Perlingual Absorption of Progesterone and Anhydrohydroxyprogesterone1,2

Abstract

Observations were made on 68 patients following the sublingual adm. of 47 courses of progesterone and 94 of anhydrohydroxyprogeste-rone. The hard pressed, slowly soluble tablets contained either 5 mg. of anhydrohydroxyprogesterone or 2.5 or 5 mg. of progesterone. The main criterion for effective absorption of each prep. was the induction of "progesterone withdrawal bleeding" in amenorrheic patients. Four to ten tablets were given at varying intervals each day for 3-10 days. In the instances in which progesterone and anhydrohydroxyprogesterone were used, withdrawal bleeding occurred in 55 and 74% of the cases, respectively. The effectual absorption of these prepns. was further surmised from the clinical results obtained in menorrhagia, mastodynia, premenstrual tension and dysmenorrhea. It may be assumed that the relative ratio of effectiveness between progesterone sublingually and parenterally is about 5-6:1 and these values are in satisfactory agreement with those obtained by Corner in the exptl. animal (4 or 5:1). Both progesterone and anhydrohydroxyprogesterone sublingually were at least as effective as anhydrohydroxyprogesterone by ingestion. There can be no doubt that progesterone sublingually is absorbed and utilized but due to the fact that part of the material is inadvertently swallowed and accordingly inactivated, it is slightly less effective than anhydrohydroxyprogesterone. This clinical study, though limited in scope, permits the conclusion that steroids are effectively absorbed sublingually and that the perlingual adm. of steroid hormones is a convenient method of adm.