Why does it cause water retention if it doesn't aromatize?

Oxymetholone's 2-hydroxymethylene group provides direct ER agonist activity – it completely bypasses the CYP19 enzymes and activates estrogen receptors directly. So anti-aromatase (Anastrozole, Letrozole) is USELESS here; only SERM (Nolvadex, Raloxifene) blocks the ER receptors directly. This is the Anadrol-specific paradoxical effect.

Can you really gain 10-15 kg in 4 weeks?

Yes, BUT the vast majority (60-70%) is water and glycogen, NOT pure muscle. After cycle end, expect 30-50% weight loss within 2-3 weeks (water shedding). Pure lean mass preservation 4-6 kg documented with proper training and PCT. The "10-15 kg" number is realistic, but the final result is NOT that much.

Why FDA-approved if so toxic?

FDA-approved indication (aplastic anemia) is life-saving – risk-benefit ratio is favorable in those patients. Bodybuilding off-label use is NOT part of FDA approval; in healthy young people, 50-100 mg/day for 4 weeks can cause life-threatening hepatotoxicity (Pavlatos 2001 PMID 11329221 DILI case reports).

Anadrol vs Dianabol – which is worse?

Hepatotoxicity roughly equal (both top-2 among 17α-alkylated AAS). Aromatization profile: Dianabol classical CYP19-aromatizing (AI effective), Anadrol direct ER agonist (only SERM works). In bulking effect Anadrol is faster and more dramatic, but Dianabol preserves more muscle after the cycle ends. Neither is recommended.

Should I avoid Anadrol due to the "rage"?

Yes, the psychological side effects (aggression, irritation, fits of rage) are the most intense with Anadrol among AAS. Kanayama 2009 PMID 19922565 cohort: 70% of Anadrol users report marked mood disturbance. If psychiatric predisposition (depression, bipolar, anxiety disorder) is present, absolutely contraindicated.

EmergingResearch compound

Anadrol (Oxymetholone)

Oxymetholone, 2-hydroxymethylene-17α-methyl-DHT derivative oral AAS. FDA-approved (Anadrol-50) for aplastic and hypoplastic anemia. Classic "wet" bulking steroid; high hepatotoxicity and paradoxical estrogen-like side effects.

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DETAILED OVERVIEW

What is Anadrol (Oxymetholone)?

Anadrol (Oxymetholone) is a 2-hydroxymethylene-17α-methyl-DHT derivative oral AAS originally synthesized by Syntex in 1960. FDA-approved clinical indications: aplastic anemia, congenital and acquired red cell deficiency anemias (Anadrol-50, now Alaven/Meda Pharmaceuticals). Anabolic:androgenic ratio 320:45 (high anabolic, moderate androgenic). High hepatotoxicity due to 17α-methyl group (one of the highest among AAS). The 2-hydroxymethylene group is NOT a CYP19 substrate (does not aromatize), BUT shows direct ER agonist activity – paradoxical "estrogen-like" side effects (water retention, gynecomastia risk) appear even without aromatization. In bodybuilding context, a "wet" bulking steroid: 10-15 kg weight gain in 4-6 weeks (substantially water + glycogen) documented. WADA-banned year-round.

Mechanism

AR agonist + direct ER agonist (paradoxical)

Anabolic:Androgenic

320:45

Half-life

8-9 hours (oral)

Onset

1-2 h (oral)

Legal status

FDA Rx (Anadrol-50), Schedule III, WADA-banned

Data console

Lab data

Androgenic:Anabolic320:45
AR bindingHigh AR affinity + atypical ER activity (Pope-Kanayama 2014…
Active half-life~16 h (with active metabolites)
Detection windowOxymetholone metabolites urinary 6-8 weeks (WADA-accredited GC-MS and LC-MS/MS; Schänzer 1996 PMID 8616181).
AromatizationNot a CYP19 substrate – BUT due to direct ER agonist activity, estrogen-like side effects (water retention, gynecomastia) appear despite anti-aromatase treatment. Only protection: SERM (Nolvadex 20 mg/day or Raloxifene 60 mg/day) (Pope-Kanayama 2014 PMID 24423981)
HepatotoxicityVery high – 17α-methyl group extreme hepatic first-pass stress, ALT/AST 5-10x rise common, cholestatic jaundice case-reported. Among the highest hepatotoxicity AAS together with Dianabol and Superdrol (Hartgens-Kuipers 2004 PMID 15233599, Pavlatos 2001 PMID 11329221)

Safety

Side effects, stop signs, contraindications

Side effects · 8

Severe hepatotoxicity: as a 17α-alkylated oral, 5-10x ALT/AST elevation, cholestatic jaundice, rarely peliosis hepatis and liver tumors (adenoma, hepatocellular carcinoma) with prolonged use
Paradoxical estrogen-like effects without aromatization: direct ER-agonist activity causes water retention, edema, bloated face and gynecomastia; aromatase inhibitors are useless here, only a SERM protects
Drastic lipid worsening and raised blood pressure: HDL drop up to 60%, rising LDL, water-retention hypertension (often above 140/90), increasing cardiovascular risk
HPTA suppression: endogenous testosterone production shuts down, testicular atrophy, reduced libido and sperm count; recovery can take months, with prolonged hypogonadism without PCT
Polycythemia (erythrocytosis): the pronounced erythropoietic effect raises hematocrit and red cell count, increasing the risk of thrombosis, stroke and heart attack
Androgenic side effects: acne, increased sebum, androgenic hair thinning (in predisposed individuals), prostate enlargement in older men
Psychiatric effects: marked aggression ("Anadrol rage"), irritability, mood swings and depression; one of the most intense mood-disturbance profiles among AAS
Virilization in women: deepened voice, facial and body hair, clitoral enlargement, menstrual disruption – develops fast and often irreversibly due to high androgenic activity

Contraindications · 7

Any pre-existing liver disease or elevated baseline ALT/AST (fatty liver, hepatitis, cholestasis) – absolute contraindication due to the extreme hepatic stress of the 17α-alkylated structure
Pregnancy and breastfeeding: teratogenic, causes fetal virilization – absolute contraindication
Existing or suspected prostate or breast carcinoma, or male breast carcinoma – may drive progression of androgen-dependent tumors
Cardiovascular risk: existing hypertension, ischemic heart disease, dyslipidemia or positive family history – due to HDL crash, raised blood pressure and polycythemia
Polycythemia or elevated baseline hematocrit, or a history of thrombosis/stroke – the erythropoietic effect raises hematocrit further
Planned fatherhood / active fertility goals: HPTA suppression can depress sperm production for months to years
Concurrent hepatotoxic load: alcohol, paracetamol, NSAIDs, other 17α-alkylated oral AAS (Dianabol, Superdrol, Winstrol), or pre-existing psychiatric disorder (depression, bipolar, anxiety)

Related Performance Compounds

Same therapeutic category

Studies

Related research and clinical findings

DailyMed NDA 12-535 (oxymetholone label)

FDA Anadrol-50 prescribing information

FDA / Alaven-Meda Pharmaceuticals

Endocr Rev. 2014;35(3):341-75.

Adverse health consequences of performance-enhancing drugs: an Endocrine Society scientific statement

Pope HG Jr, Wood RI, Rogol A, Nyberg F, Bowers L, Bhasin S.

PMID: 24423981Open

Sports Med

Effects of androgenic-anabolic steroids in athletes.

Hartgens F, Kuipers H

PMID: 15248788Open

Cureus

Development of Liver Cancers as an Unexpected Consequence of Anabolic Androgenic Steroid Use.

Khalid S, Laput G, Khorfan K, Khan A, Goyal A

PMID: 36874750Open

Int J Mol Sci

Anabolic-Androgenic Steroids Revisited: Structural Biology, Receptor Signaling, and Mechanisms of Anabolic-Androgenic Dissociation.

Wiacek M, Zubrzycki IZ

PMID: 41898445Open

AIDS

Double-blind, randomized, placebo-controlled phase III trial of oxymetholone for the treatment of HIV wasting.

Hengge UR, Stocks K, Wiehler H, Faulkner S, Esser S, Lorenz R, Brockmeyer NH

PMID: 12646793Open

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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.