[New developments in glucocorticoid therapy: selective glucocorticoid receptor agonists, nitrosteroids and liposomal glucocorticoids].
Two mechanisms of the genomic action ofglucocorticoids (GCs) can be distinguished: transrepression, yielding mainly an anti-inflammatory effect, and transactivation, resulting mainly in metabolic-endocrine side effects. Selective glucocorticoid receptor agonists (SEGRAs) cause selective transrepression, yielding the same anti-inflammatory effect as GCs, but with fewer side effects. NO is bound to several drugs to increase their effect; in nitrosteroids, NO is coupled to GC, resulting in a synergistic anti-inflammatory effect. Drug targeting can be achieved with GCs by incorporation of GC into polyethyleneglycol(PEG)-liposomes, resulting in very high concentrations ofGCs at the site of inflammation. Well-designed studies are needed to determine the place of SEGRAs, nitrosteroids and liposomal GCs in clinical practice.
Sint Franciscus Gasthuis, afd. Reumatologie, Kleiweg 500, 3045 PM Rotterdam. m.huisman@sfg.nl
A M
AM
Huisman
J W G
JW
Jacobs
F
F
Buttgereit
J W J
JW
Bijlsma
D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000627:therapeutic use*; D004357:Drug Synergism; D005938:Glucocorticoids / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D009569:Nitric Oxide / Q000378:metabolism; D011965:Receptors, Glucocorticoid / Q000819:agonists*; D015533:Transcriptional Activation
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D011965:Receptors, Glucocorticoid; D009569:Nitric Oxide