Abstract

Chapter 8 provides a broad understanding of drug metabolism, including how to detect and identify metabolic reactions. As described in this chapter, metabolic processes remove active drugs from the body by converting them, according to rational mechanisms of organic chemistry, to one or more metabolic products. These metabolites may be biologically inert or may possess biological properties similar to or different from those of the parent drug and may produce toxicological effects. The understanding of drug metabolism and its underlying mechanisms, as described in this chapter, provides a basis for the medicinal chemist to rationally design chemical modifications of a lead compound in an attempt to maximize drug effectiveness through prolonged plasma half life while minimizing potential side effects by reducing production of unfavorable metabolic products. The concept of hard and soft drugs is introduced.

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