Biochemical Pharmacology

An integrated approach to the study of drug action mechanisms Biochemical Pharmacology is a concise and contemporary textbook on the principles of drug action. It discusses representative drugs by example to explore the range of biochemical targets and mechanisms. The book explains some of the experiments that tell us how drugs work, and it outlines the physiological and pathological context that make those action mechanisms therapeutically useful. Biochemical Pharmacology is intended primarily for students in biology and biochemistry at the advanced undergraduate or graduate levels. For classroom use, the illustrations from the book are separately available as PowerPoint slides. It is written in a conversational, vivid style that readily encourages students to explore this important area of medical science. Biochemical Pharmacology can also serve as an introduction for professionals in biosciences, as well as in pharmaceutical and health sciences. Complete with numerous figures throughout the text, which are also available separately as PowerPoint slides, Biochemical Pharmacology: Explains the role of pharmacodynamics, pharmacokinetics, and drug metabolism in drug action Provides representative examples from the pharmacology of cell excitation, hormones, nitric oxide, chemotherapy, and others Examines emerging applications of ribonucleic acids as drugs and drug targets Discusses what researchers need to know about the problems of drug distribution, elimination, and toxicity Biochemical Pharmacology is an important resource for anyone wishing to gain an in-depth understanding of drug action mechanisms and extremely useful for researchers wishing to explore some of the unanswered questions .

Table of Contents:
Preface Acknowledgments 1 Introduction 1.1 Origin and preparation of drugs 1.2 Drugs and drug targets 1.3 Drug molecules may or may not resemble the physiological ligands of their receptors 1.4 Strategies of drug discovery and development 2 Pharmacodynamics 2.1 Molecular features of drug-receptor interaction 2.2 Theory of drug-receptor binding 2.3 Dose-effect relationships in signaling cascades 2.4 Potency and efficacy 2.5 Beneficial and toxic drug effects 2.6 Appendix 3 Pharmacokinetics 3.1 Anatomical barriers to drug transport 3.2 Solute transport across cell membranes 3.3 Drug application 3.4 Drug distribution 3.5 Drug elimination via the kidneys 3.6 Quantitative experimental methods in pharmacokinetics 4 Drug metabolism 4.1 Overview: Possible functional outcomes of drug metabolism 4.2 Phase I and phase II reactions 4.3 Cytochrome P450 4.4 Reductive drug metabolism 4.5 Conjugation reactions 4.6 Enzyme induction 4.7 Metabolism-related toxicity as a therapeutic target 5 G protein-coupled receptors 5.1 Overview 5.2 GPCR structure 5.3 Structural GPCR families 5.4 Activation of GPCRs 5.5 GPCR dimerization and oligomerization 5.6 G proteins 5.7 GPCR phosphorylation, endocytosis, and G protein independent signalling 5.8 Appendix 6 Pharmacology of cell excitation 6.1 Ions, pumps and channels 6.2 ATP-driven active ion transport 6.3 Voltage-gated channels and the action potential 6.4 Channels controlled by intracellular ligands 6.5 Transient receptor potential (TRP) channels 6.6 Voltage-gated channels of nerve cells as drug targets 6.7 Synaptic transmission 6.8 Pharmacology of individual transmitters 6.9 Appendix 7 Hormones 7.1 Hormone receptors 7.2 The hypothalamus and the pituitary gland 7.3 Thyroid gland hormones 7.4 Steroid hormones 7.5 Endocrine control of bone mineralization 8 Pharmacology of nitric oxide 8.1 Characterization of nitric oxide as a biological signaling molecule 8.2 Nitric oxide synthase and its isoforms 8.3 Biochemical mechanisms of NO signaling 8.4 The biological function of iNOS 8.5 NO-releasing drugs 8.6 NOS inhibitors 8.7 Phosphodiesterase inhibitors 9 Eicosanoid mediators and related drugs 9.1 Biosynthesis of eicosanoids 9.2 The cyclooxygenase reaction 9.3 Cyclooxygenase isoforms and inhibitors 9.4 Phospholipase A2 inhibitors 9.5 Derivatives of prostaglandin H2 and related drugs 9.6 Lipoxygenases, leukotrienes and related drugs 9.7 Eicosanoids synthesized by cytochrome P450 9.8 Endocannabinoids and related drugs 9.9 The role of poly-unsaturated fatty acids in eicosanoid signaling 10 Intermediate metabolism, diabetes and atherosclerosis 10.1 Hereditary enzyme defects 10.2 Gout 10.3 Diabetes mellitus 10.4 Atherosclerosis 11 Chemotherapy of infectious diseases 11.1 Pathogenic microbes: Diversity and selective toxicity 11.2 Pharmacokinetic considerations 11.3 Resistance to antimicrobials 11.4 Antibacterial chemotherapy 11.5 Chemotherapy of fungal infections 11.6 Chemotherapy of parasite infections 11.7 Antiviral chemotherapy 12 Tumor chemotherapy 12.1 Some principles of tumor biology 12.2 Cell type-specific anti-tumor drugs 12.3 Drugs that target specific oncoproteins 12.4 Cytotoxic anti-tumor drugs 13 Ribonucleic acids as drug targets and drugs 13.1 RNA as drug target 13.2 RNA as a therapeutic agent 14 Drug delivery 14.1 Improving intestinal drug absorption 14.2 Improving drug distribution 14.3 Targeted drug delivery 14.4 Kinetically controlled drug release 14.5 Controlling drug toxicity 14.6 Delivery of nucleic acids 15 Drug Discovery 15.1 Target Selection and Validation 15.2 Screening of Candidate Compounds 15.3 Computational Screening 15.4 Phenotypic Screening 15.5 Compound Acquisition Answers to study questions References Index

About the Author :
Michael Palmer, MD, is Associate Professor in the Department of Chemistry at the University of Waterloo, Ontario, Canada, where he teaches courses on metabolism, biological membranes, and biochemical pharmacology. Alice Chan, MSc, is a reader demonstrator at the University of Calgary. Thorsten Dieckmann, PhD, is Associate Professor in the Department of Chemistry at the University of Waterloo. He has written over forty articles, papers, abstracts, and presentations. John Honek, PhD, is Professor in the Department of Chemistry at the University of Waterloo, associate editor for Future Medicinal Chemistry and Biochemistry and Cell Biology, and serves on the editorial boards of BioMed Central Biochemistry, Current Medicinal Chemistry, and Letters in Drug Design and Discovery. Michael Palmer, MD, is Associate Professor in the Department of Chemistry at the University of Waterloo, Ontario, Canada, where he teaches courses on metabolism, biological membranes, and biochemical pharmacology. Alice Chan, MSc, is a reader demonstrator at the University of Calgary. Thorsten Dieckmann, PhD, is Associate Professor in the Department of Chemistry at the University of Waterloo. He has written over forty articles, papers, abstracts, and presentations. John Honek, PhD, is Professor in the Department of Chemistry at the University of Waterloo, associate editor for Future Medicinal Chemistry and Biochemistry and Cell Biology, and serves on the editorial boards of BioMed Central Biochemistry, Current Medicinal Chemistry, and Letters in Drug Design and Discovery.