Biochemical Pharmacology

  • ID: 2171811
  • Book
  • 428 Pages
  • John Wiley and Sons Ltd
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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.

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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



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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.

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