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Acute and chronic pharmacokinetic studies of slow release ketoprofen (Oruvail) in rheumatoid arthritis.

Abstract
Slow release preparations of non-steroidal anti-inflammatory drugs are used to simplify dose regimes in the treatment of rheumatoid arthritis with the aim of improving patients compliance. This study examines the acute and chronic pharmacokinetics of slow release ketoprofen in 13 rheumatoid patients with a mean age of 59.8 years. Pharmacokinetic parameters following the first dose including Tmax which was 6.92 h (s.e.m. = 0.80), Cmax 3.87 micrograms/ml (s.e.m. = 0.54), apparent half-life 8.8 h (s.e.m. = 1.0) and AUC 41.92 micrograms.h/ml (s.e.m. = 4.02) were not significantly different from those following the last dose after 3 months of chronic treatment, when these were Tmax 6.38 h (s.e.m. = 0.84) Cmax 3.57 micrograms/ml (s.e.m. = 0.33) apparent half-life 8.8 h (s.e.m. = 1.1) and AUC 43.18 micrograms.h/ml (s.e.m. = 5.34) respectively. These results show that no accumulation of ketoprofen occurred with chronic treatment. Clinical assessments were performed in an open design and showed significant improvement in pain, articular index, grip strength and duration of morning stiffness when these parameters were compared to treatment with paracetamol during an initial washout. The drug was well tolerated although there was a trend for the haemoglobin to fall and this parameter should be monitored during therapy with ketoprofen.
AuthorsN Christophidis, A Rotstein, W J Louis
JournalClinical and experimental pharmacology & physiology (Clin Exp Pharmacol Physiol) Vol. 13 Issue 7 Pg. 555-61 (Jul 1986) ISSN: 0305-1870 [Print] ENGLAND
PMID3791708 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Delayed-Action Preparations
  • Dosage Forms
  • Phenylpropionates
  • Ketoprofen
Topics
  • Administration, Oral
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Arthritis, Rheumatoid (drug therapy, metabolism)
  • Body Burden
  • Delayed-Action Preparations
  • Dosage Forms
  • Female
  • Humans
  • Ketoprofen (adverse effects, blood, metabolism)
  • Kinetics
  • Male
  • Middle Aged
  • Phenylpropionates (metabolism)

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