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A study on furosemide disposition in man.

J B Zhu1, T Koizumi

  • 1Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.

Journal of Pharmacobio-Dynamics
|August 1, 1987
PubMed
Summary
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Furosemide is rapidly absorbed orally and eliminated renally in healthy adults. Oral bioavailability was higher than previously reported, with a two-compartment model describing its disposition.

Area of Science:

  • Pharmacokinetics
  • Drug Metabolism and Transport

Background:

  • Furosemide is a widely used diuretic.
  • Understanding its disposition is crucial for optimizing therapeutic use.

Purpose of the Study:

  • To characterize the pharmacokinetic disposition of furosemide in healthy volunteers following intravenous and oral administration.
  • To determine oral bioavailability and compare it with existing data.

Main Methods:

  • Six healthy male volunteers received intravenous and oral furosemide doses.
  • Serum drug concentrations were measured using high-performance liquid chromatography.
  • Urinary excretion was quantified spectrophotometrically.
  • Data were analyzed using a two-compartment open model.

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Main Results:

  • Furosemide disposition is well-described by a two-compartment model with rapid absorption (ka = 2.33 h-1) and a lag time of 6.45 min.
  • Oral relative bioavailability was 83%, higher than previously reported.
  • Renal excretion is the primary elimination route, with systemic clearance (CLs) of 7.60 L/h and renal clearance (CLr) of 6.44 L/h after IV dosing.
  • Non-renal clearance was higher after oral administration, suggesting a first-pass effect.

Conclusions:

  • Furosemide exhibits favorable oral absorption and disposition characteristics in healthy individuals.
  • The drug is primarily eliminated by the kidneys.
  • The observed higher oral bioavailability warrants consideration in clinical practice.