Evista — raloxifene hydrochloride

Raloxifene hydrochloride is a second-generation Selective Estrogen Receptor Modulator (SERM) of the benzothiophene family. This drug is similar in effect to tamoxifen, exhibiting estrogen receptor antagonist (blocking) properties in some tissues while acting as an estrogen receptor agonist (activator) in others. The main point of variation between these two agents is their tissue selectivity. While raloxifene hydrochloride is a strong anti-estrogen in breast and uterine tissues, it appears to be estrogenic in bone. This allows it to protect bone density, mimicking the beneficial effects of endogenous estradiol. This is quite different from tamoxifen, which is anti-estrogenic in both breast and bone. In a role that was novel for an anti-estrogen, raloxifene hydrochloride was approved by the FDA for the prevention and treatment of osteoporosis in post-menopausal women. It is also being investigated for several other potential uses, including the treatment and prevention of cardiovascular disease, breast cancer, gynecomastia, prostate cancer, acromegaly, and uterine cancer.

As an anti-estrogen, athletes and bodybuilders may use this compound to combat the estrogenic side effects caused by aromatizable or estrogenic steroids. The principle among these side effects is gynecomastia, a purpose for which raloxifene hydrochloride seems better suited than tamoxifen. This was demonstrated in a July 2004 study in the Journal of Pediatrics, which looked at how these two agents compared in the treatment of persistent pubertal gynecomastia. The investigation involved a group of 38 patients, averaging 15 years of age and suffering from gynecomastia for a little over 2 years. Treatment for 3 to 9 months with either agent had a high success rate for seeing “some improvement” (91% for raloxifene and 86% for Nolvadex). However, a significant reduction of gynecomastia was seen in more than twice as many patients with raloxifene hydrochloride (86% compared to 41%). Given its relative potency, raloxifene hydrochloride may offer an alternative to surgery for some cases of gynecomastia.

Typical of an anti-estrogen, raloxifene hydrochloride should also offer some benefit as a testosterone-stimulating compound. We see this effect demonstrated in studies on a group of older men (aged 60-70 years), where daily doses of 120 mg were able to increase serum and bioavailable (unbound) testosterone by 20%. Though these figures are not dramatic, they do demonstrate an anti-estrogenic effect instead of an estrogenic (negative) one when it comes to testosterone production. This drug may, therefore, be of some value when utilized as an adjunct to HCG injections during a post-cycle testosterone recovery program. This same study above also showed raloxifene hydrochloride to have at least a partial estrogenic effect on serum lipids, exhibiting a trend toward decreases in all cholesterol values (total, LDL, and HDL). It is difficult to discern if there are any real benefits to male bodybuilders when it comes to using raloxifene hydrochloride to counteract the negative cardiovascular side effects of steroid use. As discussed in its respective profile, this may be a notable benefit with the use of Nolvadex, a first-generation SERM agent shown to improve HDL (good) cholesterol levels in many patients.

There are some negatives to inhibiting the actions of estrogen that should be addressed. For one, estrogen is a beneficial hormone when it comes to IGF-1 levels. In studies with acromegaly patients that suffer from GH hypersecretion, 60 mg of raloxifene hydrochloride twice daily was able to reliably suppress IGF-1 levels by an average of 16%. Estrogen is also understood to exert positive anabolic effects in regards to increasing androgen receptor concentrations in certain tissues, and enhancing enzymes involved in the utilization of glucose for tissue growth and repair. This is further support for the belief that anti-estrogens should not be used unless there is a defined reason for doing so. When used for simple side-effect prevention (without visible side effects occurring), the drug may inadvertently lessen the total anabolic potency of steroid therapy.

Brand name Evista, Raloxifene hydrochloride, Ketidin, Oseofem, Raxeto, Bonmax, Estroact, Ralista, Optruma

Raloxifene Hydrochloride History

Raloxifene hydrochloride was developed by Eli Lilly & Company, and FDA approved for U.S. sale in 1997. Its first indicated use was as that of an osteoporosis treatment, owing to its ability to increase bone density. In 2007, the FDA expanded the indicated uses for the drug to include reducing the risk of invasive breast cancer in two populations: postmenopausal women with osteoporosis and postmenopausal women at high risk for invasive breast cancer. Today, raloxifene hydrochloride is a fairly popular drug in clinical medicine, and is approved for sale in over 50 countries. The Evista brand from Eli Lilly & Company dominates the global market, although a small number of other brands can be found including Ketidin, Oseofem, and Raxeto (Argentina), Bonmax, Estroact, and Ralista (India), and Optruma (Spain, France, Italy).

How is Raloxifene Hydrochloride Supplied

Raloxifene hydrochloride is most commonly supplied in tablets of 60 mg.

Structural Characteristics of Raloxifene Hydrochloride

Raloxifene hydrochloride is classified a selective estrogen receptor modulator, with both agonist and antagonist properties. It has the chemical designation 6-Hydroxy-2- ( p - hyd roxypheny l ) benzo [ b ] thien - 3 - yl - p - ( 2 - piperidinoethoxy)phenyl ketone hydrochloride.

Raloxifene Hydrochloride Warnings (Stroke)

The FDA mandates that the following warning be present on the prescribing information for Evista (raloxifene hydrochloride): “WARNING: INCREASED RISK OF VENOUS THROMBOEMBOLISM AND DEATH FROM STROKE. Increased risk of deep vein thrombosis and pulmonary embolism have been reported with Evista. Women with active or past history of venous thromboembolism should not take Evista. Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. Consider risk-benefit balance in women at risk for stroke.”

Raloxifene Hydrochloride Side Effects

Common side effects associated with the use of raloxifene hydrochloride include hot flashes/flushing, headache, malaise, weakness, cramping, edema, sweating, depression, weight gain, and gastrointestinal disturbances such as nausea, vomiting, indigestion, and diarrhea. Less common side effects include breast pain, vaginal bleeding, thrombophlebitis (inflammation of vein associated with blood clot), and visual disturbances. In rare cases raloxifene hydrochloride use has been associated with stroke, narrowing of the arteries (transient ischaemic attack), pulmonary embolus, deep-vein thrombosis, low white blood cell or platelet count, upper gastrointestinal hemorrhage, or ulcer. anti-estrogens may harm the developing fetus, and should never be used during pregnancy.

Raloxifene Hydrochloride Administration

Raloxifene hydrochloride is FDA approved for the treatment and prevention of osteoporosis in postmenopausal women, reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis, and reducing the risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. The recommended dose is one 60 mg tablet administered once per day, without regard to meals.

When used (off-label) to mitigate the estrogenic side effects of anabolic/androgenic steroid use, male athletes and bodybuilders often take 30 mg to 60 mg per day.

Raloxifene Hydrochloride Availability

Raloxifene hydrochloride is available in over 50 countries. Aside from a small number of other brands, the Evista product from Eli Lilly & Company is most likely to be encountered. Price is often a concern, as raloxifene hydrochloride is considerably more expensive than some of the anti-estrogens bodybuilders and athletes are already accustomed to such as Nolvadex (20 mg) often sell for approximately $50. This is about 50 cents per dose, or 1/4th the price of raloxifene hydrochloride. Thus far, price, not availability, seem to be preventing the more widespread diversion of raloxifene hydrochloride for black market sale.

References

Wlliam Llewellyn (2011) - Anabolics

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