Fluoxymesterone is a white or nearly white, odorless, crystalline powder, melting at or about 240° C, with some decomposition. It is practically insoluble in water, sparingly soluble in alcohol, and slightly soluble in chloroform.
The chemical name for fluoxymesterone is androst-4-en-3-one, 9-fluoro-11,17- dihydroxy-17-methyl-, (11β,17β)-. The molecular formula is C20H29FO3 and the molecular weight 336.45.
The structural formula is represented below:
Each HALOTESTIN (fluoxymesterone) tablet, for oral administration, contains 2 mg, 5 mg or 10 mg fluoxymesterone. Inactive ingredients: calcium stearate, corn starch, FD&C Yellow No. 5, lactose, sorbic acid, sucrose, tragacanth. In addition, the 2 mg tablet contains FD&C Yellow No. 6 and the 5 mg and 10 mg contain FD&C Blue No. 2.
In the male—HALOTESTIN (fluoxymesterone) Tablets are indicated for:
- Replacement therapy in conditions associated with symptoms of 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 LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.
- Delayed puberty, provided it has been definitely established as such, and is not just a familialtrait.
In the female—HALOTESTIN (fluoxymesterone) Tablets are indicated for palliation of androgen-responsive recurrent mammary cancer in women who are more than one year but less than five years postmenopausal, or who have been proven to have a hormone-dependent tumor as shown by previous beneficial response to castration.
DOSAGE AND ADMINISTRATION
The dosage will vary depending upon the individual, the condition being treated, and its severity. The total daily oral dose may be administered singly or in divided (three or four) doses.
Male hypogonadism: For complete replacement in the hypogonadal male, a daily dose of 5 to 20 mg will suffice in the majority of patients. It is usually preferable to begin treatment with full therapeutic doses which are later adjusted to individual requirements. Priapism is indicative of excessive dosage and is indication for temporary withdrawal of the drug.
Delayed puberty: Dosage should be carefully titrated utilizing a low dose, appropriate skeletal monitoring, and by limiting the duration of therapy to four to six months.
Inoperable carcinoma of the breast in the female: The recommended total daily dose for palliative therapy in advanced inoperable carcinoma of the breast is 10 to 40 mg. Because of its short action, fluoxymesterone should be administered to patients in divided, rather than single, daily doses to ensure more stable blood levels. In general, it appears necessary to continue therapy for at least one month for a satisfactory subjective response, and for two to three months for an objectiveresponse.
HALOTESTIN (fluoxymesterone) Tablets, round and scored, are available in the following strengths and colors:
2 mg (peach)
Bottles of 100 NDC 0009-0014-01
5 mg (light green)
Bottles of 100 NDC 0009-0019-06
10 mg (green)
Bottles of 30 NDC 0009-0036-03
Bottles of 100 NDC 0009-0036-04
Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP].
Distributed by Pharmacia and Upjohn Company, Division of Pfizer Inc, NY, NY 10017. Revised May 2002. FDA Rev date: 4/6/1992
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 can cause virilization of external genitalia of the female fetus.
Male: Gynecomastia, and excessive frequency and duration of penile erections. Oligospermia may occur at high dosage.
Skin and appendages
Hirsutism, male pattern of baldness, seborrhea, and acne.
Fluid and electrolyte disturbances
Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates.
Nausea, cholestatic jaundice, alterations in liver function tests, rarely hepatocellular neoplasms and peliosis hepatis (See WARNINGS).
Suppression of clotting factors II, V, VII, and X, bleeding in patients on concomitant anticoagulanttherapy, and polycythemia.
Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.
Hypersensitivity, including skin manifestations and anaphylactoid reactions.
Drug Abuse And Dependence
Controlled Substance Class: Fluoxymesterone is a controlled substance under the Anabolic Steroids Control Act, and HALOTESTIN (fluoxymesterone) Tablets has been assigned to Schedule III