The state-of-the-art of emergency contraception with the cutting edge drugStand der Wissenschaft und Technik bei der Notfall-Kontrazeption mit innovativen Arzneimitteln

GMS German Medical Science — an Interdisciplinary Journal

Narendra Nath Sarkar¹ 

[1] Department of Reproductive Biology, All India Institute of Medical Sciences, Ansari Nagar, New Dellhi, India

关键词: antagonists;    agonists;    EC;    ulipristal acetate;    steroid ligands;    receptor modulator;   

Others  :  869205

实施日期：2011-04-08，发布日期：2011-07-11

【 摘 要 】

The objective of this study is to evaluate and elucidated the potential of selective progesterone receptor modulators (SPRMs) to be an effective emergency contraception (EC). The data are extracted from the literature through the MEDLINE database service from 2000–2010.

The SPRMs are in fact progesterone receptor ligands that could bind to progesterone receptor (PR) and exert antagonistic, agonistic or mixed agonist-antagonistic effects. These SPRMs are mifepristone, onapristone, asoprisnil, ulipristal, proellex among other compounds.

Currently developed SPRMs may exert contraceptive effects by inhibiting ovulation and retarding endometrial synchronization. Low-doses of progesterone antagonists retard endometrial maturation without affecting ovulation. Mifepristone being a SPRM is effective for prevention of pregnancy but with prostaglandin acts as an excellent abortifacient; yet could not compete with levonorgestrel as EC. However, a single dose of 30 mg ulipristal acetate, another SPRM with similar effectiveness and side effect profiles as 1.5 mg levonorgestrel EC, has shown wider ‘window of effect’ by inhibition of the LH peak even if administered at the advanced pre-ovulatory phase, a time when use of levonorgestrel EC is no longer effective. Thus, ulipristal acetate goes one-step ahead of levonorgestrel in the field of emergency contraception treatment.

Further studies are needed to explore the potential of other SPRMs to be cutting edge emergency contraceptive drugs.

【 授权许可】

   
© 2011 Sarkar.This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by-nc-nd/3.0/deed.en). You are free: to Share – to copy, distribute and transmit the work, provided the original author and source are credited.

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