Pharmacokinetics of indoramin in man

1 The fate of oral and intravenous indoramin has been studied after single doses in man using the 14C labelled drug. Plasma concentrations of indoramin have been determined during chronic oral antihypertensive therapy employing a stable isotope dilution assay. 2 Following singleoral dosing the drug is well absorbed and extensively metabolised. Faecal excretion in 72 h accounts for 46% of the administered radioactivity of which approximately 4% is associated with indoramin. Less than 2% of the radioactivity in urine is accountable as the concentration of total metabolites. Peak plasma levels both of drug and metabolites occur 1-2 h after dosing, the maximal lowering of blood pressure occurring at this time. 3 The clearance of indoramin, determined after intravenous administration is of the same order as liver blood flow. In the isolated perfused rat liver, the extraction ratio is 0.98.