Instructions for Furosemide
Structure Furosemide:
Furosemide 40mg;
Auxiliaries: milk sugar, potato starch, magnesium stearate
Pharmacodynamics Furosemide:
Loop diuretic; causes fast onset, strong and short-term diuresis. It disrupts the reabsorption of sodium and chlorine ions in both the proximal and distal sections of the convoluted tubules and in the thick segment of the ascending part of the Henle loop. Furosemide has a pronounced diuretic, natriuretic, and chloruretic effect.
In addition, it increases the excretion of potassium, calcium, magnesium ions.
Indications Furosemide:
Edema syndrome in heart failure stage IIB-III, cirrhosis, kidney disease (including nephrotic syndrome); acute left ventricular failure (pulmonary edema), edema with burns, arterial hypertension.
Pharmacokinetics Furosemide:
Absorption is high, Cmax is observed in blood plasma when taken orally after 1 h. Bioavailability is 60-70%. Relative Vd - 0.2 l / kg. Binding to plasma proteins - 98%.
Penetrates through the placental barrier, excreted in breast milk. It is metabolized in the liver with the formation of 4-chloro-5-sulfamoylanthranilic 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 unchanged and in the form of metabolites; the rest is by the intestines. T1 / 2 - 1-1.5 hours
Features of pharmacokinetics in certain groups of patients With renal failure, the excretion of furosemide slows down, and T1 / 2 increases; in severe renal failure, the final T1 / 2 can increase up to 24 hours. In nephrotic syndrome, a decrease in plasma protein concentrations leads to an increase in the concentration of unbound furosemide (its free fraction), which increases the risk of developing an ototoxic effect. On the other hand, the diuretic effect of furosemide in these patients may be reduced due to the binding of furosemide to the albumin located in the tubules and a decrease in tubular secretion of furosemide.
With hemodialysis, peritoneal dialysis and continuous outpatient peritoneal dialysis, furosemide is not significantly excreted. In liver failure, T1 / 2 of furosemide increases by 30-90% mainly due to an increase in the relative volume of distribution. Pharmacokinetic parameters in this category of patients can vary greatly.
In heart failure, severe arterial hypertension, and in elderly patients, furosemide excretion slows down due to decreased renal function.
Side effects Furosemide:
From the cardiovascular system: a marked decrease in blood pressure, collapse, tachycardia, arrhythmias, a tendency to thrombosis, a decrease in the volume of circulating blood. From the central nervous system: dizziness, headache, muscle weakness, spasms of the calf muscles (tetany), paresthesia, apathy, adynamia, weakness, lethargy, drowsiness, confusion. From the sensory organs: impaired vision and hearing, tinnitus. From the digestive system: anorexia, dry mucous membrane of the oral cavity, thirst, nausea, vomiting, diarrhea, constipation, cholestatic jaundice, pancreatitis (exacerbation), hepatic encephalopathy.
From the genitourinary system: oliguria, acute urinary retention (in patients with benign prostatic hyperplasia), interstitial nephritis, hematuria, decreased potency.
From the endocrine system: a decrease in glucose tolerance, a manifestation of latent diabetes mellitus.
Allergic reactions: purpura, urticaria, exfoliative dermatitis, exudative erythema multiforme, vasculitis, necrotizing angiitis, pruritus, chills, fever, photosensitivity, anaphylactic shock, Stevens-Johnson syndrome, bullous pemphygrolis pemphigrolis, toxic.
From the hemopoietic organs: leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia, eosinophilia. On the part of water-electrolyte metabolism: hypovolemia, dihydration (risk of thrombosis and thromboembolism), hypokalemia
Special conditions Furosemide:
Before starting therapy with Furosemide Sofarma, the presence of pronounced violations of the outflow of urine should be excluded, patients with partial impairment of the outflow of urine need careful monitoring. Against the background of the course of treatment, it is necessary to periodically monitor blood pressure, the content of blood plasma electrolytes (including sodium, calcium, potassium, magnesium ions), the acid-base state, residual nitrogen, creatinine, uric acid, liver function and, if necessary, appropriate treatment correction.
The use of furosemide slows the excretion of uric acid, which can provoke an exacerbation of the course of gout. Patients with hypersensitivity to sulfonamides and sulfonylurea derivatives may have cross-sensitivity to furosemide. In patients receiving high doses of furosemide, in order to avoid the development of hyponatremia and metabolic alkalosis, it is impractical to limit the intake of table salt. For the prevention of hypokalemia, the simultaneous administration of potassium and potassium-sparing diuretics is recommended, as well as a diet rich in potassium. The dosage regimen for patients with ascites against cirrhosis of the liver should be selected under stationary conditions (disturbances in the water-electrolyte balance can lead to the development of hepatic coma). This category of patients shows regular monitoring of plasma electrolytes.
With the appearance or intensification of azotemia and oliguria in patients with severe progressive kidney disease, it is recommended to suspend treatment. In patients with diabetes mellitus or with reduced glucose tolerance, periodic monitoring of the level of glucose concentration in the blood and urine is required. In patients in an unconscious state, with benign prostatic hyperplasia, narrowing of the ureters or hydronephrosis, urination control is necessary due to the possibility of acute urinary retention. The drug contains lactose monohydrate, so patients with rare hereditary problems of galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. The composition of the drug includes wheat starch in an amount that is safe for use in patients with celiac disease (celiac enteropathy).
Patients with an allergy to wheat (other than celiac disease) should not use this medication. Impact on the ability to drive vehicles and control mechanisms During treatment with Furosemide Sofarma, one should avoid engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions (driving and working with mechanisms).
Contraindications Furosemide:
Hypersensitivity to furosemide, acute renal failure with anuria (glomerular filtration less than 3-5 ml / min), severe liver failure, hepatic coma, acute glomerulonephritis, urethral stenosis, obstruction of the urinary tract with stone, hyperglycemic coma, hyperuricemia, gout, gout, mitral or aortic stenosis, increased central venous pressure (over 10 mmHg), idiopathic hypertrophic subaortic stenosis, arterial hypotension, acute nfarkt infarction, systemic lupus erythematosus, pancreatitis, violation of water-electrolyte metabolism (hypovolemia, hyponatremia, hypokalemia, chloropenia, hypocalcemia, hypomagnesemia), digitalis intoxication. Drug Interactions With the simultaneous use of phenobarbital and phenytoin, the effect of furosemide decreases. Increases the concentration and risk of nephro- and ototoxic effects of cephalosporins, chloramphenicol, ethacrylic acid, cisplatin, amphotericin B (due to competitive renal excretion). With the simultaneous use of aminoglycosides with furosemide, there is a slowdown in the elimination of aminoglycosides and an increase in the risk of developing their ototoxic and nephrotoxic effects. 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 the maintenance doses of aminoglycosides is required. Increases the effectiveness of diazoxide and theophylline, reduces hypoglycemic agents, allopurinol. Medicines blocking tubular secretion increase the concentration of furosemide in blood serum. Medicines with nephrotoxicity - when combined with f
Dosage Furosemide:
The dosage regimen is 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. The drug is prescribed orally in the morning, before meals and the initial dose for adults is 20–40 mg (1 / 2–1 tablets). With insufficient exposure, the dose is gradually increased to 80-160 mg per day (2-3 doses at intervals of 6 hours). After reducing swelling, the drug is prescribed in smaller doses with a break of 1-2 days. In case of arterial hypertension, 20–40 mg is prescribed; in the absence of a sufficient decrease in blood pressure, other antihypertensive drugs must be added to the treatment. When furosemide is added to already prescribed antihypertensive drugs, their dose should be reduced by 2 times. The initial single dose in children is 1-2 mg / kg, the maximum is 6 mg / kg.
