Radiological contrast composition and methods

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – Molecular bilayer structure

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A61K 4904

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active

044552920

ABSTRACT:
A radiological contrast composition for cerebrospinal myelography combining an iodo-benzamido-glucopyranose contrast agent and glucose, the glucose being in sufficient quantity to effectively compete in vivo with the contrast agent for brain hexokinase. Intrathecal coadministration of glucose with iodo-benzamido-glucopyranose contrast agents, exemplified by metrizamide, minimizes the central nervous system depression and irritation often associated with the intrathecal injection of the contrast agent alone. Metrizamide and related iodo-benzamido-glucopyranose contrast agents have been shown to interfere with brain glucose metabolism by competitive inhibition of the enzyme hexokinase. The competitive inhibition of hexokinase activity is counteracted by coadministration of a sufficient amount of glucose.

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patent: 4192859 (1980-03-01), Mackaness
Package insert for Amipaque brand of metrizamide marketed by Winthrop Laboratories.
Bertoni, John et al., Abstract 61 "Metrizamide Competitively Inhibits Hexokinase", poster presentation Sep. 9, 1980.
Bertoni et al., Abstract 9, "Metrizamide Competitively Inhibits Brain Hexokinase", delivered as a speech Apr. 30, 1981.
Bertoni et al., "Metrizamide Competitively Inhibits Hexokinase", reprinted from Transactions of the American Neurological Association, vol. 105, 1980.
Bertoni et al., "Studies on the Mechanism of Toxicity of Metrizamide", Biochemical Pharmacology, 30:1135-1138, (1981).
Bertoni et al., "Asterixis and Encephalopathy Following Metrizamide Myelography", Annals of Neurology 9:366-370 (Apr. 1981).

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