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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…mehr
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)
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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.
Inhaltsangabe
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
