Dexamethasone is 9-α-fluoro,16-α-methylprednisolone.* It is one of a group of prednisolone analogues synthesized and studied by Arth and his co-workers1,2 in the continuing search for modifications of hydrocortisone which would afford increased anti-inflammatory and antiallergic activity but would produce minimal mineral imbalance and the other undesirable sideeffects that sometimes result from therapy with the corticosteroids.
The formation of prednisone and prednisolone from cortisone and hydrocortisone by the introduction of a double bond (Δ-1) in the C1-C2 position increases the anti-inflammatory potency of hydrocortisone four or five times without enhancing its effect on sodium-potassium balance. Fluorination of hydrocortisone at the 9-α position increases its anti-inflammatory effect tenfold. However, the profound sodium-retaining and potassium-excreting effects of this modification interdicted its systemic use. Addition of a hydroxyl group in the 16-α position made it possible to utilize the enhanced anti-inflammatory and
KANOF NB, BLAU S. Dexamethasone in Dermatology. AMA Arch Derm. 1959;80(2):198–201. doi:10.1001/archderm.1959.01560200066007
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