Cytadren (aminoglutethimide, chemical name: 3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione) is an 'anti-steroid' drug, which blocks the production of steroids derived from cholesterol. Clinically, it is used for Cushing's syndrome and metastatic breast cancer. It has been used by bodybuilders to block cortisol and inhibit estrogen during cycles. It comes in tablet form, and it is exclusively used orally.
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Cytadren is the trade name of aminoglutethimide, which was brought to market by Novartis. 'Steroid guru' Dan Duchaine was the first to bring this drug to the forefront of bodybuilding, and it is rumored that Andreas Munzer had the drug in his system when he died in 1996.
How it works
Cytadren works by doing two things:
1. It blocks the conversion of cholesterol to pregnenolone by inhibiting the enzyme P450scc, which decreases synthesis of all hormonally active steroids including cortisol. Unfortunately, only a high dosage of this drug will accomplish this result; hence, it is always abused by bodybuilders. The dose required for reasonable results will always force guys to abuse the drug.
2. It blocks the aromatase enzyme. It is a potent aromatase inhibitor, but it's not stronger than letrozole.
Cortisol and Bodybuilding
Cortisol is a steroid hormone glucocorticoid, which is produced in the adrenal cortex. It is released in response to exercise, stress, and low level of blood glucose to increase blood sugar. It is supposed to aid the metabolism of fats, proteins, and carbohydrates, but it doesn't always work that way for bodybuilders. Cortisol is catabolic, meaning it will break down your muscles.
Cytadren is abused by bodybuilders to lower circulating levels of cortisol in the body and prevent muscle loss due to catabolism. To achieve this result, one must run a high dosage, which leads to abuse. Theoretically, this can allow bodybuilder to workout longer, harder, and without worry about extra stress being put on the body from an increase in cortisol. Essentially, they can rip up their muscle fibers more than their competition giving them a major advantage. However, there is a huge downside to this we'll discuss later.
Another benefit of cytadren is its ability to act as an aromatase inhibitor, which will strongly suppress estrogen. This helps keep water weight off and leads to a dryer and harder look ahead of a contest. This is why some bodybuilders will use this drug the last week or two ahead of their competition, but they aren't always prepared for the long-term consequences.
There are no shortage of reports of major side effects with bodybuilders, especially when this drug is used at the effective dosages. The main side effect that bodybuilders complain about is being 'sleepy and weak' outside of the gym. Also, joint problems when lifting heavier weights are reported regularly.
Other side effects that are common with aminoglutethimide:
- Nausea/stomach upset
- Thyroid problems
- Liver disease
With all the side effects above, you would think cytadren is bad enough, right? Well think again, it's a lot worse than you think. Cytadren has a huge flaw because the results are temporary. Meaning, once you stop using cytadren, your cortisol levels shoot through the roof and you start having very high cortisol levels. This means you'll be losing any muscle gains you made with the drug. In addition, it's not a suicidal aromatase inhibitor, so once use is discontinued, expect spikes in estrogen. This will lead to nasty side effects like gynecomastia (bitch tits), high blood pressure, low libido and problems with erections.
Heard enough? Well here are some anecdotal side effects guys report after discontinued Cytadren use:
- Flu-like symptoms
- Emotional problems
- Decrease in Endurance
- Huge problems in bed
- Constant Nausea
This is an old-school drug and should never be used by guys in 2015 because there are way better drugs and natural alternatives on the market today. Cytadren is dangerous and shouldn't be used in the modern bodybuilding era.
Cytadren should never be used during post cycle therapy (PCT), and it should only be used by VERY experienced bodybuilders leading up to a show.
As an AI, a typical dosage is 250mg per day, which will decrease aromatase activity by up to 92%. This is too much, so you never want to run this drug a long time. Expect an estrogen rebound after you stop using it.
The few bodybuilders that have dared run this potent drug to inhibit cortisol will run a gram a day. Again, only experienced bodybuilders who have done their homework should ever attempt to use this drug for lowering cortisol. Expect a cortisol rebound after you stop using it.
According to medical literature, the half life of cytadren averaged 12.5 +/- 1.6 hours. The drug is rapidly and completely absorbed after oral administration, and after indigestion of a single oral dose, 34-54% is excreted in the urine as unchanged drug during the first 48 hours. There is an additional fraction as a N-acetyl derivative.
These days, some companies are attempting to put out a “supplement” version of cytadren (aminoglutethimide) by using cyclohexylaminoglutethimide in their supplements, which is a terrible and dangerous idea.
Here is the chemical formula of aminoglutethimide (cytadren) vs. cyclohexylaminoglutethimide (supplement):
Essentially, these new supplements are cyclodextrin based versions of cytadren, which will lead to very serious side effects for the users.
Potential Cyclohexylaminoglutethimide side effects:
- Gynecomastia (bitch tits)
- High blood pressure
- Low libido
- Problems with erections (ED)
- Increase in cortisol levels
- Increase in estrogen levels
- Loss of sex drive
- Loss of muscle gains
- Thyroid Problems
Cytadren is a serious drug for advanced bodybuilders, and it should never be given to newbie users as an anti-estrogen. It's dangerous and irresponsible, so be warned.
Want to read about Cytadren on our forums? check out these threads:
- Nonsteroidal and steroidal aromatase inhibitors in breast cancer
- CHEBI:2654 - aminoglutethimide
- Davis's Drug Guide
- Showing metabocard for Aminoglutethimide (HMDB0014501)
- along with aminoglutethimide
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