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The state-of-the-art of emergency contraception with the cutting edge drug

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 progest...

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Autor principal: Sarkar, Narendra Nath
Formato: Online Artículo Texto
Lenguaje:English
Publicado: German Medical Science GMS Publishing House 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3141844/
https://www.ncbi.nlm.nih.gov/pubmed/21808601
http://dx.doi.org/10.3205/000139
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author Sarkar, Narendra Nath
author_facet Sarkar, Narendra Nath
author_sort Sarkar, Narendra Nath
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description 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.
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spelling pubmed-31418442011-08-01 The state-of-the-art of emergency contraception with the cutting edge drug Sarkar, Narendra Nath Ger Med Sci Article 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. German Medical Science GMS Publishing House 2011-07-11 /pmc/articles/PMC3141844/ /pubmed/21808601 http://dx.doi.org/10.3205/000139 Text en Copyright © 2011 Sarkar http://creativecommons.org/licenses/by-nc-nd/3.0/ 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 copy, distribute and transmit the work, provided the original author and source are credited.
spellingShingle Article
Sarkar, Narendra Nath
The state-of-the-art of emergency contraception with the cutting edge drug
title The state-of-the-art of emergency contraception with the cutting edge drug
title_full The state-of-the-art of emergency contraception with the cutting edge drug
title_fullStr The state-of-the-art of emergency contraception with the cutting edge drug
title_full_unstemmed The state-of-the-art of emergency contraception with the cutting edge drug
title_short The state-of-the-art of emergency contraception with the cutting edge drug
title_sort state-of-the-art of emergency contraception with the cutting edge drug
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3141844/
https://www.ncbi.nlm.nih.gov/pubmed/21808601
http://dx.doi.org/10.3205/000139
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