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Antitargets and Drug Safety (Methods and Principles in Medicinal Chemistry #66)

With its focus on emerging concerns of kinase and GPCR-mediated antitarget effects, this vital reference for drug developers addresses one of the hot topics in drug safety now and in future. Divided into three major parts, the first section deals with novel technologies and includes the utility of adverse event reports to drug discovery, the translational aspects of preclinical safety findings, broader computational prediction of drug side-effects, and a description of the serotonergic system. The main part of the book looks at some of the most common antitarget-mediated side effects, focusing on hepatotoxicity in drug safety, cardiovascular toxicity and signaling effects via kinase and GPCR anti-targets. In the final section, several case studies of recently developed drugs illustrate how to prevent anti-target effects and how big pharma deals with them if they occur. The more recent field of systems pharmacology has gained prominence and this is reflected in chapters dedicated to the utility in deciphering and modeling anti-targets. The final chapter is concerned with those compounds that inadvertently elicit CNS mediated adverse events, including a pragmatic description of ways to mitigate these types of safety risks. Written as a companion to the successful book on antitargets by Vaz and Klabunde, this new volume focuses on recent progress and new classes, methods and case studies that were not previously covered.

Antitargets and Drug Safety (Methods and Principles in Medicinal Chemistry #66)

With its focus on emerging concerns of kinase and GPCR-mediated antitarget effects, this vital reference for drug developers addresses one of the hot topics in drug safety now and in future. Divided into three major parts, the first section deals with novel technologies and includes the utility of adverse event reports to drug discovery, the translational aspects of preclinical safety findings, broader computational prediction of drug side-effects, and a description of the serotonergic system. The main part of the book looks at some of the most common antitarget-mediated side effects, focusing on hepatotoxicity in drug safety, cardiovascular toxicity and signaling effects via kinase and GPCR anti-targets. In the final section, several case studies of recently developed drugs illustrate how to prevent anti-target effects and how big pharma deals with them if they occur. The more recent field of systems pharmacology has gained prominence and this is reflected in chapters dedicated to the utility in deciphering and modeling anti-targets. The final chapter is concerned with those compounds that inadvertently elicit CNS mediated adverse events, including a pragmatic description of ways to mitigate these types of safety risks. Written as a companion to the successful book on antitargets by Vaz and Klabunde, this new volume focuses on recent progress and new classes, methods and case studies that were not previously covered.

Antithrombin — Diagnostik und Therapie

Die Indikation zur Substitution von Antithrombin wird nach wie vor kontrovers diskutiert. Experten aus verschiedenen Fachgebieten (Innere Medizin, Chirurgie, Transfusions- und Labormedizin) vermitteln einen aktuellen Überblick über den Stand der Antithrombin-Therapie. Auf Basis der Referate, der Diskussion und der Meta-Analyse gelang es, ein "State of the Art" und einen Konsens für den Einsatz von Antithrombin zu erarbeiten. Die Workshop-Teilnehmer wollen diese Ausarbeitung als Leitlinie und Orientierungshilfe verstanden wissen.

Antithrombotic Drug Therapy in Cardiovascular Disease (Contemporary Cardiology)

Substantial morbidity and mortality remains associated with thrombotic events has stimulated the rapid expansion of the available armamentarium to combat pathologic thrombosis. Pathologic thrombosis plays an essential role in the pathogenesis of acute coronary syndromes (ACS), ischemic complications of percutaneous coronary intervention (PCI), venous thromboembolic disease, and embolic complications of arrhythmias and various cardiomyopathies. Written by experts in the field, Antithrombotic Drug Therapy in Cardiovascular Disease carefully examines individual and various combinations of the available antithrombotic regimens including fibrinolytic agents, antiplatelet therapies (aspirin, thieneopyridines, glycoprotein IIb/IIIa inhibitors), and anticoagulant therapies (unfractionated heparin, low-molecular-weight heparins, direct thrombin inhibitors, and synthetic factor X inhibitors), non-ST-segment elevation (NSTE) ACS and ST-segment elevation myocardial infarction (STEMI). A detailed overview, Antithrombotic Drug Therapy in Cardiovascular Disease presents the evidence demonstrating the efficacy of available antithrombotic therapies in specific disease states such as atrial fibrillation, cardiomyopathy, valvular heart disease, and heparin-induced thrombocytopenia (HIT).

Antithrombotic Drugs in Thrombosis Models

Antithrombotic Drugs in Thrombosis Models presents a critical review of the use of thrombosis models and an original, highly sensitive methodology for testing antithrombotics based on a more adequate understanding of thrombotic processes. The methods form an integrated system stressing particularly the plurifactorial and global character of thrombosis and the key role of a generalized mild endothelial lesion. Packed with illustrations, this book documents the effectiveness of the system through the screening of a series of acknowledged and potential antithrombotics, and includes a unique study of their mutual combinations. Special emphasis is placed on the importance of biomodels for preliminary testing of antithrombotics. This book is particularly useful to researchers in pharmacology and the pharmaceutical industry; however, those interested in drug research and the field of cardiovascular medicine will benefit as well.

Antithrombotic Drugs in Thrombosis Models

Antithrombotic Drugs in Thrombosis Models presents a critical review of the use of thrombosis models and an original, highly sensitive methodology for testing antithrombotics based on a more adequate understanding of thrombotic processes. The methods form an integrated system stressing particularly the plurifactorial and global character of thrombosis and the key role of a generalized mild endothelial lesion. Packed with illustrations, this book documents the effectiveness of the system through the screening of a series of acknowledged and potential antithrombotics, and includes a unique study of their mutual combinations. Special emphasis is placed on the importance of biomodels for preliminary testing of antithrombotics. This book is particularly useful to researchers in pharmacology and the pharmaceutical industry; however, those interested in drug research and the field of cardiovascular medicine will benefit as well.

Antithrombotic Therapy in Prevention of Ischemic Stroke (Oxford American Pocket Notes)

Stroke is the most common cause of adult mortality in the United States. Antithrombotic agents form the mainstay of stroke prevention. Aspirin produces a modest reduction in the risk of second stroke and transient ischemic attack (TIA, mini-stroke) and is widely recommended for initial therapy. The thienopyridines (Ticlid) and clopodogrel (Plavix) are alternatives for secondary prevention in patients who do not respond to or cannot take aspirin. They are no more effective than aspirin and have been associated with thrombotic thrombocytopenic purpura. The combination of aspirin and extended-release dipyridamole (Aggrenox) has several mechanisms of action and an additive effect on reducing stroke risk compared with either agent alone. A 2-fold increase in risk reduction and favorable safety profile suggest that the combination can serve as first-line prophylaxis against a second stroke. This volume, as part of the Oxford American Pocket Note series, provides the clinician wtih up-to-date information on the guidelines, and therapeutic options in recurrent stroke/TIA prevention. Useful features include treatment algorithms, illustrations, medication tables, charts and figures to enable both the specialist and the primary provider to ensure the best options to their patients in order to prevent the reocurrence of stroke/TIA.

Antithrombotics: Pathophysiological Rationale for Pharmacological Interventions (Developments in Cardiovascular Medicine #126)

Antithrombotics (Handbook of Experimental Pharmacology #132)

An up-to-date overview of blood coagulation, hemostatis, and thrombosis, this volume also provides a state-of-the-art report of current anti-thrombotic and anti-coagulant strategies as well as a summary of current research interest in the area and potential future targets. It attempts to balance traditional pharmacology with the newer sciences of molecular biology and in so doing, sets a framework for future advances in the field. The book is a concise, current and useful reference for the basic researcher as well as the practicing physician working in the fields of cardiology, internal medicine or surgery.

Antitrust in Pharmaceutical Markets & Geographical Rules of Origin (LIDC Contributions on Antitrust Law, Intellectual Property and Unfair Competition)

This book gathers international and national reports from across the globe on key questions in the field of antitrust and intellectual property.The first part discusses the application of competition law in the pharmaceutical sector, which continues to be a focus for anti-trust authorities around the world. A detailed international report explores the extent to which the application of the competition rules in the pharmaceutical sector should be affected by the specific characteristics of those products and markets (including consumer protection rules, the need to promote innovation, the need to protect public budgets, and other public interest considerations). It provides an excellent comparative study of this complex subject, which lies at the interface between competition law and intellectual property law.The second part of the book gathers contributions from various jurisdictions on the topic of “What rules should govern claims by suppliers about the national or geographic origin of their goods or services?” This section presents an international report, which offers an unparalleled comparative analysis of this topic, bringing together common themes and contrasting the various national provisions dealing with indications of origin, amongst other things.The book also includes the resolutions passed by the General Assembly of the International League of Competition Law (LIDC) following a debate on each of these topics, which include proposed solutions and recommendations. The LIDC is a long-standing international association that focuses on the interface between competition law and intellectual property law, including unfair competition issues.

Antituberculosis Drugs (Handbook of Experimental Pharmacology #84)

This volume deals specifically with those antituberculosis drugs which passed the preclinical phase and have been or are used in the treatment of tuberculosis and other mycobacterial diseases (except leprosy) in at least some parts of the world. Despite this restriction, there are 14 such drugs, and as a result this volume has reached rather large proportions. To prevent it from becoming even larger and more unwidely, most derivatives of antituberculotics have been omitted, especially where it is claimed that they provide only better bioavailibility or tolerability. Only in the chapter on the chemotherapy of diseases due to so-called atypical mycobacteria is the clinical use of the drugs described to a certain extent. In addition to antituberculotics, also discussed are antimicrobials which have been found to be effective against these mycobacteria. The sequence in which the drugs are described is historical, reflecting not the time of discovery but rather the first clinical application. This order was selected for reasons which are now no longer relevant. In this volume less emphasis is placed on detection, biological or synthetic production of antituberculotics, and structure-activity relationships. In contrast, emphasis is put on the degree, type, and mechanism of antimyco bacterial activity, pharmacokinetics, and biotransformation in animals and man, on experimental pharmacodynamics, and on the toxicity of antituberculotics used therapeutically.

Antitumor Antibiotics (Recent Results in Cancer Research #63)

The scientific collaboration between the United States and Japan in the field of cancer goes back many years. In this successful international collaboration cancer chemotherapy has been one of the most productive areas. Pioneers such as YOSHIDA, UMEZAWA, SHEAR, and GOLDIN established firm links of mutual trust and respect in the period after the Second Great War. Japanese drugs, such as mitomycin C and bleomycin have become mainstays of clinical oncology in the U. S. and throughout the world. Many drugs developed in the U. S. have become established in Japanese cancer therapy. Within the cancer chemotherapy field the antitumor antibiotics rank as one of the most important groups. In the U . S. -J apanese collaboration this group of drugs has taken the paramount role. The Japanese, under the leadership of U mezawa, are considered to be among the most innovative and productive in this area which has also had great emphasis in the United States as part of the National Cancer Institute's drug development program and in the pharmaceutical industry. This extended collaboration in general oncology, and chemotherapy in particular, has received increased impetus by and support from the official U . S. -J apan Joint Agreement on cancer research, which was established in 1974 between the National Cancer Institute and the Japanese Society for the Promotion of Science. One of the subsections of this agreement is cancer therapy with emphasis on chemotherapy.

Antitumor Drug Resistance (Handbook of Experimental Pharmacology #72)

The study of tumour resistance to anticancer drugs has been the subject of many publications since the initial discovery of the phenomenon by J. H. Burchenal and colleagues in 1950. Many papers have been published since then reporting development of resistance to most of the well-known anticancer agents in many different animal tumour systems, both in vivo and in vitro. Many different mechanisms of resistance have been described, and it is clear that the tumour cell has a wide diversity of options in overcoming the cell-killing activity of these agents. Definition of the magnitude of the phenomenon in the clinic is, however, much more problematical, and it is with this in mind that the initial chapter, seeks to out­ line the problem as the clinicians see it. It appears that the phenomenon of true resistance to a drug, as the biochemist would recognise it, is an important cause of the failure which clinicians experience in treating the disease. The extent of the contribution of this phenomenon to the failure of treatment cannot easily be evaluated at the present time, but it is hoped that the development and application of new and more sophisticated techniques for the analysis of cellular sub­ populations may help to give a more exact estimate and to shed some light on the causes of failure of many of the present therapeutic techniques.

Antitumor Potential and other Emerging Medicinal Properties of Natural Compounds

The modern unhealthy diet and lifestyle in conjunction with pathogens, environmental carcinogens and multiple other risk factors increase humans’ susceptibility to different diseases exemplified by elevated levels of cancers, cardiovascular and communicable diseases. Screening of potential drugs from medicinal plants and animals provides a promising strategy for the alleviation of the impact of these diseases. Components with potential medicinal applications include RIPs, RNases, lectins, protease inhibitors and numerous small compounds. These compounds have shown both preventive and therapeutic effects for humans. This book is a compilation of articles written by internationally renowned experts exploring the different uses of medicinal compounds in human therapeutics. Here we provide a comprehensive outlook on both qualitative and quantitative studies focusing on medicinal plants and animals, and establishing a link between laboratory research discovery and clinical applications.

Antitumour and Antiviral Substances of Natural Origin (Recent Results in Cancer Research #28)

Antivaccination and Vaccine Hesitancy: A Professional Guide to Foster Trust and Tackle Misinformation

This important book provides a comprehensive guide to understanding vaccine hesitancy, as well as the nuances of antivaccination claims. It is designed to give clinicians and other professionals targeted information to help them address vaccine hesitancy and antivaccination claims, as well as ways of responding to immunisation concerns. Alongside the scientific facts around vaccinations, it considers the historical foundations of modern vaccine scepticism, while offering key insights into the psychology behind vaccine hesitancy and the factors which influence an individual’s decision-making. Separating fact from fiction, the book explores the most well-known antivaccine myths, many of which proliferate online, uncovering ways that counter-vaccine narratives can influence audiences. Importantly, it also outlines the most effective strategies to address both doubts and misinformation, detailing five general principles to improve communications, with tips and guidance to debunk false claims or provide assurance in the face of immunisation doubts. This is essential reading for anyone wishing to really understand the phenomenon of vaccine hesitancy, whether professional, student or general reader, and the methods that can be used to challenge misinformation.

Antivaccination and Vaccine Hesitancy: A Professional Guide to Foster Trust and Tackle Misinformation

This important book provides a comprehensive guide to understanding vaccine hesitancy, as well as the nuances of antivaccination claims. It is designed to give clinicians and other professionals targeted information to help them address vaccine hesitancy and antivaccination claims, as well as ways of responding to immunisation concerns. Alongside the scientific facts around vaccinations, it considers the historical foundations of modern vaccine scepticism, while offering key insights into the psychology behind vaccine hesitancy and the factors which influence an individual’s decision-making. Separating fact from fiction, the book explores the most well-known antivaccine myths, many of which proliferate online, uncovering ways that counter-vaccine narratives can influence audiences. Importantly, it also outlines the most effective strategies to address both doubts and misinformation, detailing five general principles to improve communications, with tips and guidance to debunk false claims or provide assurance in the face of immunisation doubts. This is essential reading for anyone wishing to really understand the phenomenon of vaccine hesitancy, whether professional, student or general reader, and the methods that can be used to challenge misinformation.

Antiviral Agents: Advances and Problems (Progress in Drug Research #002)

Antiviral Agents, Vaccines, and Immunotherapies

Unlike any other source on the subject, Antiviral Agents, Vaccines, and Immunotherapies analyzes the benefits and limitations of every available drug, vaccine, and immunotherapy utilized in the prevention and control of viral diseases. This reference provides in-depth reviews of more than 50 drugs and antiviral agents for HIV, human herpesviruses,

Antiviral Chemotherapy 4: New Directions for Clinical Application and Research (Advances in Experimental Medicine and Biology #394)

The three years since our last conference in San Francisco have again seen a dramatic expansion of the number of antivirals either licensed or in the late stages of clinical trials. d4T is now licensed for HIV infection, famciclovir and the oral pro-drug of acyclovir, valacyclovir, are now licensed for VZV infections in some countries. Moreover. oral ganciclovir, cidofovir, and sorivudine are not far behind. Clinical trials with the second-site reverse transcriptase inhibitors and the protease inhibitors for HlV infection are proceeding rapidly and on a broad scale, and the preliminary results would suggest that several of these classes of drugs will be licensed as well. Despite this optimism, however, there is increasing evidence that antiviral-resistant strains of pathogenic viruses will be a significant problem, perhaps especially with therapy of HIV infection, and there remains a desperate need for improved drugs (with either improved efficacy or decreased toxicity, or both) for CMV and HIV infections. This book is the edited proceedings of the Fourth Triennial Conference on Antiviral Chemotherapy, held in San Francisco, in November 1994. The conference was sponsored by the University of California, San Francisco, and co-sponsored by the International Society for Antiviral Research (ISAR), the Macfarlane Burnet Centre for Medical Research in Melbourne, Australia, and the Australian National Centre for HIV Virology Research. The conference had been organized to present an overview of the field of antiviral chemotherapy.

Antiviral Chemotherapy 5: New Directions for Clinical Application and Research (Advances in Experimental Medicine and Biology #458)

Scientists and clinicians attending the last "New Directions in Antiviral Therapy" conference in late 1994 could hardly have predicted the revolution in the management of patients with HIV infection that has occurred since. Two new classes of antiretrovirals have been licensed, the second-site RT inhibitors and the protease inhibitors; the long in­ cubation period of active HIV infection, when the infection is clinically latent, is now un­ derstood to be a period of intense viral replication and turnover of CD4 lymphocytes; measurements of HI V RNA concentration in plasma have been shown to be essential tools for monitoring the course of HIV infection, deciding when to treat, and assessing the re­ sults of treatment; and finally, combinations of antiretrovirals, particularly combinations including protease inhibitors, have been shown to have dramatically beneficial effects on patients with HIV infection. These advances, coupled with new drugs for the management of herpesvirus infections, have made dramatic differences in the quality and length of life of HIV-infected patients. Additional advances have been made since 1994 in the prevention or management of influenza virus (zanamavir), respiratory syncytial virus (palvizumab), hepatitis B virus (lamivudine and famciclovir), and enterovirus infections (pleconaril). It is difficult to re­ member that only slightly more than a decade ago there were only a handful of antiviral agents available (none of which were antiretrovirals), and a number of those were either highly toxic, of dubious efficacy, or both.

Antiviral Drug Development: A Multidisciplinary Approach (Nato Science Series A: #143)

Antiviral Drug Discovery and Development (Advances in Experimental Medicine and Biology #1322)

This book summarizes state-of-the-art antiviral drug design and discovery approaches starting from natural products to de novo design, and provides a timely update on recently approved antiviral drugs and compounds in advanced clinical development. Special attention is paid to viral infections with a high impact on the world population or highly relevant from the public health perspective (HIV, hepatitis C, influenza virus, etc.). In these chapters, limitations associated with adverse effects and emergence of drug resistance are discussed in detail. In addition to classical antiviral strategies, chapters will be dedicated to discuss the non-classical drug development strategies to block viral infection, for instance, allosteric inhibitors, covalent antiviral agents, or antiviral compounds targeting protein–protein interactions. Finally, current prospects for producing broad-spectrum antiviral inhibitors will be also addressed. The book is distinctive in providing the most recent update in the rapidly evolving field of antiviral therapeutics. Authoritative reviews are written by international scientists well known for their contributions in their topics of research, which makes this book suitable for researchers not only within the antiviral research community but also attractive to a broad audience in the drug discovery field. This book covers molecular structures and biochemical mechanisms mediating the antiviral effects, while discussing various ligand design strategies, which include traditional medicinal chemistry, computational chemistry, and chemical biology approaches. The book provides a comprehensive review of antiviral drug discovery and development approaches, particularly focusing on current innovations and future trends.

Antiviral Drug Discovery for Emerging Diseases and Bioterrorism Threats

Antiviral Drug Discovery gives readers a cutting-edge view of how chemical concepts are being mobilized to develop novel approaches that will effectively confront emerging diseases and biowarfare. Among the many topics discussed are smallpox, the Ebola virus, influenza, SARS, arenaviruses and flaviviruses. Each chapter discusses hypothetical strategies for the discovery of relevant antiviral agents, recent findings related to biochemistry or drug discovery, and advances in the further development of established leads in the area. Timely and informative, this book clearly delineates the efforts being made to develop new and effective broad-spectrum antiviral agents.

Antiviral Drug Strategies (Methods and Principles in Medicinal Chemistry #50)

By focusing on general molecular mechanisms of antiviral drugs rather than therapies for individual viruses, this ready reference provides the critical knowledge needed to develop entirely novel therapeutics and to target new viruses. It begins with a general discussion of antiviral strategies, followed by a broad survey of known viral targets, such as reverse transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, as well as their known inhibitors. The final section contains several cases studies of recent successful antiviral drug development. Edited by Erik de Clercq, the world authority on small molecule antiviral drugs, who has developed more new antivirals than anyone else.