Principles of Drug Metabolism
Published Online: 15 APR 2010
Copyright © 2003 by John Wiley & Sons, Inc. All rights reserved.
Burger's Medicinal Chemistry and Drug Discovery
How to Cite
Testa, B. 2010. Principles of Drug Metabolism. Burger's Medicinal Chemistry and Drug Discovery. 403–454.
- Published Online: 15 APR 2010
The focus of this chapter is essentially on drug metabolism reactions and their enzymes. Connected information of significance to medicinal chemists is also given attention. Introductory principles of drug metabolism are presented in the introduction. Oxidoreductases are discussed in the next section together with a systematic and extensive treatment of the chemical groups they target and the functionalization reactions they catalyze. Attention is paid to the cytochromes P450, their multiplicity, specificities and relative importance. Hydrolases are also treated. The next section is dedicated to the transferases and the conjugation reactions they catalyze, for example, glucuronidation and glutathione conjugation. The last section, which is particularly close to the interests of medicinal chemists, discusses pharmacological and toxicological consequences of metabolism, structure-metabolism relationships and the prediction of metabolism, and briefly outlines the biological factors that influence biotransformation.
- conjugation reactions;
- cytochromes P450;
- functionalization reactions;
- interindividual factors;
- intraindividual factors;
- pharmacological consequences;
- prediction of metabolism;
- toxicological consequences;
- toxophoric groups;
- structure–metabolism relationships