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Raloxifene


Pharmaceutical Name: Raloxifene Hydrochloride
Drug Classification: Selective Estrogen Receptor Modulator
Active Life: 5-7 days

Raloxifene hydrochloride is another selective estrogen receptor modulator similar to but differing in some significant ways from tamoxifen citrate, toremifene citrate, and clomiphene citrate. However unlike tamoxifen citrate which is primarily used in the treatment of breast cancer and clomiphine citrate which is prescribed most often as a fertility drug for females, raloxifene hydrochloride was approved for medical use in the treatment of osteoporosis (1). This is due to the fact that raloxifene hydrochloride has much stronger agonistic properties in bone then either tamoxifen citrate, clomiphine citrate or toremifene citrate. While these other selective estrogen receptor modulators all have varying degrees of agonistic action in bones, raloxifene hydrochloride is far superior in this regard. For strength athletes and bodybuilders however the reasons for using raloxifene hydrochloride are indeed nearly identical to those of the other selective estrogen receptor modulators. Prevention of gynecomastia, increasing the natural testosterone production of the user post-cycle, improvement of lipid/cholesterol levels and others are all potential benefits that anabolic steroid users can reap from administering raloxifene hydrochloride, although the ability of the drug to deliver these effects vary in effectiveness when compared to those of other similar drugs.

Tamoxifen citrate has long been the choice of steroid users when combating gynocomastia. Plenty of research indicates that tamoxifen citrate will compete with estrogen for the estrogen receptors in certain tissues, including the breast, and if it can bind to the receptor estrogen will not have an opportunity to interact with it and therefore gynecomastia should not be able to develop (2). It has also been demonstrated that this effect is produced with the use of raloxifene hydrochloride. However there is some evidence that raloxifene hydrochloride may actually be more effective for the treatment of gynecomastia. In one study it was shown that while both tamoxifen citrate and raloxifene hydrochloride had relatively similar rates of success in reducing the size of gynecomastia in pubertal males, raloxifene hydrochloride had a higher rate of effectively reducing the size to noticeably significant smaller levels (3). Obviously when one is faced with the option of choosing which compound to use when a treatment for gynecomastia is needed this should indicate that raloxifene hydrochloride may indeed be the more effective choice.

A second benefit of raloxifene hydrochloride is that it seemingly has the ability to lower low-density lipoprotein and total cholesterol levels in users (4, 5). The drug is able to accomplish this by way of its agonist actions on lipid metabolism. However it appears that these effects may be marginal at best and may not be all that significant in terms of the health of the user. However in a minority of studies there is some evidence that improvements in cholesterol levels can be quite significant and should improve the health of the user. It appears that more research needs to be conducted in this area before any proclamations can be made about the effect of this drug on the cardiovascular health of users. Combine this with the fact that anabolic steroid use will have a significant impact on cholesterol levels and any attempt at reaching a conclusion about this issue for bodybuilders and strength athletes is even further away. For now the use of this drug for cholesterol lowering effects is questionable.

A far less contentious issue is the ability of raloxifene hydrochloride to raise the levels of follicle stimulating hormone, luteinizing hormone and testosterone levels in male users. Like tamoxifen citrate, clomiphine citrate and toremifene citrate raloxifene hydrochloride has been demonstrated to help raise the levels of these hormones when they are suppressed (5, 6). The research regarding the ability of raloxifene hydrochloride to raise testosterone levels in males is limited when compared to both clomiphine citrate and tamoxifen citrate so it is difficult to compare their effects in this regard; however it appears that raloxifene hydrochloride is at least slightly less potent when compared to these other two selective estrogen receptor modulators. While it is premature to declare that raloxifene hydrochloride inferior to both tamoxifen citrate and clomiphine citrate for use during post-cycle therapy, for now it appears that the two more popular selective estrogen receptor modulators will remain ahead of raloxifene hydrochloride when most steroid users are choosing their post-cycle therapy compounds of choice, at least until further research can be conducted showing exactly how these drugs compare to one another in this regard.


Use/Dosing

Currently raloxifene hydrochloride is most often produced pharmaceutically in tablet form at a strength of sixty milligrams per tablet. Of course these tablets should be able to be split to accommodate dosing that fall outside of multiples of sixty. However if the drug becomes more popular among both medical professionals and steroid users more dosing options may become available in the future.

The dosing required to experience a relatively significant rise in follicle stimulating hormone, luteinizing hormone and testosterone levels in male users appears to fall in the range of between one hundred and twenty to two hundred and forty milligrams per day (5, 6). Due to the active life of the drug these doses can be taken once per day or even once every other day. However to maintain a stable concentration of the drug in the system of the user every other day dosing should be as infrequently as one should take the compound. In terms of the duration needed to see significant results in the improvement of the testosterone levels of a user it appears that as little as 14 days can be quite beneficial. However most anabolic steroid users will likely want to and will benefit from longer durations anywhere from three to six weeks in some cases when trying to restart their natural testosterone production as quickly as possible.

For prevention of gynecomastia and/or attempting to induce the possible cholesterol lowering benefits of raloxifene hydrochloride users will likely need less of the drug then when trying to raise the natural testosterone level of a user. Doses anywhere from sixty to two hundred milligrams per day should be sufficient for the majority of users (3, 7). The same dosing frequency does apply as with that of raising testosterone levels. The duration required for these effects to be achieved and maintained by the user will of course depend on exactly how long they will be using anabolic steroids and/or suffering from estrogenic side effects that can be treated using the drug.


Risks/Side Effects

The negative side effects associated with the use of raloxifene hydrochloride are significantly less serious and burdensome for the majority of users even when compared to the usually well tolerated other selective estrogen receptor modulators. For example there is some evidence via animal studies that tamoxifen citrate can be carcinogenic at some doses. Raloxifene hydrochloride has shown no such characteristic (8, 9). As well there are less ocular difficulties reported with the use of raloxifene hydrochloride then with tamoxifen citrate (1). Little to no signs of depression were experienced by male users in most studies as well (Dimaraki, Draper). This is in contrast to the often reported depression and malaise that male users suffer with the use of clomiphine citrate. Overall raloxifene hydrochloride appears to be extremely well tolerated by the vast majority of users.

Raloxifene hydrochloride is not however free from all negative side effects. Like tamoxifen citrate it appears that the drug significantly lowers insulin-like growth factor-1 levels in users when taken for substantial periods of time (6). This effect is so significant in fact that raloxifene hydrochloride has been studied as a possible treatment for men suffering from acromegaly (10). While this effect of the drug sounds quite significant for most users it should not be at all detrimental. The suppression of insulin-like growth factor-1 levels should only cause alarm for those that would be administering the drug for significant periods of time. For most steroid users their use of raloxifene hydrochloride will likely be for relatively short durations.

A unique characteristic of raloxifene hydrochloride appears to be its effect on the exogenous supplementation of the thyroid drug levothyroxine. When dosing raloxifene hydrochloride at the same time as levothyroxine, raloxifene hydrochloride has the ability to reduce the effectiveness of the thyroid medication to almost nothing it appears (11, 12). Once the dosing of the drugs are separated by a few hours however both medications appeared to be serving their intended purpose at their full potency. The mechanism by which this occurs is unknown and what implications it has potentially for other thyroid medications and selective estrogen receptor modulators needs to be studied further. However for those that are indeed administering thyroid supplements/medications at the same time that they are using a drug like raloxifene hydrochloride, this knowledge about this effect may serve to prevent any possible complications related to this potential and unique drug interaction.



References

1. Vogel VG, Costantino JP, Wickerham DL, Cronin WM, Cecchini RS, Atkins JN, Bevers TB, Fehrenbacher L, Pajon ER Jr, Wade JL 3rd, Robidoux A, Margolese RG, James J, Lippman SM, Runowicz CD, Ganz PA, Reis SE, McCaskill-Stevens W, Ford LG, Jordan VC, Wolmark N; National Surgical Adjuvant Breast and Bowel Project (NSABP). Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA. 2006 Jun 21;295(23):2727-41.

2. Schopman W, Slager E, Hackeng WH, Mulder H. Stimulation of calcitonin secretory capacity by increased serum levels of testosterone in men treated with tamoxifen. Int J Androl. 1987 Dec;10(6):747-51

3. Lawrence SE, Faught KA, Vethamuthu J, Lawson ML. Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia. J Pediatr. 2004 Jul;145(1):71-6.

4. Dayspring T, Qu Y, Keech C. Effects of raloxifene on lipid and lipoprotein levels in postmenopausal osteoporotic women with and without hypertriglyceridemia. Metabolism. 2006 Jul;55(7):972-9.

5. Duschek EJ, Gooren LJ, Netelenbos C. Effects of raloxifene on gonadotrophins, sex hormones, bone turnover and lipids in healthy elderly men. Eur J Endocrinol. 2004 Apr;150(4):539-46.

6. Duschek EJ, Gooren LJ, Netelenbos C. Comparison of effects of the rise in serum testosterone by raloxifene and oral testosterone on serum insulin-like growth factor-1 and insulin-like growth factor binding protein-3. Maturitas. 2005 Jul 16;51(3):286-93.

7.Draper MW, et al. "Antiestrogenic properties of raloxifene." Pharmacology 1995 Apr;50(4):209-17.

8. Hirsimaki P, Aaltonen A, Mantyla E. Toxicity of antiestrogens. Breast J. 2002 Mar-Apr;8(2):92-6.

9. Martino S, Disch D, Dowsett SA, Keech CA, Mershon JL. Safety assessment of raloxifene over eight years in a clinical trial setting. Curr Med Res Opin. 2005 Sep;21(9):1441-52.

10. Dimaraki EV, Symons KV, Barkan AL. Raloxifene decreases serum IGF-I in male patients with active acromegaly. Eur J Endocrinol. 2004 Apr;150(4):481-7.

11. Garwood CL, Van Schepen KA, McDonough RP, Sullivan AL. Increased thyroid-stimulating hormone levels associated with concomitant administration of levothyroxine and raloxifene. Pharmacotherapy. 2006 Jun;26(6):881-5.

12. Siraj ES, Gupta MK, Reddy SS. Raloxifene causing malabsorption of levothyroxine. Arch Intern Med. 2003 Jun 9;163(11):1367-70.






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