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Nolvadex® (tamoxifen citrate)

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Old 11-12-2003, 06:57 PM
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Nolvadex® (tamoxifen citrate)

Article source from Steroidology.com


Nolvadex® (tamoxifen citrate)


Quick overview:


Active Life: 5-7 days
Drug Class: Selective Estrogen Receptor Modulator (Oral)
Average Dose: 10-30 mg/day
Acne: Yes
Water Retention: No
High Blood Pressure: Rare
Liver Toxic: Yes

Nolvadex®, is the trade name for the drug tamoxifen citrate, it is a non-steroidal agent that demonstrates potent anti-estrogenic properties. The drug is technically an estrogen agonist/antagonist, which competitively binds to estrogen receptors in various target tissues. With the tamoxifen molecule bound to this receptor, estrogen is blocked from exerting any action, and an anti-estrogenic effect is achieved. Since many forms of breast cancer are responsive to estrogen, the ability of tamoxifen citrate to block its action in such cells has proven to be a very effective treatment. It is also utilized successfully as a preventative measure, taken by people with an extremely high familial tendency for breast cancer. While Nolvadex is effective against estrogen, it is not our strongest available remedy. We now have the drugs Arimidex, Femara, and Aromasin available to us, which notably prevents estrogen from being manufactured in the first place. Altering the effect of estrogen in the female body can cause a level of discomfort, so anti-estrogens are most bearable when used after the point of menopause. Since Nolvadex is milder in comparison, it is more widely applicable and usually the first treatment option.

As discussed earlier, an enzyme in the male body (aromatase) is capable of altering testosterone to form estradiol. The structure of estrogen is actually quite similar to testosterone, so its presence in the male body is not all that remarkable. Since this same enzyme can also aromatize many anabolic/androgenic steroids, the buildup of estrogens can be an important concern during intake. High levels can cause a number of unwanted side effects, a primary worry being gynecomastia or the development of female breast tissue in men. This can be first noticed by the appearance of swelling or a small lump under the nipple. If left to progress it can turn into a very unsightly development of tissue, often irreversible without surgery. Estrogen can also lead to an increase in the level of water retained in the body. The result here can be a notable loss of definition, the muscles beginning to look smooth and bloated due to the retention of subcutaneous fluid. Fat storage may also be increased as estrogen levels rise. This hormone is in fact the primary reason women have a higher body fat percentage, and different fat distribution (hips/thighs) than men. Individuals sensitive to the effects of estrogen will usually be sure to have an anti-estrogen on hand when taking problematic steroids, so as to minimize the impact of related side effects.

This drug also shows the ability to increase production of FSH (follicle stimulating hormone) and LH (luteinizing hormone) in the male body. This is accomplished by blocking negative feedback inhibition caused by estrogen at the hypothalamus and pituitary, which fosters the release of the mentioned pituitary hormones. This of course is also the function of Clomid and cyclofenil. Since a higher release of LH can stimulate the Leydig's cells in the testes to produce more testosterone, Nolvadex can have a positive impact on one's serum testosterone level. This "testosterone stimulating" effect is an added benefit when preparing to conclude a steroid cycle (post cycle therapy or PCT). Since most anabolic/androgenic steroids will suppress endogenous testosterone production, Nolvadex can help restore a balance in hormone levels. Nolvadex should be preferred over Clomid for this purpose in fact, as side by side it is clearly the stronger agent. It has also been shown to increase LH responsiveness to Gonadotropin Releasing Hormone after time, while Clomid slightly lowers this sensitivity as the drug is used for several weeks..

In some cases the use of only an estrogen antagonists such as Nolvadex or Clomid may be sufficient for testosterone stimulating purposes, particularly when halting the use of a milder or shorter steroid program (which should have a less pronounced impact on the hormonal system). With stronger cycles most option to enhance the stimulating effect of these drugs with HCG, a hormone that mimics the action of LH. HCG use provides an excessive level of stimulation to the testes, which in essence may shock them out of a prolonged state of inactivity. In such a condition the Leydig's cells may not be producing a normal amount of testosterone, even though the normal release of gonadotropins has been achieved. Nolvadex can be tricky at this point. Remember it only blocks the effect of estrogen that is present in the body. If it is removed at a time when estrogen levels are still unusually high, related side effects can quickly become a pronounced problem. Since HCG not only increases the production of testosterone but also enhances the rate of aromatization in the testes, anti-estrogens should not be discontinued until at least a couple of weeks after HCG is discontinued. The result otherwise of course could be many unwanted side effects that were previously under control. When using Nolvadex to ward off the effects of estrogen during the cycle, it should similarly not be removed until the user is confident that hormone levels are well under control. With a drug such as Sustanon, this may mean continuing it for several weeks after the last shot.

A typical daily dosage for men is in the range of 10 to 30mg, the amount would be dependent on the level of effect desired. It is advisable to begin with a low dosage and work up, to avoid taking an unnecessary amount. The time in which Nolvadex is started also relies on individual needs of the user. If an athlete with a known sensitivity to estrogen is starting a strong steroid cycle, Nolvadex should probably be added soon after the cycle had been initiated. If estrogen is probably not going to be a major problem during the cycle (but will likely be after), Nolvadex is administered around the time exogenous steroid levels will drop. It will be continued for some weeks after, until the point when natural testosterone is thought to be at an acceptable level. As mentioned HCG is often used at this point as well (see related profile for more detail). Women have also utilized Nolvadex in an effort to reduce the effect of their own endogenous estrogens. This can lower body fat concentrations, especially in stubborn areas like the hips and thighs. This is of course risky, as manipulating the effect of estrogen can become uncomfortable in women. Side effects like hot flashes, menstrual irregularities and a variety of complications with the reproductive system are all possible.

When looking for a stronger anti-estrogenic effect, Proviron can make a good addition to Nolvadex. Although this compound is technically an androgen, it may have a pronounced effect on the production of estrogen in the body. Its mode of action is therefore very different than that of Nolvadex. While Nolvadex only blocks the binding ability of free-floating estrogen, Proviron can minimize the creation of it. With each drug attacking estrogen via a different mechanism, we have a very synergistic combination. A daily intake of 20-30mg Nolvadex and 25-50mg Proviron can be extremely effective when dealing with a strong estrogenic cycle. Women often avoid adding Proviron to Nolvadex treatment (thought often it is still used to enhance fat loss), for fear of developing virilization symptoms (Proviron is an oral DHT). Virilizing effects can occur very quickly once there has been a dramatic rise in the activity of androgens (intensified by a decrease in estrogen activity), so at a minimum women should be careful with such a combination.

Of great interest also is that Nolvadex is an estrogen agonist in the liver, capable of activating the estrogen receptor and mimicking the actions of this sex hormone in this region of the body. As such it can have a markedly positive impact on HDL (good) cholesterol values, as does estrogen. Many similarly use this drug to counter some of the negative consequences of steroid use in regards to cholesterol values and cardiac risk, as steroids often suppress HDL and raise LDL levels considerably. in some instances an athlete is able to maintain a very favorable HDL/LDL cholesterol ratio, to spite the use of a moderate dosage (400mg weekly) of an injectable like testosterone or nandrolone. It would be foolish to think however that Nolvadex would be a sufficient remedy with the heavy use of c-l7alpha alkylated orals or extremely high dosed cycles in general.

It has been reported by many however that Nolvadex seems to slightly reduce to gains made during a steroid cycle. It appears that many androgenic/anabolic steroids will exhibit their most powerful anabolic effect when accompanied by a sufficient level of estrogen. This may be one reason why gains made with a strong androgen like testosterone are usually much more pronounced than when using an anabolic that aromatizes to a lower degree. It therefore seems like good advice to be aware of how much Nolvadex is actually needed before committing to it during a cycle. Many people in fact find it unnecessary, even when utilizing problematic compounds such as testosterone or Dianabol. Others however find they are troubled by water retention and gynecomastia, even with milder anabolics like Deca-Durabolin and Equipoise. The estrogenic response to steroid use is very individual, and may be influenced by factors such as age and body fat percentage (adipose tissue is a primary site of aromatization).

Nolvadex is certainly the most popular anti-estrogen used by athletes today, no doubt because it is simply an effective product. It is also widely manufactured, and easy to obtain. Since there never seems to be a lack of supply, there is little incentive to manufacture a counterfeit product. All of the various generics forms of this drug are no doubt trustworthy. Women should remember to be very cautious when considering the use of Nolvadex, as they are usually very sensitive to changes in the activity of estrogen. Men looking for a stronger anti-estrogenic effect may want to consider using Arimidex, Femara, or Aromasin , three powerful new anti-aromatase compounds. They are much more effective for estrogen control.
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Old 04-21-2004, 04:54 PM
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Clomid and nolvadex Characteristics:

While practically similar compounds in structure, few people ever really consider Clomid and Nolva to be similar. Its not just a common myth in steroid circles, but even in the medical community. This misconception originates from their completely different uses. Nolvadex is most commonly used for the treatment of breast cancer in women, while clomid is generally considered a fertility aid. In bodybuilding circles, from day one, clomid has generally been used as post-cycle therapy and Nolvadex as an anti-estrogen.

But as I intend to demonstrate this is in essence the same. I believe the myth to have originated because Nolva is clearly a more powerful anti-estrogen, and the people selling clomid needed another angle to sell the stuff, so it was mostly used as a post-cycle aid. But few users really understand how clomid (and also Nolvadex, logically) works to bring back natural testosterone in the body after the conclusion of a cycle of androgenic anabolic steroids. After a cycle is over, the level of androgens in the body drop drastically. The body compensates with an overproduction of estrogen to keep steroid levels up. Estrogen as well inhibits the production of natural testosterone, and in the period between the return of natural testosterone and the end of a cycle, a lot of mass is lost. So its in everybody's best interest to bring back natural test as soon as humanly possible. Clomid and Nolvadex will reduce the post-cycle estrogen, so that a steroid deficiency is constated and the hypothalamus is stimulated to regenerate natural testosterone production in the body. That's basically how the mechanism works, nothing more, nothing less.

Both compounds are structurally alike, classified as triphenylethylenes. Nolvadex is clearly the stronger component of the two as it can achieve better results in decreasing overall estrogen with 20-40 mg a day, than clomid can in doses of 100-150 mg a day. A noteworthy difference. Triphenylethylenes are very mild estrogens that do not exert a lot, if any activity at the estrogen receptor, but are still highly attracted to it. As such they will occupy the receptor and keep it from binding estrogens. This means they do not actively work to reduce estrogen in the body like Proviron, Viratase or arimidex would (by competing for the aromatase enzyme), but that it blocks the receptor so that any estrogen in the body is basically inert, because it has no receptor to bind to.

This has advantages and disadvantages. The disadvantage is that when use is discontinued, the estrogen level is still the same and new problems will develop much sooner. The advantage is that it works much faster and has results sooner than with an aromatase blocker like Proviron or arimidex. Therefor, when problems such as gynocomastia occur during a cycle of steroids one will usually start 20 mg/day of Nolva or 100 mg/day of clomid straight away, in conjunction with some Proviron or arimidex. The proviron or arimidex will actively reduce estrogen while the clomid or Nolvadex will solve your ongoing problem straight away. This way, when use is discontinued there is no immediate rebound.

So which one should you use? Well personally, I'd have to say Nolvadex. Both as an on-cycle anti-estrogen and a post-cycle therapy. As an anti-estrogen its simply much stronger, demonstrated by the fact that better results are obtained with 20-40 mg than with 100-150 mg of clomid. For post-cycle, this plays a key role as well. It deactivates rebound estrogen much faster and more effective. But most importantly, Nolvadex has a direct influence on bringing back natural testosterone, where as clomid may actually have a slight negative influence. The reason being that Tamoxifen (as in Nolvadex) seems to increase the responsiveness of LH (luteinizing hormone) to GnRH (gonadtropin releasing hormone), whereas clomid seems to decrease the responsiveness a bit1.

Another noteworthy fact about Nolvadex is that it acts more potently as an estrogen in the liver. As you remember, I mentioned that clomiphene and tamoxifen are basically weak estrogens. Well, tamoxifen is apparently still quite potent in the liver. This offers us the positive benefits of this hormone in the liver, while avoiding its negative effects elsewhere in the body. As such Nolvadex can have a very positive impact on negative cholesterol levels2 in the body, and therefore too should be considered a better choice than clomid. It will not solve the problem of bad cholesterol levels during Steroid use, but will help to contain the problem to a larger degree.

Another reason why I promote the use of Nolvadex over Clomid post-cycle (as if being 3-4 times stronger and having more of a direct effect on restoring natural test wasn't enough) is because it's a lot safer. Not just because it improves lipid profiles, but also because it simply doesn't have the intrinsic side-effects that Clomid has. Clomid causes more acne for sure, but that's mainly because you need to use a 3-4 times higher dose. But Clomid seems to also affect the eyesight. Long-term clomid therapy causes irreversible changes in eyesight3 in users. Irreversible. For me that alone is reason enough to prefer Nolvadex.

Lastly, one should be aware that use of these compounds can reduce the gains made on steroids. Nolvadex more so than clomid, simply because it is stronger. Estrogen is responsible for a number of anabolic factors such as increasing growth hormone output, upgrading the androgen receptor and improving glucose utilization. This is why aromatizing steroids like testosterone are still best suited for maximum muscle gain. When reducing the estrogen levels, we therefore reduce the potential gains being made. For this reason one may opt to try clomid during a cycle instead of Nolvadex. Although I would imagine that the problem that needed solved would be of more concern, in which case Nolva remains the weapon of choice. It's a plain fact that there is a high correlation between gains and side-effects. Either you go for maximum gains and tolerate the side-effects, or you reduce the side-effects, and with it the gains. That's life, nothing is free.

Stacking and Use:

If problems of Gynocomastia or other estrogen related symptoms tend to pop up during a cycle the use of 20-30 mg of Nolvadex or 100 mg of Clomid daily should easily contain the problem, and be used until a few days after the problem subsides. For best results and the least amount of problems upon cessation it is best stacked with Proviron (50 mg) or arimidex (0.5 mg) for this duration as well. Its not advised that these products be ran concomitantly with the steroid for the entire duration of the stack, as this will reduce your gains. Instead cease the usage of anti-estrogens once the problem is contained, and should the problem resurface, simply recommence the use of the products in the same manner as described above.

Once a cycle of steroids is concluded one should always initiate a post-cycle therapy to help bring back natural testosterone as soon as possible. This will help you to retain the mass you gained. How this is done depends highly on the type of steroid used. If only orals were used, therapy should start immediately, even the last day of the stack. If short-acting esters or water-based injectables were used, therapy should commence within 4-7 days after last injection, and if long-acting esters were used then it should commence 1.5 to 2 weeks after the last injection was given. The length of the therapy will vary as well, from 3-5 weeks. The longer acting the product was, the longer therapy should be continued to make sure all suppressive factors are cleared before use of Clomid/Nolvadex is discontinued.

For best results, it is best stacked with HCG (Human Chorionic gonadotrophin), which functions as an LH analog and can help bring testicle size back up. HCG use starts the last week of a cycle, and on from there every 5-6 days (usually 1500-3000 IU) and discontinued 1.5 to weeks prior to the cessation of Nolvadex/clomid. The reason being that HCG itself is also suppressive of natural testosterone and should be out of the body before therapy is over, or it will inhibit natural testicle function. But I can not stress enough that HCG possibly plays a more important role in post-cycle therapy than clomid/Nolvadex. For Clomid and Nolvadex, doses are usually tapered down. Its best to start with 40-50 mg of Nolvadex or 150 mg of Clomid for the first week or the first two weeks, and then finish the program with 20-25 mg of Nolvadex or 100 mg of Clomid for an additional two weeks.

References

1 Vermeulen A., Comhaire F., Hormonal effects of an anti-estrogen, tamoxifen, in normal and oligospermic men, Fertil. Ster. 29 (1978) 320-27

2 Bruning PF, Bronfer JMG, Hart AAM, Jong-Bakker M, tamoxifen, serum lipoproteins and cardiovascular risk, Br. J. Cancer 1988 Oct, 58 (4) 497-9
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