雌四醇/屈螺酮是一种联合口服避孕药(COC),具有植物合成的胎儿雌激素(雌四醇)和公认的孕激素(屈螺酮)。在临床前模型中,与雌二醇相比,雌四醇对雌激素受体-α(ER-α)的结合亲和力较低,并且在几种组织中对膜ER-α具有拮抗作用,包括乳房,同时保留位于细胞核中的受体的激动活性。雌四醇的雌激素性低可能有助于降低血栓形成风险。雌四醇/屈螺酮在II期和III期临床试验中是有效的避孕药,大多数女性保持规律和可预测的出血周期。雌四醇/屈螺酮对报告为最常见的治疗相关不良事件的子宫出血的耐受性良好。这与其他COCs是一致的。有先兆偏头痛(或严重偏头痛)的病例,深静脉血栓形成,在III期试验期间,很少有高钾血症和抑郁症的报道.总的来说,雌四醇/屈螺酮是一种有效且耐受性良好的COC,潜在的血栓形成风险降低。
2019年,全球15-49岁的女性中估计有44%使用现代避孕方法。在这些使用现代方法的女性中,18%使用口服避孕药。雌四醇/屈螺酮是一种联合口服避孕药(COC),使用雌四醇,一种由人类胎儿肝脏在怀孕期间自然产生的植物合成的雌激素,与屈螺酮结合,一种著名的孕激素.合并,这些激素抑制排卵,这构成了他们预防怀孕的主要作用方式。由于雌四醇的雌激素相关作用较弱,它可能会降低血栓的风险。雌四醇/屈螺酮在临床试验中是一种有效的避孕药,大多数女性有规律和可预测的出血周期。子宫出血(即异常出血)是最常见的治疗相关不良反应;然而,这是荷尔蒙避孕药的常见问题。严重偏头痛的病例,深静脉血栓形成,在临床试验中很少报道高钾水平或抑郁。雌四醇/屈螺酮是一种有效的口服避孕药,这可能提供了一种避孕选择,血栓风险较低。然而,需要进一步的研究来证实凝血风险的降低.
Estetrol/drospirenone is a combined oral contraceptive (COC) with a plant-synthesised foetal oestrogen (
estetrol) and a well-established progestin (drospirenone). In preclinical models,
estetrol has lower binding affinity for the oestrogen receptor-α (ER-α) in contrast to estradiol and has antagonistic properties against membrane ER-α in several tissues, including the breast, while retaining agonistic activity on receptors located in the nucleus. The low oestrogenicity of
estetrol may potentially contribute to reduced thrombotic risk. Estetrol/drospirenone was an effective contraceptive in phase II and III clinical trials, with regular and predictable bleeding cycles maintained in the majority of women. Estetrol/drospirenone was generally well-tolerated with metrorrhagia reported as the most common treatment-related adverse event, which is consistent with other COCs. Cases of migraines with aura (or severe migraines), deep vein thrombosis, hyperkalaemia and depression were rarely reported during the phase III trials. Overall, estetrol/drospirenone is an effective and generally well-tolerated COC, with a potentially reduced risk of thrombosis.
In 2019, an estimated 44% of women aged 15–49 years worldwide used modern contraception methods, and in these women using modern methods, 18% used an oral contraceptive.
Estetrol/drospirenone is a combined oral contraceptive (COC) which uses
estetrol, a plant-synthesised oestrogen naturally produced by the human foetal liver during pregnancy, in combination with drospirenone, a well-known progestin. Combined, these hormones suppress ovulation, which constitutes their primary mode of action in preventing pregnancy. As estetrol has weaker oestrogen-related effects, it may potentially reduce the risk for blood clots. Estetrol/drospirenone was an effective contraceptive in clinical trials, and most women had regular and predictable bleeding cycles. Metrorrhagia (i.e. abnormal bleeding) was the most commonly reported treatment-related adverse effect; however, this is a common issue with hormonal contraceptives. Cases of severe migraine headaches, deep vein thrombosis, high potassium levels or depression were rarely reported during clinical trials. Estetrol/drospirenone is an effective oral contraceptive, which may offer a contraceptive option with a lower risk for blood clots. However, further research is required to confirm the reduced risk of clotting.