Methasterone (Superdrol)

Methasterone, commonly known as Superdrol (or methyldrostanolone), is a powerful synthetic oral anabolic–androgenic steroid (AAS). Chemically, it is a 2α,17α-dimethylated derivative of dihydrotestosterone (DHT). In practice it was never a prescribed medicine; instead, it surfaced as a “designer steroid” sold briefly as a dietary supplement. Superdrol is renowned for its extreme anabolic potency and equally severe side-effect profile. It is much stronger for building lean mass and strength than many orals, but it places heavy strain on the liver and hormonal system.

Structure and Classification: Methasterone is a C₂₁H₃₄O₂ steroid, derived from DHT (5α-androstan-17β-ol-3-one) with two added methyl groups (at C2 and C17). The 17α-methylation allows it to survive oral ingestion but also makes it hepatotoxic. It is classified as a synthetic 17α-alkylated androgen/anabolic steroid (AAS).

Mechanism of Action: Like all AAS, methasterone binds to androgen receptors in muscle and other tissues, activating anabolic (muscle-building) and androgenic (masculinizing) effects. Its modifications give it exceptionally high anabolic potency while reducing traditional androgenic effects. In laboratory assays it was found to be about 4× as anabolic as methyltestosterone but only ~20% as androgenic, yielding an unusually high anabolic-to-androgenic ratio (roughly 20:1).

Methylation and Metabolism: The 17α-methyl group protects methasterone from rapid liver breakdown, making it effective by mouth. However, this methylation also concentrates toxic metabolites in the liver. It is metabolized hepatically and excreted in urine. Because it is a DHT derivative, methasterone does not convert to estrogen (i.e. it does not aromatize) or carry estrogenic side effects.

Pharmacokinetics: Methasterone is orally active, with an estimated bioavailability around 50%. Its elimination half-life is short, on the order of 8–12 hours. This means it is usually taken once or twice daily to maintain stable blood levels. Peak blood levels occur within several hours of an oral dose. The short half-life contributes to the need for daily dosing and quick ramp-up/clearance from the body.

Discovery and Development: Methasterone was first synthesized in the 1950s by Syntex Corporation. Early reports (1959) noted it was an orally active anabolic agent with strong growth-promoting effects and relatively weak androgenic (male hormone) activity. However, Syntex never marketed it as a drug. Instead, the related compound drostanolone propionate (Masteron) was sold for medical use (e.g. breast cancer). Methasterone itself was set aside and remained largely dormant for decades.

“Designer Steroid” Emergence: In the mid-2000s methasterone reappeared in gyms and supplement markets under the brand name Superdrol. A company called Designer Supplements LLC effectively marketed it as a legal bodybuilding prohormone (supposedly a dietary supplement). It had not been scheduled under earlier steroid laws, so it was briefly sold over the counter in the U.S. (2005–2006) as “Methasterone” or “Superdrol”. This was done by exploiting loopholes in the Anabolic Steroid Control Acts (1990/2004), which listed specific banned compounds.

Regulatory Crackdown: As its popularity and reported adverse effects grew, the U.S. Food and Drug Administration (FDA) issued warnings and took action to remove it from the supplement market. By about 2006–2012 methasterone was classified as a controlled anabolic steroid (Schedule III in the U.S.), making it illegal to sell without a license. Similar bans followed worldwide, and it is now considered a black-market steroid. Methasterone has no approved medical use in any country. Its entire history beyond early research revolves around its use and abuse as a performance drug.

Muscle Mass and Strength: Methasterone is prized for its ability to induce rapid gains in lean muscle size and raw strength. Bodybuilders and athletes who have used it typically report very large increases in muscle mass in a short time frame (e.g. 8–12+ pounds of muscle in a month-long cycle under optimal conditions). These gains tend to be very “hard” or dense, with minimal fluid or fat gain, due to its non-estrogenic nature. Strength often shoots up quickly, allowing heavier lifts in a few weeks. Because of these effects, Superdrol became popular as an oral “bulking” agent, often used by experienced lifters to jump-start a cycle or break through plateaus.

Body Composition: Unlike some other powerful orals (Dianabol or Anadrol) which cause pronounced water retention and bloating, methasterone produces lean gains. Users often note muscle hardness, vascularity, and a tight, pumped appearance rather than a puffy one. Any fat loss during a methasterone cycle is usually secondary to the increase in basal metabolic rate from added muscle and possibly appetite changes; it is not a fat-burning steroid per se. However, because it does not aromatize, it avoids estrogen-related water weight, so the added mass is mostly real muscle tissue.

Comparison with Other Orals: Methasterone is sometimes compared to other popular oral AAS:

Dianabol (Methandrostenolone): Both offer rapid mass and strength gains, but Dianabol causes significant water retention and can puff up the face, whereas methasterone delivers similar muscle gains in a dryer manner. Dianabol’s estrogenic side effects (bloat, gynecomastia) are absent with Superdrol. Methasterone is generally considered stronger pound-for-pound, though users can often handle Dianabol’s dose more easily because of lower liver stress.

Anadrol (Oxymetholone): Anadrol produces very large weight and strength gains, but much of that weight is water or glycogen. Anadrol also raises blood pressure dramatically. Superdrol rivals Anadrol for muscle-building but with much less visible fluid retention. Anadrol may cause more immediate strength surges, but Superdrol’s gains are similarly extreme (and some find Superdrol gives a more solid “lean” look).

Winstrol (Stanozolol): Winstrol is another non-aromatizing oral, prized for cutting or prepping physiques (very lean gains, lots of hardness). Superdrol is like a much stronger Winstrol: it also gives a dry, vascular appearance but yields faster and bigger muscle growth. Winstrol is milder and less toxic, often used for finishing cycles. Superdrol is usually used in bulking or cycle-bridging contexts.
In summary, methasterone occupies a role as one of the most potent oral AAS for gaining pure lean mass and strength. It delivers more impressive mass gains than Winstrol or Anavar, and gets similar “hard” gains without water that Anadrol/Dianabol produce, though with a higher cost in toxicity. Many users cycle it alongside longer-acting injectables (like testosterone) to maximize growth while mitigating extreme dosing of orals alone.

Muscle Gains and Pumps: Users almost universally report very quick, noticeable muscle growth when taking Superdrol. Even in short cycles (4–6 weeks), gains of 8–15 pounds of lean body mass are often cited (assuming adequate diet and training). A common description is a sudden jump in muscle fullness and vascular pumps during workouts, as muscles swell rapidly with growth. Many say their muscles feel rock-hard and denser, as the drug promotes nitrogen retention and protein synthesis intensely.

Strength and Energy: Along with size, users typically experience sharp strength improvements. Workouts feel more intense, and maximal lifts can rise week to week. Some report feeling unusually powerful in the gym. That said, because methasterone is not a stimulant, users do not get a hyper-caffeinated boost; instead, their performance jumps thanks to the drug’s anabolic effect on muscles. Early in a cycle, users often feel highly motivated and “aggressive” in training.

Fatigue and Lethargy: Methasterone is known to be taxing on the body. Many users note that by 3–4 weeks into a cycle, fatigue can set in. This manifests as feeling more tired than usual, needing extra rest, or lacking stamina during workouts (despite being stronger). The lethargy is thought to come from the strain on the liver, imbalanced hormones, and depletion of natural energy. Some compare it to “hitting a wall” after initial great gains if not managed with adequate nutrition and supplements. Proper on-cycle support (sleep, diet, health supplements) is often recommended to combat this slump.

Libido and Hormones: As an androgenic steroid, methasterone can influence sex drive. Anecdotally, some users report a short-term increase in libido while on cycle (common with many androgens). Others notice little change or even a slight decrease during the cycle. In all cases, after the cycle ends, libido typically falls due to suppressed testosterone production (hypogonadism from steroid use). Full sexual function usually returns after good post-cycle therapy (PCT) with SERMs (like tamoxifen or clomiphene) to restart natural hormones.

Psychological Effects: Methasterone can cause noticeable mood changes. Many users feel more confident, aggressive, or irritable while on it (the so-called “roid rage” phenomenon is mentioned by some, though it is variable). Insomnia and restlessness are reported by a few, likely due to increased cortisol or simply overstimulation of the nervous system. Mood swings or feelings of anxiety can occur, especially in heavy doses. After a cycle, feelings of depression or general malaise are not uncommon if hormone levels drop sharply. Good PCT and psychological preparation are advised. Generally, users describe methasterone as intense – it amplifies focus and drive in training but can also exacerbate stress or aggression in some personalities.

Liver Toxicity: By far the most serious concern with methasterone is its effect on the liver. The 17α-methyl group that makes it orally active also makes it highly hepatotoxic. In real cases, users have experienced cholestatic jaundice (blockage of bile flow), severe elevations in liver enzymes, and even acute liver failure. Methasterone is often listed among the most liver-stressing AAS. Symptoms of liver strain can include jaundice (yellowing of skin/eyes), dark urine, fatigue, nausea, and abdominal pain. Because of this, methasterone should never be run for long or without liver support. Periodic blood tests of liver enzymes (ALT, AST) are strongly recommended if it is used at all. The drug can also cause gallbladder sludging or stones in sensitive people.

Cardiovascular Strain: Like most oral anabolic steroids, Superdrol negatively affects cholesterol and blood pressure. It tends to drastically lower HDL (“good” cholesterol) and raise LDL (“bad” cholesterol), which increases the risk of atherosclerosis and heart disease if used repeatedly. Many users see their cholesterol profiles worsen significantly even in a short cycle. Methasterone also tends to raise blood pressure through direct fluid retention and vascular changes. Users may experience headaches or swelling from high blood pressure. Long-term or high-dose use could contribute to left ventricular hypertrophy (heart muscle thickening) and increased risk of heart attack or stroke. Cardiovascular side effects often depend on dose and duration, but even single cycles can leave noticeable effects on heart health markers.

Hormonal Suppression: Methasterone powerfully suppresses the hypothalamic–pituitary–gonadal axis. This means natural testosterone production drops sharply during the cycle. As a result, testicular shrinkage (atrophy) is common. This also causes sex hormone imbalances: estrogen and dihydrotestosterone (DHT) drop too. Upon stopping, the body can take weeks or months to recover, during which symptoms of low testosterone (fatigue, low libido, loss of muscle) occur unless proper post-cycle therapy is used. PCT usually involves drugs like tamoxifen to stimulate the testes to restart testosterone production. Without PCT, users risk significant loss of gains and prolonged hormone-related side effects.

Gynecomastia Risk: Because methasterone cannot be converted into estrogen, the classic estrogen-driven gynecomastia is unlikely from Superdrol itself. However, gynecomastia can sometimes appear indirectly. This may occur if the body produces breast tissue in response to a progesterone-like effect (methasterone has some progestogenic activity) or from liver dysfunction causing fluid shifts. In practice, full-blown gynecomastia from methasterone alone is rare, but if it is stacked with other aromatizing steroids (like testosterone or Dianabol) without an aromatase inhibitor, risk is elevated. Users concerned about breast growth should still watch for early signs (tender lumps) and have anti-estrogen drugs on hand.

Androgenic Effects: Methasterone has moderate androgenic side effects. This can include acne (especially on the back or shoulders), oily skin, and accelerated male-pattern baldness in those predisposed. Though it is less androgenic than testosterone, it is still derived from DHT and can cause hair loss or scalp acne. Women taking it (very risky and rare) would notice deepening of the voice, increased body hair, and menstrual irregularities.

Neurological/Psychiatric Symptoms: Some users report anxiety, irritability, or depressive moods associated with methasterone use (and especially withdrawal). While not directly neurotoxic, the hormonal upheaval can affect the brain. Insomnia or trouble sleeping is occasionally mentioned. There is no direct evidence it damages nerves or brain cells, but psychological side effects from AAS are well known. “Roid rage” (out-of-control anger) is more myth than reality for most, but some individuals do experience heightened aggression. More commonly, mood swings and a slight edge of irritability are noted.

Other Effects: Additional side effects have been reported anecdotally. Some users experience nausea or gastrointestinal discomfort (as with any strong oral). There have been rare reports of kidney strain or failure (often tied to dehydration and extreme body stress). Joint pain is sometimes mentioned, possibly because methasterone has little water-retaining effect on joints, leading to stiffness. Vision changes or insomnia can occur, although these are more commonly linked to other orals (like anecdotally Winstrol eye issues). Any severe or unexpected symptoms (dark urine, severe abdominal pain, swelling) should prompt immediate medical attention.

Dosage Range: Because of its potency, methasterone is dosed much lower than many other orals. Beginners generally start at 10–20 mg per day. Some sources even recommend starting as low as 5–10 mg/day to assess tolerance. Experienced users might use 20–30 mg/day, but higher doses (40+ mg) greatly increase risk without proportionally more benefit. Going above 50 mg/day is generally considered dangerous. Even at 10–20 mg, liver strain is significant.

Cycle Length: Cycles are kept short to minimize toxicity. A typical Superdrol cycle is 3–6 weeks. Many lifters do 4 weeks on, then stop. Some might push to 6 weeks if tolerance is good, but it is uncommon to exceed 6 weeks. Longer use is strongly discouraged due to escalating liver and heart risks. Users often take breaks of months between cycles to allow recovery.

Administration: Methasterone is usually taken once daily due to its ~8–12 hour half-life. To improve absorption and reduce nausea, it is best taken with food. There is no need to taper off; it can be stopped abruptly at the end of a cycle.

Stacking: Superdrol is frequently stacked with a testosterone base (e.g. injectable test 250–500 mg/week) to maintain normal androgen levels and support gains. This also means the user is using an androgen anyway, which can reduce shock to the system from shutdown. It can also be stacked with milder orals or insulins in advanced regimens, but stacking multiple liver-toxic orals is ill-advised. Many athletes prefer to run Superdrol solo or just with testosterone to avoid compounding the toxicity. It is not uncommon to use a low dose of an anabolic steroid (like Anavar or Winstrol) simultaneously, but this should only be done by very experienced users with careful monitoring.

On-Cycle Support: Because of liver and cholesterol effects, on-cycle supplements are recommended: e.g. a good liver support (milk thistle or TUDCA), a heart health supplement (fish oil/krill oil for HDL support), and staying hydrated. Alcohol and acetaminophen (Tylenol) should be strictly avoided.

Post-Cycle Therapy (PCT): A proper PCT is essential after a methasterone cycle. Typical PCT might involve a SERM like tamoxifen (Nolvadex) at 20–40 mg/day for 3–4 weeks, starting 3–4 days after the last dose of Superdrol. Clomiphene (Clomid) can also be used. The goal is to kick-start the testes to produce testosterone again. Without PCT, users risk extended low testosterone and loss of gains. Natural test boosters (e.g. DHEA, zinc, vitamin D) and adaptogens (ashwagandha, etc.) are sometimes used to support recovery.

Monitoring: Ideally, users would check blood panels before, during, and after a cycle: liver enzymes (AST/ALT), lipid profile, and hormone levels (testosterone, estrogen, liver function). This helps gauge the toll and plan timing of cycles. At the very least, periodic physical check-ups are prudent for heavy AAS users.

United States: Methasterone is classified as a Schedule III controlled substance under the Controlled Substances Act (as of 2012). This means it is illegal to manufacture, buy, or possess without a prescription (which is essentially impossible, as it has no accepted medical use). It was famously unscheduled until mid-2000s, allowing it to be sold as a “supplement”, but now any use in the U.S. is illicit.

United Kingdom: In the UK, methasterone (and all anabolic steroids) are Class C substances under the Misuse of Drugs Act. Personal possession of small quantities is not a serious offense, but importing, supplying or manufacturing them without a license is illegal. In practice, Superdrol has never had medical approval in the UK, so any sale or import is unlawful.

European Union: As a potent anabolic steroid, Superdrol is not a licensed medicine in EU countries. It is effectively banned; sales as dietary supplements are illegal under EU cosmetics and food regulations. European sports authorities ban it (see WADA below). Enforcement varies by country, but in general it is treated the same as other anabolic steroids (requiring prescriptions if any, which don’t exist).

Canada: Anabolic steroids (including methasterone) are Schedule IV drugs under Canadian law. They are available only by prescription for very limited medical conditions (none of which include methasterone). Any non-medical possession or trafficking is illegal in Canada. Recreational use is essentially criminalized.

Australia: Methasterone is a regulated drug in Australia. It likely falls under Schedule 4 (prescription) or even a banned import category. Importation of anabolic steroids for personal use is generally illegal without proper permits. Australia follows WADA guidelines as well, so use in sport is prohibited.

World Anti-Doping Agency (WADA): Methasterone is on WADA’s Prohibited List as an anabolic androgenic steroid. It is banned at all times in competition for athletes. Major sports bodies (IOC, NCAA, NFL, etc.) do random testing and will sanction any athlete testing positive for Superdrol. In practice, any use by a competing athlete risks disqualification, bans, and loss of sponsorships.

Other Sports and Organizations: All international and national athletic federations adhere to WADA rules. Military and law enforcement in many countries also ban steroid use. Even where personal possession might not be heavily punished, any competitive advantage use is strictly forbidden.

Historical Note: Methasterone’s appearance as a supplement led to legal reforms. In the U.S., its existence spurred broader laws to catch “designer steroids” by chemical class rather than name. By the late 2000s all major sporting organizations and most governments recognized it as an illicit AAS.

Methasterone (Superdrol) is one of the most potent oral anabolic steroids ever encountered. Its benefits are clear for those seeking rapid, lean muscle and strength gains without water weight: users can see dramatic size and power improvements in just a few weeks. However, these effects come at a steep price. Methasterone is extremely toxic to the liver and imposes serious cardiovascular and hormonal strains even on short cycles. Side effects include liver damage (jaundice, enzyme spikes), disastrous cholesterol changes, blood pressure elevation, and complete shutdown of natural testosterone, among others. Unlike milder orals (like Anavar) it cannot be taken casually or for extended periods; even a single cycle must be approached with caution.

In the spectrum of oral AAS, methasterone stands out as a “heavy hitter.” It produces more lean gains and strength than most other orals (outperforming many on a per-milligram basis), and without the water retention of Dianabol or Anadrol. But it also has a harsher side-effect profile, often compared to Winstrol’s dryness but far more toxic. Its role is typically as a short, intense bulking agent for experienced athletes rather than a beginner’s supplement.

For those considering methasterone, harm-reduction is critical. Recommended practice includes using only the lowest effective dose (often 10–20 mg/day), limiting cycles to 3–4 weeks, and spacing them out by months. Relying on liver support supplements (e.g. milk thistle, TUDCA) and a proper post-cycle regimen (tamoxifen or clomiphene) can help mitigate damage. Alcohol and other liver stressors should be avoided entirely. Comprehensive medical monitoring (blood tests for liver and lipid markers) is advisable, as is having realistic awareness of the legal risks.

In summary, methasterone can deliver extraordinary rapid results, but it also embodies many of the worst risks of anabolic steroids, especially the older, 17α-alkylated orals. Its use should be reserved for those fully aware of the hazards, under proper guidance if possible. Among oral AAS, it is potent and efficient, but also among the most dangerous – underscoring why caution, respect for dosage limits, and medical oversight are imperative for anyone who chooses to use it.