Furosemide

General characteristics. Structure:

Active ingredient: 40 mg of furosemide in 1 tablet.

Furosemide has a diuretic, natriuretic effect.

Pharmacological properties:

Pharmacodynamics. Works throughout a thick segment of the ascending knee of a Henle's loop and blocks a reabsorption of 15 — 20% of the filtered sodium ions. Increases removal of bicarbonates, phosphates, calcium, magnesium and potassium, raises рН urine. The diuretic effect is characterized by considerable expressiveness, short duration and depends on a dose, it comes in 15 — 30 min., reaches a maximum later 1 — 2 h and lasts 6 — 8 h.

Arginine — vazopressinovy and sympathetic systems stimulates, reduces the level of an atrial natriuretic factor in plasma, causes vasoconstriction. It is effective at heart failure (both acute, and chronic), improves a functional class of heart failure since reduces the filling pressure of a left ventricle. Reduces peripheral hypostases, developments of stagnation in lungs, the vascular pulmonary resistance, pressure of jamming of pulmonary capillaries in a pulmonary artery and the right auricle.

Keeps efficiency at a low glomerular filtration rate therefore it is used for treatment of arterial hypertension at patients with a renal failure.

Pharmacokinetics. At intake it is soaked up quickly and rather fully, bioavailability makes 60 — 70%. Linkng with proteins of plasma (it is preferential with albumine) — 91 — 97%. The elimination half-life of drug is equal to 0,5 — 1 h. In a liver is exposed to biotransformation with formation of inactive metabolites. It is excreted preferential by kidneys.

Indications to use:

Chronic heart failure, fluid lungs, hypertensive crisis, edematous and ascitic syndrome at cirrhosis, a renal failure, a nephrotic syndrome, the expressed hypernatremia, a hypercalcemia and a gipermagniyemiya.

Route of administration and doses:

Drug is accepted inside to food. The dose is selected individually. As a rule, appoint the adult in a daily dose 20 — 40 mg (0,5 — 1 tablets) once a day (morning). If necessary increase in a dose up to 80 — 160 mg a day is possible. The dose is increased by 20 — 40 mg every 6 — 8 hours. At purpose of drug in high doses the daily dose is divided into 2 — 3 receptions, accepted bucketed not less than 6 hours. At reduction of hypostases the dose is gradually reduced with an interval of 1 — 2 day. As a rule, a maintenance dose — 40 mg of furosemide every other day.

To children appoint at the rate of 1 — 2 mg/kg a day.

The maximum daily dose for adults — 600 mg, for children — 6 mg/kg.

Features of use:

In the presence of ascites without peripheral hypostases it is recommended to apply in the doses providing an additional diuresis of no more than 700 — 900 ml a day in order to avoid development of an oliguria, an azotemia and disturbances of electrolytic exchange. At treatment of arterial hypertension appoint not less than 2 times a day. The driving of motor transport and other types of activity requiring special attention and speed of response is not recommended. It is inexpedient to combine furosemide with cephalosporins, gentamycin, etc. the drugs having nephrotoxic effect. Treatment has to be carried out against the background of the diet rich with potassium.

Pregnancy and lactation: at pregnancy use of furosemide is possible only for a short time and only in that case when the estimated advantage for mother exceeds possible risk for a fruit. As furosemide can be emitted with breast milk, and also suppress a lactation, in need of use in the period of a lactation breastfeeding needs to be stopped.

Precautionary measures. Long reception can lead to emergence of weakness, fatigue, a lowering of arterial pressure and cordial emission, and the excessive diuresis at a myocardial infarction with developments of stagnation in a small circle of blood circulation can promote development of cardiogenic shock. Temporary cancellation (for several days) before purpose of APF inhibitors is necessary. Within the first months of treatment control of arterial pressure, level of electrolytes (especially potassium) is recommended, to CO2, creatinine, an urea nitrogen, uric acid, periodic definition of activity of liver enzymes, level of calcium and magnesium, content of glucose in blood and in urine (at a diabetes mellitus). At preservation of an oliguria during 24 h drug should be cancelled.

Side effects:

Hypotonia, including postural, a collapse, a thrombembolia, thrombophlebitis (it is preferential at elderly), a hypopotassemia, a hypomagnesiemia, a hyponatremia, disturbance of tolerance to glucose, a hyperuricemia, gout, increase in level of LPNP cholesterol (at reception of high doses of drug), disturbance of an acid-base state (a gipokhloremichesky alkalosis), a hypercalcuria, abnormal liver functions, an intra hepatic cholestasia, pancreatitis, diarrhea, a lock, nausea, vomiting, anorexia, damage of an inner ear, a hearing loss, sight misting, confusion of consciousness, nervousness, a headache, dizzinesses, paresthesias, weakness, a spasm of muscles, a bladder spasm, a fever, fever, thrombocytopenia, aplastic anemia, a leukopenia, a system vasculitis, intersticial nephrite, a hamaturia, a necrotizing angiitis, exfoliative dermatitis, a multiformny erythema, impotence, a photosensitization, a small tortoiseshell, a skin itch.

At emergence of side reactions a dose it is necessary to reduce or cancel drug.

Interaction with other medicines:

Aminoglycosides, Acidum etacrynicum and Cisplatinum increase ototoxicity of drug (especially at an impaired renal function).

Furosemide increases danger of damage of kidneys against the background of Amphotericinum of Century.

At co-administration of high doses of salicylates the risk of development of a salitsilizm, cardiac glycosides — a hypopotassemia and the related arrhythmia, corticosteroids — an electrolytic imbalance increases.

Reduces myorelaxation activity of tubocurarine, exponentiates effect of a suktsinilkholin.

Increases probability of intoxication lithium drugs.

Against the background of reception of furosemide the effect of APF inhibitors and anti-hypertensive means, warfarin, diazoxide, theophylline increases, it is weakened — antidiabetic drugs, noradrenaline.

Sukralfat and indometacin reduce efficiency of furosemide. Probenetsid increases concentration of furosemide in serum.

Contraindications:

Hypersensitivity (including to sulfonamides), prekomatozny states, a hepatic coma, heavy disturbances of electrolytic balance, a hypopotassemia, the expressed insufficiency of function of a liver and kidneys, an oliguria during more than 24 h, an anury, gout, a hyperuricemia, a diabetes mellitus or disturbance of tolerance to carbohydrates, a dekompensirovanny mitral or aortal stenosis, increase in pressure in a jugular vein over 10 mm Hg, a hypertrophic cardiomyopathy with obstruction of an output path of a left ventricle, hypotonia, a myocardial infarction, a system lupus erythematosus, pancreatitis, a metabolic alkalosis, mechanical impassability of urinary tract, the first half of pregnancy.

Overdose:

Symptoms: hypotonia, decrease in volume of the circulating plasma, a hypopotassemia and a gipokhloremichesky alkalosis.

Treatment: there is no specific antidote. Symptomatic therapy, maintenance of the vital functions.

Issue conditions:

According to the recipe

Packaging:

Tablets of 40 mg in packaging No. 50 (No. 10х5 in blister strip packagings or in banks).