炔诺孕酮性质、用途与生产工艺
左炔诺孕酮是一种速效、短期口服避孕药,避孕机制是显著抑制排卵和阻止孕卵着床,并使宫颈黏液稠度增加,精子穿透阻力增大,从而发挥速效避孕作用。单用孕激素或用孕激素与雌激素配伍,现已制成品种繁多的女性避孕药,以口服、外用和注射的方式达到避孕目的的药物,目前只用于妇女。
左炔诺孕酮为口服强效孕激素,其孕激素作用约为炔诺酮的5~10倍,并有雄激素、雌激素和抗雌激素活性。主要作用于下丘脑和垂体,使月经中期血中的促卵泡激素和促黄体生成激素水平高峰降低或消失,促使卵巢不排卵。可使宫颈黏液变稠,阻碍精子穿透,又可使子宫内膜变薄,分泌功能不良,不利于孕卵着床。
Norgestrel 是孕酮的合成类似物,是口服避孕药中常见的化合物,也是一种强大的神经保护性抗氧化剂,可防止光诱导的感光细胞中的 ROS 的生成以及细胞死亡。
Norgestrel (20 µM; 24 hours; 661W cells) treatment significantly increases cellular viability after serum deprivation and so it is demonstrated that Norgestrel is neuroprotective to stressed 661W cells.
Norgestrel (20 µM; 24 hours; 661W cells) treatment decreases apoptotic induced cleavage of PARP and caspase-3.
Norgestrel (20 µM; 6 hours; 661W cells) treatment bFGF is results in a significant upregulation of bFGF mRNA in photoreceptor cells.
Cell Viability Assay
Cell Line:
|
661W cells
|
Concentration:
|
20 µM
|
Incubation Time:
|
24 hours
|
Result:
|
Significantly increased cellular viability after serum deprivation.
|
Western Blot Analysis
Cell Line:
|
661W cells
|
Concentration:
|
20 µM
|
Incubation Time:
|
24 hours
|
Result:
|
Decreased apoptotic induced cleavage of PARP and caspase-3.
|
RT-PCR
Cell Line:
|
661W cells
|
Concentration:
|
20 µM
|
Incubation Time:
|
6 hours
|
Result:
|
A significant upregulation of bFGF mRNA over 1 hour.
|
Norgestrel (100 mg/kg; intraperitoneal injection; for 6, 24 or 48 hours; Balb/c mice) treatment can prevent light-induced ROS in photoreceptor cells, and subsequent cell death. Norgestrel acts via post-translational modulation of the major antioxidant transcription factor Nrf2; bringing about its phosphorylation, subsequent nuclear translocation, and increases levels of its effector protein superoxide dismutase 2 (SOD
2
).
Animal Model:
|
Balb/c mice are born into and maintained in dim cyclic light
|
Dosage:
|
100 mg/kg;
|
Administration:
|
Intraperitoneal injection; for 6, 24 or 48 hours
|
Result:
|
Increased expression and activation of Nrf2 via phosphorylation on serine 40, increased expression of its target antioxidant superoxide dismutase 2 (SOD
2
), and reduced mitochondrial oxidative stress.
|
1. 用作短效口服避孕药:口服复方炔诺酮一号片或滴丸,从月经第5天开始,每天服1片(丸),连服22天,不能间断,停药后2~4天来月经,然后于第5天继续服用下一个月的药。
2. 用作探亲避孕药:于探亲当晚开始服炔诺孕酮探亲避孕药,每天1片,服法同炔诺酮。
3. 用作事后避孕药:房事后72小时内口服2片复方炔诺孕酮事后避孕片,12小时后再服2片。
1. 较常见的有胃纳差、痤疮、液体潴留和水肿、体重增加、过敏性皮肤炎症、精神压抑、乳房疼痛、女性性欲改变、月经紊乱、不规则出血或闭经。
2. 少见的有头痛,胸、臀、腿特别是腓肠肌处疼痛,手臂和脚无力、麻木或疼痛,突然的或原因不明的呼吸短促,突然语言发音不清,突然视力改变、复视、不同程度失明等。
3. 长期应用可引起肝功能异常,缺血性心脏病发生率上升,妊娠早期时应用可能导致雄激素活性高引起的后代女婴男性化以及生殖道畸形(多见为尿道下裂)。
1. 与利福平、氯霉素、氨苄西林、苯巴比妥、苯妥英钠、扑米酮、甲丙氨酯、氯氮平、对乙酰氨基酚及吡唑酮类镇痛药(保泰松)等同服可产生肝微粒体酶效应,加速炔酮在体内的代谢,导致避孕失败、突破性出血发生率增高。
2. 维生素C能增强口服避孕药的作用,每天口服1g维生素C可使炔雌醇生物利用度从40%提高到60%~70%。
3. 与环孢素合用,可抑制环孢素的代谢清除,致其毒性增强,应避免合用。
复方炔诺孕酮一号片(或滴丸):每片(丸)含炔诺孕酮0.3mg和炔雌醇0.03mg。炔诺孕酮探亲避孕片:每片含炔诺孕酮3mg。复方炔诺孕酮事后避孕片:每片含炔诺孕酮1mg和炔雌醇0.1mg。
化学性质
白色或类白色结晶性粉末,无臭,无味。不溶于水,溶于氯仿,微溶于甲醇。
用途
避孕药。
炔诺孕酮
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