Furosemide

General characteristics. Structure:

International and chemical names: furosemide;
4-hlor-N-(2 furylmethyl) - 5-sulfamoylanthranilic acid; main physical and chemical properties: tablets of a round form, color, white with a yellowish shade, with a biconvex surface; structure: 1 tablet contains furosemide 40 mg; excipients: the starch corn modified cellulose microcrystallic, magnesium stearate, povidone, a macrogoal 6000, lactoses monohydrate.

Pharmacological properties:

Pharmacodynamics. Strong diuretic with quickly developing effect, derivative sulfonamides. The mechanism of effect of Furosemide is connected with blockade of a reabsorption of ions of sodium and chlorine in the ascending department of a Henle's loop; influences also gyrose tubules, and this effect is not connected with oppression of a karboangidraza or aldosteronovy activity. Drug renders the expressed diuretic, natriuretic, hloruretichesky effect. Increases also removal of potassium, calcium, magnesium. Drug reduces the filling pressure of a left ventricle, pulmonary pressure, improves cardiac performance at heart failure; reduces system arterial pressure.
Drug is equally effective at acidosis and an alkalosis. The diuretic effect at intake is observed in 20 - 30 minutes, a maximum of effect of drug – in     1 – 2 hour. Effect duration after a single dose – 4 h and more.

Pharmacokinetics. After intake Furosemide is soaked up from a digestive tract, bioavailability makes 64%. The maximum concentration of drug increases in a blood plasma with increase in a dose, but time of its achievement does not depend on a dose and varies over a wide range depending on a condition of the patient.
Linkng with proteins (generally with albumine) makes 95%. Furosemide gets through a placental barrier, is emitted with breast milk. It is metabolized in a liver, turning generally into a glucuronide. Furosemide and its metabolites are quickly removed   by kidneys. An elimination half-life – 1–1,5 h. With urine it is removed within 24 hours about 50% of the accepted dose, at the same time during the first 4 h – 59% of all drug which is removed per day. Other quantity is removed with a stake in not changed look.

Indications to use:

Edematous syndrome of various genesis, including at chronic heart failure ІІ B - ІІІ stages, cirrhosis (a syndrome of portal hypertensia), a nephrotic syndrome; arterial hypertension; hypertensive crisis; syndrome of premenstrual  tension;  artificial diuresis, hyperpotassemia, hypernatremia, hypercalcemia.

Route of administration and doses:

Furosemide is appointed inside to food. Doses select depending on disease severity and expressiveness of effect. Orally accept 40 mg (1 tablet) once a day in the morning. At insufficient action the dose is increased to 80 - 160 mg a day (2-3 receptions with intervals of 6 h). After reduction of hypostases appoint in smaller doses with a break 1-2 days. The maximum daily dose makes 160 mg.
At arterial hypertension the initial dose of drug for adults makes 80 mg a day, divided into 2 receptions. It has to correspond to a condition of the patient. At insufficient effect it is necessary to appoint together with other antihypertensives.
At the accompanying heart failure it is possible to increase a daily dose to 80 mg.
For children at the age of 3 years the average daily dose accepted inside in time or after food is also more senior, makes 4 – 3 mg/kg for 1 – 4 reception. Furosemide has the greatest diuretic effect in the first 3 – 5 days of reception. After disappearance of hypostases pass to discontinuous purpose of Furosemide – every other day or 1 – 2 time a week.
If the child did not receive Furosemide or other diuretics earlier, it is not necessary to appoint diuretic in an average daily dose at once. In the beginning it is necessary to apply diuretic in a dose, a component ¼ - ½ from an average daily dose, and then if the diuretic effect is absent, the dose should be increased. For children the initial dose makes 2 mg/kg, if necessary can be raised on 1-2 mg/kg.

Features of use:

With care appoint drug at heavy cardiovascular insufficiency, at long therapies cardiac glycosides, to patients of advanced age with the expressed atherosclerosis. Prior to treatment it is necessary to compensate serious electrolytic frustration.
At treatment it is necessary to control the level of electrolytes, carbonates, urea.
Treatment has to be carried out against the background of a diet rich with potassium.
During pregnancy in its first half drug is contraindicated, in the second half Furosemide can be applied only according to strict indications and short time which is determined by the doctor.
In need of reception of Furosemide in the period of a lactation feeding by a breast should be stopped as drug can get into breast milk (and also to oppress a lactation).
At use of drug it is impossible to exclude decrease in attention that is important for the drivers and people working with mechanisms.
At preservation of an oliguria for 24 hours furosemide should be cancelled.
For avoidance of a syndrome of "ricochet" at AG furosemide is appointed by not less than 2 times a day.

Side effects:

Nausea, vomiting, hypovolemia, dehydration, hyperemia, skin itch, hypotension, disturbances of a cordial rhythm, reversible hearing disorder, sight, paresthesias, intersticial nephrite are possible. Because of strengthening of a diuresis there can be dizziness, a depression; muscular weakness, thirst, dehydration, hypopotassemia, hyponatremia, hypochloraemia, metabolic alkalosis; a tranzitorny hyperuricemia, an uricosuria, an exacerbation of gout, in some cases a hyperglycemia, an aggravation of symptoms at an obstructive uropathy. As soon as there are side effects, a dose of Furosemide it is necessary to reduce or cancel drug.

Interaction with other medicines:

At simultaneous use of Furosemide with cardiac glycosides the risk of development of glikozidny intoxication increases, at a combination to glucocorticoid means – risk of development of a hypopotassemia.
Furosemide exponentiates action of muscle relaxants, anti-hypertensive drugs. At simultaneous use with aminoglycosides, cephalosporins and Cisplatinum increase in their concentration in a blood plasma is possible that can lead to development nefro-and ototoksichesky effects.
Non-steroidal anti-inflammatory drugs can reduce diuretic effect of Furosemide.
At simultaneous use with Furosemide effect of gipoglikemiziruyushchy drugs can be weakened. Simultaneous use of Furosemide with drugs of lithium can lead to the strengthened lithium reabsorption in renal tubules and to emergence of toxic effect.
Probenetsid increases concentration in blood.

Contraindications:

Acute glomerulonephritis, end-stage of a renal failure, mechanical impassability of urinary tract; liver failure, diabetic coma; disturbances of a water salt metabolism (hypopotassemia, hyponatremia, dehydration, alkalosis); the first half of pregnancy, hypersensitivity to drug (including to streptocides), an anury, gout, a dekompensirovanny arterial or mitral stenosis, the expressed hypotension, pancreatitis, a myocardial infarction, a diabetes mellitus with disturbance of tolerance to carbohydrates, a hypertrophic cardiomyopathy with obstruction of an outgoing path of a left ventricle, a lupus erythematosus. Children's age up to 3 years.

Overdose:

Symptoms: dehydration, decrease in volume of the circulating blood, the arterial hypotension, an electrolytic imbalance, a hypopotassemia and a gipokhloremichesky alkalosis caused by diuretic effect.
Treatment: symptomatic.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on 5 planimetric packagings in a pack.