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Our intention has been to provide a short introduction to the chemistry and mode of action of insecticidal phosphoric acid compounds, with particular reference to the relationship between structure and activity. The yearly production of these pesticides is now approaching 100,000 tons and thus offers an important example of applied research. If, however, one examines the historical develop ment of these compounds, it is apparent that this was preceded by a hundred years of pure chemistry of phosphorus. The utility of the phosphoric acid pesticides is undisputed today - and furthermore it can be expected that they will solve many of the world's nutritional problems" yet from this field of applied research many paths are now leading back into basic research in chemistry, biochemistry, biology and toxicology etc. This clearly illustrates the problem of attempting to define pure and applied research. Originally, this book was conceived for students of chemistry who, on completion of their study, were uncertain about the place of applied research in industry but it was soon clear that such material, when supplemented with further data, would serve as an introduction to the field of pesticidal phosphoric acid compounds for many technicians, officials and scientists who, in various authorities in agriculture, in chemical and biological research, are concerned with the problems of crop protection and more recently with questions of pollution of the environ ment.
Rapid progress in the field of organophosphate compounds has made this new edition necessary. Particular attention has been paid to new developments in biologically active products as this is probably of greatest interest to practical chemists. I have therefore updated the chapter on chemistry and, in connection with this, rewritten the chapter on metabolism. I should especially like to thank Professor Dr. HELLMUT HOFFMANN for his constant encouragement and interest in my work and for many fruitful discus sions. The co-author to the 1st edition, Dr. KARL-JULIUS SCHMIDT, died suddenly on November 21, 1980. I treasure the memory of a valued colleague of many years standing. Elberfeld, January 1982 CHRISTA FEST VII Preface to the First Edition Our intention has been to provide a short introduction to the chemistry and mode of action of insecticidal phosphoric acid compounds, with particular ref erence to the relationship between structure and activity. The yearly produc tion of these pesticides is now approaching 100,000 tons and thus offers an im portant example of applied research. If, however, one examines the historical development of these compounds, it is apparent that this was preceded by a hundred years of pure chemistry of phosphorus.
This volume pulls together a wealth of up-to-date information on the toxicology of this diverse and ubiquitous class of insecticides. Leading experts review the reactivity of organophosphorus compounds with cholinesterase, as well as their metabolism and biological effects on humans and other nontarget organisms. The book not only covers the anticholinesterase actions of organophosphates, but also other, presumably independent, effects, such as teratogenicity, delayed neuropathy, immunotoxicity, and behavioral toxicity. - Offers crucial overviews of chemical and biochemical reactivity and biological responsiveness of mainly nontarget organisms - Reviews new developments in assessment of metabolism and disposition of organophosphorus compounds - Examines organophosphorus compound-induced toxicity mediated by mechanisms other than inhibition of acetylcholinesterase - Covers new research on differences in toxicity induced by the variety of organophosphorus - Analyzes current controversies on the relevance of certain biochemical parameters in actual organophosphate toxicity in vivo
Nomenclature. Phosphates. Phosphorothionates. Phosphorothilothionates. Phosphorothiolates. Derivates of phosphoramidic acid. Phosphonates. Hydrolysis. Chemical reactions. Biochemistry. Individual Pesticides.
This book addresses the consequences of high agricultural pesticide use over the last few decades in the form of organophosphate poisoning. The authors provide a background overview of organophosphate compounds, their environmental toxicity, non-target exposures and cases of human poisoning. The authors also compile and analyze data from the last two decades to demonstrate the toxicological aspects of organophosphates, and how they can pose a threat to human health. Readers will learn about the clinical manifestation of organophosphate exposure in humans, as well as the enzymatic pathways and mechanisms by which organophosphates are processed in the body and cause harm. The book concludes by providing techniques, practices and recommendations for how to manage organophosphate exposure and poisoning. It will be useful for clinicians and public health professionals, scientists, medical practitioners, researchers and environmental toxicologists.
Many of the pesticides applied to food crops in this country are present in foods and may pose risks to human health. Current regulations are intended to protect the health of the general population by controlling pesticide use. This book explores whether the present regulatory approaches adequately protect infants and children, who may differ from adults in susceptibility and in dietary exposures to pesticide residues. The committee focuses on four major areas: Susceptibility: Are children more susceptible or less susceptible than adults to the effects of dietary exposure to pesticides? Exposure: What foods do infants and children eat, and which pesticides and how much of them are present in those foods? Is the current information on consumption and residues adequate to estimate exposure? Toxicity: Are toxicity tests in laboratory animals adequate to predict toxicity in human infants and children? Do the extent and type of toxicity of some chemicals vary by species and by age? Assessing risk: How is dietary exposure to pesticide residues associated with response? How can laboratory data on lifetime exposures of animals be used to derive meaningful estimates of risk to children? Does risk accumulate more rapidly during the early years of life? This book will be of interest to policymakers, administrators of research in the public and private sectors, toxicologists, pediatricians and other health professionals, and the pesticide industry.
Reviews of Environmental Contamination and Toxicology attempts to provide concise, critical reviews of timely advances, philosophy and significant areas of accomplished or needed endeavor in the total field of xenobiotics, in any segment of the environment, as well as toxicological implications.
This text/reference book provides the most comprehensive coverage of anticholinesterase compounds (Organophosphates and Carbamates), which constitute the largest number of chemicals that are primarily used as insecticides in agriculture, industry, and around the home/garden. Some OPs (nerve agents) have been used in chemical warfare and terrorist attacks, while some OPs and CMs have been recommended as therapeutic agents in human medicine as well as in veterinary medicine. Many chemicals of both classes are extremely toxic and lack selectivity, thus their inadvertent/accidental use continues to pose a threat to human and animal health, aquatic systems and wildlife. These anticholinesterase agents produce a variety of toxicological effects in target and nontarget organs. In light of this complexicity, this multi-authored book is written by the well known scientists from many countries. The book is organized into nine sections, with a total of 49 chapters, to provide in-depth knowledge on various aspects of OP and CM compounds, including their use, classification, mechanism-based toxicity, and prophylactic and therapeutic measurements. Several chapters are written with special emphasis to cover timely topics, such as chemical warfare agents, physiologically-based pharmacokinetic modeling, structure and function of cholinesterases, paraoxonase, carboxylesterases; developmental neurotoxicity, the intermediate syndrome, oxidative stress, endocrine disruption, and DNA damage/gene expression and carcinogenesis. Section-VI with 5 chapters is specifically devoted to risk assessment, and safety and regulatory guidelines for pesticides. - Describes everything you need to know about Organophosphates and Carbamates - Extensively covers pesticides, nerve agents, therapeutic drugs, and flame retardants - Describes epidemiology of the world's major disasters involving Organophosphates and Carbamates - Covers animal, human, aquatic, and wildlife toxicity of Anticholinesterases - Insights into in-depth cholinergic and noncholinergic mechanisms of toxicity - Describes recent advancements in cholinesterases, paraoxonases, carboxylesterases, oxidative stress, endocrine disruption, cardiac and pulmonary toxicity, and carcinogenesis - Provides in vitro and in vivo models for neurotoxicity testing - Integrates knowledge of studies in lab animals and humans - Offers risk/safety assessment and national/international guidelines for permissible levels of pesticide residues - Describes management of Anticholinesterase poisoning in humans
This volume of the IARC Monographs provides evaluations of the carcinogenicity of some organophosphate insecticides and herbicides, including diazinon, glyphosate, malathion, parathion, and tetrachlorvinphos. Diazinon acts on a wide range of insects on crops, gardens, livestock, and pets, but most uses have been restricted in the USA, Canada, and the European Union since the 1980s. Glyphosate is the most heavily used agricultural and residential herbicide in the world, and has been detected in soil, air, surface water, and groundwater, as well as in food. Malathion is one of the oldest and most widely used organophosphate insecticides, and has a broad spectrum of applications in agriculture and public health, notably mosquito control. The insecticide parathion has been largely banned or restricted throughout the world due to toxicity to wildlife and humans. Tetrachlorvinphos is banned in the European Union, but continues to be used in the USA and elsewhere as an insecticide on animals, including in pet flea collars. The IARC Monographs Working Group reviewed epidemiological evidence, animal bioassays, and mechanistic and other relevant data to reach conclusions as to the carcinogenic hazard to humans of these agents.
In recent years many of the conventional methods of insect control by broad spectrum synthetic chemicals have come under scrutiny because of their unde sirable effects on human health and the environment. In addition, some classes of pesticide chemistry, which generated resistance problems and severely affected the environment, are no longer used. It is against this background that the authors of this book present up-to-date findings-relating to biochemical sites that can serve as targets for developing insecticides with selective prop erties, and as the basis for the elucidation of resistance mechanisms and countermeasures. The book consists of eight chapters relating to biochemical targets for insec ticide action and seven chapters relating to biochemical modes of resistance and countermeasures. The authors of the chapters are world leaders in pesti cide chemistry, biochemical modes of action and mechanisms of resistance. Biochemical sites such as chitin formation, juvenile hormone and ecdysone receptors, acetylcholine and GABA receptors, ion channels, and neuropeptides are potential targets for insecticide action. The progress made in recent years in molecular biology (presented in depth in this volume) has led to the iden tification of genes that confer mechanisms of resistance, such as increased detoxification, decreased penetration and insensitive target sites. A combina tion of factors can lead to potentiation of the resistance level. Classifications of these mechanisms are termed gene amplification, changes in structural genes, and modification of gene expression.