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Ormeloxifene

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In this page talks about ( Ormeloxifene ) It was sent to us on 16/06/2021 and was presented on 16/06/2021 and the last update on this page on 16/06/2021

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{{Drugbox
Verifiedfields = changed
Watchedfields = changed
verifiedrevid = 461741567
IUPAC_name = 1-2-4-(3S,4S)-7-methoxy-2,2-dimethyl-3-phenyl-chroman-4-ylphenoxyethylpyrrolidine
image = Ormeloxifene structure.svg
width = 225px
tradename = Centron, Novex-DS, Saheli, Sevista, Chhaya
pregnancy_AU =
pregnancy_US =
pregnancy_category =
legal_AU =
legal_CA =
legal_UK =
legal_US = Not FDA approved
legal_status = Rx-only in India
routes_of_administration = By mouth
class = Selective estrogen receptor modulator
bioavailability =
protein_bound =
metabolism =
elimination_half-life = 7 days
excretion =
CAS_number_Ref =
CAS_number = 78994-24-8
ATC_prefix = G03
ATC_suffix = XC04
PubChem = 154413
DrugBank_Ref =
ChemSpiderID_Ref =
ChemSpiderID = 32935
UNII_Ref =
UNII = 44AXY5VE90
KEGG_Ref =
KEGG = D08301
ChEMBL_Ref =
ChEMBL = 301327
synonyms = Centchroman
C=30 H=35 N=1 O=3
SMILES = CC1(C@@H(C@H(c2ccc(cc2O1)OC)c3ccc(cc3)OCCN4CCCC4)c5ccccc5)C
StdInChI_Ref =
StdInChI = 1S/C30H35NO3/c1-30(2)29(23-9-5-4-6-10-23)28(26-16-15-25(32-3)21-27(26)34-30)22-11-13-24(14-12-22)33-20-19-31-17-7-8-18-31/h4-6,9-16,21,28-29H,7-8,17-20H2,1-3H3/t28-,29+/m0/s1
StdInChIKey_Ref =
StdInChIKey = XZEUAXYWNKYKPL-URLMMPGGSA-N
Ormeloxifene, also known as centchroman, is one of the selective estrogen receptor modulators, or SERMs, a class of medication which acts on the estrogen receptor. It is best known as a nonsteroidal oral contraceptive which is taken once per week. In India, ormeloxifene has been available as birth control since the early 1990s, and it was marketed there under the trade name Saheli, currently available free-of-cost for the women in India as Chhaya (Centchroman). {{Cite webdate=2017-07-28title=New Contraceptivesurl=https://humdo.nhp.gov.in/new-contraceptives/access-date=2020-06-29website=Hum Do Family Planninglanguage=en-US{{Cite weblast1=7 Aprfirst1=Ishita Bhatia TNN last2=2018last3=Istfirst3=13:08title=antara chhaya: Two months after launch, Antara, Chhaya contraceptives get good response from locals Meerut News - Times of Indiaurl=https://timesofindia.indiatimes.com/city/meerut/two-months-after-launch-antara-chhaya-contraceptives-get-good-response-from-locals/articleshow/63633454.cmsaccess-date=2020-06-29website=The Times of Indialanguage=en Ormeloxifene has also been licensed under the trade names Novex-DS, Centron, and Sevista.

Medical uses

Ormeloxifene is primarily used as a contraceptive but may also be effective for dysfunctional uterine bleeding and advanced breast cancer.

Birth control

Ormeloxifene may be used as a weekly oral contraceptive. The weekly schedule is an advantage for women who prefer an oral contraceptive, but find it difficult or impractical to adhere to a daily schedule required by other oral contraceptives.
For the first twelve weeks of use, it is advised to take the ormeloxifene pill twice per week. From the thirteenth week on, it is taken once per week.http://www.reproline.jhu.edu/english/1fp/1advances/old/1centch/ceorvw.htm
The consensus is that backup protection in the first month is a cautious but sensible choice. A standard dose is 30 mg weekly, but 60 mg loading doses can reduce pregnancy rates by 38%.
It has a failure rate of about 1-2% with ideal use which is slightly less effective than found for combined oral contraceptive pills.

Other indications

  • Ormeloxifene has also been tested in experimental setting as a treatment for menorrhagia.
  • use in treatment of mastalgia and fibroadenoma has also been described.

Side effects

There are concerns that ormeloxifene may cause delayed menstruation.

Pharmacology

Ormeloxifene is a selective estrogen receptor modulator (SERM). In some parts of the body, its action is estrogenic (e.g., bones), in other parts of the body, its action is antiestrogenic (e.g., uterus, breasts).{{Cite webtitle=CSIR-CDRI Homeurl=https://cdri.res.in/Centchroman.aspxaccess-date=2020-06-29website=cdri.res.inGara Rishi Kumar, Konwar Rituraj, Bid Hemant K and MM Singh. In-vitro anti-cancer breast activity of ormeloxifene is mediated via induction of apoptosis and autophagy. 37th annual conference of the endocrine society of India. 30 Nov – 2 Dec 2007. Abstract p. 35. It causes an asynchrony in the menstrual cycle between ovulation and the development of the uterine lining, although its exact mode of action is not well defined. In clinical trials, it caused ovulation to occur later than it normally would in some women, but did not affect ovulation in the majority of women, while causing the lining of the uterus to build more slowly. It speeds the transport of any fertilized egg through the fallopian tubes more quickly than is normal. Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.

History

Ormeloxifene was first discovered by Central Drug Research Institute (CDRI) in Lucknow, India. Ormeloxifene was marketed in Delhi in July 1991 and in India in 1992, under the brand names Saheli and Choice-7.
Since 2018, Centchroman is provided free-of-cost to the women in India by the government under the brand name Chhaya.

Society and culture

Marketing

As of 2009, ormeloxifene was legally available only in India.
Ormeloxifene has been tested and licensed as a form of birth control, as well as a treatment for dysfunctional uterine bleeding.
  • manufactured by Torrent Pharmaceuticals, and marketed as birth control under the trade name Centron. Centron was discontinued.
  • A new license for ormeloxifene was issued to Hindustan Latex Ltd., which now manufactures ormeloxifene as birth control under the trade names Saheli, Novex, and Novex-DS.
  • Torrent Pharmaceuticals has resumed manufacture of ormeloxifene under the trade name Sevista, as a treatment for dysfunctional uterine bleeding.

See also

  • Levormeloxifene

  • Further reading

  • External links

    • United States National Library of Medicine Centchroman entry in the Medical Subject Headings (MeSH) database
    • Reproductive Health Online, a Johns Hopkins University affiliate providing information on Centchroman
    • Central Drug Research Institute, Lucknow, India: a government-funded laboratory, conducting R&D on Centchroman as birth control.
    • Ministry of Health and Family Welfare - Indian government site; information about availability of Saheli.

    Category:Chromanes
    Category:Drugs acting on the genito-urinary system
    Category:Hormonal contraception
    Category:Phenol ethers
    Category:Pyrrolidines
    Category:Selective estrogen receptor modulators
     
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