Ioversol (100 mg iodine/mL) dramatically lowers 3-(4,5-dimethyloxadiazol-2-yl)-2,5-dimethylbenzoate and boosts lactate dehydrogenase release in NRK-52E cells. change in azole. In NRK-52E cells, ioversol treatment markedly elevated caspase-3 protein expression and cellular abundance. [Ca2+]i and intracellular ROS can be markedly elevated by isoversol treatment[1].

Ioversol significantly reduces endothelin release from cultivated cells and when injected into anesthetized bodies as compared to iophthalate. In both control and USIC, ioversol resulted in less renal vasoconstriction than sulfate, and radiocontrast nephropathy was mainly prevented from developing due to substantial muscle clearance and morphological damage to the renal medulla. [2].

Absorption, Distribution and Excretion
Healthy volunteers that received 50 and 150 mL of ioversol, had a corresponding Cmax of 1.45 mg/mL and 2.36 mg/mL and a corresponding tmax of 2.0 min and 4.3 min. AUC was 1.74 mg⋅hr/mL in healthy volunteers that received 50 mL of ioversol, and 4.43 mg⋅hr/mL in those that received 150 mL. The pharmacokinetics of ioversol follow an open two compartment model with first-order elimination. Since ioversol is almost completely excreted by the kidney as a parent drug, patients with renal impairment are expected to have a lower elimination rate.
Following intravascular administration, ioversol is excreted mainly through the kidneys. Within the first 24 hours, more than 95% of the administered dose is excreted. Urine concentration peaks in the first 2 hours after ioversol is administered. Fecal elimination is negligible.
In adults, the volume of distribution of ioversol was 0.26 L/kg body weight, consistent with its extracellular space distribution.
In healthy volunteers that received 50 mL of ioversol, clearance was 156 mL/min, and in those receiving 150 mL of ioversol, clearance was 185 mL/min.

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Metabolism / Metabolites
Ioversol does not undergo significant metabolism, deiodination or biotransformation.

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Biological Half-Life
The elimination half-life was 1.5 hr in healthy volunteers (n=12) receiving 50 and 150 mL of ioversol 68%. In patients with renal dysfunction, the elimination half-life of ioversol is prolonged.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Intravenous iodinated contrast media are poorly excreted into breastmilk and poorly absorbed orally so they are not likely to reach the bloodstream of the infant or cause any adverse effects in breastfed infants. Guidelines developed by several professional organizations state that breastfeeding need not be disrupted after a nursing mother receives an iodine-containing contrast medium. However, because there is no published experience with ioversol during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
Ioversol does not bind to serum or plasma proteins.

[1]. Yang D, et al. Selective inhibition of the reverse mode of Na(+)/Ca(2+) exchanger attenuates contrast-induced cell injury. Am J Nephrol. 2013;37(3):264-73. doi: 10.1159/000348526. Epub 2013 Mar 13.
[2]. Heyman SN, et al. Effects of ioversol versus iothalamate on endothelin release and radiocontrast nephropathy. Invest Radiol. 1993 Apr;28(4):313-8.
[3]. J Ueda, et al. Elimination of ioversol by hemodialysis. Acta Radiol. 1996 Sep;37(5):826-9.
[4]. N Motoji , et al. Comparison of the effects of ioversol and other contrast media on the blood-brain barrier. Biol Pharm Bull. 1994 Feb;17(2):257-61

Ioversol is an amidobenzoic acid.
Ioversol is a non-ionic compound with a tri-iodinated benzene ring used as a contrast dye in diagnostic procedures to visualize different types of organs and tissues. Iodine has a high atomic density, which gives it the ability to attenuate X-rays. The intravascular administration of iodine compounds, such as ioversol, enhances the contrast between vessels in the path of the flow of the contrast medium and normal tissue, allowing the visualization of internal structures. Ioversol is a highly hydrophilic agent considered to be generally safe; however, serious adverse reactions have been reported due to the inadvertent intrathecal administration of ioversol, which is only indicated for intra-arterial and intravenous use. Ioversol was approved by the FDA in 1989 and is currently indicated for computed tomographic (CT) imaging and contrast enhancement in peripheral arteriography, coronary arteriography, and left ventriculography.
Ioversol is a Radiographic Contrast Agent. The mechanism of action of ioversol is as a X-Ray Contrast Activity.
Ioversol is a sterile, nonpyrogenic, aqueous solution intended for intravascular administration as a diagnostic radiocontrast agent. Ioversol is available in various concentrations, ranging from 240 to 350 milligrams of iodine per milliliter.

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Drug Indication
As the product Optiray 300, the intra-arterial use of ioversol is indicated for cerebral arteriography and peripheral arteriography in adults, while its intravenous use is indicated for CT imaging of the head and body, venography, and intravenous excretory urography in adults. As the product Optiray 320, the intra-arterial use of ioversol is indicated for cerebral arteriography, peripheral arteriography, visceral and renal arteriography, aortography, coronary arteriography, and left ventriculography in adults, and angiocardiography in pediatic patients. The intravenous use of this product is indicated for CT imaging of the head and body, venography, and intravenous excretory urography in adults and CT imaging of the head and body, and intravenous excretory urography in pediatric patients. As the product Optiray 350, the intra-arterial use of ioversol is indicated for peripheral arteriography coronary arteriography, and left ventriculography in adults, and angiocardiography in pediatic patients. The intravenous use of this product is indicated for CT imaging of the head and body, venography, intravenous excretory urography, and intravenous digital subtraction angiography (IV-DSA) in adults and CT imaging of the head and body, and intravenous excretory urography in pediatric patients.

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Mechanism of Action
Ioversol is a highly soluble non-ionic ionidated contrast agent. Intravascular injection of ioversol opacifies those vessels in the path of the flow of the contrast medium, allowing the radiographic visualization of the internal structures until significant hemodilution occurs. In imaging procedures, ioversol diffuses from the vascular to the extravascular space. In brains with an intact blood-brain barrier, this agent does not diffuse to the extravascular space. However, in patients with a disrupted blood-brain barrier, ioversol accumulates in the interstitial space of the disrupted region. As the product Optiray, ioversol enhances computed tomographic imaging through augmentation of radiographic efficiency with the degree of density enhancement directly related to the iodine content in an administered dose.

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Pharmacodynamics
The contrast enhancement obtained with ioversol is related to iodine content. Immediately after ioversol is injected, a peak in iodine plasma levels can be detected. However, depending on the organ being imaged, the time to maximum contrast will vary. The time to maximum contrast enhancement will range from the time iodine plasma levels reach their highest concentration to one hour after intravenous bolus administration. The delay between a peak in iodine plasma levels and maximum contrast enhancement is partly due to the accumulation of iodine-containing medium within a lesion and outside the blood pool. For angiographies, the maximum contrast enhancement of ioversol occurs almost immediately (15-120 seconds). Following rapid intravenous injection, ioversol can be visualized in the renal parenchyma within 30 to 60 seconds. In patients with normal renal function, opacification of the calyces and pelves takes place within 1-3 minutes, with an optimum contrast within 5-15 minutes.

C18H24N3O9I3

807.109860000001

806.864

87771-40-2

3741

Typically exists as solid at room temperature

2.3±0.1 g/cm3

864.9±65.0 °C at 760 mmHg

180-182ºC

476.9±34.3 °C

0.0±0.3 mmHg at 25°C

1.739

-4.01

8

9

12

33

623

0

O=C(C1C(I)=C(N(CCO)C(CO)=O)C(I)=C(C(NCC(CO)O)=O)C=1I)NCC(CO)O

AMDBBAQNWSUWGN-UHFFFAOYSA-N

InChI=1S/C18H24I3N3O9/c19-13-11(17(32)22-3-8(29)5-26)14(20)16(24(1-2-25)10(31)7-28)15(21)12(13)18(33)23-4-9(30)6-27/h8-9,25-30H,1-7H2,(H,22,32)(H,23,33)

1-N,3-N-bis(2,3-dihydroxypropyl)-5-[(2-hydroxyacetyl)-(2-hydroxyethyl)amino]-2,4,6-triiodobenzene-1,3-dicarboxamide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~123.90 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (3.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)