The radiosynthesis, percutaneous absorption, and metabolism of the wound-healing agent calcium acexamate in the rat.
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Acetates↗
Biomedical subjects
L F Chasseaud
Publications and source records attributed to L F Chasseaud.
Metabolic fate of the beta-blocker 14C-bupranolol in humans, dogs, and rhesus monkeys.
An oral dose of 14C-bupranolol hydrochloride was well absorbed by humans (100 mg), dogs (1 mg/kg), and rhesus monkeys (1 mg/kg). These species excreted 87.8 and 3.5%, 81.1 and 13.6%, and 92.9 ad 5.0% of the 14C-dose in urine and feces, respectively, mainly in 12 or 24 hr. Mean plasma levels of 14C, which appeared to be almost entirely associated with a single metabolite, peaked at 1 hr in humans (1.6 micrograms-equiv./ml) and dogs (1.6 micrograms-/ml) and at 2 hr in monkeys (0.8 micrograms-equiv./ml). Concentrations initially declined with similar half-lives (about 1.5 hr) in all three species. Biliary excretion of 14C occurred in the animal species in which also peak plasma 14C levels exceeded those in most tissues. Unchanged bupranolol was not detected in plasma; the peak plasma and urinary 14C was mainly associated (greater than 90% in humans) with a metabolite produced by oxidation of the aromatic ring methyl group of bupranolol to a carboxyl group.
Absorption↗
Metabolic fate of bromperidol in humans: comparison with rats and dogs.
The metabolic fate of an oral dose of 2 mg of 3H-bromperidol has been studied in two human subjects. During 5 days, about 50% of the radioactive dose was excreted by both subjects, somewhat more in the urine than in the faeces. Excretion rates were slow. Concentrations of radioactivity in plasma were low reaching a peak of 6-10 ng equivalents/ml during 1.5-4 hours, but concentrations of the parent drug were less than 0.5 ng/ml at all times. A major metabolite, more polar than bromperidol was present in human urine and is under investigation. The metabolic fate of bromperidol in humans is different from that in rats or dogs.
Animals↗