| Systematic (IUPAC) name | |
|---|---|
| 1-[2-[4-[(3S,4R)-7-methoxy-2,2- dimethyl-3-phenyl-chroman-4-yl] phenoxy] ethyl] pyrrolidine | |
| Clinical data | |
| Trade names | Centron, Novex-DS, Saheli, Sevista |
| Pregnancy cat. | ? |
| Legal status | ? |
| Routes | Oral |
| Pharmacokinetic data | |
| Half-life | 7 days |
| Identifiers | |
| CAS number | 78994-24-8 |
| ATC code | None |
| PubChem | CID 154413 |
| ChemSpider | 32935 |
| UNII | 44AXY5VE90 |
| KEGG | D08301 |
| ChEMBL | CHEMBL301327 |
| Synonyms | Centchroman |
| Chemical data | |
| Formula | C30H35NO3 |
| Mol. mass | 457.604 g/mol |
| SMILES | eMolecules & PubChem |
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| (what is this?) (verify) |
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| Ormeloxifene | |
|---|---|
| Background | |
| Birth control type | Anti-estrogen |
| First use | 1991 |
| Failure rates (first year) | |
| Perfect use | 2% |
| Typical use | 9% |
| Usage | |
| Duration effect | One week |
| Reversibility | Immediate |
| User reminders | Taken twice weekly for first 13 weeks |
| Clinic review | Annually |
| Advantages and disadvantages | |
| STD protection | No |
| Periods | May disrupt |
| Weight | No proven effect |
| Medical notes | |
| Only approved as a contraceptive in India | |
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 non-hormonal, non-steroidal oral contraceptive which is taken once per week. In India, ormeloxifene has been available as birth control since the early 1990s, and it is currently marketed there under the trade name Saheli.[2] Ormeloxifene has also been licensed under the trade names Novex-DS, Centron and Sevista.
Contents |
Ormeloxifene is primarily used as a contraceptive but may also be effective for dysfunctional uterine bleeding and advanced breast cancer.[3]
Ormeloxifene may be used as a weekly oral contraceptive.[3] Hormonal birth control pills should be taken at approximately the same time each day. In the case of progestogen only pills other than Cerazette that do not consistently inhibit ovulation, a delay of as little as three hours can increase the risk of pregnancy because of the limited duration of their effect on the cervical mucus. Ormeloxifene's weekly schedule is an advantage for women who prefer an oral contraceptive, but find it difficult or impractical to adhere to a daily schedule.
For the first twelve weeks of use, it is advised to take the ormeloxifene pill twice per week.[3] From the thirteenth week on, it is taken once per week.[3][4] The consensus is that backup protection in the first month is a cautious but sensible choice. A standard dose is 30mg weekly, but 60mg loading doses can reduce pregnancy rates by 38%.[5]
It has a failure rate of about 1-2% with ideal use which is slight less effective than found for combined oral contraceptive pills.[6]
Ormeloxifene has also been proposed as a treatment for menorrhagia.[7]
Use in treatment of mastalgia and fibroadenoma has also been described.[8]
There are concerns that ormeloxifene may cause urinary incontinence or uterine prolapse.[9]
Ormeloxifene is a SERM, or selective estrogen receptor modulator. In some parts of the body, its action is estrogenic (e.g, bones), in other parts of the body, its action is anti-estrogenic (e.g., uterus, breasts.[10][11]) 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,[6] 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.[6] Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.[6]
Ormeloxifene is only legally available in India as of 2009.[12]
Ormeloxifene has been tested and licensed as a form of birth control, as well as a treatment for dysfunctional uterine bleeding. It was first 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 name Saheli. Torrent Pharmaceuticals has resumed manufacture of ormeloxifene under the trade name Sevista, as a treatment for dysfunctional uterine bleeding.
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