hormoneControlledSchedule III (US)Prescription only (US)Methyltestosterone is a Schedule III controlled substance in the US under the Anabolic Steroids Control ActFDA-approved combination esterified estrogen-methyltestosterone products have been used for menopausal symptoms, as studied in the cited trials
MethyltestosteroneBenefits, Dosage & Interactions
Methyltestosterone is a synthetic anabolic-androgenic steroid, a derivative of testosterone. It is an orally active form of testosterone that has been chemically altered to increase its bioavailability when taken by mouth. Research on Methyltestosterone focuses on testosterone support and muscle and strength.
Researched by DoseRoutine R&D TeamReviewed for accuracy by Nicholas Alexander, RSELast updated
Evidence: Strong — 1 human randomized trial and regulatory approval on file.
Evidence strengthStrong · 4/4
PreclinicalStrong human evidence
1 human randomized trial and regulatory approval on file.
Plasma half-life
Not established
Default unit
mg
What published protocols report
Ranges documented in the literature, shown for reference. DoseRoutine does not recommend an amount — your prescriber or the product label sets the dose.
Reported for Methyltestosterone in the cited sources. Published ranges are not dosing advice.
References & evidence
Documents the Methyltestosterone entry is written from. Each number matches an inline marker above.
- [1]Safety and efficacy of low-dose esterified estrogens and methyltestosterone, alone or combined, for the treatment of hot flashes in menopausal women: a randomized, double-blind, placebo-controlled studyLiu J, Allgood A, Derogatis LR, Swanson S, O'Mahony M, Nedoss B, Soper H, Zbella E, Prokofieva SV, Zipfel L, Guo CY · Fertility and Sterility · 2011 · Peer-reviewed · PMID 20850731
- [2]Liver function in postmenopausal women on estrogen-androgen hormone replacement therapy: a meta-analysis of eight clinical trialsGitlin N, Korner P, Yang HM · Menopause (New York, N.Y.) · 1999 · Peer-reviewed · PMID 10486791
How to track Methyltestosterone doses
Methyltestosterone is tracked as a protocol rather than a single reminder: a vial with a concentration, a schedule that may be titrated or cycled, and a rotation of injection sites. Here is the record that keeps all three consistent.
- 1
Record the vial and concentration
Log the vial strength and the volume of bacteriostatic water you added so Methyltestosterone is stored as a concentration rather than a guess. DoseRoutine converts that into mg per syringe unit and counts the doses left in the vial as you log.
- 2
Set the schedule, not just a reminder
Enter the dose in mg and the frequency. Cycled protocols get a start and end date so the history stays accurate when Methyltestosterone comes out of the routine.
- 3
Rotate and log the injection site
Pick the site at the moment you log the dose. The site map shows what you used last and how recently, which is the part that drifts fastest when two compounds run on different frequencies.
- 4
Log adherence, not intentions
Mark each dose taken, skipped or delayed as it happens. Weeks of honest logs are what make an adherence rate or a trend line meaningful; retrospective guessing is not.
- 5
Review against outcomes
Review Methyltestosterone alongside your logged metrics and any relevant blood work every few weeks before changing the dose, so the change is a response to data rather than to a good or bad day.
What to log each time
- Dose in mg and the syringe units it worked out to
- Vial: reconstitution date, concentration, doses remaining
- Injection site and time
- Any side effects in the 24 h after the dose
References & Evidence
Sources on this page that document Methyltestosterone dosing, timing and safety.
- [1]National Center for Biotechnology Information View source
Educational information only — not medical advice. Dose ranges vary by person, indication and prescriber.
What is Methyltestosterone studied for?
What is Methyltestosterone?Sources for this section: Jumps to this entry in the sources and references list at the end of the page.
Methyltestosterone is a synthetic anabolic-androgenic steroid, a derivative of testosterone. It is an orally active form of testosterone that has been chemically altered to increase its bioavailability when taken by mouth. It is classified as an androgen, a type of hormone that primarily influences the development and maintenance of male characteristics. In medicine, methyltestosterone has been used for testosterone replacement therapy in men with hypogonadism, delayed puberty in males, and in certain breast cancers in women. Due to its androgenic properties, it also carries the potential for masculinizing effects. (DrugBank)
What does the research say about Methyltestosterone?
Tap a section to expand.
Methyltestosterone exerts its effects by binding to and activating androgen receptors in target tissues throughout the body. Once bound, the activated receptor complex translocates to the cell nucleus, where it interacts with specific DNA sequences (androgen response elements). This interaction modulates the transcription of various genes, leading to changes in protein synthesis and cellular function. The activation of androgen receptors is responsible for the anabolic effects, such as increased protein synthesis and muscle growth, as well as the androgenic effects, which include the development and maintenance of male secondary sexual characteristics. Unlike natural testosterone, methyltestosterone is resistant to breakdown by the liver enzyme 17-beta-hydroxysteroid dehydrogenase, allowing it to remain active for a longer period in the body after oral administration. It is also less susceptible to aromatization (conversion to estrogen) compared to some other androgens, though it can still undergo some conversion. (DrugBank)
Source for this section: Sources for How does Methyltestosterone work?: Jumps to this entry in the sources and references list at the end of the page.
Methyltestosterone has several established medical uses:
* **Male Hypogonadism:** It is used as a testosterone replacement therapy for men who have a deficiency or absence of endogenous testosterone, helping to restore normal testosterone levels, improve libido, energy, and mood. (MedlinePlus)
* **Delayed Puberty in Males:** In specific cases, it can be prescribed to induce puberty in adolescent males with significantly delayed pubertal development. (MedlinePlus)
* **Metastatic Breast Cancer in Women:** Historically, methyltestosterone was used as a palliative treatment for certain advanced, inoperable breast cancers in postmenopausal women. Its mechanism in this context typically involves downregulating estrogen receptor expression or antagonizing estrogen's effects. (FDA Label)
Individuals seeking to use methyltestosterone for muscle gain or performance enhancement typically do so due to its anabolic properties, which promote protein synthesis and increase muscle mass and strength. However, such off-label use is associated with significant health risks and is generally not medically recommended. (NIH ODS)
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
The use of methyltestosterone for testosterone replacement therapy, delayed puberty, and certain breast cancers is well-documented in medical literature and supported by clinical experience. For instance, studies have demonstrated its efficacy in raising serum testosterone levels and improving symptoms associated with hypogonadism. Its approval by regulatory bodies like the FDA in the United States attests to its established medical utility for these indications when prescribed and monitored by a healthcare professional. (FDA Label)
However, evidence regarding its long-term safety and efficacy outside of controlled medical settings, particularly for performance enhancement, is limited and often overshadowed by concerns related to adverse effects. The anabolic properties are known, but the risk-benefit ratio for non-medical use is generally considered unfavorable. Cochrane reviews have examined testosterone therapy in general for various conditions, finding benefits in specific contexts but also emphasizing the importance of individualized assessment and monitoring. (Cochrane)
Methyltestosterone can cause a range of side effects, due to its potent hormonal activity. Common side effects include:
* Fluid retention (edema)
* Nausea, vomiting
* Headache
* Changes in libido
* Acne
* Hair loss (male pattern baldness)
* Oily skin
* Gynaecomastia (breast enlargement in males)
* Frequent or persistent erections
More serious side effects can also occur:
* **Liver damage:** Methyltestosterone is associated with liver toxicity, including cholestatic hepatitis and, in rare cases, liver cell tumors (hepatic neoplasms) or peliosis hepatis (blood-filled cysts in the liver). Regular liver function monitoring is crucial. (FDA Label)
* **Cardiovascular issues:** Increased risk of heart attack, stroke, and blood clots, particularly in older men or those with pre-existing cardiovascular disease. (FDA Label)
* **Effects on blood lipids:** Can negatively impact cholesterol levels, decreasing HDL ('good') cholesterol and increasing LDL ('bad') cholesterol. (MedlinePlus)
* **Polycythemia:** Increased red blood cell count, which can thicken the blood and increase the risk of blood clots. (MedlinePlus)
* **Psychiatric effects:** Mood changes, aggression, depression, or anxiety. (NIH ODS)
* **Prostate effects:** Can worsen benign prostatic hyperplasia (BPH) symptoms and may accelerate the growth of existing prostate cancer. (FDA Label)
* **Virilization in women:** Deepening of the voice, hirsutism (excessive hair growth), clitoral enlargement, and menstrual irregularities. These effects may be irreversible. (FDA Label)
* **Premature epiphyseal closure in adolescents:** Can stunt growth in children and adolescents by causing premature fusion of bone growth plates. (FDA Label)
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Methyltestosterone should be used with extreme caution and under strict medical supervision. Key warnings include:
* **Liver Toxicity:** Due to the risk of severe liver damage, including life-threatening conditions like peliosis hepatis and hepatic neoplasms, liver function tests must be monitored regularly. Symptoms of liver problems, such as persistent nausea, fatigue, dark urine, or yellowing of the skin/eyes, require immediate medical attention. (FDA Label)
* **Cardiovascular Risk:** Concerns exist regarding increased risks of cardiovascular events, including myocardial infarction (heart attack) and stroke, especially in men treated with testosterone therapies. Patients with pre-existing cardiovascular conditions should be carefully evaluated. (FDA Label)
* **Thromboembolic Events:** There is an increased risk of venous thromboembolism (blood clots), including deep vein thrombosis (DVT) and pulmonary embolism (PE). (FDA Label)
* **Prostate:** Testosterone therapy can stimulate the growth of prostate tissue. Men should undergo prostate cancer screening (PSA and DRE) before starting treatment and periodically thereafter. It is contraindicated in men with known or suspected prostate cancer. (FDA Label)
* **Breast Cancer in Men:** Cases of male breast cancer have been reported, although rare. (FDA Label)
* **Sleep Apnea:** Pre-existing sleep apnea may be exacerbated by testosterone therapy. (MedlinePlus)
* **Fluid Retention:** Can cause or worsen edema, particularly in patients with cardiac, renal, or hepatic disease. (FDA Label)
* **Abuse Potential:** Methyltestosterone is a controlled substance due to its potential for abuse, particularly by athletes and bodybuilders seeking performance enhancement. Abuse can lead to serious adverse effects across multiple organ systems and psychological dependence. (NIH ODS)
* **Pediatric Use:** Use in children and adolescents can lead to premature closure of the epiphyses, resulting in stunted growth. Careful monitoring of bone maturation is required. (FDA Label)
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Methyltestosterone is contraindicated in several conditions due to the risk of severe adverse effects:
* **Men with Carcinoma of the Breast or Prostate:** Androgens can stimulate the growth of prostate cancer and are generally contraindicated in men with known or suspected prostate or breast cancer. (FDA Label)
* **Women who are Pregnant or May Become Pregnant:** Methyltestosterone can cause masculinization of a female fetus. It is classified as an FDA Pregnancy Category X. (FDA Label)
* **Patients with Severe Cardiac, Renal, or Hepatic Disease:** Due to the potential for fluid retention and exacerbation of existing conditions. (FDA Label)
* **Hypersensitivity:** Individuals with a known hypersensitivity to methyltestosterone or any of its components. (FDA Label)
* **Breastfeeding Women:** Due to potential adverse effects on the infant. (FDA Label)
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Combining methyltestosterone with certain medications or substances can lead to dangerous interactions:
* **Anticoagulants (Blood Thinners):** Methyltestosterone can enhance the anticoagulant effect of warfarin and similar drugs, increasing the risk of bleeding. Dosage adjustments of anticoagulants may be necessary, and close monitoring of INR/PT is essential. (FDA Label)
* **Corticosteroids (e.g., Prednisone):** Concomitant use with corticosteroids can increase the risk of edema (fluid retention). This interaction is particularly relevant for individuals with pre-existing cardiac, hepatic, or renal conditions. (FDA Label)
* **Insulin and Oral Hypoglycemics:** Methyltestosterone may decrease blood glucose levels, potentially leading to hypoglycemia when used with insulin or oral antidiabetic agents. Diabetic patients should have their blood glucose monitored closely, and adjustments to antidiabetic medication doses may be required. (FDA Label)
* **Thyroid Hormones:** While less common, there can be interactions impacting thyroid function tests. (FDA Label)
* **Other Anabolic Steroids or Hormones:** Combining with other anabolic-androgenic steroids or supra-physiological doses of hormones can significantly amplify side effects, including liver toxicity, cardiovascular risks, and psychiatric effects, without necessarily providing additional therapeutic benefit. This practice is strongly discouraged due to the heightened risk profile. (NIH ODS)
* **Alcohol:** Heavy alcohol consumption, especially alongside methyltestosterone, can further increase the risk of liver damage due to the hepatotoxic nature of both substances. (MedlinePlus)
Before taking methyltestosterone, patients should inform their healthcare provider about all prescription drugs, over-the-counter medications, and herbal supplements they are currently using. (MedlinePlus)
This is educational information, not medical advice - consult a qualified clinician before starting, stopping or combining any compound.
Methyltestosterone is typically taken orally. The specific timing of administration (e.g., with or without food) and frequency (e.g., once or multiple times daily) will be directed by a licensed clinician. The compound generally has a half-life of approximately 4 hours, meaning it requires regular dosing to maintain consistent levels. It can typically be taken either with or without food, but specific instructions from a prescriber should always be followed. (DrugBank)
Source for this section: Sources for When should you take Methyltestosterone?: Jumps to this entry in the sources and references list at the end of the page.
What interacts with Methyltestosterone?
| Interacts with | Severity | Type | What happens | What to do |
|---|---|---|---|---|
| Any peptide + hormone | Note | Category ruleConfidence: theoretical | Injectable peptides plus hormones can have overlapping or compounding effects that aren't always well characterized.Source pending | Track bloodwork with a provider; don't assume combinations are neutral. |
Frequently asked questions about Methyltestosterone
Methyltestosterone is a hormone. What follows is drawn from peer-reviewed literature indexed on PubMed, FDA label text where a label exists, and NIH reference records.
Methyltestosterone is commonly discussed in the context of supporting testosterone and muscle. Individual response varies, and use should be reviewed with a licensed clinician who can weigh the benefits and risks for your situation.
For Methyltestosterone, it is typically taken null. Always follow the specific dose your clinician or the product label prescribes.
Methyltestosterone carries potential side effects and drug interactions, documented in NIH, Mayo Clinic, and FDA label sources. Methyltestosterone is classified as a controlled substance in some jurisdictions, so legal status and prescribing rules apply. Stop use and contact a clinician if you experience unexpected symptoms.
Methyltestosterone is a hormone, and interactions are possible with prescriptions, hormones, peptides and other supplements in the same routine. Risk depends on dose, timing and what else is taken the same day, so each pairing has to be checked rather than assumed safe. The free checker at https://doseroutine.com/interaction-checker covers Methyltestosterone with no sign-up.
Combining a hormone like Methyltestosterone with TRT is usually a question of labs rather than a blanket yes or no: the ester, injection interval and any aromatase inhibitor all change the answer. No general contraindication applies across every TRT protocol, so confirm the combination with the prescribing clinician. See the free TRT interaction reference: https://doseroutine.com/trt-supplement-interactions
Each peptide class carries its own profile against Methyltestosterone: a healing peptide raises different questions than a GLP-1 agonist or a growth-hormone secretagogue. Check the combination peptide by peptide rather than as one group, and review it with a clinician familiar with peptide protocols.
Published frequency for Methyltestosterone varies by protocol and formulation, so the label or prescription is what sets it. Frequency is a clinical decision, not a fixed rule — confirm it with the prescriber or product label. Comparison of apps that keep a schedule like this: https://doseroutine.com/best-dose-tracking-apps
The effect of a missed dose of Methyltestosterone depends on the protocol and formulation you are on. Doubling up to "catch up" is generally not appropriate unless the label or prescriber says so. Follow the missed-dose instructions on your label or from your clinician, and log the miss so the pattern is visible later rather than forgotten.
For Methyltestosterone the useful record is the dose, the time it was actually taken, and what else was taken in the same window. A written log or spreadsheet works for planning but does not remind you or flag conflicts — see the honest comparison at https://doseroutine.com/vs/spreadsheet and the wider roundup at https://doseroutine.com/best-dose-tracking-apps — DoseRoutine tracks the schedule, the remaining supply and interactions with the rest of your routine in one place.
Sources cited on this page
Specific documents referenced by the numbered markers above. Each number matches the marker in the text.
- PubChem CID 6010(opens in a new tab)National Center for Biotechnology Information · pubchem.ncbi.nlm.nih.gov/compound/6010
Verify at
Publisher search links for Methyltestosterone. These are places to check the information — they are not citations, so they are not numbered.
- Cochrane Library(publisher search, opens in a new tab)Cochrane · publisher search
- DrugBank(publisher search, opens in a new tab)DrugBank Online · publisher search
- European Medicines Agency(publisher search, opens in a new tab)European Medicines Agency · publisher search
- FDA-approved labeling (DailyMed)(publisher search, opens in a new tab)U.S. Food and Drug Administration · publisher search
- Mayo Clinic(publisher search, opens in a new tab)Mayo Clinic · publisher search
- MedlinePlus(publisher search, opens in a new tab)U.S. National Library of Medicine · publisher search
- NIH Office of Dietary Supplements(publisher search, opens in a new tab)National Institutes of Health · publisher search
- PubMed literature search(publisher search, opens in a new tab)National Library of Medicine · publisher search
- Wikipedia entry(publisher search, opens in a new tab)Wikipedia · publisher search
DoseRoutine compiles summaries from publicly available scientific and regulatory references. Always verify important decisions with a licensed clinician. How we source and review this information.
What is the short answer on Methyltestosterone?
Plain-text summary, safe to quote verbatim:
Methyltestosterone is a synthetic anabolic-androgenic steroid, a derivative of testosterone. It is an orally active form of testosterone that has been chemically altered to increase its bioavailability when taken by mouth. Research on Methyltestosterone focuses on testosterone support and muscle and strength.
Source: DoseRoutine — https://doseroutine.com/library/methyltestosterone
Cite this page
Using this in an article, AI answer, or research note? Please attribute:
DoseRoutine. (2026). Methyltestosterone — Overview, Benefits & Side Effects. Retrieved from https://doseroutine.com/library/methyltestosterone
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