Journal ArticleDOI
The local anti-inflammatory activity of rimexolone (Org 6216) in fibrin-induced monoarticular arthritis and adjuvant-induced arthritis.
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TLDR
The effects of a number of steroids administered intra-articularly in a chronic model of fibrin-induced monoarticular arthritis in the rabbit have been investigated and only Org 6216, hydrocortisone acetate, prednisolone tertiary butyl acetate and indomethacin produced anti-inflammatory effects throughout the 4 days of the experiments and were devoid of significant adrenolytic and thymolytic activity.Abstract:
The effects of a number of steroids administered intra-articularly in a chronic model of fibrin-induced monoarticular arthritis in the rabbit have been investigated. Org 6216 hydrocortisone acetate, prednisolone tertiary butyl acetate and triamcinolone hexacetonide each suppressed the joint swelling produced 14 days after antigen challenge. These anti-inflammatory effects lasted for at least 7 days. Hydrocortisone semisuccinate was inactive in this model. In addition, the effects of the same compounds and several other anti-inflammatory steroids and indomethacin administered locally with adjuvant was assessed on the resultant paw oedema produced in the rat. The local anti-inflammatory activity, the duration of action and the systemic effects of these drugs varied considerably and only Org 6216, hydrocortisone acetate, prednisolone tertiary butyl acetate and indomethacin produced anti-inflammatory effects throughout the 4 days of the experiments and were devoid of significant adrenolytic and thymolytic activity.read more
Citations
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Journal ArticleDOI
Somatostatin-induced modulation of inflammation in experimental arthritis.
Marco Matucci-Cerinic,Francesco Borrelli,Sergio Generini,Alfredo Cantelmo,Isabella Marcucci,Fabrizio Martelli,Paolo Romagnoli,Stefano Bacci,Angelo Conz,Paolo Marinelli,Simone Marabini +10 more
TL;DR: It is suggested that somatostatin exerts an antiinflammatory effect in this model of experimental arthritis and may represent a valid and safer alternative to corticosteroids for intraarticular therapy of arthritis.
Journal ArticleDOI
Pharmacokinetics of Rimexolone After Intra‐Articular Administration
Hartmut Derendorf,Helmut Möllmann,G. Voortman,Frank A. van den Ouweland,de Putte Levinus B. A. Van,Greet Gevers,Jan Dequeker,E. Van Vliet-Daskaiopoulou +7 more
TL;DR: It could be shown that the mean residence time of different glucocorticoids correlates well with the duration of their clinical effectiveness.
Journal ArticleDOI
Rimexolone inhibits proliferation, cytokine expression and signal transduction of human CD4+ T-cells.
Cornelia M. Spies,Timo Gaber,M. Hahne,L. Naumann,Robert Tripmacher,Saskia Schellmann,Cindy Stahn,Gerd-Rüdiger Burmester,Andreas Radbruch,Frank Buttgereit +9 more
TL;DR: It is concluded that rimexolone and dexamethasone inhibit T-cell proliferation as well as cytokine production of activated CD4+ T-cells in a similar manner and contribute to the well-known beneficial anti-inflammatory and immunomodulatory effects of glucocorticoid therapy.
Journal ArticleDOI
Protective effect of rimexolone on cartilage damage in arthritic mice: A comparative study with triamcinolone hexacetonide
TL;DR: Data indicate that although steroids may have significant side effects on chondrocytes, the overall effect on arthritic chondROcytes is beneficial, and an advantage of rimexolone over THA is its prolonged retention, which may explain its sustained anti-inflammatory action, and the lack of systemic effect.
Journal ArticleDOI
Binding affinities of rimexolone (ORG 6216), flunisolide and their putative metabolites for the glucocorticoid receptor of human synovial tissue.
G. Hochhaus,H. w. Moellmann +1 more
TL;DR: The results support previous pharmacological findings that the high ratio of local to systemic effects of both compounds are due to a pronounced receptor affinity of the parent compounds and the fast systemic metabolism to derivatives with low pharmacodynamic activity.
References
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Journal Article
The production of arthritis in rabbits by an immunological reaction to fibrin.
D. C. Dumonde,L. E. Glynn +1 more
Journal ArticleDOI
Deleterious effect of intra-articular hydrocortisone.
G.N. Chandler,V. Wright +1 more
Journal ArticleDOI
Anti-inflammatory mechanism of inflamed-tissue factor.
Ivan L. Bonta,J. Noordhoek +1 more
TL;DR: Data shows that the exudate inhibits total complement activity of serum when either added in vitro or administered in vivo, and appears to be a common pathway in the anti-inflammatory effect of the counter-irritant principle and of inflammed-tissue factor(s).
Journal ArticleDOI
Comparison of intra-articular methotrexate with intra- articular triamcinolone hexacetonide by thermography
TL;DR: Methotrexate had no immediate anti-inflammatory effect, even in psoriatic arthropathy, and did not give the relief of intra-articular steroid.
Journal ArticleDOI
A thermographic assessment of three intra-articular prednisolone analogues given in rheumatoid synovitis.
TL;DR: Three intra-articular prednisolone analogues have been studied in a group of forty-six rheumatoid arthritic subjects and both the systemic escape from the joint and the duration of effect on injected and uninjected knees were related to drug solubility.