Oxandrolone

OXANDROLONE- oxandrolone tablet
Eon Labs, Inc.

*Meets USP Dissolution Test 2

DESCRIPTION

Oxandrolone tablets USP 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:

Chemical Structure

Molecular Formula: C19 H30 O3

Molecular Weight: 306.44

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

CLINICAL PHARMACOLOGY

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.

INDICATIONS AND USAGE

Oxandrolone tablets USP are indicated as adjunctive therapy 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).

DRUG ABUSE AND DEPENDENCE

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

CONTRAINDICATIONS

1.
Known or suspected carcinoma of the prostate or the male breast.
2.
Carcinoma of the breast in females with hypercalcemia (androgenic anabolic steroids may stimulate osteolytic bone resorption).
3.
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.
4.
Nephrosis, the nephrotic phase of nephritis.
5.
Hypercalcemia.

WARNINGS

PELIOSIS HEPATIS, A CONDITION IN WHICH LIVER AND SOMETIMES SPLENIC TISSUE IS REPLACED WITH BLOOD-FILLED CYSTS, HAS BEEN REPORTED IN PATIENTS RECEIVING ANDROGENIC ANABOLIC STEROID THERAPY. THESE CYSTS ARE SOMETIMES PRESENT WITH MINIMAL HEPATIC DYSFUNCTION, BUT AT OTHER TIMES THEY HAVE BEEN ASSOCIATED WITH LIVER FAILURE. THEY ARE OFTEN 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 ARE ALSO REPORTED. MOST OFTEN THESE TUMORS ARE BENIGN AND ANDROGEN-DEPENDENT, BUT FATAL MALIGNANT TUMORS HAVE BEEN REPORTED. WITHDRAWAL OF DRUG OFTEN RESULTS IN REGRESSION OR CESSATION OF PROGRESSION OF THE TUMOR. 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 THAT ARE KNOWN TO BE ASSOCIATED WITH INCREASED RISK OF ATHEROSCLEROSIS ARE SEEN IN PATIENTS TREATED WITH ANDROGENS OR ANABOLIC STEROIDS. THESE CHANGES INCLUDE DECREASED HIGH-DENSITY LIPOPROTEINS AND SOMETIMES INCREASED LOW-DENSITY LIPOPROTEINS. THE CHANGES MAY BE VERY MARKED AND COULD HAVE A SERIOUS IMPACT ON THE RISK OF ATHEROSCLEROSIS AND CORONARY ARTERY DISEASE.

PRECAUTIONS

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).

General

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.

Information for Patients

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.

Geriatric Use:

Oxandrolone, at daily doses of 5 mg bid and 10 mg bid, was evaluated in four clinical trials involving a total of 339 patients with different underlying medical conditions. The maximum duration of treatment was 4 months with the average duration of treatment from 68.5 days to 94.7 days across the studies. A total of 172 elderly patients ( ≥ 65 years of age) received oxandrolone treatment. No significant differences in efficacy were detected between the 5 mg bid and 10 mg bid daily doses. The adverse event profiles were similar between the two age groups although the elderly, particularly in women, had a greater sensitivity to fluid retention and increases in hepatic transaminases. A single dose pharmacokinetic study in elderly volunteers revealed an increased half-life when compared to younger volunteers (see CLINICAL PHARMACOLOGY). Based on greater sensitivity to drug-induced fluid retention and transaminase elevations, a lower dose is recommended in the elderly (see DOSAGE AND ADMINISTRATION).

Laboratory Tests

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.

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