TweetBy Dan Gwartney, M.D.

The Downside of Aromatase Inhibition

Adolescence is a time of discovery in a man's life; it is a period when one first experiences romantic thoughts, pimples, independence, and begins to understand why people laugh at Dane Cook. (Adulthood is when one wonders why people laugh at Dane Cook.) Physical changes are prominent during adolescence, brought on by surges in various hormones affecting growth and secondary sexual characteristics. Most healthy men remember the awkward occurrence of spontaneous erections during math class, P.E., or in church; many also went through the confusion of adolescent gynecomastia— developing soreness or even visually evident breast tissue under the nipple.

Gynecomastia, or benign (non-cancerous) breast development in the male, occurs when estrogen concentrations are elevated, or the balance between estrogen and androgens is disrupted to favor estrogenic effects in a male. Estrogens are one class of female sex steroid hormones including estrone and the dominant form, estradiol. There are also exogenous estrogens, such as birth control pills or medications to treat menopause.

Estrogens are formed in the body by converting precursor molecules into estrogens, through the actions of the enzyme cluster called aromatase.1 The precursor molecules could be called estrogenic prohormones, but that term is almost never applied, because these precursor molecules are better known for the function they serve as hormones. The immediate precursor molecules to estrone and estradiol are androstenedione and testosterone, respectively. A third estrogen, estriol, is sometimes mentioned; it is physiologically relevant during pregnancy and is not pertinent to estrogen production in man.

Healthy, adolescent boys develop gynecomastia due to the wild swings in androgen concentration they are subjected to as the testes emerge from the hormonally-dormant state of childhood; obese men often develop gynecomastia as a consequence of estrogen excess due to the action of aromatase in adipose (body fat); elderly men, those treated medically for prostate cancer, and men who lose testicular function due to disease or trauma, can develop gynecomastia as androgen (testosterone) levels fall and the relative influence of estrogen grows; certain medications and endocrine disruptors may also stimulate breast development, but those are non-physiologic factors.1,2

Gynecomastia was once common in bodybuilders and other anabolic-steroid (AAS) using men, as the supraphysiologic (way higher than normal body production) doses of testosterone and other AAS supplied aromatase with an equally abundant source of estrogenic precursors.3 Bodybuilders quickly learned that to avoid '***** tits,' fat gain, and water retention, doses of aromatizable AAS needed to be kept to a moderate level, and stacked with non-aromatizable AAS, if one wanted to keep a lean physique that wouldn't elicit a suckling response in infants.

Early Generation Drugs

Early generation drugs used to combat the estrogenic side effects seen with AAS use were of limited value and carried additional risks, due to non-specific suppression of steroid production (steroidogenesis). Cytadren® (aminoglutethimide) was used by many elite bodybuilders, especially during pre-competition training, as it provided a dry, hard physique.4

Though Cytadren is capable of reducing estrogen concentration, it does so at an early stage of steroid hormone production. Cytadren interferes with steroidogenesis at two major junctions; it inhibits the formation of pregnenolone from cholesterol (the first step is forming many important steroids), and inhibits aromatase— the conversion of androgens to estrogens.5

Cytadren's first action, inhibiting pregnenolone formation, is dangerous, as it subsequently inhibits the formation of many adrenal steroids, including cortisol. Though known in sports for its role as either a catabolic hormone leading to muscle loss, a stress marker elevated during overtraining/overreaching, or an anti-inflammatory, used to reduce the pain and swelling associated with severe sprains, cortisol is a critical hormone. Some people are born with a condition known as Addison's disease, and are unable to produce cortisol; without hormone (cortisol) replacement treatment, they suffer and die. Cytadren has been implicated as one contributing factor in the premature death of professional bodybuilder Andreas Munzer.

Fortunately, bodybuilders have moved away from the use of Cytadren with rare exception. Other estrogen-controlling drugs emerged, gaining favor due to their lower risk of side effects, low cost, and ease of use. Tamoxifen (Nolvadex®) reduces the effect of estrogen on certain tissues by competing for the receptors that affect the actions of estrogenic hormones, rather than interfering with the aromatase enzyme complex; it does not lower estrogen levels in AAS users, but has been effective in some cases.6,7

During the 1990s, a new class of aromatase inhibitors, developed to aid in the fight against breast cancer, emerged onto the bodybuilding scene. The two most prevalently used in treating or preventing AAS-induced gynecomastia are anastrozole (Arimidex®) and letrozole (Femara®).8,9 With the advent of these two drugs, particularly letrozole, oncologists (cancer doctors) acquired a powerful set of tools that are capable of suppressing estrogen in women down to a nearly undetectable concentration in the blood, and more importantly, in cancerous breast tissue.

The role of estrogen in men is poorly understood by most non-specialists, and not fully understood by any as yet. Bodybuilders were the first adaptors of aromatase inhibitors in men, of course. Word quickly spread about the ability to use doses of the relatively inexpensive and potent testosterone esters beyond limits previously imposed by aromatase-driven, estrogenic side effects.

Aromatase inhibitors were also used during cycles with low potential for estrogenic side effects in the hopes of further honing the 'cuts' and definition. Once research was published demonstrating an elevation in testosterone concentration in non-AAS-using males, both young adults and older adults, many 'drug-free' bodybuilders, athletes, and recreational fitness enthusiasts, began using these drugs.10,11 The misconception was that since these drugs were not controlled substances, not initially placed on the banned substance lists, and used to treat side effects, there was little risk or downside.

What's the Harm?

Truthfully, it is impossible to state whether anyone has been harmed by using aromatase inhibitors for performance- or physique-enhancement; it simply is not tracked. These two drugs are oral (a similar drug, Aromasin®, is injected); they generally do not cause physically perceived, short-term symptoms; and they are rarely used long-term. These factors instill a false sense of security in users.

Yet, there are problems that may arise as a result of aromatase inhibition, particularly aggressive aromatase inhibition that suppresses estrogen concentrations to very low values. Estrogen (primarily estradiol, but let's stay with the generic term estrogen for simplicity's sake) is not a metabolic waste product in men, a primordial remnant of no greater perceived value than the appendix. It is a functioning hormone that is anabolic in some tissues (e.g., bone, fat, breast); a stimulatory hormone (i.e., enhances production of certain circulating proteins in the liver); a metabolic modifier (affects endocrine hormones as well as carrier protein concentrations, such as binding globulins for vitamin D and sex hormones); a neurosteroid affecting neurotransmitter action, behavior, and emotions; an endocrine regulator; and has other functions.

It is irrational to think that there would not be hazards when concentrations are artificially suppressed well below the lowest extreme of the physiologic range, just as occurs when estrogen is elevated past the upper limit of normal. What, then, are some of the possible consequences to creating an estrogen deficiency in adult males?

Again, there is little in the published medical literature regarding aromatase inhibition in males, as there is as yet, no approved clinical indication for prescribing the drugs for men. However, there have been some observations in the limited clinical trials investigating aromatase inhibition in males; further, there are some adverse (harmful) effects that have been noted in female breast cancer patients that are not gender-specific.

Before proceeding further, it must be clear that this article relates to aromatase inhibition in healthy, adult males— including those using AAS; other populations, specifically women, are not addressed. It is worth noting that many of these findings occurred in breast cancer survivors, who may have been on aromatase inhibitors for several years continuously, suppressing circulating estrogen concentration by 98 percent.

Many bodybuilders use anastrozole or letrozole at full doses, seeking near-complete suppression of circulating estrogen. Thankfully, the realization is spreading that the benefits of aromatase inhibition for men, particularly male athletes/bodybuilders, are likely to arise by keeping estrogen within the normal physiologic range. Protocols using every-other-day dosing, one-half, or even one-quarter therapeutic doses are being disseminated in relevant forums.

Clinically, if one were to be prescribed an aromatase inhibitor, serum concentrations of estrogens should be followed to titrate the dosing accordingly, with a watchful eye toward emerging side effects. Unfortunately, aromatase inhibitors are typically obtained through illicit channels and self-administered without any laboratory monitoring or professional guidance.

Side Effects of Aromatase Inhibition

Arthralgia. Joint pain is the most common and relevant short-term side effect of aromatase inhibition. The incidence of arthralgia and musculoskeletal pain in post-menopausal women using aromatase inhibitors is as high as 25 percent.12 Synovial cells, the cells lining joints that produce the synovial fluid that bathes the articulating surfaces, contain a high concentration of aromatase.13 Over-production of estrogen in the synovium is associated with a pro-inflammatory state.14 Imaging studies performed on estrogen-deprived women demonstrate increased fluid surrounding the tendon sheaths, causing pain and limiting mobility (such as occurs with carpal tunnel syndrome).15,16

Fracture. The typical patients receiving aromatase inhibitor therapy are post-menopausal women, a group already at increased risk of bone fracture, due to osteoporosis. However, as estrogen is one of the primary anabolic or strengthening hormones for the bone, it logically follows that decreasing estrogen to near-zero levels would decrease bone re-building and increase fracture risk. In fact, this is seen in breast cancer patients.17

There have not been any cases published in the medical literature of bone density loss or fracture in men using aromatase inhibitors for performance enhancement. One study evaluating the use of anastrozole in elderly men with testosterone deficiency did demonstrate bone loss, suggesting this is an issue relevant to men.18 Of course, another showed no effect, as is the nature of science.10 It appears that this effect would be most pronounced in people with bones that are already compromised (e.g., vitamin D deficiency, anorexics), following prolonged use of aromatase inhibitors. Weight-bearing and contact define most sports, and it would be folly to ignore the potential for serious injury if the skeleton was weakened.

Libido and sexual function. A decreased libido is commonly reported by women receiving aromatase inhibitors.17,19 Additionally, vaginal dryness, pain and decreased sexual function/response often co-exist. There has been no data collected in estrogen-deprived men, but anecdotal reports of decreased libido have been expressed. This is consistent with observations seen in men with a genetic aromatase deficiency.20

Cardiovascular Risk. Estrogen plays a role in cholesterol metabolism, and estrogen deprivation may increase the risk for heart attack or stroke by possibly raising total cholesterol and LDL (bad) cholesterol, though this response is not uniform.17 Estrogen also protects against unhealthy changes in the electrical pulse controlling the heart beat, as well as protecting against hypertrophy (an enlarged heart).21,22 Estrogen deprivation may affect the blood supply, function, and structure of the heart in a negative manner.

Mental changes. Estrogens are neurosteroids, so it is no surprise that changing concentrations severely could affect a person's memory, math and verbal skills, emotions, personality, and mood.17,23 This area is poorly understood, particularly in men.

Kidney Disease. Much was made in the press recently about findings that some AAS-using men developed a type of kidney disease called sclerosing glomerulonephritis.24 A similar condition was diagnosed in a women receiving anastrozole.25 Though the association is weak at this time, considering that most men using anastrozole also used AAS, the potential compounded increase in risk is something to acknowledge.

Eyes. Retinal hemorrhages (bleeding) have been noted in women treated with aromatase inhibitors.26 The exact cause is unknown, but may be due to damage to small vessels in the eye, or retraction of the fragile retina, due to changes in the fluid of the eye.27 Complete blockage of the artery that feeds the eye has also been reported.28

Liver. Many proteins secreted by the liver, including IGF-1, are reduced with estrogen deprivation in men.29 Two case of hepatitis/hepatotoxicity have also been reported.30,31

The list above identifies some known and suspected adverse effects that are associated with the use of aromatase inhibitors. Much of the information comes from women being treated for breast cancer, but the physiology behind the injury is similar between men and women. Some effects may be gender-specific (e.g., mood changes) or predisposed to vulnerable populations (e.g., osteoporotic post-menopausal women), but this should not dissuade the intelligent person from considering the above when evaluating the pros and cons of using aromatase inhibitors.

There is likely a great deal that remains unknown about suppressing a hormone that acts on nearly every tissue in the body. Even less is known about the impact on the health or function in men, due to the gender bias in estrogen-related research. Many bodybuilders have found that using aromatase inhibitors provides them with the benefits of reduced body fat, as well as protection against gynecomastia and other estrogen-related side effects. Performance athletes have not been as enthusiastic about the use of this class of drug. Estrogen deprivation is reported to reduce the anabolic effect of some AAS, reduce exercise tolerance due to joint and tendon pain, and decrease libido.

It is likely that aromatase inhibition will find a defined role in men's health. As for the bodybuilder, his goal of maximizing definition may justify (for him) the short-term use of aromatase inhibitors. For athletes and fitness buffs, aromatase inhibition may offer some benefit if it is used to partially suppress estrogen production. However, this would need to be monitored and directed by someone skilled in the field in order to prevent a decrease in performance, adverse effects on health, or decline in quality of life. Despite being viewed as mild and safe drugs, the information above should clearly enlighten the audience of potential risks involved with aromatase inhibition.

References:

1. Gooren LJ, Toorians AW. Significance of oestrogens in male (patho)physiology. Ann Endocrinol, (Paris) 2003 Apr;64(2):126-35.

2. Johnson RE, Murad MH. Gynecomastia: pathophysiology, evaluation, and management. Mayo Clin Proc, 2009 Nov;84(11):1010-5.

3. Evans NA. Gym and tonic: a profile of 100 male steroid users. Br J Sports Med, 1997 Mar;31(1):54-8.

4. Mareck U, Sigmund G, et al. Identification of the aromatase inhibitor aminoglutethimide in urine by gas chromatography/mass spectrometry. Rapid Commun Mass Spectrom, 2002;16(24):2209-14.

5. Santen RJ, Misbin RI. Aminoglutethimide: review of pharmacology and clinical use. Pharmacotherapy, 1981 Sep-Oct;1(2):95-120.

6. de Luis DA, Aller R, et al. [Anabolic steroids and gynecomastia. Review of the literature] – article in Spanish. An Med Interna, 2001 Sep;18(9):489-91.

7. Spano F, Ryan WG. Tamoxifen for gynecomastia induced by anabolic steroids? N Engl J Med, 1984 Sep 27;311(13):861-2.

8. Llewellyn W. Arimidex (anastrozole). Anabolics, 2005. Body of Science Publication, Jupiter, FL;2005:232.

9. Llewellyn W. Femara (letrozole). Anabolics, 2005. Body of Science Publication, Jupiter, FL;2005:243.

10. Leder BZ, Finkelstein JS. Effect of aromatase inhibition on bone metabolism in elderly hypogonadal men. Osteoporos Int, 2005 Dec;16(12):1487-94.

11. Handelsman DJ. Indirect androgen doping by oestrogen blockade in sports. Br J Pharmacol, 2008 Jun;154(3):598-605.

12. Winters L, Habin K, et al. Aromatase inhibitors and musculoskeletal pain in patients with breast cancer. Clin J Oncol Nurs, 2007;11(3):433-9.

13. Le Bail J, Liagre B, et al. Aromatase in synovial cells from postmenopausal women. Steroids, 2001 Oct;66(10):749-57.

14. Schmidt M, Weidler C, et al. Androgen conversion in osteoarthritis and rheumatoid arthritis synoviocytes--androstenedione and testosterone inhibit estrogen formation and favor production of more potent 5alpha-reduced androgens. Arthritis Res Ther, 2005;7(5):R938-48.

15. Morales L, Pans S, et al. Importance of synovial fluid retention and thickening in patients with severe musculoskeletal pains treated with letrozole or exemestane: a case series describing the impact of symptoms, clinical findings and magnetic resonance imaging [abstract 4056]. Breast Cancer Res Treat, 2006;100(1).

16. Thorne C. Management of arthralgias associated with aromatase inhibitor therapy. Curr Oncol, 2007 December;14(1):S11-9.

17. Hong S, Didwania A, et al. The expanding use of third-generation aromatase inhibitors: what the general internist needs to know. J Gen Intern Med, 2009 Nov;24 Suppl 2:S383-8.

18. Burnett-Bowie SA, McKay EA, et al. Effects of aromatase inhibition on bone mineral density and bone turnover in older men with low testosterone levels. J Clin Endocrinol Metab, 2009 Dec;94(12):4785-92.

19. Cella D, Fallowfield L, et al. Quality of life of postmenopausal women in the ATAC ("Arimidex", tamoxifen, alone or in combination) trial after completion of 5 years' adjuvant treatment for early breast cancer. Breast Cancer Res Treat, 2006 Dec;100(3):273-84.

20. Carani C, Rochira V, et al. Role of oestrogen in male sexual behaviour: insights from the natural model of aromatase deficiency. Clin Endocrinol (Oxf), 1999 Oct;51(4):517-24.

21. Atsma F, van der Schouw YT, et al. Lifetime endogenous estrogen exposure and electrocardiographic frontal T axis changes in postmenopausal women. Maturitas, 2009 Aug 20;63(4):347-51.

22. Donaldson C, Eder S, et al. Estrogen attenuates left ventricular and cardiomyocyte hypertrophy by an estrogen receptor-dependent pathway that increases calcineurin degradation. Circ Res, 2009 Jan 30;104(2):265-75.

23. Blaustein JD. The year in neuroendocrinology. Mol Endocrinol 2010 Jan;24(1):252-60.

24. Dotinga R. Long-term use can lead to severe kidney scarring, new research shows. Medline Plus, 29 October 2009. Available at: https://www.nlm.nih.gov/medlineplus/n...ory_91224.html, accessed January 19, 2009.

25. Kalender ME, Sevinc A, et al. Anastrozole-associated sclerosing glomerulonephritis in a patient with breast cancer. Oncology, 2007;73(5-6):415-8.

26. Eisner A, Falardeau J, et al. Retinal hemorrhages in anastrozole users. Optom Vis Sci, 2008 May;85(5):301-8.

27. Eisner A, Thielman EJ, et al. Vitreo-retinal traction and anastrozole use. Breast Cancer Res Treat, 2009 Sep;117(1):9-16.

28. Karagoz B, Ayata A, et al. Hemicentral retinal artery occlusion in a breast cancer patient using anastrozole. Onkologie, 2009 Jul;32(7):421-3.

29. Mauras N, O'Brien KO, et al. Estrogen suppression in males: metabolic effects. J Clin Endocrinol Metab, 2000 Jul;85(7):2370-7.

30. de la Cruz L, Romero-Vazquez J, et al. Severe acute hepatitis in a patient treated with anastrozole. Lancet, 2007 Jan 6;369(9555):23-4.

31. Zapata E, Zubiaurre L, et al. Anastrozole-induced hepatotoxicity. Eur J Gastroenterol Hepatol 2006 Nov;18(11):1233-4.

TweetArimidex

(Anastrozole)

Anastrozole is a powerful anti-estrogen medication commonly sold under the brand name “Arimidex” and it is by that name most are familiar with the compound. As an anti-estrogen medication Arimidex belongs to the aromatase inhibitor (AI) family and it is by this designation we truly see the function of this medication. First brought to the market by AstraZeneca, Arimidex was created in an effort to combat breast cancer in post-menopausal women. As we are aware estrogen is the enemy when it comes to breast cancer and Arimidex actively reduces the amount the body produces and it is by this trait one can already begin to see how this might be useful in-terms of anabolic steroid use. No, Arimidex is not an anabolic steroid; it is not a steroid in any shape or form but is commonly used in conjunction with anabolic steroids to combat estrogenic related side-effects.

Arimidex 101:

Anastrozole, commonly known as Arimidex is an aromatase inhibitor that actively blocks the aromatase enzyme by-which its duty cannot be performed, that being producing estrogen. By this inhibiting process the compound can actively reduce estrogen in the body by as much as 80%. Coupled with its estrogen reducing effects Arimidex also greatly increases testosterone in the body and can do so by as much as 50% by increasing total testosterone as well as Luteinizing Hormone (LH) and Follicle Stimulating Hormone (FSH) total output.

For the breast cancer patient this proves to be invaluable as decreased estrogen provides remedy, for in many ways breast cancer in very simplistic terms feeds off of the estrogen hormone. However, this same trait can also provide benefit to the anabolic androgenic steroid user in both hormone replacement patients who are very sensitive to testosterone treatment and of course to performance enhancers. Many anabolic androgenic steroids convert to estrogen due to the aromatase process and estrogen, while an essential hormone can lead to many unwanted side-effects when it is present in excess.

The Benefits of Arimidex:

By and large, as it pertains to anabolic androgenic steroid use the use and benefits of Arimidex greatly surround side-effect prevention. However, in men who suffer from low testosterone and who seek therapeutic remedy Arimidex can at times be a good choice, for as we discovered above the compound by its nature actively increases total testosterone output. Even so, while this remains true most men will find direct testosterone treatment to be optimal in treating their low levels and will generally require a regular dosing of an injectable or transdermal testosterone medication. In the case of low testosterone treatment most men will find the therapy well-tolerated and generally side-effect free; we must always remember, side-effects increase when dosing increases and as therapeutic dosing is very low the need for an AI is generally low in low testosterone patients.

Without question those who supplement with anabolic androgenic steroids for the purpose of performance enhancement will benefit from Arimidex use the most when comparing to therapeutic steroid users. Performance enhancing doses are necessarily larger than therapeutic doses; after all, in therapy the idea is to return hormonal levels to normal but in performance enhancement the idea is to surpass them and to do so greatly. With such doses in mind the rate of aromatase greatly increases; no, not all anabolic androgenic steroids convert into estrogen but a vast quantity do and at varying rates depending on the steroid. By this conversion process when excess levels of the estrogen hormone buildup in the body some of the most common and well-known anabolic steroid side-effects may manifest themselves; including but not limited to:

Gynecomastia
Water Retention
High Blood Pressure
High LDL Cholesterol
Low HDL Cholesterol
Loss of Libido
Hair Loss
Fat Gain
While some of these side-effects can be brought on by other factors, especially blood pressure and cholesterol, estrogen buildup can play a major role. For the majority of performance enhancing athletes the side-effects of steroid use that are of the greatest concern will remain Gynecomastia and water retention as these are the two most common but it is often in Arimidex they find remedy. As Arimidex blocks or as indicated by its name as an AI “Inhibits” estrogen buildup many of the common side-effects become nothing more than a memory or concern of the past. Think about it, if the estrogen that causes the side-effects is no longer present how can estrogenic related side-effects present themselves; they can’t, what doesn’t exist simply doesn’t exist.

Some performance enhancers, especially those who are looking to really add size to their frame often shy away from Arimidex out of a fear of losing or not obtaining gains. It is true, estrogen aids in the promotion of building muscle tissue and more importantly it is a hormone essential to our overall health, particularly our immune system. However, we are not removing all estrogen from our body through Arimidex use, we are simply reducing it, although greatly. Further, if you are going to supplement with anabolic steroids for the purpose of performance enhancement you need to ask yourself an important question; what’s worse, a few less gains or horrible unsightly side-effects? It is also important to note, while estrogen suppression will somewhat limit the amount of weight you gain it will not do so to the degree feared by many; not even close.

The Side-Effects of Arimidex:

When it comes to side-effects it is always important to note all medications from every family carry with them a potential for side-effects; this includes everything to common cold medicine, pain killers, anabolic steroids and even AI’s such as Arimidex. However, when we examine Arimidex the potential for adverse side-effects appears to be very low. There do not appear to be any strong negative indirect side-effects due to supplemental use; however, use can lead to unwanted effects due to decreased estrogen in the body. In order for the human body to maintain a proper functioning endocrine system we must have some estrogen present. Further, decreased estrogen can have a negative effect on cholesterol, a very side-effect problem you are trying to prevent through use; as you may have guessed when it comes to cholesterol there is a very fine line as it pertains to the estrogen hormone. However, Arimidex doesn’t appear to affect this greatly in a negative way and therefore remains a positive choice in this regard.

For the majority of steroid users, those who supplement with Arimidex will not want to do so indefinitely in the name of safety; while it is generally side-effect friendly it is not a good idea to keep estrogen levels so suppressed for far extended periods of time. Most will find such AI’s should only be used while on cycle and discontinued once the cycle is complete in order to let the body return to normal hormonal production. If side-effects are not a problem for you then perhaps no Arimidex will be needed; however, for competitive physique athletes, even if they rarely suffer from anabolic steroid side-effects Arimidex can still be very useful, as reduced estrogen will provide a leaner and harder physique. For this reason many competitive bodybuilders supplement with Arimidex during their contest preparation diets.

Arimidex and SERM’s:

It is very common for Selective Estrogen Receptor Modulators (SERM’s) to be thrown in the same anti-estrogen category as Arimidex and other AI’s but this is far from correct. SERM’s such as Tamoxifen Citrate (Nolvadex) and Clomiphene Citrate (Clomid) do not inhibit the aromatase process in the body; they do not actively reduce the total amount of estrogen in the body. SERM’s such as Nolvadex or Clomid simply block estrogen from binding to certain receptors in the body and this can be a very useful tool; however, as you can see it is not nearly as strong since it has no reducing capability. Even so, SERM’s in the same light as AI’s actively increase or stimulate natural testosterone production and for this reason are commonly used during what is known as the Post Cycle Therapy (PCT) plan. Yes, both SERM’s and AI’s can be used for PCT purposes, the PCT purpose being largely to return testosterone production back to normal after it has been diminished through anabolic steroid use. However, we do not recommend AI’s for PCT therapy, even though they will increase testosterone greatly we prefer SERM’s for this purpose for one simple reason. During the PCT process we are not simply trying to increase testosterone but to normalize our entire hormonal production. As AI’s greatly reduce estrogen, a much needed hormone in the human body, we prefer SERM’s over AI’s to fulfill this purpose.

Arimidex Cycles and Doses:

Most who supplement with Arimidex will be doing so for the prevention of side-effects while on cycle or to tighten up their physique for a physique based competition by reducing estrogen in the body. Most men will find 0.5mg every other day to be a good starting point while on cycle if it is needed for side-effect prevention with 1mg every other day generally being the most anyone will ever need for this purpose. However, if side-effects begin to manifest, particular Gynecomastia, many find supplementing with 1mg every day for a few weeks to be useful in combating this enemy; however, for this purpose we would in most cases recommend the slightly stronger AI Letrozole but Arimidex will often suffice. If this occurs, simply supplement with 1mg every day until symptoms pass; once they do drop the dose to every other day and finish your intended cycle. It should be noted, this is not a 100% failsafe plan; for some no amount of any AI on earth will protect from Gynecomastia.

The same dosing can be applied in physique sport competition, most notably bodybuilding; it is very common for many bodybuilders to supplement with Arimidex for 12-16 weeks leading up to a competition at a dose of 1mg every other day. However, many bodybuilders will necessarily increase the dose to 1mg every day the final 10-14 days before the show in order to ensure they are as hard and water free as possible. However, we cannot recommend anyone supplement with this compound at that high of a dose for an extended period of time, as such dosing for extended periods would be too much estrogen suppression.

Women in the physique sports world also sometimes supplement with Arimidex to provide a dryer and harder look but this will generally only occur a few weeks out from competition. Low doses for short periods of time can aid in a woman the same way it can a male competitor but as estrogen is slightly more important to a female use must necessarily be limited.

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