Iopamidol

Chemical formula: C₁₇H₂₂I₃N₃O₈  Molecular mass: 777.085 g/mol  PubChem compound: 65492

Pharmacodynamic properties

Iopamidol is contrast medium belonging to the new generation of non-ionic compound whose solubility is due to the presence of hydrophilic substitutes in the molecule. This results in a solution of low osmollity when compared with ionic media.

Iopamidol has been shown to be effective as an X-ray contrast medium in neuroradiology, angiography, venography, arthrography, urography, cerebral angiography and left ventriculography and coronary arteriography. Its toxicity particularly cardiac and CNS toxicity are less than those of ionic contrast media.

Pharmacokinetic properties

Serum iopamidol concentration curves conform to an open two compartment pharmacokinetic model with first order elimination. Iopamidol is very poorly absorbed (about 1-2%) after oral or rectal administration.

Distribution volume is equivalent to extracellular fluid.

Following parenteral administration elimination is almost completely through the kidneys. Less than 1% of the administered dose has been recovered in the faeces up to seventy two hours after dosing. Renal elimination is rapid and up to half the administered dose may be recovered in the urine within the first two hours of dosing.

There is no evidence of biotransformation.

Serum protein binding is negligible.

Preclinical safety data

Intra-ventricular / Intra-arterial / Intra-venous / Intra-articular / Intra-thecal / Intra-cisternal

No adverse effects can be predicted from animal toxicology studies other than those documented from human use of iopamidol.

Oral / Rectal administration

In animals, iopamidol was well tolerated after repeated oral administration. After 4 weeks adminstration of iopamidol equivalent to 9 gI/kg day, i.e. about 20 times higher than the recommended clinical dose, no severe symptoms of sub-acute intoxication were observed in rats. Following intraperitoneal injection of iopamidol in rats, iopamidol was rapidly cleared and almost totally eliminated by the renal route within the first 24 hours.

The intraperitoneal acute toxicity was relatively low. Necroscopic examination revealed no irritant effects on the peritoneal membrane. Iopamidol also showed good local tolerability after both local intratracheal installation and systemic administration . It therefore offers a good margin of safety for examination in which there is the risk of an accidental inspiration of the diagnostic medium.

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