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Hepatic binding and michaelis-menten metabolism of drugs

✍ Scribed by Gerald M. Rubin; Thomas N. Tozer

Publisher
John Wiley and Sons
Year
1986
Tongue
English
Weight
379 KB
Volume
75
Category
Article
ISSN
0022-3549

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✦ Synopsis

Certain drugs with metabolism that obeys Michaelis-Menten kinetics are extensively bound in the liver. During the initial distribution phase after a single dose, the binding sites act as a "sink' and compete with the metabolizing enzymes for the drug. After this phase is completed, the bound sites act as a source of drug for the enzymes. Computer simulations of a perfused liver system, with wellstirred reservoir and hepatic compartments, were performed to assess whether or not such bindlng, as measured by the partition coefficient (6) between the liver and the emergent venous blood, affects the tendency to saturate metabolism. Metabolism was assumed to follow Michaelis-Menten kinetics and only unbound drug was assumed to

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