Fluoxymesterone is a synthetic, orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated derivative of testosterone. 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.
As an AAS, fluoxymesterone is an agonist of the androgen receptor (AR), similarly to androgens like testosterone and DHT. Fluoxymesterone has been reported to be non-aromatizable due to steric hindrance by its C11β hydroxyl group, and hence is not considered to have a propensity for producing estrogenic effects such as gynecomastia or fluid retention. However, paradoxically, a case report of severe fluoxymesterone-induced gynecomastia exists, and gynecomastia associated with fluoxymesterone has also been reported in other publications.
Fluoxymesterone has an elimination half-life of approximately 9.2 hours, which is long relative to that of testosterone. In addition, unlike testosterone, fluoxymesterone has approximately 100% oral bioavailability, as the methyl group at the C17αposition of fluoxymesterone inhibits hepatic metabolism by enzymatic oxidation of 17β-hydroxyl, allowing its absorption into the bloodstream for transport around the body.
indications and usage:
In the male—Fluoxymesterone Tablets are indicated for
1.Replacement therapy in conditions associated with symptoms of deficiency or absence of endogenous testosterone.
（1）Primary hypogonadism (congenital or acquired) testicular failure due to cryptorchidism, bilateral torsion, orchitis , vanishing testis syndrome, or orchidectomy.
（2）Hypogonadotropic hypogonadism (congenital or acquired)—idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.
2.Delayed puberty, provided it has been definitely established as such, and is not just a familial trait.
In the female—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.
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 fortemporary withdrawal of the drug.
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 objective response.
1.Known hypersensitivity to the drug
2.Males with carcinoma of the breast
3.Males with known or suspected carcinoma of the prostate gland
4.Women known or suspected to be pregnant
5.Patients with serious cardiac, hepatic or renal disease
warnings and precautions:
Hypercalcemia may occur in immobilized patients and in patients with breast cancer. If this occurs, the drug should be discontinued.
Prolonged use of high doses of androgens (principally the 17-α alkyl-androgens) has been associated with development of hepatic adenomas, hepatocellular carcinoma, and peliosis hepatis—all potentially life-threatening complications.
Cholestatic hepatitis and jaundice may occur with 17-α-alkyl-androgens. Should this occur, the drug should be discontinued. This is reversible with discontinuation of the drug.
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.
Edema, with or without congestive heart failure, may be a serious complication in patients with pre-existing cardiac, renal or hepatic disease.
Gynecomastia may develop and occasionally persists in patients being treated for hypogonadism.
Androgen therapy should be used cautiously in males with delayed puberty. Androgens can accelerate bone maturation without producing compensatory gain in linear growth. The effect on bone maturation should be monitored by assessing bone age of the wrist and hand every six months.
This drug has not been shown to be safe and effective for the enhancement of athletic performance. Because of the potential risk of serious adverse health effects, this drug should not be used for such purpose.
Males with carcinoma of the breast or the prostate (known or suspected); women who are or may become pregnant.
pregnancy and lactation
Use is contraindicated in women who are or may become pregnant. May cause androgenic effects to the female fetus; clitoral hypertrophy, labial fusion, urogenital sinus defect, vaginal atresia, and ambiguous genitalia have been reported.
Males: Gynecomastia, frequent or persistent penile erections.
Females: Amenorrhea, other menstrual irregularities, inhibition of gonadotropin secretion, virilization (e.g., deepening of the voice, clitoral enlargement).
There have been no reports of acute overdosage with anabolics.
Store in cool dry place below 30℃. Protect from light.