Indications
Ioversol, marketed under the names Optiray 300, Optiray 320, and Optiray 350, has distinct indications based on its formulation and method of administration. As Optiray 300, ioversol is used intra-arterially for cerebral and peripheral arteriography in adults and intravenously for CT imaging of various body parts, venography, and excretory urography in adults. Optiray 320 expands its intra-arterial indications to include visceral and renal arteriography, aortography, coronary arteriography, left ventriculography in adults, and angiocardiography in pediatric patients. Its intravenous applications include CT imaging, venography, and urography for both adults and children. Optiray 350 is employed intra-arterially for peripheral, coronary arteriography, and left ventriculography in adults, as well as angiocardiography in children, and intravenously for a comprehensive range of imaging, such as CT scans, venography, urography, and digital subtraction angiography in adults, with some applications extended to pediatric patients.
Pharmacodynamics
The pharmacodynamic properties of ioversol are fundamentally associated with its iodine content, which facilitates contrast enhancement in diagnostic imaging. Post-injection, iodine plasma levels reach a peak, but the timeframe for maximum contrast differs by organ. The contrast intensity develops from when iodine levels peak to about an hour after an intravenous bolus is administered. This delay arises as iodine-containing compounds accumulate in targeted lesions outside the bloodstream. For angiographic applications, ioversol achieves optimal contrast within 15 to 120 seconds after administration. In cases of standard renal function, the renal parenchyma becomes visible in 30 to 60 seconds, and the calyces and pelves achieve optimal visualization within 5 to 15 minutes after injection.
Absorption
The absorption characteristics of ioversol have been studied in healthy individuals, who demonstrated Cmax values of 1.45 mg/mL and 2.36 mg/mL after receiving 50 mL and 150 mL doses, respectively. The corresponding tmax values were recorded at 2.0 minutes and 4.3 minutes. Additionally, the area under the curve (AUC) values were measured at 1.74 mg·hr/mL and 4.43 mg·hr/mL for 50 mL and 150 mL doses, respectively. The pharmacokinetics of ioversol adhere to an open two-compartment model following first-order elimination, suggesting that individuals with renal impairment may exhibit lowered elimination rates due to the drug's primary excretion through the kidneys as an unaltered compound.
Metabolism
Ioversol is characterized by its lack of significant metabolism, deiodination, or biotransformation in the body. The compound remains largely unchanged following administration, emphasizing its stability and predictability in pharmacokinetic profiles.
Mechanism of Action
Ioversol is a highly soluble, non-ionic iodinated contrast agent that improves the clarity of radiographic images. Upon intravascular injection, ioversol enhances the visibility of blood vessels along the path of the contrast medium, enabling clear visualization of internal structures until substantial hemodilution occurs. During imaging procedures, ioversol transitions from the vascular to the extravascular space. In the brain, when the blood-brain barrier is intact, ioversol does not penetrate into the extravascular space. However, if the blood-brain barrier is compromised, the agent accumulates in the interstitial space of the affected area. In its form as Optiray, ioversol significantly enhances computed tomographic imaging by increasing radiographic efficiency, with the extent of density enhancement being directly proportional to the iodine content in the administered dose.
