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Raloxifene hydrochloride (trade name Evista) is very new anti-estrogenic drug on the prescription market, and it is a member of the category of drugs known as selective estrogen receptor modulators (SERMs), which is actually a sub-category of an even broader category of drugs known as anti-estrogens. The sub-category under anti-estrogens are aromatase inhibitors (AIs), which include the three most common: Aromasin (Exemestane), Arimidex (Anastrozole), and Letrozole (Femara), though there are plenty of other aromatase inhibitors in existence as well. SERMs and AIs are what make up the broad class of anti-estrogens. SERMs and AIs differ quite greatly in terms of their mechanisms of action and how they operate physiologically. As with any profile covering SERMs and AIs, the difference between these two classes of anti-estrogenic drugs must be boldly stated and clarified before moving on to discussing Raloxifene in particular.
It is a common occurrence among the anabolic steroid using and bodybuilding community to confuse the two and assign the wrong (or opposite) properties to either of these anti-estrogens. SERMs act upon the Estrogen receptors in different tissues in the body, and in particular they serve to block the activity of Estrogen at the receptor site in breast tissue (properly referred to as Estrogen antagonism). Effectively, they occupy the Estrogen receptor (whilst simultaneously ‘booting’ out any Estrogen that is occupying those receptors), and they deny any access by Estrogen to those receptor sites. Additionally, SERMs can and do act as Estrogen agonists in other tissues in the body (namely, in the liver). As an Estrogen agonist, the drug will serve to do the opposite of the previously described action, and instead it will bind to the receptor and initiate estrogenic effects in those tissues. As a result, SERMs serve to only antagonize (or agonize) the effects of Estrogen in certain tissues – they will not reduce total circulating blood plasma levels of Estrogen in the body, and therefore some estrogenic side effects cannot be remedied by SERMs, such as water retention and bloating.
On the other hand, aromatase inhibitors disable the root cause of Estrogen production in the body by binding to the enzyme responsible for converting (aromatizing) androgens into Estrogen: the aromatase enzyme. Once inhibited and disabled, the aromatase enzyme cannot act to produce any Estrogen in the body, and thus total circulating blood plasma levels of Estrogen in the body are effectively reduced. Aromatase inhibitors can and do eliminate the estrogenic side effects that SERMs cannot possibly remedy, such as bloating and water retention.
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 Tamoxifen (Nolvadex) in that it will maintain or even increase bone density and strength through its Estrogen agonistic activity in bone tissue, whereas Tamoxifen (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.
Raloxifene Side Effects
Raloxifene is a SERM, just like other popular cousin compounds such as Tamoxifen (Nolvadex) and Clomiphene Citrate (Clomid). Like nearly all other SERMs, Raloxifene tends to be well tolerated by most male users. There are very rare and infrequent occurrences of Raloxifene side effects that are reported (both anecdotally as well as clinically). The negative Raloxifene side effects and adverse reactions that result from Raloxifene are most often in females, whom the drug was (ironically) designated for first and foremost.
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 Tamoxifen (Nolvadex), 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. 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 Tamoxifen (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.
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 Tamoxifen (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. Although this level and amount of endogenous Testosterone stimulation is not quite as efficient as Tamoxifen (Nolvadex), it is still considerable enough to warrant its use as a viable ancillary during post cycle therapy (PCT).
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.
SERMs such as Raloxifene and Tamoxifen (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.
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 Tamoxifen (Nolvadex) and Clomiphene Citrate (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.
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.
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