Centchroman
Encyclopedia
Ormeloxifene is one of the selective estrogen receptor modulator
s, 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. Ormeloxifene has also been licensed under the trade names Novex-DS, Centron and Sevista.
and advanced breast cancer
.
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.
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%.
It has a failure rate of about 1-2% with ideal use which is slight less effective than found for combined oral contraceptive pills.
.
Use in treatment of mastalgia
and fibroadenoma
has also been described.
or uterine prolapse
.
, 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.) 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 tube
s more quickly than is normal. Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.
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.
Selective estrogen receptor modulator
Selective Estrogen Receptor Modulators are a class of compounds that act on the estrogen receptor. A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively...
s, 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
Birth control
Birth control is an umbrella term for several techniques and methods used to prevent fertilization or to interrupt pregnancy at various stages. Birth control techniques and methods include contraception , contragestion and abortion...
since the early 1990s, and it is currently marketed there under the trade name Saheli. 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 bleedingDysfunctional uterine bleeding
Dysfunctional Uterine Bleeding is abnormal genital tract bleeding based in the uterus and found in the absence of demonstrable structural or organic pathology.usually due to hormonal disturbances....
and advanced breast cancer
Breast cancer
Breast cancer is cancer originating from breast tissue, most commonly from the inner lining of milk ducts or the lobules that supply the ducts with milk. Cancers originating from ducts are known as ductal carcinomas; those originating from lobules are known as lobular carcinomas...
.
As birth control
Ormeloxifene may be used as a weekly oral contraceptive. 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. From the thirteenth week on, it is taken once per week.
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%.
It has a failure rate of about 1-2% with ideal use which is slight less effective than found for combined oral contraceptive pills.
Other
Ormeloxifene has also been proposed as a treatment for menorrhagiaMenorrhagia
Menorrhagia is an abnormally heavy and prolonged menstrual period at regular intervals. Causes may be due to abnormal blood clotting, disruption of normal hormonal regulation of periods or disorders of the endometrial lining of the uterus...
.
Use in treatment of mastalgia
Mastalgia
Mastodynia, mastalgia or mammalgia are names for a medical symptom that means breast pain .Pain can range from minor discomfort to severely incapacitating pain...
and fibroadenoma
Fibroadenoma
Fibroadenomas of the breast, are lumps composed of fibrous and glandular tissue. Because breast cancer can also appear as a lump, doctors may recommend a tissue sample to rule out cancer in older patients...
has also been described.
Adverse effects
There are concerns that ormeloxifene may cause urinary incontinenceUrinary incontinence
Urinary incontinence is any involuntary leakage of urine. It is a common and distressing problem, which may have a profound impact on quality of life. Urinary incontinence almost always results from an underlying treatable medical condition but is under-reported to medical practitioners...
or uterine prolapse
Uterine prolapse
Uterine prolapse is a form of female genital prolapse Uterine prolapse is a form of female genital prolapse Uterine prolapse is a form of female genital prolapse (also called pelvic organ prolapse or prolapse of the uterus (womb).Treatment is surgical, and the options include hysterectomy or a...
.
Method of action
Ormeloxifene is a SERMSelective estrogen receptor modulator
Selective Estrogen Receptor Modulators are a class of compounds that act on the estrogen receptor. A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively...
, or selective estrogen receptor
Estrogen receptor
Estrogen receptor refers to a group of receptors that are activated by the hormone 17β-estradiol . Two types of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and the estrogen G protein-coupled receptor GPR30 , which is a G protein-coupled...
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
Uterus
The uterus or womb is a major female hormone-responsive reproductive sex organ of most mammals including humans. One end, the cervix, opens into the vagina, while the other is connected to one or both fallopian tubes, depending on the species...
, breasts.) It causes an asynchrony in the menstrual cycle
Menstrual cycle
The menstrual cycle is the scientific term for the physiological changes that can occur in fertile women for the purpose of sexual reproduction. This article focuses on the human menstrual cycle....
between ovulation
Ovulation
Ovulation is the process in a female's menstrual cycle by which a mature ovarian follicle ruptures and discharges an ovum . Ovulation also occurs in the estrous cycle of other female mammals, which differs in many fundamental ways from the menstrual cycle...
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 tube
Fallopian tube
The Fallopian tubes, also known as oviducts, uterine tubes, and salpinges are two very fine tubes lined with ciliated epithelia, leading from the ovaries of female mammals into the uterus, via the utero-tubal junction...
s more quickly than is normal. Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.
Marketing
Ormeloxifene is only legally available in India as of 2009.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
Torrent Pharmaceuticals
Torrent Pharmaceuticals Ltd. is the flagship company of the Torrent Group. Based in Ahmedabad, it was promoted by U. N. Mehta initially as Trinity Laboratories Ltd. and was later renamed to its current name Torrent Pharmaceuticals Ltd....
, 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.
External links
- United States National Library of Medicine Centchroman entry in the Medical Subject HeadingsMedical Subject HeadingsMedical Subject Headings is a comprehensive controlled vocabulary for the purpose of indexing journal articles and books in the life sciences; it can also serve as a thesaurus that facilitates searching...
(MeSH) database - Reproductive Health Online, a Johns Hopkins UniversityJohns Hopkins UniversityThe Johns Hopkins University, commonly referred to as Johns Hopkins, JHU, or simply Hopkins, is a private research university based in Baltimore, Maryland, United States...
affiliate providing information on Centchroman - Saheli manufacturer's website - Product details
- Central Drug Research Institute, Lucknow, IndiaIndiaIndia , officially the Republic of India , is a country in South Asia. It is the seventh-largest country by geographical area, the second-most populous country with over 1.2 billion people, and the most populous democracy in the world...
: 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.