Bernard Testa – författare

Advances in Drug Research, Volume 20 focuses on the general themes of drug research and description of specific drug classes. This book is divided into four chapters. Chapter 1 discusses the extrapolation of toxicological and pharmacological data from animals to humans. The second chapter deals with the tissue binding of drugs, considering the relative ponderal importance of tissue versus blood macromolecules. The therapeutic use of plants and consumption of medicinal plants are elaborated in Chapter 3. The last chapter covers the field of histaminergic agonists and antagonists, describing breakthroughs such as H2-receptor antagonists, non-sedating H1-receptor antagonists, and H3-receptors. This publication is valuable to drug researchers and students interested in advances in drugs.

Advances in Drug Research, Volume 21 comprises three chapters that deal with the general subject, specific therapeutic class, and chemical family of diverse drugs. The first chapter of this book discusses the absorption and distribution of drugs in the lymphatic system. A presentation of the anti-infective quinolones is provided in Chapter 2, while the design and therapeutic potential of peptides are elaborated in Chapter 3. Other topics covered include lymphotropic carriers and the lymph uptake mechanism; basis of circulation in lymphatic transport of molecules through various routes of administration; and general aspects and characteristics of quinolone antibacterial agents. The mode of action and mechanisms of resistance of quinolones; potent agonists and antagonists of peptides; and inhibitors of atrial natriuretic factor-degrading enzymes are also deliberated in this text. This publication is valuable to drug researchers and students interested in advances in drugs.

Advances in Drug Research, Volume 22 focuses on the concepts and facts of drug research. This book is divided into four chapters. Chapter 1 discusses the use of atomic properties and atom-centered indices in QSAR models, while Chapter 2 describes the pharmacokinetics of peptides and proteins. The nuclear receptors, emphasizing the aspects of molecular and genomic pharmacology are elaborated in Chapter 3. The last chapter covers the medicinal chemistry of a vast group of agents acting on nuclear receptors. This publication is valuable to drug researchers and students interested in advances in drugs.

This volume comprises five authoritative reviews on timely topics in drug research. The first two chapters deal with chemotherapeutic agents (selective antiviral agents and cepham antibiotics) and subsequent chapters deal with the cardiovascular system and topics in neuropharmacology.

Each volume in this distinguished series presents authoritative reviews, both generally, on topics of broad interest in drug research, and specifically, on novel and established therapeutic classes. Acknowledged experts contribute in areas such as drug design, clinical and molecular pharmacology, drug metabolism, and mechanisms of action. Reviewers have consistently praised Advances in Drug Research for its comprehensive and lucid summaries of up-to-date knowledge.

Each volume in this distinguished series presents authoritative reviews on topics of broad interest in drug research and on novel and established therapeutic classes. Acknowledged experts contribute in areas such as drug design, clinical and molecular pharmacology, drug metabolism, and mechanisms of action. Reviewers have consistently praised Advances in Drug Research for its comprehensive and lucid summaries of up-to-date knowledge.

In keeping with the outstanding importance of lipophilicity in biosciences, this volume examines all its facets in more than twenty contributions from leading experts. It offers a thorough and highly topical survey of this rapidly developing field of research. Color plates demonstrating structural aspects, a vast number of references, and the straightforward presentation of the material make this volume a invaluable tool for all researchers involved in drug design or in the investigation of drug action.

Drug Bioavailability

In order to reach its intended site of action, the drug molecules in every pill that we swallow must first be absorbed, transported via the bloodstream and evade various mechanisms that eliminate drugs from the body. Those drug properties that determine, for example, its stability in the gut or its ease of uptake into the bloodstream, are therefore of central importance in drug development. In fact, many potentially useful drugs fail because of insufficient availability at the biological target site.

This second edition of the gold standard for industrial research is thoroughly revised in line with current trends in the field, with all contributions extensively updated or rewritten. No other publication offers the same level of treatment on this crucial topic.

In 22 chapters readers can benefit from the key working knowledge of today’s leading pharmaceutical companies, including Pfizer, AstraZeneca, and Roche. Drug developers from industry and academia present all the factors governing drug bioavailability, complete with practical examples and real-life data.

Part I focuses on solubility and gastrointestinal absorption, while the second discusses in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and solubility. Part III is devoted to metabolism and excretory mechanisms. The much revised and expanded Part IV surveys current in silico approaches to predict drug properties needed to estimate the bioavailability of any new drug candidate. The final part shows new drug development approaches as well as delivery strategies.

Indispensable for all those working in the pharmaceutical industry, pharmaceutical and medicinal chemists, and toxicologists.

This book aims to guide and inspire drug researchers as they enter the 21st century. Stereochemistry is an essential dimension in pharmacology and should be understood as such by all drug researchers whatever their background. When used as probes or medicines, stereoisomeric drugs offer invaluable insights or innovative therapeutic strategies. The book spans the subject from the molecular to the clinical. The first section on chemical aspects contains chapters on chemical synthesis, analysis, natural products, chiral stability (racemezation) and physical properties. The second section is on experimental pharmacology, with chapters on drug-receptor interactions, chiral recognition, ion channels, and molecular toxicology. The third section focuses on drug disposition, with chapters on absorption, distribution, protein binding, metabolism and elimination. The final section is dedicated to regulatory and clinical aspects.

This book aims to guide and inspire drug researchers as they enter the 21st century. Stereochemistry is an essential dimension in pharmacology and should be understood as such by all drug researchers whatever their background. When used as probes or as medicines, stereoisomeric drugs offer invaluable pharmacological insights or innovative therapeutic strategies.

State-of-the-Art Chirality Stereochemistry in general and chirality in particular have long been recog- nized as major structural factors influencing pharmacological activity and pharmacokinetic behavior. For more than a century, relevant information in these fields has been accumulating at an accelerating pace, leading to rationalizations, concepts and theories of increasing breadth and depth. Frequently, fundamental advances in stereochemical aspects of molecular pharmacology, drug disposition and pharmacochemistry have been translated into corresponding progress in clinical pharmacology and pharmacotherapy. There have been exceptions, however, since some extrapolations from the biochemical and in vitro situations to the in vivo human situation have proven premature. This notion resulted in the now appeased, but far from closed, debate regarding racemic versus enantiopure drugs, which saw some pro- ponents state that "in many cases, only one isomer contributes to the thera- peutic action while the other, the 'isomeric ballast', only contributes to the side effects and toxicity" (ARIENS 1986,1989,1992).Other authors, in contrast, have cautioned against hasty generalizations and advocated a more pragmatic, case- by-case and evidence-based view (CALDWELL 1995; DE CAMP 1989; SZELENYI et al. 1998; TESTA 1991; TESTA and TRAGER 1990; TESTA et al. 1993).

Drug Bioavailability In order to reach its intended site of action, the drug molecules in every pill that we swallow must first be absorbed, transported via the bloodstream and evade various mechanisms that eliminate drugs from the body. Those drug properties that determine, for example, its stability in the gut or its ease of uptake into the bloodstream, are therefore of central importance in drug development. In fact, many potentially useful drugs fail because of insufficient availability at the biological target site. This second edition of the gold standard for industrial research is thoroughly revised in line with current trends in the field, with all contributions extensively updated or rewritten. No other publication offers the same level of treatment on this crucial topic. In 22 chapters readers can benefit from the key working knowledge of today’s leading pharmaceutical companies, including Pfizer, AstraZeneca, and Roche. Drug developers from industry and academia present all the factors governing drug bioavailability, complete with practical examples and real-life data. Part I focuses on solubility and gastrointestinal absorption, while the second discusses in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and solubility. Part III is devoted to metabolism and excretory mechanisms. The much revised and expanded Part IV surveys current in silico approaches to predict drug properties needed to estimate the bioavailability of any new drug candidate. The final part shows new drug development approaches as well as delivery strategies. Indispensable for all those working in the pharmaceutical industry, pharmaceutical and medicinal chemists, and toxicologists.