Metabolism Pharmacokinetics And Toxicity Of Functional Groups
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Author : Dennis A. Smith Publisher : Royal Society of Chemistry Page : 545 pages File Size : 55,6 Mb Release : 2010 Category : Medical ISBN : 9781849730167
Metabolism, Pharmacokinetics, and Toxicity of Functional Groups by Dennis A. Smith Pdf
Written by medicinal chemists and ADMET scientists with a combined experience of over 300 years this aid to discovering drugs provides detailed coverage on absorption, distribution, metabolism, excretion and toxicology issues associated with new drugs.
Metabolic Basis of Detoxication by William B. Jakoby Pdf
Metabolic Basis of Detoxication: Metabolism of Functional Groups considers the possible fates of the relatively circumscribed number of functional groups that xenobiotics bear. An understanding of the possible reactions, and the chemical and biological factors influencing them, will contribute to the overall predictability of the fate of "real" molecules. This approach attempts to knit together the understanding of metabolic pathways with that of the enzymes that catalyze the specific steps. The book contains 18 chapters and begins with a discussion of the biological oxidation of carbon atoms. This is followed by separate chapters on the metabolism of halogenated aliphatic hydrocarbons, aryl halides, heterocyclic rings, alcohols, aldehydes, and ketones. Subsequent chapters cover oxidative processes such as metabolic dealkylations and biological oxidation at nitrogen centers; the reduction of nitro and azo compounds and tertiary amine N-oxides; the oxidation, alkylation, acylation, and glycosylation of mercaptans; epoxide metabolism; and conjugation of phenols. The book aims to inform and interest the pharmacologist and toxicologist concerning the biochemical aspects and to orient the biochemist to the pharmacological insights required in dealing with the metabolism of xenobiotics.
Drug-like Properties: Concepts, Structure Design and Methods by Li Di,Edward H Kerns Pdf
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint
National Research Council,Policy and Global Affairs,Science, Technology, and Law Program,Committee on the Use of Third Party Toxicity Research with Human Research Participants
Author : National Research Council,Policy and Global Affairs,Science, Technology, and Law Program,Committee on the Use of Third Party Toxicity Research with Human Research Participants Publisher : National Academies Press Page : 226 pages File Size : 42,7 Mb Release : 2004-06-04 Category : Science ISBN : 9780309166416
Intentional Human Dosing Studies for EPA Regulatory Purposes by National Research Council,Policy and Global Affairs,Science, Technology, and Law Program,Committee on the Use of Third Party Toxicity Research with Human Research Participants Pdf
The EPA commissioned The National Academies to provide advice on the vexing question of whether and, if so, under what circumstances EPA should accept and consider intentional human dosing studies conducted by companies or other sources outside the agency (so-called third parties) to gather evidence relating to the risks of a chemical or the conditions under which exposure to it could be judged safe. This report recommends that such studies be conducted and used for regulatory purposes only if all of several strict conditions are met, including the following: The study is necessary and scientifically valid, meaning that it addresses an important regulatory question that can't be answered with animal studies or nondosing human studies; The societal benefits of the study outweigh any anticipated risks to participants. At no time, even when benefits beyond improved regulation exist, can a human dosing study be justified that is anticipated to cause lasting harm to study participants; and All recognized ethical standards and procedures for protecting the interests of study participants are observed. In addition, EPA should establish a Human Studies Review Board (HSRB) to evaluate all human dosing studiesâ€"both at the beginning and upon completion of the experimentsâ€"if they are carried out with the intent of affecting the agency's policy-making.
Mechanisms of Drug Toxicity, Volume 4 presents the proceedings of the 3rd International Pharmacological Meeting held in Sao Paulo, Brazil in 1966. The book discusses the drug-induced pathobiotic effects; the mechanisms of adverse reactions; and enzyme induction in the mechanism of chronic toxicity. The text also describes the influence of inducing substances on the growth of liver and microsomal electron transport systems; the quantitative aspects of chronic toxicity; and the facts and fallacies in predicting drug effects in human.
Bioactive Carboxylic Compound Classes by Clemens Lamberth,Jürgen Dinges Pdf
Following the successful and proven concept used in "Bioactive Heterocyclic Compound Classes" by the same editors, this book is the first to present approved pharmaceutical and agrochemical compounds classified by their carboxylic acid functionality in one handy volume. Each of the around 40 chapters describes one or two typical syntheses of a specific compound class and provides concise information on the history of development, mode of action, biological activity and field of application, as well as structure-activity relationships. In addition, similarities and differences between pharmaceuticals and agrochemicals are discussed in the introduction. Written by a team of experts in the field, this is a useful reference for researchers in academia and chemical or pharmaceutical companies working in the field of total synthesis and natural product chemistry, drug development, and crop protection research.
This practical guide covers background information on liver function, the principles of drug use in liver disease and includes a section of worked examples of commonly asked questions. It will be invaluable to clinical pharmacists and anyone making medicine choices in patients with liver impairment.
Volatile Organic Compounds in the Atmosphere by Ralf Koppmann Pdf
Every day, large quantities of volatile organic compounds (VOCs) are emitted into the atmosphere from both anthropogenic and natural sources. The formation of gaseous and particulate secondary products caused by oxidation of VOCs is one of the largest unknowns in the quantitative prediction of the earth’s climate on a regional and global scale, and on the understanding of local air quality. To be able to model and control their impact, it is essential to understand the sources of VOCs, their distribution in the atmosphere and the chemical transformations which remove these compounds from the atmosphere. In recent years techniques for the analysis of organic compounds in the atmosphere have been developed to increase the spectrum of detectable compounds and their detection limits. New methods have been introduced to increase the time resolution of those measurements and to resolve more complex mixtures of organic compounds. Volatile Organic Compounds in the Atmosphere describes the current state of knowledge of the chemistry of VOCs as well as the methods and techniques to analyse gaseous and particulate organic compounds in the atmosphere. The aim is to provide an authoritative review to address the needs of both graduate students and active researchers in the field of atmospheric chemistry research.
Advances in Nucleic Acid Therapeutics by Michael J Gait,Sudhir Agrawal Pdf
The sequencing of the human genome and subsequent elucidation of the molecular pathways that are important in the pathology of disease have provided unprecedented opportunities for the development of new therapeutics. Nucleic acid-based drugs have emerged in recent years to yield extremely promising candidates for drug therapy to a wide range of diseases. Advances in Nucleic Acid Therapeutics is a comprehensive review of the latest advances in the field, covering the background of the development of nucleic acids for therapeutic purposes to the array of drug development approaches currently being pursued using antisense, RNAi, aptamer, immune modulatory and other synthetic oligonucleotides. Nucleic acid therapeutics is a field that has been continually innovating to meet the challenges of drug discovery and development; bringing contributions together from leaders at the forefront of progress, this book depicts the many approaches currently being pursued in both academia and industry. A go-to volume for medicinal chemists, Advances in Nucleic Acid Therapeutics provides a broad overview of techniques of contemporary interest in drug discovery.
Information Resources in Toxicology, Volume 1: Background, Resources, and Tools by Steve Gilbert,Asish Mohapatra,Sol Bobst,Antoinette Hayes,Sara T. Humes Pdf
This new fifth edition of Information Resources in Toxicology offers a consolidated entry portal for the study, research, and practice of toxicology. Both volumes represents a unique, wide-ranging, curated, international, annotated bibliography, and directory of major resources in toxicology and allied fields such as environmental and occupational health, chemical safety, and risk assessment. The editors and authors are among the leaders of the profession sharing their cumulative wisdom in toxicology’s subdisciplines. This edition keeps pace with the digital world in directing and linking readers to relevant websites and other online tools. Due to the increasing size of the hardcopy publication, the current edition has been divided into two volumes to make it easier to handle and consult. Volume 1: Background, Resources, and Tools, arranged in 5 parts, begins with chapters on the science of toxicology, its history, and informatics framework in Part 1. Part 2 continues with chapters organized by more specific subject such as cancer, clinical toxicology, genetic toxicology, etc. The categorization of chapters by resource format, for example, journals and newsletters, technical reports, organizations constitutes Part 3. Part 4 further considers toxicology’s presence via the Internet, databases, and software tools. Among the miscellaneous topics in the concluding Part 5 are laws and regulations, professional education, grants and funding, and patents. Volume 2: The Global Arena offers contributed chapters focusing on the toxicology contributions of over 40 countries, followed by a glossary of toxicological terms and an appendix of popular quotations related to the field. The book, offered in both print and electronic formats, is carefully structured, indexed, and cross-referenced to enable users to easily find answers to their questions or serendipitously locate useful knowledge they were not originally aware they needed. Among the many timely topics receiving increased emphasis are disaster preparedness, nanotechnology, -omics, risk assessment, societal implications such as ethics and the precautionary principle, climate change, and children’s environmental health. Introductory chapters provide a backdrop to the science of toxicology, its history, the origin and status of toxicoinformatics, and starting points for identifying resources Offers an extensive array of chapters organized by subject, each highlighting resources such as journals, databases,organizations, and review articles Includes chapters with an emphasis on format such as government reports, general interest publications, blogs, and audiovisuals Explores recent internet trends, web-based databases, and software tools in a section on the online environment Concludes with a miscellany of special topics such as laws and regulations, chemical hazard communication resources, careers and professional education, K-12 resources, funding, poison control centers, and patents Paired with Volume Two, which focuses on global resources, this set offers the most comprehensive compendium of print, digital, and organizational resources in the toxicological sciences with over 120 chapters contributions by experts and leaders in the field
Cyclic Nucleotide Phosphodiesterases in Health and Disease by Joseph A. Beavo,Sharron H. Francis,Miles D. Houslay Pdf
Since the last major compendium dedicated to cyclic nucleotide phosphodiesterases (PDEs) was published over 15 years ago, an enormous amount of progress has occurred in the field. There is great need for a centralized source for key information in this burgeoning and therapeutically important area of medical research. Cyclic Nucleotide Phosph
Molecular Pharmacology by John Dickenson,Fiona Freeman,Chris Lloyd Mills,Christian Thode,Shiva Sivasubramaniam Pdf
This textbook provides a fresh, comprehensive and accessible introduction to the rapidly expanding field of molecular pharmacology. Adopting a drug target-based, rather than the traditional organ/system based, approach this innovative guide reflects the current advances and research trend towards molecular based drug design, derived from a detailed understanding of chemical responses in the body. Drugs are then tailored to fit a treatment profile, rather than the traditional method of ‘trial and error’ drug discovery which focuses on testing chemicals on animals or cell cultures and matching their effects to treatments. Providing an invaluable resource for advanced under-graduate and MSc/PhD students, new researchers to the field and practitioners for continuing professional development, Molecular Pharmacology explores; recent advances and developments in the four major human drug target families (G-protein coupled receptors, ion channels, nuclear receptors and transporters), cloning of drug targets, transgenic animal technology, gene therapy, pharmacogenomics and looks at the role of calcium in the cell. Current - focuses on cutting edge techniques and approaches, including new methods to quantify biological activities in different systems and ways to interpret and understand pharmacological data. Cutting Edge - highlights advances in pharmacogenomics and explores how an individual’s genetic makeup influences their response to therapeutic drugs and the potential for harmful side effects. Applied - includes numerous, real-world examples and a detailed case-study based chapter which looks at current and possible future treatment strategies for cystic fibrosis. This case study considers the relative merits of both drug therapy for specific classes of mutation and gene therapy to correct the underlying defect. Accessible - contains a comprehensive glossary, suggestions for further reading at the end of each chapter and an associated website that provides a complete set of figures from within the book.
Biopharmaceutics and Clinical Pharmacokinetics by Notari Pdf
For a decade and a half, Biopharmaceutics and Clinical Pharmacokinetics has been used in theclassrooms around the world as an introductory textbook on biophannaceutics and phannacokinetics. Now, the new Fourth Edition, Revised and Expanded further enhances the preceding editions'proven features, introducing significant advances in clinical pharmacokinetics, pharmacokineticdesign of drugs and dosage forms, and model-independent analyses. Still usable without prior knowledge of calculus or kinetics, this successfully implemented workbookmaintains a carefully graduated "building block" presentation, incorporating sample problemsand exercises throughout for a thorough understanding of the material.Biopharmaceutics and Clinical Pharmacokinetics features a growth-oriented format that systematicallydevelops and interrelates all subject matter .. . introduces basic theory and fields of application... emphasizes model-independent pharmacokinetic analyses ... presents biopharmaceutical aspectsof product design and evaluation .. . offers a unique approach to teaching dosage regimen design andindividualization . .. and considers structural modification of drug molecules for problems associatedwith pharmacokinetics. As a comprehensive coverage of the basic principles and the recent achievements in the field, noother textbook does as much for students of pharmacy, pharmacology, medicinal chemistry, andmedicine, or for scientists who desire a simple but thorough introduction to theory and application.
Author : Ray H. Liu,Dennis V. Canfield,Sheng-Meng Wang Publisher : CRC Press Page : 510 pages File Size : 43,7 Mb Release : 2009-08-05 Category : Law ISBN : 142009498X
Quantitation and Mass Spectrometric Data of Drugs and Isotopically Labeled Analogs by Ray H. Liu,Dennis V. Canfield,Sheng-Meng Wang Pdf
The analysis of drugs and their metabolites in biological media are now expected to routinely achieve ± 20% accuracy in the ng/mL concentration level. Therefore, the availability and the selection of quality ion-pairs designating the analytes and their isotopically labeled analogs (ILAs) are important considerations in achieving the accuracy of quantitation results. Assisting scientists with this process, Quantitation and Mass Spectrometric Data of Drugs and Isotopically Labeled Analogs provides an extremely valuable reference for labs involved in the analysis of therapeutic and abused drugs. Part One of this comprehensive volume illustrates approaches, mechanisms, and challenges pertaining to the use of isotopic analogs as internal standards for drug quantitation. The second section is a systematic compilation of full-scan mass spectra of drugs and their analogs, as parent compounds and as derivatives resulting from various chemical derivatization approaches, commonly encountered in today’s labs. Based on the mass spectra data presented in the second section, Part Three provides corresponding tables of ion-pairs which can potentially be adapted to designate the drugs and their isotopic analogs in the analytical processes. Relative quality of these ion-pairs (cross-contribution to the intensity of these ions by their isotopic analogs) is included in these tables. With more than 1500 full-scan mass spectra and quick access data tables, this text represents the authors’ years of work compiling mass spectra of the many chemical derivatization forms of drugs, their metabolites, and their isotopically labeled counterparts. The unparalleled scope of this compilation makes it a critical one-stop reference for those involved in drug analyses of biological specimens and interpretation of results.
