Biotransformation and Bioactivation

Abstract

The terms metabolism and biotransformation are used interchangeably in this book. As described in Chap. 2, metabolism is a major route of elimination of drugs from the body and, in general, results in the formation of metabolites that are more polar than the parent drug. Here, we discuss techniques for detection of metabolites, bioactivation and its ramifications, metabolites in drug safety studies, and what transformation happens to different common moieties in drugs as a result of metabolism.

Contents

6.1 List of Abbreviations 97

6.2 Overview of Biotransformation 98

6.3 Metabolite Detection and Identification 98

6.4 Metabolite Testing in Safety (MIST) Considerations 102

6.5 Overview of Bioactivation 107

6.6 Biotransformation/Bioactivation of Moieties 113

References 124

Additional Reading 125

6.1 LIST OF ABBREVIATIONS

DME

Drug metabolizing enzyme

DBE

Double bond equivalent

GSH

Glutathione

GST

Glutathione S-transferase

H/D

Hydrogen/deuterium

HAT

Hydrogen atom transfer

ICH

International Conference on Harmonisation

LC

Liquid chromatography

MIST

Metabolites in safety testing

MS

Mass spectroscopy

S.C. Khojasteh et al., Drug Metabolism and Pharmacokinetics 97

Quick Guide, DOI 10.1007/978-1-4419-5629-3_6, © Springer Science+Business Media, LLC 2011

S.C. Khojasteh et al., Drug Metabolism and Pharmacokinetics 97

Quick Guide, DOI 10.1007/978-1-4419-5629-3_6, © Springer Science+Business Media, LLC 2011

NADPH

Nicotinamide adenine dinucleotide phosphate

NAPQI

N-acetyl-p -quinoneimine

NMR

Nuclear magnetic resonance

P450

Cytochrome P450

PD

Pharmacodynamic

PK

Pharmacokinetic

SET

Single electron transfer

UV

Ultraviolet

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