Žigová Lucia, Massarová Petra, Vranecová Katarína, Hrubá Orsolya, Adamičková Adriana, Gažová Andrea
Ceska Slov Farm. 2022 Fall;71(4):142-150.
Pregnancy and postpartum period are associated with demanding physical and psychological changes that often lead to the development of psychological disorders. Depression is diagnosed in more than one in six women after childbirth. However, the prevalence of postpartum depression can be much higher because many cases are undiagnosed. In the case of severe depression, the patient is switched to pharmacological treatment, with sertraline being the most commonly used for this diagnosis. A new drug used in the treatment of postpartum depression is brexanolone, which was registered by FDA in 2019. The advantage over conventional therapy is its rapid onset of action. The structure represents the neuroactive steroid - allopregnanolone, which acts as an agonist on the δ-subunit of the GABA receptor and improves the symptoms of postpartum depression. In addition to the registered brexanolone, another steroidal drug, zuranolone, is available in the third phase of the clinical trial. The steroid structure was chemically altered to improve bioavailability and create an oral dosage form. Another synthetic analogue of neuroactive allopregnanolone, known as ganaxolone, did not show a significant reduction in depressive symptoms in the second phase of the clinical trial compared to placebo. Nevertheless, it has great therapeutic potential in the treatment of various types of epilepsy.
怀孕和产后时期伴随着要求苛刻的生理和心理变化，这些变化常常导致心理障碍的发展。超过六分之一的女性在产后被诊断出患有抑郁症。然而，产后抑郁症的患病率可能更高，因为许多病例未被诊断出来。对于重度抑郁症患者，会转而采用药物治疗，舍曲林是最常用于该诊断的药物。一种用于治疗产后抑郁症的新药是布雷沙诺龙，它于2019年被美国食品药品监督管理局（FDA）批准上市。与传统疗法相比，其优势在于起效迅速。其结构代表神经活性甾体——别孕烯醇酮，它作为GABA受体的δ亚基的激动剂，可改善产后抑郁症的症状。除了已获批的布雷沙诺龙外，另一种甾体药物——祖拉诺龙正处于临床试验的第三阶段。对甾体结构进行了化学改造以提高生物利用度并制成口服剂型。神经活性别孕烯醇酮的另一种合成类似物——加奈索酮，在临床试验的第二阶段与安慰剂相比，并未显示出抑郁症状有显著减轻。尽管如此，它在治疗各种类型的癫痫方面具有巨大的治疗潜力。
