Description
Pharmacological action
Loop diuretic. It disrupts the reabsorption of sodium ions, chlorine in the thick segment of the ascending part of the Henle loop. Due to the increase in the release of sodium ions, secondary (indirectly osmotically bound by water) enhanced excretion of water and increased secretion of potassium ions in the distal part of the renal tubule occur. At the same time, the excretion of calcium and magnesium ions increases.
Possesses secondary effects due to the release of intrarenal mediators and redistribution of intrarenal blood flow. Against the background of course 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 the excretion of sodium chloride and a decrease in the response of vascular smooth muscle to vasoconstrictive effects and as a result of a decrease in bcc. The action of furosemide after iv administration occurs 5-10 minutes after ingestion – after 30-60 minutes, the maximum effect – after 1-2 hours, the duration of the effect is 2-3 hours (with reduced renal function – up to 8 hours). During the period of action, the excretion of sodium ions increases significantly, but after its termination, the excretion rate decreases below the initial level (rebound syndrome, or withdrawal). The phenomenon is due to the sharp activation of the renin-angiotensin and other antinatriuretic neurohumoral regulatory units 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. With iv administration, it causes dilatation of peripheral veins, reduces preload, reduces the filling pressure of the left ventricle and the pressure in the pulmonary artery, as well as systemic blood pressure.
The diuretic effect develops 3-4 minutes after iv administration and lasts 1-2 hours after oral administration – after 20-30 minutes, lasts up to 4 hours.
Pharmacokinetics
After oral administration, 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 with albumin) – 95-99%. Metabolized in the liver. It is excreted by the kidneys – 88%, with bile – 12%. T1 / 2 in patients with normal renal and hepatic function is 0.5-1.5 hours. With anuria, T1 / 2 may increase to 1.5-2.5 hours, with combined renal and hepatic insufficiency – up to 11-20 hours
Indications
Edematous syndrome of various origins, including with chronic heart failure stage II-III, cirrhosis (portal hypertension syndrome), nephrotic syndrome. Pulmonary edema, cardiac asthma, cerebral edema, eclampsia, forced diuresis, severe hypertension, some forms of hypertensive crisis, hypercalcemia.
Contraindications
Acute glomerulonephritis, urethral stenosis, obstruction of the urinary tract with stones, acute renal failure with anuria, hypokalemia, alkalosis, precomatous conditions, severe hepatic failure, hepatic coma, coma, and coma decompensated mitral or aortic stenosis, hypertrophic obstructive cardiomyopathy, increased central venous pressure (more than 10 mm p t.t.), arterial hypotension, acute myocardial infarction, pancreatitis, impaired water-electrolyte metabolism (hypovolemia, hyponatremia, hypokalemia, hypochloremia, hypocalcemia, hypomagnesemia), digitalis intoxication, hypersensitivity to furosemide.
Use during pregnancy and lactation
During pregnancy, the use of furosemide is possible only for a short time and only if the intended benefit of the therapy to the mother outweighs the potential risk to the fetus.
Since furosemide can be excreted in breast milk and also inhibit lactation, if necessary, use during lactation should stop breast-feeding.
Special instructions
Use with caution in case of prostatic hyperplasia, SLE, hypoproteinemia (risk of ototoxicity), diabetes mellitus (decreased glucose tolerance), with stenosing atherosclerosis of cerebral arteries, during prolonged treatment with cardiac patients with advanced glycoside atherosclerosis, pregnancy (especially the first half), lactation.
Before starting treatment, electrolyte abnormalities should be compensated. During treatment with furosemide, it is necessary to control blood pressure, serum electrolytes and glucose, and 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, dose adjustment of the latter may be required.
It is not recommended to mix furosemide solution in one syringe with any other drugs.
Influence on the ability to drive vehicles and control mechanisms
When using furosemide, it is impossible to exclude the possibility of a decrease in the ability to concentrate, which is important for people driving vehicles and working with mechanisms.
Composition
Injection 1%
1 ml 1 amp.
furosemide 10 mg 20 mg
Dosage and administration
Set individually, depending on the indications, clinical situation, age of the patient. During treatment, the dosage regimen is adjusted depending on the magnitude of the diuretic response and the dynamics of the patient’s condition.
When administered, 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 on / in (jet) or intramuscular administration, 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 of
From the cardiovascular system: decreased blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decreased bcc.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, myasthenia gravis, muscle cramps (tetany), paresthesia, apathy, adynamia, weakness, lethargy, drowsiness, confusion.
On the part of the sensory organs: impaired vision and hearing.
From the digestive system: decreased appetite, dry mouth, thirst, nausea, vomiting, constipation or diarrhea, cholestatic jaundice, pancreatitis (exacerbation).
From the genitourinary system: oliguria, acute urinary retention (in patients with prostatic hypertrophy), interstitial nephritis, hematuria, decreased potency.
From the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia.
On the part of water-electrolyte metabolism: hypovolemia, dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloremia, hypocalcemia, hypomagnesemia, metabolic alkalosis.
From the side of metabolism: hypovolemia, hypokalemia, hyponatremia, hypochloremia, hypokalemic metabolic alkalosis (as a result of these disorders – arterial hypotension, dizziness, dry mouth, thirst, arrhythmia, muscle weakness, cramps), hyperuricemia (with possible hyperglycemia.
Allergic reactions: purpura, urticaria, exfoliative dermatitis, erythema multiforme exudative, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitivity, anaphylactic shock.
Other: with iv administration (optional) – thrombophlebitis, calcification of the kidneys in premature infants.
Drug Interactions
With simultaneous use with antibiotics of the aminoglycoside group (including with gentamicin, tobramycin), an increase in nephro- and ototoxic effects is possible.
Furosemide reduces the clearance of gentamicin and increases plasma concentrations of gentamicin, as well as tobramycin.
When used with antibiotics, the cephalosporins group, which can cause impaired renal function, there is a risk of increased nephrotoxicity.
With simultaneous use with beta-adrenergic agonists (including phenoterol, terbutaline, salbutamol) and with corticosteroids, hypokalemia may be increased.
With simultaneous use with hypoglycemic agents, insulin, a decrease in the effectiveness of hypoglycemic agents and insulin is possible, as furosemide has the ability to increase plasma glucose.
With simultaneous use with ACE inhibitors, the antihypertensive effect is enhanced. Pronounced arterial hypotension is possible, 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 is increased and the development of hypokalemia is not ruled out.
When used simultaneously with furosemide, the effects of non-depolarizing muscle relaxants are enhanced.
With simultaneous use with indomethacin and other NSAIDs, a decrease in the diuretic effect is possible, 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 COX inhibitor, a decrease in antihypertensive effect.
It is believed that furosemide likewise interacts with other NSAIDs.
When used simultaneously with NSAIDs, which are selective COX-2 inhibitors, this interaction is much less pronounced or practically absent.
When used simultaneously with astemizole, the risk of developing arrhythmias is increased.
With simultaneous use with vancomycin, an increase in oto- and nephrotoxicity is possible.
With simultaneous use with digoxin, digitoxin, an increase in toxicity of cardiac glycosides is possible, associated with the risk of hypokalemia while taking furosemide.
There are reports of the development of hyponatremia with concomitant use with carbamazepine.
With simultaneous use with colestyramine, colestipol, the absorption and diuretic effect of furosemide are reduced.
When used simultaneously with lithium carbonate, intensification of the effects of lithium is possible due to an increase in its concentration in blood plasma.
With simultaneous use with probenecid, renal clearance of furosemide decreases.
With simultaneous use with sotalol, hypokalemia and the development of ventricular arrhythmias such as pirouette are possible.
With simultaneous use with theophylline, a change in theophylline concentration in blood plasma is possible.
With simultaneous use with phenytoin, the diuretic effect of furosemide is significantly reduced.
After iv administration of furosemide during therapy with chloral hydrate, increased sweating, a feeling of heat, blood pressure instability, and tachycardia are possible.
With simultaneous use with cisapride, increased hypokalemia is possible.
It has been suggested that furosemide may reduce the nephrotoxicity of cyclosporin.
With simultaneous use with cisplatin, an increase in the ototoxic effect is possible.
Active ingredient
Furosemide
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