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Aromatase Inhibitors (AIs)
Keep in mind Estrogen is good for you in many ways (libido, mood, skin quality, hair, nails etc). But, most importantly, Estrogen is good for your lipids. I am sure you have heard how Arimidex and Letrozole are bad for your lipid values while Aromasin is ‘better’, in reality all AI’s are as bad as each other for your liver values. The more you lower Estrogen, the worse your liver values will get – it doesn’t matter which AI you use, all that matters is how much you are lowering your Estrogen. If you lower your Estrogen by 10 pg/mL you won’t notice much difference. If you crash your Estrogen down to single digits I guarantee you that your HDL/LDL will be completely out of whack no matter which AI you used.Suicidal AI vs. Non-Suicidal/Binding AI
Arimidex and Letrozole are non-suicidal AI’s, all they do is bind any Estrogen you convert directly on your aromatase enzyme. Each AI binds a different percentage of Estrogen, Letrozole binds more than Arimidex of course. The problem with binding AI’s is that once you cease use, all of the Estrogen that had accumulated when you were using that AI suddenly gets released – this process is called "Estrogen rebound" and I am sure you know it can be far worse than Estrogen while on a cycle since normally when you drop your AI you either cruise with a low dose of Test or PCT. In both cases you have far less Test in you and once all that Estrogen is released you got a much higher chance of getting Gyno and of course you are going to be bloated and feel soft for weeks till your Estrogen comes down to normal levels.Aromasin is the new generation of AI and it is suicidal, the difference between Aromasin and the other AI’s is Aromasin will actually destroy/kill a certain percentage of your aromatase enzyme so by doing so it also 'kills' any estrogen that was attached to that enzyme. This means when you stop using Aromasin you won’t rebound at all like you would with the binding AI’s. If anything, you will have to wait for a while for your body to start producing more aromatase (very bad if you crashed your Estrogen comparing to using the other AI’s). Each person is different in the rate they create new aromatase; it can take one to three weeks.
Arimidex (Anastrozole)
Arimidex (Adex) will lower your Estrogen by about 50-60%. Of course, if you keep taking it that percentage accumulates so you lower 50% by another 50% and so on, you can easily end up with your Estradiol in the singles if you take it for long enough at a high enough dose and you aren’t converting much Estrogen from aromatizing gear (using low dose of Test and high dose AI). Arimidex is a good for new steroid users as if they overestimate their dosing for AI and get symptoms of low E2, they will bounce back back up fairly quickly and adjust as needed.Dosage on cycle: dosing is user dependent and you should get blood work to dial in your dose, but MOST users will find .5 mg of Arimidex E3D or E3.5D to be a good starting dose for 500-600 mg Testosterone (just for a reference). Some may need more frequent (EOD) dosing or some may even need less than E3.5D; this is really something that varies person-to-person too much and without blood work there is no way to know for sure what dosage you need.
Aromasin (Exemestane)
Aromasin (Asin) is an orally available suicidal aromatase inhibitor. Because Aromasin is steroidal this gives it a favorable Estrogen suppression profile and confers a few really awesome benefits over other anti-estrogens both on paper and in real experience. Steroidal anti-estrogens have the benefit of being lipid-friendly and they all lower SHBG which increases the ratio of free to bound Testosterone, which as many experienced bodybuilders know can have a relatively profound, positive impact on gains.It is important to understand how drugs work in order to properly dose them, Aromasin is a suicidal aromatase inhibitor, this means that it binds with aromatase enzymes and as it does so permanently disables the enzyme and destroys it. Hence the “suicidal” this compound. Just beware, if you crash your estrogen on Aromasin, it can take a long time waiting for your E2 to rise again (compared to the non-suicidal AIs), which will have a negative impact on lipid profile, joint integrity, mental health, libido and overall gains.
Aromasin’s half life in the male body is actually very short (~9 hours) and it is quickly eliminated, however, since as soon as it enters your bloodstream it quickly destroys the aromatase enzymes present in your body, it is effective in maintaining significant reductions in estrogen for up to +72 hours after a single 25mg dose. Estrogen levels only begin to rise again after your body has begun to make new aromatase enzymes to replace the ones destroyed by Aromasin.
There is a great study on the pharmacokinetics of Aromasin in men which found the following:
- 24 hours after one 25mg dose estrogen levels are reduced by 58 ± 21%
- 3-6 days after initial dose estrogen levels return to baseline (without rebounding)
BUT WAIT, there’s more. In males, Aromasin was found to increase total testosterone by ~60% after 10 days @ 25mg/day, however the same study found that while it increased total testosterone by 60%, free testosterone was increased by over 100 percent! that’s right, it DOUBLES bio-available testosterone (in naturals of course). With all this said, it is an option to be ran into PCT like the study, when utilizing HCG right before or the first couple week of PCT. See the PCT wiki page for more info.
The Good:
- Lowers SHBG, increasing free test & makes all other anabolic steroids more bio-available (i.e. more gains)
- Increases IGF-1
- No adverse changes in lipid profiles for men (unless you crash estrogen - studies were also not on cycle and may be different)
- Is not liver toxic
- No Estrogen rebound
- Typical aromatase inhibitor issues here, include stiff joints and possibly lethargy if E2 gets too low
- If you crash your E2 levels, it will remained crashed until your body makes more aromatase at it's own rate.
- Typically more expensive than Arimidex or Letrozole
- Alopecia. The other two AI’s have hair loss/hair thinning as a side effect, but not full blown Alopecia.
Letrozole
Letrozole is by far the harshest of all AI’s, not necessarily because your Estrogen will be too low but because Letrozole as a compound/active ingredient is really harsh. The main applications for Letrozole is for Contest Prep or apart of Gyno Reversal (along with a SERM) as this is the nuclear option. Whenever used, always be sure to taper off to avoid rebound.On cycle dosage: This AI is very easy to crash your estrogen with. It is not typically recommended as your main AI
Selective Estrogen Receptor Modulators (SERMs)
After your cycle is complete and the steroid esters start to clear the system, a post cycle therapy (PCT) is done to help get the pituitary glands running again. SERM's work by blocking estrogen going into the pituitary glands, which cause a rise in LH/FSH and testosterone levels, temporarily. This helps give a boost after cycle, and it helps maintain gains.Keep in mind all 3 SERMs will work in favor of your liver (Agonists) since they are mild Estrogens, like stated earlier Estrogen is good for your liver so adding a SERM will always improve your HDL/LDL. All SERMs don’t lower Estrogen, in fact they will increase your total Estrogen. They also block your Estrogen in the nipple area.
Nolvadex (Tamoxifen)
Agonist: Liver, Uterus (female)Antagonist: Breast/Nipple
Nolvadex is more suited for PCT purposes rather than Gyno Flair-Ups or Gyno Reversal, as it increases natural Test levels by 60%, but will decrease IGF-1 levels +25%.
Dosage on cycle: 20-40mg ED
Dosage for PCT: See PCT
Raloxifene (Evista)
Agonist: Liver, bone (increases bone density and is a recognized treatment for osteoporosis)Antagonist: Breast/nipple
Raloxifene doesn’t affect IGF-1 levels whatsoever, also it increases bone density. It is the ideal SERM for Gyno Flair-Ups or Gyno Reversal since its an agonist for your bones, doesn’t affect IGF-1 levels, and is perfectly safe to run with a 19-Nor. Raloxifene shouldn’t be used in PCT since it raises natural test levels by 40% only, 20% less than Nolvadex.
Dosage on cycle: 60mg-120mg ED
Nolvadex vs. Raloxifene for HGH/IGF-1
Taken from this studyConclusions: Tamoxifen, but not Raloxifene, reduces IGF-I levels. Both SERMs stimulate the gonadal axis, with tamoxifen imparting a greater effect. We conclude that in therapeutic doses, Raloxifene perturbs the GH and gonadal axes to a lesser degree than Tamoxifen.
Nolvadex vs. Raloxifene for Gyno
Taken from this studyConclusion: Inhibition of estrogen receptor action in the breast appears to be safe and effective in reducing persistent pubertal gynecomastia, with a better response to Raloxifene than to tamoxifen. Further study is required to determine that this is truly a treatment effect.
Gyno Flare-Up Protocol
If your Estrogen is wildly out of control and you are developing puffy, sore, or itchy nipples, UP your AI dose and start taking your SERM.Note: If you choose Arimidex as your AI, just be aware the blood levels of Arimidex can drop a bit when used alongside Nolvadex.](/r/steroids/wiki/faq/list#wikiq.3A_can_nolvadex.28tamoxifene.29and_arimidex.28anastrozole.29_be_used_together.3F) To avoid this, you may choose Raloxifene.
Dosing: Pharmaceutical Raloxifene 60mg ED or Pharmaceutical Nolvadex 20mg ED. It usually will subside after a 7-12 days. Continue the SERM for 3 days after the symptoms have subsided before you drop the SERM. It is suggested to use Raloxofine over Nolvadex when possible, due to Nolvadex decreasing IGF-1 as seen above.
Gyno Reversal Protocol
If your Gyno is pubertal, as seen above, this potentially could help, but most likely surgery is your best option. If your Gyno is from AAS use, this has worked for multiple users on our board:Dosing: Pharmaceutical Raloxifene 120mg ED - split the dose ½ in the AM, ½ in the PM for a month, then 60mg ED - split the dose ½ in the AM, ½ in the PM until you've seen sufficient reduction in size.
Toremifene (Fareston)
[Under Construction]Clomid
Agonist: LiverAntagonist: Breast/nipple
Clomiphene is a harsh drug, if you get the visual sides/blurry vision from clomid they stay for life. They are rare, but do happen.
Clomiphene is a mixed agonist/antagonist. This is due to the fact that Clomiphene is composed of two isomers: enclomiphene (trans-clomiphene) and zuclomiphene (cis-clomiphene). Enclomiphene is an Estradiol receptor antagonist. Zuclomiphene is an estradiol receptor agonist. In all likelihood, the net antagonist effect might be due to the composition being 70% trans (enclomiphene) and 30% cis (zuclomiphene). Nolvadex/Raloxifene is more of a strict anti-estrogen, decreases the effect of estrogen in the body, and potentiates the action of clomiphene. This combination came about after 100s of clinical experience.
So Nolvadex/Raloxifene is more of an antagonist, than Clomid is. They are better at blocking the ER than Clomid is. Clomid also seems to exert agonistic effects in parts of the brain that control emotion. That would explain why some turn into women on periods during there experiences with Clomid.
Tamoxifen is also made of slightly more isomers, the cis isomer of tamoxifen (inactive one) trans-tamoxifen and trans-4-OHT isomer.
All you really need to know about clomid can be learned here: Product Information: Clomid(R), Clomiphene citrate. Aventis Pharmaceuticals, Kansas City, MO, 96.
Here is the clomiphene drug monograph
- If you want to learn about any drug, the manufacturer PRODUCT INFORMATION and DRUG MONOGRAPH are excellent and probably the best way to learn about any drug, especially these PCT medications, as these sources are FDA approved and studied in large clinical trials.
- The FDA recommended dosage for clomid for male hypogonadism (what we are trying to beat with PCT) is 25 mg EOD or every day, titrated up to 50 mg EOD MAXIMUM for HPTA restart.
