Clinical Experiences with the Sublingual Administration of Alpha Estradiol

Anumber of investigators have reported that when estrogens are administered orally a considerable proportion, as much as 90 per cent, is inactivated in the liver. Thus, in order to achieve the same estrogenic effect, ten times more material must be given by mouth than is necessary to achieve the same result by hypodermic injection. This same principle applies to other steroid hormones, except that in some cases the hormone is completely inactivated if given by mouth. The original work by Anderson, Haymaker and Henderson (1) showed that when the steroid hormone, desoxycorticosterone acetate, was dissolved in a propylene glycol-alcohol solution it could be successfully administered sublingually in the treatment of Addison's disease. A number of investigators have applied this same principle to estrogens, androgens, and other hormones. Salmon and Geist (2) have shown that sublingual administration of alpha estradiol produces a typical cornified vaginal smear. The advantages of a highly active oral estrogen are obvious.