Active substanceFurosemideFurosemide
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  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the solution contains active substance furosemide - 10 mg;

    auxiliary substances: sodium hydroxide - 20 μl, sodium sulfite - 1 mg, water for injection up to 1 ml.

    Description:

    Transparent colorless or slightly yellowish 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 ("rebound" or "cancel" 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 with 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; with feces - 12%. Clearance - 1,5-3 ml / min / kg.

    Indications:

    Edema syndrome of various genesis (with chronic heart failure, cirrhosis of the liver (syndrome of portal hypertension), edematous syndrome of renal genesis (in the nephrotic syndrome in the foreground is the treatment of the underlying disease), acute heart failure, especially with swelling of the lungs (used in combination with other therapeutic measures), cerebral edema, severe forms of arterial hypertension, hypertensive crisis, conducting forced diuresis with poisoning by chemical compounds that are excreted points in unchanged form.

    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:

    systemic lupus erythematosus, prostatic hyperplasia, hypoproteinemia (risk of ototoxicity development), diabetes mellitus (decrease in glucose tolerance), stenosing cerebral arteries atherosclerosis, pregnancy (especially the first half, possible use for life indications), lactation period.

    Dosing and Administration:

    Furosemide-Vial is administered intravenously (slowly struyno), if not possible - intramuscularly (efficacy is much lower) for 7-10 days or more. Parenteral administration is advisable to perform in urgent situations, or with a pronounced edematous syndrome. The question of the duration of treatment is decided by the doctor, given the nature and severity of the disease.

    It is recommended to use the maximum effective minimum dose of the drug.

    The drug is administered in doses of 20-40 mg 1-2 times a day; in the absence of a diuretic response every 2 hours, injected in an increased 50% dose until an adequate diuresis is achieved.

    The average daily dose for intravenous administration in children is 1 mg / kg body weight.

    Patients with reduced glomerular filtration and low diuretic response are prescribed in large doses - 1-1.5 g.

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

    Side effects:

    From the cardiovascular system: decrease in arterial pressure (BP), collapse, tachycardia, arrhythmia, a decrease in the volume of circulating blood, thrombophlebitis, orthostatic hypotension.

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

    From the sense organs: impaired vision and hearing.

    From the digestive tract: 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, renal 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 or hemolytic anemia.

    From the side of water-electrolyte exchange: hypovolemia, dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloraemia, hypocalcemia, hypomagnesemia, metabolic alkalosis.

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

    In premature infants, the formation of calcium-containing kidney stones (nephrolithiasis) and the deposition of calcium salts in the kidney parenchyma (nephrocalcinosis) is possible.

    Preterm infants during the first weeks of life furosemide may increase the risk of Botallov duct preservation.

    Possible local pain reaction in the place of intramuscular injection.

    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 the volume of circulating blood, 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 developing hypokalemia, with cardiac glycosides - the risk of digitalis intoxication due to hypokalemia (for high and low-polar) and the elongation of the half-life (for low-polarity) increase.

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

    Non-steroidal 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).

    The administration of angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists to patients previously treated with furosemide may lead to impaired renal function,and in some cases to the development of acute renal failure.

    Recommended the withdrawal of furosemide, or reduce the dose of furosemide 3 days before the start therapy with ACE inhibitors or angiotensin II receptor antagonists.

    The simultaneous use of probenicide or methotrexate may decrease the effectiveness of furosemide (the same pathway of secretion). On the other hand furosemide can lead to a decrease in renal elimination of these drugs.

    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:

    On the background of treatment, it is necessary to periodically monitor blood pressure, the content of electrolytes of blood plasma, 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 parenteral injected fluids), control of excreted urine.

    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.

    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 inappropriate to limit the intake of table salt.

    For the prevention of hypokalemia, the simultaneous administration of potassium and potassium-sparing diuretics (especially spironolactone) is recommended, and also to adhere to a diet rich in potassium (lean meat, potatoes, bananas, tomatoes, cauliflower, spinach, dried fruits, etc.).

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

    The choice of dosage regimen for patients with ascites against the background of cirrhosis of the liver should be carried out under stationary conditions (violations of the water-electrolyte state may lead to the development of 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.

    A drug furosemide should not be mixed in the same syringe with other medicines.

    Form release / dosage:

    Solution for intravenous and intramuscular injection 10 mg / ml. .

    Packaging:

    2 ml into the ampoules of a neutral light-protective glass.

    10 ampoules per contour cell package. One contour pack together with instructions for use in a cardboard pack

    Storage conditions:

    List B. In the dark place at a temperature of no higher than 25 ° C and inaccessible to children.

    Shelf life:

    3 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000777/08
    Date of registration:15.02.2008
    The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspVIAL, LLCVIAL, LLC
    Information update date: & nbsp16.11.2015
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