Aspirin and the Salicylates

Abbreviations and Nomenclature 1 History and Development of the Salicylates Early Use of Salicylate-Containing Plants Hippocratic Era Roman and Greek Medicine Asia and America European Middle Ages Nineteenth Century Chemical Developments Isolation and Purification of Salicylic Acid Synthesis and Commercial Development of Aspirin (Acetylsalicylic Acid) Other Salicylates 2 Occurrence, Properties and Synthetic Developments of the Salicylates Naturally Occurring Salicylates Commercial Synthesis And Properties of The Salicylates Salicylic and Acetylsalicylic Acids, Their Salts and Esters Salicylamide Salicylate Derivatives Experimental Drugs 3 Methylsalicylic Acid Aspirin Anhydride Dihydroxy- and Diacetoxybenzoic Acids Salicylazosulphapyridine (Sulphasalazine) and 5-Aminosalicyclic Acids Ester Pro-Drugs Other Sahcylate Derivatives Conclusions 3 Absorption, Metabolism and Disposition of the Salicylates Introduction Absorption, Metabolism and Distribution Aspirin, Salicylate and Their Esters Analytical Methods Colorimetric and Spectrophotometric Procedures Spectrofluorimetry Thin-Layer Chromatography Gas-Liquid Chromatography High Pressure (Performance) Liquid Chromatography Determination of Glucuronides and Sulphate Metabolites 4 Pharmacological and Biochemical Actions of the Salicylates Introduction Anti-Inflammatory Effects Studies in Animal Models Acute Inflammatory Models Actions of Salicylates in Acute Inflammatory Models Chronic Adjuvant Polyarthritis (Rats) Comparative Effects of Salicylates and Other NSAI Drugs in Adjuvant Arthritis Biochemical and Cellular Responses of Salicylates in Adjuvant Disease Actions of Salicylates in Other Chronic Models of Inflammation Biochemical Effects of Salicylates in Relation to Their Anti-Inflammatory Actions Analgesic Activity Introduction Anti-Pyresis5 Side-Effects and Toxicology of the Salicylates Introduction Gastrointestinal Side-Effects Historical Aspirin as a Major Cause of Bleeding and Ulceration Gastrointestinal Side-Effects from Salicylates in Arthritic Patients Assessment of Gastrointestinal Damage in Man Site and Pathology of Lesions Studies in Laboratory Animals Mechanisms of Gastric Mucosal Damage by Salicylates Summary Nephropathy Analgesic Abuse Syndrome Studies in Arthritic Patients Pathology Biochemical Effects of Salicylates Hepatotoxicity Clinical Evidence Pathology and Biochemical Changes Hypersensitivity Reactions and Asthma Aspirin-Sensitive Asthma Urticaria and Angioedema Teratogenesis and Pregnancy Miscellaneous Side-Effects Acute Salicylate Poisoning Toxic Manifestations Conclusions 6 Therapeutic Uses of the Salicylates Introduction Arthritic Conditions Rheumatoid Arthritis Osteoarthritis (Osteoarthrosis) Miscellaneous Drug Monitoring Interactions with Other Anti-Inflammatory Drugs Analgesia Assessment of Pain Assessment of Pain Acute Surgery Postpartum and Episiotomy Dysmenorrhoea Cancer Anti-Pyresis Thromboembolic Conditions Perturbed Metabolic States Diabetes Melhtus Thyroiditis and Thyrotoxicosis Bartter's Syndrome Obesity Cystic Fibrosis Other Possible Uses Dermatological Conditions Diarrhea Ductus Arteriosus Sickle-Cell Anemia Thrombocytic Thrombocytopenic Purpura Anti-Tumor Activity Prevention of Allograft Rejection Anti-Viral and Anti-Parasitic Activities Multiple Sclerosis Miscellaneous