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Description
Furosemide pills - a drug diuretic (diuretic) action.
Active ingredients
Furosemide
Release form
Pills
Composition
Furosemide.
Pharmacological effect
"Loopback" 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 increases the excretion of calcium and magnesium ions. 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. In heart failure, it quickly leads to a decrease in preload on the heart through the expansion of large veins. It has a hypotensive effect due to an increase in sodium chloride excretion 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 intravenous injection occurs after 5-10 minutes, after ingestion - after 30-60 minutes, the maximum action - after 1-2 hours, the duration of effect - 2-3 hours (with reduced kidney function - up to 8 hours) . During the period of action, the excretion of sodium ions increases significantly, however, after its termination, the rate of excretion decreases below the initial level ("rebound" or "cancellation" syndrome). 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 phenomenon of "rebound" when taken 1 time / day may not have a significant impact on the daily excretion of sodium ions and blood pressure. When a / in the introduction 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 blood pressure. The diuretic action develops 3-4 min after i / v administration and lasts 1-2 h, after ingestion - after 20-30 min, lasts up to 4 h.
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
Edematous syndrome of various genesis, incl. with chronic heart failure II-III stage, cirrhosis of the liver (portal hypertension syndrome), nephrotic syndrome. Pulmonary edema, cardiac asthma, brain edema, eclampsia, forced diuresis, severe hypertension, some forms of hypertensive crisis, hypercalcemia.
Contraindications
Acute glomerulonephritis, stenosis of the urethra, obstruction of the urinary tract with a stone, an acute problem with anuria, hypopaniemia, alkalosis, precomatosis, severe hepatic insufficiency, hepatic coma and precoma, diabetic coma, precomatozia, hyperglycemic template, hyperglycemic template. aortic stenosis, hypertrophic obstructive cardiomyopathy, increased central venous pressure (more than 10 mm Hg), arterial hypotension, os ing myocardial infarction, pancreatitis, disruption of water-electrolyte metabolism (hypovolemia, hyponatremia, hypokalemia, hypochloremia, hypocalcemia, hypomagnesemia), digitalis intoxication, hypersensitivity to furosemide.
Precautionary measures
With caution used in elderly patients with severe atherosclerosis. Contraindicated in severe hepatic insufficiency, hepatic coma and precoma. Contraindicated in acute glomerulonephritis, acute renal failure with anuria.
Use during pregnancy and lactation
In pregnancy, the use of furosemide is possible only for a short time and only in the case when the intended benefit of therapy for the mother outweighs the potential risk to the fetus. Since furosemide can be excreted in breast milk, as well as suppress lactation, if necessary, use during lactation breastfeeding should be stopped.
Dosage and administration
Set individually, depending on the evidence, the clinical situation, the patient's age.During treatment, the dosage regimen is adjusted depending on the size of the diuretic response and the dynamics of the patient's condition. When ingestion, 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 oral dose for children is 6 mg / kg. With the / in (jet) or in / m injection 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 cardiovascular system: decrease in blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decrease in BCC. From the side of the central nervous system and peripheral nervous system: dizziness, headache, myasthenia, convulsions of the gastrocnemius muscles (tetany), paresthesia, apathy, weakness, weakness, lethargy, drowsiness, confusion. From the senses: visual and hearing impairment. On the part of the digestive 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. On the part of the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia. From the side of water-electrolyte metabolism: hypovolemia, dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloremia, hypocalcemia, hypomagnesemia, metabolic alkalosis. On the part of metabolism: hypovolemia, hypokalemia, hyponatremia, hypochloremia, hypokalemic metabolic alkalosis (as a consequence of these disorders - hypotension, dizziness, dry mouth, thirst, arrhythmias, muscle weakness, seizures), hyperuricemia (with the possible exacerbation of gout), hyperglycemia . Allergic reactions: purpura, urticaria, exfoliative dermatitis, erythema multiforme, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitization, anaphylactic shock. Other: with the on / in the introduction (optional) - thrombophlebitis, calcification of the kidneys in premature babies.
Interaction with other drugs
With simultaneous use of aminoglycoside groups with antibiotics (including with gentamicin, tobramycin), the nephrototoxic effect can be enhanced. Furosemide reduces clearance of gentamicin and increases plasma concentrations of gentamicin, as well as tobramycin. When used simultaneously with antibiotics of the cephalosporins group, which can cause renal dysfunction, there is a risk of increased nephrotoxicity. With simultaneous use with beta-adrenergic drugs (including fenoterol, terbutaline, salbutamol) and with GCS, hypokalemia may increase. With simultaneous use with hypoglycemic agents, insulin may decrease the effectiveness of hypoglycemic agents and insulin, because Furosemide has the ability to increase the content of glucose in the blood plasma. With simultaneous use with ACE inhibitors increases antihypertensive effect. 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 renal dysfunction increases and the development of hypokalemia is not excluded. When applied simultaneously with furosemide, the effects of non-depolarizing muscle relaxants are enhanced. With simultaneous use with indomethacin and other NSAIDs, it is possible to reduce the diuretic effect, apparently due to inhibition of prostaglandin synthesis in the kidneys and sodium retention in the body under the influence of indomethacin, which is a nonspecific inhibitor of COX, a decrease in antihypertensive action. It is believed that in this way, furosemide interacts with other NSAIDs. With simultaneous use with NSAIDs, which are selective inhibitors of COX-2, this interaction is expressed to a much lesser extent or virtually absent. With simultaneous use with astemizole increases the risk of arrhythmia. With simultaneous use with vancomycin may increase oto-and nephrotoxicity. With simultaneous use with digoxin, digitoxin, it is possible to increase the toxicity of cardiac glycosides, associated with the risk of developing hypokalemia in patients receiving furosemide.There are reports of the development of hyponatremia with simultaneous use with carbamazepine. With simultaneous use with colestiramine, colestipol decreases the absorption and diuretic effect of furosemide. With simultaneous use of lithium carbonate may increase the effects of lithium due to the increase in its concentration in the blood plasma. With simultaneous use of probenecid, renal clearance of furosemide is reduced. With simultaneous use with sotalol possible hypokalemia and the development of ventricular arrhythmias such as "pirouette". With simultaneous use with theophylline may change the concentration of theophylline in the blood plasma. With simultaneous use with phenytoin, the diuretic effect of furosemide is significantly reduced. After the on / in the introduction of furosemide during therapy with chloral hydrate may increase sweating, a feeling of heat, blood pressure instability, tachycardia. With simultaneous use with cisapride may increase hypokalemia. It is assumed that furosemide may reduce the nephrotoxic effect of cyclosporine. With simultaneous use with cisplatin may increase the ototoxic effect.
special instructions
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. 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. For the prevention of hypokalemia, it is advisable to combine furosemide with potassium-saving diuretics. With 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 one syringe with any other drugs. Impact on the ability to drive motor vehicles and control mechanisms: the use of furosemide can not exclude the likelihood of reduced ability to concentrate, which is important for those driving vehicles and working with mechanisms.