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Single-dose pharmacokinetics of fenquizone in healthy volunteers.

Abstract
A pharmacokinetic study of fenquizone (Idrolone), a thiazide-like diuretic, was conducted with single oral doses in 6 healthy volunteers. The substance thus administered was readily absorbed from the gut, with peak plasma levels being detected on average at 3 h after dosing; after that, plasma concentrations of fenquizone decreased biexponentially in a pattern fitting an open two-compartment model. Plasma half-life values were 1 h for phase alpha and 17 h for phase beta. The half-life calculated from urinary concentrations was 18 h. The apparent distribution volume for phase beta was 686 l; renal clearance was 220 ml/min, and the absorption constant (Ka) was 1055 h-1. Cumulative urinary excretion accounted for 53.1% of the administered dose in 72 h. Thus the pharmacokinetic profile of fenquizone was that of an "intermediate-acting" diuretic about half-way between the short-acting hydrochlorothiazide, chlorothiazide and furosemide and the long-acting chlorthalidone. In summation, fenquizone is described as a low-dosage diuretic apparently not conducive to accumulation; its pharmacokinetic profile qualifies the product particularly well for maintenance therapy, such as is needed for the management of essential hypertension, both as sole medication and in fixed-ratio combination with beta-blockers, and at any rate with once-a-day administration.
AuthorsG C Maggi, C Donati, D Gueli Alletti
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 35 Issue 6 Pg. 994-8 ( 1985) ISSN: 0004-4172 [Print] Germany
PMID4026929 (Publication Type: Journal Article)
Chemical References
  • Diuretics
  • Quinazolines
  • Sulfonamides
  • fenquizone
Topics
  • Adult
  • Blood Pressure (drug effects)
  • Diuretics (blood, pharmacology, urine)
  • Female
  • Half-Life
  • Heart Rate (drug effects)
  • Hemodynamics (drug effects)
  • Humans
  • Kinetics
  • Male
  • Quinazolines (blood, pharmacology, urine)
  • Sulfonamides

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