Fluoxymesterone

Other drugs may interact with fluoxymesterone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Contraindications

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• Males with breast cancer or known or suspected prostate cancer.a b c

• Known or suspected pregnancy.b c

• Some manufacturers state that fluoxymesterone is contraindicated in patients with serious cardiac, hepatic, or renal disease.a b

• Known hypersensitivity to fluoxymesterone or any ingredient in the formulation.a b

Warnings/Precautions

Warnings

May cause fetal harm; dose-related virilization of the external genitalia (e.g., clitoral hypertrophy, labial fusion of the external genital fold to form a scrotal-like structure, abnormal vaginal development, persistence of a urogenital sinus) of female fetus reported, particularly when exposure to androgens occurs during the 1st trimester.a c If used during pregnancy or patient becomes pregnant, apprise of potential fetal hazard;c contraindicated in pregnant women.a b c (See Contraindications under Cautions.)

Potentially serious and/or life-threatening adverse hepatic effects (e.g., peliosis hepatis, hepatic adenomas, hepatocellular carcinoma) associated with prolonged use of high dosages of androgens.a b c Discontinuance of androgen therapy following development of hepatocellular carcinoma dose not always result in regression of the tumor.a

If cholestatic hepatitis or jaundice occurs, or if liver function test results become abnormal during therapy, discontinue the drug and investigate the etiology of these disorders.a b c Drug-induced jaundice usually is reversible following discontinuance of the drug.a b c

Periodic liver function evaluation recommended.a b c

Priapism or excessive sexual stimulation possible, especially in geriatric men.a b Oligospermia and decreased ejaculatory volume also may occur in men receiving excessive dosage or prolonged administration.a b Acute urethral obstruction possible in patients with benign prostatic hypertrophy.b If any of these adverse effects occur, discontinue the drug temporarily.a b If therapy is restarted, use lower dosages.a b

Possible increased risk for the development of prostatic hyperplasia and prostate cancer, particularly in geriatric patients.a b c

Possible increased or decreased libido.b c

Gynecomastia frequently develops and occasionally persists in patients being treated for hypogonadism.a b c

Edema, with or without CHF, possible as a result of sodium and water retention and may be a serious complication in patients with preexisting cardiac, renal, or hepatic disease.a b c (See Contraindications under Cautions.) If edema occurs and is considered a serious complication, discontinue drug and, if necessary, initiate diuretic therapy.a c If therapy is restarted, use lower dosages.c

Retention of potassium and inorganic phosphates also has occurred.a b c

Possible hypercalcemia resulting from osteolysis, especially in immobile patients and those with metastatic breast cancer.a b c In patients with cancer, hypercalcemia may indicate progression of metastases to the bone.a c Monitor urine and serum calcium concentrations frequently during the course of androgen therapy in women with metastatic breast cancer.b c If hypercalcemia occurs, discontinue the druga b c and institute appropriate measures.c

Potential for serious adverse effects (e.g., increased aggression, antisocial behavior, manic episode, depression, changes in libido, increased risk of cardiovascular disease, hepatotoxicity) associated with misuse and abuse of androgens (see Misuse and Abuse under Uses); fluoxymesterone preparations currently subject to control under the Federal Controlled Substances Act of 1970, as amended by the Anabolic Steroids Control Act of 1990 and 2004 as schedule III (C-III) drugs.a b c d

Sensitivity Reactions

Halotestin tablets contain tartrazine (FD&C Yellow No. 5), which may cause allergic reactions, including bronchial asthma in susceptible individuals.b Incidence of tartrazine sensitivity is low, but it frequently occurs in patients who are sensitive to aspirin.b

General Precautions

Virilization, including deepening of the voice, hirsutism, acne, menstrual irregularities, and clitoral enlargement, occurs commonly in females receiving high-dose fluoxymesterone therapy;a b c changes may not be reversible following discontinuance of the drug.a

Monitor women receiving fluoxymesterone therapy for signs of virilization.a b c If virilization occurs, discontinue therapy.a b c

Possible polycythemia, especially with high dosages of androgens.b c Perform periodic hemoglobin and hematocrit determinations in patients receiving high dosagesa c or long-term administration of fluoxymesterone.a b

Androgens may alter serum cholesterol concentration;b c therefore, administer with caution in patients with history of MI or CAD.c

Monitor serum cholesterol throughout therapy; adjust therapy accordinglyc .

Specific Populations

Category X.b c f (See Fetal/Neonatal Morbidity and also Contraindications, under Cautions.)

Not known whether fluoxymesterone is distributed into milk.a c Discontinue nursing or the drug.a b c

May accelerate bone maturation without producing compensatory gain in linear growth, possibly resulting in compromised adult stature.a b c The younger the child, the greater the risk of fluoxymesterone compromising final mature stature.a c Use with extreme caution in children and only under the supervision of a specialist who is aware of the adverse effects of fluoxymesterone on bone maturation.a Perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.a b c

Possible risk of developing prostatic hypertrophy and carcinoma during androgen therapy.a b c

Males, especially geriatric patients, may become overly sexually stimulated during therapy and such stimulation may be a sign of excessive dosage.a Carefully monitor males for the development of excessive sexual stimulation.a

Common Adverse Effects

Males: Gynecomastia,a b c frequent or persistent penile erections.b c

Females: Amenorrhea,a b c other menstrual irregularities,a b c inhibition of gonadotropin secretion,a b c virilization (e.g., deepening of the voice, clitoral enlargement).a b c

• It is used to treat low testosterone levels.
• It is used for delayed puberty in certain male children.
• It is used to treat breast cancer in women.
• It may be given to you for other reasons. Talk with the doctor.

• Tell all of your health care providers that you take fluoxymesterone. This includes your doctors, nurses, pharmacists, and dentists.
• This medicine does not help you to be better at sports.
• If you have high blood sugar (diabetes), you will need to watch your blood sugar closely.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take this medicine.
• If you are taking warfarin, talk with your doctor. You may need to have your blood work checked more closely while you are taking it with fluoxymesterone.
• This medicine is an anabolic steroid. Anabolic steroid drugs have been abused and misused before. Anabolic steroid abuse can lead to dependence and very bad health problems. These health problems include heart or blood vessel problems, stroke, liver problems, and mental or mood problems. Talk with the doctor.
• This medicine may affect sperm in men. This may affect being able to father a child. Talk with the doctor.
• If you are 65 or older, use this medicine with care. You could have more side effects.
• Use with care in children. Talk with the doctor.
• This medicine may affect growth in children and teens in some cases. They may need regular growth checks. Talk with the doctor.
• This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking fluoxymesterone, call your doctor right away.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high calcium levels like weakness, confusion, feeling tired, headache, upset stomach and throwing up, hard stools (constipation), or bone pain.
• Shortness of breath, a big weight gain, or swelling in the arms or legs.
• Change in color of skin.
• Low mood (depression).
• A burning, numbness, or tingling feeling that is not normal.
• Upset stomach or throwing up.
• For males, erections (hard penis) that happen often or that last a long time.
• For females, a deep voice, facial hair, pimples, or period changes.
• Very bad and sometimes deadly liver problems have happened with this medicine. Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about fluoxymesterone, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about fluoxymesterone. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using fluoxymesterone.

Review Date: October 4, 2017

• Androxy

• Androgen

Synthetic derivative of testosterone; responsible for the normal growth and development of male sex hormones, male sex organs, and maintenance of secondary sex characteristics; large doses suppress endogenous testosterone release

Absorption

Rapid

Metabolism

Hepatic; enterohepatic recirculation

Excretion

Urine (90%); feces (6%)

Half-Life Elimination

10 hours (range: 10-100 minutes)

Protein Binding

98%

Concerns related to adverse effects:

• Dyslipidemia: Anabolic steroids may alter serum lipid profile; use caution in patients with history of myocardial infarction or coronary artery disease.

• Gynecomastia: May cause gynecomastia.

• Hepatic effects: Prolonged use of high doses of oral androgens has been associated with serious hepatic effects (eg, peliosis hepatis, hepatic neoplasms, cholestatic hepatitis, jaundice). Discontinue use in patients with cholestatic hepatitis with jaundice or abnormal liver function tests.

Disease-related concerns:

• Carbohydrate intolerance: May have adverse effects on glucose tolerance; use caution in patients with diabetes.

• Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, migraine, seizure disorder, renal impairment); may cause fluid retention.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Hypercalcemia: Use with caution in patients with breast cancer or immobilization; may cause hypercalcemia by stimulating osteolysis. Discontinue use if hypercalcemia occurs; may indicate bony metastasis.

Special populations:

• Elderly: Elderly patients may be at greater risk for prostatic hyperplasia and prostate cancer; use with caution.

• Pediatric: May accelerate bone maturation without producing compensatory gain in linear growth in children. In prepubertal children, perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.

• Women: During treatment for metastatic breast cancer, women should be monitored for signs of virilization (eg, deepening of voice, hirsutism, acne, clitoromegaly, menstrual irregularities); discontinue use with evidence of mild virilization to prevent irreversible symptoms.

2.5 to 20 mg orally per day; generally in the lower range of 2.5 to 10 mg orally per day, taken in one single dose or in divided doses for a limited duration (e.g., 4 to 6 months).

Comments:
-Various dosage regimens have been used: some call for lower dosages initially with gradual increases as puberty progresses, with or without a decrease to maintenance level; other regimens call for higher dosage to induce pubertal changes and lower dosage for maintenance after puberty.
-The chronological and skeletal ages should be taken into consideration in determining the initial dose and when adjusting the dose.
-Brief treatment with conservative doses may occasionally be justified in these male patients if they do not respond to psychological support.
-Patients and parents should be advised of the potential adverse effect on bone maturation prior to treatment.
-Hand and wrist x-rays to determine bone age should be obtained every 6 months to assess the effect of treatment on the epiphyseal centers.

Use: Stimulate puberty in adolescent males with clearly delayed puberty

Dosage adjustments will depend on age, sex, diagnosis, patient response to treatment, and appearance of adverse effects.