Furosemide

Brand Dalkhimpharm

In stock 1325 Items

Available since: 2019-09-19

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Clinical Pharmacology

"Loop" diuretic. Violates the reabsorption of sodium ions, chlorine in a thick segment of the ascending part of the loop of Henle. Due to the increased 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 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, 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 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 for 1-2 h; 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

Edematous syndrome of various genesis, incl. in chronic heart failure stage II-III, liver cirrhosis (portal hypertension syndrome), nephrotic syndrome. Pulmonary edema, cardiac asthma, cerebral edema, eclampsia, forced diuresis, severe hypertension, some forms of hypertensive crisis, hypercalcemia.

Composition

Solution for injection 1%

1 ml of 1 amp.

Furosemide 10 mg 20 mg

Furosemide is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Furosemide	Dalkhimpharm	Russia	ampoules
Furosemide-SOLOpharm			solution
Furosemide	Dalkhimpharm	Russia	pills
Lasix	Sanofi-aventis	France	pills
Lasix	Sanofi-aventis	France	ampoules
Furosemide	BPMP	Belarus	pills

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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 IM 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.

Adverse reactions

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, calf muscles (tetany), paresthesia, apathy, weakness, weakness, lethargy, drowsiness, confusion.

From the sense organs: 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 exudative, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitization, anaphylactic shock.

Other: with a / in the introduction (optional) - thrombophlebitis, calcification of the kidneys in premature babies.

Contraindications

Acute glomerulonephritis, stenosis of the urethra, obstruction of the urinary tract with a stone, an acute problem with anurimia, hypokalemia, alkalosis, prekomatoznye states, severe hepatic insufficiency, hepatic coma and precoma, diabetic coma, precomatozia, hyperglycemic category 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.

Drug interactions

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-adrenergicami (including fenoterol, terbutalina, 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.

With simultaneous use with ACE inhibitors, the antihypertensive effect is enhanced. Severe 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 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, 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 COX inhibitor; decrease in antihypertensive effect.

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 of 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 of the "pirouette" type.

With simultaneous use with theophylline, the concentration of theophylline in the blood plasma may change.

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 can reduce the nephrotoxic effect of cyclosporine.

With simultaneous use with cisplatin may increase ototoksicheskogo action.

Pregnancy and Lactation

In pregnancy, the use of furosemide is possible only for a short time and only if 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, breastfeeding should be discontinued if necessary during lactation.

Special instructions

C is used with caution in prostatic hyperplasia, SLE, hypoproteinemia (risk of ototoxicity), diabetes mellitus (reduced glucose tolerance), with stenotic atherosclerosis of the cerebral arteries, against the background of prolonged therapy with cardiac glycosides, in elderly patients with marked 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.

Influence on ability to drive motor transport and control mechanisms

When using furosemide, it is impossible to exclude the likelihood of reduced ability to concentrate, which is important for those driving vehicles and working with mechanisms.