Ormeloxifene

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Ormeloxifene
ファイル:Ormeloxifene structure.svg
Systematic (IUPAC) name
1-[2-[4-[(3S,4S)-7-methoxy-2,2-dimethyl-3-phenyl-chroman-4-yl]phenoxy]ethyl]pyrrolidine
Clinical data
Trade names Centron, Novex-DS, Saheli, Sevista, Chhaya
Pregnancy cat. ?
Legal status ? (US) Rx-only in India
Routes By mouth
Pharmacokinetic data
Half-life 7 days
Identifiers
CAS number 31477-60-8 N
ATC code G03XC04
PubChem CID 154413
ChemSpider 32935 YesY
UNII 44AXY5VE90 YesY
KEGG D08301 YesY
ChEMBL CHEMBL301327 YesY
Synonyms Centchroman
Chemical data
Formula C30H35NO3 
 N (what is this?)  (verify)

テンプレート:Infobox Birth control

Ormeloxifene, also known as centchroman, is one of the selective estrogen receptor modulators,[1] 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,[2] currently available free-of-cost for the women in India as Chhaya (Centchroman).[3][4]

Ormeloxifene has also been licensed under the trade names Ormalin, 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.[5]

Birth control

Ormeloxifene may be used as a weekly oral contraceptive.[5] 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.[citation needed]

For the first twelve weeks of use, it is advised to take the ormeloxifene pill twice per week.[5] From the thirteenth week on, it is taken once per week.[5][6] 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%.[7]

It has a failure rate of about 1-2% with ideal use which is slightly less effective than found for combined oral contraceptive pills.[8]

Other indications

Side effects

There are concerns that ormeloxifene may cause delayed menstruation.[11]

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).[12][13][14] 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,[8] 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.[8] Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.[8]

History

Ormeloxifene was first discovered by Central Drug Research Institute (CDRI) in Lucknow, India.[12][15] Ormeloxifene was marketed in Delhi in July 1991 and in India in 1992, under the brand names Saheli and Choice-7.[8][16]

Since 2018, Centchroman is provided free-of-cost to the women in India by the government under the brand name Chhaya.[3][17][18][19]

Society and culture

Marketing

As of 2009, ormeloxifene was legally available only in India.[20]

Ormeloxifene has been tested and licensed as a form of birth control, as well as a treatment for dysfunctional uterine bleeding.[citation needed]

  • 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

References

  1. ↑ Makker A, Tandon I, Goel MM, Singh M, Singh MM (6月 2009). "Effect of ormeloxifene, a selective estrogen receptor modulator, on biomarkers of endometrial receptivity and pinopode development and its relation to fertility and infertility in Indian subjects". Fertility and Sterility. 91 (6): 2298–2307. doi:10.1016/j.fertnstert.2008.04.018. PMID 18675966.
  2. ↑ "HLL - Product Overview". Archived from the original on 1 11月 2018. {{cite web}}: |archive-date= / |archive-url= timestamp mismatch; 1 11月 2018 suggested (help)
  3. ↑ 3.0 3.1 "Chhaya". Centre for Health Informatics (CHI) of the National Health Portal (NHP), by the Ministry of Health and Family Welfare (MoHFW). Government of India. Archived from the original on 11 5月 2021. Retrieved 29 6月 2020. {{cite web}}: |archive-date= / |archive-url= timestamp mismatch; 11 5月 2021 suggested (help)
  4. ↑ "Contraception and women's empowerment: Here's how safe, reliable contraceptives are freeing women to earn". Hindustan Times (in English). 10 7月 2018. Retrieved 29 6月 2020.
  5. ↑ 5.0 5.1 5.2 5.3 Lal J (4月 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.
  6. ↑ "Home | ReproLinePlus".
  7. ↑ Lal J, Nitynand S, Asthana OP, Nagaraja NV, Gupta RC (1月 2001). "Optimization of contraceptive dosage regimen of Centchroman". Contraception. 63 (1): 47–51. doi:10.1016/S0010-7824(00)00189-X. PMID 11257249.
  8. ↑ 8.0 8.1 8.2 8.3 8.4 Singh MM (7月 2001). "Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders". Medicinal Research Reviews. 21 (4): 302–347. doi:10.1002/med.1011. PMID 11410933. S2CID 37474826.
  9. ↑ Kriplani A, Kulshrestha V, Agarwal N (8月 2009). "Efficacy and safety of ormeloxifene in management of menorrhagia: a pilot study". The Journal of Obstetrics and Gynaecology Research. 35 (4): 746–752. doi:10.1111/j.1447-0756.2008.00987.x. PMID 19751337. S2CID 39172838.
  10. ↑ Dhar A, Srivastava A (6月 2007). "Role of centchroman in regression of mastalgia and fibroadenoma". World Journal of Surgery. 31 (6): 1178–1184. doi:10.1007/s00268-007-9040-4. PMID 17431715. S2CID 22828570.
  11. ↑ Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB (3月 2008). "Selective estrogen receptor modulators: an update on recent clinical findings". Obstetrical & Gynecological Survey. 63 (3): 163–181. doi:10.1097/OGX.0b013e31816400d7. PMID 18279543. S2CID 23585991.
  12. ↑ 12.0 12.1 "CSIR-CDRI | Home". cdri.res.in. Retrieved 29 6月 2020.
  13. ↑ テンプレート:Cite conference
  14. ↑ Nigam M, Ranjan V, Srivastava S, Sharma R, Balapure AK (3月 2008). "Centchroman induces G0/G1 arrest and caspase-dependent apoptosis involving mitochondrial membrane depolarization in MCF-7 and MDA MB-231 human breast cancer cells". Life Sciences. 82 (11–12): 577–590. doi:10.1016/j.lfs.2007.11.028. PMID 18279897.
  15. ↑ "Centchroman". CSIR-CDRI. Archived from the original on 14 2月 2019. Retrieved 25 9月 2018. {{cite web}}: |archive-date= / |archive-url= timestamp mismatch; 14 2月 2019 suggested (help)
  16. ↑ Lal J (4月 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.
  17. ↑ "परिवार नियोजन विधियों में छाया से अधिक अंतरा में बढ़ी महिलाओं की दिलचस्पी, जानिये इनके बारे में". Patrika News (in hindi). 22 5月 2018. Retrieved 29 6月 2020.{{cite web}}: CS1 maint: unrecognized language (link)
  18. ↑ Bhatia I (7 4月 2018). "antara chhaya: Two months after launch, Antara, Chhaya contraceptives get good response from locals". The Times of India (in English). Retrieved 29 6月 2020.
  19. ↑ Shelar J (12 1月 2018). "BMC rolls out new contraceptive pill". The Hindu (in English). ISSN 0971-751X. Retrieved 29 6月 2020.
  20. ↑ Tribhuwan RD, Patil BD (2009). Body image : human reproduction and birth control : a tribal perspective. New Delhi: Discovery Pub. House. p. 20. ISBN 978-81-8356-388-8.

Further reading

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  • Ray S, Grover PK, Kamboj VP, Setty BS, Kar AB, Anand N (2月 1976). "Antifertility agents. 12. Structure-activity relationship of 3,4-diphenylchromenes and -chromans". Journal of Medicinal Chemistry. 19 (2): 276–279. doi:10.1021/jm00224a014. PMID 1249807.

External links

テンプレート:Birth control methods テンプレート:Other sex hormones and modulators of the genital system

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