Zomepirac and nevirapine: Bioactivation involving the sulfation pathway.
Published: 2007
Language: eng
Number of pages: 78
ISBN-13: 9780494273890
Description: Idiosyncratic drug reactions (IDRs), although rare, can be life-threatening. The patho-mechanisms of IDRs are unclear; however, reactive metabolites of drugs and the immune system are thought to be involved. For carboxylate drugs, their acyl glucuronide metabolites have been implicated as the mediators of the adverse effects; however, a direct link has yet to be established. For the carboxylate drug zomepirac (ZP), this study aimed to explore the sulfation pathway involving the conversion of the metabolite hydroxy-ZP to ZP 4-methylsulfate. The role of ZP 4-methylsulfate as a reactive metabolite was unclear, as it was not isolated and characterized, either synthetically or enzymatically. For the drug nevirapine (NVP), it was proposed that its metabolite 12-hydroxy-NVP is converted to NVP 12-sulfate, which could form a reactive iminoquinone. This project is still in progress, but with the help of the animal model, the role of the 12-hydroxy-NVP should be elucidated more clearly.
Notes: Source: Masters Abstracts International, Volume: 45-06, page: 3143.

Thesis (M.Sc.)--University of Toronto, 2007.

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