Note: Androxy has been discontinued in the Unites States for >1 year.
Breast cancer, metastatic (females): Oral: Manufacturer labeling: 10 to 40 mg daily in divided doses for ≥3 months.
Delayed puberty (males): Oral: 2.5 to 20 mg daily for 4 to 6 months.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
Hepatic impairment prior to therapy: There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
Hepatic impairment during therapy: Discontinue use if abnormal liver function tests or cholestatic hepatitis with jaundice occur.
(For additional information see "Fluoxymesterone (United States: Not available): Pediatric drug information")
Note: Androxy has been discontinued in the US for more than 1 year. Dosage and duration of therapy depend upon age, sex, diagnosis, patient’s response to therapy, and appearance of adverse effects.
Delayed puberty: Adolescent Males: Typically not recommended for use before 14 years of age (Palmert 2012): Oral: Usual range: 2.5 mg to 10 mg daily, dose may be administered once daily or divided; reported range: 2.5 to 20 mg; most experts recommend a daily a dose of 2.5 mg for 6 to 60 months dependent upon clinical response (Melmed 2011; Strickland 1993); with testosterone therapy, response may be evaluated every 3 to 6 months and dose titrated as appropriate (Palmert 2012)
Male hypogonadism: Children ≥12 years and Adolescents (Han 2010; Young 2012): Oral: 2.5 to 20 mg daily; dose may be administered once daily or in divided doses for 4 to 6 months; some experts suggest beginning testosterone therapy with low doses and titrating gradually to prevent rapid over-virilization (Young 2012)
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Dosing adjustment for toxicity: Children ≥12 years and Adolescents:
Edema: All patients: If therapy is discontinued due to edema, may reinitiate (if indicated) at a reduced dosage.
Hypogonadism: In adult males, the following have been suggested: Hematocrit (HCT) >50%: Use is not recommended; if HCT >54% during therapy, discontinue until HCT falls to a safe level, assess for hypoxia and sleep apnea; if reinitiating therapy, reduce the dose (Bhasin 2010)
Children ≥12 years and Adolescents: There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
Children ≥12 years and Adolescents:
Hepatic impairment prior to therapy: There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
Hepatic impairment during therapy: Discontinue use if abnormal liver function tests or cholestatic hepatitis with jaundice occur.
Refer to adult dosing.
Edema: If therapy is discontinued due to edema, may reinitiate (if indicated) at a reduced dosage.
Hypercalcemia during therapy for metastatic breast cancer (females): Discontinue use.
Yes
Androxy has been discontinued in the US for more than 1 year.
C-III
Males: May be administered in single or divided doses. Females: Administer in divided doses.
Oral: May take without regard to food
Hazardous agent (NIOSH 2016 [group 2]).
Use appropriate precautions for receiving, handling, administration, and disposal. Gloves (single) should be worn during receiving, unpacking, and placing in storage. NIOSH recommends single gloving for administration of intact tablets or capsules (NIOSH 2016). Assess risk to determine appropriate containment strategy (USP-NF 2017).
Breast cancer, metastatic (females): Salvage treatment of inoperable metastatic breast cancer in postmenopausal females.
Delayed puberty (males): Replacement therapy in the treatment of delayed male puberty.
Halotestin [Great Britain] may be confused with Haldol brand name for haloperidol [U.S. and multiple international markets]
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.
Cardiovascular: Edema
Central nervous system: Anxiety, depression, headache, paresthesia
Dermatologic: Acne vulgaris, androgenetic alopecia
Endocrine & metabolic: Change in libido (decreased libido or increased libido), electrolyte disturbance (calcium, chloride, inorganic phosphate, potassium, and sodium retention), fluid retention, gynecomastia (males), hirsutism, hypercholesterolemia, menstrual disease (females; including amenorrhea)
Gastrointestinal: Gastrointestinal irritation, nausea, vomiting
Genitourinary: Benign prostatic hypertrophy (males), oligospermia (males; at higher doses), priapism (males), testicular atrophy (males), virilization (females; including clitoromegaly, deepening of the voice in females)
Hematologic & oncologic: Clotting factors suppression, polycythemia, prostate carcinoma (males)
Hepatic: Abnormal hepatic function tests, cholestatic jaundice, hepatic insufficiency
Hypersensitivity: Anaphylactoid reaction (non-immunologic anaphylaxis), hypersensitivity reaction
<1%, postmarketing, and/or case reports: Hepatic coma, hepatocellular neoplasm, hepatotoxicity (idiosyncratic; Chalasani 2014), peliosis hepatitis
Males with carcinoma of the breast or the prostate (known or suspected); women who are or may become pregnant
Concerns related to adverse effects:
• Cardiovascular events: Available studies are inconclusive regarding the risk of developing major adverse cardiovascular events such as nonfatal myocardial infarction, stroke, or cardiovascular death following testosterone use; most data are specific to men who were prescribed testosterone therapy (Basaria 2010; Corona 2014; Finkle 2014; Morgentaler 2015; Vigen 2013). Evaluate patients for cardiovascular risk factors prior to initiating therapy and monitor closely during therapy for cardiovascular events.
• 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 LFTs.
• Polycythemia: May increase hematocrit requiring dose adjustment or discontinuation. Withhold initial treatment in patients with hematocrit >48% or >50% if living at higher altitudes. Discontinue therapy if hematocrit exceeds 54% (Endocrine Society [Bhasin 2018]).
• Priapism: Priapism or excessive sexual stimulation may occur.
• Venous thromboembolism: Venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), have been reported with testosterone products (FDA Drug Safety Communication 2014). Evaluate patients with symptoms of pain, edema, warmth, and erythema in the lower extremity for DVT and those with acute shortness of breath for PE. Discontinue therapy if a venous thromboembolism is suspected.
Disease-related concerns:
• Benign prostatic hyperplasia: Androgens may worsen benign prostatic hyperplasia (BPH); do not use in patients with severe lower urinary tract symptoms (American Urological Association [AUA]/International Prostate Symptom Score [IPSS] >19) (Endocrine Society [Bhasin 2018]). Discontinue therapy if urethral obstruction develops in patients with BPH (use lower dose if restarted).
• Carbohydrate intolerance: May have adverse effects on glucose tolerance; use caution in patients with diabetes.
• Diseases exacerbated by fluid retention: Use with caution in patients with diseases that may be exacerbated by fluid retention, including cardiac 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.
• Prostate cancer: May increase the risk of prostate cancer. Withhold therapy pending urological evaluation in patients with palpable prostate nodule or induration, PSA >4 ng/mL, or PSA >3 ng/mL in men at high risk of prostate cancer (Endocrine Society [Bhasin 2018]).
• Renal impairment: Use with caution in renal impairment; not recommended for androgen replacement in hypogonadal males with severe lower urinary tract symptoms (eg, IPSS >19) (Endocrine Society [Bhasin 2018]).
• Sleep apnea: May potentiate sleep apnea; withhold initial treatment in patients with untreated obstructive sleep apnea (Endocrine Society [Bhasin 2018]).
Special populations:
• 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.
Other warnings/precautions:
• Abuse/misuse/diversion: Anabolic steroids may be abused, typically at doses higher than recommended and in combination with other anabolic androgenic steroids; abuse may be associated with serious cardiovascular and psychiatric adverse reactions. Inform patients of the serious adverse reactions associated with abuse of testosterone and anabolic androgenic steroids; if abuse is suspected, check serum testosterone levels (testosterone levels may be in the normal or subnormal range in men abusing synthetic testosterone derivatives). Consider the possibility of abuse in suspected patients who present with serious cardiovascular or psychiatric adverse events.
• Dependence: Drug dependence in individuals using approved doses of testosterone for approved indications has not been documented; however, dependence may occur when used outside of approved dosage/indications.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Agents with Blood Glucose Lowering Effects: Androgens may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Risk C: Monitor therapy
Ajmaline: Androgens may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased. Risk C: Monitor therapy
C1 inhibitors: Androgens may enhance the thrombogenic effect of C1 inhibitors. Risk C: Monitor therapy
Corticosteroids (Systemic): May enhance the fluid-retaining effect of Androgens. Risk C: Monitor therapy
CycloSPORINE (Systemic): Androgens may enhance the hepatotoxic effect of CycloSPORINE (Systemic). Androgens may increase the serum concentration of CycloSPORINE (Systemic). Management: Consider avoiding concomitant use of androgens and cyclosporine. If concomitant use is unavoidable, monitor serum cyclosporine concentrations and for signs and symptoms of hepatotoxicity. Cyclosporine dose reductions may be required. Risk D: Consider therapy modification
Hypertension-Associated Agents: May enhance the hypertensive effect of Androgens. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): Androgens may enhance the anticoagulant effect of Vitamin K Antagonists. Management: Monitor for increased effects of vitamin K antagonists if an androgen is initiated/dose increased, or decreased effects if androgen is discontinued/dose decreased. Significant reductions in vitamin K antagonist dose are likely required. Risk D: Consider therapy modification
Use is contraindicated in women who may become pregnant.
Use is contraindicated in women who are pregnant. May cause androgenic effects to the female fetus; clitoral hypertrophy, labial fusion, urogenital sinus defect, vaginal atresia, and ambiguous genitalia have been reported.
It is not known if fluoxymesterone is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother.
LFTs, lipid panel, hemoglobin and hematocrit (at 3 to 6 months then annually). Monitor urine and serum calcium and signs of virilization in women treated for breast cancer. Serum glucose (may be decreased by testosterone, monitor patients with diabetes). Monitor for cardiovascular events closely during therapy. Monitor PSA if clinically indicated. In prepubertal patients, perform radiologic examination of wrist and hand every 6 months.
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
Protein binding: 98%
Metabolism: Hepatic; enterohepatic recirculation
Half-life elimination: 10 hours (range: 10-100 minutes)
Excretion: Urine (90%); feces (6%)
Tablets (Androxy Oral)
10 mg (100): $577.84
Disclaimer: The pricing data provide a representative AWP and/or AAWP price from a single manufacturer of the brand and/or generic product, respectively. The pricing data should be used for benchmarking purposes only, and as such should not be used to set or adjudicate any prices for reimbursement or purchasing functions. Pricing data is updated monthly.
