Serum levels of progesterone and some of its metabolites including deoxycorticosterone after oral and parenteral administration

Single 100-mg doses of progesterone were given orally and as intramuscular injections to four women during the follicular phase of the menstrual cycle. After oral administration serum levels of progesterone increased rapidly to reach luteal phase values (mean maximum level 55.6 nM) within 1-4 h and were still elevated after 12 h. The serum concentrations of 20 alpha-hydroxy-4-pregnen-3-one showed a similar pattern while there were only minor transient changes in 17 alpha-hydroxyprogesterone concentrations. The serum levels of cortisol and 4-androstene-3,17-dione were unaffected. In comparison, after intramuscular administration values two to three times higher than by the oral route were achieved. A significant increase in serum deoxycorticosterone was recorded in all women. The mean ratio between the change in deoxycorticosterone and progesterone was increased after oral administration. Oral treatment with natural progesterone may develop into an attractive alternative to synthetic progestogens but the conversion of progesterone into a potent mineralocorticoid may be a potential disadvantage.