From the Research
Centochroman, also known as ormeloxifene, is a selective estrogen receptor modulator (SERM) that is not recommended for use in patients with hypercholesterolemia, as it is not indicated for this condition and may have adverse effects on the uterus with long-term use, as reported in a case study 1.
Key Points
- Centochroman is primarily used as a non-hormonal contraceptive and for treatment of dysfunctional uterine bleeding.
- It works by blocking estrogen receptors in the uterus and cervix, preventing implantation of a fertilized egg while not affecting ovulation.
- Common side effects may include delayed menstruation, occasional spotting, or mild nausea.
- It's contraindicated during pregnancy, in women with liver disease, and in those with hormone-dependent cancers.
- For patients with hypercholesterolemia, statins are the first-line treatment, and alternatives such as ezetimibe, PCSK9 inhibitors, and bempedoic acid may be considered for those who cannot tolerate statins, as they have shown an excellent safety profile and efficacy in reducing LDL-C levels 2, 3, 4.
Treatment of Hypercholesterolemia
- Statins are the primary treatment for hypercholesterolemia, with alternatives considered for those who cannot tolerate them.
- Ezetimibe, a cholesterol absorption inhibitor, can be added to statin therapy to further reduce LDL-C levels, and has been shown to be safe and effective in combination with atorvastatin 4.
- PCSK9 inhibitors, such as alirocumab and evolocumab, can also be used to lower LDL-C levels, but may have a higher cost and risk of injection site reactions 2, 3.
Conclusion Not Applicable
Instead, the following is a continuation of the discussion:
Safety and Efficacy
- The safety and efficacy of ezetimibe/simvastatin combination versus atorvastatin alone have been evaluated in older adults with hypercholesterolemia, and the combination was found to provide significantly greater improvements in key lipid parameters and higher attainment of LDL-C targets 5.
- Centochroman, on the other hand, has been reported to have a prominent estrogenic effect on the uterus with long-term use, highlighting the need for medical surveillance and further studies 1.