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.
|
Authors | G C Maggi, C Donati, D Gueli Alletti |
Journal | Arzneimittel-Forschung
(Arzneimittelforschung)
Vol. 35
Issue 6
Pg. 994-8
( 1985)
ISSN: 0004-4172 [Print] Germany |
PMID | 4026929
(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
|