Furosemide - instructions for use, dose, side effects, contraindications

1 ml of the solution contains active substance furosemide - 10 mg; auxiliary substances: sodium hydroxide solution 1 M, sodium chloride, water for injection.

Description:

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:diuretic

ATX: & nbsp

C.03.C.A.01 Furosemide

Pharmacodynamics:

high-speed diuretic with pronounced diuretic effect. Disrupts the reabsorption of sodium, chlorine ions in the thick segment of the ascending loop of Henle. Furosemide has a pronounced diuretic, natriuretic, chlororetic effect. In addition, it increases the excretion of potassium, calcium, and magnesium ions.

With heart failure quickly leads to a decrease in preload on the heart through the expansion of large veins. Has hypotensive effect due to an increase in the excretion of sodium chloride and a decrease in the response of the smooth muscles of the vessels to vasoconstrictor effects, and as a result of a decrease in the volume of circulating blood.

With intravenous administration of furosemide develops in 15-20 minutes and reaches a maximum at the end of the first hour; diuretic effect lasts for 3 hours, with reduced renal function - up to 8 hours.

During the period of action, excretion of sodium ions increases significantly, but after its termination, the rate of excretion decreases below the initial level ("ricochet" or "cancellation" syndrome). The phenomenon is caused by a sharp activation of the renin-angiotensin and other antinatriuretic neurohumoral regulating units in response to massive diuresis.

Pharmacokinetics:

the time to reach the maximum concentration for intravenous administration is 30 minutes. The relative volume of the distribution is 0.2 l / kg. Furosemide on 98% is associated with blood plasma proteins, mainly with albumins. Penetrates through the placental barrier, excreted in breast milk.

Metabolized in the liver to form 4-chloro-5-sulfamoyl-anthranilic acid. It is secreted into the lumen of the renal tubules through the anion transport system existing in the proximal nephron. The half-life of furosemide after intravenous administration is 0.5 to 1 hour.Bioavailability is 60-70%. It is excreted mainly (88%) by the kidneys in unchanged form and in the form of metabolites; through the intestine - 12%. Clearance - 1,5-3 ml / min / kg. With renal failure, the excretion of furosemide slows down, and the half-life increases; with severe renal failure, the final half-life can be increased to 24 hours.

With hemodialysis and peritoneal dialysis furosemide output is insignificant.

In liver failure, the half-life of furosemide is increased by 30-90%, mainly due to an increase in the volume of distribution. Pharmacokinetic parameters in this category of patients can vary greatly.

In chronic heart failure, severe degree of arterial hypertension and in elderly patients, excretion of furosemide slows down due to decreased kidney function.

After intravenous administration of furosemide to newborns of low mass, the diuretic effect begins to develop after 15-20 minutes, reaches a maximum after 1-2 hours, and the return of urine volume to the initial one is observed after 6-16 hours.

The repeated administration of full-dose furosemide to infants is not recommended until at least 24 hours,and in preterm infants, it is better to increase the interval to 48 hours.

Indications:Ocular syndrome of various genesis (with chronic heart failure, cirrhosis of the liver (syndrome of portal hypertension), edematous syndrome of kidney genesis (with nephrotic syndrome in the foreground is the treatment of the underlying disease), acute heart failure, especially with swelling of the lungs (used in conjunction with other therapeutic measures), cerebral edema, severe forms of arterial hypertension, hypertensive crisis, conducting forced diuresis in case of poisoning with chemical compounds that are excreted kidneys unchanged.

Contraindications:

Hypersensitivity to furosemide, acute glomerulonephritis, acute renal failure with anuria (glomerular filtration value less than 3-5 ml / min), severe hepatic insufficiency, hepatic coma and precoma, stenosis of the urethra, obstruction of the urinary tract by stone, precomatitis, hyperglycemic coma, hyperuricemia, gout, decompensated mitral or aortic stenosis, increased central venous pressure (> 10 mm Hg.), idiopathic hypertrophic subaortal stenosis, arterial hypotension, acute myocardial infarction, pancreatitis, disturbance of water electrolyte metabolism and acid-base balance (hypokalemia, alkalosis, hypovolemia, hyponatremia, hypochloraemia, hypocalcemia, hypomagnesemia), digitalis intoxication.

Carefully:

In conditions in which excessive reduction in blood pressure is particularly dangerous (stenosing lesions of coronary and / or cerebral arteries); with acute myocardial infarction (increased risk of cardiogenic shock);

with a violation of the outflow of urine (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis); with hypoproteinemia (risk of development of ototoxicity); at a diabetes (depression of tolerance to a glucose); with systemic lupus erythematosus.

The simultaneous use of respiridone with furosemide in elderly patients with cerebrovascular dementia was associated with high mortality.

When furosemide is used in preterm infants, nephrocalcinosis / nephrolithiasis and thrombophlebitis may develop.In this regard, it is necessary to monitor the function of the kidneys and perform ultrasonography of the kidneys.

Pregnancy and lactation:

Furosemide penetrates the placental barrier, so the drug should not be administered during pregnancy. If for vital reasons furosemide is prescribed to pregnant women, careful monitoring of the fetus is necessary.

If it is necessary to use the drug during lactation at the time of treatment, breastfeeding should be stopped, since furosemide It is secreted with breast milk, and can also suppress lactation.

Dosing and Administration:

Furosemide is administered intravenously (honeystreaming), if not possible - insidemuscular (effectiveness is much lower) for 7-10 days or more. The dose is selected individually. It is recommended that the smallest doses of the drug, sufficient for achieve the necessary therapeutic effect.

Intravenous administration of furosemide prois found when taking the drug inside It is impossible or there is a violation of absorptionin the small intestine or in ursituations, or at the expressed edematous syndrome.

The drug is administered in doses of 20-60 mg 1-2 times per day; in the absence of diuretic responsethat every 2 hours is injected in an enlarged 50% dose to achieve an adequate diuresis. The average daily dose for intravenous administration in children is 1 mg / kg body weight, but not more than 20 mg / day.

The maximum daily dose of furosemide in adults is 1500 mg / day, the rate of administration should not exceed 4 mg / min, and in patients with severe renal failure - not more than 2.5 mg / min.

After the onset of the desired effect, they switch to taking the drug inside.

Side effects:

From the cardiovascular system: lowering blood pressure (BP), collapse, tachycardia, arrhythmia, a decrease in the volume of circulating blood,

thrombophlebitis, orthostatic hypotension.

From the nervous system: dizziness, headache, muscle weakness, calf muscle cramps (tetany), paresthesia, apathy, adynamia, weakness, lethargy, drowsiness, confusion.

From the sense organs: visual and hearing impairments.

On the part of the gastrointestinal tract, liver: anorexia, dry mouth, thirst, nausea, vomiting, diarrhea or constipation, cholestatic jaundice, pancreatitis (exacerbation)

From the genitourinary system: oliguria, acute urinary retention (in patients with prostate adenoma), interstitial nephritis, hematuria, impotence, kidney calcification in premature infants.

Allergic reactions: purpura, urticaria, exfoliative dermatitis, erythema multiforme, vasculitis, necrotizing angiitis, itching, chills, fever, photosensitivity, anaphylactic shock.

From the hematopoiesis: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia.

On the part of water-electrolyte metabolism: hypovolemia, dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloraemia, hypocalcemia, hypomagnesemia, metabolic alkalosis.

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

Overdose:

Symptoms: decreased blood pressure, collapse, shock, hypovolemia, dehydration, hemoconcentration, arrhythmias (including atrioventricular block, ventricular fibrillation), acute renal failure with anuria, thrombosis, thromboembolism, drowsiness, confusion, flaccid paralysis, apathy.

Treatment: correction of water-salt balance and acid-base state, replenishment of circulating blood volume, symptomatic treatment. There is no specific antidote.

Interaction:

Increases the concentration and risk of nephro- and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid, cisplatinum, amphotericin B (due to competitive renal excretion).

Increases the effectiveness of diazoxide and theophylline, reduces - hypoglycemic drugs, allopurinol.

Pressor amines and furosemide mutually reduce efficiency.

Drugs that block the tubular secretion, increase the concentration of furosemide in the blood serum.

With the simultaneous use of glucocorticosteroids, amphotericin B increases the risk of hypokalemia, with cardiac glycosides - the risk of developing digitalis intoxication due to hypokalemia (for high and low-polar) and elongation of the half-life (for low-polarity) increases.

Reduces renal clearance of lithium preparations and increases the likelihood of development of intoxication.

Heteroidal anti-inflammatory drugs, sucralfate reduce the diuretic effect due to inhibition of prostaglandin synthesis, renin level in the blood plasma and aldosterone removal.

Strengthens the hypotensive effect of antihypertensive drugs, neuromuscular blockade of depolarizing muscle relaxants (suxamethonium) and weakens the effect of nondepolarizing muscle relaxants (tubocurarine).

Simultaneous reception of large doses of salicylates against furosemide therapy increases the risk of their toxicity (due to competitive renal excretion).

Intravenously administered furosemide has a slightly alkaline reaction, so it can not be mixed with drugs with a pH of less than 5.5.

Special instructions:

Against the background of course treatment, it is necessary to periodically monitor blood pressure, blood plasma electrolytes, acid-base state, residual nitrogen, creatinine, uric acid, liver function and, if necessary, appropriate correction of treatment (with higher multiplicity in patients with frequent vomiting and background of parenterally injected fluids).

Patients with hypersensitivity to sulfonamides and sulfonylureas may have cross-sensitivity to furosemide.

Patients receiving high doses of furosemide, in order to avoid the development of hyponatremia and metabolic alkalosis, it is not advisable to limit the intake of table salt.

For the prevention of hypokalemia, the simultaneous administration of potassium and potassium-sparing diuretics (primarily spironolactone) is recommended, as well as adherence to a diet rich in potassium.

Increased risk of development of violations of water-electrolyte balance is observed in patients with renal insufficiency.

Selection of the dosing regimen for patients with ascites against the background of cirrhosis of the liver should be done in a stationary setting (violations of the water-electrolyte balance may lead to the development of the hepatic coma).

This category of patients shows regular monitoring of the content of plasma electrolytes.

When azotemia and oliguria appear or increase in patients with severe progressive kidney disease, it is recommended to suspend treatment.

Isolated with milk in women during lactation, in connection with which, it is advisable to stop feeding.

In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of the level of glucose in the blood and urine is required.

In patients with unconsciousness, with prostatic adenoma, narrowing of the ureters or hydronephrosis, control of urinary excretion is necessary, in connection with the possibility of acute urinary retention.

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from driving vehicles and practicing other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 10 mg / ml.

Packaging:

2 ml per ampoule of neutral glass.

For 10 ampoules together with instructions for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard.

5 ampoules per circuit cell packaging

from a film of polyvinylchloride and a foil of aluminum printed varnished or without a foil.

2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.

When using ampoules with notches, rings and break points, the ampoule opener opener or ampoule scarifier is allowed not to be inserted.

Storage conditions:

In the dark place at a pacefrom 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001295 / 02

Date of registration:24.04.2008

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Representation: & nbspDALHIMFARM, OJSCDALHIMFARM, OJSC

Information update date: & nbsp16.11.2015

Illustrated instructions

Instructions

Furosemide (Furosemide)