Chemical formula: C₃₅H₄₄I₆N₆O₁₅ Molecular mass: 1,550.182 g/mol PubChem compound: 3724
Iodixanol is a dimeric, non-ionic, water-soluble, radiographic contrast medium with a molecular weight of 1550.20 (iodine content 49.1%). The organically bound iodine absorbs radiation in the blood vessels/tissues when it is injected.
For most of the haemaodynamic, clinical-chemical and coagulation parameters examined following intravenous injection of iodixanol in healthy volunteers, no significant deviation from pre-injection values has been found. The few changes observed in laboratory parameters were minor and considered to be of no clinical importance.
In a study involving 129 diabetic patients with serum creatinine levels of 1.5-3.5 mg/dl, use of iodixanol resulted in 3% of patients experiencing a rise in creatinine of ≥0.5 mg/dl and no patients with a rise of ≥1.0 mg/dl. The peak increase in the serum creatinine concentration within three days after the administration of iodixanol was 0.13 mg per dl (11.2 µmol per litre). A transient increase in tubular enzyme excretion was observed after contrast media injection. However, lower or similar effects on the release of enzymes (alkaline phosphatase and N-acetyl-ß-glucosaminidase) from the proximal tubular cells were observed for iodixanol in comparison to ioxaglate.
Cardiovascular parameters such as LVEDP, LVSP, heart rate and QT-time as well as femoral blood flow were less influenced after iodixanol than after other contrast media, where measured.
Iodixanol is rapidly distributed in the body with a mean distribution half-life of approximately 21 minutes. The apparent volume of distribution is of the same magnitude as the extracellular fluid (0.26 Ι/kg b.w.), indicating that iodixanol is distributed in the extra-cellular volume only.
Iodixanol displayed no protein binding in vitro (less than 2% detectable limit) at a 1.2 mg I/ml concentration in human plasma. No significant metabolism, de-iodination or biotransformation has been detected in animals.
The mean elimination half-life is approximately 2 hours. Iodixanol is excreted mainly through the kidneys by glomerular filtration. Approximately 80% of the administered dose is recovered unmetabolised in the urine within 4 hours and 97% within 24 hours after intravenous injection in healthy volunteers. Only about 1.2% of the injected dose is excreted in faeces within 72 hours. The maximum urinary concentration appears within approximately 1 hour after injection.
No dose dependent kinetics have been observed in the recommended dose range.
Forty three (43) paediatric patients <12 years old, with renal function that is normal for their age, received multiple intra-arterial administrations of iodixanol injection in doses of 0.32 to 3.2 g I/kg body weight. The elimination half-lives for these patients are derived from the mean terminal elimination rate constants (Kel): 0.185/hr (newborn to 2 months old), 0.256/hr (2 to <6 months old), 0.299/hr (6 months to <1 year), 0.322/hr (1 to <2 years), and 0.307/hr (2 to <12 years old). The adult mean terminal elimination rate constant is 0.336/hr.
The actual iodixanol clearance and volume of distribution in paediatric patients were not determined. Pharmacodynamic dose adjustments to account for differences in elimination halflife in paediatric patients under 6 months of age have not been studied.
No long-term animal studies have been performed to evaluate the carcinogenic potential of iodixanol.
Iodixanol did not induce gene mutation in bacteria or Chinese hamster ovary (CHO) cells in vitro. It was not clastogenic in CHO cells in vitro or in mice in vivo.
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