As experience has taught us, the biologic properties of cortisone and hydrocortisone may be altered, both favorably and unfavorably, through changes in their basic structure. The unending search to build better clinical properties into adrenocortical steroids appears to have moved an important step ahead with the synthesis of dexamethasone, achieved by addition of a methyl radical at carbon 16 and a fluorine atom at carbon 9 of the prednisolone structure.1,2 Preliminary observations indicate that the alteration to produce dexamethasone certainly has resulted in an improved compound with greatly increased milligram activity along with substantially decreased undesirable effects.
Initial studies with dexamethasone revealed that this compound has a milligram activity approximately 8-10 times that of prednisone or prednisolone and 30 times that of cortisone. Certain undesirable effects reported with the hydroxylated steroids (such as triamcinolone) of muscle wasting, increased tendency to ecchymoses, and abnormal weight loss are not associated with
NIELSEN RH. The Use of Dexamethasone in Ophthalmologic Steroid TherapyA Preliminary Report. AMA Arch Ophthalmol. 1959;62(3):438-444. doi:10.1001/archopht.1959.04220030094014