Azapropazone

Azapropazone is a chemically unique non-steroidal anti-inflammatory drug (benzotriazine oxide) which has found successful clinical applications in the therapy of a wide variety of arthritic conditions. This book summarizes the progress and critically reviews the clinical use and experimental studies since its introduction 20 years ago. Several studies focus on the physiochemical, pharmacological and toxico logical properties of this drug. The studies suggest that it has some unique properties compared with other non-steroidal anti-inflammatory drugs. Among these the novel observations are that azapropazone inhibits several non-prostaglandin-related leucocyte functions, especially superoxide anion production. These serve as a basis for investigations which are reviewed showing the potential for the drug to prevent the pathological consequencies of myocardial ischaemia. The preparation of this book would not have been possible without the cooperation of the four companies who produce, market, or have research involvement with azapropazone, namely Siegfried AG (the manufacturers of the drug), A.H. Robins (U.K.) Co. Ltd., Robapharm AG (Switzerland) and E.!. duPont de Nemours (U.S.A., Switzerland and F.R.G.).

Inhalt
Section I Experimental.- 1 Introduction to therapy with azapropazone.- 2 The chemical classification of azapropazone.- 3 Survey of toxicological investigations of azapropazone.- 4 The mode of action of azapropazone in relation to its therapeutic actions in rheumatic conditions and its major side-effects.- 5 Pharmacokinetic properties of azapropazone in comparison to other NSAIDs.- 6 The pharmacokinetics of azapropazone.- 7 Mathematical model for assessing risk of gastrointestinal reactions to NSAIDs.- 8 Reduction of irreversible injury in animal models of myocardial ischaemia by treatment with azapropazone.- 9 Dual inhibitory effects of azapropazone on both neutrophil migration and function: relation to cardiovascular function.- 10 Aspects of clinical pharmacology and bioavailability of azapropazone.- 11 Immunochemical studies on azapropazone.- Section II Therapeutic Actions.- 12 Untersuchungen zur Arthrose [Studies in osteoarthritis].- 13 Studies on gout and urate elimination by azapropazone.- 14 Die Analgetische Wirksamkeit von Azapropazon [Analgesic effects of azapropazone].- 15 Überblick über die Anwendung von Azapropazon nach operativen Eingriffen und bei traumatisierten Patienten [Review of application of azapropazone in post-operative and traumatic conditions].- 16 Clinical trial methodology in rheumatoid arthritis: azapropazone studies.- 17 Comparative effects of azapropazone on the progression of joint pathology on osteoarthritis.- 18 Serious gastrointestinal reactions to azapropazone: an estimate of the risk.- 19 Tolerance of azapropazone: allergic and pseudo-allergic reactions and comparison with other NSAIDs.- 20 Haematological reactions.- 21 Epilogue, with some thoughts for research on azapropazone.