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Absorption, Distribution, Metabolism and Excretion (ADME) processes and their relationship with the design of dosage forms and the success of pharmacotherapy form the basis of this upper level undergraduate/graduate textbook. Whereas primarily oriented to Pharmacy students and graduates, it can also be useful for scientist from different fields elated to pharmaceutics and pharmacology. (e.g., material scientists, material engineers, medicinal chemists, physicians) who might be working in a positions in pharmaceutical companies or whose work might benefit from basic training in the ADME concepts and related biological background.Pedagogical features such as objectives, keywords, discussion questions, summaries and case studies are included as teaching tools. This book will provide not only general knowledge on ADME processes but also an updated insight on some hot topics such as drug transporters, multi-drug resistance related to pharmacokinetic phenomena, last generation pharmaceutical carriers (nanopharmaceuticals), in vitro and in vivo bioequivalence studies, biopharmaceuticals, pharmacogenomics, drug-drug and food-drug interactions, in silico and in vitro prediction of ADME properties, or chronopharmacokinetic. In comparison with other similar textbooks, around half of the volume would be focused on the relationship between expanding scientific fields and ADME processes. Each of these burgeoning fields has a separate chapter in the second part of the volume, and is written with experts on the correspondent topic, including industrial scientists and academics from USA and UK.Additionally, each of the initial chapters dealing with the generalities of drug absorption, distribution, metabolism and excretion would include relevant, classic examples related to each topic with appropriate illustrations. ADME Processes and Pharmaceutical Sciences is written as a core textbook for courses on pharmaceutical sciences: pharmacology, pharmacokinetics,drug delivery, biopharmaceutics, drug design and medicinal chemistry courses.

This new edition of Pharmacoresistance in Epilepsy addresses all issues relating to drug-resistance in epilepsy, including studies in patients as well in experimental models and presents the basis for an understanding of recent developments in the pathogenesis and treatment of this condition. Important issues associated with drug-resistant epilepsy are reviewed and updated, such as abnormalities in inhibitory mechanisms, neurotoxicity and changes the immune system associated with this disorder, and the development of drug-resistance as consequence of chronic exposure to antiseizure-medications. Considering that a major obstacle is that epilepsy associated with drug-resistance cannot be controlled with the traditional antiseizure medications, specific chapters describe therapeutic strategies to prevent or reduce the progression of the disease with complementary medical therapies, such as transcranial focal stimulation to promote neuroprotection. Pharmacoresistance in Epilepsy is a valuable resource for anyone working in the field, whether studying epilepsy in the lab or treating it in an office.

This unique volume covers specific aspects of the biological chemistry of terpenoids. It provides extensive information related to classification, general methods of extraction and isolation of terpenoids, synthesis and pharmacological activities of monoterpenoids, synthesis and medicinal uses of diterpenoids, biogenesis of terpenoids, synthesis and medicinal uses of sesqui terpenoids and sesterpenoids. Some terpenes are also classified as diterpene alkaloids. Most of the terpenoids with diverse molecular structures are biologically active and are used for the treatment of various diseases such as cancer, malaria, inflammation, tuberculosis and infection, and this is discussed.Features:Activities and biological relationships of terpenes An accurate assessment of where and what terpenes can lead to Discusses how microbes, in particular the actinomycetales, have well over 400 different gene clusters that produce terpenes Arranged by biological activities and usage Provides information on eukaryotic enzymes that have been shown to be a source of “ethnobotanical” terpenes

This book provides comprehensive information, both for clinicians and scientists, on the basic mechanisms, clinical features, and therapeutic approaches to epilepsy as an inflammatory disease. Inflammation has been for many years considered as an etiologic player (and a therapeutic target) for a specific group of epilepsies. However, it turns out that this concept underestimated the impact of inflammation in seizure disorders. Many accepted therapies for non-inflammatory epilepsies act in part as an inflammatory drug. The CNS actively responds to acute immune challenges by altering body temperature, stimulating the HPA axis, as well as up- and down-regulating specific sympathetic pathways.

Targeting protein degradation using small molecules is one of the most exciting small-molecule therapeutic strategies in decades and a rapidly growing area of research. In particular, the development of proteolysis targeting chimera (PROTACs) as potential drugs capable of recruiting target proteins to the cellular quality control machinery for elimination has opened new avenues to address traditionally ‘difficult to target'proteins. This book provides a comprehensive overview from the leading academic and industrial experts on recent developments, scope and limitations in this dynamically growing research area; an ideal reference work for researchers in drug discovery and chemical biology as well as advanced students.

This book is a fascinating overview of one of the first pharmacogenetic traits to be identified as responsible for genetic variation in response to drugs — the understanding of the arylamine N-acetyltransferases (NATs) is linked to many important therapeutic areas, particularly tuberculosis and also cancer. NATs have been important in the metabolism of established anti-tubercular drugs and also in carcinogenesis and susceptibility to bladder cancer. The reach of these enzymes spans pharmacology and therapeutics as well as toxicology and pharmacogenetics. The NAT genes are encoded in a highly polymorphic region of the human genome which has been explored for fine mapping in molecular anthropological studies.The book takes a wide ranging approach covering all aspects of the arylamine N-acetyltransferases from genetics to the chemistry and structural biology of the enzymes in the organisms in which they are found, from humans to bacteria and fungi where they appear to have distinct roles. The coverage is by experts in the field from across the globe.

Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations

Aging is a natural phenomenon that is peculiar to all living things. However, accumulating findings indicate that senescence could be postponed or prevented by certain approaches. Substantial evidence has emerged supporting the possibility of radical human health and lifespan extension, in particular through pharmacological modulation of aging. A number of natural dietary ingredients and synthetic drugs have been assumed to have geroprotective potential. In the development of anti-aging therapeutics, several cell, insect, and animal models may provide useful starting points prior to human studies.This book provides an overview of current research aimed to search for life-extending medications and describes pharmacological aspects of anti-aging medicine. Readers are introduced to the fascinating historical background of geroprotection in the first chapter. In-depth information on models for investigating geroprotective drugs precedes a section covering anti-aging properties of pharmaceutical compounds, such as calorie restriction mimetics, autophagy inducers, senolytics and mitochondrial antioxidants. Finally, strategies to translate discoveries from aging research into drugs and healthcare policy perspectives on anti-ageing medicine are provided to give a complete picture of the field.A timely and carefully edited collection of chapters by leading researchers in the field, this book will be a fascinating and useful resource for pharmacologists, gerontologists and any scientifically interested person wishing to know more about the current status of research into anti-aging remedies, challenges and opportunities.

As opposed to other books on the topic, this volume is unique in also covering emerging transporter targets. Following a general introduction to the importance of targeting transporter proteins with drugs, the book systematically presents individual transporter classes and explains their pharmacology and physiology. The text covers all transporter families with known or suspected importance as drug targets, including neurotransmitter transporters, ABC transporters, glucose transporters and organic ion transporters. The final part discusses recent advances in structural studies of transport proteins, assay methods for transport activity, and the systems biology of transporters and their regulation. With its focus on drug development issues, this authoritative overview is required reading for researchers in industry and academia targeting transport proteins for the treatment of disease.

Understanding and quantifying the effects of membrane transporters within the human body is essential for modulating drug safety and drug efficacy. The first volume comprehensively reviewed current knowledge and techniques in the transporter sciences and their relations to drug metabolism and pharmacokinetics. In this second volume on Drug Transporters, emphasis is placed on emerging sciences and technologies, highlighting potential areas for future advances within the drug transporter field. The topics covered in both volumes ensure that all relevant aspects of transporters are described across the drug development process, from in silico models and preclinical tools through to the potential impact of transporters in the clinic. Contributions are included from expert leaders in the field, at-the-bench industrial scientists, renowned academics and international regulators. Case studies and emerging developments are highlighted, together with the merits and limitations of the available methods and tools, and extensive references to reviews on specific in-depth topics are also included for those wishing to pursue their knowledge further. As such, this text serves as an essential handbook of information for postgraduate students, academics, industrial scientists and regulators who wish to understand the role of transporters in absorption, distribution, metabolism, and excretion processes. In addition, it is also a useful reference tool on the models and calculations necessary to predict their effect on human pharmacokinetics and pharmacodynamics.

Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant – and most challenging – areas of drug discovery. • Written by world experts to provide practical solutions to increase brain penetration or minimize CNS side-effects • Reviews state-of-the-art in silico, in vitro, and in vivo tools to assess brain penetration and advanced CNS drug delivery strategies • Covers BBB physiology, medicinal chemistry design principles, free drug hypothesis for the BBB, and transport mechanisms including passive diffusion, uptake/efflux transporters, and receptor-mediated processes • Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNS drugs, lessons learned and paths to the market

Following the success of the first edition, this pioneering study of pharmaceuticals in the environment has been updated and greatly extended. It includes the status of research on pharmaceuticals in soil, with attention to terrestrial and aquatic environments as well as new substance categories such as tetracylines and chinolones and the latest results concerning contamination of the environment and risk reduction.

A natural product is a chemical compound or substance produced by a living organism - found in nature that usually has a pharmacological or biological activity for use in pharmaceutical drug discovery and drug design. A natural product can be considered as such even if it can be prepared by total synthesis. In this book, the authors present current research in the study of the structure, bioactivity and applications of natural products. Topics discussed include the in-vitro assessment of chromones and alkaloids from Caribbean plants as potential anti-tuberculars and chemopreventors; natural products as inhibitors of ubiquitin and ubiquitin-like protein-proteasome pathways; the biological activities of red propolis; nanoencapsulation of natural products; and natural products as a source of potential drugs for the treatment of fungal infections.

Springer Handbook of Enzymes provides data on enzymes sufficiently well characterized. It offers concise and complete descriptions of some 5,000 enzymes and their application areas. Data sheets are arranged in their EC-Number sequence and the volumes themselves are arranged according to enzyme classes. This new, second edition reflects considerable progress in enzymology: many enzymes are newly classified or reclassified. Each entry is correlated with references and one or more source organisms. New datafields are created: application and engineering (for the properties of enzymes where the sequence has been changed). The total amount of material contained in the Handbook has more than doubled so that the complete second edition consists of 39 volumes as well as a Synonym Index. In addition, starting in 2009, all newly classified enzymes are treated in Supplement Volumes Springer Handbook of Enzymes is an ideal source of information for researchers in biochemistry, biotechnology, organic and analytical chemistry, and food sciences, as well as for medicinal applications.

Textbook of Clinical Neuropsychiatry provides a comprehensive, encyclopedic and up to date coverage of the complete range of neuropsychiatric disorders. The text is clearly written and well organized, utilizing a consistent and easy to read format throughout. Part I describes the diagnostic assessment of patients and details the interview, mental s

Novel drugs are being developed which interact with the programmed cell death (apoptotic) machinery in cancer cells, thereby causing these cells to commit suicide and to be removed from the body. Research is also directed to investigate why the cancer cells sometimes lose the ability to undergo apoptosis after a certain period of time and methods are being developed to reactivate this cell death process. This book is intended for workers in the field and clinicians as a useful guide of the state of affairs in this exciting field which may offer more effective possibilities for treatment of cancer patients. Mels Sluyser is the Editor of the journals APOPTOSIS and ANTI-CANCER DRUGS. He brings together a collection of papers written by the world's leading experts in these fields.