The effects of the glucocorticoids prednisolone, deflazacort and beclomethasone-dipropionate on the RM 3/1 macrophage in human peripheral blood.
Different glucocorticoids (GC) applied intravenously, subcutaneously or in vitro exert only small differences in the ability to raise RM 3/1 macrophages from human blood monocytes. Dermal application however reveals a dose-dependent difference between GC. The present experiments were designed to study the efficacy of oral and topical application in this model. We also intended to obtain some information about the qualitative differences between the effects of prednisolone and deflazacort, which was reported to cause less adverse reactions than other GC. Both GC were orally administered to probands in doses regarded as equivalent with respect to general GC effects by the manufacturers of deflazacort (5-6 mg or multiples). A single dose of 5 mg prednisolone had no effect; 50 mg increased the number of RM 3/1 macrophages within 12 h from a basal level of 8.5% to about 80% similar to an intravenous or subcutaneous administration of GC. 10 mg prednisolone enhanced the number of RM 3/1 macrophages also within 12 h, reaching a mean maximum of about 60% at 24 h, declining thereafter. 12 mg deflazacort raised the number of RM 3/1 macrophages much slower, reaching a maximum of 30% (average) after 48 h. The interindividual variation was found to be mainly the time lag between dosage and maximum effect. Interindividual differences of prednisolone effects concerned mainly the maximal increase of RM 3/1 macrophages after 24 h. These results show that in this test system deflazacort was found to be less effective than expected. To elucidate the topical influence of GC, probands inhaled twice daily 0.5 mg beclomethasone-dipropionate over a period of 11 days. No effect on the number of RM 3/1 macrophages was observed, suggesting that beclomethasone applied in this dose did not cause systemic GC reactions.
Zwadlo-Klarwasser
G
G
Institute of Pharmacology and Toxicology, Medical Faculty, RWTH Aachen, Germany.
Schmutzler
W
W
D000280:Administration, Inhalation; D000284:Administration, Oral; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001507:Beclomethasone / Q000008:administration & dosage / Q000494:pharmacology*; D005260:Female; D006801:Humans; D007958:Leukocyte Count; D008264:Macrophages / Q000187:drug effects*; D008297:Male; D008875:Middle Aged; D011239:Prednisolone / Q000008:administration & dosage / Q000494:pharmacology*; D011282:Pregnenediones / Q000008:administration & dosage / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D011282:Pregnenediones; D011239:Prednisolone; D001507:Beclomethasone; C021988:deflazacort