Metabolism of Systematically Given Corticosteroids

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Abstract
In the metabolism of a systemically administered corticosteroid, one of three possible main pathways is determined by the position in the molecule of the substituents which are added in the drugs to the naturally occurring ones. (I) Chiefly, hydrogenation in ring A and/or the 20-position: cortisol, cortisone, prednisolone, prednisone, and 6α-methylprednisolone. (II) In the presence of a substituent in the 16-position mainly 6β-hydroxylation: dexamethasone, betamethasone, and triamcinolone. (Ill) In the presence of a substituent in the 16-position, and fluorine in the 6α-position principally defluorination in the 6α-position and 6β-hydroxylation: fluocortolone and paramethasone. Complete metabolism, in long-term use, can be expected in the case of the ubstances mentioned under II and III, but not of those under I. Enzyme induction, both actively and passively, is negligible in group I and marked in groups II and III.