Boxed Warning
Peliosis hepatis:
Peliosis hepatis, a condition in which liver and, sometimes, splenic tissue is replaced with blood-filled cysts, has occurred in patients receiving androgenic anabolic steroids. These cysts are sometimes present with minimal hepatic dysfunction and have been associated with liver failure. Often, they are not recognized until life-threatening liver failure or intra-abdominal hemorrhage develops. Withdrawal of drug usually results in complete disappearance of lesions.
Liver cell tumors:
Most often these tumors are benign and androgen-dependent, but fatal malignant tumors have occurred. Withdrawal of drug often results in regression or cessation of tumor progression. However, hepatic tumors associated with androgens or anabolic steroids are much more vascular than other hepatic tumors and may be silent until life-threatening, intra-abdominal hemorrhage develops.
Blood lipid changes:
Blood lipid changes associated with increased risk of atherosclerosis are seen in patients treated with androgens and anabolic steroids. These changes include decreased high-density lipoprotein (HDL) and, sometimes, increased low-density lipoprotein (LDL). The changes may be very marked and could have a serious impact on the risk of atherosclerosis and coronary artery disease.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Anadrol-50: 50 mg [scored]
Pharmacology
Mechanism of Action
Enhances production of erythropoietin in patients with anemias which are due to bone marrow failure; stimulates erythropoiesis in anemias due to deficient red cell production
Pharmacokinetics/Pharmacodynamics
Onset of Action
Response is not often immediate; a minimum trial of 3 to 6 months is recommended
Use: Labeled Indications
Anemia: Treatment of anemias caused by deficient red cell production. Note: Androgen therapy (eg, oxymetholone) is generally not appropriate for the treatment of anemias except in certain rare situations (eg, Fanconi anemia).
Use: Off Label
Fanconi anemiac
Data from a limited number of patients in a retrospective review suggests that oxymetholone may be beneficial in the treatment of Fanconi anemia Paustian 2016. However, due to significant risks associated with therapy, a careful risk vs. benefit assessment is advised. Additional data may be necessary to further define the role of oxymetholone in this condition.
Contraindications
Hypersensitivity to oxymetholone or any component of the formulation; breast cancer in men; breast cancer in women with hypercalcemia; prostate cancer; severe hepatic dysfunction; nephrosis or nephrotic phase of nephritis; pregnancy or use in women who may become pregnant
Dosage and Administration
Dosing: Adult
Erythropoietic effects: Oral: 1 to 5 mg/kg/day once daily; usual effective dose: 1 to 2 mg/kg/day; give for a minimum trial of 3 to 6 months because response may be delayed
Fanconi anemia (off-label use): Limited data available: Oral: Initial: 2 mg/kg/day (median dose reported); most patients had a documented dose reduction although exact doses were not provided
Duration of therapy: 4.1 years (median for responders); 1.3 years (median for non-responders) (Paustian 2016). Additional data may be necessary to further define the role of oxymetholone in this condition.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Note: The National Kidney Foundation does not recommend the use of androgens as an adjuvant to ESA treatment in anemic patients with chronic kidney disease (KDOQI, 2006).
Anemia; treatment (erythropoietic effect [eg, aplastic or Fanconi anemias]): Children and Adolescents: Oral: 1 to 5 mg/kg/day once daily; usual effective dose: 1 to 2 mg/kg/day; some have suggested higher dosing initially (2 to 5 mg/kg/day) and then tapering to lowest effective dose (Carmitta, 1979; Lanzkowsky, 2010); response often is not immediate; give for a minimum trial of 3 to 6 months
Storage
Store at room temperature 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light.
Drug Interactions
Ajmaline: Androgens may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased. Monitor therapy
Blood Glucose Lowering Agents: Androgens may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy
C1 inhibitors: Androgens may enhance the thrombogenic effect of C1 inhibitors. Monitor therapy
Corticosteroids (Systemic): May enhance the fluid-retaining effect of Androgens. Monitor therapy
CycloSPORINE (Systemic): Androgens may enhance the hepatotoxic effect of CycloSPORINE (Systemic). Androgens may increase the serum concentration of CycloSPORINE (Systemic). Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Androgens may enhance the anticoagulant effect of Vitamin K Antagonists. Consider therapy modification
Test Interactions
Decreased thyroxine-binding globulin, T4; increased resin uptake of T3 and T4
Adverse Reactions
Frequency not defined:
Cardiovascular: Coronary artery disease, peripheral edema
Central nervous system: Chills, deepening of the voice (females), excitement, insomnia
Dermatologic: Acne vulgaris, androgenetic alopecia (postpubertal males, females), hyperpigmentation
Endocrine & metabolic: Amenorrhea, change in libido (decreased/increased), decreased glucose tolerance, decreased HDL cholesterol, gynecomastia, hirsutism (women), hypercalcemia, hyperchloremia, hyperkalemia, hypernatremia, hyperphosphatemia, increased LDL cholesterol, menstrual disease
Gastrointestinal: Diarrhea, nausea, vomiting
Genitourinary: Benign prostatic hypertrophy (elderly males), clitoromegaly, decreased ejaculate volume, epididymitis, erectile dysfunction (increased erections; prepubertal males), impotence, irritable bladder, oligospermia, phallic enlargement, priapism, testicular atrophy, testicular disease, virilization (females)
Hematologic & oncologic: Clotting factors suppression (II, V, VII, X), hemorrhage, increased INR, iron deficiency anemia, leukemia, malignant neoplasm of prostate, prolonged prothrombin time
Hepatic: Cholestatic hepatitis, cholestatic jaundice, hepatic failure, hepatic necrosis, hepatocellular neoplasm (including carcinoma), increased serum alkaline phosphatase, increased serum bilirubin, increased serum transaminases, peliosis hepatitis
Neuromuscular & skeletal: Increased creatine phosphokinase, premature epiphyseal closure (children)
Renal: Increased serum creatinine
Respiratory: Hoarseness (females)
<1%, postmarketing, and/or case reports: Hepatotoxicity (idiosyncratic; Chalasani 2014)
Warnings/Precautions
Concerns related to adverse effects:
- Blood lipid changes: [US Boxed Warning]: Anabolic steroids may cause changes in blood lipids (decreased high density lipoproteins and sometimes increased low density lipoproteins), increasing the risk of arteriosclerosis and coronary artery disease.
- Clotting factor alterations: Anabolic steroids may suppress factors II, V, VII, and X; prothrombin time may be increased.
- Hepatic effects: [US Boxed Warning]: Androgenic anabolic steroid treatment may cause peliosis hepatis, which occurs when splenic or hepatic tissue is replaced by cysts (blood-filled); may only cause minimal hepatic dysfunction although has been associated with hepatic failure. Androgenic liver cell tumors, which may be benign, although malignant tumors have also been reported; generally regress when anabolic steroid treatment is withdrawn. Both conditions (peliosis and tumors) may not be apparent until liver failure or intra-abdominal hemorrhage develops. Androgen use (low doses) has also been associated with cholestatic hepatitis and jaundice; may be associated with hepatomegaly and right upper-quadrant pain; jaundice is typically reversible upon discontinuation (continuing treatment has been associated with coma and death). Monitor liver function periodically.
- Prostate conditions: Androgenic anabolic steroid use may cause prostatic hypertrophy or prostate cancer in elderly men.
Disease-related concerns:
- Breast cancer: May cause hypercalcemia in women with breast cancer by stimulating osteolysis.
- Diabetes: Use with caution in patients with diabetes mellitus; insulin or oral hypoglycemic needs may be altered; monitor carefully.
- Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, migraine, seizure disorder, renal impairment); may cause fluid retention.
Special populations:
- Pediatric: May accelerate bone maturation without producing compensatory gain in linear growth in children; effect may continue for 6 months after treatment discontinuation; in prepubertal children perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.
- Women: Discontinue with evidence of mild virilization in women.
Other warnings/precautions:
- Appropriate use: Oxymetholone should not replace other anemia treatment supportive measures such as transfusion, correction of iron, folic acid, vitamin B12 or pyridoxine deficiency, antibacterial therapy, and the appropriate use of corticosteroids.
Monitoring Parameters
Periodic liver function tests, lipid profile, hemoglobin and hematocrit; iron studies; serum glucose (may be decreased by testosterone, monitor patients with diabetes); radiologic examination of bones every 6 months (when using in prepubertal children); monitor urine and serum calcium and signs of virilization in women treated for breast cancer
Pregnancy
Pregnancy Risk Factor
X
Pregnancy Considerations
Oligospermia or amenorrhea may occur resulting in an impairment of fertility. Use is contraindicated in women who are or may become pregnant.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience diarrhea, trouble sleeping, or sexual dysfunction. Have patient report immediately to prescriber signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), erection that lasts more than 4 hours, acne, shortness of breath, excessive weight gain, swelling of arms or legs, unable to pass urine, change in amount of urine passed, muscle weakness, bruising, bleeding, severe anxiety, or signs of virilization (in females a deep voice, facial hair, pimples, or period changes) (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
