Pharmacology of 11 beta-hydroxysteroid dehydrogenase.

In clinical practice synthetic glucocorticoids are mainly used as therapy for inflammatory disorders and in suppressing immunological responses to transplanted allografts. The presence of an 11 beta-hydroxyl (11 beta-OH) group is mandatory for the antiinflammatory effects of glucocorticosteroids. The interconversion of the 11 beta-OH into the corresponding 11-keto group and vice versa by 11 beta-OH-steroid dehydrogenase might thus play a pivotal role for the efficacy of these steroids. Estimates of the apparent capacity to interconvert these steroids have been derived from plasma and tissue concentration measurements. Such estimates reveal that the interconversion process is concentration dependent and tissue specific. It remains to be established whether modulating that process might allow the immunosuppressive effect to be targeted within certain organs, thereby increasing the ratio between therapeutic and side effects of glucocorticoid administration.