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Published on: August 17, 2016
Human pharmacokinetics of iodixanol
M G Svaland1, T Haider, K Langseth-Manrique
1Department of Bioanalysis, Nycomed AS, Oslo, Norway.
Insights
This study investigated iodinated contrast media pharmacokinetics in healthy volunteers. Iodixanol demonstrated predictable excretion, primarily via glomerular filtration, supporting its safety profile for X-ray imaging.
Area of Science:
- Pharmacology
- Radiology
- Nephrology
Background:
- X-ray contrast media are essential for medical imaging.
- Understanding the pharmacokinetic properties of new contrast agents is crucial for safety and efficacy.
- Iodixanol is a novel nonionic dimer contrast agent.
Purpose of the Study:
- To evaluate the pharmacokinetic properties of iodixanol in healthy male volunteers.
- To determine the absorption, distribution, metabolism, and excretion (ADME) profile of iodixanol.
- To assess the impact of different intravenous doses on iodixanol pharmacokinetics.
Main Methods:
- Phase I clinical study involving 40 healthy male volunteers.
- Intravenous administration of iodixanol at doses of 0.3, 0.6, 0.9, and 1.2 g iodine/kg body weight.
- Concomitant administration of 51Cr-EDTA to assess renal excretion via glomerular filtration.
Main Results:
- Mean half-lives for iodixanol were 26 minutes (distribution phase) and 131 minutes (elimination phase).
- Apparent volume of distribution was 0.28 L/kg, indicating distribution limited to extracellular fluid.
- Approximately 97% of the administered dose was excreted unchanged in urine within 24 hours, with 1.2% in feces.
- Pharmacokinetic parameters were dose-independent.
Conclusions:
- Iodixanol exhibits predictable pharmacokinetics characterized by rapid distribution and elimination primarily through glomerular filtration.
- The excretion profile of iodixanol is comparable to other intravascular contrast media.
- These findings support the safety and suitability of iodixanol for diagnostic imaging procedures.
Abstract:
The pharmacokinetic properties of the x-ray contrast medium, iodixanol, a new nonionic dimer, were investigated in a phase I study including 40 healthy male volunteers. Iodixanol (300 mg I/mL) was administered intravenously (i.v.) at four dose levels--0.3, 0.6, 0.9, and 1.2 g iodine (I)/kg body weight--and saline was given as a control. 51Cr-EDTA was given concomitantly with iodixanol at all dose levels to study renal excretion of iodixanol. Mean half-lives were 26 and 131 minutes in the distribution and elimination phase, respectively. Apparent volume of distribution was 0.28 1/kg body weight, indicating distribution to extracellular fluid only. Within 24 hours after injection, 97% of the dose was excreted unmetabolized in the urine via glomerular filtration. The excretion in feces was 1.2% of the dose. The parameters calculated were independent of the given dose. The pharmacokinetics of iodixanol are comparable with those reported for other intravascular contrast media.
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