Torasemide

When ATH:
C03CA04

Pharmacological action.

Torasemide acts as saluretikami, inhibiting renal reabsorption of sodium and chlorine ions in the ascending part of the loop of Henle.

The diuretic effect after / in administration shows quickly, peaking in the first action 1-3 h and maintained for nearly 12 no. In healthy probands in a dosage range 5-100 mg dose was observed proportional to the logarithm of the increase in urine output.

Urine output increased, even in cases, when other diuretics (such as thiazides) no longer have the desired effect (such as renal failure). Because of these properties Torasemide eliminates puffiness.

The antihypertensive effect of torasemide associated with decreased systemic vascular resistance due to the normalization of electrolyte balance and the decrease in the activity of free Ca 2+ cells in the muscle layer of arteries.

Pharmacokinetics

Binding torasemide plasma proteins exceeds 99%. The half-life of torasemide and its metabolites in healthy people is 3-4 no. Total clearance of torasemide - 40 ml / min, Renal clearance - about 10 ml / min. The main metabolite M5 diuretic action is not, while the share of M1 and M3 metabolites account for about 10% pharmacodynamic action.

In renal insufficiency, total clearance and half-life of torasemide unchanged, and half-life of the M3 and M5 increases. Nonetheless, pharmacodynamic characteristics of the drug remains unchanged. In patients with impaired liver function or heart failure half-life of torasemide and metabolite M3 increased slightly. Torasemide and its metabolites in the body does not cumulate.

Indications

Essential hypertension .

Treatment and prevention of recurrence of swelling and / or effusion due to heart failure.

Dosing and Administration

Treatment of essential hypertension

The recommended initial dose of torasemide - 2,5 mg / day (1/2 Cor or tablet Trifas 1/4 Tablets Trifas 10).

Hypotensive effect begins gradually already in the 1st week of treatment and reaches its maximum no later than 12 weeks of continuous reception. If during this period, normalization of blood pressure is not reached - torasemide daily dose can be increased to 5 mg.

When initially severe hypertension (diastolic blood pressure - above 115 mm Hg. Art.), and limited kidney function can count on an additional antihypertensive effect. You should not exceed the daily dose 5 mg, as it hardly will lead to a further decrease in blood pressure.

Treatment of swelling and / or effusion

Treatment starts with 5 torasemide mg per day. Depending on severity of the disease the dose can be increased to 20 mg / day.

Contraindications

Hypersensitivity to torasemide or related in structure means (sulfonylurea compounds) history.

Gipotenziya.

Renal failure with anuria.

Serious liver with impaired consciousness (pechenochnaya coma or coma).

Gipovolemiя.

Giponatriemiya.

Kaliopenia.

Pronounced urinary disorders (eg due to prostatic hypertrophy).

In the absence of clinical experience should not be given torasemide in the following conditions or diseases:

Podagre.

Expressed disturbances of intracardiac conduction (синоатриальная или атриовентрикулярная блокада II или III степени).

Pathological changes in acid-base balance.

In the simultaneous therapy with lithium, aminoglycosides or cephalosporins.

Blood dyscrasia (thrombocytopenia or anemia patients without renal failure).

Impaired renal function, caused by nephrotoxic agents.

Children under 12 years.

Pregnancy and breast-feeding

Torasemide can be used during pregnancy only if absolutely necessary, the potential benefit outweighs the potential risk to the mother and / or fetus, as the experience of the drug in pregnant women is not enough.

Unknown, Have there torasemide in breast milk, therefore, breast-feeding is best not to prescribe medication.

Side effects

Depending on the applied doses and duration of treatment possible violations of water and electrolyte balance, eg hypovolemia, kaliopenia, giponatriemiya; in rare cases - increased metabolic alkalosis. Sometimes, especially at the beginning of treatment, having a headache, dizziness , fatigue, muscle spasms.

Cardio-vascular system and blood (hematopoiesis, hemostasis)

At considerable loss of fluid and electrolytes, due to the strong urination, possible hypotension, confusion, in rare cases - thrombosis, cardiac and cerebral ischemia, including the development of cardiac arrhythmias , syncope , angina, Acute myocardial infarction. Occasionally noted decline in the number of platelets , erythrocytes and / or leukocytes .

On the part of the digestive tract

Early treatment may be constipated, anorexia, nausea, vomiting , stomach ache, diarrhea. Can increase the activity of certain liver enzymes ( c-глутамил-транспептидазы ).

With the genitourinary system

Patients with disorders of urination, such as prostatic hypertrophy, intense urination can cause urinary retention and bladder hyperextension. Occasionally there was an increase in serum creatinine and blood urea.

Local reactions

Allergic reactions, such as itching, eczema, photosensitivity, identify rare. In some cases, after the / in the introduction may develop anaphylactic shock, requiring emergency. The possibility of severe skin reactions.

Metabolism

Sometimes elevated levels of uric acid in blood glucose, and lipids ( triglycerides , cholesterol ) serum.

Other

Sometimes there is a dry mouth and unpleasant sensations in the extremities ( paraesthesia ), in some cases - visual disturbances, in single - tinnitus and hearing loss.

Drug Interactions

Torasemide enhances the effect of other antihypertensive agents, in particular ACE inhibitors. At their simultaneous application may excessive reduction of blood pressure.

In an application with drugs digitalis torasemide potassium deficiency, caused by diuretic, can extend the range of side effects of both drugs. Torasemide reduces efficiency antidiabetics.

Probenecid and NSAIDs reduce the diuretic and hypotensive effect of torasemide. In the treatment of high-dose salicylates torasemide may enhance their toxic effect on the CNS. Torasemide, especially in high doses, can enhance GRT- and nephrotoxicity of aminoglycoside antibiotics and platinum derivatives.

Torasemide enhances the action of theophylline and muscle relaxants curariform. Diuretic, and mineralogy- glucocorticoids and may enhance the loss of potassium, due torasemide. With simultaneous use of torasemide and drugs lithium may increase the concentration of lithium in the blood with the strengthening of its side effects. Torasemide weakens the vasoconstrictor effects of catecholamines. In an application with cholestyramine may decrease absorption of torasemide and thus its effectiveness.

Overdose

Symptoms: possible strong diuresis with excessive loss of water and electrolytes, drowsiness, confusion, gipotenziya, collapse and gastrointestinal rastrojstva.

Treatment: spetsificheskiy no known antidote. When administered hypokalemia 7,4% rr potassium chloride (when alkalosis) or 10,01% rr potassium bicarbonate (with acidosis). In both cases, as a supplement to an infusion p-py. In the case of hyponatremia in infusion rr added 5,8% rr nariya chloride or with concomitant acidosis, 8,4% rr sodium bicarbonate .

Precautions

Long-term treatment with torasemide requires regular monitoring of the electrolyte balance, in particular serum potassium . Also requires regular monitoring of glucose levels in the blood, Uric acid,creatinine and blood lipids.

Effects on ability to drive vehicles and management mechanisms

Even with the proper application of torasemide can change a person's response, impairing its ability to participate in road traffic, servicing machinery or perform hazardous work without a safety net. This particularly applies to the initial period of treatment and simultaneous reception of alcohol.