Human Drug Metabolism provides a concise, user-friendly introduction to drug metabolism.

Features:

• Focuses on a conceptual understanding of the drug metabolism system
• Illustrates the basic mechanisms on how xenobiotics are detected, chemically modified and then eliminated from human systems

Contents

Introduction

• Therapeutic Window
• Consequences of Drug Concentration Changes
• Clearance
• Hepatic Extraction and Intrinsic Clearance
• First Pass and Plasma Drug Levels
• Drug and Xenobiotic Metabolism

Drug Biotransformational Systems - Origins and Aims

• Biotransforming enzymes
• Threat of Aromatic Hydrocarbons
• Cell Communication
• Potential Food Toxins
• Sites of Biotransforming Enzymes
• Biotransformation

How Phase I Systems Metabolise Substrates

• Introduction
• Capture of Lipophilic Molecules
• Cytochrome P450s Basic Structure
• CYPs-Main and Associated Structures
• CYP Substrate Specificity and Regulation
• Main Human CYP Families
• Cytochrome P450 Catalytic Cycle
• Real-life Operations
• CYP Isoforms: how aims are translated into function
• Aromatic Ring Hydroxylation
• Alkyl Oxidations
• Rearrangement and Reactions
• Other Oxidation Processes
• Reduction Reactions
• Control of CYP Metabolic Function

Induction of Phase I Systems

• Introduction
• Causes of Accelerated Clearance
• Enzyme Induction
• Mechanisms of Enzyme induction
• Induction-General Clinical Aspects

Phase I Enzyme Inhibition

• Introduction
• Inhibition of Metabolism-general aspects
• Mechanisms of Inhibition
• Cell transport systems and CYP 3A inhibitors
• Clinical Consequences of Drug Inhibition
• Use of Inhibitors for Positive Clinical Intervention

Phase II and III Processes

• Introduction
• Glucuronidation
• Sulphation
• The GSH System
• Glutathione S-Transferases
• Epoxide hydrolases
• Acetylation
• Methylation
• Esterases/amidases
• Amino Acid Conjugation (Glycine or Glutamate)
• Phase III Processes

Factors Affecting Drug Metabolism

• Introduction
• Genetic Polymorphisms
• Effects of Age on Drug Metabolism
• Effects of Diet on Drug Metabolism
• Gender Effects
• Effects of Disease on Drug Metabolism
• Summary

Role of Metabolism in Drug Toxictiy

• Adverse Drug Reactions
• Reversible Drug Adverse Effects Type A
• Irreversible Toxicity (Type B)
• Type B1 Necrotic Reactions
• Type B2 Reactions: Immunotoxicity
• Type B3 Reactions: Role of Metabolism in Cancer
• Summary Of Biotransformational Toxicity

Appendix A: Methods in Drug Metabolism

• Introduction
• Human liver microsomes
• Human hepatocytes
• Heterolohous systems
• Toxicological metabolism-based assays
• In silico studies

Appendix B: Metabolism of Major Ilicit Drugs

• Introduction
• Opiates
• Cocaine
• Hallucinogens
• Amphetamines:ecstacy (MDMA)
• Cannabis
• PCP

Appendix C: Examination Techniques

• Introduction
• A first-class answer
• Preparation
• The day of reckoning

Index

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