Bygdeman M, Christensen N, Gréen K, Lundström V
Contraception. 1980 Aug;22(2):153-64. doi: 10.1016/0010-7824(80)90059-1.
9-Deoxo-16, 16-dimethyl-9-methylene-PGE2 is a new prostaglandin analogue which is stable in suppository form. Estimates of potential for gastrointestinal side effects in monkey in vivo indicated that the frequency of diarrhea was low with retention of uterine stimulating potency. In the present study the effect of the compound on uterine contractility and its efficacy for cervical dilatation and for termination of pregnancy during the second trimester was evaluated in 89 women. The uterine stimulating potency of 9-deoxo-16, 16-dimethyl-9-methylene-PGE2 during mid-pregnancy following bolus intravenous injection or intravenous infusion was four to five times that of PGE2 alpha. Pretreatment with one single vaginal suppository containing 40 mg of the 9-methylene analogue resulted in dilatation of the cervical canal sufficiently to allow evacuation of the uterus without further dilatation in most patients in the 13th to 14th week of pregnancy. In more advanced pregnancies (15th to 24th week of gestation), 83 percent of the patients aborted following vaginal administration of 75 mg of the compound at 0 and 8 hours. All patients had aborted 42 hours after start of treatment if intramuscular injections of 15-methyl-PGE2alpha Tham were added after 24 hours. Both treatments were associated with a significantly lower frequency of gastrointestinal side effects than following vaginal administration of 15-methyl-PGF2alpha methyl ester. The incidence of temperature elevation on the other hand seemed to be higher.
9-脱氧-16,16-二甲基-9-亚甲基-PGE2是一种新型前列腺素类似物,其栓剂形式稳定。对猴子体内胃肠道副作用可能性的评估表明,腹泻频率较低,同时保留了子宫刺激效力。在本研究中,对89名妇女评估了该化合物对子宫收缩性的影响及其在妊娠中期扩张宫颈和终止妊娠的疗效。妊娠中期静脉推注或静脉输注后,9-脱氧-16,16-二甲基-9-亚甲基-PGE2的子宫刺激效力是PGE2α的四到五倍。在妊娠第13至14周时,大多数患者预先使用一枚含40mg 9-亚甲基类似物的阴道栓剂,可使宫颈管充分扩张,从而无需进一步扩张即可进行子宫排空。在更晚期的妊娠(妊娠第15至24周)中,83%的患者在0小时和8小时阴道给予75mg该化合物后流产。如果在24小时后加用15-甲基-PGE2α氨丁三醇肌肉注射,所有患者在治疗开始后42小时均流产。与阴道给予15-甲基-PGF2α甲酯相比,这两种治疗的胃肠道副作用频率均显著更低。另一方面,体温升高的发生率似乎更高。