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  • Trimethadione as a probe drug to estimate hepatic oxidizing capacity in humans.

Trimethadione as a probe drug to estimate hepatic oxidizing capacity in humans.

Comparative biochemistry and physiology. Part C, Pharmacology, toxicology & endocrinology (1996-11-01)
E Tanaka, A Ishikawa, M Abei, S Kobayashi
ABSTRACT

Trimethadione (TMO) has the properties required of probe drugs for the evaluation of hepatic drug-oxidizing capacity in humans in vivo. TMO is demethylated to dimethadione (DMO), its only metabolite, in the liver after oral administration. Involvement of two cytochrome P450's--CYP2C9 and 3A4--in TMO metabolism has been seen in humans, but involvement of 1A2 is not clearly established. In humans with various types of liver disease and hepatectomy, the serum DMO/TMO ratios, which were measured on blood samples obtained by a single collection 4 hr after oral administration of TMO, correlated well with the degree of hepatic damage. This finding suggests that TMO may be used as a probe drug in the rapid determination of the functional reserve mass of the liver as well as hepatic drug-oxidizing capacity in humans in vivo.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
5,5-Dimethyl-2,4-oxazolidinedione
Pricing and availability is not currently available.
Trimethadione, European Pharmacopoeia (EP) Reference Standard
Pricing and availability is not currently available.