Furosemide

General characteristics. Structure:

Active ingredient: 0,01g furosemide in 1 ml of 1% solution.

Vvspomogatelny substances: solution natrayedky 1M, sodium chloride, water for injections.

High-speed diuretic with the expressed diuretic effect.

Pharmacological properties:

Pharmacodynamics. Breaks a reabsorption of ions of sodium, chlorine in a thick segment of the ascending Henle's loop. Furosemide renders the expressed diuretic, natriuretic, hloruretichesky effect. Besides, increases removal of potassium ions, calcium, magnesium.

At heart failure quickly leads to decrease in preload of heart by means of expansion of large veins. Has hypotensive effect owing to increase in removal of sodium of chloride and decrease in reaction of smooth muscles of vessels to vasopressor influences, and as a result of reduction of volume of the circulating blood.

At intravenous administration effect of furosemide develops in 15-20 minutes and reaches a maximum by the end of the first hour; the diuretic effect proceeds within 3 hours, at reduced function of kidneys – to 8 h. During action removal of ions of sodium considerably increases, however after its termination the speed of removal decreases below the initial level (a syndrome of "ricochet" or "cancellation"). The phenomenon is caused by sharp activation reninangiotenzinovy and other anti-natriuretic neurohumoral links of regulation in response to a massive diuresis

Pharmacokinetics. Time of achievement of the maximum concentration at intravenous administration - 30 minutes. The relative volume of distribution - 0,2 l/kg. The patient with reduced glomerular filtering and the low diuretic answer appoint in high doses - 1-1,5 g. After approach of necessary effect pass to administration of drug inside

Indications to use:

- an edematous syndrome of various genesis (at chronic heart failure, cirrhosis (a syndrome of portal hypertensia));

- an edematous syndrome of renal genesis (at a nephrotic syndrome in the forefront there is a treatment of a basic disease);

- an acute heart failure, especially at a fluid lungs (it is applied in combination with other medical actions);

- wet brain;

- hypostases at burns;

- severe forms of arterial hypertension;

- hypertensive crisis;

- for maintenance of an artificial diuresis at poisonings.

Route of administration and doses:

Furosemide is appointed intravenously (slowly struyno), at impossibility - intramusculary (efficiency is much lower) within 7-10 days and more.

It is reasonable to carry out parenteral administration in urgentny situations, or at sharply expressed edematous syndrome. The drug is administered in doses 20-60 mg by 1-2 times a day; in the absence of the diuretic answer each 2 h enter in the dose increased by 50% before achievement of an adequate diuresis.

Average daily dose for intravenous administration at children - 0,5-1,5 mg/kg, maximum – 20 mg.

Features of use:

Against the background of course treatment it is necessary to control periodically the arterial pressure, content of electrolytes of plasma (including Na, Sa, To, Mg), an acid-base condition, residual nitrogen, creatinine, uric acid, function of a liver and to carry out, if necessary, the corresponding correction of treatment (with bigger frequency rate at patients with frequent vomitings and against the background of parenterally entered liquids). Patients with hypersensitivity to streptocides and derivatives of sulphonylurea can have cross sensitivity to furosemide.

To the patient receiving high doses of furosemide in order to avoid development of a hyponatremia and a metabolic alkalosis it is inexpedient to limit consumption of table salt.

For prevention of a hypopotassemia co-administration of drugs of potassium and kaliysberegayushchy diuretiyok is recommended (first of all Spironolactonum), and also to adhere to the diet rich with potassium.

The increased risk of development of disturbances of water and electrolytic balance is noted at patients with a renal failure.

Selection of the mode of dosing by the patient with ascites against the background of cirrhosis needs to be carried out in stationary conditions (a narusheyoniya of water and electrolytic balance can entail development of a hepatic coma). Regular control of the content of electrolytes of a blood plasma is shown to this category of patients.

At emergence or strengthening of an azotemia and oliguria in patients with the serious progressing illness of kidneys rekomenyodutsya to suspend treatment.

It is allocated with milk at women in the period of a lactation in this connection the feeding termination is reasonable.

Periodic control of glucose level in blood and urine is required from patients with a diabetes mellitus or with reduced tolerance to glucose.

At patients in unconsciousness, with prostate adenoma, narrowing of ureters or a hydronephrosis, control of a mocheotdeleniye, in connection with a possibility of an acute ischuria is necessary. Furosemide for 98% contacts proteins of a blood plasma, generally albumine. Gets through a placental barrier, it is allocated with breast milk.

It is metabolized in a liver with formation of 4-chlorine-5-sulfamoylanthranilic acid. Cosecretes in a gleam of renal tubules through the system of transport of anions existing in proximal department of nephron. The elimination half-life (Т½) of furosemide after intravenous administration makes from 0,5 to 1 hours.

It is removed preferential (88%) by kidneys in not changed look and in the form of metabolites; with a stake - 12%. Clearance of-1,5-3 ml/min.

Side effects:

From cardiovascular system: a lowering of arterial pressure, a collapse, tachycardia, arrhythmia, decrease in an objeyom of the circulating blood, thrombophlebitis.

From a nervous system: dizziness, headache, muscular weakness, spasms of gastrocnemius muscles (tetany), paresthesias, apathy, adynamia, weakness, slackness, drowsiness, confusion of consciousness.

From sense bodys: vision disorder and hearing

From digestive tract, liver: anorexia, dryness in a mouth, thirst, nausea, vomiting, diarrhea, a lock, cholestatic jaundice, pancreatitis (aggravation).

From urinogenital system: an oliguria, an acute ischuria (at patients with prostate adenoma), intersticial nephrite, a hamaturia, impotence, calcification of kidneys at premature children

Allergic reactions: purpura, urticaria, exfoliative dermatitis, multiformny erythema, vasculitis, necrotizing angiitis, skin itch, fever, fever, photosensitization, acute anaphylaxis.

From bodies of a hemopoiesis: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia.

From water and electrolytic exchange: hypovolemia, dehydration (risk of development of thrombosis and thromboembolism), hypopotassemia, hyponatremia, hypochloraemia, hypocalcemia, hypomagnesiemia, metabolic alkalosis.

Laboratory indicators: hyperglycemia, hypercholesterolemia, hyperuricemia, glucosuria, hypercalcuria.

Contraindications:

Hypersensitivity to furosemide, an acute glomerulonephritis, an acute renal failure with an anury (the size of glomerular filtering less 3-5ml/mines), a heavy liver failure, a hepatic coma and a prekoma, an urethra stenosis, obstruction of urinary tract a stone, prekomatozny states, a hyper glycemic coma, a hyperuricemia, gout, a dekompensirovanny mitral or aortal stenosis, increase in the central venous pressure (over 10 mm hg), an idiopathic hypertrophic subaortal stenosis, arterial hypotension, an acute myocardial infarction, a system lupus erythematosus, pancreatitis, disturbance of water and electrolytic exchange and acid-base equilibrium (a hypopotassemia, an alkalosis, a hypovolemia, a hyponatremia, a hypochloraemia, a hypocalcemia, a hypomagnesiemia), digitalis intoxication.

With care - a prostate hyperplasia, a hypoproteinemia (risk of development of ototoxicity), the diabetes mellitus (decrease in tolerance to glucose) stenosing atherosclerosis of cerebral arteries, pregnancy (especially the first half, use according to vital indications is possible), the lactation period.

Overdose:

Symptoms: decrease in the ABP, a collapse, shock, a hypovolemia, dehydration, haemo concentration, arrhythmias (including AV blockade, a fibrilyolyation of ventricles), an acute renal failure with an anury, thrombosis, a thrombembolia, drowsiness, confusion of consciousness, sluggish paralysis, apathy.

Treatment: correction of water-salt balance and an acid-base state, completion of volume of the circulating blood, a symptomatic treatment is not present the Specific antidote.

Storage conditions:

Period of validity 2 years. Not to use after the date specified on packaging. In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 10 mg/ml.

On 2 ml in ampoules of neutral glass. On 10 ampoules place in a pack from a cardboard for a retail container with partitions or lattices, or a separator from a cardboard or paper bag.

On 10 ampoules place in a box from a cardboard. Put the application instruction, a knife in each pack or a box ampoule or the scarificator ampoule.

5 ampoules in a blister strip packaging. 2 blister strip packagings together with the application instruction, a knife ampoule or the scarificator ampoule ceramic in a pack from a cardboard.

When using ampoules with notches, rings or points the knife ampoule or the scarificator ampoule is not put.