Drug Metabolism

  • Alan TaleviEmail author
  • Carolina Leticia Bellera


Living systems have developed elimination mechanisms to dispose waste products and to protect themselves from exposure to potentially harmful chemical compounds. Protective strategies to limit such exposure include the existence of biological barriers with selective permeability, the chemical disposal of xenobiotics by chemical biotransformations, and the physical disposal of xenobiotics (or its biotransformation products) through excretion routes. This chapter discusses the enzymatic systems involved in drug metabolism and the strong integration of these systems with other elimination mechanisms.


Bioactivation Biotransformation Conjugation CYP3A4 CYP450 Cytochrome P450 Drug biotransformation Drug disposition Drug elimination Drug metabolism Efflux transporters Enzyme induction Enzyme inhibition Functionalization reactions Glucuronide Liver Metabolite Personalized medicine Phase I reactions Phase II reactions Precision medicine Stratified medicine Synthetic reactions 


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Further Reading

  1. Drug metabolism is a vast topic, and entire books have been written about it. Here, we intended to provide a summary of the more relevant points of drug biotransformation, but the chapter is far from exhaustive. For a much deeper insight on the topic, the reader is advised to Pearson and Wienkers’s Handbook of Drug Metabolism (currently in its 3rd edition by CRC Press); the Drug Metabolism Handbook edited by Nassar, Hollenberg, and Scatina (2008, Wiley & Sons); and the extensive and unbelievably comprehensive series of articles by Testa and Krämer, many of which have been included in the reference list of the present chapter.Google Scholar

Copyright information

© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.Laboratory of Bioactive Research and Development (LIDeB), Department of Biological Sciences, Faculty of Exact SciencesUniversity of La Plata (UNLP)La PlataArgentina
  2. 2.Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET)La PlataArgentina
  3. 3.Medicinal Chemistry/Laboratory of Bioactive Research and Development (LIDeB), Faculty of Exact SciencesUniversidad Nacional de La Plata (UNLP)La PlataArgentina
  4. 4.Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET)Buenos AiresArgentina

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