Ormeloxifene: Difference between revisions

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[[Ormeloxifene]], commercially known as Saheli, Chhaya, Novex-DS, Centron, and Sevista, is a selective estrogen receptor modulator (SERM). This medication interacts with the [[estrogen receptor]], serving a unique role in the world of birth control. Uniquely, it's a nonsteroidal oral contraceptive that is typically taken once per week.
== Ormeloxifene ==


== Pharmacology and Mode of Action ==
[[File:Ormeloxifene_structure.svg|thumb|right|Chemical structure of Ormeloxifene]]


Ormeloxifene functions as a SERM, which implies that it has selective agonistic and antagonistic activity on estrogen receptors in different tissues. Its unique mechanism involves its ability to prevent implantation by keeping the endometrium in a proliferative phase, making it unsuitable for implantation of a fertilized egg. Furthermore, it can inhibit the release of gonadotropins, which also contributes to its contraceptive effects.
'''Ormeloxifene''', also known as '''centchroman''', is a selective estrogen receptor modulator (SERM) used primarily as a contraceptive. It is a non-steroidal compound that exhibits both estrogenic and anti-estrogenic effects depending on the target tissue. Ormeloxifene is notable for its use in [[India]] as a weekly oral contraceptive.


== Use and Efficacy ==
== Mechanism of Action ==
Ormeloxifene acts by modulating the [[estrogen receptor]]s in various tissues. In the [[endometrium]], it exerts an anti-estrogenic effect, preventing the proliferation of the endometrial lining, which is crucial for [[implantation (embryo)|implantation]] of a fertilized egg. In the [[breast]], it has a weak estrogenic effect, which may contribute to its potential use in [[breast cancer]] prevention.


Ormeloxifene is primarily used as a contraceptive but can also be used to manage menorrhagia (excessive menstrual bleeding), and dysmenorrhea (painful periods). Despite being taken only once per week, studies suggest that it's as effective as daily oral contraceptives in preventing pregnancy when used correctly and consistently.
== Clinical Uses ==
Ormeloxifene is primarily used as a contraceptive. It is taken once a week, which is a unique dosing schedule compared to other oral contraceptives. Besides contraception, it is also used in the management of [[dysfunctional uterine bleeding]] and has been studied for its potential benefits in [[osteoporosis]] and [[breast cancer]] prevention.


== Availability ==
== Side Effects ==
Common side effects of Ormeloxifene include [[nausea]], [[headache]], and [[dizziness]]. Some users may experience changes in [[menstrual cycle|menstrual patterns]], such as delayed periods or spotting. Long-term use has not been associated with significant adverse effects on [[bone mineral density]].


This medication has been available in India since the early 1990s and is currently provided free-of-cost to women under the trade name Chhaya (Centchroman). The drug has also been made available under the trade names Novex-DS, Centron, and Sevista.
== Pharmacokinetics ==
Ormeloxifene is well absorbed after oral administration. It has a long half-life, which allows for its weekly dosing schedule. The drug is metabolized in the [[liver]] and excreted primarily in the [[feces]].


== Safety and Side Effects ==
== History and Development ==
Ormeloxifene was developed in India and has been available since the early 1990s. It was initially marketed under the brand name "Saheli" and has been part of the national family planning program in India. Its development was part of an effort to provide a safe, effective, and convenient contraceptive option.


Ormeloxifene is generally well-tolerated. Side effects can include mild weight gain, nausea, leg cramps, and minor menstrual irregularities, but these typically resolve over time. As with all contraceptives, it is not effective against sexually transmitted infections.
== Related Pages ==
* [[Selective estrogen receptor modulator]]
* [[Contraception]]
* [[Estrogen receptor]]
* [[Endometrium]]


== References ==
* [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3113371/ Ormeloxifene – A selective estrogen receptor modulator]
* [https://pubmed.ncbi.nlm.nih.gov/11384874/ Phase III clinical trial with Centchroman]
* [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5393179/ Selective Estrogen Receptor Modulators: An Update on Recent Clinical Findings]{{stub}}
[[Category:Pharmacology]]
[[Category:Birth control methods]]
[[Category:Selective estrogen receptor modulators]]
[[Category:Selective estrogen receptor modulators]]
[[Category:Women's health]]
[[Category:Contraception]]

Latest revision as of 11:09, 15 February 2025

Ormeloxifene[edit]

Chemical structure of Ormeloxifene

Ormeloxifene, also known as centchroman, is a selective estrogen receptor modulator (SERM) used primarily as a contraceptive. It is a non-steroidal compound that exhibits both estrogenic and anti-estrogenic effects depending on the target tissue. Ormeloxifene is notable for its use in India as a weekly oral contraceptive.

Mechanism of Action[edit]

Ormeloxifene acts by modulating the estrogen receptors in various tissues. In the endometrium, it exerts an anti-estrogenic effect, preventing the proliferation of the endometrial lining, which is crucial for implantation of a fertilized egg. In the breast, it has a weak estrogenic effect, which may contribute to its potential use in breast cancer prevention.

Clinical Uses[edit]

Ormeloxifene is primarily used as a contraceptive. It is taken once a week, which is a unique dosing schedule compared to other oral contraceptives. Besides contraception, it is also used in the management of dysfunctional uterine bleeding and has been studied for its potential benefits in osteoporosis and breast cancer prevention.

Side Effects[edit]

Common side effects of Ormeloxifene include nausea, headache, and dizziness. Some users may experience changes in menstrual patterns, such as delayed periods or spotting. Long-term use has not been associated with significant adverse effects on bone mineral density.

Pharmacokinetics[edit]

Ormeloxifene is well absorbed after oral administration. It has a long half-life, which allows for its weekly dosing schedule. The drug is metabolized in the liver and excreted primarily in the feces.

History and Development[edit]

Ormeloxifene was developed in India and has been available since the early 1990s. It was initially marketed under the brand name "Saheli" and has been part of the national family planning program in India. Its development was part of an effort to provide a safe, effective, and convenient contraceptive option.

Related Pages[edit]