Pharmacokinetics of lodamide in Normal Subjects and in Patients with Renal Impairment

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Abstract
The pharmacokinetic characteristics of iodamide, a contrast agent for excretion urography, were studied in 7 normal subjects and in 15 patients with various degrees of renal impairment. Two different formulations were administered, namely, a 65% solution (iodamide 300) by slow i.v. injection and 24% solution by slow i.v. (drip) infusion. Both preparations of iodamide exhibited characteristics of an open 2-compartment model. In both normal subjects and patients, the contrast agent was excreted almost exclusively in urine. In normal subjects, the pharmacokinetic parameters of both formulations were similar, with a distribution half-life (t1/2.alpha.) of about 3 min and a disposition half-life (t1/2.beta.) of about 69 min. An average of 84% of the dose was excreted in urine within 4 h after administration of iodamide with net renal tubular secretion of about 38%. The binding of iodamide to plasma proteins was negligible and the extent of biotransformation of iodamide was minimal. In patients with renal impairment, the t1/2.beta. of iodamide ranged from 4.1-16.4 h. Other changes in pharmacokinetic parameters were also seen in patients with renal impairment.