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  • hydroxylated metabolites  (1)
  • inflammation  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Plasma and synovial fluid concentrations of diclofenac sodium and its major hydroxylated metabolites during long-term treatment of rheumatoid arthritis (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 389-394 
    Details
    ISSN: 1432-1041
    Keywords: diclofenac sodium ; synovial fluid levels ; hydroxylated metabolites ; rheumatoid patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma and synovial fluid concentrations of diclofenac sodium and its principal hydroxylated metabolites have been measured in sixteen rheumatoid patients on chronic therapy to investigate possible reasons for the drug's extended duration of action despite its apparent short elimination half-life in plasma. Diclofenac was detected in synovial fluid 2 h after dosing but at a lower level than in plasma. Thereafter synovial fluid concentrations remained relatively constant through to 11 h post-dosing whereas plasma levels in the same period declined rapidly from an initially high peak to near the sensitivity limit of the assay. Hydroxylated metabolites (free + conjugated) were rapidly formed with measurable concentrations of the 4′ and 5 mono and dihydroxy derivatives being detected in plasma 2 h after dosing; levels of the 3′ hydroxy metabolite were negligible at this time. Initially plasma levels of all metabolites were higher than those in synovial fluid but after 4 h synovial fluid levels were equal to or slightly higher than those in plasma. The significance of these findings is discussed in relation to the drug's overall clinical effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01037953
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Osmosin: its effect on plasma and synovial fluid kinetics of indomethacin (1985)
    Springer
    European journal of clinical pharmacology 27 (1985), S. 689-691 
    Details
    ISSN: 1432-1041
    Keywords: indomethacin ; Osmosin ; plasma and synovial fluid ; polyarthritis ; inflammation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary ‘Osmosin’ (sodium indomethacin trihydrate, now withdrawn) produced a constant rate of release of indomethacin into the gut. Paired plasma and synovial fluid samples were obtained at regular intervals following a single dose of ‘Osmosin’ (19 patients) and after continuous daily dosing (15 patients). Indomethacin is rapidly absorbed and plasma concentrations maintained in the range 0.3 to 0.6 µg/ml after the first 4 h. Equilibrium between plasma and synovial fluid occurs, with SF/plasma ratios 0.74 to 0.82 12–24 h after a single dose and up to 0.96 thereafter. The indomethacin synovial fluid/plasma profile is changed by Osmosin from the pattern of a short half-life drug to the pattern typical of a long half-life drug. Results from serial samples obtained by use of indwelling cannulae (in vein and knee joint) show close agreement with our single paired sampling technique. Our method may have theoretical disadvantages but it has many practical advantages.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547050
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
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