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外観
白色～黄色～緑色粉末～結晶
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効能
避妊薬, プロゲステロン受容体作動/拮抗薬
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説明
Ulipristal acetate is a synthetic steroid derived from 19-nor-progesterone that exerts potent progesterone receptor (PR) antagonist activity at
the transcriptional level. It is an orally administered drug indicated for
emergency contraception (i.e., postcoital contraception) up to 120 h following unprotected intercourse. Ulipristal acetate is the second oral progestogen marketed for this indication behind levonorgestrel. As PR
antagonists, both drugs are believed to act via delay of ovulation and
inhibition of follicular development. Levonorgestrel 1.5 mg is approved
for contraception up to 72 h following unprotected intercourse and is
widely accessible via prescription, and directly from clinics and community pharmacies. Prior to ulipristal acetate, the only approved postcoital
contraceptive option between 72 and 120 h was the insertion of an intrauterine device (IUD). The recommended dose of ulipristal acetate is one
30-mg tablet taken as soon as possible and no more than 120 h following
intercourse. The vast majority of PR antagonists belonging to the mifepristone (RU486) family also bind to the glucocorticoid receptor (GR)
with high affinity and thereby exert antiglucocorticoid activity.
The most common adverse effects with ulipristal acetate were headache, dysmenorrhea, nausea, abdominal pain, dizziness, fatigue, and upper abdominal pain.
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化学的特性
Pale Yellow Solid
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使用
Ulipristal acetate is a selective progesterone receptor modulator
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定義
ChEBI: A 20-oxo steroid obtained by acetylation of the 17-hydroxy group of (11beta,17alpha)-17-acetyl-11-[4-(dimethylamino)phenyl]-3-oxoestra-4,9-dien-17-ol (ulipristal). A selective progesterone receptor modulator, which is empl
yed as an emergency contraceptive.
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臨床応用
Ulipristal acetate, a selective progesterone receptor modulator
(SPRM), was developed at the Research Triangle Institute. In
2009, HRA Pharma received FDA approval for emergency contraception
within 120 h (5 days) of unprotected sexual intercourse or contraceptive failure. Ulipristal acetate is a well-known steroid
that possesses antiprogestational and antiglucocorticoid activity.
It is the first SPRM that was specifically designed as an oral
emergency contraceptive. Unlike earlier levonorgestrel-based
emergency contraceptives, this SPRM drug maintains efficacy for
5 days after unprotected intercourse while having safety profile
comparable to levonorgestrel.
