Oxandrolone Tablets USP*

*Meets USP Dissolution Test 2

Oxandrolone oral tablets contain 2.5 mg or 10 mg of the anabolic steroid oxandrolone. Oxandrolone is 17β-hydroxy-17α-methyl-2-oxa-5α-androstan-3-one with the following structural formula:

Molecular Formula: C₁₉H₃₀O₃

Molecular Weight: 306.44

Inactive ingredients include: hypromellose, lactose monohydrate, pregelatinized starch, and magnesium stearate.

Anabolic steroids are synthetic derivatives of testosterone. Certain clinical effects and adverse reactions demonstrate the androgenic properties of this class of drugs. Complete dissociation of anabolic and androgenic effects has not been achieved. The actions of anabolic steroids are therefore similar to those of male sex hormones with the possibility of causing serious disturbances of growth and sexual development if given to young children. Anabolic steroids suppress the gonadotropic functions of the pituitary and may exert a direct effect upon the testes.

During exogenous administration of anabolic androgens, endogenous testosterone release is inhibited through inhibition of pituitary luteinizing hormone (LH). At large doses, spermatogenesis may be suppressed through feedback inhibition of pituitary follicle-stimulating hormone (FSH).

Anabolic steroids have been reported to increase low-density lipoproteins and decrease high-density lipoproteins. These levels revert to normal on discontinuation of treatment.

In a single dose pharmacokinetic study of Oxandrolone in elderly subjects, the mean elimination half-life was 13.3 hours. In a previous single dose pharmacokinetic study in younger volunteers, the mean elimination half-life was 10.4 hours.

No significant differences between younger and elderly volunteers were found for time to peak, peak plasma concentration or AUC after a single dose of Oxandrolone. The correlation between plasma level and therapeutic effect has not been defined.

Oxandrolone is indicated to offset the protein catabolism associated with prolonged administration of corticosteroids, and for the relief of the bone pain frequently accompanying osteoporosis (see DOSAGE AND ADMINISTRATION).

Oxandrolone is classified as a controlled substance under the Anabolic Steroids Control Act of 1990 and has been assigned to Schedule III (non-narcotic).

• Known or suspected carcinoma of the prostate or the male breast.
• Carcinoma of the breast in females with hypercalcemia (androgenic anabolic steroids may stimulate osteolytic bone resorption).
• Pregnancy, because of possible masculinization of the fetus. Oxandrolone has been shown to cause embryotoxicity, fetotoxicity, infertility, and masculinization of female animal offspring when given in doses 9 times the human dose.
• Nephrosis, the nephrotic phase of nephritis.
• Hypercalcemia.

Concurrent dosing of oxandrolone and warfarin may result in unexpectedly large increases in the International Normalized Ratio (INR) or prothrombin time (PT). When oxandrolone is prescribed to patients 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 (See PRECAUTIONS, Drug Interactions).

Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly). Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Some virilizing changes in women are irreversible even after prompt discontinuance of therapy and are not prevented by concomitant use of estrogens. Menstrual irregularities may also occur.

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

The physician should instruct patients to report immediately any use of warfarin and any bleeding.

The physician should instruct patients to report any of the following side effects of androgens:

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

Females: Hoarseness, acne, changes in menstrual periods, or more facial hair.

All patients: Nausea, vomiting, changes in skin color, or ankle swelling.

Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of therapy (see WARNINGS).

Because of the hepatotoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically.

Periodic (every 6 months) x-ray examinations of bone age should be made during treatment of children to determine the rate of bone maturation and the effects of androgen therapy on the epiphyseal centers.

Androgenic anabolic steroids have been reported to increase low-density lipoproteins and decrease high-density lipoproteins. Therefore, caution is required when administering these agents to patients with a history of cardiovascular disease or who are at risk for cardiovascular disease. Serum determination of lipid levels should be performed periodically and therapy adjusted accordingly.

Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of anabolic steroids.

It is not known whether anabolic steroids are excreted in human milk. Because of the potential of serious adverse reactions in nursing infants from oxandrolone, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

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 adult height. Androgenic anabolic steroid therapy should be used very cautiously in children and only by speciauls who are aware of the effects on bone maturation (see WARNINGS).

Patients with moderate to severe COPD or COPD patients who are unresponsive to bronchodilators should be monitored closely for COPD exacerbation and fluid retention.

The following adverse reactions have been associated with use of anabolic steroids:

Cholestatic jaundice with, rarely, hepatic necrosis and death. Hepatocellular neoplasms and peliosis hepatis with long-term therapy (see WARNINGS).

Reversible changes in liver function tests also occur including increased bromsulfophthalein (BSP) retention, changes in alkaline phosphatase and increases in serum bilirubin, aspartate aminotransferase (AST, SGOT) and alanine aminotransferase (ALT, SGPT).

Clitoral enlargement, menstrual irregularities.

CNS

Habituation, excitation, insomnia, depression, and changes in libido.

Hematologic

Bleeding in patients on concomitant anticoagulant therapy.

Breast

Gynecomastia.

Larynx

Deepening of the voice in females.

Hair

Hirsutism and male pattern baldness in females.

Skin

Acne (especially in females and prepubertal males).

Skeletal

Premature closure of epiphyses in children (see PRECAUTIONS, Pediatric Use).

Fluid and Electrolytes

Edema, retention of serum electrolytes (sodium chloride, potassium, phosphate, calcium).

Metabolic/Endocrine

Decreased glucose tolerance (see PRECAUTIONS, Laboratory Tests), increased creatinine excretion, increased serum levels of creatinine phosphokinase (CPK). Masculinization of the fetus. Inhibition of gonadotropin secretion.

No symptoms or signs associated with overdosage have been reported. It is possible that sodium and water retention may occur.

The oral LD50 of oxandrolone in mice and dogs is greater than 5,000 mg/kg. No specific antidote is known, but gastric lavage may be used.

Therapy with anabolic steroids is adjunctive to and not a replacement for conventional therapy. The duration of therapy with Oxandrolone will depend on the response of the patient and the possible appearance of adverse reactions. Therapy should be intermittent.

The response of individuals to anabolic steroids varies. The daily adult dosage is 2.5 mg to 20 mg given in 2 to 4 divided doses. The desired response may be achieved with as little as 2.5 mg or as much as 20 mg daily. A course of therapy of 2 to 4 weeks is usually adequate. This may be repeated intermittently as indicated.

For children the total daily dosage of Oxandrolone is ≤0.1 mg per kilogram body weight or ≤ 0.045 mg per pound of body weight. This may be repeated intermittently as indicated.

Oxandrolone Tablets USP are supplied as follows:

2.5 mg Tablets: white, modified oval-shaped, debossed " E271" on one side and bisected on the reverse side.

• Bottles of 100
• Bottles of 1000

10 mg Tablets: white, capsule-shaped, debossed " E272" on one side and plain on the reverse side.

• Bottles of 60
• Bottles of 100
• Bottles of 1000

Store at 20° to 25°C (68 to 77°F) [see USP Controlled Room Temperature].

Sandoz Inc.

Princeton, NJ 08540

Rev. 03/07

MF0271REV03/07

OS8072