Fluoxymesterone Tablets

ANDROXY™ (Fluoxymesterone Tablets, USP) contains fluoxymesterone, a synthetic androgen. The androgens are steroids that develop and maintain primary and secondary male sex characteristics. Androgens are derivatives of cyclopentano-perhydrophenanthrene. Endogenous androgens are C-19 steroids with a side chain at C-17, and with two angular methyl groups. Testosterone is the primary endogenous androgen. Fluoxymesterone is a synthetic derivative of testosterone.

In their active form, all drugs in the class have a 17-beta-hydroxy group. 17-alpha-alkylation and halogenation at position 9 (fluoxymesterone) increase the pharmacologic activity per unit weight compared to testosterone when given orally. Fluoxymesterone is a white or practically white odorless, crystalline powder, melting at about 240°C with some decomposition. It is practically insoluble in water, sparingly soluble in alcohol and slightly soluble in chloroform. Chemically fluoxymesterone is designated 9-fluoro-11β, 17β-dihydroxy-17-methylandrost-4-en-3-one. Structurally it may be represented as follows:

ANDROXY™ (Fluoxymesterone Tablets, USP) for oral administration contains 10 mg of fluoxymesterone USP.

Inactive Ingredients: croscarmellose sodium, D&C Yellow #10 Aluminum Lake, FD&C Blue #1 Aluminum Lake, FD&C Yellow #6 Aluminum Lake, anhydrous lactose, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), and sodium lauryl sulfate.

Males

ANDROXY™ Tablets are indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone.

Primary hypogonadism (congenital or acquired)—Testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy.

Hypogonadotropic hypogonadism (congenital or acquired)—Idiopathic gonadotropin or luteinizing hormone-releasing hormone (LHRH) deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation. (Appropriate adrenal cortical and thyroid hormone replacement therapy are still necessary, however, and are actually of primary importance.)

If the above conditions occur prior to puberty, androgen replacement therapy will be needed during the adolescent years for development of secondary sexual characteristics. Prolonged androgen treatment will be required to maintain sexual characteristics in these and other males who develop testosterone deficiency after puberty.

Delayed puberty - ANDROXY™ (Fluoxymesterone Tablets, USP) may be used to stimulate puberty in carefully selected males with clearly delayed puberty. These patients usually have a familial pattern of delayed puberty that is not secondary to a pathological disorder; puberty is expected to occur spontaneously at a relatively late date. Brief treatment with conservative doses may occasionally be justified in these patients if they do not respond to psychological support. The potential adverse effect on bone maturation should be discussed with the patient and parents prior to androgen administration. An X-ray of the hand and wrist to determine bone age should be obtained every six months to assess the effect of treatment on the epiphyseal centers (see WARNINGS).

Females

Metastatic mammary cancer - ANDROXY™ (Fluoxymesterone Tablets, USP) may be used secondarily in women with advancing inoperable metastatic (skeletal) mammary cancer who are one to five years postmenopausal. Primary goals of therapy in these women include ablation of the ovaries. Other methods of counteracting estrogen activity are adrenalectomy, hypophysectomy, and/or antiestrogen therapy. This treatment has been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor. Judgment concerning androgen therapy should be made by an oncologist with expertise in this field.

ANDROXY™ (Fluoxymesterone Tablets, USP) 10 mg are round, green, scored compressed tablets debossed with 832 and 86 and are available in bottles of 100.

Dispense in a tight, light-resistant container as defined in the USP.

Store at controlled room temperature 15 – 30°C (59 – 86°F).

Keep out of reach of children.

Manufactured by : UPSHER-SMITH LABORATORIES, INC., Maple Grove, MN 55369. Revised: Jul 2013

Endocrine And Urogenital, Female

The most common side effects of androgen therapy are amenorrhea and other menstrual irregularities, inhibition of gonadotropin secretion, and virilization, including deepening of the voice and clitoral enlargement. The latter usually is not reversible after androgens are discontinued. When administered to a pregnant woman, androgens cause virilization of external genitalia of the female fetus.

Gynecomastia, and excessive frequency and duration of penile erections. Oligospermia may occur at high dosages (see CLINICAL PHARMACOLOGY).

Hirsutism, male pattern baldness, and acne.

Retention of sodium, chloride, water, potassium, calcium (see WARNINGS), and inorganic phosphates.

Nausea, cholestatic jaundice, alterations in liver function tests; rarely, hepatocellular neoplasms, peliosis hepatis, hepatic coma, and death (See WARNINGS).

Suppression of clotting factors II, V, VII, and X; bleeding in patients on concomitant anticoagulant therapy; and polycythemia.

Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.

Increased serum cholesterol.

Hypersensitivity; rarely, anaphylactoid reactions.

Drug Abuse And Dependence

ANDROXY™ Tablets are classified as a Schedule III controlled substance under the Anabolic Steroids Control Act of 1990.

When administered concurrently, the following drugs may interact with androgens:

Anticoagulants, oral—C-17 substituted derivatives of testosterone, such as methandrostenolone, have been reported to decrease the anticoagulant requirement. Patients receiving oral anticoagulant therapy require close monitoring especially when androgens are started or stopped.

Antidiabetic drugs and insulin—In diabetic patients, the metabolic effects of androgens may decrease blood glucose and insulin requirements.

ACTH and corticosteroids—Enhanced tendency toward edema. Use caution when giving these drugs together, especially in patients with hepatic or cardiac disease.

Oxyphenbutazone—May result in elevated serum levels of oxyphenbutazone.

Carcinogenesis

Testosterone has been tested by subcutaneous injection and implantation in mice and rats. The implant induced cervical-uterine tumors in mice, which metastasized in some cases. There is suggestive evidence that injection of testosterone into some strains of female mice increases their susceptibility to hepatoma. Testosterone is also known to increase the number of tumors and decrease the degree of differentiation of chemically-induced carcinomas of the liver in rats.

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 for the development of prostatic hypertrophy and prostatic carcinoma.

Pregnancy

Category X (see CONTRAINDICATIONS)

Nursing Mothers

It is not known whether androgens are excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from androgens, 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.

Pediatric Use

Androgen therapy should be used very cautiously in children and only by specialists who are aware of the adverse effects on bone maturation. Skeletal maturation must be monitored every six months by an X-ray of the hand and wrist (see INDICATIONS AND USAGE, and WARNINGS).

There have been no reports of acute overdosage with androgens.