The Pharmacokinetics of Plasma Total and Free Prednisolone during an Alternate-day Regimen

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  • FUWA Yoshiyuki
    The Third Department of Internal Medicine, Gifu University School of Medicine
  • YASUDA Keigo
    The Third Department of Internal Medicine, Gifu University School of Medicine
  • ADACHI Kayoko
    The Third Department of Internal Medicine, Gifu University School of Medicine
  • GOSHIMA Eiichi
    The Third Department of Internal Medicine, Gifu University School of Medicine
  • YAMAKITA Noriyoshi
    The Third Department of Internal Medicine, Gifu University School of Medicine
  • MIURA Kiyoshi
    The Third Department of Internal Medicine, Gifu University School of Medicine

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Other Title
  • プレドニゾロン (PSL) 隔日投与時の総及び遊離PSL薬物動態

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To determine the pharmacokinetic changes of prednisolone associated with an alternate-day regimen, 12 patients with various diseases were studied longitudinally. There were 9 patients (6 with systemic lupus erythematosus, 2 with sarcoidosis and one with polymyositis), who were treated with prednisolone (daily period) and subsequently put on an alternate-day regimen (alternate-day period). In 2 of the other patients (one with systemic lupus erythematosus and one with multiple sclerosis), the alternate-day regimen was preceded by the daily regimen, and subsequently an intermittent regimen consisting of 4 consecutive days on therapy and 3 days off therapy was followed. In the remaining patient with systemic lupus erythematosus, the treatment with the alternate - day regimen was initiated and followed throughout the treatment period. The mean duration and the mean total administered dose during the study were 1.1 months and 1.9g in the daily period, and 7.8 months and 7.7g in the alternate-day period. The test was done and blood was drawn for 6 hours after an intravenous administration of 20mg prednisolone (0.36mg/kg on the average) at the end of the respective regimen periods. In the daily period and the on-day of the alternate-day regimen, the pharmacokinetic study of iv prednisolone injection was done before the ingestion of oral prednisolone. The off-day test was done the next morning of the on-day. Plasma total and free prednisolone concentrations were measured by RIA. On-day and off-day tests in the alternate-day period were performed during the same week.<BR>The mean half life of both total and free prednisolone was prolonged significantly in the daily period and during the on-day and off-day of the alternate-day regimen compared with the pretreatment values. The mean metabolic clearance rates (MCR) of both total and free prednisolone decreased significantly in the daily period and during the on-day and off-day of the alternate-day period in comparison with the pretreatment values. No significant difference was found between either mean half life or MCR during the on-day and off-day of the alternate-day period. These findings were in contrast with our previously observed prednisolone pharmacokinetics during the intermittent regimen (4 days on therapy and 3 days off therapy within one week), in which pharmacokinetic parameters during the on-day (after 3 days of prednisolone ingestion) and off-day (after 3 off-days of prednisolone ingestion) periodically changed and were similar to those in the pre-treatment period and during the daily therapy period, respectively. Clinically, the side effects such as infections and cushingoid appearance observed during the daily period were not always reduced by the shifting to the alternate-day regimen.<BR>These findings may suggest no marked differences in pharmacokinetic indices between the alternate-day and the daily periods.

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