Diver - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 58.44 mg, corn starch 14.56 mg, sodium carboxymethyl starch 0.80 mg, silicon dioxide colloidal anhydrous 0.60 mg, magnesium stearate 0.60 mg.

1 tablet of 10 mg contains:

active substance: torasemide 10.00 mg;

Excipients: lactose monohydrate 116.88 mg, corn starch 29.12 mg, sodium carboxymethyl starch 1.60 mg, silicon dioxide colloidal anhydrous 1.20 mg, magnesium stearate 1.20 mg.

Description:

Dosage of 5 mg:

white or almost white round biconvex tablets with a bevel, with a risk on one side and engraved "915" on the other side.

Dosage of 10 mg:

white or almost white round biconvex tablets with a bevel, with a risk on one side and engraved "916" on the other side.

Pharmacotherapeutic group:Diuretic agent.

ATX: & nbsp

C.03.C.A Sulfonamide diuretics

C.03.C.A.04 Torasemide

Pharmacodynamics:Torasemide is a "loop" diuretic. The maximum diuretic effect develops 2-3 hours after ingestion. The main mechanism of action of the drug is due to the reversible binding of torasemide to the sodium / chlorine / potassium ion transportator located in the apical membrane of the thick segment of the ascending loop of Henle,

or completely inhibited reabsorption of sodium ions and decreases the osmotic pressure of the intracellular fluid and reabsorption of water. It blocks aldosterone receptors of the myocardium reduces fibrosis and improves diastolic function of the myocardium.

Torasemide is less than furosemide, causes hypokalemia, while it shows great activity and its effect is more prolonged.

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

Pharmacokinetics:

After oral administration torasemide quickly and almost completely absorbed in the gastrointestinal tract.The maximum concentration of torasemide in the blood plasma is noted 1-2 hours after ingestion after eating. Bioavailability is 80-90% with minor individual variations.

Diuretic effect persists up to 18 hours, which facilitates the tolerability of therapy due to the lack of very frequent urination during the first hours after taking the drug inside, which limits the activity of patients.

Communication with plasma proteins is more than 99%. Visible volume of distribution is 16 liters.

Metabolised in the liver with the help of cytochrome P450 isoenzymes. As a result of successive oxidation, hydroxylation or ring hydroxylation reactions, three metabolites (Ml, M3 and M5) are formed, which bind to plasma proteins by 86%, 95% and 97%, respectively.

The half-life (T1 / 2) of torasemide and its metabolites is 3-4 hours and does not change with 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 is excreted by the kidneys: unchanged (24%) and mostly inactive metabolites (Ml-12%, M3-3%, M5-41%).

With renal insufficiency T 1/2 does not change, T 1/2 metabolites M3 and M5 increases. Torasemide and its metabolites are slightly excreted by hemodialysis and haemofiltration.

In liver failure, 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 T 1/2 torasemide and metabolite M5 is slightly increased, cumulation of the drug is unlikely.

Indications:

- edematous syndrome of various genesis, incl. with chronic heart failure, liver, lung and kidney diseases;

- arterial hypertension.

Contraindications:Hypersensitivity to torasemide 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; pronounced hypokalemia; severe 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; decompensated aortic and mitral stenosis,hypertrophic obstructive cardiomyopathy; increased central venous pressure (> 10 mm Hg); hyperuricemia; age to 18 years; lactation period; lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:Arterial hypotension, stenosing arteriosclerosis of cerebral arteries, hypoproteinemia, predisposition to hyperuricemia, violation of urine 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, diabetes mellitus (decreased glucose tolerance), hepatorenal syndrome, gout, anemia, pregnancy.

Pregnancy and lactation:

Torasemide does not have a teratogenic effect and fetotoxicity, it penetrates the placental barrier, causing disturbances in water-electrolyte metabolism and thrombocytopenia in the fetus.

The drug Diver during pregnancy can be used only if the benefit to the mother exceeds the potential potential risk for the fetus only under the supervision of a doctor and only in minimum doses.

It is not known whether the torasemide in breast milk.If you need to use the drug Diver during lactation it is necessary to stop breastfeeding.

Dosing and Administration:

Inside, once a day, after breakfast, washed down with a small amount of water.

Ocular syndrome of various genesis, incl. with chronic heart failure, liver, lung and kidney diseases

The usual therapeutic dose is 5 mg orally once a day. If necessary, the dose should be gradually increased to 20-40 mg once a day, in some cases - up to 200 mg per day. The drug is prescribed for a long period or until the disappearance of edema.

Arterial hypertension

The initial dose is 2.5 mg (1/2 tablet of 5 mg) once a day. If necessary, the dose may be increased to 5 mg once a day.

To patients of advanced age correction of the dose is not required.

Side effects:

From the side of water-electrolyte and acid-base balance: hyponatremia, hypochloraemia, hypokalemia, hypomagnesemia, hypocalcemia, metabolic alkalosis. Symptoms that indicate the development of violations of electrolyte and acid-alkaline state, there may be headache, confusion, cramps, tetany, muscle weakness, heart rhythm disturbances and dyspepsia disorders; hypovolemia and dehydration (usually in elderly patients), which can lead to hemoconcentration with a tendency to develop thrombosis.

From the cardiovascular system: excessive reduction of arterial

pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decrease

volume of circulating blood.

From the side of metabolism: hypercholesterolemia, hypertriglyceridemia; transient increase in the concentration of creatinine and urea in the blood; increasing the concentration of uric acid in the blood, which can cause or intensify the manifestations of gout; decrease in glucose tolerance (manifestation of latent diabetes mellitus is possible).

From the urinary system: oliguria, acute urinary retention (for example, with prostatic hyperplasia, narrowing of the urethra, hydronephrosis); interstitial nephritis, hematuria, decreased potency.

From the digestive tract: nausea, vomiting, diarrhea, intrahepatic cholestasis, increased activity of "liver" enzymes, acute pancreatitis.

From the central nervous system, the organ of hearing: hearing impairment, usually reversible, and / or tinnitus, especially in patients with renal insufficiency or hypoproteinemia (nephrotic syndrome), paresthesia.

From the skin: dermal itching, urticaria, other types of rash or bullous skin lesion, polymorphic erythema, exfoliative dermatitis, purpura, fever, vasculitis, eosinophilia, photosensitivity; severe anaphylactic or anaphylactoid reactions up to shock, which until now have been described only after intravenous administration.

From the peripheral blood: thrombocytopenia; leukopenia; agranulocytosis, aplastic or hemolytic anemia.

Overdose:Symptoms: excessively increased diuresis, accompanied by a decrease in the volume of circulating blood and a violation of the electrolyte balance of blood, followed by a marked decrease in blood pressure, drowsiness and confusion, collapse. Gastrointestinal disorders may occur.

Treatment: there is no specific antidote. Provocation of vomiting, gastric lavage,

Activated carbon. Treatment is symptomatic, reduced dose or cancellation

preparation and at the same time 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.

Interaction:

Increases the concentration and risk of nephro- and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid, cisplatinum, amphotericin B (due to competitive renal excretion). Increases the effectiveness of diazoxide and theophylline, reduces hypoglycemic agents, allopurinol.

Pressor amines and torasemide mutually reduce efficiency. Drugs that block the tubular secretion, increase the concentration of torasemide in the blood serum.

With the simultaneous use of 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) and prolongation of the half-life (for low-polarity) increases. Reduces renal clearance of lithium preparations and increases the likelihood of development of intoxication.

Non-steroidal anti-inflammatory drugs, sucralfate reduce diuretic effect due to inhibition of prostaglandin synthesis, disturbance of renin activity in plasma and aldosterone removal. Strengthens the hypotensive effect of antihypertensive drugs, neuromuscular blockade of depolarizing muscle relaxants (suxamethonium) and weakens the effect of nondepolarizing muscle relaxants (tubocurarine).

Simultaneous reception of large doses of salicylates against the background of torasemide therapy increases the risk of their toxicity (due to competitive renal excretion).

Sequential or simultaneous use of torasemide with angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists can lead to a significant reduction in blood pressure. This can be avoided by reducing the dose of torasemide or temporarily canceling it. Simultaneous use of probenecid or methotrexate may decrease the effectiveness of torasemide (the same way of secretion). On the other hand torasemide can lead to a decrease in renal elimination of these drugs.

With the simultaneous use of cyclosporine and torasemide, the risk of gouty arthritis is increased due to the fact that ciclosporin may cause impairment of urate excretion by the kidneys, and torasemide hyperuricemia.

It was reported that in patients with a high risk of developing nephropathy, torasemide Inside, with the introduction of radiocontrast agents, renal dysfunction was observed more often than in patients with a high risk of developing nephropathy, who received intravenous hydration prior to the administration of radiocontrast agents.

Special instructions:

Apply strictly according to the doctor's prescription.

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

Patients receiving high doses of Diver for a prolonged period, in order to avoid the development of hyponatremia, metabolic alkalosis and hypokalemia, a diet with a sufficient content of table salt and the use of potassium preparations is recommended.

Increased risk of development of violations of water-electrolyte balance is observed in patients with renal insufficiency.During course treatment it is necessary to periodically monitor the concentration of plasma electrolytes blood (including sodium, calcium, potassium, magnesium), acid-base state, residual nitrogen, creatinine, uric acid and carry out if necessary appropriate corrective therapy (with a higher multiplicity in patients with frequent vomiting and against the background of parenterally injected fluids).

With the appearance or strengthening of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended to suspend treatment.

The choice of the dose regimen for patients with ascites on the background of liver cirrhosis to conduct in stationary conditions (violations of water-electrolyte balance may lead to the development of hepatic coma). This category of patients is shown regular monitoring of blood plasma electrolytes.

In patients with diabetes mellitus or with reduced tolerance to glucose periodic monitoring of glucose concentrations in blood and urine is required.

In patients with unconsciousness, with hyperplasia of the prostate gland, narrowing of the ureters, control of diuresis is necessary in connection with the possibility of acute urinary retention.

During treatment, patients should refrain from management vehicles and occupations of other potentially hazardous species Activities that require increased concentration and speed psychomotor reactions.

Form release / dosage:

Tablets 5 mg and 10 mg.

Packaging:

For 10 tablets in a blister of PVC / PVDC film and aluminum foil. For 2 or 6 blisters together with instructions for use in a cardboard box.

Storage conditions:At a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001027

Date of registration:31.08.2010

The owner of the registration certificate:Pliva of Hrvatska dooPliva of Hrvatska doo Croatia

Manufacturer: & nbsp

PLIVA HRVATSKA, d.o.o. Croatia

Representation: & nbspTeva Teva Israel

Information update date: & nbsp11.09.2015

Illustrated instructions

Instructions

Diver (Diuver)