Pharmacokinetics and bioavailability of piretanide in healthy volunteers following intramuscular administration
Trenk, D.; Wagner, F.; Jähnchen, E.; Spahn, H.; Mutschler, E.
Arzneimittel-Forschung 37(12): 1382-1385
1987
ISSN/ISBN: 0004-4172 PMID: 3449067 Document Number: 287079
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 characteristic 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 ng/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.