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Main description:
Drug metabolism and transport are very important facets within the discipline of pharmaceutical sciences, with enzyme kinetic concepts utilized regularly in characterizing and modeling the disposition and elimination of drugs. Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications focuses on very practical aspects of applying kinetic principles to drug metabolizing enzymes and transporters. Divided into five convenient sections, topics include the fundamental principles of enzyme kinetics, the kinetics of oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for both drug metabolizing enzymes and transporters including novel systems biology approaches, understanding of variability both experimental and interindividual (pharmacogenomic), and case studies that provide real life examples of applying these principles. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics especially suitable for the novice, in some cases step-by-step, readily reproducible protocols, and insights to help with troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning.
Authoritative and easily accessible, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications serves as a very practical teaching tool for novice, non-mathematically trained scientists interested in these fundamental concepts and as an aid for their supervisors in teaching these principles.
Contents:
1. Enzyme Kinetics in Drug Metabolism - Fundamentals and Applications
Swati Nagar, Upendra A. Argikar, and Donald J. Tweedie
Part I. Fundamentals of Enzyme Kinetics
2. Fundaments of Enzyme Kinetics
Eleanore Seibert and Timothy S. Tracy
3. Different Enzyme Kinetic Models
Eleanore Seibert and Timothy S. Tracy
4. Reversible Mechanisms of Enzyme Inhibitors and Resulting Clinical Significance
Barbara Ring, Steven A. Wrighton, and Michael Mohutsky
5. Irreversible Enzyme Inhibition Kinetics and Drug-Drug Interactions
Michael Mohutsky and Stephen D. Hall
6. Multi-Enzyme Kinetics and Sequential Metabolism
Larry C. Wienkers and Brooke VandenBrink
7. Consideration of the Unbound Drug Concentration in Enzyme Kinetics
Nigel J. Waters, R. Scott Obach, and Li Di
Part II. Kinetics of Drug Metabolizing Enzymes and Transporters
8. Enzyme Kinetics of Oxidative Metabolism - Cytochromes P450
Ken Korzekwa
9. Enzyme Kinetics, Pharmacokinetics, Inhibition, and Regioselectivity of Aldehyde Oxidase
John T. Barr, Kanika Choughule, and Jeffrey P. Jones
10. Enzyme Kinetics of Conjugative Enzymes - PAPS
Margaret O. James
11. Enzyme Kinetics of Uridine Diphosphate Glucuronosyltransferases (UGTs)
Jin Zhou and John Miners
12. Principles and Experimental Considerations for in vitro Transporter Interaction Assays
Sid Bhoopathy, Chris Bode, Vatsala Naageshwaran, Erica A. Wiskercher, and Ismael J. Hidalgo
Part III. Modeling Considerations
13. Rationalising Under-Prediction of Drug Clearance from Enzyme and Transporter Kinetic Data - from in vitro Tools to Mechanistic Modeling
Aleksandra Galetin
14. The Structural Model for the Mass Action Kinetic Analysis of P-gp Mediated Transport Through Confluent Cell Monolayers
Joseph Bentz and Harma Ellens
15. Systems Biology Approaches to Enzyme Kinetics: Analyzing Network Models of Drug Metabolism
Nnena A. Finn and Melissa L. Kemp
Part IV. Variability in Kinetics
16. Variability in Human in vitro Enzyme Kinetics
Ying-Hong Wang and Christopher R. Gibson
17. Sources of Interindividual Variability
Yvonne Lin and Kenneth E. Thummel
Part V. Case Studies
18. Case Study 1. Practical Considerations with Experimental Design and Interpretation
John T. Barr, Darcy R. Flora, and Otito Iwuchukwu
19. Case Study 2. Practical Analytical Considerations for Conducting in vitro Enzyme Kinetic Studies
Upendra A. Argikar and Swati Nagar
20. Case Study 3. Application of Basic Enzyme Kinetics to Metabolism Studies - Real Life Examples
Yongmei Li, Michelle McCabe, Lalitha Podila, Timothy S. Tracy, and Donald J. Tweedie
21. Case Study 4. Predicting the Drug Interaction Potential for Inhibition of CYP2C8 by Montelukast
Ken Korzekwa
22. Case Study 5. Deconvoluting Hyperbilirubinemia: Differentiating Between Hepatotoxicity and Reversible Inhibition of UGT1A, MRP2 or OATP1B1 in Drug Development
Ian Templeton, Gary Eichenbaum, Rucha Sane, and Jin Zhou
23. Case Study 6. Drug Transporters: in vitro Solutions for Translatable Outcomes
Sid Bhoopathy, Chris Bode, Vatsala Naageshwaran, Erica A. Weiskircher, and Ismael J. Hidalgo
24. Case Study 7. Compiled Aha Moments in Enzyme Kinetics: Authors' Experiences
Donald J. Tweedie
PRODUCT DETAILS
Publisher: Springer (Humana Press Inc.)
Publication date: February, 2014
Pages: 520
Weight: 652g
Availability: Available
Subcategories: Pharmacology
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