Superdrol

Superdrol (methasterone; 2-alpha,17-alpha-dimethyl-5-alpha-androstan-17-beta-ol-3-one) is a synthetic, orally active anabolic-androgenic steroid (AAS) of the 5-alpha-dihydrotestosterone (DHT) structural class. The compound was first synthesized by researchers at Syntex Corporation in 1956 and characterized in a 1959 publication as a potent orally active anabolic agent exhibiting only weak androgenic activity. Despite this favorable preclinical dissociation profile, methasterone was never advanced to clinical development or marketed as a prescription pharmaceutical. The compound resurfaced in 2005 when it was introduced to the United States consumer market under the trade name Superdrol, sold as an over-the-counter dietary supplement and marketed deceptively as a prohormone to circumvent the Anabolic Steroid Control Act of 1990. In preclinical rat bioassays using methyltestosterone as the reference standard, methasterone demonstrated approximately 400 percent anabolic potency and 20 percent androgenic potency, yielding a Q-ratio (anabolic-to-androgenic dissociation index) of 20, among the highest reported for any oral AAS. The compound's oral bioavailability (approximately 50 percent) is conferred by the 17-alpha-methyl group, which protects the steroid nucleus from hepatic first-pass metabolism but simultaneously renders the compound hepatotoxic through a mechanism common to all C17-alpha-alkylated androgens. Methasterone is non-aromatizable owing to its 5-alpha-reduced A-ring saturation, and therefore does not produce estrogenic effects such as gynecomastia or water retention. Hepatotoxicity is the principal and most serious adverse effect: a distinctive pattern of bland cholestatic liver injury, characterized by severe hyperbilirubinemia with only modest aminotransferase elevation, has been documented in multiple case series and case reports. A comprehensive literature review of 52 reported cases identified a median presentation bilirubin of 314 micromol/L, peak bilirubin of 705 micromol/L occurring approximately 28 days after cessation, and resolution over a median of 90 days with supportive care alone; no deaths or liver transplantations were reported in the published literature. Acute kidney injury occurred in 43 percent of cases, with peak creatinine correlating with peak bilirubin. The World Anti-Doping Agency placed methasterone on its prohibited list in 2006. The United States Drug Enforcement Administration classified methasterone as a Schedule III controlled substance in January 2012 under the Controlled Substances Act, and the Designer Anabolic Steroid Control Act of 2014 further expanded regulatory authority over designer steroids of this class. Methasterone has no approved medical indication in any jurisdiction. This monograph documents the complete chemistry, synthesis, pharmacology, pharmacokinetics, hepatotoxicity profile, clinical case evidence, sourcing considerations, handling, combination interactions, adverse event signal, and a comparative assessment against five alternative oral anabolic-androgenic steroids (oxandrolone, oxymetholone, stanozolol, methyltestosterone, and epistane) on five competency standards.