Pharmacokinetics and bioavailability of piretanide in healthy volunteers following intramuscular administration.
The pharmacokinetics of the diuretic compound 4-phenoxy-3-(1-pyrrolidinyl)-5-sulfamoylbenzoic acid (piretanide, Arelix) were investigated in 10 healthy male volunteers following intravenous and intramuscular administration of single doses of 6 mg. Plasma concentration-time data followed in general characteristics of a three-compartment model. Following intravenous administration, the terminal half-life of elimination was 1.29 +/- 0.40 h, the total clearance 219 +/- 36 ml/min and the steady state volume of distribution was calculated to be 12.4 +/- 2.1 l. The renal excretion of unchanged drug amounted to 34.4 +/- 6.9% of the dose. Following intramuscular administration, peak plasma concentrations of 366 +/- 85 mg/ml were achieved 13.8 +/- 4.8 min after administration. All other parameters were not statistically significantly different from those obtained after i.v. bolus. The bioavailability of piretanide following intramuscular administration was 0.88 +/- 0.17.
Trenk
D
D
Abteilung für Klinische Pharmakologie, Johann Wolfgang Goethe-Universität, Frankfurt/Main, Fed. Rep. of Germany.
Wagner
F
F
Jähnchen
E
E
Spahn
H
H
Mutschler
E
E
D000328:Adult; D001682:Biological Availability; D004232:Diuretics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D008297:Male; D011897:Random Allocation; D013449:Sulfonamides / Q000008:administration & dosage / Q000493:pharmacokinetics*
D004232:Diuretics; D013449:Sulfonamides; C015451:piretanide