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
Following administration of 50 mL and 150 mL of iodofol, the peak plasma concentrations (Cmax) in healthy volunteers were 1.45 mg/mL and 2.36 mg/mL, respectively, with time to peak concentrations (tmax) of 2.0 min and 4.3 min, respectively. The AUC in healthy volunteers receiving 50 mL of iodofol was 1.74 mg·hr/mL, and the AUC in those receiving 150 mL was 4.43 mg·hr/mL. The pharmacokinetics of iodofol conformed to an open two-compartment model with first-order elimination. Since iodofol is almost entirely excreted unchanged by the kidneys, clearance is expected to be reduced in patients with renal impairment. Following intravenous administration, iodofol is primarily excreted by the kidneys. Over 95% of the administered dose is eliminated within 24 hours. Urinary concentrations peak within the first 2 hours after administration. Fecal excretion is negligible. In adults, the volume of distribution of iodofol is 0.26 L/kg body weight, consistent with its extracellular distribution. In healthy volunteers receiving 50 mL of iodofol, the clearance rate was 156 mL/min; in healthy volunteers receiving 150 mL of iodofol, the clearance rate was 185 mL/min. Metabolism/Metabolites: Iodofol does not undergo significant metabolism, deiodination, or biotransformation. Biological Half-Life: In healthy volunteers (n=12) receiving 50 mL and 150 mL of iodofol, the elimination half-life was 1.5 hours. In patients with renal impairment, the elimination half-life of iodofol is prolonged.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Very little iodinated contrast agents are excreted into breast milk after intravenous administration, and oral absorption is also poor. Therefore, they are unlikely to enter the infant's bloodstream and will not cause any adverse effects on breastfed infants. Guidelines developed by multiple professional organizations indicate that breastfeeding mothers do not need to interrupt breastfeeding after receiving iodinated contrast agents. However, since there is currently no published experience regarding the use of iodofol during lactation, other contrast agents may be preferred, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants
No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.
Protein Binding
iodofol 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 aminobenzoic acid. Ioversol is a nonionic compound containing a triiodobenzene ring in its molecular structure, used as a contrast agent in diagnostic procedures to visualize different types of organs and tissues. Iodine has a high atomic density, enabling it to attenuate X-rays. Intravascular administration of iodine compounds, such as Ioversol, enhances the contrast between blood vessels and normal tissue along the contrast agent's flow path, thus enabling visualization of internal structures. Ioversol is a highly hydrophilic contrast agent and is generally considered safe; however, serious adverse reactions have been reported due to accidental intrathecal injection, and it is only suitable for intra-arterial and intravenous administration. Ioversol was approved by the U.S. Food and Drug Administration (FDA) in 1989 and is currently used for contrast enhancement in computed tomography (CT) imaging, peripheral arteriography, coronary angiography, and left ventricular angiography. Ioversol is a radioactive contrast agent. Its mechanism of action is as an X-ray contrast agent. Ioversol is a sterile, pyrogen-free aqueous solution intended for use as an intravascular diagnostic contrast agent. Ioversol is available in various concentrations, with iodine content ranging from 240 to 350 mg per milliliter.

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Indications
Ioversol (trade name Optiray 300) is indicated for intra-arterial administration of cerebral angiography and peripheral angiography in adults, while intravenous administration is indicated for adult head and trunk CT imaging, venography, and intravenous urography. As a product, Optiray 320, intra-arterial administration of Ioversol is indicated for adult cerebral angiography, peripheral angiography, visceral and renal angiography, aortic angiography, coronary angiography, and left ventricular angiography, as well as pediatric cardiovascular angiography. Intravenous administration of this product is indicated for adult head and trunk CT imaging, venography, and intravenous urography, as well as pediatric head and trunk CT imaging and intravenous urography. As a product, Optiray 350, intra-arterial administration of iodofol is indicated for peripheral angiography, coronary angiography, and left ventricular angiography in adults, and cardiovascular angiography in children. This product is also indicated for head and trunk CT imaging, venography, intravenous urography, and intravenous digital subtraction angiography (IV-DSA) in adults, and head and trunk CT imaging and intravenous urography in children.

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Mechanism of Action
Iodofol is a highly soluble, non-ionic, ionized contrast agent. Intravascular injection of iodofol allows visualization of blood vessels along the contrast agent's flow path, thus achieving radiographic imaging of internal structures before significant hemodilution occurs. During imaging, iodofol diffuses from the blood vessels into the extravascular space. In brain tissue with an intact blood-brain barrier, this contrast agent does not diffuse into the extravascular space. However, in patients with a compromised blood-brain barrier, iodofol accumulates in the interstitial space of the damaged area. As an Optiray product, iodofol improves the quality of computed tomography (CT) images by enhancing radiographic imaging efficiency; the degree of density enhancement is directly related to the iodine content in the administered dose.

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Pharmacodynamics
Iodofol's contrast enhancement is related to iodine content. Peak plasma iodine concentration can be detected immediately after iodofol injection. However, the time required to reach maximum contrast varies depending on the imaging organ. The time to reach maximum contrast enhancement ranges from the time when plasma iodine concentration reaches its highest value to one hour after intravenous bolus administration. The delay between peak plasma iodine concentration and the achievement of maximum contrast enhancement is partly due to the accumulation of iodine-containing mediators within the lesion and outside the blood pool. For angiography, maximum contrast enhancement with iodofol occurs almost immediately (15-120 seconds). Imaging within the renal parenchyma occurs within 30 to 60 seconds after rapid intravenous injection of iodofol. In patients with normal renal function, the renal calyces and pelvis become visible within 1 to 3 minutes, with optimal imaging achieved within 5 to 15 minutes.

C18H24N3O9I3

807.109860000001

806.864

87771-40-2

3741

White to off-white solid powder

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.)