部份中文地诺孕素处方资料（仅供参考）
英文名：Dienogest
商品名：DINAGEST Tab
中文名：地诺孕素片
生产商：日本持田制药公司
药品介绍
子宫内膜异位症的治疗药是由日本Mochida开发为子宫内膜异位症的治疗剂。这是一种新型的口服药物, 可选择性地激活黄体酮受体, 并通过抑制卵巢功能和子宫内膜细胞增殖来显示其治疗效果。
ディナゲスト錠1mg
药用类别名称
子宫内膜异位症治疗与子宫腺肌病的改善治疗方法
批准日期：2016年12月
商標名
DINAGEST Tab. 1mg
一般名：ジエノゲスト（Dienogest）
化学名：17-Hydroxy-3-oxo-19-nor-17α-pregna-4,9-diene-21-nitrile
構造式：
分子式：C20H25NO2
分子量：311.42
性状：
Dienoguest 是一种白色到细黄的白色结晶粉末。 本品不溶于甲醇, 不易溶于乙醇 (99.5), 几乎不溶于水。
熔点: 210 至218°c
批准条件
制定药品风险管理计划并加以实施。
药用药理学
1. 作用机制
该制剂对孕激素受体具有选择性激动作用, 相信通过抑制卵巢功能抑制和子宫内膜细胞, 改善子宫内膜异位症的疗效和子宫腺肌症的疼痛。
2. 对类固醇激素受体的影响
(1) 受体激动剂活性
利用与人类类固醇激素受体基因转染的细胞进行的体外测试显示, 黄体酮受体具有选择性激动剂活性。
(2) 孕酮作用
在使用大鼠和兔子的体内测试中, 黄体酮对子宫有影响。另一方面, 雄激素效应、糖皮质激素作用和矿物皮质类固醇效应没有表现出来。
3. 卵巢功能的抑制作用
(1) 健康的成年妇女
当药物 1天2mg 对健康成年妇女口服21天, 抑制血清雌二醇和黄体酮浓度的增加观察到在正常月经周期中观察到, 失去短暂增加的血清LH和FSH 浓度。
(2) 子宫内膜异位症患者
当药物 1天1~4毫克为子宫内膜异位症患者口服时, 血清雌二醇浓度随剂量的增加而降低。 此外, 在该制剂1天1~4毫克*, 血清黄体酮浓度小于卵泡期的参考值的所有情况下, 建议排卵抑制。
(3) 子宫腺肌症患者
本制剂1天1mg子宫腺肌症患者, 当2毫克或安慰剂16周口服*时, 血清雌二醇浓度显示低值随剂量的增加。 此外, 血清雌二醇浓度在目前的制剂1天2mg是一个较低的价值相比安慰剂, 血清雌二醇浓度的抑制作用观察。
*: 此制剂的已批准使用剂量是 "每天口服两次2毫克"。
4. 对子宫内膜的影响
(1) 子宫内膜细胞的生长抑制作用
体外试验, 利用人子宫内膜间质细胞, 观察细胞增殖的抑制作用。
(2) 子宫内膜的假脱落
在子宫内膜异位症患者的临床药理研究中, 当制剂 1天2mg 口服16周时, 观察到该制剂的黄体酮作用对子宫内膜的假脱落。
5. 实验性子宫内膜异位症的影响
在大鼠和家兔实验性子宫内膜异位症试验中, 观察到对移植子宫内膜碎片体积减少或重量的抑制增加, 提示了对子宫内膜异位症的治疗作用。
适应症
● 子宫内膜异位症
● 子宫腺肌症相关疼痛的改善
用法与用量
通常情况下, 成人被分为两次, 每天2毫克作为二分最食, 从月经周期2-5 口服。
包装
PTP：100錠
制造和销售来源
持田製薬
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明附件：http://www.info.pmda.go.jp/go/pack/2499010F1023_1_10/
Norovirus is a new contraceptive drug developed by JENAPHARM, Germany, and is used for oral contraception due to its powerful ovulation inhibition.
The 1995-year Enoxaparin and acetylene combination preparation (2MG+0.03MG), listed in Germany as a contraceptive pill, was listed in Australia in 2007 with a Valette of commodity names.
2001-year combination of norovirus and estradiol two alcohol valproate (including Enoxaparin 2mg and female two alcohols 1 or 2mg) listed in Germany by Schering company, used for hormone replacement therapy for estrogen deficiency in women for more than one year.
2002 in Denmark, France, Belgium and other European countries listed, the name of the commodity Climodien.
2007-year Norovirus tablets (1mg) are listed in Japan for the treatment of endometriosis.
2008.3.31 Bayer Pharma applied for the import of female valproate two alcohols (five-phase) in clinical practice, and a review plan is being developed. Enoxaparin is a mixture of progesterone and has the pharmacological advantages of natural and synthetic progesterone. Norovirus has a high progesterone activity, and its oral semi-effective dose is 0.11mg/kg. The endocrine pharmacological properties of enoxaparin are ideal, because they are only combined with progesterone receptors, so there is no estrogen, anti-estrogen and androgen activity, anti-gonadotropin action (inhibiting the secretion of follicle-stimulating hormones and luteal hormones) is also very weak.
The lowest effective dose of oral norovirus to inhibit ovulation in normal women is only 1mg/days. The effect of 17β-on ovulation inhibition is mainly achieved through its peripheral mechanism, such as inhibiting ovulation and ovarian female two alcohol peak, rather than the central mechanism affecting gonadotropin secretion.
Normal menstrual women during the treatment of oral 2mg/, their serum progesterone was reduced to non-ovulation level, but serum follicle-stimulating hormone and luteal hormone levels were not much affected.
From the ratio of ovulation inhibition dose (mg/days) to intrauterine membrane conversion dose (mg/menstrual cycle), ketamine acetate, levonorgestrel and progesterone were L, levofloxacin and Nordson were 3, ciprofloxacin acetate and ketamine acetate were 5~7, and was as high as l7 in the same way as in the case.
Enoxaparin shows an obvious characteristic of peripheral action, similar to that produced by natural flavonoids, which is beneficial to endometrium.
Enoxaparin also has a certain anti-androgen activity. The improved Hershberger method was carried out to detect the gonadal resection male rats treated with testosterone, and it was found that the anti-androgen activity of Enoxaparin was greater than that of ketamine acetate, which was about 40% of ciprofloxacin acetate. After normal treatment, women treated 3 menstrual cycles (21 days before the menstrual cycle and 7 days after the withdrawal of the drug) by oral 2mg/, and the level of serum androgenic diol glucose acetaldehyde could be reduced by 38%, the total testosterone level in serum decreased 17~40%,
Free testosterone levels decreased by 48~54%, and the level of dehydroepiandrosterone sulfate decreased by 51%. Enoxaparin does not bind to steroid transporter protein and does not affect the level of serum prolactin, cortisol binding globulin and sex hormone binding globulin in normal women.
There is also no glucocorticoid and salt corticosteroid activity in Enoxaparin, but the anti-hyperplasia effect has been confirmed by experiments in vivo and outside. The absorption of oral enoxaparin was complete and rapid, with absolute bioavailability greater than 90%, and the maximum serum and plasma concentrations were about 2 and l~2 hours, respectively.
In plasma, about 10% of the norovirus is present in the free form, and the proportion of this bioactive part is quite higher than that of progesterone (0.5~4%).
Another 90% of the heparin in the plasma binds to plasma albumin. Enoxaparin is metabolized mainly through aromatic and 11β-hydroxyl, and metabolites are quickly eliminated from urine within 24 hours of administration.
The plasma half-life of enoxaparin is shorter than that of other progesterone, only 6.5~l2 hours, so the daily administration also has no accumulation, this property is also better than levonorgestrel progesterone.
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