|
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 and Dosing of Raloxifene
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 and Side Effects while using Raloxifene
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.
Books and Courses
|
Great Websites
|
Excellent Stores
|
Recipe Cook Books
|
|
|
