Oxymetholone is a synthetic anabolic-androgenic steroid (AAS), known commercially as Anadrol or Anapolon. It is a 17-alpha-alkylated steroid, which allows it to be effective when taken orally. Derived from dihydrotestosterone (DHT), its chemical structure is modified to enhance its anabolic activity. Oxymetholone is considered one of the most potent oral anabolic agents available, used for specific medical applications but carrying significant potential for misuse.
Therapeutic Applications and Biological Mechanism
Oxymetholone was developed to treat conditions characterized by low red blood cell counts and muscle mass loss. In the United States, its medical use is primarily for treating anemias caused by deficient red cell production. This includes acquired and congenital aplastic anemia, myelofibrosis, and hypoplastic anemias resulting from myelotoxic drug administration. The drug stimulates the body’s own production processes and is not intended to replace supportive care like transfusions.
Oxymetholone addresses anemia by stimulating the production and excretion of erythropoietin. This action directly enhances erythropoiesis, increasing the number of circulating red blood cells and hemoglobin levels. Improving the oxygen-carrying capacity of the blood helps alleviate the fatigue and weakness associated with these blood disorders.
Beyond its hematological effects, the compound is an anabolic agent that influences protein metabolism. It maintains a positive nitrogen balance, a state where nitrogen intake exceeds excretion. This positive balance is a prerequisite for tissue growth, leading to increased protein synthesis and reduced protein breakdown.
The anabolic effect is therapeutically exploited to treat muscle wasting syndromes, particularly cachexia associated with severe illnesses like HIV/AIDS. Increased protein synthesis supports the regeneration and growth of muscle tissue, promoting weight gain in malnourished or chronically ill patients. Historically, the steroid has also been used to treat osteoporosis and stimulate weight gain following severe trauma or infection.
Comprehensive Safety Profile and Adverse Effects
Due to its high potency, Oxymetholone carries a significant risk profile, particularly concerning the liver. As a 17-alpha-alkylated compound, it is highly hepatotoxic, which can lead to cholestatic hepatitis and jaundice (impaired bile flow causing yellowing of the skin and eyes). More severe hepatic complications include peliosis hepatis, a rare condition characterized by blood-filled cysts in the liver and spleen. Prolonged use is also linked to hepatocellular neoplasms (liver tumors), which are usually benign but can be malignant. Physicians must monitor liver function frequently, though these toxicities often resolve upon discontinuation.
The steroid also presents significant cardiovascular risks stemming from its adverse effects on blood lipid profiles. Oxymetholone administration often causes a marked decrease in high-density lipoprotein (HDL) cholesterol and concurrently increases low-density lipoprotein (LDL) cholesterol. This combination heightens the risk of arteriosclerosis and coronary artery disease. Furthermore, the drug can cause fluid retention, or edema. This is of particular concern for individuals with pre-existing cardiac, renal, or hepatic disease, as it can worsen conditions like congestive heart failure.
Hormonal and androgenic side effects are also common due to the drug’s nature as a synthetic androgen. In men, the introduction of exogenous anabolic steroids suppresses the body’s natural production of testosterone, which can lead to testicular atrophy and a decreased sperm count. While Oxymetholone has a relatively low tendency to convert to estrogen, it can still cause gynecomastia, the enlargement of male breast tissue.
For women, the androgenic effects can result in virilization, or the development of male characteristics. These symptoms include a deepening of the voice, which is often irreversible even after the drug is stopped, as well as hirsutism, or excessive growth of body hair. Other virilizing effects include clitoral enlargement and menstrual irregularities. Common androgenic side effects for both sexes include the development of acne and the acceleration of male-pattern baldness in individuals genetically predisposed to the condition.
Regulatory Classification and Non-Medical Use
In the United States, Oxymetholone is subject to strict control and regulation as a Schedule III controlled substance under the Code of Federal Regulations. This classification indicates that the compound has accepted medical uses but also a potential for abuse or dependence. Consequently, the drug can only be legally obtained through a valid prescription from a licensed healthcare provider, and illegal possession or distribution carries significant criminal penalties.
The high anabolic power of Oxymetholone has led to its extensive use in non-medical contexts, primarily for physique enhancement and performance improvement. Athletes and bodybuilders often misuse the compound to achieve rapid and substantial gains in muscle mass and overall body weight. This non-medical use typically involves administration cycles that are not medically supervised and often exceed prescribed dosages. Users often combine Oxymetholone with other performance-enhancing compounds in a practice known as “stacking” to maximize its effects. This pattern of misuse dramatically increases the risk of severe adverse effects, particularly hepatotoxicity and cardiovascular complications.
Reflecting its status as a performance enhancer, the compound is explicitly prohibited by major sports organizations, including the World Anti-Doping Agency (WADA).