Oxymetholone

Oxymetholone
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Kiran Singh, M.D. [2]

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Overview

Oxymetholone is an anabolic steroid that is FDA approved for the treatment of anaemia. Common adverse reactions include cholestatic jaundice, clitoral enlargement, menstrual irregularities,insomnia, nausea, vomiting, diarrhea, gynecomastia.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

• Oxymetholone tablets is indicated in the treatment of anemias caused by deficient red cell production. Acquired aplastic anemia, congenital aplastic anemia, myelofibrosis and the hypoplastic anemias due to the administration of myelotoxic drugs often respond. Anadrol®-50 Tablets should not replace other supportive measures such as transfusion, correction of iron, folic acid, vitamin B12 or pyridoxine deficiency, antibacterial therapy and the appropriate use of corticosteroids.

Dosage

• The recommended daily dose in adults is 1-5 mg/kg of body weight per day. The usual effective dose is 1-2 mg/kg/day but higher doses may be required, and the dose should be individualized. Response is not often immediate, and a minimum trial of three to six months should be given. Following remission, some patients may be maintained without the drug; others may be maintained on an established lower daily dosage. A continued maintenance dose is usually necessary in patients with congenital aplastic anemia.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Oxymetholone in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxymetholone in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Indications

• Oxymetholone tablets is indicated in the treatment of anemias caused by deficient red cell production. Acquired aplastic anemia, congenital aplastic anemia, myelofibrosis and the hypoplastic anemias due to the administration of myelotoxic drugs often respond. Anadrol®-50 Tablets should not replace other supportive measures such as transfusion, correction of iron, folic acid, vitamin B12 or pyridoxine deficiency, antibacterial therapy and the appropriate use of corticosteroids.

Dosage

• The recommended daily dose in children is 1-5 mg/kg of body weight per day. The usual effective dose is 1-2 mg/kg/day but higher doses may be required, and the dose should be individualized. Response is not often immediate, and a minimum trial of three to six months should be given. Following remission, some patients may be maintained without the drug; others may be maintained on an established lower daily dosage. A continued maintenance dose is usually necessary in patients with congenital aplastic anemia.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Oxymetholone in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxymetholone in pediatric patients.

Contraindications

There is limited information regarding Oxymetholone Contraindications in the drug label.

Warnings

• The following conditions have been reported in patients receiving androgenic anabolic steroids as a general class of drugs:

This image is provided by the National Library of Medicine.

• Cholestatic hepatitis and jaundice occur with 17-alpha-alkylated androgens at relatively low doses. Clinical jaundice may be painless, with or without pruritus. It may also be associated with acute hepatic enlargement and right upper-quadrant pain, which has been mistaken for acute (surgical) obstruction of the bile duct. Drug-induced jaundice is usually reversible when the medication is discontinued. Continued therapy has been associated with hepatic coma and death. Because of the hepatoxicity associated with oxymetholone administration, periodic liver function tests are recommended.

• In patients with breast cancer, anabolic steroid therapy may cause hypercalcemia by stimulating osteolysis. In this case, the drug should be discontinued.

• Edema with or without congestive heart failure may be a serious complication in patients with pre-existing cardiac, renal or hepatic disease. Concomitant administration with adrenal steroids or ACTH may add to the edema. This is generally controllable with appropriate diuretic and/or digitalis therapy.

• Geriatric male patients treated with androgenic anabolic steroids may be at an increased risk for the development of prostate hypertrophy and prostatic carcinoma.

• Anabolic steroids have not been shown to enhance athletic ability.

PRECAUTIONS

Concurrent dosing of an anabolic steroid and warfarin may result in unexpectedly large increases in the INR or prothrombin time (PT). When an anabolic steroid is prescribed to a patient being treated with warfarin, doses of warfarin may need to be decreased significantly to maintain the desirable INR level and diminish the risk of potentially serious bleeding.

General:

• Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne and clitoromegaly). To prevent irreversible change, drug therapy must be discontinued when mild virilism is first detected. Such virilization is usual following androgenic anabolic steroid use at high doses. Some virilizing changes in women are irreversible even after prompt discontinuance of therapy and are not prevented by concomitant use of estrogens. Menstrual irregularities, including amenorrhea, may also occur.

• The insulin or oral hypoglycemic dosage may need adjustment in diabetic patients who receive anabolic steroids.

• Anabolic steroids may cause suppression of clotting factors II, V, VII and X, and an increase in prothrombin time.

Information for the patient:

• The health care provider should instruct patients to report immediately any use of warfarin and any bleeding.

• The health care provider should instruct patients to report any of the following effects of androgens.

Adult or Adolescent Males: Too frequent or persistent erections of the penis, appearance or aggravation of acne.

Women: Hoarseness, acne, changes in menstrual periods or more hair on the face.

All Patients: Any nausea, vomiting, changes in skin color or ankle swelling.

Adverse Reactions

Clinical Trials Experience

Hepatic: Cholestatic jaundice with, rarely, hepatic necrosis and death. Hepatocellular neoplasms and peliosis hepatis have been reported in association with long-term androgenic anabolic steroid therapy.

Genitourinary System:

In Men:

• Prepubertal: Phallic enlargement and increased frequency of erections.

• Postpubertal: Inhibition of testicular function, testicular atrophy and oligospermia, impotence, chronic priapism, epididymitis, bladder irritability and decrease in seminal volume.

In Women: Clitoral enlargement, menstrual irregularities.

In Both Sexes: Increased or decreased libido.

CNS: Excitation, insomnia.

Gastrointestinal: Nausea, vomiting, diarrhea.

Hematologic: Bleeding in patients on concomitant anticoagulant therapy, iron-deficiency anemia.

Leukemia has been observed in patients with aplastic anemia treated with oxymetholone. The role, if any, of oxymetholone is unclear because malignant transformation has been seen in patients with blood dyscrasias and leukemia has been reported in patients with aplastic anemia who have not been treated with oxymetholone.

Breast: Gynecomastia.

Larynx: Deepening of the voice in women.

Hair: Hirsutism and male-pattern baldness in women, male-pattern of hair loss in postpubertal males.

Skin: Acne (especially in women and prepubertal boys).

Skeletal: Premature closure of epiphyses in children, muscle cramps.

Body as a Whole: Chills.

Fluid and Electrolytes: Edema, retention of serum electrolytes (sodium, chloride, potassium, phosphate, calcium).

Metabolic/Endocrine: Decreased glucose tolerance , increased serum levels of low-density lipoproteins and decreased levels of high-density lipoproteins , increased creatine and creatinine excretion, increased serum levels of creatinine phosphokinase (CPK). Reversible changes in liver function tests also occur, including increased Bromsulphalein (BSP) retention and increase in serum bilirubin, glutamic-oxaloacetic transaminase (SGOT) and alkaline phosphatase.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Oxymetholone in the drug label.

Drug Interactions

• Warfarin: Clinically significant pharmacokinetic and pharmacodynamic interactions between anabolic steroids and warfarin have been reported in healthy volunteers. When anabolic steroid therapy is initiated in a patient already receiving treatment with warfarin, the INR (international normalized ratio) or prothrombin time (PT) should be monitored closely and the dose of warfarin adjusted as necessary until a stable target INR or PT has been achieved. Furthermore, in patients receiving both ANADROL®-50 Tablets and warfarin, careful monitoring of the INR or PT and adjustment of the warfarin dosage, if indicated, are recommended when the ANADROL®-50 dose is changed or discontinued. Patients should be closely monitored for signs and symptoms of occult bleeding.

• Anticoagulants: Anabolic steroids may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may have to be decreased in order to maintain the desired prothrombin time. Patients receiving oral anticoagulant therapy require close monitoring, especially when anabolic steroids are started or stopped.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): Pregnancy category X.
Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Oxymetholone in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Oxymetholone during labor and delivery.

Nursing Mothers

• It is not known whether anabolics are excreted in human milk. Because of the potential for serious adverse reactions in nursed infants from anabolics, women who take oxymetholone should not nurse.

Pediatric Use

• Anabolic/androgenic steroids should be used very cautiously in children and only by specialists who are aware of their effects on bone maturation.

• Anabolic agents may accelerate epiphyseal maturation more rapidly than linear growth in children, and the effect may continue for 6 months after the drug has been stopped. Therefore, therapy should be monitored by x-ray studies at 6-month intervals in order to avoid the risk of compromising the adult height.

Geriatic Use

• Clinical studies of ANADROL®-50 Tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Gender

There is no FDA guidance on the use of Oxymetholone with respect to specific gender populations.

Race

There is no FDA guidance on the use of Oxymetholone with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Oxymetholone in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Oxymetholone in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Oxymetholone in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Oxymetholone in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

Monitoring

There is limited information regarding Monitoring of Oxymetholone in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Oxymetholone in the drug label.

Overdosage

• There have been no reports of acute overdosage with anabolics.

Pharmacology

Mechanism of Action

There is limited information regarding Oxymetholone Mechanism of Action in the drug label.

Structure

• Anadrol®-50 (oxymetholone) Tablets for oral administration each contain 50 mg of the steroid oxymetholone, a potent anabolic and androgenic drug.

• The chemical name for oxymetholone is 17β-hydroxy-2-(hydroxymethylene)-17-methyl-5α-androstan-3-one. The structural formula is:

This image is provided by the National Library of Medicine.

Inactive Ingredients- lactose, magnesium stearate, povidone, starch

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Oxymetholone in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Oxymetholone in the drug label.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

• A two-year carcinogenicity study in rats given oxymetholone orally was conducted under the auspices of the US National Toxicology Program (NTP). A wide spectrum of neoplastic and non-neoplastic effects was observed. In male rats, no effects were classified as neoplastic in response to doses up to 150 mg/kg/day (5 times therapeutic exposures with 5 mg/kg based on body surface area). Female rats given 30 mg/kg/day (1 fold the maximum recommended clinical dose of 5 mg/kg/day based on the body surface area) had increased incidences of lung alveolar/bronchiolar adenoma and adenoma or carcinoma combined. At 100 mg/kg/day (about 3 fold the maximum recommended clinical dose of 5 mg/kg/day based on BSA), female rats had increased incidences of hepatocellular adenoma and adenoma or carcinoma combined; the combined incidence of squamous cell carcinoma and carcinoma of the sweat glands also was increased.

• Human data: There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with androgens in high doses. Withdrawal of the drugs did not lead to regression of the tumors in all cases.

• Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.

• In studies conducted under the auspices of the US National Toxicology Program, no evidence of genotoxicity was found using standard assays for mutagenicity, chromosomal aberrations, or induction of micronuclei in erythrocytes.

• Impairment of fertility was not tested directly in animal species. However, as noted below under adverse reactions, oligospermia in males and amenorrhea in females are potential adverse effects of treatment with ANADROL®-50 Tablets. Therefore, impairment of fertility is a possible outcome of treatment with ANADROL®-50 Tablets.

Clinical Studies

There is limited information regarding Clinical Studies of Oxymetholone in the drug label.

How Supplied

• ANADROL®-50 (oxymetholone) Tablets is supplied in bottles of 100 (NDC 68220-055-10) white scored tablets embossed with 0055 and ALAVEN. Keep out of reach of children. Dispense in a tight, light-resistant container.

Storage

• Store at controlled room temperature 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP].

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Oxymetholone in the drug label.

Precautions with Alcohol

• Alcohol-Oxymetholone interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

ANADROL-50

Look-Alike Drug Names

There is limited information regarding Oxymetholone Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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