Title: [26] Alteration of drug metabolism by the use of prodrugs
Abstract: This chapter focuses on the effects of prodrug structure on pathways of metabolism that involve the formation of highly reactive and sometimes toxic products. When a prodrug is developed from a compound with documented therapeutic and toxicological properties, the effects of prodrug structure on both of these properties should be investigated. Two basic requirements for such investigations are choosing an appropriate animal model and accurate methods for metabolite analysis. The structural modification to drug structure that is imparted by development of a prodrug needs to be assessed in regards to potential drug interactions. For example, the mutual prodrug benorylate (V) has the potential for drug interactions between its two-hydrolysis products, aspirin and acetaminophen, both pharmacokinetically and pharmacodynamically. Metabolite profiles of each in the presence of the other need to be compared with those generated by the prodrug. Subtle changes brought about by prodrug structure can markedly influence the metabolism of the prodrug itself, the products of its metabolism, and the metabolism of other drugs. Therefore, metabolism studies of prodrugs need to be carefully designed and performed.
Publication Year: 1985
Publication Date: 1985-01-01
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 2
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