Cytadren
Aminoglutethimide
Cytadren (Aminoglutethimide) is one of the more interesting compounds found in the bodybuilder´s arsenal of Ancillaries. It´s really not too popular today, but a decade or two ago, it was considered state of the art, and was prized by bodybuilders for many of it´s properties.
Lets first consider it´s primary use, which is that of an Anti-Estrogenic compound. is able to produce highly significant (almost total) estrogen suppression (1), and this is of course of interest to athletes who are using steroids which convert to estrogen. Unfortunately, this suppression of estrogen is not followed by an increase in any of the other hormones (testosterone, LH, FSH, etc... ) that many other anti-estrogenic compounds will cause. Thus, Cytadren is probably not going to be anyone´s first choice for use in Post-Cycle-Therapy.
The thing which, in my mind, sets it apart from other ancillary compounds currently in use today is its unique ability to inhibit the production of cortisol. Cortisol, as you recall, is a catabolic hormone, and breaks down muscle. Cytadren inhibits the conversion of cholesterol to pregnenolone (2) as well as having an aromatase inhibiting effect. Thus, Cytadren is quite unique in having both of these abilities, and certainly none of the AI´s I´ve seen thus far has anything resembling such an effect on cortisol.
Cytadren is used, medically, to fight breast cancer and/or hyperadrenocorticism, and it is the only drug currently available (to my knowledge) that can be used successfully for both purposes (1)(3). It may even have anti-depressive properties (4)(5). During a cycle, it may be used to both lower cortisol levels from intense training, and to lower estrogen levels. Sounds almost perfect, right? It´s use would allow us to consider the use of Arimidex, Nolvadex, or a similar compound for strictly post cycle use, when an increase in test, LH, and FSH would be more necessary...
Well, it´s not quite perfect, as you´ll soon see. The first problem is that it (possibly) could reduce androgen levels. The best we could hope for is that it doesn´t have much of an effect on circulating androgen levels (1).
The next problem is that eventually your body, smart cookie that it is, will start to figure out ways to compensate for the reduction in cortisol, by either producing more, or inhibiting the Cytadren´s effects. Great... And while the cortisol isn´t present in your body, your joints will be aching. Yeah, I´ve actually used this stuff (the things I do in the name of science!), and it worked& made me look a bit "dryer" and more cut; but as I recall, it also made me sleepy. This could be due to its effects on the adrenal cortex, I don´t really know, but that´s a pretty good guess.
If you are thinking about using Cytadren for this purpose, I´d have to tell you to forget it. Three grams of Vitamin C lowers your Cortisol around as much as 1,000mgs of Cytadren, from the literature I´ve seen on both, and the Vitamin C doesn´t do it at the expense of your adrenal responsiveness (7). A gram of Vitamin C lowered cortisol by 1/3rd in UltraMarathon Competitors (8) (these are the people who apparently don´t have cars, so they feel compelled to run 90 kilometers at a time). I just can´t justify taking Cytadren for an extended period of time to reduce cortisol, when Vitamin can do the same thing, more cheaply, and has other added benefits.
Next, we have to deal with Cytadren´s liver toxicity (3). This stuff is pretty stressful on your liver. I guess we can use some milk thistle and such, but do we really want to risk it, when it´s effects on cortisol are short lived and it may reduce circulating androgen levels?
Maybe...
See you can use this stuff for (maybe) the last week or so while you are dieting for a bodybuilding contest, when your circulating androgens are being totally replaced by synthetic androgens, and you aren´t giving your adrenal-cortex much chance to shut down and make you lethargic, then I think it may be useful. Taking 500mgs/day for your last week of contest prep may help you to dry out that last little bit, and edge out that ever increasing specter of cortisol over production for long enough to do dial in for your contest. For athletes considering this compound in their cycles, I think this is not a viable option when you consider all of the other available options.
References:
- Preservation of androgen secretion during estrogen suppression with aminoglutethimide in the treatment of metastatic breast carcinoma. J Clin Invest. 1980 March; 65(3): 602 612.
- Adrenocortical steroidogenesis and aminoglutethimide I. Biomedical studies. Biomedicine. 1973 May;18(3):185-91.
- Use of aminoglutethimide in the treatment of pituitary-dependent hyperadrenocorticism in the dog. J Small Anim Pract. 2002 Mar;43(3):104-8.
- Treatment of depression with antiglucocorticoid drugs.Psychosom Med. 1999 Sep-Oct;61(5):698-711.
- Neuroendocrine responses to inhibitors of steroid biosynthesis in patients with major depression resistant to antidepressant therapy.Can J Psychiatry. 1998 Apr;43(3):279-86.
- Treatment of metastatic breast cancer with aminoglutethimide.Cancer. 1981 Apr 15;47(8):1954-8.
- A randomized controlled trial of high dose ascorbic acid for reduction of blood pressure, cortisol, and subjective responses to psychological stress. Psychopharmacology (Berl). 2002 Jan;159(3):319-24. Epub 2001 Nov 20.
- Attenuation of increase in circulating cortisol and enhancement of the acute phase protein response in vitamin C-supplemented ultramarathoners.Int J
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