Absorption, Distribution and Excretion
To characterize the saturation kinetics of iopamidol, we collected timed blood, urine, and bile samples from two conscious dogs. These dogs were infused with iopamidol at increasing rates to achieve different steady-state plasma concentrations. The bile excretion rate of iopamidol reached an asymptote with increasing plasma concentrations, indicating a bile transport maxima (Tm) of 15.2 to 16.2 mgI/min. Urinary excretion was not a purely first-order kinetic process, and the urinary excretion rate was higher than the glomerular filtration rate after adjusting for plasma protein binding, suggesting that active tubular secretion may play a role. Extrarenal elimination conformed to Michaelis kinetics. Estimates of the maximal excretion rate (Vm) and Michaelis constant (Km) were obtained graphically. The estimated Vm was 4 to 6 times the bile Tm. In acute infusion experiments, only a small fraction of the administered dose of iopamidone was excreted in bile and urine, and only a small fraction remained in the analyzed organs; no significant accumulation of iopamidone in the liver was observed. Iopamidone, a contrast agent used for biliary tract imaging, binds strongly to serum albumin. The relationship between the contrast agent's affinity for albumin and its preferential uptake and excretion in the liver remains unclear. Therefore, this study investigated the effect of serum albumin on the hepatic uptake and excretion of iopamidone in isolated perfused rabbit liver. When the perfusion fluid contained only fully reconstituted rabbit plasma protein or 3.5 g/100 mL rabbit albumin, the excretion of iopamidone was initially very slow. Subsequently, the excretion gradually increased, reaching approximately 6 μg/g liver/min at 60 minutes, and then remained stable. The half-life of iopamidone transported to bile was approximately 130 minutes. When the perfusion fluid did not contain albumin, the initial clearance of iopamidone was rapid, with a half-life of approximately 40 minutes transported to bile. Rabbit serum globulin has no effect on the excretion of iopamidrone. Therefore, the binding of iopamidrone to albumin delays its transport from plasma to bile, possibly due to competition between albumin and hepatic anion-binding proteins. Contrast agents are primarily excreted in feces, bypassing enterohepatic circulation; only about 10% of intravenously administered doses are excreted by the kidneys. Metabolism/Metabolites: Liver.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Very little iodine 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. Guidelines from multiple professional organizations indicate that breastfeeding mothers do not need to interrupt breastfeeding after receiving iodine-containing contrast agents. However, since there is currently no published experience regarding the use of iopamidol 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 Breastfeeding and Breast Milk
No published information found as of the revision date.

[1]. NCIt.

Adipiodone is an organic iodine compound with the chemical formula 3-amino-2,4,6-triiodobenzoic acid, in which one amino hydrogen atom is replaced by a 6-(3-carboxy-2,4,6-triiodoaniline)-6-oxohexanoyl group. It is a water-soluble radioactive contrast agent used for cholecystography and intravenous cholangiography. It is a radiopaque contrast agent. It is an organic iodine compound belonging to the benzoic acid class and also a secondary amide class. It is the conjugate acid of Adipiodone (2-). Iopamidrone is a water-soluble radioactive contrast agent used for cholecystography and intravenous cholangiography. Iopamidrone is a radioactive contrast agent. The mechanism of action of iopamidrone is as an X-ray contrast agent. Iopamidrone meglumine is the meglumine salt form of iopamidrone, a triiodobenzoic acid ester derivative, and also an ionic dimer contrast agent used for diagnostic imaging. After administration in vivo, iopamidrone is cleared from the liver and secreted into the bile ducts. Like other organic iodine compounds, this drug blocks X-rays, appearing opaque on X-ray films; therefore, it enhances the visualization of the bile ducts and gallbladder during cholangiography and cholecystography.
A water-soluble radiocontrast agent used for cholecystography and intravenous cholangiography.
See also: Iopamidol meglumine (note moved to).

---

Drug Indications
Iopamidol is used as a contrast agent for cholecystography and intravenous cholangiography.

---

Mechanism of Action
Organic iodine compounds block 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 visualization produced by these iodinated organic compounds is proportional to the total amount (concentration and volume) of the iodinated contrast agent in the X-ray path. Iopamilide is primarily excreted via the hepatobiliary system and concentrated in bile, thus allowing visualization of the gallbladder and bile ducts. ...Iodine in the contrast agent is responsible for absorbing X-rays, thereby visualizing the examined organ system or other areas. ...

---

Therapeutic Use
Contrast Agents
Iopamilide meglumine is indicated for the following intravenous cholangiography and cholecystography: (a) for the differential diagnosis of acute abdominal diseases, to visualize the gallbladder and bile ducts; (b) for cholangiography, especially in patients with symptoms after cholecystectomy; (c) for patients who cannot take contrast agents orally or absorb them from the gastrointestinal tract, to visualize the gallbladder. /US Product Label Contains/
Therapeutic Category: Diagnostic Aids (Radiosensitive Media - Cholecystography)
Therapeutic Category (Veterinary): Diagnostic Aids (Radiosensitive Media)

---

Drug Warnings
Iopamilide meglumine is contraindicated for intrathecal injection.
Iopamilide meglumine is contraindicated in patients with hypersensitivity to iopamilide salts or who have experienced a hypersensitivity reaction to the test dose. Contraindicated in patients with severe renal and hepatic impairment. Serious adverse reactions have been reported due to accidental intrathecal administration of iodinated contrast agents unsuitable for intrathecal injection. These serious adverse reactions include: death, seizures, cerebral hemorrhage, coma, paralysis, arachnoiditis, acute renal failure, cardiac arrest, seizures, rhabdomyolysis, hyperthermia, and cerebral edema. Special care must be taken to ensure that this product is not accidentally administered intrathecally. There is a possibility of accidental entry into the intrathecal space during epidural administration. Therefore, epidural procedures, such as pain management catheter placement, should not be performed while using this product. For more complete data on drug warnings for iopamidol (15 in total), please visit the HSDB record page. Pharmacodynamics: Following intravenous injection of cholelithoxine meglumine, iopamidol is transported to the liver and rapidly secreted. It becomes visible in bile within 10 to 15 minutes after injection, and the hepatic ducts and common bile duct can be observed even in patients who have undergone cholecystectomy. Except for patients with impaired liver function, the bile ducts become clearly visible approximately 25 minutes after injection. The gallbladder begins to fill within 1 hour after injection and reaches maximum filling volume after 2 to 2.5 hours. Except for approximately 10% of the intravenously injected dose, which is excreted through the kidneys, the remaining contrast agent does not undergo enterohepatic circulation and is ultimately excreted in the feces.

C20H14N2O6I6

1139.75896

1139.51

606-17-7

606-17-7;3521-84-4 (meglumine);2618-26-0 (Na+);

3739

White to off-white solid powder

2.8g/cm3

908.6ºC at 760 mmHg

306-308ºC (dec.)

503.3ºC

1.835

6.994

4

6

9

34

714

0

FFINMCNLQNTKLU-UHFFFAOYSA-N

InChI=1S/C20H14I6N2O6/c21-7-5-9(23)17(15(25)13(7)19(31)32)27-11(29)3-1-2-4-12(30)28-18-10(24)6-8(22)14(16(18)26)20(33)34/h5-6H,1-4H2,(H,27,29)(H,28,30)(H,31,32)(H,33,34)

3-[[6-(3-carboxy-2,4,6-triiodoanilino)-6-oxohexanoyl]amino]-2,4,6-triiodobenzoic acid

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)

DMSO : ~125 mg/mL (~109.67 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (1.82 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.

---

Solubility in Formulation 2: 2.08 mg/mL (1.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
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.

---

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (1.82 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.

---

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