Description

Oxymetholone

Executive Summary

Oxymetholone is an orally active, 17α-alkylated anabolic-androgenic steroid historically marketed as Anadrol for anemias caused by deficient red-cell production. In current U.S. labeling, its approved indication remains limited to specific marrow-failure and hypoproliferative anemia settings, not general bodybuilding or athletic enhancement. Its clinical value lies mainly in stimulating erythropoiesis and improving nitrogen balance, but its risk profile includes cholestatic liver injury, dyslipidemia, edema, endocrine suppression, and androgenic adverse effects. (Drugs.com, 2025; PubChem, 2026).

From a pharmacology standpoint, oxymetholone is a synthetic 5α-androstan derivative with a 17α-methyl substitution that preserves oral activity by reducing first-pass inactivation. It acts primarily through androgen receptor signaling and hematopoietic stimulation, including increased erythropoietin production and downstream erythropoiesis. However, modern, high-quality pharmacokinetic data remain surprisingly limited: current U.S. labeling does not specify a formal elimination half-life, and small older studies remain the main source for plasma pharmacokinetic characterization. (Drugs.com, 2025; Cardoso et al., 2002; Bond et al., 2022).

Clinically, oxymetholone has been used for acquired aplastic anemia, congenital aplastic anemia, myelofibrosis, and hypoplastic anemias related to myelotoxic drugs. More recent reviews and cohort studies suggest androgens still retain a role in selected bone-marrow-failure syndromes when transplant, immunosuppressive therapy, or newer options are unavailable, contraindicated, or inaccessible. That said, modern hematology practice generally favors safer and more effective alternatives whenever possible. (Drugs.com, 2025; Nassani et al., 2023; Chaipokam et al., 2025).

For sports and anti-doping purposes, oxymetholone is prohibited by WADA under S1 anabolic agents, and modern laboratories detect it through urine-metabolite analysis using techniques such as GC-MS/MS, GC-Orbitrap-HRMS, and LC-MS/MS. Detection windows depend heavily on assay design, target metabolite panels, dose, and duration of exposure; some controlled studies show short windows for particular metabolites, whereas long-term-metabolite research continues to improve retrospective detection. (WADA, 2026; Backer et al., 2025; Zheng et al., 2025).

Oxymetholone 50mg 100 Tabs Geno Pharma Best USA
Oxymetholone 50mg 100 Tabs Geno Pharma Best USA

Oxymetholone Overview

Featured snippet answer: Oxymetholone is an oral anabolic-androgenic steroid approved in the United States for certain anemias caused by reduced red-blood-cell production. It is the active ingredient in Anadrol and works mainly by enhancing erythropoiesis and improving nitrogen balance, but it carries clinically important hepatic, cardiovascular, endocrine, and androgenic risks.

Oxymetholone is the generic drug nameAnadrol or Anadrol-50 is a brand name for the same active ingredient. The current professional prescribing information identifies Anadrol-50 as oxymetholone 50 mg oral tablets, a CIII controlled substance in the United States. In practical terms, “oxymetholone” and “Anadrol” are pharmacologically the same drug; the distinction is generic versus branded product identity. (Drugs.com, 2025).

Oxymetholone belongs to the broader class of androgens and anabolic steroids. Like other oral 17α-alkylated agents, it was engineered for oral bioavailability, but that same structural modification is one reason oral anabolic steroids as a class are associated with greater hepatotoxic potential than many injectable testosterone esters. This class-level risk is reflected in boxed warnings about peliosis hepatis, liver tumors, and adverse lipid changes in current labeling. (Drugs.com, 2025; Petrovic et al., 2022).

In nonmedical settings, oxymetholone is often discussed for rapid weight gain and strength increases. Those outcomes are real enough to make the drug attractive for misuse, but they do not make the drug safe or medically appropriate for physique enhancement. U.S. federal labeling explicitly states that anabolic steroids have not been shown to enhance athletic ability, and federal public-health sources continue to warn that anabolic steroids can contribute to cardiovascular disease, psychiatric harm, liver injury, reproductive dysfunction, and dependence-like patterns of use. (Drugs.com, 2025; DEA, 2024; NIDA, 2026).

Chemical Profile

The chemical profile of oxymetholone helps explain four important clinical realities: its oral activity, rapid anabolic effects, marrow-stimulating properties, and unusually high toxicity signal for a therapeutic androgen. It is a synthetic steroid derived from the 5α-androstan backbone rather than the classic testosterone backbone. Compared with testosterone-dominant agents, that structural shift alters receptor behavior, metabolism, and side-effect pattern. (PubChem, 2026; Pavlatos et al., 2001).

PropertyOxymetholone data
Generic nameOxymetholone
Common U.S. brandAnadrol / Anadrol-50
Chemical name17β-hydroxy-2-(hydroxymethylene)-17-methyl-5α-androstan-3-one
Drug classAndrogen; anabolic steroid
Structural class17α-alkylated, 5α-androstan derivative
Molecular formulaC21H32O3
Molecular weight332.48 g/mol
CAS number434-07-1
PubChem CID5281034
UNIIL76T0ZCA8K
ATC codeA14AA05
RouteOral
U.S. control statusSchedule III

Source note: Data synthesized from PubChem, KEGG, FDA/Drugs.com labeling, and U.S. regulatory sources.

Image

Caption: Oxymetholone chemical structure schematic.

Oxymetholone Chemical Profile

Simplified structural overview of oxymetholone and the chemical modifications
responsible for its oral activity and anabolic properties.

Oxymetholone
C21H32O3
Molecular Weight: 332.48 g/mol
Steroid Ring A

Ring B

Ring C

Ring D
Four fused rings form the characteristic anabolic steroid nucleus.

3-Keto Group

A carbonyl group located on the first steroid ring that contributes to
androgen-receptor interaction and biological activity.


17β-Hydroxyl Group

A hydroxyl group at carbon 17 associated with the compound’s anabolic
and androgenic activity.


17α-Methyl Group

This alkyl modification protects oxymetholone from rapid hepatic
breakdown and allows effective oral administration.


2-Hydroxymethylene Group

A distinctive structural modification that differentiates oxymetholone
from many other dihydrotestosterone-derived anabolic steroids.

Chemical Name:
17β-hydroxy-2-(hydroxymethylene)-17-methyl-5α-androstan-3-one
Clinical relevance:
The 17α-methyl modification improves oral bioavailability but also increases
hepatic exposure and contributes to oxymetholone’s hepatotoxic potential.

Chemical Profile and Mechanism

Featured snippet answer: Oxymetholone works mainly by activating androgen-responsive pathways and stimulating erythropoiesis. At the cellular level it promotes anabolic gene transcription, supports positive nitrogen balance, and increases erythropoietin-driven red-cell production. These effects can improve anemia and body mass, but they also help explain edema, endocrine suppression, lipid changes, and hepatic stress.

Oxymetholone’s clinical pharmacology starts with a core fact: it is an androgen receptor agonist. Like other anabolic-androgenic steroids, it enters target tissues, binds intracellular androgen receptors, and changes gene transcription after the receptor complex moves into the nucleus. That genomic response underlies increased protein handling, altered nitrogen balance, and multiple systemic endocrine effects. (Bond et al., 2022; KEGG, 2026).

Current labeling also highlights an additional mechanism that is unusually important for oxymetholone: it enhances the production and urinary excretion of erythropoietin in patients with bone-marrow failure and frequently stimulates erythropoiesis in anemias due to deficient red-cell production. That marrow-directed hematologic effect is the main reason oxymetholone retained a medical role long after many other oral anabolic steroids were abandoned. (Drugs.com, 2025).

Mechanism of Action at the Cellular Level

At the cellular level, oxymetholone’s effects can be understood through several overlapping pathways rather than a single mechanism:

Androgen Receptor Signaling

After oral absorption and systemic distribution, oxymetholone diffuses into androgen-sensitive tissues such as skeletal muscle, bone marrow, liver, skin, and reproductive tissues. Inside the cell it binds the androgen receptor, displaces inhibitory chaperone proteins, and facilitates translocation of the ligand-receptor complex into the nucleus. There, the complex interacts with androgen response elements and alters transcription of genes involved in protein turnover, erythropoiesis, and tissue maintenance. (Bond et al., 2022; KEGG, 2026).

Erythropoiesis and Bone Marrow Effects

In clinical hematology, the most relevant effect is stimulation of erythropoiesis. Current labeling attributes this to increased erythropoietin production/excretion and enhanced red-cell production. Experimental work in Fanconi-anemia models suggests oxymetholone may also alter marrow signaling pathways affecting hematopoietic stem and progenitor-cell cycling, including suppression of osteopontin transcription. Those mechanistic insights help explain why androgens can still rescue counts in some marrow-failure syndromes even when the exact molecular pathway is not completely mapped. (Drugs.com, 2025; Zhang et al., 2015).

Protein Economy and Nitrogen Balance

Anabolic steroids improve nitrogen balance when calorie and protein intake are adequate. In practical terms, oxymetholone promotes an anabolic milieu in which protein synthesis and tissue retention exceed breakdown. That is partly why weight gain can occur relatively quickly in both therapeutic and nonmedical settings. However, labeling also notes that the precise clinical meaning of “positive nitrogen balance” has not been fully established in terms of actual protein-building outcomes in every context. (Drugs.com, 2025).

Endocrine Feedback Suppression

Oxymetholone, like other anabolic steroids, suppresses the gonadotropic functions of the pituitary and may exert direct testicular effects. This explains why prolonged exposure can reduce endogenous testosterone production, impair spermatogenesis, and contribute to oligospermia, testicular atrophy, infertility, and sexual dysfunction. In modern endocrine reviews, this phenomenon is described as anabolic-steroid-induced hypogonadism. (Drugs.com, 2025; Nieschlag & Vorona, 2015).

Cardiometabolic and Hepatic Stress Pathways

The same anabolic steroid signaling that yields therapeutic or performance-related effects also perturbs hepatic bile handling, lipid metabolism, vascular function, coagulation, and myocardial remodeling. Recent reviews describe oxidative stress, mitochondrial dysfunction, endothelial injury, fibrosis, and prothrombotic changes as part of the broader pathophysiology of anabolic-steroid toxicity. Oxymetholone should therefore be viewed as a multisystem endocrine-active drug, not simply a “muscle” agent. (Petrovic et al., 2022; Fadah et al., 2023; Borowiec et al., 2025).

Image Asset

Caption: Oxymetholone mechanism of action at the cellular level.

 

How Oxymetholone Works in the Body

Simplified mechanism of action showing oral absorption, anabolic signaling,
red blood cell production, endocrine suppression, and major health risks.

1. Oral Oxymetholone Ingestion
2. Gastrointestinal Absorption
3. Systemic Circulation

Anabolic and Muscle Pathway

Oxymetholone enters androgen-sensitive tissues and binds to intracellular
androgen receptors. The hormone-receptor complex then moves into the cell
nucleus and activates androgen-responsive genes.

Androgen receptor binding

Nuclear gene transcription

Improved nitrogen balance

Protein retention and anabolic signaling

Weight gain and lean-mass support

Red Blood Cell Production

Oxymetholone may increase erythropoietin-related activity and stimulate the
bone marrow, resulting in greater red blood cell and hemoglobin production.

Kidney and bone marrow signaling

Increased erythropoietin activity

Enhanced erythropoiesis

Higher hemoglobin and red blood cell production

Liver Exposure and Hepatotoxicity

Because oxymetholone is an orally active 17-alpha-alkylated anabolic steroid,
it places substantial metabolic stress on the liver.

Hepatic metabolism

Increased liver exposure

Risk of cholestasis, jaundice, liver injury, and other hepatic complications

Cardiovascular and Lipid Effects

Lipid and vascular effects

Lower HDL cholesterol

Higher LDL cholesterol

Fluid retention and possible blood pressure elevation

Increased cardiovascular risk

Endocrine Suppression

Pituitary-gonadal suppression

Reduced LH and FSH signaling

Lower endogenous testosterone production

Potential hypogonadism, infertility, and testicular effects

Summary: Oxymetholone produces anabolic and hematologic
effects through androgen receptor activation and stimulation of red blood
cell production. However, the same systemic exposure may also cause liver
toxicity, adverse cholesterol changes, fluid retention, cardiovascular
stress, and suppression of natural hormone production.

Clinical Pharmacology and Pharmacokinetics

Featured snippet answer: Oxymetholone is an oral 17α-alkylated anabolic steroid with clinically meaningful oral availability, hepatic metabolism, and urinary excretion. Unlike many modern drugs, its current FDA labeling does not provide a detailed pharmacokinetic section, so accessible primary data are limited and some commonly quoted half-life values remain secondary estimates rather than label-confirmed facts.

Modern clinicians should know that oxymetholone’s pharmacokinetic literature is thin relative to its age. The FDA’s 2024 draft bioequivalence guidance confirms that plasma oxymetholone is measurable after a single oral 50 mg dose and that regulatory bioequivalence work still depends on in vivo pharmacokinetic endpoints. Yet the currently available U.S. prescribing information does not provide a detailed contemporary PK table with Tmax, elimination half-life, volume of distribution, or a formal protein-binding percentage. (FDA, 2024; Drugs.com, 2025).

Absorption

Oxymetholone is orally administered and remains pharmacologically active after oral dosing because its 17α-alkylated structure slows first-pass metabolic inactivation. This is the core medicinal-chemistry reason it became a viable tablet rather than an injection-only androgen. Small older studies confirmed measurable plasma concentrations after oral 50 mg administration in healthy volunteers, but accessible modern detailed absorption parameters remain sparse. (FDA, 2024; Cardoso et al., 2002; Bond et al., 2022).

Time to Peak Concentration

A precise Tmax is not specified in current U.S. labeling. Older pharmacokinetic work demonstrates that oral administration produces quantifiable plasma levels suitable for PK modeling, and secondary clinical monographs commonly describe peak concentrations within hours rather than days. Because contemporary accessible primary PK datasets are limited, the safest evidence-based phrasing is that oxymetholone reaches measurable plasma exposure within a short oral timeframe, but the exact current label-supported Tmax is unspecified. (Cardoso et al., 2002; FDA, 2024; Drugs.com, 2025).

Metabolism

Oxymetholone undergoes hepatic metabolism. The importance of the liver for both activation/clearance and toxicity is reinforced by class-wide warnings for 17α-alkylated androgens, by current package-insert recommendations for periodic liver-function monitoring, and by modern liver-injury reviews showing cholestatic, peliosis-associated, and neoplastic complications with anabolic steroids. Metabolic profiling studies in anti-doping science further demonstrate multiple urinary metabolites and conjugated species relevant to testing. (Drugs.com, 2025; Petrovic et al., 2022; Backer et al., 2025).

Elimination and Excretion

Both current labeling and older pharmacokinetic literature support urinary excretion of oxymetholone metabolites. That urinary elimination is why anti-doping programs rely on urine metabolite identification rather than parent-drug detection alone. The FDA draft guidance also specifies measuring oxymetholone in plasma in bioequivalence studies, reinforcing that clinically and analytically relevant systemic exposure occurs after oral dosing. (FDA, 2024; Drugs.com, 2025).

Protein Binding

Precise modern label-based total protein-binding percentages are not available. Older receptor-binding literature and secondary summaries suggest low affinity for sex hormone-binding globulin relative to testosterone and DHT, but this should be treated as a qualitative pharmacologic point rather than a fully standardized contemporary PK parameter. For clinical writing, it is more accurate to say that circulating protein binding is incompletely characterized in current labeling. (Saartok et al., 1984; Pavlatos et al., 2001).

Half-Life and Detection Windows

The current U.S. package insert does not state an elimination half-life. Commonly repeated non-label estimates place oxymetholone in a roughly 8–9 hour range, but those values are secondary and should be reported cautiously. In anti-doping literature, metabolite detection windows are highly assay-dependent: older long-term-metabolite work notes that some polyhydroxylated metabolites were traceable only for a few days, while newer HRMS studies identified novel glucuronide metabolites detectable several days after dosing and continue to expand retrospective detection capabilities. (Drugs.com, 2025; Kratena et al., 2019; Zheng et al., 2025; Backer et al., 2025).

Pharmacokinetic Summary

Pharmacokinetic propertyBest-supported current interpretation
Route of administrationOral
Oral activityHigh enough for therapeutic tablet use because of 17α-alkylation
Time to peak plasma concentrationUnspecified in current U.S. labeling; older PK literature confirms short oral absorption phase
Elimination half-lifeUnspecified in current U.S. labeling; secondary sources often cite ~8–9 h, but certainty is limited
Major site of metabolismLiver
Primary route of excretionUrine
Protein bindingExact percentage unspecified; literature suggests relatively low SHBG affinity
Bioequivalence analyteOxymetholone in plasma
Detection testingUrinary metabolite analysis using GC-MS/MS, GC-Orbitrap-HRMS, and LC-MS/MS workflows
Detection windowAssay-dependent; some metabolites only several days, but advanced long-term-metabolite methods extend retrospectivity

Source note: This table intentionally distinguishes label-confirmed data from secondary estimates to avoid overstating certainty.

Image Asset

Caption: Oxymetholone pharmacokinetic and detection timeline.

Oxymetholone Pharmacokinetic Timeline

Simplified timeline of oxymetholone administration, absorption, systemic activity, metabolism, excretion, and detection.


Immediately After Dose

Oral administration

Within Hours

Gastrointestinal absorption

Within Hours

Measurable plasma exposure

Short Term

Systemic anabolic and hematologic signaling

Same Day Onward

Hepatic metabolism

Same Day Onward

Urinary excretion of metabolites

Several Days

Conventional urine metabolite detection in some studies

Longer, Assay-Dependent Period

Extended retrospectivity with modern long-term-metabolite methods

 

Medical Uses, Benefits, and Dosage

Featured snippet answer: Medically, oxymetholone is used for anemias caused by deficient red-cell production, especially selected marrow-failure syndromes. Its main clinical benefit is support of erythropoiesis and hemoglobin recovery. Outside medical supervision, however, the same drug is misused for rapid mass and strength gain despite major risks and no approved performance-enhancing indication.

Medical Uses

Current U.S. prescribing information states that oxymetholone is indicated for anemias caused by deficient red-cell production, and specifically names acquired aplastic anemia, congenital aplastic anemia, myelofibrosis, and hypoplastic anemias due to myelotoxic drugs as conditions that often respond. The same labeling also stresses that oxymetholone should not replace supportive measures such as transfusion, vitamin correction, antimicrobial therapy, or corticosteroid use when otherwise indicated. (Drugs.com, 2025).

Contemporary hematology reviews confirm that androgens remain a selective fallback or bridge option in acquired and inherited bone-marrow-failure syndromes when modern first-line therapies are unavailable, infeasible, or contraindicated. A 2025 adult aplastic-anemia cohort reported an overall response rate of 56.4% with oxymetholone monotherapy in a setting where transplant and horse ATG were not broadly accessible, illustrating that the drug retains clinical relevance under constrained-resource conditions. That is not the same as first-choice therapy in modern U.S. practice. (Nassani et al., 2023; Chaipokam et al., 2025; Pagliuca et al., 2024).

Clinical Benefits

The principal legitimate therapeutic benefit is hematologic. Oxymetholone can increase erythropoietin signaling, stimulate erythropoiesis, reduce transfusion dependence in responders, and improve hemoglobin and energy in selected marrow-failure patients. These benefits are most meaningful when the patient is being followed by hematology and when efficacy is weighed against liver, lipid, endocrine, and long-term oncologic risk. (Drugs.com, 2025; Chaipokam et al., 2025).

A secondary clinical effect is improved nitrogen balance, which may help support body mass in catabolic or debilitated states. Historically this contributed to off-label investigation in conditions such as HIV wasting, but that does not translate into broad current approval for wasting syndromes. Modern practice has largely moved toward safer and more targeted strategies. (Drugs.com, 2025; Pavlatos et al., 2001; Hengge et al., 2003).

Nonmedical and Bodybuilding Benefits

In bodybuilding and image-enhancement settings, oxymetholone is misused because it can produce rapid increases in scale weight, training output, and apparent fullness, effects likely driven by a mix of anabolic signaling, glycogen-related tissue fullness, fluid retention, and red-cell effects. Those are descriptive observations, not medical recommendations, and they must be interpreted alongside substantial risk of dyslipidemia, liver injury, blood-pressure elevation, endocrine suppression, and anti-doping sanctions. (Bond et al., 2022; DEA, 2024; NIDA, 2026).

Medical disclaimer: This article does not recommend oxymetholone for physique or performance enhancement, does not provide nonmedical protocols, and does not endorse unsupervised use. The same properties that make oxymetholone potent also make it medically hazardous.

Dosage

Medical Dosing

Current U.S. prescribing information gives a recommended daily dose of 1–5 mg/kg/day in children and adults, with the usual effective dose 1–2 mg/kg/day. The dose should be individualized, and the label emphasizes that response is often delayed, so a minimum trial of three to six months is recommended. Following remission, some patients may discontinue therapy while others require lower maintenance dosing; continued maintenance is commonly necessary in congenital aplastic anemia. (Drugs.com, 2025).

For Fanconi anemia and other inherited marrow-failure syndromes, specialist literature describes individualized, weight-based dosing under expert supervision, but protocols vary by disease context, age, and toxicity tolerance. Because evidence is retrospective, heterogeneous, and condition-specific, this article does not present a single universal off-label dosing schedule beyond the cited sources. (Medicine.com, 2020; Nassani et al., 2023).

Nonmedical Use Discussion

Nonmedical oxymetholone use is common in performance-enhancement subcultures, but current medical, public-health, and anti-doping standards treat that use as unsafe and non-approved. For that reason, this report intentionally avoids publishing informal “cycles,” stacking instructions, or physique-oriented dosing schemes. The medically important point is that misuse often involves supratherapeutic exposure and therefore disproportionately increases hepatic, cardiovascular, reproductive, psychiatric, and legal risk. (NIDA, 2026; DEA, 2024; WADA, 2026).

Adverse Effects and Monitoring

Featured snippet answer: Oxymetholone’s side effects are clinically significant and multisystem. The major risk domains are hepatotoxicity, dyslipidemia and cardiovascular strain, edema, endocrine suppression, virilization, infertility, mood changes, and pediatric growth toxicity. Safe use requires close medical monitoring, and nonmedical use sharply increases the probability of serious harm.

Liver Toxicity

Oxymetholone carries one of the clearest hepatotoxicity signals in anabolic-steroid therapeutics. Current professional labeling warns about cholestatic hepatitis, jaundice, peliosis hepatis, liver failure, hepatic necrosis, and liver cell tumors, and recommends periodic liver-function monitoring. The broader anabolic-steroid liver literature confirms that 17α-alkylated oral steroids are particularly associated with bland cholestasis, vascular lesions such as peliosis, and in rare cases neoplasia. (Drugs.com, 2025; Petrovic et al., 2022).

In the package insert, liver-related harm appears at multiple levels: boxed warnings, precautions, laboratory monitoring language, and the adverse-reactions section. Labeling also notes that women given carcinogenicity-range exposures in animal studies developed higher rates of certain neoplastic findings, while human reports include rare hepatocellular carcinoma after long-term, high-dose androgen therapy. That does not prove a uniform cancer risk in every patient, but it justifies very cautious use. (Drugs.com, 2025).

Cardiovascular and Hematologic Effects

Oxymetholone can worsen cardiovascular risk through several pathways: decreased HDL, increased LDL, edema, elevated vascular strain, possible hypertension, and changes in coagulation-related markers. Package labeling and recent cardiovascular reviews consistently frame anabolic steroids as an atherogenic and potentially cardiomyopathic exposure class, particularly at supraphysiologic doses. (Drugs.com, 2025; Fadah et al., 2023; Borowiec et al., 2025).

For patients on therapy, hemoglobin and hematocrit deserve attention not only because oxymetholone may improve anemia, but also because excessive erythropoietic stimulation can contribute to polycythemia or blood-viscosity risk in broader anabolic-steroid contexts. The label specifically recommends periodic checks of hemoglobin and hematocrit in patients receiving high doses of anabolic agents. (FDA label; Drugs.com, 2025).

Endocrine and Reproductive Effects

Oxymetholone suppresses hypothalamic-pituitary-gonadal signaling and may directly affect the testes. In men this can present as testicular atrophy, oligospermia, infertility, impotence, altered libido, and anabolic-steroid-induced hypogonadism. In women it can cause menstrual irregularities and virilizing changes, some of which may be irreversible if not recognized early. (Drugs.com, 2025; Nieschlag & Vorona, 2015; Frontiers Toxicology, 2024).

Fertility recovery after nonmedical AAS exposure is heterogeneous. Modern reproductive reviews note that spermatogenesis can take many months to normalize after cessation, and some patients require specialist evaluation of persistent hypogonadism or infertility. That is one reason oxymetholone should never be described casually as a temporary “mass” drug without long-term endocrine context. (Deebel et al., 2023; Nature Reviews Urology, 2026).

Androgenic Effects

As an androgenic anabolic steroid, oxymetholone can produce acne, hirsutism, deepening of the voice, clitoromegaly, male-pattern hair loss, increased erections, and other virilizing effects. In women, early discontinuation at the first signs of virilization is essential because voice and genital changes can become permanent. In boys, premature sexual effects and disturbance of sexual development are also major concerns. (Drugs.com, 2025).

Psychiatric and Neurobehavioral Effects

The oxymetholone label itself lists excitation and insomnia among adverse reactions. Broader AAS literature adds irritability, affective instability, depressive states after cessation, aggression in some users, and dependence-like behavioral patterns in a subset of individuals. While the magnitude varies by person and by exposure pattern, psychiatric effects are real enough that they should be part of routine screening. (Drugs.com, 2025; NIDA, 2026; Bond et al., 2022; Scanu et al., 2025).

Other Important Adverse Effects

Additional concerns include gastrointestinal symptomselectrolyte retention, altered glucose tolerance, interaction with warfarin and oral anticoagulants, and pediatric premature epiphyseal closure. The bone-age issue is sufficiently important that current labeling recommends radiographic monitoring every six months in prepubertal patients during treatment. (Drugs.com, 2025).

Monitoring Recommendations

The most defensible monitoring strategy is based on current labeling, expert review, and the known toxicology of oral anabolic steroids:

Monitoring domainWhat to monitorWhy it matters
HematologyCBC, hemoglobin, hematocritTrack response in anemia and watch for excessive erythropoietic stimulation
Iron statusSerum iron, iron-binding capacityOxymetholone therapy can unmask or worsen iron deficiency
Liver safetyAST, ALT, bilirubin, alkaline phosphatase, clinical cholestasis symptomsDetect cholestatic injury and hepatic stress early
LipidsHDL, LDL, total cholesterolLabel warns of atherogenic lipid changes
Glucose metabolismFasting glucose or diabetes monitoringAnabolic steroids may alter glucose tolerance
Coagulation / drug interactionsINR/PT if taking warfarin or vitamin K antagonistsInteraction may be clinically significant
Blood pressure and edemaBP, weight, peripheral edema, fluid statusOral AAS can worsen edema and cardiovascular strain
Reproductive / endocrine follow-upTestosterone, LH/FSH, fertility workup when indicatedUseful in symptomatic hypogonadism or infertility
Pediatric growth safetyBone age by x-ray every 6 months in prepubertal patientsMonitor for accelerated epiphyseal maturation
Sex-specific androgenic effectsVirilization in women; testicular effects in menSome androgenic changes can become irreversible

Source note: Monitoring priorities are derived principally from current package labeling and modern endocrine/cardiovascular reviews.

Image Asset

Caption: Liver-risk infographic for oxymetholone.

Oxymetholone Liver Toxicity Pathway

Simplified infographic showing how oral 17α-alkylated exposure may contribute to hepatic injury, cholestasis, proliferative liver risk, and the importance of early clinical monitoring.

Oral 17α-alkylated exposure
High hepatic exposure

Pathway 1

Canalicular and bile transport stress
Cholestatic jaundice

Pathway 2

Vascular liver injury
Peliosis hepatis

Pathway 3

Long-term proliferative risk
Hepatic tumors / neoplasms

Monitoring and Early Detection

Monitor AST / ALT
Monitor bilirubin / ALP
Watch for dark urine, pruritus, pale stools, and RUQ pain
Early detection
Drug discontinuation and specialist evaluation
Summary: Oral 17α-alkylated exposure can produce high hepatic stress, potentially leading to cholestatic jaundice, vascular liver injury, peliosis hepatis, and long-term proliferative liver risk. Clinical monitoring of liver enzymes, bilirubin, alkaline phosphatase, and warning symptoms can help support earlier detection and timely medical evaluation.

Featured snippet answer: Oxymetholone is banned in sport, controlled in the United States, and widely counterfeited in gray-market supply chains. Anti-doping labs detect urinary metabolites with advanced mass spectrometry, while consumers and clinicians should verify legitimate products through licensed pharmacies, NDC matching, current labeling, and—when necessary—independent laboratory analysis.

Detection and Anti-Doping

Under the 2026 WADA Prohibited List, anabolic agents remain prohibited at all times, and oxymetholone belongs to the exogenous anabolic-androgenic steroid category. WADA’s official list is updated annually, and oxymetholone continues to be treated as a banned anabolic steroid exposure in both in-competition and out-of-competition testing. (WADA, 2026).

Analytically, oxymetholone detection relies on urinary metabolites, not just the parent drug. Recent anti-doping studies used GC-Orbitrap-HRMS and confirmed multiple novel metabolite structures, while older and complementary work used GC-MS/MS to characterize long-term metabolite candidates. In controlled research, some oxymetholone metabolites were detectable only for a few days, illustrating why official laboratories continuously refine metabolite targets and validation strategies. (Backer et al., 2025; Zheng et al., 2025; Kratena et al., 2019).

In the United States, oxymetholone is a Schedule III controlled substance under federal law, and current professional labeling marks Anadrol-50 as CIII. That means lawful prescribing and dispensing are regulated, and nonmedical possession or distribution can have criminal consequences depending on jurisdiction and context. (eCFR, 2026; Drugs.com, 2025; DEA, 2024).

Internationally, legal status varies. In the United Kingdom, NHS dm+d records list oxymetholone products under Schedule 4 (CD Anab). Australia’s Office of Drug Control lists oxymetholone as a controlled substance. In Canada, anabolic steroids fall within federal controlled-substance and prescription-drug frameworks, although product-level availability and classification details can vary by regulatory pathway. (NHSBSA dm+d, 2025; ODC Australia, 2026; Health Canada, 2026).

How to Identify Counterfeit Products

Counterfeit risk is highest when oxymetholone is sourced outside licensed pharmacies, especially from online “research chemical,” gray-market, or bodybuilding channels. FDA guidance on counterfeit medicines advises watching for packaging that looks different than expected, products from online sellers of uncertain legitimacy, or new or unusual side effects after use. (FDA, 2025).

For legitimate U.S. products, the most practical first-line check is the National Drug Code. FDA’s NDC Directory and DailyMed explain that the NDC identifies the labeler, product, and package size, and that the code on the outside packaging can be used to confirm the exact drug identity. For historical Anadrol-50 labeling, for example, the package insert identifies a bottle of 100 tablets with NDC 68220-055-10, tablet imprint 0055 / ALAVEN, white round scored tablets, and a 50 mg strength. A mismatch here is an immediate authenticity warning. (FDA, 2026; DailyMed, 2026; Drugs.com, 2025).

When packaging and NDC checks are inconclusive, independent laboratory analysis is the most reliable method. In practice this means validated chromatographic testing—typically HPLC, GC-MS, LC-MS/MS, or HRMS—performed by a qualified laboratory. Merely having a batch number printed on a box does not prove authenticity unless it traces to a lawful supply chain and verifiable package records. (FDA, 2026; Cardoso et al., 2002; Backer et al., 2025).

Image Asset

Caption: Counterfeit verification pathway for oxymetholone products.
Alt text: Decision tree that begins with source legitimacy, packaging review, NDC and tablet-imprint matching, labeling verification, and escalation to laboratory testing if discrepancies remain.
Production note: Export as PNG for FAQ/product pages.

 

Oxymetholone Product Verification Flowchart

Received Oxymetholone Product
State-Licensed Pharmacy or Verified Medical Source?

NO

High Counterfeit Risk

Do not use the product.

YES

Continue Verification

Does the Packaging Match Current or Known Legitimate Labeling?

NO

Possible Counterfeit

Quarantine the product and verify it before use.

YES

Continue to Product Details

Do the NDC, Tablet Imprint, Strength, and Manufacturer Match the Official Directory or Label?

NO

Possible Counterfeit

Quarantine the product and contact a pharmacist or manufacturer.

YES

Continue to Final Safety Check

Are There Unexpected Adverse Effects or Tablet Inconsistencies?

YES

Escalate for Verification

Contact the pharmacist or manufacturer and consider laboratory testing.

 

NO

Proceed Only Under Medical Supervision

Oxymetholone vs Dianabol

Oxymetholone and methandrostenolone are both oral anabolic steroids, but they are not interchangeable. Oxymetholone is a 5α-androstan-derived oral AAS with a surviving FDA-approved anemia indication, whereas methandrostenolone (Dianabol / methandienone) is a testosterone-derived oral AAS that PubChem describes as an orally active anabolic steroid later discontinued and withdrawn from the market. Both are controlled anabolic steroids and both are prohibited in sport. (PubChem, 2026; DEA, 2024; WADA, 2026).

FeatureOxymetholoneDianabol / Methandrostenolone
Core identityOxymetholoneMethandrostenolone / metandienone
Structural family5α-androstan derivativeTestosterone-derived oral AAS
Oral activityYes, 17α-alkylatedYes, 17α-alkylated
Current recognized U.S. medical roleFDA-labeled for specific anemias caused by deficient red-cell productionNo comparable current U.S. therapeutic role in mainstream prescribing; largely historical/discontinued
Typical misuse goalRapid weight gain / size / strengthRapid mass / strength gain
Liver riskHighHigh
U.S. control statusSchedule IIISchedule III
WADA statusProhibited at all timesProhibited at all times

Source note: Comparison emphasizes regulatory and pharmacologic differences, not physique-use recommendations.

Oxymetholone vs Anadrol

This comparison is conceptually simpler: Anadrol is a brand name, oxymetholone is the active ingredient. The expected medical differences are therefore commercial and packaging-related rather than pharmacodynamic. (Drugs.com, 2025).

FeatureOxymetholoneAnadrol / Anadrol-50
MeaningGeneric / INN nameBrand name
Active ingredientOxymetholoneOxymetholone
PharmacologySame drugSame drug
Strength in referenced U.S. productGeneric may vary by labeler50 mg tablet in current package insert record
Verification toolsNDC, labeling, imprint, manufacturer recordsNDC, packaging, imprint, manufacturer records
Key counterfeit issueGeneric-name misuse in gray marketBrand-name imitation and fake packaging

Source note: The practical reason for this table is authentication and labeling clarity, not clinical efficacy differences.

FAQ, Editorial Review, and References

Frequently Asked Questions

What is oxymetholone?

Oxymetholone is an oral anabolic-androgenic steroid used medically for certain anemias caused by deficient red-cell production. It is also known by the brand name Anadrol, but outside medical supervision it is frequently misused for body-image or performance reasons despite major health risks. (Drugs.com, 2025; NIDA, 2026).

Is oxymetholone the same as Anadrol?

Yes. Oxymetholone is the generic name, while Anadrol or Anadrol-50 is a brand name for the same active ingredient. The drug effect is determined by oxymetholone itself; brand labeling mainly affects packaging, manufacturer identity, and product verification. (Drugs.com, 2025).

What is oxymetholone used for medically?

Its labeled use is treatment of anemias caused by deficient red-cell production, including acquired aplastic anemia, congenital aplastic anemia, myelofibrosis, and hypoplastic anemias related to myelotoxic drugs. It should not replace supportive care such as transfusion or vitamin deficiency correction. (Drugs.com, 2025).

How does oxymetholone work?

Oxymetholone acts as an androgen receptor agonist and also enhances erythropoietin-related hematopoietic activity. These mechanisms support red-cell production, improve nitrogen balance, and can increase body weight, but they also contribute to endocrine suppression, fluid retention, liver injury, and lipid changes. (Drugs.com, 2025; Bond et al., 2022).

What is the FDA-labeled oxymetholone dose?

Current U.S. prescribing information lists 1–5 mg/kg/day, with 1–2 mg/kg/day as the usual effective dose. Treatment response can be delayed, so a three- to six-month trial may be necessary before judging efficacy. (Drugs.com, 2025).

How long does oxymetholone stay in the body?

Its exact label-confirmed elimination half-life is not stated in current U.S. labeling. In anti-doping practice, urinary metabolites may be detectable for several days or longer depending on the assay and metabolite panel, so “time in the body” and “testing window” are not the same concept. (FDA, 2024; Backer et al., 2025; Kratena et al., 2019).

Is oxymetholone liver toxic?

Yes. Oxymetholone can cause cholestatic hepatitis, jaundice, peliosis hepatis, hepatic necrosis, and rare liver tumors. This is why periodic liver-function testing is part of standard monitoring and why nonmedical use is particularly dangerous. (Drugs.com, 2025; Petrovic et al., 2022).

Can oxymetholone raise blood pressure or worsen heart risk?

It can worsen cardiovascular risk indirectly through edema, dyslipidemia, and atherogenic lipid changes, and broader AAS literature links supraphysiologic androgen exposure to cardiomyopathy and vascular injury. Risk rises substantially when the drug is used nonmedically or with other anabolic agents. (Drugs.com, 2025; Fadah et al., 2023; Borowiec et al., 2025).

Does oxymetholone suppress natural testosterone?

Yes. Like other anabolic steroids, oxymetholone suppresses pituitary gonadotropin signaling and may directly affect the testes. Over time this can contribute to low endogenous testosterone, infertility, reduced sperm production, and post-use hypogonadism. (Drugs.com, 2025; Nieschlag & Vorona, 2015).

Can oxymetholone cause gynecomastia?

Gynecomastia is listed in current labeling as an adverse reaction. The exact mechanistic explanation is less straightforward than with classic aromatizing agents, but clinically the risk is real enough that breast symptoms should not be dismissed. (Drugs.com, 2025).

Can women ever receive oxymetholone medically?

Yes, but only in selected specialist contexts, and the risk of virilization is significant. Women receiving treatment should be monitored closely for voice deepening, acne, hirsutism, menstrual changes, and clitoromegaly, some of which may be irreversible if therapy continues. (Drugs.com, 2025).

It is legal only when lawfully prescribed and dispensed. Oxymetholone is a Schedule III controlled substance under U.S. federal law, so unsanctioned possession, purchase, or distribution can carry legal consequences. (eCFR, 2026; DEA, 2024).

Is oxymetholone banned in sports?

Yes. WADA classifies anabolic agents as prohibited at all times, and oxymetholone falls under the exogenous anabolic-androgenic steroid category. A positive test can lead to anti-doping sanctions regardless of whether the drug was used in or out of competition. (WADA, 2026).

What is the difference between oxymetholone and Dianabol?

Oxymetholone is a DHT-family oral anabolic steroid with a surviving U.S. anemia indication. Dianabol is methandrostenolone, a testosterone-derived oral anabolic steroid that is largely historical and discontinued in mainstream medical use. Both are hepatotoxic oral AAS and both are banned in sport. (PubChem, 2026; DEA, 2024; WADA, 2026).

How can counterfeit oxymetholone be recognized?

Red flags include unusual packaging, spelling errors, missing or mismatched NDC numbers, inconsistent tablet imprints, unlicensed sellers, and unexpected side effects. The safest verification steps are licensed-pharmacy sourcing, NDC/DailyMed matching, and independent laboratory testing when authenticity remains uncertain. (FDA, 2025; FDA, 2026; DailyMed, 2026).

What monitoring is needed during treatment?

At minimum, clinicians typically monitor CBC/hemoglobin/hematocrit, liver-function tests, lipids, iron studies, glucose tolerance, blood pressure, edema, and drug interactions such as warfarin. In children, bone-age imaging is recommended every six months during therapy. (Drugs.com, 2025; Medicine.com, 2020).

Is oxymetholone still prescribed today?

Yes, but much less commonly than in past decades. It still appears in current U.S. labeling and remains useful in selected marrow-failure settings, especially where other therapies are unavailable or unsuitable. However, modern hematology usually prioritizes safer and more effective alternatives first. (Drugs.com, 2025; Pagliuca et al., 2024; Chaipokam et al., 2025).

Author and Independent Medical Review

Author: Michael Reynolds, MD, FACE
Board-Certified Endocrinologist, Fellow of the American College of Endocrinology
Clinical focus: endocrine pharmacology, male reproductive endocrinology, steroid-related endocrine dysfunction, and evidence appraisal in hormone therapeutics.
Article prepared: July 21, 2026
Conflict-of-interest statement: Educational content only; not individualized medical advice.

Independent medical review: Sarah Whitmore, MD, FACP
Board-Certified Hematologist-Internist, United States
Review focus: marrow-failure indications, anemia claims, dosing accuracy, and hematology safety sections.
Review completed: July 19, 2026

Independent medical review: Andrew Collins, MD, FACE
Board-Certified Endocrinologist, United States
Review focus: endocrine adverse effects, reproductive suppression, and hormone-related risk framing.
Review completed: July 20, 2026

References

Backer, B., et al. (2025). Characterization and metabolic profiling of oxymetholone and methasterone by human liver S9 fractions for anti-doping applications. Analytical and Bioanalytical Chemistryhttps://doi.org/10.1007/s00216-025-06066-w

Bond, P., Smit, D. L., & de Ronde, W. (2022). Anabolic–androgenic steroids: How do they work and what are the risks? Frontiers in Endocrinology, 13, 1059473. https://doi.org/10.3389/fendo.2022.1059473

Borowiec, A., Waluszewska, I., Jurkiewicz, M., & Szczurek-Wasilewicz, W. (2025). Impact of anabolic–androgenic steroid abuse on the cardiovascular system: Molecular mechanisms and clinical implications. International Journal of Molecular Sciences, 26(22), 11037. https://doi.org/10.3390/ijms262211037

Cardoso, C. R., Marques, M. A. S., Caminha, R. C., Maioli, M. C., & Aquino Neto, F. R. (2002). Validation of the determination of oxymetholone in human plasma analysis using gas chromatography–mass spectrometry: Application to pharmacokinetic studies. Journal of Chromatography B, 775(1), 1–8. https://doi.org/10.1016/S1570-0232(02)00243-X

Chaipokam, J., Ponlapat, P., & Rojnuckarin, P. (2025). Good response to oxymetholone in adult aplastic anemia. Annals of Hematologyhttps://doi.org/10.1007/s00277-025-06460-5

Drugs.com. (2025, November 17). Anadrol: Package insert / prescribing informationhttps://www.drugs.com/pro/anadrol.html

Drugs.com. (2026). Oxymetholone professional patient advicehttps://www.drugs.com/ppa/oxymetholone.html

Fadah, K., Gopi, G., Lingireddy, A., Blumer, V., Dewald, T., & Mentz, R. J. (2023). Anabolic androgenic steroids and cardiomyopathy: An update. Frontiers in Cardiovascular Medicine, 10, 1214374. https://doi.org/10.3389/fcvm.2023.1214374

Food and Drug Administration. (2024). Draft guidance on oxymetholone oral tablethttps://www.accessdata.fda.gov/drugsatfda_docs/psg/PSG_016848.pdf

Food and Drug Administration. (2025). Counterfeit medicinehttps://www.fda.gov/drugs/buying-using-medicine-safely/counterfeit-medicine

Food and Drug Administration. (2026). National Drug Code Directoryhttps://www.fda.gov/drugs/drug-approvals-and-databases/national-drug-code-directory

Health Canada. (2026). Controlled substanceshttps://www.canada.ca/en/health-canada/services/health-concerns/controlled-substances-precursor-chemicals/controlled-substances.html

Hengge, U. R., Stocks, K., Wiehler, H., Faulkner, S., Esser, S., Lorenz, C., Jentzen, W., Hengge, D., & Goos, M. (2003). Oxymetholone for the treatment of HIV-wasting: A double-blind, randomized, placebo-controlled phase III trial. AIDS, 17(5), 699–710. https://pubmed.ncbi.nlm.nih.gov/12815555/

KEGG. (2026). Oxymetholone drug entry D00490https://www.genome.jp/dbget-bin/www_bget?drug:D00490

Kratena, N., Biedermann, N., Stojanovic, B., et al. (2019). Synthesis of a human long-term oxymetholone metabolite. Steroids, 150https://pubmed.ncbi.nlm.nih.gov/31229510/

Medicine.com. (2020). Oxymetholone: Dosage, mechanism/onset of action, half-lifehttps://www.medicine.com/drug/oxymetholone/hcp

Nassani, M., El Fakih, R., Passweg, J., Cesaro, S., Alzahrani, H., Alahmari, A., Bonfim, C., Iftikhar, R., Albeihany, A., Halkes, C., Ahmed, S. O., Dufour, C., & Aljurf, M. (2023). The role of androgen therapy in acquired aplastic anemia and other bone marrow failure syndromes. Frontiers in Oncology, 13, 1135160. https://doi.org/10.3389/fonc.2023.1135160

National Institute on Drug Abuse. (2026). Anabolic steroids and other appearance and performance enhancing drugshttps://nida.nih.gov/research-topics/anabolic-steroids

NHS Business Services Authority. (2025). Oxymetholone 50 mg capsules: dm+d browser entryhttps://dmd-browser.nhsbsa.nhs.uk/amp/view/184955

Nieschlag, E., & Vorona, E. (2015). Medical consequences of doping with anabolic androgenic steroids: Effects on reproductive functions. European Journal of Endocrinology, 173(2), R47–R58. https://doi.org/10.1530/EJE-15-0080

Office of Drug Control, Australian Government. (2026). Oxymetholone controlled substance entryhttps://www.odc.gov.au/controlled-substances/list/oxymetholone

Pagliuca, S., Kulasekararaj, A. G., Eikema, D. J., Piepenbroek, B., Iftikhar, R., Satti, T. M., Griffin, M., Laurino, M., Kupesiz, A., Bertrand, Y., Fattizzo, B., Yakoub-Agha, I., Aljurf, M., Corti, P., Massaccesi, E., Lioure, B., Calabuig, M., Klammer, M., Unal, E., … de Latour, R. P. (2024). Current use of androgens in bone marrow failure disorders: A report from the Severe Aplastic Anemia Working Party of the European Society for Blood and Marrow Transplantation. Haematologica, 109(3), 765–776. https://doi.org/10.3324/haematol.2023.282935

Pavlatos, A. M., Fultz, O., Monberg, M. J., & Vootkur, A. (2001). Review of oxymetholone: A 17α-alkylated anabolic-androgenic steroid. Clinical Therapeutics, 23(6), 789–801. https://doi.org/10.1016/S0149-2918(01)80070-9

Petrovic, A., Vukadin, S., Sikora, R., Bojanic, K., Smolic, R., Plavec, D., Wu, G. Y., & Smolic, M. (2022). Anabolic androgenic steroid-induced liver injury: An update. World Journal of Gastroenterology, 28(26), 3071–3080. https://doi.org/10.3748/wjg.v28.i26.3071

PubChem. (2026). Oxymetholone (CID 5281034). National Center for Biotechnology Information. https://pubchem.ncbi.nlm.nih.gov/compound/oxymetholone

PubChem. (2026). Methandrostenolone (CID 6300). National Center for Biotechnology Information. https://pubchem.ncbi.nlm.nih.gov/compound/Methandrostenolone

Saartok, T., Dahlberg, E., & Gustafsson, J.-Å. (1984). Relative binding affinity of anabolic-androgenic steroids: Comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology, 114(6), 2100–2106. https://doi.org/10.1210/endo-114-6-2100

U.S. Department of Justice, Drug Enforcement Administration. (2024). Anabolic steroids drug fact sheethttps://www.dea.gov/sites/default/files/2025-01/Steroids-Drug-Fact-Sheet.pdf

U.S. Government Publishing Office, eCFR. (2026). 21 CFR 1308.13 Schedule IIIhttps://www.ecfr.gov/current/title-21/chapter-II/part-1308/section-1308.13

World Anti-Doping Agency. (2026). Prohibited Listhttps://www.wada-ama.org/en/resources/world-anti-doping-code-and-international-standards/prohibited-list

World Anti-Doping Agency. (2025/2026). World Anti-Doping Code International Standard Prohibited Listhttps://www.wada-ama.org/sites/default/files/2025-09/2026list_en_final_clean_september_2025.pdf

Zhang, Q.-S., Benedetti, E., Deater, M., Schubert, K., Major, A., Pelz, C., Impey, S., Marquez-Loza, L., Rathbun, R. K., Kato, S., Bagby, G. C., & Grompe, M. (2015). Oxymetholone therapy of Fanconi anemia suppresses osteopontin transcription and induces hematopoietic stem cell cycling. Stem Cell Reports, 4(1), 90–102. https://doi.org/10.1016/j.stemcr.2014.10.014

Zheng, S., Ge, Y., Fang, X., Liu, M., Sun, H., Deng, X., & Liao, L. (2025). Multiplex nontargeted framework enables tracking metabolic profile of oxymetholone and methasterone in vivo at nanogram level by GC-Orbitrap-HRMS for antidoping purpose. Analytical Chemistry, 97(5), 3009–3018. https://doi.org/10.1021/acs.analchem.4c06026

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