Ottoson U B, Carlstrom K, Damber J E, von Schoultz B
Br J Obstet Gynaecol. 1984 Nov;91(11):1111-9. doi: 10.1111/j.1471-0528.1984.tb15086.x.
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.
在月经周期的卵泡期,对4名女性口服和肌内注射单剂量100毫克孕酮。口服给药后,孕酮血清水平迅速升高,在1 - 4小时内达到黄体期水平(平均最高水平55.6纳摩尔),12小时后仍保持升高。20α - 羟基 - 4 - 孕烯 - 3 - 酮的血清浓度呈现类似模式,而17α - 羟基孕酮浓度仅有轻微短暂变化。皮质醇和4 - 雄烯 - 3,17 - 二酮的血清水平未受影响。相比之下,肌内给药后达到的值比口服途径高两到三倍。所有女性的血清脱氧皮质酮均有显著升高。口服给药后,脱氧皮质酮与孕酮变化之间的平均比值增加。天然孕酮口服治疗可能成为合成孕激素的有吸引力的替代方法,但孕酮转化为强效盐皮质激素可能是一个潜在缺点。