Abstract
1. The metabolism of isoprenaline has been studied in man and dog following intravenous and oral or intra-duodenal administration.
2. Intravenous isoprenaline was excreted largely unchanged in urine in both species. Only one-third of the radioactivity in urine was in the form of the O-methyl metabolite.
3. After oral doses in man or intraduodenal doses in dogs, plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine.
4. Catechol-O-methyl transferase may be less important than Uptake2 in limiting the pharmacological action of isoprenaline.
5. Pharmacological response (heart-rate increase) was related to plasma concentration of isoprenaline only after rapid intravenous injections. In dogs, following prolonged infusion or intraduodenal doses, heart rate returned to base-line values when plasma concentrations of isoprenaline were high.
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Selected References
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