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Encyclopedia of Drug Metabolism and Interactions

Encyclopedia of Drug Metabolism and Interactions

Alexander V. Lyubimov (Editor)

ISBN: 978-0-470-45015-4

Nov 2012

4784 pages

Select type: Hardcover

In Stock



“This one-stop reference brings together information scattered throughout the literature, and it involved the efforts of 270 expert authors from 16 countries — a global endeavor accomplished under the leadership of editor Alexander Lyubimov.” –Book News Inc., February 2013

The Encyclopedia of Drug Metabolism and Interactions provides essential support during all phases of drug development, from drug design to drug action and interaction in patients.

This multivolume work covers both preclinical and clinical aspects of drug metabolism and interactions. It also provides a wealth of toxicological, regulatory, and marketing information, all written by leading international experts in the field. Using this reference you’ll discover:

• Enzymes that can be inhibited or induced and their impact on drug toxicity and altered response in both animal and human models
• Effect of genetic differences and non-genetic factors on drug metabolism
• Balance among drug metabolism, its inactivation/activation, and its potential toxicity
• Examples demonstrating all aspects of drug metabolism and interactions in silico, in laboratory animals, and in humans
• Methods and detailed protocols enabling you to perform seamless studies of metabolism and drug interactions

This reference is essential for researchers interested in all aspects of drug development, and chemists, pharmacologists, pharmaceutical specialists, toxicologists, molecular toxicologists, and clinicians, including practitioners and physicians.

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Part 1: Basics Overview of Drug Metabolism

Chapter 1 Review of Drug Metabolism in Drug Discovery and Development

Chapter 2 Reactions and Models of Drug Metabolism

Chapter 3 Enzyme kinetics of drug metabolism reactions and drug-drug interactions

Chapter 4 Developmental changes in drug metabolizing enzymes

Chapter 5 Species differences in drug metabolizing enzymes

Part II: Enzyme systems involved in drug metabolism and interactions in animals and humans

Chapter 6 Structure and function of cytochrome P450 enzymes

Chapter 7 Mechanism of cytochrome P450 mediated reactions

Chapter 8 Transcriptional regulation of cytochrome P450 enzymes

Chapter 9 Cytochrome P450 polymorphisms

Chapter 10 Flavin monooxygenase

Chapter 11 Molybdenum containing enzymes

Chapter 12 Amine odidases and reductases

Chapter 13 Epoxide hydrolase

Chapter 14 Esterases and amidases

Chapter 15 UDP- glucuronosyltransferases

Chapter 16 Sulfotransferases

Chapter 17 Glutathione S- transferases

Chapter 18 Amino acid conjugation


Part III: General principals of ADME. Drug transporters and other mechanisms of transport

Chapter 1 Introduction to ADME. Overview

Chapter 2 Anatomical and Physiological Parameters that Influence Gastrointestinal Absorption

Chapter 3 Absorption of drugs into the body

Chapter 4 General principles of drug distribution

Chapter 5 ABC drug transporters and their impact on drug disposition/drug sensitivity and resistance

Chapter 6 SLC family transporters

Chapter 7 General principles of drug metabolism

Chapter 8 Systems where drug metabolism occurs

Chapter 9 Mass balance studies in animals and humans

Chapter 10 Bioavailability and bioequivalence

Chapter 11 Allometric scaling

Chapter 12 Effect of protein binding in ADME

Chapter 13 Excretion systems

Chapter 14 Pharmacokinetics (PK) and toxicokinetics (TK)

Chapter 15 Experimental design/mathematical models and data analysis/interpretation for PK /TK studies

Chapter 16 Physiologically-Based Pharmacokinetic Modeling

Chapter 17 Pharmacodynamics

Chapter 18 Interrelationships between Pharmacokinetics / Pharmacodynamics and metabolism

Part IV: ADME of some specific groups of drugs and delivery systems

Chapter 19 ADME of herbal and dietary constituents

Chapter 20 ADME of anticancer drugs

Chapter 21 ADME of cardiovascular drugs

Chapter 22 ADME of biological drugs

Chapter 23 ADME of natural toxins

Chapter 24 Metabolism and drug-drug interactions in pregnant mother/placenta/fetus


Part V: Drug Design and development

Chapter 1 Where and when does drug metabolism enter as a concern?

Chapter 2 Challenges in frontloading toxicity testing of anti- cancer drugs in drug discovery

Chapter 3 Role of ADME for selection of new drug candidates

Chapter 4 Efficient drug development. How to speed up the development process

Chapter 5 Metabolite profiling and identification

Chapter 6 Bioactivation and oxidative stress

Chapter 7 Metabolism in drug safety evaluation

Part VI: Methods and protocols for prediction and evaluation of drug metabolism and drug interaction studies

Chapter 8 In silico models of drug metabolism and drug interactions

Chapter 9 Methods for determination of enzyme kinetics and metabolic rates

Chapter 10 Assays and microarrays for metabolic pathways

Chapter 11 Applications using Caco-2 cells and TC7 cells for drug metabolism studies

Chapter 12 In vitro liver systems to study induction/inhibition. Prediction of in vivo metabolism and drug-drug interactions

Chapter 13 Assessing the Hepatic Disposition and Toxicity of Xenobiotics Using Primary Hepatocytes

Chapter 14 Monoclonal Antibody Based Analyses of Human Drug Metabolism and Multifuctional Cytochromes P450

Chapter 15 Validation of precision- cut slices as a tool to study induction of drug metabolism

Chapter 16 Practical aspects of high throughput solubility and dissolution assessment in preformulation

Chapter 17 Integrated Approaches to Blood Brain Barrier and its role for drug metabolism and interactions

Chapter 18 In vivo models (not genetically modified)

Chapter 19 Using mouse knockout and transgenic models to study metabolism


Part VII: Pharmacology and toxicology

Chapter 1 Introduction. Overview. Role of metabolism in drug toxicity

Chapter 2 Bioactivation I: Phase I (P450)

Chapter 3 Bioactivation II: Phase I (non P450)

Chapter 4 Bioactivation III: Phase II

Chapter 5 Covalent Binding

Chapter 6 MIST

Chapter 7 Cell- based predictors for Toxicities of Metabolites

Chapter 8 Toxicogenomics

Chapter 9 Metabonomics

Chapter 10 Proteomics

Chapter 11 Stereoselectivity in drug metabolism

PART VIII: Influence of physiological conditions, diseases, drug- food interactions, age, sex, and other factors on drug metabolism and effect

Chapter 12 Genetic influence on metabolism

Chapter 13 Drug- Drug interactions 1: Inhibition

Chapter 14 Drug- Drug Interactions 2: Induction

Chapter 15 Ontogeny and Metabolism

Chapter 16 Natural Modulators of Human Drug Metabolism: Dietary supplements and their Clinical Relevance (Food Effects on Toxicity and Pharmacology)

Chapter 17 Idiosyncratic drug interactions

Chapter 18 Influence of inflammatory stress on drug (or xenobiotic) hepatotoxicity

Chapter 19 Regulation of Drug-Metabolizingnzymes and Transporters in Infection, Inflammation, and Cancer


Part IX: Bioanalytical methods of studying metabolism

Chapter 1 Introduction. Importance of in vivo/in vitro analytical results in drug development Walter

Chapter 2 General principles of mass spectrometry: LC-MS, LC-MS/MS, and GC-MS

Chapter 3 Electrospray and Infusion nanospray ionization

Chapter 4 Emerging Atmospheric pressure ionization

Chapter 5 Matrix assisted laser desorption ionization (MALDI)

Chapter 6 Ion trap and quadrupole MS

Chapter 7 Hybrid LTQ- FTMS for Drug Metabolism Applications

Chapter 8 Mass Spectrometry Imaging (MSI)

Chapter 9 Ion Mobility Spectrometry and High Performance Tandem MS for metabolism studies and identification

Chapter 10 Inductively coupled plasma mass spectrometry (ICP MS) for element- containing drug metabolism analysis

Chapter 11 Online Electrochemical LC- MS Techniques for Profiling

Chapter 12 NMR

Chapter 13 Whole body autography and radioactive and non- radioactive isotope assays

Chapter 14 Ligand binding assays (immunoassays)

Chapter 16 Direct plasma analysis systems

Chapter 17 Analytical method development and validation in accordance to the regulatory guidelines

Chapter 18 Leveraging advances in HPLC to maximize DMPK data quality

Chapter 19 Methodologies to Increase Analytical Throughput

Chapter 20 Biomarkers to enable PK/PD

Chapter 21 Bioanalytics for Human Microdosing

Chapter 22 Bioactivation and Reactive Metabolite Assays

Chapter 23 Plasma protein binding


Part X: Clinical aspects of drug metabolism and interactions

Chapter 1 Overview and introduction. Role of drug metabolism and drug interactions in humans

Chapter 2 Human cytochrome P450 enzymes

Chapter 3 DDI Risk Assessment and Evaluation in Clinical Development: Interfacing Drug Metabolism and Clinical Pharmacology

Chapter 4 Current and future tools for predicting clinical drug interactions

Chapter 5 Predicting human biotransformation pathways

Chapter 6 Conjugation, transport, and elimination of drugs in humans

Chapter 7 Role and clinical consequences of human UDP- Glucuronosyltransferases

Chapter 8 Drug/food and drug/herb interactions

Chapter 9 Effects of disease on metabolism of drugs in humans

Chapter 10 Role of Phase I metabolism in drug activation and clinical treatment outcomes

Chapter 11 Role of metabolism in toxicity of drugs in humans

Chapter 12 Idiosyncratic drug reactions and the potential role of metabolism

Part XI Metabolism of specific drug groups and patient populations

Chapter 13 Metabolism of psychotropic drugs

Chapter 14 Metabolic-based consequences of polytherapy with AED

Chapter 15 Oral chemotherapeutic agents: Understanding mechanisms of action and drug interactions

Chapter 16 Drug metabolism and interactions in pediatric patients

Chapter 17 Population- based pharmacokinetic modeling and simulation

Chapter 18 Clinical Pharmacology in drug labeling. The impact of drug metabolism and clinical pharmacology on recommended dose of drugs

“This one-stop reference brings together information scattered throughout the literature, and it involved the efforts of 270 expert authors from 16 countries — a global endeavor accomplished under the leadership of editor Alexander Lyubimov (pharmacology, The U. of Illinois, Chicago).”  (Book News, 1 February 2013)

"Summing Up: Recommended.  Graduate students through professionals/practitioners.”   (Choice, 1 March 2013)