Pharmacological properties

Pharmacodynamics. torasemid sandoz is loopback diuretic; in the low doses applied to antihypertensive treatment has weak diuretic and saluretichesky effect. in higher doses torasemid strengthens a diuresis in a dose-dependent way. torasemid sandoz shows the maximum diuretic activity in 2–3 h after intake.

Pharmacokinetics. After oral administration torasemid quickly and almost it is completely absorbed; The C _max in blood plasma is reached in 1–2 h after reception. The system bioavailability is 80–90%. Linking of a torasemid with proteins of blood plasma makes 99%, metabolites of M ₁ , M ₃ and M ₅ — 86; 95 and 97% respectively. Distribution volume — 16 l. Torasemid is metabolized by oxidation and hydroxylation with formation of three metabolites: M ₁ , M ₃ and M ₅ . The m ₅ pharmacological is inactive, and and the M ₃ is the share of a share of metabolites of M _{1 about 10% of pharmacological effect of drug. Final T ½ a torasemid and its metabolites makes at healthy volunteers of 3-4 h. The general clearance of a torasemid — 40 ml/min., renal clearance — about 10 ml/min. About 80% of a dose are allocated in the form of not changed torasemid (24%) and its metabolites: M 1 (12%), M 3 (3%), M 5 (41%). In a renal failure of T ½ torasemida does not change, and T ½ metabolites of M 3 and M 5 is extended. Torasemid and his metabolites are practically not removed by a hemodialysis or haemo filtration. At patients with an abnormal liver function or with heart failure of T ½ a torasemid and a metabolite of M 5 are slightly extended, however cumulation of a torasemid and its metabolites is improbable.}

Indication

Tablet on 5 mg — ag.

Tablet on 5; 10 and 20 mg — the hypostases caused by heart failure.

Tablet on 50; 100 and 200 mg — hypostases, raised by the ABP in a heavy renal failure (clearance of creatinine of 20 ml/min.) in the presence though any residual diuresis (200 ml for 24 h), including when carrying out a hemodialysis.

Use

Pill should be taken in the morning, without chewing, washing down with a small amount of liquid.

Duration of treatment depends on the course of the disease; in heart failure the treatment has to continue before disappearance of hypostases.

AG. The recommended dose for adults makes 2.5 mg/days (tablets on 5 mg have to risk and it is possible to divide them into equal doses on 2.5 mg). If after 2-month therapy the torasemidy ABP in a dose of 2.5 mg/days of normalization it is not reached, the dose can be raised to 5 mg (1 times a day). The maximum effect is usually noted in 3 months after an initiation of treatment. Use of doses does not lead more than 5 mg to strengthening of antihypertensive effect.

Hypostases. Therapy it is necessary to begin 5 mg/days with a dose. Usually this dose is considered supporting. If the daily dose of 5 mg is not enough, it is necessary to apply a daily dose of 10 mg which it is necessary to appoint daily. Depending on weight of a condition of the patient the daily dose can be gradually increased up to 20 mg of a torasemid (1 times a day).

Cirrhosis. The general initial dose makes 5–10 mg of 1 times a day at the combined use with medicaments — antagonists of Aldosteronum or with the diuretics promoting a potassium delay in an organism. In case of lack of necessary diuretic action it is necessary to double a dose (10–20 mg/days) before achievement of necessary effect.

In chronic kidney disease individually and depends on degree of a renal failure. If the dose of 20 mg/days is not enough, it can be raised to 50 mg of a torasemid of 1 times a day and, in case of need, gradually to raise to maximum — 200 mg of 1 times a day. The maximum daily dose of 200 mg patients should appoint only with heavy renal failures (clearance of creatinine of 20 ml/min.) (including during a hemodialysis) in the presence of a diuresis not less than 200 ml / 24 h

Patients with a liver failure. Treatment of such patients should be carried out with care as increase in concentration of a torasemid in blood plasma is possible.

Patients of advanced age. Special selection of a dose is not required.

Contraindication

Hypersensitivity to a torasemid, to derivatives of sulphonylurea or any of excipients. a renal failure with an anury, a hepatic coma or a prekoma, arterial hypotension, arrhythmia. hypovolemia, hyponatremia, hypopotassemia. considerable disturbance of urination, for example owing to a prostatauxe. gout. simultaneous use with aminoglycosides or cephalosporins. the renal failure caused by nephrotoxic substances.

Side reactions are classified by

by emergence frequency: very often (≥1/10); often (≥1/100 and 1/10); infrequently (≥1/1000 and 1/100); seldom (≥1/10,000 and 1/1000); very seldom (1/10,000); it is unknown (frequency cannot be estimated due to the lack of data).

from metabolism: often — strengthening of a metabolic alkalosis; a hypopotassemia at the accompanying diet with the low content of potassium, in vomiting, diarrhea, after excessive use of depletive and also at patients with chronic dysfunction of a liver. Depending on a dosage and duration of treatment disturbances of water and electrolytic balance, for example a hypovolemia, a hypopotassemia, a hyponatremia are possible. At considerable loss of liquid and electrolytes owing to the strengthened urination can note arterial hypotension, a headache, an asthenia, drowsiness, especially in an initiation of treatment and at patients of advanced age.

from a cardiovascular system: very seldom — thromboses, arterial hypotension, cardial and cerebral ischemia with possible development of disturbances of a warm rhythm, stenocardia, acute myocardial infarction, a syncope.

from a digestive tract: often — loss of appetite, nausea, vomiting, a stomach ache, indigestion and diarrhea, a constipation, a meteorism, mainly in an initiation of treatment; infrequently — dryness in a mouth; very seldom — pancreatitis.

from an urinary system: infrequently — patients with disorders have urinations, for example in a prostatauxe, the ischuria and a recystectasia is possible; desires to urination.

from a gepatobiliarny system: often — increase in level of some liver enzymes (γ-glutamil-transpeptidaza) in blood plasma.

from blood and lymphatic system: very seldom — reduction of quantity of thrombocytes, erythrocytes and/or leukocytes.

from skin and hypodermic fabric: very seldom — allergic reactions (for example an itching, rash, a dieback, photosensitivity), it was reported about heavy skin reactions.

from an organ of sight: very seldom — disorders of vision.

from an organ of hearing: very seldom — sonitus, a hearing loss.

General disorders: often — confusion of consciousness, increased fatigue, the general weakness (especially in an initiation of treatment).

Laboratory researches: often — increase in concentration of uric acid, glucose and lipids (XC, TG) in blood plasma; infrequently — increase in level of creatinine and urea in blood plasma is possible.

Special instructions

before use of medicament the existing hypopotassemia, a hyponatremia or a hypovolemia and to otkorrigirovat urination disturbances.

At long-term treatment by diuretic recommends to control regularly electrolytic balance (especially at patients who at the same time apply glycosides of a foxglove, GKS, a mineralokortikosteroida or depletive), the level of glucose, uric acid, creatinine and lipids of blood.

Special attention is required by patients with a tendency to development of a hyperuricemia and gout.

to Patients with obvious or latent diabetes needs to control metabolism of carbohydrates.

due to the lack of sufficient experience of clinical use torasemid at pathological changes of acid-base equilibrium; at pathological changes of a picture of blood, for example thrombocytopenia or anemia at patients without renal failure; along with lithium, aminoglycosides, cephalosporins; in the renal failure caused by nefrotoksichny substances; to children; to patients of advanced age (recommendations about dosing are absent).

Torasemid should be applied with extra care at patients with the liver diseases which are followed by cirrhosis and ascites as sudden changes of water and electrolytic balance can lead to a hepatic coma. Therapy using a torasemid (as well as other diuretics) at patients of this group needs to be carried out in the conditions of a hospital. For prevention of a hypopotassemia and a metabolic acidosis it is necessary to appoint medicament with medicaments — antagonists of Aldosteronum or the medicaments promoting a potassium delay in an organism.

After reception of a torasemid were noted by the ototoxicity phenomena (sonitus and a hearing loss) which had reversible character, but direct link with use of medicament is not established.

When prescribing diuretics needs to control carefully clinical symptoms of disturbance of electrolytic balance, a hypovolemia, an extrarenal azotemia and other disturbances which can be shown in the form of dryness in a mouth, thirst, weakness, slackness, drowsiness, excitement, muscular pain or spasms, a myasthenia, hypotonia, an oliguria, tachycardia, nausea, vomiting. The excessive diuresis can become the cause of dehydration of an organism, lead to decrease in volume of the circulating blood, a thrombogenesis and an embolism of blood vessels, especially at patients of advanced age. It is necessary to pay attention to signs of haemo concentration and loss of electrolytes in an initiation of treatment and at patients of advanced age.

to Patients with disturbances of water and electrolytic balance needs to stop use of medicament and after elimination of undesirable effects to restore therapy, since lower doses.

When prescribing medicament regular laboratory control of indicators of content of potassium and other electrolytes in blood plasma. It is also regularly necessary to control blood cells (quantity of erythrocytes, leukocytes, thrombocytes).

. Patients with a liver failure should appoint medicament with care as increase in plasma concentration of a torasemid is possible.

Tablet Torasemid Sandoz on 5 mg, 10 mg, 20 mg contain lactose. If at the patient the intolerance of some sugars is established, it is necessary to consult with the doctor before taking this drug. To patients with rare hereditary intolerance of a galactose, deficiency of lactase or a sprue of glucose galactose medicament is not recommended.

Tablet Torasemid Sandoz on 50 mg, 100 mg, 200 mg contain the castor oil hydrogenated which can cause indigestion and diarrhea.

Use during pregnancy or feeding by a breast

Pregnancy. Reliable data about influence of a torasemid on an embryo and a fruit at the person are absent. There is information of rather reproductive toxicity of a torasemid. Torasemid gets through a placental barrier. Due to the above torasemid it is possible to apply during pregnancy only according to vital indications and in minimum possible effective dose.

for the standard scheme of treatment of arterial hypertension or hypostases at pregnant women as they are capable to reduce perfusion of a placental barrier and to make toxic impact on pre-natal fetation. If torasemid to apply to treatment of pregnant women with a heart or renal failure, then it is necessary to carry out careful monitoring of electrolytes and a hematocrit and also fetation.

feeding Period breast. Now it is not established whether gets torasemid into breast milk of animals or the person. It is impossible to exclude risk of use of medicament for newborns/babies. Therefore use of medicament during feeding by a breast contraindicated. If it is necessary to apply a torasemid during this period, feeding by a breast it is necessary to stop.

Fertility. The research of influence of a torasemid on fertility at people was not conducted.

Children. Drug is not used at children due to the lack of data.

Ability to influence speed of response at control of vehicles or work with mechanisms. Before clarification of individual reaction on torasemid during treatment it is necessary to be careful at control of vehicles and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Period of pregnancy or feeding by a breast.

Interaction

At simultaneous use of a torasemid with cardiac glycosides the sensitivity of a cardiac muscle to these medicines owing to deficiency of potassium or magnesium can increase. at simultaneous use with mineralo- and glucocorticoids, depletive the risk of emergence of deficiency of potassium increases.

Torasemid strengthens effect of other medicinal antihypertensive drugs, in particular APF inhibitors. Simultaneous use with APF inhibitors can lead to heavy arterial hypotension. It can be avoided if to lower an initial dose of APF inhibitor or a dose of a torasemid in 2–3 days prior to use of APF inhibitors.

Torasemid can weaken vasoconstrictive effect of epinephrine and Norepinephrinum.

Torasemid reduces expressiveness of action of antidiabetic means.

Torasemid, especially in high doses, can exponentiate nephrotoxic and ototoksichesky effects of aminoglikozidny antibiotics (for example Kanamycinum, gentamycin, Tobramycinum), toxic effects of medicaments of platinum and nephrotoxic effects of cephalosporins.

Torasemid strengthens effect of theophylline and kurarepodobny muscle relaxants.

Probenetsid and NPVP (for example indometacin, derivatives of propionic acid) weaken diuretic and hypotensive action of a torasemid.

At simultaneous use of a torasemid and medicaments of lithium the concentration of lithium in blood can increase and amplify kardio- and neurotoxicity of the last.

.

At simultaneous use with Colestyraminum the absorption of a torasemid can decrease therefore the expressiveness of its action decreases.

Overdose

Symptoms. the typical symptomatology is unknown. in case of overdose can note an artificial diuresis with risk of excessive loss of liquid and electrolytes. drowsiness, confusion of consciousness, arterial hypotension, cardiovascular insufficiency and disturbances from a digestive tract are possible.

Treatment. Specific antidote is absent. Depending on symptoms of overdose the dose decline or medicament withdrawal is recommended. Actions for recovery of water and electrolytic balance are carried out. Torasemid is not brought from blood by means of a hemodialysis. Treatment in case of a hypovolemia: substitution of volume of liquid. Treatment in case of a hypopotassemia: prescribing of medicaments of potassium. Treatment of cardiovascular insufficiency: sitting position of the patient and, if necessary, purpose of symptomatic therapy.

Acute anaphylaxis (urgent measures). At the first emergence of skin reactions (such as, for example, small tortoiseshell or erubescence), the excited condition of the patient, a headache, the increased sweating, nausea, cyanosis to carry out vein catheterization; to give to the patient horizontal position, to provide free intake of air, to appoint oxygen. If necessary to apply administration of epinephrine, the solutions substituting the volume of liquid, GKS.

Storage conditions

At a temperature not above 25 °C.

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