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Active ingredients
Furosemide
Release form
Pills
Composition
1 tablet contains: Active substance: furosemide 40 mg. Adjuvants: lactose - 53 mg, starch - 56.88 mg, pregelatinized starch - 7 mg, talc - 2.4 mg, colloidal silicon dioxide - 0.4 mg, magnesium stearate - 0.32 mg.
Pharmacological effect
Loop diuretic. Violates the reabsorption of sodium ions, chlorine in a thick segment of the ascending part of the loop of Henle. Due to an increase in the excretion of sodium ions, a secondary (mediated osmotically bound water) enhanced water excretion and an increase in the secretion of potassium ions in the distal part of the renal tubule occurs. At the same time, the excretion of calcium and magnesium ions increases. It has secondary effects due to the release of intrarenal mediators and the redistribution of intrarenal blood flow. Against the background of a course of treatment, the effect does not weaken. When heart failure quickly leads to a decrease in the preload on the heart through the expansion of large veins. It has a hypotensive effect due to increased excretion of sodium chloride and a decrease in the reaction of vascular smooth muscle on vasoconstrictor effects and as a result of a decrease in the BCC. The action of furosemide after the on / in the introduction occurs in 5-10 minutes; after ingestion - after 30-60 minutes, the maximum action - after 1-2 hours, the duration of the effect - 2-3 hours (with reduced kidney function - up to 8 hours). During the period of action, the excretion of sodium ions increases significantly, but after its termination, the rate of excretion decreases below the initial level (rebound syndrome, or cancellation). The phenomenon is caused by a sharp activation of the renin-angiotensin and other antinatriuretic neurohumoral regulation links in response to massive diuresis; stimulates the arginine-vasopressive and sympathetic systems. Reduces the level of atrial natriuretic factor in plasma, causes vasoconstriction. Due to the rebound phenomenon when taken 1 time / day, it may not have a significant effect on the daily excretion of sodium ions and blood pressure. When i / v administration causes dilatation of peripheral veins, reduces preload, reduces the filling pressure of the left ventricle and pressure in the pulmonary artery, as well as systemic BP. The diuretic effect develops 3-4 min after i / v injection and lasts 1-2 hours; after ingestion - after 20-30 minutes, lasts up to 4 hours.
Pharmacokinetics
After ingestion, the absorption is 60-70%.In severe kidney disease or chronic heart failure, the degree of absorption decreases. Vd is 0.1 l / kg. Binding to plasma proteins (mainly albumin) - 95-99%. Metabolized in the liver. Excreted by the kidneys - 88%, with bile - 12%. T1 / 2 in patients with normal renal function and liver is 0.5-1.5 hours. With anuria, T1 / 2 can increase up to 1.5-2.5 hours, with combined renal and hepatic insufficiency, up to 11-20 hours.
Indications
Edema syndrome in chronic congestive heart failure (if diuretic treatment is required) - edema syndrome in acute congestive heart failure - edema syndrome in chronic renal failure - maintaining fluid secretion in acute renal failure, including during pregnancy and childbirth - edema caused by nephrotic syndrome (if treatment with edematics is required) - edema syndrome in case of liver diseases (if additional treatment is necessary with aldosterone antagonists) - arterial hypothyroidism Etension - hypertensive crisis (as maintenance therapy) - maintenance of forced diuresis
Contraindications
Hypersensitivity to furosemide or to any of the components of the drug; for hypersensitivity to sulphonamide
Precautionary measures
C is used with caution in prostatic hyperplasia, SLE, hypoproteinemia (risk of developing ototoxicity), diabetes mellitus (decreased glucose tolerance), with stenotic atherosclerosis of the cerebral arteries, against the background of prolonged therapy with cardiac glycosides, in patients with atherosclerosis with a history of atherosclerosis, a heart disease, in patients with atherosclerosis, a heart disease, in patients with atherosclerosis, with an atherosclerosis. first half), lactation period.
Use during pregnancy and lactation
During pregnancy, the use of furosemide is possible only for a short time and only when the intended benefit of therapy for the mother outweighs the potential risk to the fetus. Because furosemide can be excreted in breast milk and can also suppress lactation, if necessary, breast feeding should be stop it.
Dosage and administration
Set individually, depending on the evidence, the clinical situation, the patient's age. In the course of treatment, the dosage regimen is adjusted depending on the size of the diuretic response and the dynamics of the patient's condition. When taken orally, the initial dose for adults is 20-80 mg / day, then, if necessary, the dose is gradually increased to 600 mg / day. For children, a single dose is 1-2 mg / kg. The maximum dosage for oral administration for children is 6 mg / kg. For intravenous (jet) or intramuscular injection, the dose for adults is 20-40 mg 1 time / day, in some cases - 2 times / day. For children, the initial daily dose for parenteral use is 1 mg / kg.
Side effects
From the side of the cardiovascular system: decrease in blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decrease in BCC. On the part of the central nervous system and peripheral nervous system: dizziness, headache, myasthenia weakness, lethargy, drowsiness, confusion. From the sense organs: visual and hearing impairment. From the alimentary system: loss of appetite, dry mouth, thirst, nausea, vomiting, constipation or diarrhea, cholestatic jaundice, pancreatitis (exacerbation). On the part of the urogenital system: oliguria, acute urinary retention (in patients with prostatic hypertrophy), interstitial nephritis, hematuria, decreased potency. From the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia. dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloremia, hypocalcemia, hypomagnemia, metabolic alkalosis. On the metabolic side: hypovolemia, hypokalemia, hyponatremia, hypochloremia, hypokalemic metabolic alkalosis (as a result of these disorders - arterial hypotension, dizziness, dry mouth, thirst, arrhythmia, muscle weakness, convulsions), hyperuricemia (with possible exacerbation of gout), hyperglycemia. Allergic reactions: purpura, purpura, martial erythema multiforme exudative, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitization, anaphylactic shock. Other: with a / in the introduction (optional) - thrombophlebitis, renal calcification in Ocean children.
Overdose
In the case of an overdose of Lasix, arterial hypotension, imbalance of electrolytes, dizziness, dry mouth, and visual disturbances are most often observed. The treatment is aimed at restoring the water-electrolyte balance and normalizing the BCC.
Interaction with other drugs
With simultaneous use of aminoglycoside groups with antibiotics (including with gentamicin, tobramycin), the nephrototoxic effect can be enhanced. Furosemide reduces the clearance of gentamicin and increases plasma concentrations of gentamicin and tobramycin. When used simultaneously with cephalosporins antibiotics, which can cause renal dysfunction, there is a risk of increased nephrotoxicity. When used simultaneously with beta-adrenergic mimics (including fenoterol, terbutaline, salbutamol) and with GCS may increase hypokalemia. With simultaneous use with hypoglycemic agents, insulin may decrease the effectiveness of hypoglycemic agents and insulin, because Furosemide has the ability to increase the glucose content in the blood plasma. When used simultaneously with ACE inhibitors, the antihypertensive effect is enhanced. Possible pronounced arterial hypotension, especially after taking the first dose of furosemide, apparently due to hypovolemia, which leads to a transient increase in the hypotensive effect of ACE inhibitors. The risk of impaired renal function increases and the development of hypokalemia is not excluded. When used simultaneously with furosemide, the effects of non-depolarizing muscle relaxants are enhanced. When used simultaneously with indomethacin and other NSAIDs, the diuretic effect may decrease, apparently due to inhibition of prostaglandin synthesis in the kidneys and sodium retention in the body the effects of indomethacin, which is a non-specific inhibitor of COX; reduction of antihypertensive effect. It is believed that furosemide interacts with other NSAIDs in a similar way. When used simultaneously with NSAIDs, which are selective COX-2 inhibitors, this interaction is much less pronounced or practically absent. If used simultaneously with astemizole, the risk of arrhythmia increases .In simultaneous use with vancomycin, it is possible to increase oto-and nephrotoxicity. If used simultaneously with digoxin, digitoxin may increase toxicity. spine of cardiac glycosides,associated with the risk of hypokalemia in patients receiving furosemide. There are reports of the development of hyponatremia with simultaneous use with carbamazepine. When used simultaneously with Kolestiramine, colestipol decreases the absorption and diuretic effect of furosemide. blood plasma. At simultaneous use with probenecid the renal clearance of furosemide decreases. At simultaneous use with sotalol Hypokalemia and the development of ventricular arrhythmias such as pirouette are possible. With simultaneous use with theophylline, the concentration of theophylline in the blood plasma can be changed. With simultaneous use with phenytoin, the diuretic effect of furosemide is significantly reduced. instability of blood pressure, tachycardia. With simultaneous use with cisapride may increase hypokalemia. It is assumed that furosemide may reduce nephro classically action tsiklosporina.Pri simultaneous use of cisplatin may increase Valium actions.
special instructions
Electrolyte disturbances should be compensated before treatment begins. During treatment with furosemide, it is necessary to control blood pressure, serum electrolytes and glucose levels, liver and kidney function. To prevent hypokalemia, it is advisable to combine furosemide with potassium-sparing diuretics. With the simultaneous use of furosemide and hypoglycemic drugs may require dose adjustment of the latter. It is not recommended to mix the solution of furosemide in the same syringe with any other drugs. Effect on the ability to drive motor vehicles and control mechanisms driving vehicles and working with mechanisms.