Microsomes and Drug Oxidations is a record of the proceedings of the Third International Symposium on Microsomes and Drug Oxidations, held in Berlin, Germany in July 1976. The compendium provides an overview of knowledge on the oxidative metabolism of drugs, carcinogens, and various other environmental chemicals. Topics discussed include lipid structure of liver microsomal membranes; interactions between cytochrome p-450 and nadphcytochrome p-450 reductase in the microsomal membrane; impact of drug monoxygenases in clinical pharmacology; and the manner in which oxygen participates in mixed-function oxidation reactions. Pharmacologists, toxicologists, biochemists, and researchers in the pharmaceutical industry will find the book highly insightful.

Of drug-metabolising reactions. p. 25.

This volume of the Handbook of Experimental Pharmacology (Concepts in Biochemical Pharmacology) will show that pharma cology has finally arrived as a true discipline in its own right, and is no longer the handmaiden of organic chemistry and physiology. Instead it is an amalgam of all the biological sciences including biochemistry, biophysical chemistry, physiology, pathology and clinical medicine. In the volumes that make up Concepts in Bio chemical Pharmacology we hope to convince Medical Schools what should now be obvious, that pharmacology is no longer that dull topic bridging the basic sciences with medicine, but is probably the most important subject in the medical curriculum. We are grateful for the advice of Dr. Byron Clark, Director of the Pharmacology-Toxicology Program at the National Institutes of Health whose support made possible much of the work described in this volume. Contents Section Four: Methods 01 Stooging the MetoholiBm 01 Drugs Subsection A. Assay 01 Drugs and Their M etoholites Chapter 22 : Basic Principles in Development of Methods for Drug Assay. B. B. BRODIE. With 2 Figures 1 1 A. Introduction . . . . . . . . . . B. Principles of Developing a Method. . . . . . 1 I. Section of Method of Assay . . . . . . 1 II. Choice of Solvent for Extraction of Drug 2 III. Adsorption of Drugs by Glass Surfaces . . . . . . . . . . . . . . 3 IV. Recoveries of Known Amounts of Compound from Biological Material. 4 V. Assessment of Sensitivity 5 VI. Assessment of Specificity 5 References. . . . . . . . . . .

Microsomes and Drug Oxidations documents the proceedings of symposium on microsomes and drug oxidations held at Bethesda, Maryland, 16-17 February 1968. The theme of the symposium centered on the morphology of the liver endoplasmic reticulum, the localization of enzyme systems, the mechanisms for regulating enzyme activity, and the mechanisms of enzyme action. The results of this symposium presented in this book illustrate the complexity of the enzyme systems under investigation and the multiplicity of the variables altering their function. It is hoped the information presented will serve as a stimulus to other investigators in the elucidation of these problems. The book contains 27 papers organized into four parts. The papers in Part I examine the morphological and biochemical characteristics of microsomes. Part II presents studies on electron transfer components. Part III examines alterations of microsomal enzymes while Part IV focuses on drugs and protein synthesis.

Microsomes, Drug Oxidations, and Chemical Carcinogenesis, Volume II, documents the proceedings of the 4th International Symposium on Microsomes and Drug Oxidations held in Ann Arbor, July 1979. The symposium reviewed progress in the understanding of scientific and biomedical problems from a biochemical, biophysical, pharmacological, and toxicological perspective. Volume I contained 117 contributions made by researchers at the symposium, which were organized into three sections (Sections I-III). This second volume contains 122 contributions, divided into four sections (Sections IV-VII). The papers on Section IV examine the metabolic fate of oxygenated compounds. Section V provides studies on microsomal enzymes and lipid metabolism. Section VI includes papers on microsomal enzymes and toxicity of foreign compounds. Section VII covers microsomal enzymes and chemical mutagenesis and carcinogenesis. This book seeks to aid future progress in understanding the complexities of metabolic transformations by these versatile enzyme systems that act on physiologically important lipids as well as on a wide array of foreign substances, including drugs, anesthetics, industrial chemicals, food additives, pesticides, carcinogens, and nonnutrient dietary chemicals.

TRANSPORTERS AND DRUG-METABOLIZING ENZYMES IN DRUG TOXICITY Explore up-to-date coverage on the interaction between drug metabolism enzymes, transporters, and drug toxicity with this leading resources Transporters and Drug-Metabolizing Enzymes in Drug Toxicity delivers a comprehensive and updated review of the relationship between drug metabolism, transporters, and toxicity, providing insights into a major challenge in drug development – accurate assessment of human drug toxicity. Combining two disciplines frequently considered independently of one another, the book combines drug metabolism and toxicology with a focus on the role of biotransformation on drug toxicity and as a major factor for species and individual differences. Mechanism and species differences in drug metabolizing enzymes and transporters are discussed, as are the methods used to investigate the role of drug metabolizing enzymes and transporters in drug toxicity. Finally, the distinguished authors describe promising new experimental approaches to accurately assessing human drug toxicity via the consideration of human-specific drug metabolism in toxicity assays. In addition to topics as diverse as extended clearance models, experimental approaches for the estimation of DILI potential of drug candidates and roles of transporters in renal drug toxicity, readers will also enjoy the inclusion of such subjects as: A thorough overview of and introduction to drug metabolism and transporters and drug toxicity An exploration of drug metabolism enzymes and transporter activities as risk factors of marketed drugs associated with drug-induced fatalities A discussion of human-based in vitro experimental models for the evaluation of metabolism-dependent drug toxicity A treatment of mechanism-based experimental models for the evaluation of BSEP inhibition and DILI An examination of transporters and cochlea toxicity Perfect for scientists, students, and practitioners with interests in metabolism, toxicology, and drug development in the pharmaceutical industry, Transporters and Drug-Metabolizing Enzymes in Drug Toxicity will also earn a place in the libraries of medicinal chemists, pharmacologists, biochemists, toxicologists, and regulators in the pharmaceutical and health industries.