Furosemide solution 10mg/ml 2ml ampoules, 10pcs

Composition

Solution for injection 1%

1 ml 1 amp.

furosemide 10 mg 20 mg

Pharmacological action

“Loop” diuretic. Disrupts the reabsorption of sodium and chlorine ions in the thick segment of the ascending part of the Henle loop. Due to an increase in the release of sodium ions, secondary (mediated by osmotically bound water) increased water excretion and an increase in the 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.

It has secondary effects due to the release of intrarenal mediators and redistribution of intrarenal blood flow. During the course of treatment, the effect does not weaken.

In heart failure, it quickly reduces the preload on the heart by dilating large veins. It has a hypotensive effect due to an increase in the excretion of sodium chloride and a decrease in the reaction of vascular smooth muscles to vasoconstrictor effects and as a result of a decrease in BCC. The effect of furosemide after intravenous use occurs in 5-10 minutes; after oral use-in 30-60 minutes, the maximum effect – in 1-2 hours, the duration of the effect-2-3 hours (with reduced renal function-up to 8 hours). During the period of action, the elimination of sodium ions increases significantly, but after its termination, the rate of elimination decreases below the initial level (“rebound” or “withdrawal” syndrome). The phenomenon is caused by a sharp activation of renin-angiotensin and other antinatriuretic neurohumoral regulatory units in response to massive diuresis; it 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, it may not significantly affect the daily excretion of sodium ions and blood pressure. When administered intravenously, it causes dilation of peripheral veins, reduces preload, reduces left ventricular filling pressure and pulmonary artery pressure, as well as systemic blood pressure.

Diuretic effect develops in 3-4 minutes after intravenous use and lasts 1-2 hours; after oral use – in 20-30 minutes, lasts up to 4 hours

. Pharmacokinetics

After oral use, 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 albumins) is 95-99%. It is metabolized in the liver. It is excreted by the kidneys-88%, with bile-12%. T1 / 2 in patients with normal kidney and liver function is 0.5-1.5 hours. With anuria, T1 / 2 can 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 stage II-III chronic heart failure, cirrhosis of the liver (portal hypertension syndrome), and nephrotic syndrome. Pulmonary edema, cardiac asthma, cerebral edema, eclampsia, forced diuresis, severe arterial hypertension, some forms of hypertensive crisis, hypercalcemia.

Contraindications

Acute glomerulonephritis, urethral stenosis, urinary tract obstruction with stone, acute renal failure with anuria, hypokalemia, alkalosis, precomatous conditions, severe liver failure, hepatic coma and precoma, diabetic coma, precomatous conditions, hyperglycemic coma, hyperuricemia, gout, decompensated mitral or aortic stenosis, hypertrophic hypertrophy obstructive cardiomyopathy, increased central venous pressure (more than 10 mm Hg), hypotension, acute myocardial infarction, pancreatitis, impaired water and electrolyte metabolism (hypovolemia, hyponatremia, hypokalemia, hypochloremia, hypocalcemia, hypomagnesemia), digitalis intoxication, hypersensitivity to furosemide.

Side effects

From the cardiovascular system:  reduced blood pressure, orthostatic hypotension, collapse, tachycardia, arrhythmias, decreased BCC.

From the central nervous system and peripheral nervous system:  dizziness, headache, myasthenia gravis, calf muscle spasms (tetany), paresthesia, apathy, adynamia, weakness, lethargy, drowsiness, confusion.

From the side of the senses:  visual and hearing impairments.

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 hematopoietic 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.

From the side of metabolism:  hypovolemia, hypokalemia, hyponatremia, hypochloremia, hypokalemic metabolic alkalosis (as a result of these disorders – hypotension, dizziness, dry mouth, thirst, arrhythmia, muscle weakness, convulsions), hyperuricemia (with possible exacerbation of gout), hyperglycemia.

Allergic reactions:  purpura, urticaria, exfoliative dermatitis, erythema multiforme, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitization, anaphylactic shock.

Other services:  with intravenous use (additionally) – thrombophlebitis, renal calcification in premature infants.

Interaction

Concomitant use with antibiotics of the aminoglycoside group (including gentamicin, tobramycin) may increase the nephrotoxic and ototoxic effects.

Furosemide reduces the clearance of gentamicin and increases the plasma concentrations of gentamicin and tobramycin.

Concomitant use with antibiotics of the cephalosporin group, which can cause impaired renal function, may increase the risk of nephrotoxicity.

When used concomitantly with beta-adrenomimetics (including fenoterol, terbutaline, salbutamol) and corticosteroids, hypokalemia may increase.

When used concomitantly with hypoglycemic agents, insulin, it is possible to reduce the effectiveness of hypoglycemic agents and insulin, since furosemide has the ability to increase the content of glucose in blood plasma.

When used concomitantly with ACE inhibitors, the antihypertensive effect is enhanced. Severe 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 increases and hypokalemia is not excluded.

When used concomitantly with furosemide, the effects of non-depolarizing muscle relaxants are enhanced.

When used concomitantly with Indometacin and other NSAIDs, the diuretic effect may decrease, apparently due to inhibition of prostaglandin synthesis in the kidneys and sodium retention in the body under the influence of Indometacin, which is a non-specific COX inhibitor; a decrease in antihypertensive effect.

Furosemide is believed to interact similarly with other NSAIDs.

When used concomitantly with NSAIDs that are selective COX-2 inhibitors, this interaction is expressed to a much lesser extent or practically absent.

When used concomitantly with astemizole, the risk of arrhythmia increases.

Concomitant use with vancomycin may increase oto-and nephrotoxicity.

When used concomitantly with digoxin, digitoxin may increase the toxicity of cardiac glycosides associated with the risk of hypokalemia while taking furosemide.

Hyponatremia has been reported with concomitant use with carbamazepine.

When used concomitantly with colestyramine, colestipol, the absorption and diuretic effect of furosemide decreases.

When used concomitantly with lithium carbonate, it is possible to increase the effects of lithium due to an increase in its concentration in blood plasma.

When used concomitantly with probenecid, the renal clearance of furosemide decreases.

When used concomitantly with sotalol, hypokalemia and the development of ventricular arrhythmia of the “pirouette” type are possible.

When used concomitantly with theophylline, it is possible to change the concentration of theophylline in blood plasma.

When used concomitantly with phenytoin, the diuretic effect of furosemide is significantly reduced.

After intravenous use of furosemide on the background of chloral hydrate therapy, increased sweating, a feeling of heat, unstable blood pressure, and tachycardia may occur.

When used concomitantly with cisapride, hypokalemia may increase.

It is suggested that furosemide may reduce the nephrotoxic effect of cyclosporine.

When used concomitantly with cisplatin, it is possible to increase the ototoxic effect.

How to take it, course of use and dosage

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 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 oral dose for children is 6 mg / kg.

With intravenous (jet) or intramuscular use, 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.

Special instructions

should be used with caution in patients with prostatic hyperplasia, SLE, hypoproteinemia (risk of ototoxicity), diabetes mellitus (reduced glucose tolerance), stenosing atherosclerosis of the cerebral arteries, against the background of prolonged therapy with cardiac glycosides, in elderly patients with severe atherosclerosis, pregnancy (especially the first half), lactation.

Electrolyte disturbances should be compensated before starting treatment. During treatment with furosemide, it is necessary to monitor blood pressure, the level of electrolytes and glucose in the blood serum, liver and kidney function.

To prevent hypokalemia, it is advisable to combine furosemide with potassium-sparing diuretics. When furosemide and hypoglycemic drugs are used simultaneously, a dose adjustment of the latter may be required.

It is not recommended to mix furosemide solution in the same syringe with any other medications.

Influence on the ability to drive motor vehicles and manage 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.

Storage conditions

In a dark place, at a temperature not exceeding 20 °C

Shelf life

2 years

Active ingredient

Furosemide

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection