Mishell Daniel R
Department of Obstetrics and Gynecology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA.
J Reprod Med. 2008 Sep;53(9 Suppl):721-8.
Drospirenone is a novel progestin that is structurally related to 17 alpha-spirolactone and has antimineralocorticoid and antiandrogenic activity. A 3-mg dose of drospirenone was first used in combination with ethinyl estradiol (EE) 30 microg in a combination oral contraceptive (COC) that is administered for 21 days, followed by a 7-day hormone-free interval (HFI) (drospirenone/30EE, or Yasmin). The 21/7 regimen is considered to be the standard regimen for COC delivery. A formulation with the metabolic benefit of COCs containing a lower estrogen dose has been developed combining drospirenone 3 mg with EE 20 microg and using a regimen of 24 days of active pills, followed by a 4-day HFI (drospirenone/20EE-24/4), or YAZ (Bayer HealthCare Pharmaceuticals Inc., Wayne, New Jersey). Since drospirenone has a half-life of > 30 hours, its activity extends for a prolonged time into the shortened HFI. This new COC has been shown to provide effective contraception and to have a good safety profile. Two large noninterventional studies have recently evaluated the safety of drospirenone/30EE in 2 areas of special interest: hyperkalemia and thromboembolic events. Use of a drospirenone-containing COC was not associated with an increased risk of either type of disorder in comparison with COCs containing other progestins. Drospirenone/20EE-24/4 provides a low dose of EE in combination with drospirenone in an effective and safe COC that is administered using a regimen with a shortened HFI. Drospirenone/20EE-24/4 is the only COC with 3 indications: contraception and the treatment of premenstrual dysphoric disorder in women who wish to use a COC for birth control, and the treatment of moderate acne in women who are at least 14-years-old, have achieved menarche and wish to use a COC for birth control.
屈螺酮是一种新型孕激素，其结构与17α-螺内酯相关，具有抗盐皮质激素和抗雄激素活性。3毫克剂量的屈螺酮最初与30微克炔雌醇（EE）联合用于一种复方口服避孕药（COC），该避孕药服用21天，随后是7天的无激素间隔期（HFI）（屈螺酮/30EE，即优思明）。21/7方案被认为是COC给药的标准方案。已研发出一种具有代谢益处的COC制剂，其雌激素剂量较低，将3毫克屈螺酮与20微克EE联合使用，并采用24天活性药丸、随后4天HFI的方案（屈螺酮/20EE - 24/4，即 Yaz）（拜耳医疗保健制药公司，新泽西州韦恩）。由于屈螺酮的半衰期大于30小时，其活性会在缩短的HFI中延长较长时间。这种新型COC已被证明能提供有效的避孕效果且安全性良好。最近有两项大型非干预性研究评估了屈螺酮/30EE在两个特别关注领域的安全性：高钾血症和血栓栓塞事件。与含其他孕激素的COC相比，使用含屈螺酮的COC与这两种疾病的风险增加均无关。屈螺酮/20EE - 24/4在一种有效且安全的COC中提供低剂量的EE与屈螺酮联合使用，该COC采用缩短HFI的方案给药。屈螺酮/20EE - 24/4是唯一具有三种适应证的COC：避孕以及用于希望使用COC进行避孕的女性的经前烦躁障碍的治疗，以及用于至少14岁、已初潮且希望使用COC进行避孕的女性的中度痤疮的治疗。
