The chemical Raloxifene is a research chemical and can be successfully used as a selective estrogen receptor modulator in postmenopausal women against vertebral fractures. But that’s not all. New studies are now also examining its use in the prevention of cardiovascular diseases and breast cancer.
For many countries therapy for osteoporosis is still in its infancy. Therapy is denied even to high-risk patients. Patients who have already had a vertebral fracture or a fracture of the femur often do not even receive calcium or vitamin D, let alone the urgently needed movement therapy or effective pharmacotherapy. There are hardly any scientific reasons for this because there are some active ingredients available, and the effectiveness of which is beyond question. There are excellent study results for the selective estrogen receptor modulator (SERM) raloxifene (Evista) and the bisphosphonates. The data situation for estrogens is classified as moderate. All of these substances belong to the “resorption inhibitors”, and stop the bone breakdown, which is promoted by excessive osteoclast activity.
Choosing the Right Medicine – SERMs Osteoporosis
The choice of the right medication for the respective patient is decisive for the success of the therapy. Women are usually victims of osteoporosis (widow’s hump). This is because estrogens have a low, but significantly increased risk of malignancy. For example, they are not suitable for women with an increased risk of breast cancer. There are many doctors that prescribe one 60 mg Evista tablet daily (taken anytime) of the brand name Evista to treat osteoporosis.
Raloxifene Dosage for Vertebral Body Fractures!
The SERM Raloxifene has an estrogen agonistic effect on the bones and cardiovascular system, an antagonistic effect on the breast and uterus. The reason is similar to the sympathetic nervous system, where alpha and beta receptors exist, and also different estrogen receptors. While the beta receptors predominate in bones and blood vessels, the alpha receptors in the tissues of the breast, uterus, and liver. Raloxifene selectively attacks the beta receptors.
Study and Research: Raloxifene Review
The MORE study, published in late 1999, showed what can be achieved with this principle of action. 7705 women were involved, two-thirds of whom “only” had a pathological bone density (T-Score -2.5SD) and one third already had a vertebral body fracture. In addition to calcium and vitamin D, they received randomly 60 mg or 120 mg raloxifene or placebo for three years. Raloxifene reduced the rate of vertebral fractures by 30 to 50 percent during this period. It was 6.6 percent below 60 mg raloxifene, 5.4 percent below 120 mg raloxifene and 10.1 percent under placebo. Non-vertebral fractures, such as hip fractures, femoral neck fractures or forearm fractures, occurred approximately equally frequently in all study groups.
Positive Study Results with Raloxifene Osteoporosis
Our Raloxifene blogs the amazing fact that this is particularly suitable for younger postmenopausal women with an increased risk of fracture of the spine. Its advantage over hormone replacement therapy: it neither stimulates the mammary gland tissue nor does it lead to the proliferation of the endometrium. However, raloxifene is contraindicated in women who suffer from menopausal symptoms, for example, because hot flashes can be increased.
RUTH: Raloxifene reduces the risk of heart attack
However, osteoporosis will probably not remain the only indication for SERMs. With the discovery of the various estrogen receptors, the possible uses have expanded considerably. At least in the animal model, raloxifene dilates the vessels – at least in part through an increased release of vascular-dilating NO. The lipid profile also appears to improve with raloxifene: For example the total cholesterol, LDL cholesterol, and lipoprotein decreased by six to twelve percent, while HDL cholesterol increases by 15 to 17 percent.
Homocysteine, also an independent risk factor for cardiovascular diseases, is also kept within the normal range. The RUTH (Raloxifene Use for the HEART) study in 10,000 postmenopausal women with an increased risk of CHD is currently investigating whether these effects are also clinically evident.
STAR: Raloxifene to Prevent Breast Cancer?
Raloxifene, because of its estrogen-antagonistic properties, similar to tamoxifen, could also be suitable for the therapy and prevention of breast cancer. In the MORE study, raloxifene reduced the risk of breast cancer, in particular, the risk of estrogen receptor-positive tumors, by a remarkable 76 percent within 40 months. Long-term effects are now recorded in the continuing CORE (Continuing Outcomes Relevant to Evista) study.
A study recently launched by the National Cancer Institute, the STAR (Study of Tamoxifen and Raloxifene) study, compares the preventive effects of tamoxifen and raloxifene in 22,000 postmenopausal women with an increased risk of breast cancer. Particular attention is paid to the effect on the endometrial tissue. While tamoxifen can promote proliferation and thus bleeding and carcinogenesis, raloxifene is clearly antagonistic in this organ.
Raloxifene Side Effects
As with all medicine there, the pros and cons involved with new drugs, and not everyone can take them. They are not recommended during pregnancy and breastfeed. Also, Raloxifene contraindication can occur if combined with other medications such as birth control pills, blood thinners, cholestyramine, diazepam, diazoxide and HRT (hormone replacement therapy). Possible side effects that can occur with an Evista/Raloxifene dosage are:
- Dizziness, Excessive sweating, Headaches, Hot flashes, Joint pain, Leg pain, Nausea, Runny Nose, Spinning sense, stomach pain, and Sickness.
Rare side effects include; blood clots in the eyes, lungs, and legs and strokes. It is important to seek medical advice if any of the following side effects occur:
- Breathing problems, chest pain, confusion, leg swelling, severe headaches, vision changes, and weakness sensations in the body.
Raloxifene Blogs Summary
As we mentioned early on in this blog the chemical Raloxifene has shown huge positivity as an ingredient for the future in treating not only osteoporosis but other serious diseases.