Assessment of drugs in out-patients with rheumatoid arthritis. Evaluation of methods and a comparison of mefenamic and flufenamic acids with phenylbutazone and aspirin.

Mason, R. M.; Barnardo, David E.; Fox, WilliamW.; Weatherall, M.

doi:10.1136/ard.26.5.373

Cited by 29 publications

(6 citation statements)

References 17 publications

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“…The treatment periods in this study lasted 4 weeks. Mason, Barnardo, Fox, and Weatherall (1967) identified possible sources of bias as subjective improvement regardless of treatment, spurious improvement due to drop-out of the most severely ill, and the contribution of the physician to the assessment. The second of these was answered in this study by analysis of the sub-group undergoing the full trial, and by the analysis of admission parameters of the patients dropping out, which showed them to have lesser disease activity.…”

Section: Discussionmentioning

confidence: 99%

Naproxen. A new non-hormonal anti-inflammatory agent. Studies in rheumatoid arthritis.

Hill¹,

Hill²,

Mowat³

et al. 1974

Annals of the Rheumatic Diseases

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Section: Discussionmentioning

confidence: 99%

Naproxen. A new non-hormonal anti-inflammatory agent. Studies in rheumatoid arthritis.

Hill¹,

Hill²,

Mowat³

et al. 1974

Annals of the Rheumatic Diseases

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“…Indomethacin ( 1 , Figure ) is a well-known nonsteroidal anti-inflammatory drug (NSAID) and is effective against severe rheumatoid arthritis, ankylosing spondylitis, osteoarthritis of large joints, and other inflammations. − The beneficial effect is associated with inhibition of cyclooxygenases (COX) that convert arachidonic acid into prostaglandins in inflammatory processes . The major limitation of long-term therapeutic use of NSAIDs (COX-1 inhibitors) is their gastrotoxicity.…”

Section: Introductionmentioning

confidence: 99%

“…Prodrugs 1a-d were crystalline when screened in a Bruker AXS D8 advance diffractometer. Powder XRD profiles of prodrugs are shown inFigures 3,4,5,and 6.…”

mentioning

confidence: 99%

Synthesis and Biological Evaluation of Orally Active Prodrugs of Indomethacin

et al. 2011

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Synthesis and biological evaluation of orally active prodrugs (1a-d) of indomethacin are described. Prodrugs 1a-c showed a similar degree of anti-inflammatory activity, and prodrug 1d was found to be less potent than the parent drug indomethacin (1). Ulcer index (UI) data indicated that 1a (UI = 19), 1c (UI = 0), and 1d (UI = 0) were substantially less ulcerogenic and 1b (UI = 62) was more ulcerogenic than parent drug 1 (UI = 47). These prodrugs demonstrated good stability at acidic and basic pH and found to be more lipophilic than parent drug compound 1, indicated by partition coefficients measured in octanol-buffer system at pH 7.4 and 3.0. On the basis of in vivo studies, 1a and 1c compounds were selected for metabolic stability in rat liver microsome (RLM) and rat plasma (RP), and both were found to be enzymatically labile. Prodrugs 1a and 1c emerged as potent anti-inflammatory agents with a lesser potential for ulcer than the parent drug indomethacin.

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“…Diclofenac sodium ( 1a , Figure ) is a nonsteroidal anti-inflammatory drug (NSAID) widely used for the treatment of pain and stiffness associated with a variety of inflammatory diseases including active inflammatory arthritis. − NSAIDs exert their therapeutic activity by inhibiting cyclooxygenase-derived prostaglandin synthesis, but this mechanism of action is inherently responsible for the gastrointestinal (GI), − renal, − and hepatic side effects observed in patients undergoing a long-term treatment. The most common effects associated with NSAID therapy are upper GI irritation, ulceration, dyspepsia, bleeding, and in some cases death .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Biological Evaluation of Novel Diclofenac Prodrugs

et al. 2011

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Diclofenac ester pro drugs (4, 5, 6) were synthesized and evaluated in vitro and in vivo for their potential use for oral delivery, with the aim of obtaining enzymatically labile and less ulceration drugs than the parent drug diclofenac sodium (1a). Prodrugs 4, 5, 6 were found to be potent anti-inflammatory drugs with less ulcerogenic potential than the parent diclofenac sodium. Prodrugs 4, 5, 6 rapidly underwent enzymatic hydrolysis to release the parent drug diclofenac in 30-60 min in rat liver microsomes (RLM) and rat plasma (RP). Prodrugs were found to be more lipophilic when the partition coefficient was measured in 1-octanol and buffer system at pH 7.4 and 3.0. Diclofenac prodrugs 4, 5, 6 were found to be crystalline in nature (analyzed by PXRD). Prodrug 4 was found to be a superior candidate for the treatment of chronic inflammatory diseases.

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Assessment of drugs in out-patients with rheumatoid arthritis. Evaluation of methods and a comparison of mefenamic and flufenamic acids with phenylbutazone and aspirin.

Cited by 29 publications

References 17 publications

Naproxen. A new non-hormonal anti-inflammatory agent. Studies in rheumatoid arthritis.

Naproxen. A new non-hormonal anti-inflammatory agent. Studies in rheumatoid arthritis.

Synthesis and Biological Evaluation of Orally Active Prodrugs of Indomethacin

Synthesis, Characterization, and Biological Evaluation of Novel Diclofenac Prodrugs

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