Most drugs, toxins, hormones, and the like bring about their biologic actions by reacting with specific receptors somewhere in the body. Scientists working in all areas of biologic science have shown increasing interest in the analysis of drug-receptor interactions in the broadest sense. Studies of drugs (binding) to receptors in situ and to isolated and partly purified receptors are becoming common practice. The action of a drug in the body is, however, a kinetic event not only with respect to transport of drug molecules to the environment of the receptors, but also with respect to the drug-receptor interaction itself. Kinetics of Drug Action is an integrative approach to drug transport through the body, membrane transport toward the receptors, and the kinetics of drug receptor interaction. This volume is aimed at providing a critical and penetrating study of the problems relevant to the kinetics or drug action from drug dosage to the final response. It is felt that the critical surveys presented in this volume will contribute significantly to receptor study research in various biologic fields and to a better understanding of drug action. I would like to express my gratitude to our secretary Miss MARGOT JANSSEN for the extensive typing of manuscripts and to our laboratory assistant Miss COBY HURKMANS for her dedicated assistance in the correcting some of the manuscripts and preparating the index.

Inhalt
General Introduction.- 1 Physicochemical Fundamentals and Thermodynamics of the Membrane Transport of Drugs..- I. Introduction.- II. Systems and Membrane Types.- III. Classification of Membrane Transport.- IV. Kinetics and Thermodynamics of Membrane Transport.- Appendix. Glossary of Symbols.- References.- 2 Pharmacokinetics. Kinetic Aspects of Absorption, Distribution, and Elimination of Drugs..- I. Introduction.- II. Pharmacokinetic Models.- III. Models for Single-Dose Administration.- IV. Multiple Dose Administration.- V. Conclusion.- References.- 3 Pharmacokinetics of Biotransformation..- I. Introduction.- II. Conclusion.- References.- 4 General Theory of Drug-Receptor Interactions. Drug-Receptor Interaction Models. Calculation of Drug Parameters..- I. Introduction.- II. Drugs, Receptors and Effects.- III. Agonistic Interaction.- IV. Competitive Interaction.- V. Metactoid Interaction.- VI. Metaffinoid Interaction.- VII. Functional Interaction.- VIII. Plural Affinities.- IX. Numerical Expressions of Intrinsic Activity and Affinity.- References.- 5 A Critical Survey of Receptor Theories of Drug Action..- I. Introduction.- II. The Mathematics of Drug-Receptor Interactions.- III. Occupation Theories of Drug Action.- IV. The Rate Theory of Drug Action.- V. A General Discussion of the Various Receptor Models.- VI. A General Discussion of the Possible Uses of Receptor Models.- Appendix. Glossary of Symbols.- References.- 6 Drug-Receptor Inactivation: A New Kinetic Model..- I. Introduction.- II. Energetics of Receptor Activity.- III. Models in Which Trigger Energy is Generated.- IV. Models Involving Irreversible Alterations of Agonist or Receptor.- V. A Receptor Inactivation Theory.- VI. Stationary State Behavior with Single Agonists.- VII. Transient State Behavior with Single Agonists.- VIII. Stationary State Behavior with Agonist-Antagonist Mixtures.- IX. Transient State Behavior with Agonist-Antagonist Mixtures.- X. General Discussion.- XI. Summary.- Addendum A.- Addendum B.- Appendices: GlossaryGeneralized Rate Equations for the Receptor Inactivation ModelOn EffectOff EffectAnalysis of OscillationsReceptor Interactions with Agonist-Antagonist Mixtures.- References.- 7 Kinetics of Drug-Receptor Interaction..- I. Introduction.- II. Diffusion of Drug to Receptor.- III. Intermolecular Forces in Drug-Receptor Reactions.- IV. Kinetics of Drug-Receptor Association and Dissociation.- V. Possibilities for Measuring Rate Constants in Drug-Receptor Interaction.- VI. Conformational Changes in the Drug-Receptor Complex.- VII. Kinetics of Drug-Receptor Interaction, Including Conformational Changes.- VIII. Some Other Notions in Molecular Pharmacology.- IX. Activation Parameters.- References.- Conclusion.- Author Index.