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Progestational activity of a new diacetate progesterone derivative
Authors:E Vázquez  J Arias  M Alvarez
Abstract:The synthetic progestogen AY-11440 (pregna-4,6-dien-20-one-6-chloro-3, 17-dihydroxydiacetate) was tested at several doses for 3 cycles in 14 postmenopausal women and 7 ovulating women. Data collected included cervical mucus, vaginal smear stained by Papanicolaou's method, and endometrial biopsy stained by several standard methods, all taken on the day after the last pill. Patients and doses were the following: 14 postmenopausal women with vasomotor syndrome who were given 1.25 mg Premarin for 21 days and .1 mg, 1 mg, or 3 mg AY-11440, for the last 10 days of a cycle; and 7 cycling women seeking contraception, given .1, .5, or 1 mg AY-11440 daily from Day 5-25. Cervical musuc was usually negative for ferning. In postmenopausal women, vaginal smears were estrogenic and comparable to normal Cycle Day 12 in those given .1 mg; progestational like Day 20-22 in those given 1 mg; and early progestational like Day 18 in those given 3 mg. Endometria appeared early proliferative at the .1 and 1 mg doses and progestational (Day 22-23) at 3 mg. Among the fertile women vaginal smears ranged from progestational (Day 18 to late progestational (Day 25) and endometria resembled Day 22-24. Although the effects were variable among individuals, generally the effects were dissociated, in the sense that cervical mucus was most sensitive and endometrium was least changed by the drug.
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