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Raloxifene Doses

Raloxifene Doses

Raloxifene Doses

 

Medical raloxifene dosage

Evista (raloxifene) is the first FDA-approved medication for the treatment and prevention of osteoporosis by acting as an estrogen in bone tissue to reduce bone resorption and promote osteoclastogenesis (bone formation).

The use of raloxifene for this purpose is primarily in postmenopausal women, when osteoporotic conditions are most prevalent.

The use of raloxifene for this purpose is also associated with the treatment of estrogen-responsive breast cancer in postmenopausal women, where the estrogen antagonistic action of raloxifene prevents the cancer-promoting effects of estrogen in breast tissue.


The standard medical dose of raloxifene for the treatment of osteoporosis and female breast cancer is one 60 mg tablet per day.

A single 60 mg dose of raloxifene can be administered with or without food.


Raloxifene dosage during anabolic steroid use

Notably, raloxifene cannot be categorized into three tiers (beginner, intermediate, advanced) as is commonly described and listed in general profiles for other compounds and drugs. This is due to the fact that raloxifene is not specifically used for performance enhancement purposes, but rather is an ancillary drug used to prevent or mitigate various estrogen-related side effects when aromatizing anabolic steroids are used.


In many cases, raloxifene may be used to increase endogenous testosterone secretion in men, and the compound may be used as an ancillary drug during the post cycle therapy (PCT) phase at the end of an anabolic steroid cycle, but its use alone for this purpose is uncommon and is unlikely to produce any noticeable performance enhancing effects.


For the prevention/reduction of gynecomastia during a cycle:

Raloxifene is commonly used to prevent the development of gynecomastia during anabolic steroid cycles using aromatizing anabolic steroids, or as a blocking medication shortly after the onset of gynecomastia.

For both conditions, the raloxifene dosage is the same, ranging from 30 to 60 mg daily during an anabolic steroid cycle, although 30 mg per day is the most common standard.


It is very important to make it clear to the reader that the use of raloxifene can negatively impact athletic performance, muscle and strength gains during an anabolic steroid cycle.

Like Nolvadex, raloxifene has been proven to decrease serum levels of IGF-1 (insulin-like growth factor 1), which is known to be a very important mediator of muscle growth responsible for increased nitrogen retention, protein synthesis, and new muscle cell growth (proliferation) [5].

Another study showed a statistically significant decrease in IGF-1 levels when measured before and after administration in patients taking raloxifene [6].

 

The bottom line is that SERMs like raloxifene and Nolvadex have a detrimental effect on muscle growth by reducing plasma levels of an important hormone (i.e. IGF-1) that is necessary for muscle growth.

Therefore, it is recommended that raloxifene be administered only for as long as necessary to mitigate estrogen-related side effects during aromatization for any reason (PCT or gynecomastia control/reduction).

While short-term use of raloxifene is unlikely to have a significant effect, long-term use may negatively impact muscle growth and performance.

One study examined long-term use of raloxifene and found that after 24 months of raloxifene administration, subjects' IGF-1 levels were measured to be significantly lower than the control group [7].

Another study examined the effects of raloxifene and tamoxifen (Nolvadex) in men and found that raloxifene did not significantly reduce IGF-1 compared to Nolvadex [8].

In one study of patients with acromegaly, 120 mg of raloxifene per day (split into two 60 mg doses per day) resulted in a 16% reduction in IGF-1 levels [9].

Since most studies using raloxifene have demonstrated statistically significant reductions in IGF-1 levels, while few have not, prospective users of anabolic steroids would be wise to consider these effects of raloxifene.

 

Female Raloxifene Dosage

Because raloxifene is primarily used in men who want to alleviate and/or prevent the development of gynecomastia and stimulate endogenous testosterone production, there is little to no need for gynecomastia users.

Women do not have a specific need for these features, and raloxifene in women should only be used if it is deemed medically indicated.

Use of raloxifene in women without medical necessity may lead to additional physiologic complications due to the estrogen agonist/antagonist nature of raloxifene as it relates to female endocrine physiology.


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

The effects of taking raloxifene in relation to endogenous testosterone production in men are fairly well documented.

This occurs through raloxifene's estrogen antagonistic effects on the hypothalamus and pituitary gland, resulting in a significant release of FSH and LH (two hormones that signal the testes to begin or increase production and secretion of testosterone).

This is not surprising, as most SERMs have this effect on men from the start.

For this reason, raloxifene and related SERMs such as Nolvadex and Clomid are known to be very essential components of a properly structured PCT program aimed at hormonal recovery after an anabolic steroid cycle has ended.


However, it is important to note that one of the aforementioned studies (Birzniece et al. 2010) found raloxifene to be significantly inferior to Nolvadex in stimulating testosterone production in men when compared to Nolvadex.

Other studies have also found raloxifene to be at a distinct disadvantage compared to Nolvadex (and even toremifene) in stimulating endogenous testosterone production in men [10].

Therefore, when choosing between raloxifene and Nolvadex for testosterone stimulation, it should be clear that Nolvadex is the preferred agent.

Nolvadex has proven time and time again historically and even today to be a superior (and probably much cheaper) choice compared to other SERMs, not only for the purpose of stimulating endogenous testosterone secretion, but also for combating gynecomastia.

Ideally, you should take 30 to 60 mg of raloxifene per day to stimulate endogenous natural testosterone production, although a dose of 60 mg per day is more common for this purpose.

 

The right dose of raloxifene and when to take it

The dosing restrictions (or lack thereof) for raloxifene are very flexible, and raloxifene doses can be administered before, during, or after meals.

It can also be taken in the morning or evening, depending on your preference.

You can also take your full dose of raloxifene all at once instead of spreading it out over the day.

Splitting or breaking up your dose is not necessary because raloxifene has a long half-life of 27.7 hours.


Expectations and results of taking raloxifene

Raloxifene is an effective solution for preventing and relieving problematic estrogen side effects, especially gynecomastia.

It has an advantage over other SERMs such as Nolvadex in that it maintains or even increases bone density and strength through its estrogenic action in bone tissue, whereas Nolvadex exerts the opposite activity in bone.

Furthermore, since raloxifene is quite effective in stimulating endogenous natural testosterone production in men, it can be concluded that it can be used very effectively to restore endogenous testosterone production after cycle therapy.


Medical references

[1] Lawrence SE1, Fout KA, Betamutu J, Lawson ML. 2004. Beneficial effects of raloxifene and tamoxifen in the treatment of adolescent gynecomastia. J Clin Endocrinol. 2004 Jul;145(1):71-6.

[2] Malozowski S. 2005. Treatment of adolescents with gynecomastia. 2005 Apr;146(4):576; Author response 576-7.

[3] Nordt CA, DiVasta AD. 2008. Gynecomastia in adolescents. MOP. 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, Leach JP, Prokopczyk B, Demers LM, Hamilton C, Hartman TJ, Liao J, El-Bayoumi K, Mani A. 2012. Administration of omega-3 fatty acids and raloxifene to women at high risk for breast cancer: interim feasibility and biomarker analysis of a clinical trial. Eur J Cancer Res. 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 breast density in postmenopausal women. Menopause. 2006 Sep-Oct;13(5):787-92.

[8] Birzniece V, Sata A, Sutanto S, Ho KK. 2010. Neuroendocrine modulation of the growth hormone and androgen axis 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, Simmons KV, Barkan AL. Eur J Endocrinol. 2004. Raloxifene reduces 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. 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.

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