Principles in General Pharmacology

1 General Principles: History and Overview.- Historical Perspective.- Principles.- Overview of Pharmacologic Principles.- References.- 2 Dose-Effect Relations.- Dose-Effect Graphs: Potency and Efficacy.- Antagonists.- Quantal (All-or-None) Dose-Response Relations.- Additivity and Synergism.- References.- 3 Pharmacokinetics.- Absorption.- Diffusion.- Rate Constant for Absorption.- Lipid-Water Partition Coefficient.- Transport Mechanisms.- Electrochemical Potential.- The Liver.- Drug Elimination.- Volume of Distribution.- Clearance.- Drug-Protein Binding.- Protein Binding and Disease.- Renal Excretion.- Glomerular Filtration.- Urine pH and Clearance.- Hepatic Clearance.- Intravenous Dosing.- Repeated Intravenous Injections.- Intravenous Infusion.- Absorption and Elimination.- Extravascular Multiple Dosing.- Time Course of Effect and Drug Receptor Concentration.- References.- 4 Drug Metabolism (Biotransformation).- General Principles.- Anatomical Sites of Biotransformation.- Biotransformation Reactions.- Factors Affecting Drug Metabolism.- Biotransformations of Selected Common Drugs.- References.- 5 Introduction to Specific Drug Action and Membrane Surface Phenomena.- Nonspecific Drug Action.- Specific Drug Action: The Development of the Concept of Receptors.- Coated Pits and Coated Vesicles.- Membrane Capping.- Conclusion.- References.- 6 Drugs and Receptors: Chemical Bonding.- General Principles.- Types of Bonds.- Bond Formation in the Drug-Receptor Interaction.- References.- Appendix A. Physical Constants.- Appendix B. Comparison of Atomic, Ionic, and Hydrated Radii of Some Chemical Elements.- Appendix C. Structures of Drug Groups.- 7 The Rate of Drug-Receptor Interactions.- Measuring the Rate of Chemical Reactions.- Rates of Equilibrium Reactions.- Rate of the Drug-Receptor Interaction.- Influence of Diffusion on Reaction Rate.- Suggested Reading.- 8 Pharmacodynamics: The Interaction of Drugs with Receptors.- Pharmacologic Receptors.- Formation of the Drug-Receptor Complex.- Classical Theory.- Alterations in Classical Drug-Receptor Theory and Alternative Approaches.- Dissociation Constants.- Drug Combinations: Isoboles.- A Changing Receptor Concentration: Modification of Rate Equations.- References.- 9 Radioligand Binding.- Direct Binding.- Analysis of Receptor Subtypes.- Radioligand-Binding Techniques.- References.- Appendix: Mathematical Tables.