Letrozole (Femara) is a reversible aromatase inhibitor that is noted as the most potent nonsteroidal AI. It is one of the three most commonly used aromatase inhibitors by steroid users to control side effects related to estrogen as a result of the use of aromatizing steroids (the other two common AIs being Arimidex – nonsteroidal and Aromasin – steroidal).
Letrozole is a drug that will appeal to users of the most popular aromatizing steroids such as Testosterone, Dianabol, and countless others where the development of water retention, high blood pressure, and gynecomastia are serious concerns.
Author’s Note: The following guide is based on my personal experience and does NOT promote the illegal use of steroids (PEDs).
What is Letrozole (Femara)?
Like most of the AIs we look at for use alongside anabolic steroids, Letrozole was also developed for the medical treatment of breast cancer in post-menopausal women.
The reason it is only used in women of such an age is due to its powerful estrogen-blocking ability, which would have serious health implications for pre-menopausal women. Still, for male steroid users in particular, it is this trait that makes AIs like Letrozole so appealing as we aim to combat the adverse effects of estrogen when using aromatizing steroids.
Letrozole is able to lower your overall estrogen levels because it blocks the aromatase enzyme. This is in contrast to the other popular category of estrogen control drugs for steroid users, SERMs, which only target very specific areas of the body.
Letrozole combats a wider range of estrogenic side effects caused by steroids, with the two main ones being gynecomastia and water retention. This will also help prevent the high blood pressure that can come along when excess water retention is not addressed.
Letrozole Effects for Gynecomastia and Estrogen Control
Letrozole is such a powerful AI and so effective at controlling estrogen that some steroid users have reported being able to reverse the effects of gyno when using this drug successfully.
Even so, it is always preferable to try and prevent gyno from rearing its head at all rather than depending on any drug to reverse it because while some people might have luck with this when using Letrozole, others will find that more advanced gyno is still not reversible without surgery.
Letrozole will reduce the entire circulating levels of estrogen in the body, unlike SERM drugs, which will target specific receptors and are most useful for controlling gyno – Letrozole will also be powerful for controlling water retention, which is the other main adverse effect of steroid use that we all want to avoid.
When using Letrozole, you can expect your estrogen levels to be reduced considerably, as this is currently the most powerful AI we can access. In fact, it could result in your estrogen dropping too low at times (yes, this can be an issue for men as we do require a small amount of estrogen for normal functioning). But during a steroid cycle, your main aim with an AI is to reduce, minimize, and ultimately prevent the estrogenic side effects that are almost certain to come about when using steroids that aromatize.
There are additional benefits to this estrogen-controlling power of Letrozole, too: because it means you can prevent water retention, your physique will take on a much harder, drier, and ripped appearance because you’re not holding on to water. This can make Letrozole particularly useful for competitive bodybuilders who want to eliminate as much fluid retention as possible, and Letrozole is the best AI to help with this goal.
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Even at very low doses, Letrozole is a potent drug, so you do not require much of it to benefit from its full effects. Unlike with many of the other AIs or SERMs you might use as a steroid user where doses are normally higher than those used for medical treatment, with Letrozole, we can get away with using a similar dose or even lower than is administered when the drug is used medically.
Letrozole Dosage During Anabolic Steroid Use
Making the mistake of taking too much Letrozole during steroid use will have no benefit and bring about negative effects, like fatigue. So, it’s critical to maintain a sensible dose.
With a medical dose usually around 2.5mg daily, we would look at no higher than that and, most of the time, even lower. To protect from estrogen-related side effects during steroid use, a dose of as low as 0.5mg to 1.25mg every two days is often enough for excellent estrogenic-related protection for most men.
Only if you are experiencing early signs of gynecomastia would increasing the dose at this time up to 2.5mg per day potentially fully reverse the symptoms, but be prepared for a noticeable zap in energy during this time. Once gyno symptoms subside, it’s important to reduce your Letrozole dose back down to regular estrogenic protection levels.
Female Letrozole Dosage
Increased estrogen levels are not anywhere near as great a concern for female steroid users as it is for males. The main reason for using an AI like Letrozole by females would be to mitigate water retention, especially for competitive bodybuilders or physique athletes, where this is most important.
In fact, Letrozole is not recommended as a first choice for females due to its potency in reducing estrogen so much, hence why it is not used medically by females who have not gone through menopause. Females who are determined to use this AI are advised to dose at just 0.5mg every other day and gauge results and effects from there.
Letrozole Dosage for Increased Endogenous Testosterone Secretion and PCT
This AI may have some ability to raise testosterone levels, mainly through its ability to reduce estrogen. Both luteinizing hormone and follicle-stimulating hormone have been shown to be able to be increased by Letrozole, and these are essential to the production of testosterone.
So while a reduction of estrogen is important for bringing about a rise in testosterone levels, this is a fine balance in men, and reducing estrogen too low can actually have the opposite effect, with testosterone not able to increase to a normal level if estrogen is suppressed too powerfully, which Letrozole has the ability to do.
For this reason many will choose not to make use of this drug during post-cycle therapy at all in favor of using a SERM like Nolvadex. However, suppose you find that Letrozole is preferable for you for post-cycle therapy use. In that case, a low dose similar to or lower than that stated above during your steroid cycle is the only way to reduce the risk of very low estrogen occurring.
Making use of Letrozole alongside Nolvadex, which is a staple in PCT for most men, results in both drugs, making the other less effective. Combining these drugs is not recommended for PCT. Therefore, most people will opt to use the better PCT option in the SERM Nolvadex while enjoying the benefits that Letrozole can provide during the steroid cycle only.
Letrozole vs. Arimidex for PCT
Letrozole and Arimidex are very similar compounds. Both are nonsteroidal aromatase inhibitors, and both are favored by anabolic steroid users to prevent estrogenic side effects. Both drugs have a similar side effect risk profile. Out of these two AIs, Arimidex generally takes the lead as being more widely used by bodybuilders, but this can come down to a number of factors, including availability, cost, and wanting to follow in the path of what friends and online acquaintances might recommend.
While both of these AIs can help stimulate natural testosterone production, neither is considered by most guys to be the right choice for PCT when used alone; in fact, many people won’t use a powerful AI like Arimidex or Letrozole during PCT at all, and instead go for a SERM drug with Nolvadex being a popular choice, alongside Clomid and often hCG as well.
The main reason for this is that Arimidex is very good at lowering estrogen, and Letrozole even more so. They are so powerful at this task that they can result in estrogen levels that are too low even for the male body.
This causes complications in the hormonal balance and will have a negative impact on your natural testosterone recovery; males still need a small amount of estrogen to keep things in balance, and since PCT is all about getting your natural hormone function back to normal, continuing with a high estrogen suppression drug like Letrozole or Arimidex after the steroid cycle can make this difficult, if not impossible.
Another issue when considering the use of Letrozole during PCT is that when it is combined with the staple PCT drug of choice for most people, Nolvadex, a negative interaction occurs where the concentrations of drugs counteract each other. This is also an issue when Arimidex is combined with Nolvadex.
This is another reason why combining either of these AIs with a SERM during PCT is not advisable at all – and since a SERM is basically essential for PCT, it will take priority over either Letrozole or Arimidex. Both of these AIs offer far more advantages when their use is limited to during your steroid cycle, where you can greatly benefit from their powerful anti-estrogen effects during that time.
Letrozole Side Effects
As with all types of drugs, the effects that each individual experiences will vary, and that means some people will be able to use Letrozole without a single side effect, while others might have one or more adverse reactions to the drug. The good news is that you have a good selection of other drugs available if Letrozole proves problematic for you.
The profile of possible side effects is comparable for Letrozole to that of the similar AI Arimidex. Fatigue, muscle aches, diarrhea, constipation, and chest pain are noted as specific side effects that Letrozole can experience, but this usually applies to women using it long-term as a cancer medication.
Most male steroid users who make use of Letrozole tolerate it well when it’s used at the recommended dosages. Many men will experience no noticeable side effects at all. Taking excessive doses of Letrozole provides an obvious increased risk of serious side effects.
Taking a closer look at some of the possible side effects of Letrozole can help you to be aware of any signs that you might need to lower your dose:
When the Letrozole dose is too high, we see a greatly increased risk of fatigue, and this comes about because estrogen levels are reduced too low – men still require some estrogen at low levels to function normally and because Letrozole is so powerful at reducing estrogen, taking too much can lower your levels beyond what is required for the central nervous system to operate normally – bringing on potentially chronic fatigue. This can be rectified efficiently and easily by reducing your Letrozole dosage until the fatigue subsides as estrogen rises slightly and remaining at the more appropriate dose from then on.
Pain in the Bones or Joints
This side effect is again a result of estrogen reduction going too far, which brings about a negative impact on bone mineral content, resulting in the associated pain. While long-term use of this drug has a serious risk of decreased bone strength, the short-term use that steroid users will make of Letrozole is unlikely to present the same risks. However, if you do experience joint or bone pain, it’s another sign that your Letrozole dose is too high. Lowering the dose should eliminate this side effect without any harm done.
A risk that comes with the use of any aromatase inhibitor is a negative impact on cholesterol levels, once again a significantly higher risk if your Letrozole dose is too high. In these cases, HDL can lower, and LDL can rise – the bad cholesterol increasing while the good cholesterol is minimized, exactly the opposite effect we need.
Estrogen has a beneficial effect on cholesterol, so once again, we want to maintain as low an effective dose of Letrozole as possible to minimize or eliminate this possible cholesterol-related side effect. Various studies on women using Letrozole for cancer treatment mostly show that no long-term impact on cholesterol is noted, so this does point to this drug being low risk in terms of adversely affecting your cholesterol health – the negative impacts on cholesterol from some anabolic steroids is of far greater concern.
Rebound of Estrogen
Unlike some other types of AIs, which are known as suicide or non-reversible aromatase inhibitors such as Aromasin, Letrozole is a non-suicidal AI. Therefore, once you stop using it, it’s possible to get a “rebound” in estrogen levels: the sudden halt of the drug’s estrogen reduction effect brings about a bounce in estrogen levels.
For this reason it is important to slower lower your dose of Letrozole rather than stopping it abruptly. Some people will choose to take a SERM like Nolvadex to provide extra protection during the end of a Letrozole dosage period and mitigate the effects of a possible estrogen rebound at this time.
Common Q&A Related to Letrozole
Does Letrozole cause fatigue?
Taking Letrozole at too high of a dosage will cause a noticeable onset of fatigue and a general lack of energy, something that no athlete or bodybuilder wants to experience. This is just one reason why it’s essential to stick to the lowest possible dose that still gives you the intended benefits without causing this or other side effects that will seriously hamper your performance and results and outweigh any benefit that Letrozole can provide you.
Can you drink alcohol while taking Letrozole?
Drinking alcohol while taking steroids (and even when not) is not something any serious bodybuilder or athlete wants to do as alcohol is a well-known performance decreaser, health hazard, liver stressor, and so many more negative things. Alcohol and medications are never a wise mix either, with interactions between the two being very possible.
When it comes to Letrozole, drinking alcohol alongside the use of the drug is known to increase the risk of headaches and nausea as both substances individually can cause these effects; when combined, these issues can become more pronounced.
Which is better, Clomid or Letrozole?
Clomid (clomiphene citrate) is another drug often used by steroid users. Unlike Letrozole, an aromatase inhibitor, Clomid is a selective estrogen receptor modulator (SERM). Both drugs are very effective, but they work differently, so one can not be said to be better than the other.
If you want an AI, Letrozole is possibly the best at controlling estrogen symptoms while you’re on a steroid cycle, while Clomid is a standard choice for PCT use. Letrozole effectively lowers overall estrogen, so it is excellent for water retention control and gyno, while Clomid specifically targets breast tissue.
For PCT usage, Clomid is considered a better choice because it does not suppress overall estrogen levels the way that Letrozole does, which provides a better hormonal balance for restoring your normal testosterone production after a steroid cycle. By comparison, Letrozole is generally considered too powerful as an estrogen-reduction drug to be a good choice for PCT.
Does Letrozole cause hair loss?
Some women who have used Letrozole for breast cancer treatment have experienced thinning of the hair – this is an expected effect on women whose estrogen levels have been drastically reduced by the drug. This is not known to be an issue for male steroid users who take Letrozole, and hair loss is a much larger concern with the steroids themselves, of which some can stimulate male pattern baldness because of an increase in dihydrotestosterone (DHT) as an androgenic side effect of steroid use.
What is the best time of day to take Letrozole?
There is no guide as to when steroid users should take Letrozole. For medical purposes, it is taken once a day, either morning or night. Whichever time you choose to take your daily dose, it should be taken at a regular time each day or every other day, depending on your preferred dose. So, you are maintaining a balanced level of the drug in your system for maximum estrogen control.
Letrozole has a half-life of two days, and many steroid users will find that taking it every second day is best not only for results but also to reduce possible side effects (especially fatigue) from this powerful aromatase inhibitor.
Does Letrozole increase cholesterol?
Most aromatase inhibitor drugs will pose some risk to cholesterol health, particularly lowering good cholesterol levels while raising bad cholesterol. This is partly because of the lowering of estrogen – a hormone that plays a role in maintaining cholesterol health. Taking too high of a dose of Letrozole brings about the highest risk of this happening, but most steroid users will only be using it at very low doses and for short periods of time.
Studies on the impacts of Letrozole on cholesterol have not been conclusive overall. One study found that cholesterol levels did rise after women used Letrozole for six months but returned to normal when the drug was stopped. Another study showed that women on Letrozole for several years did not show any effects at all on cholesterol.
My Conclusion and Recommendation
Letrozole is possibly the most powerful aromatase inhibitor for preventing gyno, and this should be your ultimate goal: to stop the condition from starting to develop at all while you’re using steroids. Prevention is better than cure when it comes to gyno, but if you do find that you’re starting to get those early signs, then Letrozole has sometimes stopped them and reversed them.
Fully developed gyno can’t be reversed by Letrozole or any other drug (only surgery), but it is a very effective AI overall for gyno and other estrogen-related effects. There are no known studies proving how effective Letrozole might be at reversing or improving gyno, unlike the SERM Nolvadex, which has been shown in studies to deliver very positive improvements to men with gyno.
If you enjoyed this guide and would like more real, NO-BS information on cycling steroids, then pick up Straight From the Underground (my recommended underground steroid handbook). Everything in this book is based on first-hand experience, not theory.