Kinetics of fenoximone, a new cardiotonic, in healthy subjects

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Abstract
Fenoximone was given to 6 healthy men as a single i.v. dose of 1 mg/kg and a single oral dose of 3 mg/kg as solution in a crossover study. Plasma concentrations were monitored or 8 h and urine was collected for 24 h. Peak plasma concentrations (Cmax) were reached 30 min after the oral dose. Decay of plasma concentrations was fitted to a mean (.+-. SD) elimination t1/2 (t1/2 .beta. [.beta.-phase half-life]) of 60 .+-. 14 min after i.v. injection and 78 .+-. 26 min after oral dosing. Mean total body clearance for i.v. dosing was 2062 .+-. 846 ml/min, renal clearance (ClR) was 5.3 .+-. 2.4 ml/min and extrapolated volume of distribution was 0.37 .+-. 0.26 l/kg. The sulfoxide derivative was detected as the main metabolite. Cmax of the sulfoxide metabolite occurred 10 min after the end of the i.v. infusion and 20-60 min after oral dosing. From the decay of the plasma concentrations of the sulfoxide, the t1/2.beta. were calculated as 132 .+-. 15 min after i.v. injection and 140 .+-. 27 min after oral dosing of fenoximone. ClR of the sulfoxide was 499 .+-. 106 ml/min after i.v. injection; 24-h urinary recovery of the sulfoxide was 75.7% .+-. 5.7% after i.v. injection and 64.3% .+-. 10.4% after oral dosing. Mean oral bioavailability of fenoximone was 53% (range 44-69%).

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