Non-ionic radiocontrast agent

Iodixanol is a dimeric, non-ionic, water-soluble, radiographic contrast agent, used particularly in coronary angiography. It has a role as a radioopaque medium.

DTI-derived mean diffusivity(MD) and fractional anisotropy(FA) values can be used to evaluate CI-AKI effectively. Quercetin significantly increased the expression of Sirt 1 and reduced oxidative stress by increasing Nrf 2/HO-1/SOD1. The antiapoptotic effect of quercetin on CI-AKI was revealed by decreasing proteins level and by reducing the number of apoptosis-positive cells. In addition, flow cytometry indicated quercetin-mediated inhibition of M1 macrophage polarization in the CI-AKI.Conclusions: DTI will be an effective noninvasive tool in diagnosing CI-AKI. Quercetin attenuates CI-AKI on the basis of DM through anti-oxidative stress, apoptosis, and inflammation[1]. Redox Rep. 2024 Dec;29(1):2398380.

To investigate the renal pathophysiological processes and protective effect of quercetin on contrast-induced acute kidney injury (CI-AKI) in mice with type 1 diabetic mellitus(DM) using diffusion tensor imaging(DTI).Methods: Mice with DM were divided into two groups. In the diabetic + contrast medium(DCA) group, the changes of the mice kidneys were monitored at 1, 24, 48, and 72 h after the injection of iodixanol(4gI/kg). The mice in the diabetic + contrast medium + quercetin(DCA + QE) group were orally given different concentrations of quercetin for seven days before injection of iodixanol. In vitro experiments, renal tubular epithelial (HK-2) cells exposed to high glucose conditions were treated with various quercetin concentrations before treatment with iodixanol(250 mgI/mL) [1]. Redox Rep. 2024 Dec;29(1):2398380.

Absorption, Distribution and Excretion
In adults, approximately 97% of the injected iodixanol dose is excreted unchanged in the urine within 24 hours, and less than 2% is excreted in the feces within 5 days. 0.26 L/kg This study investigated the absorption and excretion of iodixanol (320 mg I/ml) in rats, who were administered 2.5 g I/kg body weight via intragastric gavage. Animals were observed for up to 96 hours post-administration, and blood, urine, and fecal samples were collected at multiple time points throughout the experiment. Serum and urine iodixanol concentrations were determined using reversed-phase high-performance liquid chromatography (RP-HPLC). Fecal iodixanol concentrations were determined using X-ray fluorescence spectrometry based on iodine measurements. A series of X-ray films were taken, and selected tissues were examined histopathologically. The results showed that less than 1% of the intragastric-injected iodixanol dose was absorbed into the bloodstream from the intestines. No adverse clinical symptoms or treatment-related histomorphological changes were observed. In 40 healthy young male volunteers, a single intravenous injection of iodixanol at doses ranging from 0.3 to 1.2 gI/kg body weight resulted in a renal clearance of 110 mL/min (±14), equivalent to a glomerular filtration rate (GFR) of 108 mL/min. These values were independent of the administered dose. In a study of 16 adult patients scheduled for kidney transplantation, the clearance of iodixanol at 320 mgI/mL was investigated. The patients' baseline mean creatinine level was 6.3 mg/dL (±1.5), and the mean creatinine clearance was 13.61 mL/min (±4.67). Iodixanol levels were detected 5 days post-administration in these patients. The time to renal contrast enhancement increased from 6 hours to at least 24 hours. Plasma and urinary levels indicate that iodixanol is primarily cleared from the kidneys. In adults, approximately 97% of the injected dose of iodixanol is excreted unchanged in the urine within 24 hours, and less than 2% is excreted in the feces within 5 days after injection. For more complete data on the absorption, distribution, and excretion of iodixanol (14 types), please visit the HSDB record page. Metabolites/Metabolites Excreted unchanged: No iodixanol metabolites have been identified. Biological half-life: 2.1 hours. In patients with significantly impaired renal function (mean creatinine clearance 9.91 ± 3.58 mL/min), the plasma half-life was prolonged to 23 hours. Forty pediatric patients ≤12 years of age with age-appropriate renal function received multiple intra-arterial injections of iodixanol at doses ranging from 0.32 to 3.2 gI/kg body weight. The elimination half-lives for these patients were: 0.185 hours⁻¹ (newborns to 2 months), 0.256 hours⁻¹ (2 to <6 months), 0.299 hours⁻¹ (6 months to <1 year), 0.322 hours⁻¹ (1 to <2 years), and 0.307 hours⁻¹ (2 to ≤12 years). The mean terminal elimination rate constant for adults was 0.336 hr⁻¹. …
In 40 healthy young male volunteers, the elimination half-life after a single intravenous injection of iodixanol (dose ranging from 0.3 to 1.2 gI/kg body weight) was 2.1 hours (± 0.1 hours). …
Iodixanol is primarily excreted rapidly via the kidneys, with plasma half-lives of 25 minutes and 76 minutes in rats and monkeys, respectively. ...
In a study of 16 adult patients scheduled for kidney transplantation, the elimination of 320 mgI/mL iodixanol was investigated. ...In these patients, the plasma half-life was prolonged to 23 hours (normal t₁/₂ = 2 hours). ...

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Very little iodinated contrast agents administered intravenously are excreted into breast milk, 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. A report on extremely low levels of iodixanol in breast milk supports this generalization. Guidelines developed by multiple professional organizations state that breastfeeding mothers do not need to interrupt breastfeeding after receiving iodinated contrast agents. ◉ 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.

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Protein Binding
Negative

[1]. Iodixanol.

Iodixanol is a dimer, nonionic, water-soluble radiocontrast agent, particularly used for coronary angiography. It is a radiopaque contrast agent. Iodixanol is a nonionic hydrophilic compound commonly used in coronary angiography, especially suitable for patients with renal insufficiency, as it has less nephrotoxicity compared to most other intravascular contrast agents. Iodixanol is a radiocontrast agent. Its mechanism of action is as an X-ray contrast agent. Iodixanol is a dimer, isotonic, nonionic, hydrophilic iodinated radiocontrast agent used for diagnostic imaging. After intravascular administration, during computed tomography (CT) imaging, iodixanol blocks X-rays, appearing radiopaque on the X-ray image. This allows the visualization of iodine-absorbing human structures. The degree of visualization produced by iodixanol is proportional to the total amount of iodinated contrast agent in the X-ray path. The visualization of human structures depends on the distribution and clearance of iodixanol. Iodixanol appears to have lower nephrotoxicity compared to other iodinated contrast agents.
Drug Indications

Iodixanol is a contrast agent used in coronary angiography.
FDA Label

Mechanism of Action

Organic iodine compounds attenuate X-rays as they pass through the human body, thus creating a clear contrast between iodine-containing and non-iodine-containing structures. The degree of contrast enhancement produced by these compounds is proportional to the total amount (concentration and volume) of the iodinated contrast agent in the X-ray path. Intravascular injection of iodixanol opaques internal structures flowing through its path, allowing for radiographic visualization until significant blood dilution and clearance occur.
Intravascular injection of iodixanol opaques the blood vessels through which the contrast agent flows, allowing for radiographic visualization of internal structures until significant blood dilution and clearance occur.

C35H44I6N6O15

1550.18

1549.713

C, 27.12; H, 2.86; I, 49.12; N, 5.42; O, 15.48

92339-11-2

3724

White to off-white solid powder

2.3±0.1 g/cm3

1250.9±65.0 °C at 760 mmHg

262-267ºC (dec.)

710.3±34.3 °C

0.0±0.3 mmHg at 25°C

1.752

-5.88

13

15

22

62

1330

0

NBQNWMBBSKPBAY-UHFFFAOYSA-N

InChI=1S/C35H44I6N6O15/c1-13(52)46(30-26(38)20(32(59)42-3-15(54)9-48)24(36)21(27(30)39)33(60)43-4-16(55)10-49)7-19(58)8-47(14(2)53)31-28(40)22(34(61)44-5-17(56)11-50)25(37)23(29(31)41)35(62)45-6-18(57)12-51/h15-19,48-51,54-58H,3-12H2,1-2H3,(H,42,59)(H,43,60)(H,44,61)(H,45,62)

5-[acetyl-[3-[N-acetyl-3,5-bis(2,3-dihydroxypropylcarbamoyl)-2,4,6-triiodoanilino]-2-hydroxypropyl]amino]-1-N,3-N-bis(2,3-dihydroxypropyl)-2,4,6-triiodobenzene-1,3-dicarboxamide

Visipaque; Indixanol; Iodixanolum; Visipaque 270; Visipaque 320; OptiPrep;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

H2O : ~602.41 mg/mL (~388.61 mM)
DMSO : ~125 mg/mL (~80.64 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (1.34 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 20.8 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: ≥ 2.08 mg/mL (1.34 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 20.8 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: ≥ 2.08 mg/mL (1.34 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 20.8 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.)