Торсид® (tablets)

General characteristics. Structure:

Active ingredient: torasemide;

1 tablet contains 5 mg or 10 mg of a torasemid in terms of 100% substance;

excipients: lactoses monohydrate, starch prezhelatinizirovanny, silicon dioxide colloid anhydrous, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. The main mechanism of diuretic action is caused by reversible linkng with a kotransporter of Na+/2Cl-/K + in an apical part of a Henle's loop owing to what decreases or the renal reabsorption of ions of sodium and chlorine in the ascending part of a Henle's loop is completely oppressed, the osmotic pressure of intracellular liquid and a reabsorption of water decreases. In the range of doses of 5 - 100 mg increase in a diuresis is proportional to a dose logarithm. Increase in a diuresis arises and when other diuretic drugs (for example, tiazida) do not render sufficient effect, for example, at bounded function of kidneys any more. Eliminates hypostases, has anti-hypertensive effect which is caused by reduction of peripheric resistance of vessels due to reduction of content of free calcium in cells of a muscular layer of arteries and normalization of the broken electrolytic balance. Thereof the kontraktilnost and reaction of vessels to own pressor substances of an organism, in particular catecholamines decreases. Improves operating conditions of heart due to reduction before - and afterloads. After oral administration the maximum diuretic action continues 1 - 3 h, and the diuretic effect remains for nearly 12 h. Hypotensive action of a torasemid develops gradually within the first week and reaches a maximum no later than 12 weeks.

Pharmacokinetics. After intake it is quickly and almost completely soaked up from a digestive tract. The maximum concentration in a blood plasma is observed in 1-2 h. Linkng of a torasemid with proteins of plasma makes more than 99%, metabolites of M1, M3 and M5 – 86%, 95% and 97% respectively. Bioavailability makes about 80% with insignificant individual variations and does not depend on meal. It is metabolized in a liver by system of P450 cytochrome with formation of metabolites (M1, M3 and M5). The main metabolite of M5 of diuretic effect does not render, the operating metabolites of M1 and M3 jointly cause about 10% of pharmakodinamichesky action. The elimination half-life of a torasemid and its metabolites at healthy volunteers makes 3 – 4 h. About 83% of the accepted dose are removed through renal tubules: in not changed look (24%) and in the form of metabolites (M1 – 12%, M3 – 3%, M5 – 41%). The general clearance makes 40 ml/min., renal clearance - about 10 ml/min. At a renal failure the general clearance and an elimination half-life of a torasemid do not change, and the elimination half-life of M3 and M5 is extended. However pharmakodinamichesky characteristics remain invariable, severity of a renal failure does not influence action duration. At patients with abnormal liver functions or with heart failure elimination half-lives of a torasemid and a metabolite of M5 are slightly extended, cumulation of a torasemid and its metabolites is not observed.

Pharmaceutical characteristics:

main physical and chemical properties: tablets with a flat surface with risky and a facet, white or almost white color.

Indications to use:

Essential hypertensia. Treatment and prevention of a recurrence of hypostases and/or exudates.

Route of administration and doses:

Appoint to adults and children 12 years are more senior. Accept in 1 times a day in the morning after food, do not chew, wash down with a small amount of liquid. The dose and duration of a course of treatment are established individually taking into account indications, efficiency and portability of therapy.

At essential hypertensia. Usually the dose makes 2,5 mg of Torsid. If after 12 weeks therapy by drug in a dose of 2,5 mg a day normalization of arterial pressure is not reached, it is possible to increase a dose to 5 mg. Further increase in a dose is inexpedient because it will not lead to a further lowering of arterial pressure.

At hypostases or exudates: the initial dose makes 5 mg of Torsid a day, at insufficiently expressed effect the dose can be raised, depending on disease severity, to 20 mg of drug a day.

Features of use:

At long therapy by Torsid regular control of electrolytic balance (in particular serum potassium), the level of glucose, uric acid, creatinine and lipids in blood serum, blood pictures is necessary.

It is necessary to consider that increase in level of glucose in blood of the patient can be connected with a possible latent or manifest diabetes mellitus therefore such patients should carry out careful control of sugar of blood.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

It is not necessary to use drug during control of vehicles or during the work which is connected with the increased concentration of attention.

Side effects:

From cardiovascular system: disturbances of water and electrolytic balance (hypovolemia, hypopotassemia, hyponatremia); in isolated cases - strengthening of a metabolic alkalosis. At considerable losses of liquid and electrolytes, owing to strong urination arterial hypotension, confusion of consciousness can be observed; in isolated cases - fibrinferments, cardial and cerebral ischemia with possible development of disturbances of a cordial rhythm, stenocardia, acute myocardial infarction, a syncope.

From the central nervous system: headache, dizziness, increased fatigue, myotonia.

From a digestive tract: lock, anorexia, nausea, vomiting, stomach ache, diarrhea, increase in some enzymes of a liver (in particular gamma глутамилтранспептидазы).

From an urinary system: at patients with disorders of urination (for example, at a prostatauxe) intensive urination can lead to an ischuria and hyperdystension of a bladder; seldom – increase in creatinine and urea in blood.

From a metabolism: seldom – increase in level in blood of uric acid, glucose, lipids (triglycerides, cholesterol).

From system of blood: seldom – reduction of number of thrombocytes, erythrocytes and/or leukocytes.

Allergic reactions: seldom - an itch, a dieback, photosensitivity; in some cases – heavy skin reactions.

Others: seldom – dryness in a mouth, paresthesia; in some cases – vision disorders; in isolated cases - a sonitus, a hearing impairment.

Interaction with other medicines:

Torsid strengthens action of other medicinal anti-hypertensive means, in particular inhibitors of an angiotensin-converting enzyme therefore the corresponding combination therapy can lead to an excessive lowering of arterial pressure.

At simultaneous use with Torsid of foxglove drugs the deficit of potassium caused torasemidy can lead to expansion of range of side effect of both drugs.

Torsid weakens action of antidiabetic means. Probenetsid and non-steroidal anti-inflammatory drugs weaken diuretic and hypotensive action of Torsid. At therapy by salicylates in high doses Torsid can strengthen their toxic action on the central nervous system. Torsid, especially in high doses, can strengthen from - and nephrotoxic action of aminoglikozidny antibiotics and derivatives of platinum. Torsid strengthens effect of theophylline and kurarepodobny muscle relaxants. Purgatives, and also mineralo-and glucocorticoids can strengthen the possible loss of potassium caused by Torsid. At simultaneous use of Torsid and drugs of lithium concentration of lithium in blood and by that to amplify effect of lithium and its side effects can increase. Torsid weakens vasoconstrictive action of catecholamines. At simultaneous use with holestiraminy absorption of a torasemid can decrease and by that its action can be weakened.

Contraindications:

Arterial hypotension, the renal failure which is followed by an anury, heavy abnormal liver functions with a loss of consciousness (a hepatic coma or a prekoma), a hypovolemia, a hyponatremia, a hypopotassemia, the expressed disturbances of a mochevyvedeniye (for example, as a result of a prostatauxe), gout, high extent of disturbances of cordial excitement and conductivity (for example, a sinoauricular block or an atrioventricular block ІІ or ІІІ degrees), pathological changes of acid-base balance, simultaneous therapy by lithium drugs, aminoglycosides or cephalosporins, pathological changes of a picture of blood (for example, thrombocytopenia or anemia at patients without renal failure), the renal failures caused by nephrotoxic substances, children's age up to 12 years, pregnancy, the feeding period a breast, the increased individual sensitivity to a torasemid related with it on structure to substances (compound of sulfanylurea) and/or drug components.

Overdose:

At overdose strengthening of a diuresis with danger of loss of liquid and electrolytes, drowsiness, confusion of consciousness, arterial hypotension, a collapse and disorders of a digestive tract can be observed. Treatment. Drug withdrawal, medical actions for normalization of water and electrolytic balance: at a hypopotassemia appoint 7,4% chloride potassium solution (at an alkalosis) or 10% hydrocarbonate potassium solution (at acidosis), in both cases – as addition to carrier solution; at a hyponatremia – 5,8% solution of sodium of chloride or 8,4% bicarbonate sodium solution (at simultaneous acidosis), in both cases – as addition to carrier solution. There is no specific antidote.

Use during pregnancy or feeding by a breast.

Administration of drug during pregnancy is contraindicated. During treatment by Torsid feeding by a breast should be stopped.

Children.

It is contraindicated to children aged up to 12 years.

Storage conditions:

Period of validity. 2 years. It is not necessary to use drug after the termination of the period of validity specified on packaging. To store in the dry, protected from light place at a temperature not over 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 5 mg. On 10 tablets in the blister. On 1 or 3 blisters enclosed in a pack.

Tablets on 10 mg. On 10 tablets in the blister. On 1, 3 or 9 blisters enclosed in a pack.