Toppozada M K
Department of Obstetrics and Gynaecology, Shatby Hospital, Alexandria, Egypt.
Contraception. 1994 Apr;49(4):293-301. doi: 10.1016/0010-7824(94)90029-9.
Long-acting contraception by monthly intramuscular injection is an attractive method for family planning which fills a gap in birth control technology. The main advantage of this approach over long-acting (2-6 months) progestin injectables is much better cycle control. To achieve this goal, an estrogen had to be included in the formulation with significant reduction in the progestin dose. Until 1976, there were only three monthly injectables available (Injectable No. 1, Cycloprovera and Deladroxate), but they were faced with logistic, toxicological or clinical problems. It took over 15 years to resolve many of these problems and add a new product (Mesigyna = 50 mg norethisterone enantate plus 5 mg estradiol valerate in an oily solution). Cycloprovera, at a lower dose, received the new name of Cyclofem and Deladroxate was manufactured under the trade names of Perlutal or Topasel. The latter requires in-depth re-evaluation of its toxicological hazards. There are many other formulations currently being developed with incomplete data so far on safety and efficacy.
通过每月肌肉注射进行长效避孕是一种颇具吸引力的计划生育方法,它填补了节育技术的一项空白。与长效(2 - 6个月)孕激素注射剂相比,这种方法的主要优势在于对月经周期的控制要好得多。为实现这一目标,制剂中必须加入雌激素,并大幅降低孕激素剂量。直到1976年,仅有三种每月注射剂可供使用(一号注射剂、醋酸甲羟孕酮和羟孕酮己酸酯),但它们面临着后勤、毒理学或临床方面的问题。解决其中许多问题并推出新产品(美孕剂 = 50毫克炔诺酮庚酸酯加5毫克戊酸雌二醇的油溶液)花费了15年多时间。醋酸甲羟孕酮以较低剂量使用时,有了新名称Cyclofem,羟孕酮己酸酯则以Perlutal或Topasel的商品名生产。后者需要对其毒理学危害进行深入重新评估。目前还有许多其他制剂正在研发中,到目前为止关于其安全性和有效性的数据尚不完整。