Synopses & Reviews
Emphasizing the molecular action of drugs, this text incorporates recent findings from biochemical pharmacology along with the latest insights into the interactions of drugs with their receptors. It is organized by targets of drug action--endogenous messengers and their receptors, membranes, enzymes, and DNA, among others--and covers all drug groups and their therapeutic applications. This new edition has been thoroughly revised to provide expanded coverage of co-transmitters and neurohormones as well as adenosine receptors and calcium channel blockers. The chapter on drug distribution and metabolism has been extended, and the final chapter on principles of drug design outlines new methods, such as numerical techniques and computer graphics. Other new topics include atrial natriuretic factors, antiarrhythmic drugs, and DNA topoisomerase inhibitory mechanism of antitumor and antibacterial agents. The text is illustrated with hundreds of formulas and tables, and the index includes an extensive listing of drugs.
Table of Contents
PART I: Physiochemical Principles of Drug Action
1. Role and Structure of Water
2. Solubility
3. Partition Coefficients
4. Surface Activity and Drug Effects
5. Stereochemical Aspects of Drug Action
6. Electronic Structure and its Effects on Drug Activity
7. Chemical Bonding and Biological Activity
8. Quantum Chemical Aspects of Drug Action
9. Quantitative Structure-Activity Relationships
PART II: Receptor-Effector Theories
1. The Receptor Concept and its History
2. The Nature of Receptors and the Criteria of Receptor Identity
3. Definition of Pharmacological Binding Terms
4. Classical Theories of Concentration-Response Relationships
5. Molecular Concepts of Receptor Function
PART III: Methods of Receptor Characterization
1. Methodological Principles
2. Indirect Methods of Receptor Characterization
3. Direct Methods of Receptor Characterization
4. Data Treatment
PART IV: Drugs Acting on Neurotransmitters and Their Receptors
1. Outline of Neuroanatomy and Neurophysiology
2. Acetylcholine and the Cholinergic Receptors
3. Norepinephrine and the Adrenergic Receptors
4. Dopamine and the Dopaminergic Receptors
5. Serotonin and the Serotonergic Drug Effects
6. Histamine and the Histamine Receptors
7. Purinergic Neuromodulation and the Adenosine Receptors
8. Aminoacid Neurotransmitters and the Drug Effects They Mediate
PART V: Drugs Acting on Hormones, Neurohormones, and Their Receptors
1. Steroid Hormones and Their Receptors
2. Peptide and Protein Hormones and Neurohormones
3. Enkephalins, Endorphins, and Opiate Analgesics
4. Prostaglandins and Thromboxanes
5. Atrial Natriuretic Factors
PART VI: Non-Messenger Targets for Drug Action
1. Excitable Membranes
2. Cell-Wall Synthesis Inhibitors
3. Enzymes as Drug Targets
4. Vitamins
5. Nucleic Acids as Targets for Drug Action
PART VII: Drug Distribution and Metabolism
1. Drug Distribution
2. Drug Metabolism
PART VIII: Principles of Drug Design
1. Analogue Synthesis Versus Rational Design
2. Discovery of "Lead" Compounds
3. Pharmacophore Identification
4. Pro-Drugs and "Soft" Drugs