Kinetic disposition and diuretic effect of frusemide in acute pulmonary oedema.

Perez, J.; Sitar, Daniel S.; Ogilvie, Raymond

doi:10.1111/j.1365-2125.1980.tb05842.x

Cited by 22 publications

(10 citation statements)

References 16 publications

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“…This observation has been confirmed by the studies of Perez et al [22], performed in 16 adult patients with acute pulmonary edema (12 of these patients had a creatinine clearance higher than 100 ml/min). These authors, however, have demonstrated a relationship between the amount of furosemide excreted in a 24-hour urine collection and the volume of urine collected at that time, while in the present study this correlation was not significant.…”

Section: Amount Of Furosemide In Urine and Diuretic Effect Of Furosemidesupporting

confidence: 77%

“…These authors, however, have demonstrated a relationship between the amount of furosemide excreted in a 24-hour urine collection and the volume of urine collected at that time, while in the present study this correlation was not significant. This discrepancy is probably due to the difference in furosemide disposition kinetics in the body, since the drug half-life in the plasma of patients studied by Perez et al [22] averaged 420 min, while the t% of furosemide in the children calculated from the drug urinary excretion data was about 120 min [25,27]. Although renal clear ance values found in the patients with acute pulmonary edema were nor mal, implying a normal excretory process for furosemide by the kidneys, Perez et al [22] have observed a reduced percentage of the dose eliminated by the renal route as unchanged furosemide and interpreted this as being due to the greater than normal peripheral volume of distribution of the drug.…”

Section: Amount Of Furosemide In Urine and Diuretic Effect Of Furosemidementioning

confidence: 99%

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Pharmacodynamic Determinants of Furosemide Diuretic Effect in Children

Prandota¹

1986

Dev Pharmacol Ther

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The pharmacodynamics of 1 or 2 mg/kg of furosemide administered as a single dose orally or intravenously were studied in 34 hospitalized children (ranging in age from 9 days to 16.5 years) with normal renal function. These patients were divided into 3 groups: infants (furosemide 1 mg/kg, intravenously); children with steroid-responsive nephrotic syndrome (furosemide 2 mg/kg, orally and intravenously); patients with urinary tract infections and mild hypertension (furosemide 2 mg/kg, orally). A statistically significant positive linear relationship was found in these groups between the furosemide urinary excretion rate and urine flow rate, but log dose-response curves to furosemide were found to vary between the groups of patients studied. This variability reflects differences in the relationship between the amounts of furosemide reaching active sites and the pharmacodynamic effect of the drug. No sigmoid-shaped log dose-response curve (i.e., one approaching a zero response at very low furosemide urinary excretion rates, and a maximum response at very high excretion rates) was attained in this study. This suggests that the capacity of the kidney tubules to respond diuretically to the administered doses of furosemide was not exceeded in the studied patients. However, in the infants, a very steep log dose-response curve to a 1 mg/kg intravenous dose of furosemide suggests that higher doses may not result in a significant increase in diuretic response in infants with reasonably normal renal function. The lowest mean furosemide urinary excretion rate associated with significant diuresis was 0.58 ± 0.33 gg/kg/min. Also, a significant correlation was found between the amount (in milligrams), of furosemide excreted in the urine during the first 6 h after administration and the urine volume collected during that time (r = 0.71; p < 0.001; number of measurements = 43).

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Section: Amount Of Furosemide In Urine and Diuretic Effect Of Furosemidesupporting

confidence: 77%

Section: Amount Of Furosemide In Urine and Diuretic Effect Of Furosemidementioning

confidence: 99%

Pharmacodynamic Determinants of Furosemide Diuretic Effect in Children

Prandota¹

1986

Dev Pharmacol Ther

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“…The disposition of F in children and adults has been analyzed by either a one-or two-compartment open model [2,5,14,17,22], In the present study the one-compartment model was used because semilogarithmic plots of the F urinary excretion profiles were compatible with a one-compartment open model. The validity of the one-compartment model is supported by the fact that the measured values and the calculated curves fit well, as shown by the good correlation and regression coefficients in table III.…”

Section: Kinetic Data Analysismentioning

confidence: 99%

Kinetics of Urinary Furosemide Elimination in Infants

Prandota¹,

Houin²

1984

Dev Pharmacol Ther

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Using a one-compartment model, the urinary elimination kinetics of a single intravenous 1 mg/kg dose of furosemide (F) was studied in 13 infants, 9 days to 12 months old (mean 3.7 ± (SD) 3.48 months old), and 1, 23-month-old child, with bilateral multifocal pneumonia, recovering from respiratory and cardiac insufficiency accompanying pneumonia and/or other diseases. F elimination half-life was determined with the use of a noninvasive method based on the drug’s urinary excretion data. The drug urinary elimination t(½) in the infants ranged from 0.654 to 3.29 h. Cumulative excretion of F in the infants' urine was similar to the values in healthy adults. Since the furosemide urinary half-lives found in infants were similar to the data reported in older children and healthy adults it is suggested that immaturity of renal function during the 1st year of life, i.e. in older infants, has no evident effect on the elimination kinetics of a 1 mg/kg intravenous dose of F. Mean F urinary elimination t(½) in infants with pneumonia and cardiac insufficiency was significantly longer compared with the F(t½) found in children with the pneumonia alone (2.15 vs. 1.01 h, respectively), suggesting slower elimination of the drug in these patients.

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“…The hydrolysis product, 4-chloro-N-furfuryl-5-sulphamoylantranilic acid (CSA), has been demonstrated in the urine after intravenous administration of frusemide. In healthy young males 1-5% of the frusemide dose was excreted as CSA (Andreasen et al, 1981) and in patients with hypertension, coronary artery disease and myocardial infarction 0.13-3.92% of the administered frusemide dose was recovered as CSA (Perez et al, 1980). Cruz et al, (1979) For comparison with three of the above mentioned gastric juices buffer solutions were made (NaCl = 40 mM, KCl = 5 mm, and adjusted to pH = 1.2-1.4-1.6 with HCI, respectively).…”

Section: Introduction Methodsmentioning

confidence: 99%

In vitro studies on the hydrolysis of frusemide in gastrointestinal juices.

Andreasen¹,

Bøtker²,

Lorentzen³

1982

Brit J Clinical Pharma

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To elucidate a possible explanation for a relatively low bioavailability, the hydrolysis of frusemide in gastrointestinal juices was studied in vitro at concentrations likely to be present in vivo. Between 1.0 and 4.4% of the frusemide molecules were hydrolyzed to 4‐ chloro‐N‐furfuryl‐5‐sulphamoyl‐antranilic acid (CSA) after 1 h at 37 degrees C in gastric juices. The rate of hydrolysis was inversely connected to pH. No fall in frusemide concentration was observed and no CSA was found in duodenal juices after 4 h at 37 degrees C. In three buffer solutions with the same pH as three gastric juices frusemide was hydrolyzed to CSA at a lower rate than in the gastric juices (pH 1.2, P less than 0.15;pH 1.4, P less than 0.001; pH 1.6, P less than 0.001). The solubility of frusemide was significantly higher in gastric juice from two fasting subjects (83‐104 mg l‐1) than in buffer solutions with the same pH (52‐58 mg 1‐1). The solubility of frusemide was significantly increased (by 40‐50%) in gastric juice obtained after pentagastrin stimulation compared with its solubility in the mixed gastric secretion obtained after fasting. The binding of frusemide to macromolecules was 28.0 +/‐ 9.7% in ventricular secretion after fasting while it was 1.4 +/‐ 2.6% in the fluid obtained after pentagastrin stimulation. It is concluded that a hydrolysis of frusemide in the stomach prior to absorption cannot explain the relatively low bioavailability of the drug observed after oral intake.

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Kinetic disposition and diuretic effect of frusemide in acute pulmonary oedema.

Cited by 22 publications

References 16 publications

Pharmacodynamic Determinants of Furosemide Diuretic Effect in Children

Pharmacodynamic Determinants of Furosemide Diuretic Effect in Children

Kinetics of Urinary Furosemide Elimination in Infants

In vitro studies on the hydrolysis of frusemide in gastrointestinal juices.

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