EFFECT OF INTRAVENOUS DEFLAZACORT 21-HEMISUCCINATE ON HUMAN PERIPHERAL-BLOOD LYMPHOCYTES

A clinical trial was performed in order to evaluate the safety and the variations of lymphocyte subpopulations induced by the intravenous administration of Deflazacort 21-hemisuccinate (DFZ-HS), the water-soluble derivative of the prednisolone analogue deflazacort acetate. DFZ-HS was tested at doses ranging from 1 to 10.55 mg/kg and was compared with methylprednisolone (MPR) administered at equipotent doses. Sixteen healthy volunteers were studied according to a double-blind, 4 period balanced, incomplete cross-over design. Both drugs were well tolerated. DFZ-HS dramatically, but transiently, reduced the number of total and CD4(+) T lymphocytes at all doses tested, the maximum decrease being observed at the 8(th) hour after injection. Similar effects were observed following MPR administration. The potency ratio between DFZ-HS and MPR, calculated on the basis of CD4(+) T cells decrease, was about 1:1, suggesting that both drugs exert comparable immunomodulatory activities. These data, toghether with the well known low impact of DFZ-HS on glucidic and calcium metabolisms, support its possible use when high glucocorticoid doses are required in immunosuppressive therapy.