Clinical ResearchResearch compound

Superdrol

Methasterone (2α,17α-dimethyl DHT derivative). Two market formats: oral 17α-methylated tablet with extreme hepatotoxicity, and underground in-oil injectable with reduced (but NOT eliminated) hepatic stress.

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Superdrol vial

WHAT IS SUPERDROL?

Detailed overview

Superdrol (chemically Methasterone, 2α,17α-dimethyl-17β-hydroxy-5α-androstan-3-one) was originally synthesized in 1956. Designer Supplements LLC marketed the oral form as a dietary supplement in 2005; the FDA classified it as a Schedule III controlled substance in 2012 (DASCA) and pulled it from the supplement market. An injectable variant later appeared on the underground market – methyldrostanolone dissolved in oil (NOT esterified) – which bypasses hepatic first-pass and lowers hepatic stress, but the 17α-methyl group means hepatotoxicity is NOT fully eliminated. Strong AR agonist (anabolic 400, androgenic 20 vs. testosterone reference); the 2α,17α-dimethyl structure means it does NOT aromatize in either form.

Mechanism

AR agonist (anabolic 400 / androgenic 20)

Anabolic ratio

400:20

Legal status

USA: Schedule III (2012 DASCA). EU: controlled, illegal without prescription.

Data console

Lab data

/lab/molecular-data.jsonLIVE
> Androgenic:Anabolic400:20
> AR bindingStrong AR agonist, ~5× stronger binding than testosterone i…
> Active half-life6-8 h
> Detection window4-6 hét vizelet (metilezett metabolitok: 17α-metil-5α-androsztán-3α-ol-17β-on, WADA-akkreditált laborban).
> Aromatizationnone
> Hepatotoxicityvery-high

Safety

Side effects, stop signs, contraindications

Side effects · 8

  • Severe hepatotoxicity (oral form): the 17α-methyl group causes cholestatic liver injury, ALT/AST elevation of 3-5x, documented jaundice and hepatocellular injury cases in healthy young men (Singh 2009, Shah 2008).
  • Cholestasis: bile acid accumulation in hepatocytes, with skin itching and dark urine as warning signs; reduced but NOT zero risk with the injectable form, since the 17α-methyl group remains hepatotoxic even via IM route.
  • Drastic lipid deterioration: HDL can crash by over 30% and LDL rises, posing an acute cardiovascular risk; this effect is identical for both the oral and injectable forms.
  • Strong hypertension: significant blood pressure rises are common, so daily blood pressure monitoring is mandatory; systolic >150 mmHg warrants stopping the cycle.
  • HPTA suppression: as a potent AR agonist it rapidly shuts down endogenous testosterone production (LH/FSH drop), so PCT (Clomid + Nolvadex) is mandatory; low libido and fatigue follow the cycle.
  • "Superdrol flu": loss of appetite, nausea, headache, low energy and lethargy, especially above 20 mg/day; more pronounced with the oral form.
  • Androgenic effects: can trigger acne, increased sebum, temporal hair thinning and male-pattern baldness in predisposed users; risk of virilization (voice deepening, hair growth) in women.
  • Injectable-specific: methyldrostanolone in-oil is notoriously painful (injection-site irritation, PIP), plus risk of abscess and infection without aseptic technique.

Contraindications · 7

  • Any pre-existing liver disease or elevated baseline liver enzymes (fatty liver, hepatitis, elevated ALT/AST): absolute contraindication due to the hepatotoxicity of the 17α-methyl group, for both forms.
  • Cardiovascular risk (family history, high LDL, existing hypertension, known heart disease): absolute contraindication due to severe HDL crash and blood pressure elevation.
  • Concurrent hepatotoxic agents: alcohol, NSAIDs, paracetamol and statin therapy are strictly forbidden; these cause cumulative liver injury with Superdrol.
  • Concurrent use of other 17α-alkylated oral AAS (Dianabol, Anadrol, Winstrol): extreme, potentially life-threatening hepatotoxicity, so combination is forbidden.
  • Women, especially during pregnancy or breastfeeding: contraindicated due to risk of virilization and fetal harm (teratogenicity).
  • Kidney disease or existing renal impairment: the Nasr 2009 case report (PMID 18720005) documented Methasterone-induced cholestatic jaundice and acute kidney injury (AKI).
  • Adolescents and young adults with open epiphyseal plates: the androgenic effect can cause premature bone maturation and permanent stunting of growth.

Related Performance Compounds

Same therapeutic category

Studies

Related research and clinical findings

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MolekulaX Editorial Team·Source-verified · PubMed · FDA · EMA
Updated: June 19, 2026

The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.