Active substanceFurosemideFurosemide
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains: active substance: furosemide 40.0 mg. Excipients: lactose monohydrate (25.50 mg), silicon dioxide colloidal anhydrous (1.00 mg), wheat starch (30.50 mg), magnesium stearate (1.00 mg), talc (2.00 mg).

    Description:

    Round, biconcave tablets, from white to almost white.

    Pharmacotherapeutic group:diuretic
    ATX: & nbsp

    C.03.C.A.01   Furosemide

    Pharmacodynamics:

    "Loopback" diuretic, causes a rapidly advancing, strong and short-term diuresis. It blocks the reabsorption of sodium and chlorine ions in both the proximal and distal sections of the renal tubules and in the thick segment of the ascending part of the Gentle loop. Furosemide has a pronounced diuretic, natriuretic and chlororetic effects. Due to the increase in the release of sodium ions, a secondary (osmotically bound water-mediated) enhanced water removal and an increase in the secretion of potassium ions in the distal part of the renal tubule occur simultaneously. The excretion of calcium and magnesium ions simultaneously increases.Has secondary effects due to the release of intracellular mediators and redistribution of the intrarenal blood flow. Against the background of course treatment, there is no weakening of the effect.

    With heart failure furosemide quickly reduces preload (by expanding the veins), reduces pulmonary artery pressure and filling pressure of the left ventricle. It has an antihypertensive effect due to an increase in elimination of sodium chloride and a decrease in the response of the smooth muscles of the vessels to vasoconstrictive effects and as a result of a decrease in the volume of circulating blood.

    After ingestion of 40 mg furosemide diuretic effect begins within 60 minutes and lasts about 3-6 hours (with reduced renal function - up to 8 hours). During the period of action, excretion of sodium ions increases significantly, but after its termination, the elimination rate decreases below the initial level ("rebound" syndrome, or "cancellation"). The phenomenon is caused by a sharp activation of the renin-angiotensin-aldosterone system and other antinatriuretic neurohumoral regulating units in response to massive diuresis; stimulates arginine-vasopressive and sympathetic systems.Reduces the level of the atrial natriuretic factor in the blood plasma, causes vasoconstriction. Due to the "ricochet" syndrome, when taken once a day, it can not cause a significant effect on the daily excretion of sodium ions and arterial pressure (BP).

    Pharmacokinetics:

    Absorption is high, the maximum concentration is noted in the blood plasma when ingested after 1 hour.

    Bioavailability - 60 - 70%. The relative volume of the distribution is 0.2 l / kg. Communication with blood plasma proteins - 98%. Penetrates through the placental barrier, excreted in breast milk. Metabolised in the liver with the formation of 4-chloro-5-sulfamoylantranilic acid. It is secreted into the lumen of the renal tubules through the anion transport system existing in the proximal nephron. It is excreted mainly (88%) by the kidneys in unchanged form and in the form of metabolites; the rest is intestinal. Half-life (T1 / 2) - 1-1.5 h.

    Peculiarities of pharmacokinetics in selected groups of patients

    With renal failure, the excretion of furosemide slows down, and the half-life increases; with pronounced renal failure, the final T 1/2 can increase to 24 hours.

    In the nephrotic syndrome, a decrease in plasma protein concentrations leads to an increase in the concentrations of unbound furosemide (its free fraction), which increases the risk of ototoxic action. On the other hand, the diuretic effect of furosemide in these patients can be reduced by binding furosemide to albumin in the tubules and reducing the tubular secretion of furosemide.

    With hemodialysis, peritoneal dialysis and permanent ambulatory peritoneal dialysis furosemide output is insignificant.

    Inadequate liver function T1 / 2 furosemide is increased by 30-90% mainly due to an increase in the relative volume of distribution. Pharmacokinetic parameters in this category of patients can vary greatly.

    With heart failure, severe arterial hypertension and in elderly patients, excretion of furosemide slows down due to decreased kidney function.

    Indications:
    • edematous syndrome with chronic heart failure, edematous syndrome with chronic renal failure,edematous syndrome with nephrotic syndrome (with nephrotic syndrome in the foreground is the treatment of the underlying disease); edematous syndrome with liver diseases;

    • Arterial hypertension in adults, as a monotherapy or in combination with other antihypertensive drugs.

    Contraindications:

    Increased sensitivity to the active substance and to any of the components of the drug; allergy to sulfonamides (sulfanilamide antimicrobial agents or sulfonylureas); anuria or acute renal failure with anuria; kidney failure due to poisoning with nephrotoxic or hepatotoxic products; renal failure with hepatic coma; Precomatous and comatose conditions associated with hepatic encephalopathy; disturbance of water-electrolyte metabolism (hypovolemia or dehydration, severe hyponatremia and hypokalemia, pregnancy, lactation, age up to 3 years (solid dosage form), lactose intolerance, lactase insufficiency, glucose-galactose malabsorption syndrome (due to the presence of lactose in the formulation monohydrate).

    Carefully:

    should prescribe the drug to patients with hypotension or an increased risk of a sharp decrease in blood pressure; patients with latent or manifest diabetes mellitus (impaired glucose tolerance) or diabetic patients with an increased need for insulin; gout; with hepatorenal syndrome; hypoproteinemia due to nephrotic syndrome (risk of ototoxicity development); preterm neonates - nephrocalcinosis / nephrolithiasis may develop; patients with acute porphyria.

    Pregnancy and lactation:

    Pregnancy

    Furosemide penetrates the placental barrier, so it should not be administered during pregnancy. If desired destination Sofarma drug Furosemide pregnant should weigh the benefits of the drug to the risk for the mother to the fetus.

    Breast-feeding

    Excreted in breast milk. If it is necessary to treat the drug, breastfeeding should be discontinued.

    Dosing and Administration:

    Tablets should be taken on an empty stomach without chewing and drinking with a sufficient amount of liquid.

    The daily dose and the regimen of the drug are set individually, depending on the therapeutic response, while determining the minimum effective dose.

    Taking the drug is possible every day or every other day.

    Dosage

    Adults

    The initial single dose is 40 mg. An additional dosage adjustment may be required before the maintenance dose is reached.

    In mild cases, a dose of 40 mg every other day may be sufficient.

    In cases of resistant edema, the usual daily dose is 80 mg or more, once or twice a day, or if necessary.

    With severe edematous conditions, a gradual increase in the dose to 600 mg per day is possible.

    The maximum daily intake for adults is 1500 mg.

    Edema Syndrome in Chronic Heart Failure

    The initial dose is 40-80 mg / day. The required dose is selected depending on the diuretic response

    Edema Syndrome in Chronic Renal Failure

    The recommended initial dose is 40-80 mg / day. In patients with chronic renal failure, careful dose selection is required, by gradually increasing it so that fluid loss occurs gradually (at the beginning of treatment, a loss of fluid of up to about 2 kg of body weight / day is possible).

    In patients on hemodialysis, the usual maintenance dose is 250-1500 mg / day.

    Edema with nephrotic syndrome

    The initial dose is 40-80 mg / day. The necessary dose is selected depending on the diuretic response.

    Edema syndrome with liver diseases

    The initial dose is 40-80 mg / day. Furosemide Sopharma is prescribed in addition to treatment with aldosterone antagonists in case of their insufficient effectiveness. To prevent the development of complications, such as a violation of orthostatic regulation of blood circulation or a violation of the electrolyte or acid-base state, careful selection of the dose is required so that the loss of fluid occurs gradually (at the beginning of the treatment, a loss of fluid up to about 0.5 kg of body weight / day is possible) .

    Arterial hypertension

    Furosemide Sopharma can be used in monotherapy or in combination with other antihypertensive drugs. The usual maintenance dose is a dose of 40 mg / day. When furosemide is added to already prescribed medications, their dose should be reduced 2 times. With arterial hypertension in combination with chronic renal failure may require the use of higher doses of the drug.

    Children

    The recommended single dose in children is determined from the calculation of 1-3 mg / kg body weight / day, with the possible increase in the dose - up to 40 mg per day.

    Elderly patients

    In elderly patients furosemide is output more slowly, therefore, if necessary, dosage adjustment is possible to achieve a therapeutic effect.

    Side effects:

    from the cardiovascular system: a marked decrease in blood pressure (in more severe cases it occurs with symptoms of decreased concentration and delayed reactions, dizziness, headache, sensation of rotation, drowsiness, weakness, visual impairment, dry mouth); orthostatic collapse, propensity to thrombosis, vasculitis, decrease in the volume of circulating blood

    from the central nervous system: paresthesia, hepatic encephalopathy (in patients with hepatocellular insufficiency), apathy, adynamia, weakness, lethargy, drowsiness, confusion.

    from the side of the hearing organ and labyrinthine disorders: hearing impairment, tinnitus. Usually are transient. More often they appear in patients with renal insufficiency, hypoproteinemia (with nephrotic syndrome).

    from the gastrointestinal tract: acute pancreatitis; nausea, vomiting, diarrhea.

    hepatobiliary disorders: intrahepatic cholestasis, elevation of hepatic transaminase levels, cholestatic jaundice, pancreatitis (exacerbation).

    from the genitourinary and urinary systems: acute urinary retention (in patients with benign prostatic hyperplasia with partial obstruction of the urinary tract), interstitial nephritis, nephrocarydanosis / nephrolithiasis in premature infants.

    from the endocrine system: decrease in glucose tolerance.

    from the immune system: purpura, urticaria, exfoliative dermatitis, multiforme exudative erythema, pruritus, other rashes or bullous lesions, fever, photosensitivity, severe anaphylactic or anaphylactoid type reactions (including shock), Stevens-Johnson syndrome, bullous pemphigoid, toxic epidermal necrolysis.

    from the hematopoiesis: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia, hemolytic anemia, eosinophilia. Hemoconcentration.

    There are reports of suppression of bone marrow function, which requires immediate cessation of furosemide treatment,

    from the water-electrolyte exchange: hypovolemia, in elderly patients - hypovolemia and dehydration (risk of hemoconcentration, thrombosis and thromboembolism), hypokalemia, hyponatremia, hypochloraemia, hypocalcemia, hypomagnesemia, metabolic alkalosis. Reversible increase in plasma levels of creatinine and urea; hypercholesterolemia and hypertriglyceridemia; hyperuricemia with gout attacks. Violations of the water-electrolyte balance are expressed in increased thirst, headache, hypotension, confusion, muscle cramps, tetany, muscle weakness, heart rhythm disturbances and gastrointestinal symptoms.

    congenital, hereditary and genetic disorders: increased risk persistent arterial duct, when furosemide is used in preterm infants in the first weeks of their life.

    Overdose:

    Symptoms: marked decrease in blood pressure, collapse, shock, hypovolemia, dehydration, hemoconcentration, arrhythmias (incl. AV blockade, ventricular fibrillation) due to increased diuresis, acute renal failure with anuria, thrombosis, thromboembolism, drowsiness, confusion, flaccid paralysis, apathy.

    Treatment: correction of water-electrolyte balance and acid-base state, replenishment of the volume of circulating blood, gastric lavage, reception of activated charcoal, symptomatic treatment. There is no specific antidote.

    Interaction:

    With simultaneous use with phenobarbital and phenytoin, the action of furosemide is reduced.

    Increases the concentration and risk of developing nephro- and ototoxic effects of cephalosporins, cisplatin, amphotericin B (due to competitive renal excretion).

    With the simultaneous use of aminoglycosides with furosemide, aminoglycoside excretion slows down and the risk of developing their ototoxic and nephrotoxic action increases. For this reason, use of such a combination of drugs should be avoided, except when necessary for life indications, in which case correction (reduction) of aminoglycoside doses is required.

    Increases the effectiveness of diazoxide and theophylline, reduces - hypoglycemic agents (oral antidiabetics, insulin), allopurinol. Medicines with nephrotoxic action - when combined with furosemide, the risk of developing their nephrotoxic effect increases. Glucocorticosteroids, corticotropin and amphotericin B lead to loss of potassium. When combined with furosemide, this can lead to a serious decrease in plasma potassium levels. Carbenoksolon, nicotine, beta2-sympathomimetics in high doses, prolonged use of laxatives, reboxetine may increase the risk of hypokalemia.

    With simultaneous use with cardiac glycosides, the risk of developing digitalis intoxication against a background of water-electrolyte disorders (hypokalemia or hypomagnesemia) that cause the syndrome of an elongated interval QT.

    Strengthens the neuromuscular blockade of depolarizing muscle relaxants (suxamethonium) and weakens the effect of nondepolarizing muscle relaxants (tubocurarine).

    Non-steroidal anti-inflammatory drugs (NSAIDs) (including indomethadine and acetylsalicylic acid) in combination with furosemide maycause a temporary decrease in creatinine clearance and an increase in serum potassium content and reduce the diuretic and antihypertensive effects of furosemide. In patients with hypovolemia and dehydration (including furosemide), NSAIDs can cause acute renal failure. Furosemide can enhance the toxic effect of salicylates (due to competitive renal excretion).

    Sucralfate reduces the absorption of furosemide and weakens its effect (these preparations should be taken at intervals of not less than 2 hours).

    Combination with carbamazepine may increase the risk of hyponatremia, and with corticosteroids, on the contrary, can cause sodium retention. Hypotensive drugs, diuretics or other means that can reduce blood pressure when combined with furosemide can lead to a more pronounced antihypertensive effect.

    The use of angiotensin-converting enzyme (ACE) angiotensin inhibitors or angiotensin II receptor antagonists in patients previously treated with furosemide may result in excessive lowering of blood pressure with impaired renal function,and in some cases to the development of acute renal failure, therefore, three days before the start of treatment with ACE inhibitors or angiotensin II receptor antagonists, or increasing their dose, it is recommended that furosemide be withdrawn or reduced.

    Probenecid, methotrexate and other medications, which, like furosemide, are secreted in the renal tubules, can reduce the action of furosemide (the same pathway of kidney secretion), on the other hand furosemide can lead to a decrease in the excretion of these drugs by the kidneys. Simultaneous use with metolazonom (thiazide diuretic) can cause increased diuresis.

    Lithium salts - under the influence of furosemide, lithium excretion decreases, which increases the serum concentration of lithium and increases the risk of its toxic effects, including damaging effects on the heart and nervous system. Therefore, when using this combination, control of serum lithium concentrations is required.

    Simultaneous administration of cyclosporin A and furosemide increases the risk of gouty arthritis due to hyperuricemia,caused by furosemide and violation of cyclosporin excretion of urate by the kidneys.

    Pressor amines (epinephrine, norepinephrine) and furosemide mutually reduce efficiency.

    Radiopaque substances - in patients with a high risk of developing nephropathy for the introduction of radiopaque preparations that received furosemide, a higher incidence of renal dysfunction was observed compared to patients at high risk of developing nephropathy for the introduction of radiopaque preparations that received only intravenous hydration prior to the administration of the radiopaque preparation.

    The use of diuretics is considered potentially dangerous when used simultaneously with risperidone. In placebo-controlled trials with risperidone, encompassing elderly patients with dementia, a higher mortality was observed in patients treated simultaneously with furosemide and risperidone compared to patients treated with only furosemide or only risperidone, therefore special caution is required when using furosemide simultaneously with risperidone in such patients.

    As a combined or concomitant treatment, such therapy can only be used after an assessment of the benefit / risk ratio.

    There are no reports of increased mortality among patients taking other diuretics (mainly thiazide diuretics, at low doses) as concomitant treatment with risperidone.

    Patients who are prescribed cholestyramine. Use this medication at least 1 hour after taking furosemide.

    Special instructions:

    Excessively aggressive diuresis can cause orthostatic hypotension, and acute hypotensive episodes.

    Before starting therapy with Furosemide Sopharma, it is necessary to provide a passable way for removing urine from the body. Patients with a partial impairment of urine outflow may be provoked by complaints or exacerbated by existing ones. In patients with prostatic hypertrophy or with severe impairment of urinary efflux of any etiology (including unilateral urinary tract damage), an acute urinary retention may develop if bladder emptying is not previously provided. On the background course of treatment should periodically monitor blood pressure, the content of plasma electrolytes (including sodium, calcium, potassium, magnesium ions), acid-base state, residual nitrogen, creatinine, uric acid, liver function and, if necessary, appropriate treatment correction. The states of hypovolemia or dehydration should also be adjusted before starting treatment.

    The use of furosemide slows the excretion of uric acid, which can provoke an exacerbation of gout.

    Patients with increased sensitivity to sulfonamides and sulfonylureas may have cross-sensitivity to furosemide.

    For the prevention of hypokalemia, simultaneous administration of potassium and potassium-sparing diuretics is recommended, as well as adherence to a diet rich in potassium.

    In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of the level of glucose in the blood and urine is required.

    In patients with unconsciousness, benign prostatic hyperplasia, narrowing of the ureters, or hydronephrosis, monitoring of urinary excretion is necessary because of the possibility of acute urinary retention.

    Because of the possibility of developing nephrocalcinosis / nephrolithiasis in preterm neonates; it is necessary to monitor kidney function and echographic control. Furosemide Sopharma contains lactose monohydrate, so patients with rare hereditary problems of galactose intolerance, lactase deficiency Lapp or malabsorption of glucose-galactose, should not take this drug.

    The composition of the drug includes wheat starch in an amount that is safe for use in patients with celiac disease (gluten enteropathy). Patients with wheat allergy (other than celiac disease) should not use this drug.

    During the treatment with Furosemide Sopharma, avoidance of potentially dangerous activities that require increased attention and speed of psychomotor reactions (vehicle management and work with mechanisms) should be avoided.

    Form release / dosage:

    Tablets of 40 mg.


    Packaging:For 10 or 50 tablets in a blister of PVC film of orange color / aluminum foil.
    2 blisters for 10 tablets or 1 blister for 50 tablets together with instructions for use in a pack of cardboard.
    50 blisters for 50 tablets together with instructions for use in a pack of cardboard (for hospitals).
    Storage conditions:
    In dry the dark place at a temperature of no higher than 25 C.
    Keep out of the reach of children!
    Shelf life:5 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N008776
    Date of registration:19.08.2011
    The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria
    Manufacturer: & nbsp
    Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria
    Information update date: & nbsp13.11.2015
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