Dose proportionality of iopromide pharmacokinetics and tolerability after IV injection in healthy volunteers

Abstract

Twelve healthy male volunteers participated in a single-blind, randomised, placebo-controlled cross-over study of i.v. iopromide in doses of 15 g iodine or 80 g iodine infused over a period of 15 min. The volunteers were observed for three days during which time blood samples, urine and faeces were collected. The terminal disposition phase half-life of iopromide was 2 h and 1.9 h, and the total clearance was 110 and 103 ml.min-1 at the lower and at the higher dose levels, respectively. The steady state volume of distribution was 16 and 17 l, indicating predominantly extracellular distribution of iopromide. Statistical analysis (one-sided t-test) showed that all the target parameters (AUC, half-life and urinary excretion) were equivalent at both dose levels, indicating dose proportionate, first order kinetics of iopromide over the large dose range tested. Iopromide was well tolerated after both doses.

Dialysis and iodinated contrast media

“…The decrease of the serum level caused by renal elimination leads to a rediffusion of the contrast medium out of the tissue and back into the intravascular space, 3 and the decrease in plasma concentration follows a two-part exponential function. [4][5][6][7][8] In normal subjects and in subjects with mild, moderate, and severe renal impairment, the plasma concentration of the low osmolar contrast medium iomeprol declines biexponentially after intravenous administration. 8 Comparison of the fractions of the area under curve for each phase and comparison of the volume terms indicate that the first phase can be regarded as the distribution phase and the terminal phase as the elimination phase.…”

“…The half-life for iodinated contrast media in patients with normal glomerular function is between 40 and 120 min for ionic contrast media. [4][5][6] The half-life for nonionic iopromide has been reported to be 110 min. 6 Cumulative mean 120 h urinary excretion of low osmolar contrast medium iomeprol averages 93.5 and 63.8% in healthy subjects and those with severe renal impairment, respectively.…”

The Achilles tendon and the retrocalcaneal bursa

“… 16 Iopromide with different chemical properties is less permable in soft tissues 17 and this has been confirmed experimentally. 18 Intravenous injection of iopromide is distributed only in extracellular fluid. In contrast, intravenous corticosteroids are widely distributed in tissues.…”

Measurement of Glomerular Filtration Rate By Low-Dose Iopromide Plasma Clearance

“…There was no dosedependent difference in GFR in iohexol plasma clearance, whereas metrizoate clearance increased significantly in higher doses, possibly because of active tubular secretion of metrizoate (1). KRAUSE et al failed to find any dose-dependency of the pharmacokinetics of iopromide in a comparison of 15 g I and 80 g I (iopromide 300 mg I/ml) in 12 healthy male volunteers (12).…”

“…K rause et al failed to find any dose‐dependency of the pharmacokinetics of iopromide in a comparison of 15 g I and 80 g I (iopromide 300 mg I/ml) in 12 healthy male volunteers (12).…”