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Biomedical subjects

Walter F Kean

Publications and source records attributed to Walter F Kean.

6 recordsLinked to original sources

The use of NSAIDs in rheumatic disorders 2005: a global perspective.

Population studies and World Health Organisation (WHO) statistics indicate that 10-50% of individuals suffer from musculoskeletal disorders. Up to 3% will be classified as disabled due to their bone and joint condition, and the majority will suffer from pain. Almost all will require non-steroidal anti-inflammatory drugs (NSAIDs) and other analgesics for their management. The large majority of this population is elderly and, hence, at greater risk of adverse effects to the NSAIDs. The NSAIDs are a necessary choice in pain management because of the integrated role of the cyclo-oxygenase (COX) pathway in the generation of inflammation and in the biochemical recognition of pain. For over 80 years the management of musculoskeletal pain was hampered by NSAID toxicity problems related to the traditional NSAIDs. In the early 1990s, paracetamol was recommended as the first-choice analgesic for osteoarthritis, but subsequent studies have shown that paracetamol has a significant gastrointestinal (GI) toxicity profile. In addition, it has lower analgesic efficacy than NSAIDs and is, thus, not an effective alternative to NSAIDs in any of the inflammatory arthritides. The identification of cyclo-oxygenase 2 (COX-2) and the subsequent introduction of the COX-2-selective inhibitor NSAID drugs was thought to be a major breakthrough with the expectation of a significant reduction in G/I side-effects. This has not been the case for celecoxib, and indeed for all COX-2-selective inhibitors when given with ASA. The COX-2-selective inhibitors also inhibit renal COX-2 with the potential for problems of fluid retention, oedema, hypertension and congestive heart failure. The major controversy with respect to the COX-2-selective inhibitors as a class has been the increase in myocardial infarction and other cardiovascular events observed in some studies. Thus, the initial expected global benefits of the COX-2-selective inhibitors may be outweighed by their potential for toxicity. Recent studies have shown that the use of a proton-pump inhibitor drug with traditional NSAIDs and with COX-2-selective inhibitors has been shown to significantly reduce GI symptoms and peptic ulceration. Thus, the traditional NSAIDs have been re-established as the preferred choice in the management of arthritis and musculoskeletal disorders.

Acetaminophen↗

Oxaprozin: kinetic and dynamic profile in the treatment of pain.

Oxaprozin (4,5-diphenyl-2-oxazolepropionic acid) is a non-steroidal anti-inflammatory drug (NSAID) which is effective in models of inflammation, pain and pyrexia. It is effective and well tolerated in the clinical management of adult rheumatoid arthritis (RA), osteoarthritis (OA), ankylosing spondylitis, soft tissue disorders and post operative dental pain. Oxaprozin has a high oral bioavailability (95%), with peak plasma concentrations at 3 to 5 hours after dosing. It is metabolised in the liver by oxidative and conjugative pathways and readily eliminated by the renal and faecal routes. Oxaprozin's strong analgesic qualities are particularly useful in painful musculoskeletal conditions such as periarthritis of the shoulder, since it exhibits actions such as inhibition of COX-1 and COX-2 isoenzymes, inhibition of nuclear translocation of NF-kappaB and of metalloproteases, and modulates the endogenous cannabinoid system. This editorial addresses the accompanying paper by Barbara Heller and Rosanna Tarricone on the management of shoulder periarthritis pain, in which they studied the efficacy and safety of oxaprozin compared to the comparator drug diclofenac over a 15 day period. Both oxaprozin and diclofenac compared well in the primary study endpoint of reduction in shoulder pain. Oxaprozin and diclofenac were well tolerated and oxaprozin showed better improvement in shoulder function and in the mental health item of the SF-36 quality of life component. The study by Heller and Tarricone is an addition to the large number of clinical trials which demonstrate that oxaprozin has equal efficacy in comparison with standard doses of commonly used anti-rheumatic agents such as aspirin, diclofenac, ibuprofen, indomethacin etc. in several different painful musculoskeletal conditions.

Anti-Inflammatory Agents, Non-Steroidal↗