Ormeloxifene

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

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

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

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

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

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

• Selective estrogen receptor modulator
• Contraception
• Estrogen receptor
• Endometrium