Improved Non-Steroid Anti-Inflammatory Drugs: COX-2 Enzyme Inhibitors PDF Download
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Author: Sir John R. Vane
Publisher: Springer Science & Business Media
ISBN: 9401090297
Category : Medical
Languages : en
Pages : 249
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Book Description
In 1971, Vane proposed that the mechanism of action of the aspirin-like drugs was through their inhibition of prostaglandin biosynthesis. Since then, there has been intense interest in the interaction between this diverse group of inhibitors and the enzyme known as cyclooxygenase (COX). It exists in two isoforms, COX-l and COX-2 (discovered some 5 years ago). Over the last two decades several new drugs have reached the market based on COX-l enzyme screens. Elucidation of the three-dimensional structure of COX-l has provided a new understanding for the actions of COX inhibitors. The constitutive isoform of COX, COX-l has clear physiological functions. Its activation leads, for instance, to the production of prostacyclin which when released by the endothelium is anti-thrombogenic and anti-atherosclerotic, and in the gastric mucosa is cyto protective. COX-l also generates prostaglandins in the kidney, where they help to maintain blood flow and promote natriuresis. The inducible isoform, COX-2, was discovered through its activity being increased in a number of cells by pro inflammatory stimuli. A year or so later, COX-2 was identified as a distinct isoform encoded by a different gene from COX-I. COX-2 is induced by inflammatory stimuli and by cytokines in migratory and other cells. Thus the anti-inflammatory actions of non-steroid anti-inflammatory drugs (NSAIDs) may be due to the inhibition of COX-2, whereas the unwanted side-effects such as irritation of the stomach lining and toxic effects on the kidney are due to inhibition of the constitutive enzyme, COX-I.
Author: Sir John R. Vane
Publisher: Springer Science & Business Media
ISBN: 9401090297
Category : Medical
Languages : en
Pages : 249
Get Book Here
Book Description
In 1971, Vane proposed that the mechanism of action of the aspirin-like drugs was through their inhibition of prostaglandin biosynthesis. Since then, there has been intense interest in the interaction between this diverse group of inhibitors and the enzyme known as cyclooxygenase (COX). It exists in two isoforms, COX-l and COX-2 (discovered some 5 years ago). Over the last two decades several new drugs have reached the market based on COX-l enzyme screens. Elucidation of the three-dimensional structure of COX-l has provided a new understanding for the actions of COX inhibitors. The constitutive isoform of COX, COX-l has clear physiological functions. Its activation leads, for instance, to the production of prostacyclin which when released by the endothelium is anti-thrombogenic and anti-atherosclerotic, and in the gastric mucosa is cyto protective. COX-l also generates prostaglandins in the kidney, where they help to maintain blood flow and promote natriuresis. The inducible isoform, COX-2, was discovered through its activity being increased in a number of cells by pro inflammatory stimuli. A year or so later, COX-2 was identified as a distinct isoform encoded by a different gene from COX-I. COX-2 is induced by inflammatory stimuli and by cytokines in migratory and other cells. Thus the anti-inflammatory actions of non-steroid anti-inflammatory drugs (NSAIDs) may be due to the inhibition of COX-2, whereas the unwanted side-effects such as irritation of the stomach lining and toxic effects on the kidney are due to inhibition of the constitutive enzyme, COX-I.
Author: Sir John R. Vane
Publisher: Springer Science & Business Media
ISBN: 9401148724
Category : Medical
Languages : en
Pages : 153
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Book Description
The mainstay of therapy for rheumatoid disease is the non-steroid antiinflammatory drugs (NSAIDs), despite their inherent gastrointestinal toxicity and ability to cause renal damage in susceptible patients. The theory that the beneficial and toxic effects of NSAIDs stem from a reduction in prostanoid production through inhibition of cyclooxygenase implied that particular toxicities were inevitable with NSAIDs and would always be correlated with efficacy. However, over the years, it became apparent that at therapeutic doses, some NSAIDs had greater toxic side-effects than others, a fact not explained by the general theory. A significant clarification arose from the discovery that there are two distinct isoforms of COX, a constitutive enzyme (COX-I) responsible for the production of prostanoids necessary for platelet aggregation and protection of the gastric mucosa and kidney; and an inducible enzyme (COX-2) that is newly synthesized at sites of tissue damage and produces prostaglandins that manifest pathological effects. It became clear that different NSAIDs had greater or lesser effects on COX-I when used in therapeutic doses, explaining the variation in side-effects. ' The elucidation of the crystal structure of these different enzymes and the skills of medicinal chemists have led to the synthesis of new chemicals with a selectivity for the inducible enzyme, and thus with therapeutic efficacy without those toxic effects result ing from inhibition of the constitutive enzyme.
Author: Raymond S. Sinatra
Publisher: Cambridge University Press
ISBN: 0521874912
Category : Medical
Languages : en
Pages : 729
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Book Description
This textbook provides an overview of pain management useful to specialists as well as non-specialists, surgeons, and nursing staff.
Author: C.N. Serhan
Publisher: Springer Science & Business Media
ISBN: 9783540667476
Category : Science
Languages : en
Pages : 300
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Book Description
Over the last few years, we have witnessed tremendous progress in the field of eicosanoids and their therapeutic applications. Receptor an tagonists for leukotrienes have been tested as anti-inflammatories and are on the market as a treatment for asthma. Receptor agonists for pro stacyclin are being tested for the treatment of peripheral vascular dis ease, and selective inhibitors of cyclooxygenase type II were just ap proved for the treatment of rheumatoid arthritis. All these developments are the culmination of many years and man-hours of careful research. The field has now entered an upswing that will result in novel thera peutic applications within the next 10 years. New molecules and me diators have been identified, new enzymes and pathways elucidated and new therapeutic approaches have emerged. The concept of ei cosanoids as "pro-inflammatory" molecules is being challenged, and their role as regulators is increasingly recognized. In fact, some of these molecules may be important endogenous anti-inflammatory agents.
Author: Alex S. Evers
Publisher: Cambridge University Press
ISBN: 1139497022
Category : Medical
Languages : en
Pages : 2902
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Book Description
In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.
Author: Derek G. Waller
Publisher: Elsevier Health Sciences
ISBN: 0702055034
Category : Medical
Languages : en
Pages : 741
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Book Description
This book covers all the pharmacology you need, from basic science pharmacology and pathophysiology, through to clinical pharmacology to therapeutics, in line with the integrated approach of new medical curricula. The first section covers the basic principles, and the rest is organised by body systems. The book ends with sections on toxicity and prescribing practice. Integrates basic science pharmacology, clinical pharmacology and therapeutics Brief review of pathophysiology of major diseases Case histories and multiple choice questions (and answers) Tabular presentation of all common drugs within each class Section on further reading Kinetics chapter simplified with more practical examples Includes more on genetic issues Drug tables made more concise to make information more accessible Fully updated to reflect current clinical practice
Author: John R. Vane
Publisher: Lippincott Williams & Wilkins
ISBN: 9780412323706
Category : Medical
Languages : en
Pages : 613
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Book Description
Author: Angel Lanas
Publisher: Springer
ISBN: 3319338897
Category : Medical
Languages : en
Pages : 271
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Book Description
This volume is a state-of-the art resource on the recent advances and clinical management of NSAIDs and aspirin. The text provides a thorough overview of NSAIDS and aspirin, reviewing such topics as pharmacology and mechanisms, clinical effects, and the safety and efficacy of these drugs. It also focuses on the effect of the drugs on the cardiovascular system and in the prevention of GI cancer. Practical recommendations for a safe prescription of NSAIDs are also included. Written by experts in the field, NSAIDs and Aspirin: Recent Advances and Implications for Clinical Management is a comprehensive text of great value to gastroenterologists, rheumatologists, cardiologists, oncologists, orthopedists, trauma and internal medicine specialists.
Author: Colin Pinnock
Publisher: Cambridge University Press
ISBN: 9780521690799
Category : Medical
Languages : en
Pages : 990
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Book Description
The second edition of Fundamentals of Anaesthesia builds upon the success of the first edition, and encapsulates the modern practice of anaesthesia in a single volume. Written and edited by a team of expert contributors, it provides a comprehensive but easily readable account of all of the information required by the FRCA Primary examination candidate and has been expanded to include more detail on all topics and to include new topics now covered in the examination. As with the previous edition, presentation of information is clear and concise, with the use of lists, tables, summary boxes and line illustrations where necessary to highlight important information and aid the understanding of complex topics. Great care has been taken to ensure an unrivalled consistency of style and presentation throughout.
Author: Charles E. Argoff
Publisher: Elsevier Health Sciences
ISBN: 0323074650
Category : Medical
Languages : en
Pages : 408
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Book Description
No matter what questions arise in practice or while preparing for boards, Pain Management Secrets, 3rd Edition has the answers. A two-color page layout, portable size, and a list of the “Top 100 Secrets in pain management help you better meet the challenges you face today. You’ll find all the features you rely on from the Secrets Series®—a question-and-answer format, lists, mnemonics, tables and an informal tone—that make reference fast and easy. Expedites reference and review with a question-and-answer format, bulleted lists, mnemonics, and practical tips from the authors. Features a two-color page layout, "Key Points" boxes, and lists of useful web sites to enhance your reference power. Presents a chapter containing "Top 100 Secrets", providing you with an overview of essential material for last-minute study or self-assessment. Fits comfortably in the pocket of your lab coat so you have it conveniently on hand at all times. Features new editors, Charles E. Argoff, MD and Gary McCleane, MD who present a thorough update on the latest in pain management. Presents a new contemporary internal design that helps you navigate the text easier.
