Absorption, Distribution and Excretion
To characterize the saturation kinetics of iodipamide, timed samples of blood, urine, and bile were taken from two unanesthetized dogs infused with iodipamide at increasing rates to achieve various steady state blood concentrations. Biliary excretion rate of iodipamide reached an asymptote with increasing blood concentration, indicating a biliary transport maximum (Tm) of 15.2 to 16.2 mgI/min. Urinary excretion was not a pure, first order process and urinary excretion rate was higher than the glomerular filtration rate corrected for plasma protein binding, suggesting that active tubular secretion may play a part. Extrarenal elimination followed Michaelis-Menten kinetics. Estimates of maximum rate (Vm) and Michaelis-Menten constant (Km) were obtained graphically. The estimated values of Vm were 4 to 6 times that of biliary Tm. In acute infusion experiments the iodipamide excreted in the bile and urine and that remaining in the organs analyzed accounted for only a fraction of the dose administered; no significant accumulation of iodipamide was found in the liver.
The contrast agent for biliary tract visualization, iodipamide, is strongly bound to serum albumin. The relationship between the affinity of the contrast agent for albumin and its preferential uptake and excretion by the liver has been unclear. The role of serum albumin on hepatic uptake and excretion of iodipamide therefore was investigated on the isolated perfused rabbit liver. With the perfusate containing fully reconstituted rabbit plasma protein or 3.5 g/100 mL rabbit albumin alone, the iodipamide excretion is initially extremely slow. It then increases gradually to about 6 mug/gm liver per min by 60 minutes and thereafter remains constant. The half-time of transfer to the bile is about 130 min. Without albumin in the perfusate the initial clearance rate of iodipamide is rapid, with half-time transfer to the bile of about 40 min. Rabbit serum globulins have no effect on iodipamide excretion. Thus, binding of iodipamide to albumin retards the transfer of iodipamide from plasma to the bile, probably due to competition between albumin and the anion binding protein of the liver.
The contrast medium is eliminated in the feces without passing through the enterohepatic circulation, except for approximately 10 percent of the intravenously administered dose which is excreted through the kidneys.

---

Metabolism / Metabolites
Hepatic.

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 iodipamide 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.

[1]. NCIt.

Adipiodone is an organoiodine compound that is 3-amino-2,4,6-triiodobenzoic acid in which one of the amino hydrogens is substituted by a 6-(3-carboxy-2,4,6-triiodoanilino)-6-oxohexanoyl group. It is a water-soluble radiographic contrast media for cholecystography and intravenous cholangiography. It has a role as a radioopaque medium. It is an organoiodine compound, a member of benzoic acids and a secondary carboxamide. It is a conjugate acid of an adipiodone(2-).
Iodipamide is a water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.
Iodipamide is a Radiographic Contrast Agent. The mechanism of action of iodipamide is as a X-Ray Contrast Activity.
Iodipamide Meglumine is the meglumine salt form of iodipamide, a tri-iodinated benzoate derivative and an ionic dimeric contrast agent used in diagnostic imaging. When administered in vivo, iodipamide is removed from the liver and secreted into the biliary tract. Like other organic iodine compounds, this agent blocks x-ray and appears opaque on x-ray film; thereby it enhances the visibility of the bile ducts and gallbladder during cholangiography and cholecystography procedures.
Iodipamide is a tri-iodinated benzoate derivative and ionic dimeric contrast agent used in diagnostic imaging. When administered in vivo, iodipamide is removed from the liver and secreted into the biliary tract. Like other organic iodine compounds, this agent blocks x-rays and appears opaque on x-ray film; thereby it enhances the visibility of the bile ducts and gallbladder during cholangiography and cholecystography procedures.
A water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.
See also: Iodipamide Meglumine (annotation moved to).

---

Drug Indication
Iodipamide 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 body, thereby allowing body structures containing iodine to be delineated in contrast to those structures that do not contain iodine. The degree of opacity produced by these iodinated organic compounds is directly proportional to the total amount (concentration and volume) of the iodinated contrast agent in the path of the x-rays. Iodipamide's primary excretion through the hepato-biliary system and concentration in bile allows visualization of the gallbladder and biliary ducts.
... The iodine in the contrast medium is responsible for the absorption of x-rays and the resulting opacification of the organ system or other area under investigation. ...

---

Therapeutic Uses
Contrast Media
Cholografin Meglumine is indicated for intravenous cholangiography and cholecystography as follows: (a) visualization of the gallbladder and biliary ducts in the differential diagnosis of acute abdominal conditions, (b) visualization of the biliary ducts, especially in patients with symptoms after cholecystectomy, and (c) visualization of the gallbladder in patients unable to take oral contrast media or to absorb contrast media from the gastrointestinal tract. /Included in US product label/
THERAPEUTIC CATEGORY: Diagnostic aid (radiopaque medium-cholecystographic)
THERAPEUTIC CATEGORY (VETERINARY): Diagnostic aid (radiopaque medium)

---

Drug Warnings
Iodipamide meglumine is contraindicated for use in intrathecal procedures.
Iodipamide meglumine is contraindicated in patients with a hypersensitivity to salts of iodipamide or who exhibit sensitivity reactions to the test dose. It is also contraindicated in patients with concomitant severe impairment of renal and liver function.
Serious adverse reactions have been reported due to the inadvertent intrathecal administration of iodinated contrast media that are not indicated for intrathecal use. These serious adverse reactions include: death, convulsions, cerebral hemorrhage, coma, paralysis, arachnoiditis, acute renal failure, cardiac arrest, seizures, rhabdomyolysis, hyperthermia, and brain edema. Special attention must be given to insure that this drug product is not inadvertently administered intrathecally.
The possibility exists for inadvertent administration into the intrathecal space during epidural administrations. Therefore, epidural administration procedures, such as pain management catheter placement, should not be performed with use of this product.
For more Drug Warnings (Complete) data for Iodipamide (15 total), please visit the HSDB record page.

---

Pharmacodynamics
Following intravenous administration of Cholografin Meglumine, iodipamide is carried to the liver where it is rapidly secreted. The contrast medium appears in the bile within 10 to 15 minutes after injection, thus permitting visualization of the hepatic and common bile ducts, even in cholecystectomized patients. The biliary ducts are readily visualized within about 25 minutes after administration, except in patients with impaired liver function. The gallbladder begins to fill within an hour after injection; maximum filling is reached after two to two and one-half hours. The contrast medium is finally eliminated in the feces without passing through the enterohepatic circulation, except for approximately 10 percent of the intravenously administered dose which is excreted through the kidneys.

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.)