TORASEMIDE PILLS 5MG

Trade name of the drug:

Torasemide-SZ

International non-proprietary name:

torasemide

Dosage Form:

pills

Composition:

1 pill contains:

dosage 5 mg:

active ingredient:Torsemide-5 mg

excipients: lactose monohydrate (lactopress) (milk sugar) - 89.3 mg; pregelatinized starch (starch 1500) - 24.5 mg; colloidal silicon dioxide (Aerosil) - 0.6 mg;Magnesiumstearate - 0.6 mg.

dosage 10 mg:

active ingredient: Torsemide - 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 of white or almost white color, round, flat-cylindrical with a facet and

on one side.

Pharmacotherapeutic group of the drug:

diuretic agent

Pharmacological properties

Pharmacodynamics

Torsemide is a “loopback” diuretic. Maximum diuretic effect

develops 2-3 hours later after taking the drug inside. The main mechanism of the drug’s action is due to the reversible binding of Torsemide to the sodium / chlorine / potassium ion transporter located in the apical membrane of the thick segment of the ascending loop of Henle,as a result, the reabsorption of sodium ions is reduced or completely inhibited and the osmotic pressure of the intracellular fluid and water reabsorption are reduced. Blocks myocardial aldosterone receptors; reduces fibrosis and improves the diastolic function of the myocardium.

Torsemide to a lesser extent thanFurosemide, causes hypokalemia, while it exhibits greater activity and its effect is longer.

The use of Torsemide is the most reasonable choice for

long-term therapy.

Pharmacokinetics

After ingestion, Torsemide is rapidly and almost completely absorbed in the gastrointestinal tract. Eating does not have a significant effect on the absorption of the drug. The maximum concentration of Torsemide in plasma is noted 1-2 hours after ingestion. Bioavailability is 80 -90% with minor individual variations.

The diuretic effect lasts up to 18 hours, which facilitates tolerability of therapy due to the lack of very frequent urination in the first hours after taking the drug inside, which limits the activity of patients.

Communication with plasma proteins is more than 99%. The apparent volume of distribution is 16 liters. Metabolized in the liver using cytochrome P450 isoenzymes. As a result of successive reactions of oxidation, hydroxylation or ring hydroxylation, three metabolites are formed (M1, M3 and M5), which bind to plasma proteins by 86%, 95% and 97%, respectively.

The half-life (T1 / 2) of Torsemide and its metabolites is 3-4 hours and does not change in chronic renal failure.The total clearance of Torsemide is 40 ml / min, the renal clearance is 10 ml / min. On average, about 83% of the accepted dose is excreted by the kidneys: unchanged (24%) and mostly inactive metabolites (M1 -12%, M3 -3%, M5 -41%).

In renal failure, T1 / 2 does not change, T1 / 2 metabolites M3 and M5

increases. Torsemide and its metabolites are slightly excreted by

hemodialysis and hemofiltration.

In liver failure, the concentration of Torsemide 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 Torsemide and the metabolite M5 are slightly increased, the drug is unlikely to accumulate.

Indications for use

- edematous syndrome of various genesis, including in case of chronic heart failure, diseases of the liver, lungs and kidneys;

-arterial hypertension.

Contraindications

Hypersensitivity to Torsemide or to any of the components of the drug; in patients with allergies to sulfonamides (sulfanilamide antimicrobial agents or sulfonylureas); renal failure with anuria; hepatic coma and precoma; refractory hypokalemia / refractory hyponatremia; hypovolemia (with or without hypotension) or dehydration; pronounced violations of urine outflow of any etiology (including unilateral damage to the urinary tract);

glycoside intoxication; acute glomerulonephritis; decompensated aortic and mitral stenosis,hypertrophic obstructive cardiomyopathy; increase in central venous pressure (over 10 mm Hg); hyperuricemia; simultaneous use of aminoglycosides and cephalosporins; age up to 18 years; pregnancy, breastfeeding period; lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

 

Carefully

Arterial hypotension, stenosing atherosclerosis of cerebral arteries,

hypoproteinemia, predisposition to hyperuricemia, impaired urine outflow

(benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis), a history of ventricular arrhythmia, acute myocardial infarction (increased risk of developing cardiogenic shock), diarrhea, pancreatitis, diabetes mellitus (reduced glucose tolerance), hemorrhagic syndrome, hemorrhagic syndrome (reduced glucose tolerance), hemorrhagic syndrome, hemorrhage, pancreatitis, diabetes mellitus (reduced glucose tolerance), hemorrhoids, pancreatitis, diabetes mellitus (reduced glucose tolerance), hemorrhoid syndrome, pancreatitis, diabetes mellitus (reduced glucose tolerance), hemorrhagic syndrome, hemorrhage simultaneous use of cardiac glycosides, corticosteroids and adrenocorticotropic hormone (ACTH).

Use during pregnancy and during breastfeeding

Torsemide does not have a teratogenic effect and fetotoxicity, penetrates the placental barrier, causing disruption of water-electrolyte metabolism and

thrombocytopenia in the fetus.

Controlled studies on the use of Torsemide in pregnant women have not been conducted, the drug is not recommended for use during pregnancy.

It is not known whether Torsemide penetrates into breast milk. If necessary, the use of the drug Torasemide-SZ in the period of lactation should stop breastfeeding.

Dosage and administration

Inside, once a day, without chewing, drinking plenty of water.Tablets can be taken at any convenient constant time, regardless of the meal.

Edematous syndrome in chronic heart failure

The usual initial dose is 10-20 mg once a day. If necessary, the dose can be doubled to obtain the desired effect.

Edematous syndrome with kidney disease

The usual starting dose is 20 mg once a day. If necessary, the dose can be doubled to obtain the desired effect.

Edema syndrome with liver disease

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

Arterial hypertension

The initial dose is 2.5 mg (1/2 pills of 5 mg) once a day. In the absence of a therapeutic effect within 4 weeks, the dose is increased to 5 mg once a day.

In the absence of an adequate reduction in blood pressure, when taken in 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, the antihypertensive drug of another group is added to the treatment regimen.

Elderly patients dose adjustment is not required.

Side effect

The incidence of side effects is classified as recommended.

World Health Organization:

very often: ≥ 1/10 (> 10%);

often: ≥ 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: frequency cannot be estimated based on available data.

From the nervous system:

often - headache, dizziness, drowsiness;

infrequently - muscle cramps of the lower limbs;

the frequency is unknown - confusion, fainting, paresthesia in the extremities (feeling of numbness, "crawling goosebumps" and tingling).

From the senses:

the frequency is unknown - impaired vision, hearing loss, tinnitus and hearing loss (usually reversible), usually in patients with renal

deficiency or hypoproteinemia (nephrotic syndrome).

Since the cardiovascular system:

infrequently - extrasystole, arrhythmia, tachycardia;

frequency is unknown - excessive reduction in blood pressure, orthostatic hypotension, collapse, deep vein thrombosis, thromboembolism, decrease in circulating blood volume.

On the part of the respiratory system:

infrequently - nosebleeds.

From the digestive system:

often - diarrhea;

infrequently - abdominal pain, flatulence, polydipsia;

frequency is unknown - dry mouth, nausea, vomiting, loss of appetite, pancreatitis,

dyspeptic disorders, intrahepatic cholestasis .

Skin and Subcutaneous Tissues:

frequency is unknown - pruritus, rash, urticaria, erythema polymorphic,

exfoliative dermatitis, purpura, vasculitis, photosensitivity.

From the musculoskeletal system:

frequency unknown - muscle weakness.

From the urinary system:

often - an increase in the frequency of urination, polyuria, nocturia;

infrequently - increased urge to urinate;

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

From the reproductive system:

frequency unknown - decrease in potency.

Metabolism:

frequency is unknown - hypokalemia, hyponatremia, hypomagnesemia, hypocalcemia, hypochloremia, metabolic alkalosis, hypovolemia, dehydration (more often in elderly patients).

From the laboratory indicators:

infrequently - hypercholesterolemia, hypertriglyceridemia;

frequency unknown - hyperuricemia, a slight increase in plasma alkaline phosphatase activity, an increase in plasma creatinine and urea concentrations, an increase in the activity of certain “liver” enzymes in the blood plasma (for example, gamma-glutamyltransferase), thrombocytopenia, leukopenia, agranulocytosis, hyperglycemia, decrease glucose tolerance (latent diabetes mellitus is possible to manifest).

Other:

frequency unknown - aplastic or hemolytic anemia.

Overdose

Symptoms:

increased diuresis, accompanied by a decrease in circulating volume

blood and violation of water and electrolyte balance of blood, followed by a pronounced decrease in blood pressure, drowsiness and confusion, collapse.

Gastrointestinal disturbances may occur.

Treatment:

There is no specific antidote. Provocation of vomiting, gastric lavage,

Activated carbon. Treatment is symptomatic, dose reduction or drug withdrawal and at the same time replenishment of the BCC and indicators of water and electrolyte balance and acid-base status under the control of serum electrolyte concentrations, hematocrit, symptomatic treatment.

Hemodialysis is ineffective.

Interaction with other drugs

Increases concentration and risk of nephro and ototoxic effects

cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid,Cisplatin, amphotericin B (due to competitive renal excretion).

Increases the effectiveness of diazoxide and theophylline, reduces - hypoglycemic

agents,Allopurinol.

Pressor amines and Torsemide mutually reduce effectiveness. Drugs that block canalic secretion, increase the concentration of Torsemide in serum.

With simultaneous use of glucocorticosteroids, amphotericin B increases the risk of developing hypokalemia, with cardiac

glycosides - increases the risk of glycosidic intoxication due to hypokalemia (for high-and low-polar) and lengthening half-life (for low-polar).

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

Non-steroidal anti-inflammatory drugs, sucralfat reduce the diuretic effect due to inhibition of prostaglandin synthesis, impaired renin activity in blood plasma and aldosterone elimination.

Enhances the antihypertensive effect of antihypertensive drugs, neuromuscular

blockade of depolarizing muscle relaxants (suxametonium) and weakens the effect

non-polarizing muscle relaxants (tubocurarine).

The simultaneous reception of large doses of salicylates during therapy with Torsemide

increases the risk of their toxicity (due to competitive renal

deductions).

Consistent or simultaneous use of Torsemide with inhibitors

angiotensin-converting enzyme (ACE) or angiotensin II receptor antagonists can lead to a strong reduction in blood pressure. This can be avoided by lowering the dose of Torsemide or temporarily canceling it.

Simultaneous use of probenecid orMethotrexatemay reduce

efficacy of Torsemide (identical secretion pathway). On the other hand, Torsemide may lead to a decrease in the renal elimination of these drugs.

With the simultaneous use of cyclosporine and Torsemide increases the risk of developing gouty arthritis due to the fact that cyclosporine can cause a violation of the excretion of urate by the kidneys, and Torsemide - hyperuricemia.

It has been reported that in patients at high risk of developing nephropathy, taking

Torsemide orally, with the introduction of radiopaque agents, renal dysfunction was observed more often than in patients with a high risk of developing nephropathy, who underwent intravenous hydration before the administration of radiopaque agents.Bioavailability and, as a result, the effectiveness of Torsemide can be reduced with co-therapy with colestyramine.

special instructions

Apply strictly on doctor's prescription.

Patients with hypersensitivity to sulfonamides and derivatives

sulfonylureas may have a cross-sensitivity to Torasemide-C3.

Patients receiving high doses of the drug Torasemid-SZ for a long period, in order to avoid the development of hyponatremia, metabolic alkalosis and hypokalemia, are recommended to have a diet with an adequate amount of sodium chloride and the use of potassium preparations.

An increased risk of developing disorders of water and electrolyte balance is noted in

patients with renal failure. During the course of treatment is necessary

periodically monitor the concentration of electrolytes in blood plasma (including

sodium,Calcium, potassium, magnesium), acid-base state, residual nitrogen,

creatinine, uric acid and, if necessary, carry out the corresponding

corrective therapy (with greater frequency in patients with frequent vomiting and on the background of

parenterally administered fluids).

With the onset or increase of azotemia and oliguria 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 liver cirrhosis should be carried out in

stationary conditions (violations of water and electrolyte balance may lead to the development of hepatic coma).This category of patients shows regular monitoring of plasma electrolytes.

Patients with diabetes mellitus or with reduced glucose tolerance require periodic monitoring of the concentration of glucose in the blood and urine.

In unconscious patients with hyperplasia of the prostate gland, narrowing of the ureters, control of diuresis is necessary due to the possibility of acute urinary retention.

Influence on ability to drive motor transport and control mechanisms

During the treatment period, patients should refrain from managing transport

means and activities of other potentially hazardous activities that require increased concentration of attention and quickness of psychomotor reactions (risk of dizziness and drowsiness).

Storage conditions

In a dry, dark place, at a temperature not higher than 25 ° C.

Keep out of the reach of children.