma increased concentration of creatinine and urea in blood plasma increased activity of certain “liver” enzymes in blood plasma (for example, gamma-glutamyltransferase) thrombocytopenia leukopenia agranulocytosis.

Disorders of the blood and lymphatic system:

the frequency is unknown-aplastic or hemolytic anemia.

General disorders and disorders at the injection

site infrequently-asthenia thirst weakness increased fatigue

Interaction

Concomitant use of torasemide with the mineral-and glucocorticosteroids amphotericin B increases the risk of hypokalemia; with cardiac glycosides-increases the risk of glycoside intoxication due to hypokalemia (for high-and low-polar cardiac glycosides) and prolongation of the half-life (for low-polar cardiac glycosides).

Taking torasemide 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.

Consistent or concomitant use of torasemide with angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists can lead to a sharp decrease in blood pressure. This can be avoided by reducing the dose of torasemide or temporarily stopping it.

Nonsteroidal anti-inflammatory drugs sucralfate reduce the diuretic effect of torasemide due to inhibition of prostaglandin synthesis, impaired plasma renin activity and aldosterone excretion.

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

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.

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

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.

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.

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

The bioavailability and resulting efficacy of torasemide may be reduced with co-therapy with colestyramine.

How to take, course of use and dosage

Inside once a day without chewing with a sufficient amount of water. Tablets can be taken at any convenient constant time, regardless of food intake.

Edematous syndrome in chronic heart failure

The usual 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 usual starting dose is 20 mg once daily. If necessary, the dose can be doubled until the desired effect is obtained.

Edematous syndrome in liver disease

The usual starting dose is 5-10 mg once a day. If necessary, the dose can be doubled until the desired effect is obtained. The maximum single dose is 40 mg. It is not recommended to exceed it (there is no experience of using it). The drug is used for a long period or until the edema disappears.

Arterial hypertension

The initial dose is 25 mg once a day. In the absence of a therapeutic effect for 4 weeks, the dose is increased to 5 mg once a day. If there is no adequate reduction in blood pressure when taking a dose of 5 mg once a day for 4-6 weeks, the dose is increased to 10 mg once a day. If the use of the drug at a dose of 10 mg per day does not give the desired effect, a hypotensive drug of another group is added to the treatment regimen.

Elderly patients do not need to adjust the dose.

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 symptomatic dose reduction or discontinuation of the drug and simultaneously replenishment of BCC and indicators of water-electrolyte balance and acid-base state under the control of serum concentrations of electrolytes hematocrit symptomatic treatment. Hemodialysis is ineffective.

Special instructions

Use strictly as directed by your doctor.

Patients with hypersensitivity to sulfonamides and sulfonylureas may have cross-sensitivity to Torasemide.

In patients, especially at the beginning of treatment with Torasemide and in the elderly, it is recommended to monitor the electrolyte balance of the volume and concentration of circulating blood.

During long-term treatment with Torasemide, it is recommended to regularly monitor the electrolyte balance (especially potassium levels) of glucose, uric acid, creatinine, lipids and cellular components of the blood.

Patients receiving high doses of Torasemide for a long period of time to avoid the development of hyponatremia. for metabolic alkalosis and hypokalemia, a diet with a sufficient amount of table salt is recommended (it is not advisable to limit the intake of table salt) and the use of potassium preparations.

The risk of hypokalemia is greatest in patients with cirrhosis of the liver with severe diuresis with insufficient intake of electrolytes with food as well as with simultaneous treatment with corticosteroids or ACTH.

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, conduct appropriate correction therapy (with greater frequency in patients with frequent vomiting and against the background of parenterally administered fluids).

In patients with advanced water-electrolyte disorders or prerenal azotemia, laboratory test data may include hyper-or hyponatremia hyper – or hypochloremia hyper – or hypokalemia acid-base balance disorders and elevated blood urea levels. If these disorders occur, it is necessary to stop taking Torasemide until normal values are restored, and then resume treatment with Torasemide at a lower dose.

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

Selection of the dosage regimen for patients with ascites on the background of 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.

For the prevention of hypokalemia, the use of potassium preparations and potassium-sparing diuretics (primarily spironolactone) is recommended, as well as a diet rich in potassium.

The use of the drug Torasemide can cause an exacerbation of gout.

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 and narrowing of the ureters, monitoring of diuresis is necessary due to the possibility of acute urinary retention.

In patients with cardiovascular diseases, especially those taking cardiac glycosides, diuretic-induced hypokalemia can cause arrhythmias.

Influence on the ability to drive vehicles and fur. :

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, as there is a risk of dizziness and drowsiness.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Torasemide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets