Principles of Drug Metabolism

Xenobiotic metabolism, which includes drug metabolism, has become a major pharmacological science with particular relevance to biology, therapeutics and toxicology. Drug metabolism is also of great importance inmedicinal chemistry because it influences in qualitative, quantitative, and kinetic terms the deactivation, activation, detoxification, and toxification of the vast majority of drugs. As a result, medicinal chemists engaged in drug discovery and development should be able to integrate metabolic considerations into drug design. To do so, however, requires a fair or even good knowledge of xenobiotic metabolism. This chapter, which is written by a medicinal chemist for medicinal chemists, aims at offering knowledge and understanding rather than encyclopedic information. Readerswanting to go further in the study of xenobiotic metabolism may consult various classical or recent books [1–15], broad reviews, and book chapters [16–27].