两种剂量的7-甲异炔诺酮对60例绝经后妇女症状控制的比较

目的:探讨两种剂量的7-甲异炔诺酮(OrgOD14,利维爱)对绝经症状控制的比较。方法:60例绝经后妇女随机分为两组:①A组30例,每日口服7-甲异炔诺酮2.5mg。②B组30例,隔日口服7-甲异炔诺酮2.5mg,共6个月。观察服药前后的Kupperman评分变化及血雌二醇、促卵泡激素水平的改变。结果:两组服药后绝经症状明显改善,Kupperman评分明显降低(P<0.01),雌二醇水平显著上升(P<0.01),促卵泡激素水平明显下降(P<0.05),而两组之间差异无显著性。结论:7-甲异炔诺酮可有效地控制绝经症状,每日口服2.5mg并不比隔日口服2.5mg有较好的控制效果(除控制失眠外),故推荐隔日口服2.5mg7-甲异炔诺酮。     

Progestin receptors in human uterine cytosol

Progestin(norethindrone and norethindrone acetate)-binding protein, exhibiting characteristics similar to uterine progesterone receptor, has been identified in human uterine cytosol. The progestin receptor was characterized by sedimentation coefficient 4.2 S; Stokes radius, 39 Å; frictional ratio 1.29; isoelectric pH 4.6; molecular radius 2.7 nm; and molecualr weight in the range 67 000–74 000. The ammonium-sulfate-precipitated progestin-receptor complex was eluted from a DEAE-cellulose column at 0.18 M KC1. The progestin binding was saturable and stereospecific. The sequential variation in receptor concentration (early proliferative, 3800–4300 sites/cell; late proliferative, 9500–11200 sites/cell; early secretory, 4900–6200 sites/cell; late secretory, 1800–2300 sites/cell) was in conformity for progesterone and the progestins, when concurrently measured. Oral administration of norethindrone significantly reduced the cytoplasmic and nuclear receptor concentration for estradiol and progesterone. A significant observation was that the progestins stabilized the progestin receptor by forming a slowly dissociating complex with a $\text{t}{}_{\mathrm{<mtext>1</mtext><mtext>2</mtext>}}\text{～ 110?130}\text{min}$ as compared with the progesteronereceptor complex dissociating with $\text{t}{}_{\mathrm{<mtext>1</mtext><mtext>2</mtext>}}\text{～41}\text{min}$. Thus, the uterine progestin receptor recognizes progestins in general, although with a varying degree of affinity, and the altered rate constants could be of putative importance in determining the biological potency of the progestins.