Lasix solution for injections 20mg/2ml 2ml #10

Lasix solution for injections instruction for use

You can buy Lasix solution for injections on this page

Composition

In 1 ml of solution contains:
active substance - furosemide - 10.00 mg.
excipients: sodium chloride, sodium hydroxide, water for injection.
Description: a clear, colorless solution.
Pharmacotherapeutic group:
diuretic agent.
KODATH-S03SA01

Pharmacological properties

Pharmacodynamics

Lasix injections are a fast-acting diuretic derived from sulfonamide. Lasix injections blocks the system of transport of Na +, K +, Cl- ions in the thick segment of the ascending knee of the loop of Henle, and therefore, its saluretic action depends on Lasix for injections entering the lumen of the renal tubules (due to the anion transport mechanism). The diuretic effect of Lasix is associated with inhibition of sodium chloride reabsorption in this section of the loop of Henle.
Secondary effects with respect to an increase in sodium excretion are: an increase in the amount of urine secreted (due to osmotically bound water) and an increase in potassium secretion in the distal part of the renal tubule. At the same time increases the excretion of calcium and magnesium ions.
With repeated administration of Lasix injections, its diuretic activity does not decrease, since the drug interrupts the tubular-glomerular feedback in Macula densa (the tubular structure closely associated with the juxtaglomerular complex). Lasix induces a dose-dependent stimulation of the renin-angiotensin-aldosterone system.
In heart failure, Lasix injections rapidly reduces preload (due to the expansion of the veins), decreases the pressure in the pulmonary artery and the filling pressure of the left ventricle. This rapidly developing effect appears to be mediated through the effects of prostaglandins and therefore the condition for its development is the absence of impairments in the synthesis of prostaglandins, in addition to which this effect also requires sufficient preservation of kidney function.
Lasix for injections has a hypotensive effect, which is caused by an increase in sodium excretion, a decrease in circulating blood volume and a decrease in the reaction of vascular smooth muscle to vasoconstriction effects (due to the natriuretic effect, furosemide reduces the response of vessels to catecholamines, which are increased in patients with arterial hypertension).
Dose-dependent diuresis and natriuresis are observed when taking Lasix injections at a dose of 10 mg to 100 mg. (healthy volunteers). After intravenous administration of 20 mg of Lasix injections, the diuretic effect develops in 15 minutes and lasts about 3 hours.
The relationship between intratubular concentrations of unbound (free) furosemide and its natriuretic effect is in the form of a sigmoidal curve with a minimum effective rate of excretion of furosemide of approximately 10 μg / min. Therefore, continuous infusion administration of furosemide is more effective than repeated bolus administration. In addition, when a certain bolus dose is exceeded, there is no significant increase in effect. When the canalicular secretion of furosemide decreases or when the drug is bound to albumin in the tubule lumen (for example, in nephrotic syndrome), the effect of furosemide decreases.

Pharmacokinetics

The distribution of furosemide is 0.1-0.2 l / kg body weight and varies considerably depending on the underlying disease. Furosemide is very strongly bound to plasma proteins (more than 98%), mainly albumin. Furosemide is excreted mainly in unchanged form and mainly by secretion in the proximal tubule. After intravenous administration of furosemide, 60-70% of the administered dose is eliminated in this way. The gluconated metabolites of furosemide account for 10–20% of the renal excreted drug. The remaining dose is excreted through the intestines, apparently by biliary secretion.
The final half-life of furosemide after intravenous administration is approximately 1-1.5 hours.
Furosemide penetrates the placental barrier and is secreted into the mother's milk. Its concentrations in the fetus and newborn are the same as in the mother.

Features of pharmacokinetics in certain groups of patients

In renal failure, the elimination of furosemide is slowed down, and the half-life is increased; in case of severe renal failure, the final period of elimination may increase up to 24 hours.
In nephrotic syndrome, a decrease in plasma concentrations of proteins leads to an increase in the concentrations of unbound furosemide (its free fraction), therefore, the risk of ototoxic action increases. On the other hand, the diuretic effect of furosemide in these patients may be reduced due to the binding of furosemide to albumin in the tubules, and a decrease in the tubular secretion of furosemide.
With hemodialysis and peritoneal dialysis and continuous ambulatory peritoneal dialysis, furosemide is only slightly excreted.
In liver failure, the half-life of furosemide is increased by 30-90% mainly due to an increase in the volume of distribution. Pharmacokinetic parameters in this category of patients can vary greatly.
In heart failure, severe hypertension, and in the elderly, the elimination of furosemide is slowed down due to a decrease in kidney function.
In premature and full-term infants, excretion of furosemide can slow down, which depends on the degree of maturity of the kidneys, the metabolism of Lasix for injections in infants can also be slowed down, since their glucurinating ability of the liver is inadequate. In children whose age after conception exceeds 33 weeks, the final half-life does not exceed 12 hours. In infants of two months of age, elimination of furosemide is not different from that in adults.

Indications for use

Edematous syndrome in chronic heart failure.
Edematous syndrome in acute heart failure.
Edematous syndrome in chronic renal failure.
Acute renal failure, including those during pregnancy and burns (to maintain fluid excretion).
Edematous syndrome in nephrotic syndrome (in nephrotic syndrome in the foreground is the treatment of the underlying disease).
Edematous syndrome in liver diseases (if necessary, in addition to treatment with aldosterone antagonists).
Cerebral edema.
Hypertensive crisis.
Maintenance of forced diuresis in case of poisoning with chemical compounds excreted by the kidneys in unchanged form.

Contraindications

Hypersensitivity to the active substance or to any of the components of the drug; Patients with a sulfonamide allergy (sulfanilamide antimicrobial agents or sulfonylurea drugs) may develop a "cross" allergy to furosemide.
Renal failure with anuria not responding to the introduction of furosemide.
Hepatic precoma and coma.
Severe hypokalemia.
Severe hyponatremia.
Hypovolemia (with or without arterial hypotension) or dehydration.
Pronounced disorders of urine outflow of any etiology (including unilateral damage to the urinary tract).
Pregnancy (see "Pregnancy and lactation").
Lactation period.

Carefully

arterial hypotension;
in conditions in which an excessive decrease in blood pressure is particularly dangerous (stenosing lesions of the coronary and / or cerebral arteries);
in acute myocardial infarction (increased risk of cardiogenic shock),
with latent or manifest diabetes mellitus;
gout;
with hepatorenal syndrome;
with hypoproteinemia (for example, with nephrotic syndrome, when it is possible to reduce the diuretic effect and increase the risk of the development of the ototoxic effect of furosemide, therefore, dose selection in such patients should be carried out with extreme caution);
in violation of the outflow of urine (prostatic hyperplasia, narrowing of the urethra or hydronephrosis);
with hearing loss,
with pancreatitis, diarrhea,
with a ventricular arrhythmia in history,
with systemic lupus erythematosus;
in premature babies (the possibility of formation of calcium-containing kidney stones (nephrolithiasis) and the deposition of calcium salts in the kidney parenchyma (nephrocalcinosis), therefore, regular monitoring of kidney function and an ultrasound of the kidneys is necessary).

Pregnancy and lactation period

Furosemide penetrates the placental barrier, so it should not be prescribed during pregnancy. If for life reasons, Lasix injections are prescribed for pregnant women, then careful monitoring of the condition of the fetus is necessary.
During lactation, furosemide is contraindicated. Furosemide inhibits lactation. Dosage and administration

General recommendations

At purpose of the drug Lasix injections it is recommended to use its smallest doses, sufficient to achieve the desired therapeutic effect.
Lasix for injections is administered intravenously and in exceptional cases intramuscularly (when intravenous administration is not possible or the drug is used orally). Intravenous administration of Lasix injections are carried out only when the drug is not taken inside or there is a violation of the drug's absorption in the small intestine or, if necessary, to obtain the fastest possible effect. When using intravenous administration of Lasix, it is always recommended to transfer the patient to the oral Lasix form as early as possible.
For intravenous administration, Lasix injections should be administered slowly. The rate of intravenous administration should not exceed 4 mg per minute. In patients with severe renal insufficiency (serum creatinine> 5 mg / dL), it is recommended that the rate of intravenous Lasix does not exceed 2.5 mg per minute. To achieve optimal efficacy and suppress counter-regulation (activation of the renin-angiotensin and antinatriuretic neurohumoral regulation links), a prolonged infusion intravenous administration of Lasix should be preferable compared to repeated intravenous bolus administration of Lasix for injections. If, after one or several bolus intravenous administrations in acute conditions, it is not possible to perform a continuous intravenous infusion, then it is more preferable to administer low doses with small intervals between doses (approximately 4 hours later) than intravenous bolus administration of higher doses with longer intervals between injections.

Parenteral Solution

About the introduction has a pH of about 9 and does not have buffer properties. At pH below 7, the active substance may precipitate out, therefore, when diluting Lasix injections, it is necessary to strive for the pH of the resulting solution to range from neutral to slightly alkaline. For breeding, you can use saline. The diluted solution of Lasix should be used as early as possible. The recommended maximum daily dose for intravenous administration for adults is 1500 mg. In children, the recommended dose for parenteral administration is 1 mg / kg body weight (but not more than 20 mg per day).
The duration of treatment is determined by the doctor individually, depending on the evidence.
Special recommendations for dosing regimen in adults:

Edematous syndrome in chronic heart failure

The recommended initial dose is 20-80 mg per day. The required dose is selected depending on the diuretic response. It is recommended that the daily dose be administered two to three times.

Edematous syndrome in acute heart failure

The recommended starting dose is 20-40 mg as an intravenous bolus. If necessary, the dose of Lasix injections may be adjusted depending on the therapeutic effect.

Edematous syndrome in chronic renal failure

The natriuretic reaction to furosemide depends on several factors, including the severity of renal failure and the sodium content in the blood, so the dose effect cannot be accurately predicted. Patients with chronic renal failure require careful dose selection, by gradually increasing it so that fluid loss occurs gradually (at the beginning of treatment, loss of fluid to about 2 kg of body weight per day is possible).
In patients on hemodialysis, the maintenance dose is usually 250–1500 mg / day.
When administered intravenously, the dose of furosemide can be determined as follows: treatment begins with intravenous drip at a rate of 0.1 mg per minute, and then gradually increase the rate of administration every 30 minutes, depending on the therapeutic effect.

Acute renal failure (to maintain fluid clearance)

Before starting treatment with Lasix injections, hypovolemia, hypotension and significant electrolyte and acid-base disorders should be eliminated. It is recommended that the patient be transferred as soon as possible from intravenous administration of Lasix to receiving Lasix tablets (the dose of Lasix tablets depends on the selected intravenous dose). The recommended initial intravenous dose is 40 mg. If, after its administration, the required diuretic effect is not achieved, then Lasix can be administered as a continuous intravenous infusion, starting at the administration rate of 50–100 mg per hour.

Edema in nephrotic syndrome

The recommended initial dose is 20-40 mg per day. The required dose is selected depending on the diuretic response.

Edematous syndrome in liver diseases

Furosemide is prescribed in addition to treatment with aldosterone antagonists if they are insufficiently effective. To prevent the development of complications, such as impaired orthostatic regulation of blood circulation or impaired electrolyte or acid-base status, careful dose selection is required so that fluid loss occurs gradually (at the beginning of treatment, fluid loss of up to about 0.5 kg of body weight per day is possible). If intravenous administration is absolutely necessary, then the initial dose for intravenous administration is 20-40 mg.

Hypertensive crisis, swelling of the brain

The recommended starting dose is 20-40 mg by intravenous bolus. The dose may be adjusted depending on the effect.

Maintenance of forced diuresis in case of poisoning

Furosemide is administered after intravenous infusion of electrolyte solutions. The recommended initial dose for intravenous administration is 20-40 mg. The dose depends on the reaction to furosemide. Before and during treatment with Lasix, the loss of fluids and electrolytes should be monitored and restored.

Side effect

From the side of water-electrolyte and acid-base balance:
hyponatremia, hypochloremia, hypokalemia, hypomagnesemia, hypocalcemia, metabolic alkalosis, which can develop as either a gradual increase in electrolyte deficiency or massive electrolyte loss in a very short time, for example, in the case of high doses of furosemide in patients with normal kidney function. Symptoms that indicate the development of electrolyte and acid-base disorders can be headache, confusion, convulsions, tetany, muscle weakness, cardiac arrhythmias, and dyspeptic disorders. Factors contributing to the development of electrolyte disorders are the main diseases (for example, cirrhosis of the liver or heart failure), concomitant therapy and nutrition. In particular, with vomiting and diarrhea, the risk of hypokalemia may increase; hypovolemia and dehydration (more often in elderly patients), which can lead to hemoconcentration with a tendency to develop thrombosis.
Since the cardiovascular system:
excessive reduction in blood pressure, which, especially in elderly patients, may manifest the following symptoms: impaired concentration and reaction, feeling of "emptiness" in the head, feeling of pressure in the head, headache, dizziness, drowsiness, weakness, visual disturbances, dry mouth , violation of orthostatic regulation of blood circulation. Development of a collapse, tachycardia, arrhythmias, decrease in the volume of the circulating blood is possible.
Metabolism:
increased serum levels of cholesterol and triglycerides;
transient increases in creatinine and urea in the blood;
elevated serum uric acid concentrations that may cause or increase the manifestations of gout;
decrease in glucose tolerance (possible manifestation of latent flowing diabetes mellitus).
From the urinary system:
the appearance or intensification of symptoms due to partial obstruction of the urinary tract (for example, in case of prostatic hyperplasia, narrowing of the urethra);
rarely interstitial nephritis;
nephrocalcinosis / nephrolithiasis in premature babies.
From the digestive tract:
rarely - nausea, vomiting, diarrhea, isolated cases of intrahepatic choleetasis, elevated levels of "liver" enzymes, acute pancreatitis.
From the central nervous system, organ of hearing:
rarely, paresthesias;
in rare cases, hearing loss, usually reversible, and / or tinnitus, especially in patients with renal insufficiency or hypoproteinemia (nephrotic syndrome), as well as in the case of rapid intravenous administration of the drug.
On the part of the skin, allergic reactions:
rarely - allergic skin reactions: itching, urticaria, other types of rash or bullous skin lesions, polymorphic erythema, exfoliative dermatitis, purpura, fever, vasculitis, photosensitization;
extremely rarely, severe anaphylactic or anaphylactoid reactions up to shock, which until now have been described only after intravenous administration.
Peripheral Blood:
rarely - thrombocytopenia, eosinophilia;
in rare cases, leukopenia;
in some cases, agranulocytosis, aplastic anemia or hemolytic anemia.

Others

in premature babies, the formation of calcium-containing kidney stones (nephrolithiasis) and the deposition of calcium salts in the renal parenchyma (nephrocalcinosis) is possible;
in premature babies, during the first weeks of life, furosemide may increase the risk of preserving the Botallova duct;
intramuscular soreness at the injection site.
Since some adverse reactions (such as changes in the blood picture, severe anaphylactic or anaphylactoid reactions, severe skin allergic reactions) can, under certain conditions, threaten the lives of patients, any side effects should be immediately reported to your doctor.

Overdose

The clinical picture of an acute or chronic overdose of a drug depends mainly on the degree and consequences of the loss of fluid and electrolytes; overdose may be manifested by hypovolemia, dehydration, hemoconcentration, abnormal heart rhythm and conduction (including atrioventricular block and ventricular fibrillation). Symptoms of these disorders are reduced blood pressure (up to the development of shock), acute renal failure, thrombosis, delusional condition, flaccid paralysis, apathy and confusion.
The treatment is aimed at correcting clinically significant disorders of water-electrolyte and acid-base status under the control of serum concentrations of electrolytes, indicators of acid-base status, hematocrit, as well as the prevention or therapy of possible serious complications developing on the background of these disorders.

Interaction with other drugs

Cardiac glycosides, drugs that cause prolongation of the QT interval - if electrolyte disturbances develop during the administration of furosemide (hypokalemia or hypomagnesia), the toxic effect of cardiac glycosides and drugs that prolong the QT interval increases (the risk of developing rhythm increases).
Glucocorticosteroids, carbenoxolone, licorice preparations in large quantities and prolonged use of laxatives when combined with furosemide increase the risk of developing hypokalemia.
Aminoglycosides - slowing down the excretion of aminoglycosides by the kidneys while they are used concurrently with furosemide and increasing the risk of the development of ototoxic and nephrotoxic action of aminoglycosides. For this reason, the use of this combination of drugs should be avoided, unless it is necessary for health reasons, and in this case, correction (reduction) of maintenance doses of aminoglycosides is required.
Drugs with nephrotoxic action - when combined with furosemide increases the risk of their nephrotoxic action.
High doses of some cephalosporins (especially those with predominantly renal excretion) - in combination with furosemide increases the risk of nephrotoxic action.
Cisplatin - when used concurrently with furosemide, there is a risk of ototoxic action. In addition, in the case of co-administration of cisplatin and furosemide in doses above 40 mg (with normal renal function), the risk of the development of the nephrotoxic effect of cisplatin increases.
Nonsteroidal anti-inflammatory drugs (NSAIDs) - NSAIDs, including acetylsalicylic acid, can reduce the diuretic effect of furosemide. In patients with hypovolemia and dehydration (including against the background of taking furosemide), NSAIDs can cause the development of acute renal failure. Furosemide may enhance the toxic effect of salicylates.
Phenytoin - reducing the diuretic action of furosemide
Antihypertensive drugs, diuretics, or other drugs that can lower blood pressure — when combined with furosemide, a more pronounced hypotensive effect is expected.
Angiotensin-converting enzyme (ACE) inhibitors - the appointment of an ACE inhibitor to patients who have previously received treatment with furosemide may lead to an excessive decrease in blood pressure with deterioration of renal function, and in some cases to the development of acute renal failure, therefore, three days before the start of treatment with inhibitors ACE or increasing their dose is recommended cancellation of furosemide, or reducing its dose.
Probenecid, methotrexate, or other drugs that, like furosemide, are secreted in the renal tubules, can reduce the effects of furosemide (the same way the kidney secretion), on the other hand, furosemide can lead to a decrease in kidney excretion of these medicines.
Hypoglycemic agents, pressor amines (norepinephrine epinephrine) - weakening effects when combined with furosemide.
Theophylline, diazoxide, curare-like muscle relaxants - increased effects when combined with furosemide.
Lithium salts - under the influence of furosemide, lithium excretion is reduced, thereby increasing the serum concentration of lithium and increasing the risk of the development of the toxic effect of lithium, including its damaging effects on the heart and nervous system. Therefore, when using this combination, monitoring of serum lithium concentrations is required.
Sucralfate - reducing the absorption of furosemide and reducing its effect (furosemide and sucralfate should be taken at least two hours apart).
Cyclosporin A - when combined with furosemide increases the risk of developing gouty arthritis due to hyperuricemia caused by furosemide, and cyclosporine disturbances in the excretion of urates by the kidneys.
Chloral hydrate - intravenous infusion in a 24-hour period after using chloral hydrate can lead to hyperemia of the skin, excessive sweating, anxiety, nausea, high blood pressure and tachycardia.
Radiocontrast agents - in patients with a high risk of nephropathy for the administration of radiopaque drugs treated with furosemide, there was a higher incidence of renal dysfunction compared with patients with a high risk of nephropathy for radiopaque drugs that received only intravenous hydration before the administration of the radiopaque drug. Intravenous furosemide has a slightly alkaline reaction, so it can not be mixed with drugs with a pH less than 5.5.

special instructions

Before starting treatment with Lasix injections, the presence of sharply expressed violations of urine outflow, including unilateral, should be excluded.
Patients with partial violation of urine outflow need careful observation, especially at the beginning of treatment with Lasix injections.
During treatment with Lasix injections, regular monitoring of serum concentrations of sodium, potassium and creatinine is usually required, especially careful monitoring should be carried out in patients with a high risk of electrolyte imbalance in cases of additional fluid and electrolyte losses (for example, due to vomiting, diarrhea or intense sweating).
Before and during treatment with Lasix injections, it is necessary to control and, in case of occurrence, eliminate hypovolemia or dehydration, as well as clinically significant disorders of the electrolyte and / or acid-base state, which may require a short-term discontinuation of treatment with Lasix.
When treating with Lasix injections, it is always advisable to eat foods rich in potassium (lean meat, potatoes, bananas, tomatoes, cauliflower, spinach, dried fruits, etc.). In some cases, it may be shown taking potassium supplements or prescribing potassium-sparing drugs.
In premature babies -: regular monitoring of renal function and ultrasound of the kidney is required (possibility of nephrolithiasis and nephrocalcinosis).
Some side effects (for example, a significant reduction in blood pressure and the accompanying symptoms - see the section "Side Effects") may impair the ability to concentrate and reaction, which can be dangerous when driving or working with mechanisms. This applies particularly to the period of initiation of treatment or increase in the dose of Lasix for injections, as well as to the cases of simultaneous administration of antihypertensive drugs or alcohol.
The selection of the dosing regimen for patients with ascites on the background of cirrhosis should be carried out in the hospital (violations of the water-electrolyte state may lead to the development of hepatic coma).

Compatibility Guidelines

Lasix 20 mg should not be mixed in the same syringe with other drugs.

Emergency measures in the development of anaphylactic shock

As a rule, the following measures are recommended: at the first signs (severe weakness, cold sweat, nausea, cyanosis), stop the injection, leaving the needle in the vein. Along with other usual urgent measures, it is necessary to ensure a low position of the head and body and maintain airway patency.
Emergency medical measures (recommendations for dosage are designed for an adult with a normal body weight, in the treatment of children, the dosage should be reduced in proportion to body weight):
Immediate intravenous administration of epinephrine (adrenaline): after dilution with 1 ml of a standard solution of epinephrine 1: 1000 to 10 ml, 1 ml of the resulting solution (= 0.1 mg of adrenaline) is slowly administered first under the control of heart rate, blood pressure and heart rate). If necessary, the administration of epinephrine can be continued by intravenous infusion. Simultaneously with the administration of epinephrine, intravenous administration of glucocorticosteroids (250-1000 mg of methylprednisolone or prednisolone) is made, which can be repeated if necessary. In addition to these activities, intravenous infusion of plasma substitutes and / or electrolyte solutions is performed to replenish circulating blood volume.
If necessary: ​​artificial respiration, inhalation of oxygen, antihistamines.

Forms of release

Solution for intravenous and intramuscular administration of 10 mg / ml.
2 ml of the drug in a vial of dark glass (type I). 10 ampoules per carton box together with instructions for use.

Storage conditions

At a temperature not higher than 25 ° С in the place protected from light.
Keep out of the reach of children.
Expiration date - 3 years. Do not use beyond the expiration date printed on the package.

Pharmacy sales terms

You don't need a prescription to buy Lasix for injections.