Methyltestosterone is a classic anabolic steroid, an old-school drug that is effective for increasing muscle mass and enhancing athletic performance.
Although most people are unfamiliar with this compound, it has actually been widely used.
Methyltestosterone is the first synthetic version of testosterone and the first oral steroid, a unique drug created through C17-alpha alkylation.
In 1937, the first esterified version, Testosterone Propionate, was released and achieved commercial success thanks to its delayed absorption effect.
Methyltestosterone was an early form of the oral testosterone hormone. Ciba’s Metandren was a famous sublingual formulation that increased bioavailability, but it is no longer found on the market today.

Today, Methyltestosterone is primarily used in medical and hormone replacement therapy, prescribed for treating low testosterone levels or andropause.
Due to side effects like high estrogenic activity and hepatotoxicity, most athletes seek better alternatives.
Characteristics and Qualities of Methyltestosterone
The effects of Methyltestosterone are particularly potent because the saturation rate of androgens in the bloodstream is a key catalyst.
By rapidly increasing the body’s androgen levels, its effects can be felt quickly, and it’s used to improve low levels or treat related issues.
Immediately after use, libido increases, and motivation and energy are restored.
This is also why it is favored by people suffering from menopause or andropause.
For enhancing athletic performance, it is not recommended due to its high toxicity.
Most methylated compounds are highly toxic and should not be used for performance enhancement purposes.
Furthermore, its high estrogen content makes other alternatives more suitable.
It is not preferred because high-dose, long-term use is required.
While it can be effective for increasing muscle mass in athletes, the androgenic effects of Methyltestosterone are particularly strong, leading to a significant increase in aggression and focus.
This can be advantageous in fields like combat sports and can also be beneficial for strength athletes.
Aggression can be either a positive or a negative, depending on the user’s goals.
While its mental benefits can be helpful in a competitive environment, there are better options due to its strong estrogenic effects.
Individuals with violent tendencies or a lack of self-control should avoid taking it; it is only recommended for those who can manage the aggression.
Side Effects of Methyltestosterone
While testosterone is a drug with very low side effects for most men, it’s important to note that Methyltestosterone, in particular, has several troublesome side effects that make it harder to recommend compared to other forms of testosterone.

Estrogenic Side Effects
Regarding estrogenic side effects, Methyltestosterone is highly likely to cause bloating.
When it binds to aromatase receptors, side effects such as gynecomastia, bloating, and increased mood swings can occur.
As a methylated compound, Methyltestosterone converts to methylestradiol, making its aromatization effects even more pronounced.
Therefore, it is crucial to be prepared for these side effects by having an Aromatase Inhibitor (AI) or a SERM on hand.
Cholesterol levels must also be monitored, and if they become uncontrollable, the use of an AI may be necessary.
While all forms of testosterone can cause similar issues, the methylated nature of Methyltestosterone makes the potential for side effects especially high.
Androgenic Side Effects
Like most forms of testosterone, androgenic side effects are present.
When testosterone converts to DHT, symptoms like acne or baldness can occur, and it can accelerate the rate of male pattern baldness in those who are predisposed.
Similar to its estrogenic side effects, the potency of this compound can make androgenic side effects more pronounced.
Taking a 5-alpha reductase inhibitor like Finasteride can slow the progression of baldness, but there is no guarantee it will stop it completely.
Methyltestosterone Side Effects in Women
Due to these androgenic effects, women should not use Methyltestosterone unless it is in extremely low doses under the supervision of a medical professional.
The risk of virilization is too high, and its use for performance purposes is not recommended.
If symptoms of virilization appear, such as clitoral enlargement, a deepening voice, hair growth, estrogen imbalance, or an increase in masculine features, use must be discontinued immediately.
Cardiovascular Side Effects
Cardiovascular side effects can include an increase in bad cholesterol, where an AI can be helpful.
Increased water retention can lead to a rise in blood pressure, so it must be managed carefully.
HDL levels can be suppressed, but using an AI to control estrogen can help mitigate this issue.
Maintaining a healthy diet and lifestyle can reduce the risk of cardiovascular disease, but failure to do so can increase the risk.
Testosterone Suppression Side Effects
The use of an exogenous hormone like Methyltestosterone can suppress endogenous testosterone production, so a Post Cycle Therapy (PCT) plan must be in place.
PCT is necessary to help restore endogenous hormone production and normalize estrogen levels.
Men with normal testosterone levels will likely need a PCT after using Methyltestosterone.
Women or men with low testosterone levels will not require a PCT.
Hepatotoxicity
This drug is highly hepatotoxic and can cause organ damage.
Since the liver regenerates slowly, liver health must be a top priority. Enzyme levels should be monitored, and alcohol consumption should be minimized to avoid putting strain on the liver.
Methyltestosterone Dosage and Administration
Methyltestosterone packs a very powerful punch.
To enhance aggression and athletic performance with Methyltestosterone, a dose of 40-50mg for no more than 8 weeks is recommended.
In a therapeutic setting, a dose of 10-40mg is often sufficient to see most of the benefits.
In most cases, the starting dose is higher and is tapered down over time until it reaches the 10mg level.
For women using Methyltestosterone, the dosage must be kept very low.
It should not exceed 2.5mg, and even that can be too much for many women.
When women are prescribed or choose to use Methyltestosterone, it is often administered alongside an estrogen tablet.
Conclusion
Overall, this is a very potent drug that not only offers therapeutic benefits but also enhances mental fortitude, focus, and aggression.
However, due to its estrogenic and hepatotoxic effects, Methyltestosterone ranks a bit lower among preferred forms of testosterone.
If you are looking for a great form of testosterone, there are many other testosterone products to choose from besides Methyltestosterone.
| Chemical Name | 17alpha-methyl-4-androstene-3-one,17b-ol |
| Molecular Weight | 302.4558 |
| Formula | C20 H30 O2 |
| Melting Point | 162-167 |
| Manufacturer | Major pharmaceutical companies |
| Effective Dose | (Men) 25-100mg/day |
| Active Life | 6-8 hours |
| Detection Time | 4-6 weeks |
| Anabolic/Androgenic Ratio (Range) | 94-130/115-150 |



