Toradiv 10 mg tablets # 30

Toradiv (TORADIV) instructions for use

Composition

active ingredient: torasemide; 1 tablet contains torasemide 10 mg
auxiliary substances: lactose, corn starch, silicon dioxide colloid, magnesium stearate.

Dosage form

Pills.

Basic physical and chemical properties:

white round tablets with one-sided notching for division.

Pharmacological group

Diuretic preparations . Highly active diuretics. The ATX code is C03C A04.

Pharmacological properties

Pharmacological.

Torasemide acts as a saluretic, the action is associated with the inhibition of renal absorption of sodium and chlorine ions in the ascending part of the Henle loop. In humans, the diuretic effect quickly reaches its maximum within the first 2-3 hours after parenteral and oral administration, respectively, and remains constant for almost 12:00. In healthy volunteers in the dose range of 5-100 mg, an increase in diuresis was observed in proportion to the logarithm of the dose. An increase in diuresis was observed even in cases when other diuretics, for example, distally acting effective thiazide series diuretics, no longer showed the desired effect, for example, in renal failure. Due to this mechanism of action, torasemide leads to a decrease in edema. In the case of heart failure, torasemide reduces the manifestations of the disease and improves the functioning of the myocardium by reducing pre- and postnagruzku. After ingestion, the antihypertensive effect of torasemide develops gradually, starting from the first week after the start of treatment.Maximum antihypertensive action is achieved no later than 12 weeks. Torasemide reduces blood pressure by reducing the overall peripheral resistance of blood vessels. This influence is explained by the normalization of the disturbed electrolyte balance, mainly due to a decrease in the increased activity of free calcium ions in muscle cells of arterial vessels, and was found in patients suffering from arterial hypertension. This influence probably reduces the increased susceptibility of the vessels to endogenous vasopressor substances, for example catecholamines.

Pharmacokinetics.

After oral administration, torasemide is rapidly and completely absorbed within 1-2 hours. Bioavailability is approximately 80-90%; under the condition of full absorption, the maximum value of the effect of the first passage is 10-20%. Eating does not affect the absorption of torasemide. The binding of torasemide to plasma proteins is 99%, the metabolites M 1, M 3, and M 5 are 86%, 95% and 97%, respectively. In humans, torasemide is metabolized with the formation of three metabolites - M 1, M 2 and M 5. There is no evidence of the existence of other metabolites. Metabolites M 1 and M 5 are formed as a result of oxidation of the propellant group located on the phenyl ring to the carboxylic acid. Metabolite M 3 is formed as a result of hydroxylation of the ring. The kinetics of torasemide and its metabolites is characterized by a linear relationship, which means that the maximum serum concentration and the area under the serum content curve increases in proportion to the dosage. The final half-life (t 1/2) of torasemide and its metabolites in healthy volunteers is 3-4 hours. The total clearance of torasemide is 40 ml / min, the renal clearance is about 10 ml / min. The main metabolite M 5 does not have a diuretic effect, and the metabolites M 1 and M 3, taken together, account for about 10% of the pharmacodynamic effect. With renal failure, the total clearance and half-life of torasemide do not change, and the half-life of M 3 and M 5 increases. However, the pharmacodynamic characteristics remain unchanged, and the severity of renal failure for duration of action is not affected. In patients with impaired hepatic function or heart failure, the half-life of torasemide and metabolite M 5 slightly lengthen, and the amount of the substance excreted in the urine corresponds to the amount withdrawn in healthy people, therefore, the cumulation of torasemide and its metabolites should not be expected. Torasemide and its metabolites are practically not excreted in hemodialysis and haemofiltration.

Indications

Treatment and prevention of relapses of edema and / or effusions caused by heart failure.

Contraindications

Hypersensitivity to the active substance, other preparations of sulfonylurea or to auxiliary substances. Renal failure with anuria. Hepatic coma or precoma. Arterial hypotension. Hypovolemia. Hyponatremia. Hypokalemia. Significant impairment of urination, for example, due to prostatic hypertrophy.

Interaction with other drugs and other interactions

Torasemide enhances the effect of other antihypertensive agents, in particular ACE inhibitors, which can lead to an excessive decrease in blood pressure when they are used simultaneously. With the simultaneous use of torasemide with digitalis preparations, a potassium deficiency caused by the use of a diuretic can lead to an increase or increase in the side effects of both drugs. Torasemide may reduce the effectiveness of antidiabetics. Probenecid and non-steroidal anti-inflammatory drugs can inhibit the diuretic and hypotensive effect of torasemide. When treating salicylates in high doses, torasemide can increase their toxic effect on the central nervous system. Torasemide, especially in high doses, can enhance the nephrotoxic effect of aminoglycoside antibiotics, for example, kanamycin, gentamicin, tobramycin and cytostatics-platinum derivatives, as well as the nephrotoxic effect of cephalosporins. Torasemide can enhance the effect of theophylline, as well as the effect of curare-like drugs on muscle relaxation. Laxatives, as well as mineral and glucocorticoids, can enhance potassium loss due to torasemide. With the simultaneous use of torasemide and lithium preparations, an increase in the concentration of lithium in the plasma may increase the influence and actions of lithium.Torasemide can reduce the vasoconstrictive action of catecholamines, for example epinephrine and norepinephrine.With simultaneous application with colestyramin, the absorption of torasemide and, accordingly, its expected efficacy may decrease.

Application features

Before starting the use of the drug, it is necessary to eliminate the existing hypokalemia, hyponatremia or hypovolemia.With prolonged use of torasemide, regular monitoring of the electrolyte balance, in particular potassium in the blood serum, is necessary, especially in patients who simultaneously take glycosides of digitalis, SCS, mineralocorticosteroids or laxatives. In addition, it is necessary to regularly monitor the glucose, uric acid, creatinine and lipid levels in the blood.

Torasemide should be used with extreme caution in patients with liver disease, accompanied by cirrhosis and ascites, as sudden changes in the water-electrolyte balance can lead to hepatic coma. Therapy with torasemide (as well as other diuretics) patients of this group should be performed in a hospital. To prevent hypokalemia and metabolic acidosis, the drug should be prescribed with preparations of aldosterone antagonists or drugs that promote the retention of potassium in the body. After using the drug, there were cases of ototoxicity (tinnitus and hearing loss) that were reversible, but there was no direct connection with the use of the drug.

When prescribing diuretics, it is necessary to carefully monitor the clinical symptoms of electrolyte imbalance, hypovolemia, extrarenal azotemia and other disorders that may manifest as dry mouth, thirst, weakness, lethargy, drowsiness, agitation, muscle pain or judgment, myasthenia gravis, hypotension, oliguria, tachycardia, nausea, vomiting.Excessive diuresis can cause dehydration, lead to a decrease in the volume of circulating blood, thrombosis and embolism, especially in elderly patients.

Patients with impaired water-electrolyte balance should stop using the drug and after eliminating the undesirable effects of regaining therapy, starting with lower doses.

Due to the fact that when the diuretic is treated with an increase in blood glucose in patients with latent and overt diabetes, a thorough check of the metabolism of carbohydrates is necessary. Also, regular monitoring of the blood picture (red blood cells, white blood cells, platelets) is necessary. Especially at the beginning of treatment of elderly patients it is necessary to pay special attention to the appearance of symptoms of electrolyte loss and blood thickening.

Because there is not sufficient clinical experience, torasemide should not be administered in the following conditions and conditions: gout; arrhythmia, for example sinoatrial block, blockade of II and III degrees; pathological changes in acid-base metabolism; concomitant therapy with lithium, aminoglycoside or cephalosporins; pathological changes in the blood picture, such as thrombocytopenia or anemia in patients without renal failure, renal dysfunction caused by nephrotoxic substances. The drug contains lactose, therefore, patients with rare hereditary diseases such as galactose intolerance, Lappease lactase deficiency or malabsorption of glucose-galactose should not use this drug.

The use of torasemide tablets may be the reason for obtaining a positive result in the doping test. It is impossible to predict the effect on the health status if the torasemide tablet is applied incorrectly, that is, for the purpose of doping, in this case, possible harm to health can not be ruled out.

Use during pregnancy or lactation

Pregnancy. There is no reliable data on the effect of torasemide on the embryo and human fetus. In animal experiments, the toxic effect of torasemide on reproductive function was shown. Torasemide penetrates the placental barrier. In connection with the foregoing, torasemide can be used during pregnancy only for vital indications and in the minimum effective dose. Diuretics are unsuitable for a standard treatment of edema in pregnant women, because they can reduce the perfusion of the placental barrier and cause toxic effects on fetal development. If torasemide is used to treat pregnant women with heart failure, then careful monitoring of the electrolyte and hematocrit level, as well as fetal development, is necessary.

The period of breastfeeding. The use is contraindicated. If torasemide should be used during this period, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Even with proper use, torasemide can have a significant negative impact on the ability to drive vehicles or work with machinery. This is in many respects related to such cases as the initiation of treatment, an increase in the dose of the drug, the replacement of the drug or the appointment of concomitant therapy. Therefore, during the use of the drug should be very careful when driving vehicles or other mechanisms.

Dosing and Administration

Adults. Treatment begins with the application of a daily dose of 5 mg torasemide, which is ½ tablets of the drug torada.Usually this dose is considered to be supportive. If the daily dose of 5 mg is not sufficient, a daily dose of 10 mg of torasemide should be applied, which the doctor appoints daily. Depending on the severity of the patient's condition, the daily dose can be increased to 20 mg of torasemide. The maximum daily dose is 40 mg. Tablets take on an empty stomach without chewing, squeezed with a small amount of liquid. The duration of treatment depends on the course of the disease.

Patients with hepatic insufficiency. Treatment of such patients should be carried out with caution, since an increase in the concentration of torasemide in the blood plasma is possible.

Patients of advanced age. A special dose selection is not required.

Children

Do not use torasemide in children, because there is not enough clinical experience.

Overdose

The typical symptomatology is unknown. Overdosing can cause a strong diuresis, including the risk of excessive loss of water and electrolytes, drowsiness, anemic syndrome (a form of impaired consciousness), symptomatic arterial hypotension, cardiovascular failure and disorders of the digestive tract.

Treatment of overdose. The specific antidote is unknown. Symptoms of intoxication disappear, as a rule, when the dose is reduced and the drug is withdrawn, as well as when the fluid and electrolytes are properly replaced (control is necessary). Torasemide is not excreted from the blood by hemodialysis. Treatment in the case of hypovolemia - replacement of the volume of fluid. Treatment in the case of hypokalemia - the appointment of potassium preparations.Treatment of cardiovascular failure is to provide the patient with a sitting position and, if necessary, prescribe symptomatic therapy.

Anaphylactic shock (emergency measures). At the first appearance of skin reactions (such as urticaria or reddening of the skin), the excited state of the patient, headache, sweating, nausea, cyanosis, the catheterization of the vein of the patient should be placed in a horizontal position, ensure free air intake, and assign oxygen. If necessary, enter epinephrine, solutions that replace the volume of fluid, glucocorticoid hormones.

Adverse Reactions

To assess the side effects, such a classification of frequency of their manifestations was used: very often - ≥ 10%; often - ≥ 1% - <10%; sometimes - ≥ 0.1% - <1%; rarely - ≥ 0.01% - <0.1%; very rarely - <0.01%, including isolated cases.

Metabolism / electrolytes. Often intensification of metabolic alkalosis; muscle spasms (especially at the beginning of treatment), non-digestibility of food, flatulence, urge to urinate, rash, increased uric acid and glucose levels in the blood, and hyperlipidemia (including increased cholesterol and triglycerides) hypokalemia with a concomitant low-calorie diet, with vomiting , diarrhea, after excessive use of laxatives, as well as in patients with chronic liver dysfunction. Depending on the dosage and duration of treatment, there may be abnormalities in the water and electrolyte balance, for example, hypovolemia, hypokalemia and / or hyponatremia. With significant losses of fluid and electrolytes as a result of increased urination, there may be arterial hypotension, headache, fatigue, thirst, drowsiness, especially at the beginning of treatment and in elderly patients.

From the cardiovascular system. Very rarely, due to possible thickening of the blood, thromboembolic complications, confusion, arterial hypotension, as well as impaired blood circulation and cardiac activity, including ischemia of the heart and brain, can occur, which can lead, for example, to arrhythmia, angina, acute myocardial infarction , syncope.

From the digestive system. Often disorders of the digestive tract (especially at the beginning of treatment), including lack of appetite, stomach pain, nausea, vomiting, diarrhea, constipation. Very rarely pancreatitis.

From the side of the kidneys and urinary tract. Sometimes an increase in the concentration of creatinine and urea. In patients with urinary disorders, increased urine production can lead to delay and excessive stretching of the bladder.

From the liver and biliary tract. Often: increase in the concentration of certain hepatic enzymes (gamma-glutamyltranspeptidase) in the blood.

From the skin and the immune system. Very rarely: allergic reactions, such as pruritus, rash, photosensitivity, skin reactions.

From the side of the blood. Very rarely: decrease in the number of platelets, red blood cells and / or leukocytes, as a result of hemoconcentration.

General manifestations. Often: headache, dizziness, fatigue, general weakness (especially at the beginning of treatment). Sometimes dry mouth, unpleasant sensations in the extremities (paresthesia). Very rarely: visual disturbances, ringing in the ears, hearing loss.

Shelf life

2 years.

Storage conditions

Store in the original packaging at a temperature not higher than 25 ° C. Keep out of the reach of children.

Packaging

For 10 tablets in a blister, 3 blisters per pack.

Category of leave

On prescription.