Volumes in this widely revered series present comprehensive reviews of drug substances and additional materials, with critical review chapters that summarize information related to the characterization of drug substances and excipients. This organizational structure meets the needs of the pharmaceutical community and allows for the development of a timely vehicle for publishing review materials on this topic.
The scope of the Profiles series encompasses review articles and database compilations that fall within one of the following six broad categories: Physical profiles of drug substances and excipients; Analytical profiles of drug substances and excipients; Drug metabolism and pharmacokinetic profiles of drug substances and excipients; Methodology related to the characterization of drug substances and excipients; Methods of chemical synthesis; and Reviews of the uses and applications for individual drug substances, classes of drug substances, or excipients.

Key features:

* Contributions from leading authorities * Informs and updates on all the latest developments in the field

This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics. The chapters in this book describe how these approaches can be applied to address key drug discovery issues, such as receptor structure modelling, function and dynamics, prediction of protein-water-ligand interactions and binding kinetics, free energy of binding, interconversion between agonists and antagonists, deorphanization of GPCRs, and the discovery of biased and allosteric modulators. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modelling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique,Computational Methods for GPCR Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.

Emerging approaches to treating addictions and minimizing relapse are spotlighted in this idea-packed volume, as alternatives or adjuncts to standard psychological and pharmacological therapies. Its biopsychosocial perspective delves into the causes and processes of chemical dependence, and the clinical characteristics it shares with other addictions (e.g., food, sex, gambling, online activities), to identify client needs that substance abuse may fulfill. Accordingly, the diverse modalities featured here address substance addiction on multiple levels, offering clients physical or mental stimulation and/or emotional relief as well as affording different degrees of autonomy. Methods can be mixed and matched to reinforce treatment goals, and clinicians can tailor treatment to individual issues and interests to assure clients nuanced and meaningful care. Included in the coverage: * Use of herbal medicine to treat drug addiction. * EMDR therapy and the treatment of substance abuse and addiction. * Evaluating the change processes in drug users' interventions. * Web-based interventions for substance abuse. * Physical exercise and treatment of addiction. * Mindfulness to reduce the anxiety during the abstinence * Neurofeedback to deal with craving and anxiety symptoms Psychologists, psychiatrists, clinical social workers, and addiction counselors and educators will find Innovations in the Treatment of Substance Addiction a valuable sourcebook for understanding addiction-and intervention-in its wider context.

Ibuprofen is one of the most successful drugs used worldwide for the treatment of mild to moderate pain and various inflammatory conditions. Over the past 40 years, ibuprofen has been proven to be as safe or even safer and also as effective as the established non-steroidal anti-inflammatory drugs (NSAIDs) and the coxibs. This well-written book reviews the pharmacology, clinical uses and the various adverse effects of Ibuprofen, the disposition and unique modes of action in relation to clinical effects of the drug as well as various formulations. The use of combinations with other drugs (e.g. paracetamol, codeine, caffeine) are critically assessed and the impact of natural products and Chinese Medicines on the safety of ibuprofen.

Leading researchers are specially invited to provide a complete understanding of a key topic within the multidisciplinary fields of physiology, biochemistry and pharmacology. In a form immediately useful to scientists, this periodical aims to filter, highlight and review the latest developments in these rapidly advancing fields.

The "Side Effects of Drugs Annual" was first published in 1977. It has been continually published since then as a yearly update to the voluminous encyclopedia, "Meyler's Side Effects of Drugs." Each new Annual continues to provide clinicians and medical investigators with a reliable and critical yearly survey of new data and trends in the area of adverse drug reactions and interactions. An international team of specialists has contributed to the informative Annual by critically interpreting it and by pointing to whatever is misleading.
Provides a critical yearly survey of new data and trendsSpecial reviews in this Annual include, among other topics, epidemiology of the use of ecstasy, paracetamol and the risk of asthma, combination vaccines/multiple immunizations, interactions of herbal medicines with warfarin, and tyrosine kinase inhibitors

Innovative approach to drug design that's more likely to result in an approvable drug product Retrometabolic drug design incorporates two distinct drug design approaches to obtain soft drugs and chemical delivery systems, respectively. Combining fundamentals with practical step-by-step examples, Retrometabolic Drug Design and Targeting gives readers the tools they need to take full advantage of retrometabolic approaches in order to develop safe and effective targeted drug therapies. The authors, both pioneers in the fields of soft drugs and retrometabolic drug design, offer valuable ideas, approaches, and solutions to a broad range of challenges in drug design, optimization, stability, side effects, and toxicity. Retrometabolic Drug Design and Targeting begins with an introductory chapter that explores new drugs and medical progress as well as the challenges of today's drug discovery. Next, it discusses: * Basic concepts of the mechanisms of drug action * Drug discovery and development processes * Retrometabolic drug design * Soft drugs * Chemical delivery systems Inside the book, readers will find examples from different pharmacological areas detailing the rationale for each drug design. These examples set forth the relevant pharmacokinetic and pharmacodynamic properties of the new therapeutic agents, comparing these properties to those of other compounds used for the same therapeutic purpose. In addition, the authors review dedicated computer programs that are available to support and streamline retrometabolic drug design efforts. Retrometabolic Drug Design and Targeting is recommended for all drug researchers interested in employing this newly tested and proven approach to developing safe and effective drugs.

"Pharmacogenomics: Challenges and Opportunities in Therapeutic Implementation" includes discussions and viewpoints from the academic, regulatory, pharmaceutical, clinical, socio-ethical and economic perspectives. Each chapter presents an overview of the potential or opportunity within the areas discussed and also outlines foreseeable challenges and limitations in moving pharmacogenomics into drug development and direct therapeutic applications. This edited book contains review questions for a more in-depth analysis of the implications of pharmacogenomics and discussion points to generate ideas on best to move the field forward. Clinical pearls and case studies are used to illustrate real-life experiences and both successful and unsuccessful applications. Tables, figures, and annotations are included throughout the book to facilitate understanding and further reference.
Multi-contributed book and chapters are written by contributors who are experts in their fieldProvides perspectives from those involved in all aspects of pharmacogenomics-including academic, regulatory, economic, industry and medical-to illustrate how all of the pieces fit together and where the challenges may beIncludes case studies of both successful and unsuccessful applications so readers can consider the potential and challenges in moving the science into drug development and direct therapeutic applicationsChapters contain discussion questions and clinical pearls and enable readers to reflect on how to move pharmacogenomics forward and apply these observations and useful tips to their own work and research

A companion website offers an elaboration on key points and discussion questions and provides patient case scenarios that illustrate how pharmacogenomics may be applied to a clinical setting

This book provides a comprehensive look at renal cell carcinoma, exploring its biology as well as current and future molecular targets for renal cancer carcinoma.

The goal for this volume is to provide an up-to-date review of the discriminative stimulus properties of major psychoactive drug classes with an emphasis on how this paradigm enhances our understanding of these drugs and how these findings translate from animals to humans. The drug discrimination paradigm applies to both drugs of abuse and drugs for treating mental illnesses, and research from these studies has provided immense translational value for learning about the mechanisms responsible for drug effects in humans.

International Cooperation, Convergence and Harmonization of Pharmaceutical Regulations: A Global Perspective provides the current status of the complex and broad phenomenon of cooperation, convergence and harmonization in the pharmaceutical sector (Part I), thoroughly evaluates its added value and its critical parameters and influencing factors (Part II) in order to recommend actions and measures to support the next steps for cooperation, convergence and harmonization (Part III). All of these recommendations in the book support the establishment of a better coordinated global pharmaceutical system which represents the best realistic alternative to fulfill the objective to establish a global coalition of regulators and to respond to an increased demand to further cooperation in the pharmaceutical sector. This proposed framework, which leverages all of the ongoing positive cooperation initiatives and uses as foundations all of the numerous harmonization projects developed over the years, presents advantages for all stakeholders and would definitively have significant added value to the promotion and protection of global public health.
The status of all major worldwide harmonization and cooperation initiatives (at bilateral, regional, and global levels)The value of cooperation in the pharmaceutical sector and the driving factors behind harmonizationThe proposition of a structure for the global pharmaceutical system and timely recommendations for enhancing international cooperation, as well as further discussion and policy changes in this area

Updated every five years, the series represents the optimal compromise between currency and a sufficient body of material for cohesive and comprehensive treatment in a monograph. Provides a quick yet thorough overview of the synthetic routines that have been used to access specific classes of therapeutic agents. Materials are organized by chemical class, and syntheses are taken back to available starting materials. Discusses disease state, rational for method of drug therapy, biological activities of each compound and preparation. Coverage also includes those generic pharmaceutical compounds not accorded clinical status. A glossary defines biological terms.

Recent findings have implied a distinct therapeutic potential for drugs targeting Transient Receptor Potential (TRP) channels in a wide variety of diseases, many with no existing satisfactory treatment options. Thus, the TRP superfamily of ion channels has attracted a great deal of well-deserved attention. TRP Channels in Drug Discovery provides a thorough collection of the most up-to-date reviews and protocols on the subject, coming from top experts in the field. Volume II presents a practical methodologies involving models for disorders of the cardiovascular system, the brain, skin, the metabolic system, as well as colitis, cancer, thermosensation, and musculoskeletal disorders. Written for the Methods in Pharmacology and Toxicology(t) series, this work includes the kind of detailed description and key implementation advice that ensures successful results in the lab. Comprehensive and cutting-edge, TRP Channels in Drug Discovery serves as an ideal reference for graduate students in academic laboratories as well as for pharmaceutical scientists developing new drugs and clinicians interested in novel drugs in the pipeline.

Edited by Kenneth A. Jacobson and Michael F. Jarvis
The roles of extracellular purines and pyrimidines in cellular homeostasis and disease etiology have come to be understood gradually over the past 40 years. However, due to the recent cloning and expression of receptors for ATP and adenosine, novel compounds have been developed with unique therapeutic potential for the treatment of thrombosis, stroke, epilepsy, chronic pain, immunological disorders, and cancer. As a result, the study of adenosine- and ATP-mediated responses in cellular regulation is entering a phase of opportunity and development unmatched since the days of serotonin receptor research in the 1970s.
The only definitive book on the topic, Purinergic Approaches in Experimental Therapeutics covers all of the major therapeutic applications of purinergic receptors and reflects the very latest developments in this new area of therapeutic research. Twenty-eight chapters, authored by an international group of contributors who are the leading authorities in the field, provide details on molecular pharmacology; medicinal chemistry; and therapeutic implications, including cardiology, metabolism, immunology, neurology, and cancer.
Among the topics covered:
* Purinergic Neurotransmission and Neuromodulation: A Historical Perspective
* Adenosine Receptor Subtypes: New Insights from Cloning and Functional Studies
* Modulators of Adenosine Uptake, Release, and Inactivation
* Cardiac Electrophysiology of Adenosine: Antiarrhythmic and Proarrhythmic Actions
* Purinergic Modulation of Gastrointestinal Function
* The Role of Adenosine in Asthma
* ATP in Brain Function
* ATP in the Treatment of Cancer

For researchers in pharmacology, physiology, molecular biology, and medicinal chemistry, Purinergic Approaches in Experimental Therapeutics heralds an exciting new era in the understanding of purinergic neurotransmission and the development of novel therapeutic modalities.

The large number of new antitumour antibiotics that have been discovered and evaluated since the first volume of "The Chemistry of Antitumour Antibiotics" was published in 1978 are described in this up-to-date work. It covers the results of mode and action studies which have benefitted from high-field NMR, including 2-D techniques, computer modelling and DNA sequencing methods. The volume also notes how biosynthesis has been helped by NMR to follow the incorporation of compounds containing stable isotopes.

This book provides new structural, biochemical, and clinical information on ABC transporters. The authors explore and describe the state of the art of research, knowledge, and prospects for the future for this important family of proteins. The first ABC transporter was discovered in 1973 and was named P-glycoprotein. It elicits resistance to cytotoxic drugs, chiefly in human tumours, within which chemotherapy failure is observed in about 50% of cases. Together with its complex pharmacology, and even a suspected role in Alzheimer's disease, this ABC transporter still eludes a clinical solution to its multidrug resistance property. ABC transporters are integral membrane active proteins and they belong to one of the largest protein families across all species. Their myriad roles encompass the import or export of a diverse range of allocrites, including ion, nutrients, peptides, polysaccharides, lipids, and xenobiotics. They are of major medical importance with many members elaborating multidrug resistance in bacteria, fungi, yeast, parasites, and humans. Other ABC transporters are involved in a number of inherited diseases, including cystic fibrosis, macular degeneration, gout, and several other metabolic disorders

Zacarias Leon's thesis describes the development and validation of analytical methods to estimate the processes set in motion by percutaneous absorption of UV filters in sunscreen cosmetic products. Leon describes these methods in both in vitro and non-invasive in vivo methodologies. Currently dermatologists recommend the use of sunscreen products not only under conditions of extreme exposure to the sun but also in daily situations. However the chemical compounds in these products contain may lead to undesired processes and cause induced toxicity, estrogenic effects and endocrine activity. Leon establishes methods to investigate these effects and provides valuable information on the undesired side effects associated with the use of UV filters found in sunscreen products. The work in this thesis has led to a number of publications in renowned analytical chemistry journals.

"Translational Neuroimaging: Tools for CNS Drug Discovery, Development and Treatment" combines the experience of academic, clinical and industrial neuroimagers in a unique collaborative approach to provide an integrated perspective of the use of small animal and human brain imaging in developing and validating translational models and biomarkers for the study and treatment of neuropsychiatric disorders. "Translational Neuroimaging: Tools for CNS Drug Discovery, Development and Treatment" examines the translational role of neuroimaging in model development from preclinical animal models, to human experimental medicine, and finally to clinical studies. The focus of this book is to identify and provide common endpoints between species that can serve to inform both the clinic and the bench with the information needed to accelerate clinically-effective CNS drug discovery. This book covers methodical issues in human and animal neuroimaging translational research as well as detailed applied examples of the use of neuroimaging in neuropsychiatric disorders and the development of drugs for their treatment. Offering an accompanying website with illustrations and text available for further knowledge and presentations, "Translational Neuroimaging: Tools for CNS Drug Discovery, Development and Treatment" appeals to non-clinical and clinical neuroscientists working in and studying neuropsychiatric disorders and their treatment as well as providing the novice researcher or researcher outside of his/her expertise the opportunity to understand the background of translational research and the use of imaging in this field.
Provides a background to translational research and the use of brain imaging in neuropsychiatric disordersCritical discussion of the potential and limitations of neuroimaging as a translational tool for identifying and validating biomarkersIdentifies cross species neurosystems and common endpoints necessary to help accelerate CNS drug discovery and development for the treatment of neuropsychiatric disordersFeatures an accompanying website with additional images and text

Obesity is an epidemic with enormous health, economic and social burdens. Current drugs for obesity treatment are far from ideal in terms of efficacy and side effects. Reviews in this volume of Progress in Molecular Biology and Translational Science summarize current status in studies of a number of G protein-coupled receptors that were shown to be promising targets for obesity treatments. Some of these receptors also cause monogenic obesity in humans.
Subject matter: obesity is an epidemic and G protein-coupled receptors are promising drug targets, with significant potential as new anti-obesity drugs.

Chapters are written by leading experts.