Raloxifene Doses

 

Raloxifene is one of the newer anti-estrogens on the market for the treatment of Estrogen-related medical indications, of which the two most prominent are osteoporosis and Estrogen responsive breast cancer. As with other similar SERMs such as Nolvadex (Tamoxifen), its use extends past the primary medical indications and is frequently applied by anabolic steroid using bodybuilders as an ancillary drug to combat and/or prevent Estrogen related side effects and issues. Although Raloxifene is not as popular as Nolvadex for this purpose, growing amounts of evidence in the form of research indicates that it is almost or equally effective for this purpose[1] [2] [3]. Although Raloxifene does not have anywhere near as much of a history of research and clinical data compared to more well-established SERMs such as Nolvadex, it is quickly gaining popularity and interest among the bodybuilding and anabolic steroid using community, and many within said community have regarded Raloxifene as a somewhat safer alternative, though these claims are currently unfounded.

Raloxifene doses for the treatment and prevention of Estrogen related side effects as a result of anabolic steroid use are generally higher than more established SERMs such as Nolvadex, necessitating higher Raloxifene dosages for the purpose of combating and controlling estrogenic side effects. The estrogenic side effects that Raloxifene is used to combat in the arena of anabolic steroid use is primarily gynecomastia, with little assistance for other estrogenic side effects. This is due to the fact that, as mentioned in the introduction of this profile, Raloxifene does not serve to reduce total Estrogen levels in the body, but merely serves to block Estrogen’s activity in select tissues. This is a commonality among all SERMs, and is an intrinsic method by which all SERMs operate. This should be kept in mind by anabolic steroid users, as any attempt to combat other estrogenic side effects such as bloating and water retention with Raloxifene doses will be inevitably met with failure. Aromatase inhibitors are best suited for those purposes instead.

Aside from its use in mitigating Estrogen, Raloxifene has demonstrated considerable use as an endogenous Testosterone stimulating compound, as studies have demonstrated an increase of serum Testosterone levels by 20% from 120mg of Raloxifene per day[4]. Although this level and amount of endogenous Testosterone stimulation is not quite as efficient as Nolvadex, it is still considerable enough to warrant its use as a viable ancillary during post cycle therapy (PCT).

Prior to delving into any further details, an important note must be made to the reader:

The use of SERMs or any anti-Estrogens should only be utilized when absolutely required, and should be discontinued as soon as the requirements to use them (such as gynecomastia or insufficient androgen production) have desisted.

Medical Raloxifene Doses

As a medication, Evista (Raloxifene) is approved by the FDA first and foremost in the treatment and prevention of osteoporosis through its Estrogen agonism in bone tissue, thus reducing bone resorption and promoting ossification (bone formation). The administration of Raloxifene for this purpose is primarily for postmenopausal females, in which the condition of osteoporosis is most prominent. The use of Raloxifene for this purpose is also linked with the treatment of Estrogen responsive breast cancer in postmenopausal females, where Raloxifene’s Estrogen antagonism serves to prevent the cancer-promoting effects of Estrogen in breast tissue.

For the purpose of osteoporosis and female breast cancer treatment, the medical standard Raloxifene dosage is that of one 60mg tablet per day. The single 60mg Raloxifene dosage can be administered with or without food.

Raloxifene Doses During Anabolic Steroid Use

Raloxifene in particular cannot be categorized into the three tiers of users (beginner, intermediate, and advanced) as normally outlined and listed in common profiles of the different compounds and drugs. This is due to the fact that Raloxifene is an ancillary drug not particularly used for the purpose of performance enhancement, but instead is utilized to combat or mitigate various Estrogen-related side effects when aromatizable anabolic steroids are utilized.

In many instances, Raloxifene doses might possibly also be utilized to increase the endogenous secretion of Testosterone in men, which allows this compound to be utilized as an ancillary medication during PCT (Post Cycle Therapy) phases after the conclusion of the end of an anabolic steroid cycle, but its use on its own for this purpose is not very common and is unlikely to produce noticeable performance enhancing effects.

For the purpose of gynecomastia prevention/reduction during a cycle: Raloxifene dosages are normally utilized for either the prevention of the development of gynecomastia during an anabolic steroid cycle that includes the use of aromatizable anabolic steroids, or as an interceptive medication shortly after the development of gynecomastia has begun. For both conditions, the Raloxifene doages are the same, in which 30 – 60mg daily is utilized during an anabolic steroid cycle, though the standard is most usually 30mg per day.

It is very important to make clear to the reader that the use of Raloxifene can possibly impact performance, muscle, and strength gains during an anabolic steroid cycle negatively. Like Nolvadex, Raloxifene too has demonstrated to reduce serum levels of IGF-1 (Insulin-like Growth Factor 1) in the body[5], which is known to be a very important mediator of muscle growth that is responsible for increased nitrogen retention, protein synthesis, and new muscle cell growth (hyperplasia). Other studies conducted have found a statistically significant reduction in IGF-1 levels of patients who were administered Raloxifene when pre and post-administration IGF-1 levels were measured[6].

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The conclusion here is that SERMs such as Raloxifene and Nolvadex do exhibit a detrimental effect on muscle growth through the reduction of blood plasma levels of important hormones (namely, IGF-1) required for muscle growth. It is therefore advised that the administration of Raloxifene for whatever reasons (either for PCT or gynecomastia control/reduction) should be only as long as necessary to mitigate any Estrogen-related side effects during the use of aromatizable anabolic steroids. Short-term administration of Raloxifene doses should not mark a dramatic impact, but long term administration would indeed exhibit negative effects on muscle growth and performance. When long-term use of Raloxifene was examined in one study, after 24 months of Raloxifene treatment, test subjects’ IGF-1 levels were measured to be significantly lower than controls[7]. Another study, this time examining the effect of Raloxifene versus Tamoxifen (Nolvadex) on men, demonstrated no significant reduction of IGF-1 as a result of Raloxifene compared to Nolvadex[8]. One study conducted on acromegaly patients, 120mg per day of Raloxifene was administered (in split dosages of 60mg twice per day), which resulted in a reduction of IGF-1 levels by 16%[9]. The vast majority of studies conducted with Raloxifene have demonstrated statistically significant reductions of IGF-1 levels compared to the few studies that do not, and so it would be wise for any prospective anabolic steroid users to take this effect of Raloxifene dosages into account.

Female Raloxifene Doses

Raloxifene is of very little to no use for female anabolic steroid users, as the primary use of a drug such as Raloxifene among anabolic steroid users is for males that wish to mitigate and/or prevent the development of gynecomastia as well as for the stimulation of endogenous Testosterone production. Females have no particular need for either of these functions, and Raloxifene as it pertains to females should only be for medical indications for which it is deemed necessary for. The use of Raloxifene in females outside of any medical necessities can possibly result in further physiological complications due to the nature of Raloxifene’s Estrogen antagonism/agonism concerning female endocrine physiology.

Raloxifene Doses for Increased Endogenous Testosterone Secretion and PCT (Post Cycle Therapy)

The documentation on the effect of Raloxifene dosages as it pertains to the endogenous production of Testosterone in men has been documented fairly well. This occurs via Raloxifene’s Estrogen antagonistic effects on the hypothalamus and pituitary gland, which results in the significant release of FSH and LH (the two hormones responsible for signaling the testes to begin and/or increase the production and secretion of Testosterone). This is not surprising, as the majority of SERMs express this effect in males to begin with. It is for this reason that Raloxifene, as well as its relative SERMs such as Nolvadex and Clomid, are known to be very essential components to a properly constructed PCT program for the purpose of hormonal recovery after an anabolic steroid cycle ended.

It is very important to note, however, that one study mentioned earlier (Birzniece et al. 2010) discovered that the Testosterone stimulating effects of Raloxifene in comparison with Nolvadex, Raloxifene did fall quite significantly short in comparison with Nolvadex in the effect of stimulating Testosterone production in men. Other studies have also demonstrated that Raloxifene is indeed at a clear disadvantage with Nolvadex (and even Toremifene) when it comes to the stimulation of endogenous Testosterone production in men[10]. It should therefore be clearly noted that between the choice of Raloxifene and Nolvadex for the purpose of Testosterone stimulation, Nolvadex should be the preferred agent of the two. Time and time again, Nolvadex has demonstrated itself against other SERMs throughout history and even today as the superior (and perhaps much cheaper) choice not only for the purpose of stimulating endogenous Testosterone secretion, but for combating gynecomastia as well.

For the purpose of stimulating endogenous natural Testosterone production, a Raloxifene dose of 30 – 60mg per day is ideal, though for this purpose a 60mg daily dose is more common.

Proper Administration and Timing of Raloxifene Doses

Raloxifene’s administration restrictions (or a lack thereof) are quite flexible, and Raloxifene dosages can be administered before, during, or after meals. It can also be consumed in the morning or at night time, as per the user’s preference. Raloxifene doses in their entirety can be consumed all at once as opposed to splitting the Raloxifene doses up throughout the day. The partitioning and splitting up of Raloxifene dosages are unnecessary due to its long half-life of 27.7 hours.

Expectations and Results from Raloxifene Doses

Raloxifene is an efficient solution for the prevention and mitigation of problematic estrogenic side effects, especially for gynecomastia in particular. It does hold an advantage over other SERMs such as Nolvadex in that it will maintain or even increase bone density and strength through its Estrogen agonistic activity in bone tissue, whereas Nolvadex on the other hand expresses the opposite activity in bone. Furthermore, Raloxifene dosages are considerably efficient at stimulating endogenous natural Testosterone production in males, leading to the conclusion that it can be utilized quite effectively during post cycle therapy in the restoration of endogenous Testosterone production.

 

Medical References:


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[2] Malozowski S. 2005. Treatment of adolescents with gynecomastia. J Pediatr. 2005 Apr;146(4):576; author reply 576-7.

[3] Nordt CA, DiVasta AD. 2008. Gynecomastia in adolescents. Curr Opin Pediatr. 2008 Aug;20(4):375-82. doi: 10.1097/MOP.0b013e328306a07c.

[4] Effects of raloxifene on gonadotropins, sex hormones, bone turnover and lipids in healthy elderly men. Eur J Endocrinol. 2004 Apr;150(4):539-46

[5] Signori C1, DuBrock C, Richie JP, Prokopczyk B, Demers LM, Hamilton C, Hartman TJ, Liao J, El-Bayoumy K, Manni A. 2012. Administration of omega-3 fatty acids and Raloxifene to women at high risk of breast cancer: interim feasibility and biomarkers analysis from a clinical trial. Eur J Clin Nutr. 2012 Aug;66(8):878-84. doi: 10.1038/ejcn.2012.60. Epub 2012 Jun 6.

[6] da Silva BB, Moita DS, Pires CG, Sousa-Junior EC, dos Santos AR, Lopes-Costa PV. 2007. Evaluation of insulin-like growth factor-I in postmenopausal women with breast cancer treated with raloxifene. Int Semin Surg Oncol. 2007 Jul 23;4:18.

[7] Lasco A1, Gaudio A, Morini E, Morabito N, Nicita-Mauro C, Catalano A, Denuzzo G, Sansotta C, Xourafa A, Macrì I, Frisina N. 2006. Effect of long-term treatment with raloxifene on mammary density in postmenopausal women. Menopause. 2006 Sep-Oct;13(5):787-92.

[8] Birzniece V, Sata A, Sutanto S, Ho KK. 2010. Neuroendocrine regulation of growth hormone and androgen axes by selective estrogen receptor modulators in healthy men. J Clin Endocrinol Metab. 2010 Dec;95(12):5443-8. doi: 10.1210/jc.2010-1477. Epub 2010 Sep 15.

[9] Dimaraki EV, Symons KV, Barkan AL. Eur J Endocrinol. 2004. Raloxifene decreases serum IGF-1 in male patients with active acromegaly. 2004 Apr;150(4):481-7.

[10] Tsourdi E, Kourtis A, Farmakiotis D, Katsikis I, Salmas M, Panidis D. 2009. The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia. Fertil Steril. 2009 Apr;91(4 Suppl):1427-30. doi: 10.1016/j.fertnstert.2008.06.002. Epub 2008 Aug 9.