Basic Pharmacokinetics and Pharmacodynamics - An Integrated Textbook and Computer Simulations

Informationen zum Autor Sara E. Rosenbaum, PhD, is Professor of Biomedical and Pharmaceutical Sciences at the University of Rhode Island, where she teaches courses in pharmacokinetics and pharmacodynamics. Her research interests concentrate on the development and application of pharmacokinetic and pharmacodynamic models to better understand the drug dose-response relationship. Klappentext Updated with new chapters and topics, this book provides a comprehensive description of all essential topics in contemporary pharmacokinetics and pharmacodynamics. It also features interactive computer simulations for students to experiment and observe PK/PD models in action. ¿    Presents the essentials of pharmacokinetics and pharmacodynamics in a clear and progressive manner ¿    Helps students better appreciate important concepts and gain a greater understanding of the mechanism of action of drugs by reinforcing practical applications in both the book and the computer modules ¿    Features interactive computer simulations, available online through a companion website at: https://web.uri.edu/pharmacy/research/rosenbaum/sims/ ¿    Adds new chapters on physiologically based pharmacokinetic models, predicting drug-drug interactions,  and pharmacogenetics while also strengthening original chapters to better prepare students for more advanced applications ¿    Reviews of the 1st edition: "This is an ideal textbook for those starting out ... and also for use as a reference book ...." (International Society for the Study of Xenobiotics) and "I could recommend Rosenbaum's book for pharmacology students because it is written from  a perspective of drug action . . . Overall, this is a well-written introduction to PK/PD .... "  (British Toxicology Society Newsletter) Zusammenfassung This book provides a comprehensive foundation for the contemporary application of pharmacokinetics and pharmacodynamics. The second edition updates and strengthens existing chapters and adds new topics to address current needs including physiologically based pharmacokinetic modeling, pharmacogenomics and predicting drug-drug interactions. Inhaltsverzeichnis Preface xix Contributors xxi 1 Introduction to Pharmacokinetics and Pharmacodynamics 1 Sara E. Rosenbaum 1.1 Introduction: Drugs and Doses 2 1.2 Introduction to Pharmacodynamics 3 1.2.1 Drug Effects at the Site of Action 3 1.2.2 Agonists, Antagonists, and Concentration-Response Relationships 6 1.3 Introduction to Pharmacokinetics 9 1.3.1 Plasma Concentration of Drugs 9 1.3.2 Processes in Pharmacokinetics 11 1.4 Dose-Response Relationships 12 1.5 Therapeutic Range 14 1.5.1 Determination of the Therapeutic Range 15 1.6 Summary 18 Reference 18 2 Passage of Drugs Through Membranes 19 Sara E. Rosenbaum 2.1 Introduction 20 2.2 Structure and Properties of Membranes 20 2.3 Passive Diffusion 21 2.3.1 Transcellular Passive Diffusion 23 2.3.2 Paracellular Passive Diffusion 25 2.4 Carrier-Mediated Processes: Transport Proteins 26 2.4.1 Uptake Transporters: SLC Superfamily 27 2.4.2 Efflux Transporters: ABC Superfamily 29 2.4.3 Characteristics of Transporter Systems 31 2.4.4 Simulation Exercise 32 2.4.5 Clinical Examples of Transporter Involvement in Drug Response 32 References 33 3 Drug Administration and Drug Absorption 35 Steven C. Sutton 3.1 Introduction: Local and Systemic Drug Administration 36 3.2 Routes of Drug Administration 37 3.2.1 Common Routes of Local Drug Administration 37 3.2.2 Common Routes of Systemic Drug Administration 38 3.3 Overview of Oral Absorption 41 3.3.1 Anatomy and Physiology of the Oral-Gastric-Intestinal Tract and Transit Time 41

List of contents

Preface xix
 
Contributors xxi
 
1 Introduction to Pharmacokinetics and Pharmacodynamics 1
Sara E. Rosenbaum
 
1.1 Introduction: Drugs and Doses, 2
 
1.2 Introduction to Pharmacodynamics, 3
 
1.3 Introduction to Pharmacokinetics, 9
 
1.4 Dose-Response Relationships, 12
 
1.5 Therapeutic Range, 14
 
1.6 Summary, 18
 
Reference, 18
 
2 Passage of Drugs Through Membranes 19
Sara E. Rosenbaum
 
2.1 Introduction, 20
 
2.2 Structure and Properties of Membranes, 20
 
2.3 Passive Diffusion, 21
 
2.4 Carrier-Mediated Processes: Transport Proteins, 26
 
References, 33
 
3 Drug Administration and Drug Absorption 35
Steven C. Sutton
 
3.1 Introduction: Local and Systemic Drug Administration, 36
 
3.2 Routes of Drug Administration, 37
 
3.3 Overview of Oral Absorption, 41
 
3.4 Extent of Drug Absorption, 44
 
3.5 Determinants of the Fraction of the Dose Absorbed (F), 46
 
3.6 Factors Controlling the Rate of Drug Absorption, 61
 
3.7 Biopharmaceutics Classification System, 64
 
3.8 Food Effects, 65
 
Problems, 66
 
References, 67
 
4 Drug Distribution 71
Sara E. Rosenbaum
 
4.1 Introduction, 72
 
4.2 Extent of Drug Distribution, 72
 
4.3 Rate of Drug Distribution, 89
 
4.4 Distribution of Drugs to the Central Nervous System, 93
 
Problems, 96
 
References, 98
 
5 Drug Elimination and Clearance 99
Sara E. Rosenbaum
 
5.1 Introduction, 100
 
5.2 Clearance, 102
 
5.3 Renal Clearance, 108
 
5.4 Hepatic Elimination and Clearance, 119
 
Problems, 139
 
References, 142
 
6 Compartmental Models in Pharmacokinetics 145
Sara E. Rosenbaum
 
6.1 Introduction, 146
 
6.2 Expressions for Component Parts of the Dose-Plasma Concentration Relationship, 146
 
6.3 Putting Everything Together: Compartments and Models, 149
 
6.4 Examples of Complete Compartment Models, 152
 
6.5 Use of Compartmental Models to Study Metabolite Pharmacokinetics, 155
 
6.6 Selecting and Applying Models, 156
 
Problems, 157
 
Suggested Readings, 157
 
7 Pharmacokinetics of an Intravenous Bolus Injection in a One-Compartment Model 159
Sara E. Rosenbaum
 
7.1 Introduction, 160
 
7.2 One-Compartment Model, 160
 
7.3 Pharmacokinetic Equations, 162
 
7.4 Simulation Exercise, 163
 
7.5 Application of the Model, 165
 
7.6 Determination of Pharmacokinetic Parameters Experimentally, 168
 
7.7 Pharmacokinetic Analysis in Clinical Practice, 173
 
Problems, 174
 
Suggested Reading, 176
 
8 Pharmacokinetics of an Intravenous Bolus Injection in a Two-Compartment Model 177
Sara E. Rosenbaum
 
8.1 Introduction, 178
 
8.2 Tissue and Compartmental Distribution of a Drug, 179
 
8.3 Basic Equation, 181
 
8.4 Relationship Between Macro and Micro Rate Constants, 183
 
8.5 Primary Pharmacokinetic Parameters, 183
 
8.6 Simulation Exercise, 188
 
8.7 Determination of the Pharmacokinetic Parameters of the Two-Compartment Model, 191
 
8.8 Clinical Application of the Two-Compartment Model, 194
 
Problems, 197
 
Suggested Readings, 199
 
9 Pharmacokinetics of Extravascular Drug Administration 201
Dr. Steven C. Sutton
 
9.1 Introduction, 202
 
9.2 First-Order Absorption in a One-Compartment Model, 203
 
9.3 Modified Release and Gastric Retention Formulations, 214
 
9.4 Bioavai

Product details

• Authors: Sara E Rosenbaum, Sara E. Rosenbaum, Sara E. (University of Rhode Island) Rosenbaum, Se Rosenbaum
• Assisted by: Sar E Rosenbaum (Editor), Sara E Rosenbaum (Editor), Sara E. Rosenbaum (Editor), Rosenbaum Sara E. (Editor)
• Publisher: Wiley, John and Sons Ltd
• Languages: English
• Product format: Paperback / Softback
• Released: 17.01.2017
• EAN: 9781119143154
• ISBN: 978-1-119-14315-4
• No. of pages: 576
• Subjects: Natural sciences, medicine, IT, technology > Chemistry; Non-fiction book > Nature, technology > Natural science; Statistik, Chemie, Medizin, Pharmakologie, Statistics, Pharmakokinetik, chemistry, PHARMAKODYNAMIK, Medical Science, Molecular Pharmacology, Molekulare Pharmakologie, Klinische Pharmakologie u. Therapie, Clinical Pharmacology & Therapeutics, Pharmazeutische Statistik, Pharmaceutical Statistics