PDR MEMBER LOGIN:
  • PDR Search

    Required field
  • Advertisement
  • CLASSES

    Androgens

    DEA CLASS

    Rx, schedule III

    DESCRIPTION

    Synthetic androgen given orally without loss of bioavailability; has less hepatic metabolism following oral administration when compared to testosterone; has been used in the management of congenital or acquired hypogonadism; pathological, delayed puberty; and as palliative treatment for breast cancer in postmenopausal women. -schedule C-III controlled substance.

    COMMON BRAND NAMES

    Android, Methitest, Testred, Virilon

    HOW SUPPLIED

    Android/Methyltestosterone/Testred/Virilon Oral Cap: 10mg
    Methitest/Methyltestosterone Oral Tab: 10mg

    DOSAGE & INDICATIONS

    For androgen replacement therapy, related to cryptorchidism.
    Oral dosage (capsules or tablets)
    Adults

    The recommended dose is 10 mg PO 3 times per day.

    Buccal dosage (buccal tablets)
    Adults

    The recommended dose is 5 mg 3 times per day, dissolved in the buccal cavity.

    For the treatment of delayed puberty in males.
    Oral dosage (capsules or tablets)
    Adolescents

    The recommended dose is 5 to 25 mg PO per day for a limited period, usually for 4 to 6 months.

    Buccal dosage (buccal tablets)
    Adolescents

    The recommended dose is 2.5 to 12.5 mg per day, dissolved in the buccal cavity, for a limited period, usually for 4 to 6 months.

    For palliative treatment of breast cancer in women.
    Oral dosage (capsules or tablets)
    Adults

    The recommended dose is 50 mg PO once daily up to 4 times per day. If a suitable response occurs within 2 to 4 weeks, the dose may be reduced to 50 mg 2 times per day.

    Buccal dosage (buccal tablets)
    Adults

    The recommended dose is 25 mg dissolved in the buccal cavity once daily up to 4 times per day. If a suitable response occurs within 2 to 4 weeks, the dose may be reduced to 25 mg 2 times per day.

    For androgen replacement therapy, including symptoms consistent with andropause†, erectile dysfunction (ED)†, or hypogonadism.
    NOTE: In the management of erectile dysfunction (ED), methyltestosterone therapy may increase libido and may or may not be effective at improving erectile function in hypogonadal men. Testosterone therapy, however, is not indicated for the treatment of erectile dysfunction in the patient with a normal serum testosterone concentration.
    Oral dosage (capsules or tablets)
    Adult males

    The recommended dose is 10 to 50 mg PO per day.

    Buccal dosage (buccal tablets)
    Adult males

    The recommended dose is 5 to 25 mg per day, dissolved in the buccal cavity.

    †Indicates off-label use

    MAXIMUM DOSAGE

    Adults

    The maximum dosage is dependent on indication for therapy.

    Elderly

    The maximum dosage is dependent on indication for therapy.

    Adolescents

    The maximum dosage is dependent on indication for therapy.

    Children

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Generally, androgen use is contraindicated in patients with severe hepatic dysfunction. Specific guidelines for dosage adjustment in hepatic impairment are not available; use caution in patients with mild to moderate hepatic disease.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Oral Administration

    Administer with food.

    Other Administration Route(s)

    Buccal Administration
    Place buccal tablet in the upper or lower buccal pouch between the cheek and gum. Allow to dissolve completely; do not swallow.
    Advise patients not to eat, drink, chew, or smoke while the buccal tablet is in place. Emphasize the importance of proper oral hygiene after the use of buccal tablets.

    STORAGE

    Android:
    - Store at controlled room temperature (between 68 and 77 degrees F)
    Methitest :
    - Avoid exposure to heat
    - Protect from light
    - Protect from moisture
    - Store at room temperature (between 59 to 86 degrees F)
    Testred:
    - Store at controlled room temperature (between 68 and 77 degrees F)
    Virilon:
    - Store at controlled room temperature (between 68 and 77 degrees F)

    CONTRAINDICATIONS / PRECAUTIONS

    Breast cancer, geriatric, hypercalcemia, prostate cancer, prostatic hypertrophy

    Methyltestosterone may stimulate the growth of cancerous tissue and is contraindicated in male patients with prostate cancer or breast cancer. Patients with prostatic hypertrophy should be treated with caution because of the possible development of malignancy; geriatric male patients may be more likely to have prostatic hypertrophy as an underlying condition. Methyltestosterone has induced osteolysis and should be used with caution in hypercalcemia, which may be exacerbated in patients with metastatic breast cancer; discontinue methyltestosterone in the event of new onset hypercalcemia. According to the Beers Criteria, methyltestosterone is considered a potentially inappropriate medication (PIM) for use in geriatric patients and should be avoided due to the potential for cardiac problems and its contraindication in men with prostate cancer. The Beers expert panel considers use of methyltestosterone for confirmed hypogonadism with clinical symptoms as acceptable in the elderly.

    Cardiac disease, coronary artery disease, heart failure, hepatic disease, myocardial infarction, renal disease

    During treatment with androgens, peripheral edema occurs because of water retention in association with sodium retention. Methyltestosterone should be used cautiously in severe cardiac disease, severe hepatic disease, and severe renal disease because of possible exacerbation of these conditions. Patients with heart failure, nephritis, nephrosis, coronary artery disease, myocardial infarction, or existing edema should also be treated with caution. Patients with severe hepatic disease or hepatic dysfunction also may be at risk of drug accumulation because of reduced clearance.

    Pregnancy

    Methyltestosterone is classified as FDA pregnancy category X; its use is absolutely contraindicated during pregnancy because of probable adverse effects on the fetus. Androgens have caused virilization of the external genitalia of the female fetus, including clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is dependent on the amount of drug given and the age of the fetus; these effects are most likely to occur in the female fetus when the drugs are given in the first trimester. Females of childbearing potential should use adequate methods of contraception, and should commence therapy during menstruation to ensure a nonpregnant state. If pregnancy occurs, the drug should be immediately discontinued and the patient should be counseled concerning the potential risks to the fetus.

    Breast-feeding

    Methyltestosterone distribution into breast milk has not been determined, but exposure to this androgen via breast-feeding may have adverse androgenic effects on the infant and the drug may also interfere with proper establishment of lactation in the mother. Because methyltestosterone is both structurally and mechanistically similar to testosterone, and testosterone products are to be avoided in lactating women, methyltestosterone should also be avoided in lactating women. Alternative methods to breast-feeding are recommended if methyltestosterone therapy is necessary. Historically, testosterone/androgens have been used adjunctively for lactation suppression.

    Diabetes mellitus

    Androgen therapy, such as methyltestosterone, can result in loss of diabetic control and should be used with caution in patients with diabetes mellitus. Close monitoring of blood glucose is recommended.

    Children

    Use of methyltestosterone in children should be undertaken only with extreme caution. Methyltestosterone may accelerate bone maturation without stimulating compensatory linear growth, sometimes resulting in compromised adult stature. If testosterone is administered to prepubertal males, radiographic examinations of the hand and wrist should be performed every 6 months to assess the rate of bone maturation and the effect of the drug on epiphyseal centers.

    ADVERSE REACTIONS

    Severe

    anaphylactoid reactions / Rapid / 0-1.0
    clitoromegaly / Delayed / Incidence not known
    virilization / Delayed / Incidence not known
    feminization / Delayed / Incidence not known
    new primary malignancy / Delayed / Incidence not known
    epididymitis / Delayed / Incidence not known
    prostatic hypertrophy / Delayed / Incidence not known
    pulmonary embolism / Delayed / Incidence not known
    thrombosis / Delayed / Incidence not known
    thromboembolism / Delayed / Incidence not known
    epiphyseal closure / Delayed / Incidence not known
    erythrocytosis / Delayed / Incidence not known

    Moderate

    dysphonia / Delayed / Incidence not known
    priapism / Early / Incidence not known
    fluid retention / Delayed / Incidence not known
    peripheral edema / Delayed / Incidence not known
    elevated hepatic enzymes / Delayed / Incidence not known
    hepatitis / Delayed / Incidence not known
    jaundice / Delayed / Incidence not known
    peliosis hepatis / Delayed / Incidence not known
    hypercalcemia / Delayed / Incidence not known
    polycythemia / Delayed / Incidence not known
    bleeding / Early / Incidence not known
    hypercholesterolemia / Delayed / Incidence not known
    depression / Delayed / Incidence not known

    Mild

    headache / Early / 1.0-10.0
    amenorrhea / Delayed / Incidence not known
    oligomenorrhea / Delayed / Incidence not known
    hirsutism / Delayed / Incidence not known
    gynecomastia / Delayed / Incidence not known
    alopecia / Delayed / Incidence not known
    weight gain / Delayed / Incidence not known
    acne vulgaris / Delayed / Incidence not known
    libido increase / Delayed / Incidence not known
    libido decrease / Delayed / Incidence not known
    nausea / Early / Incidence not known
    vomiting / Early / Incidence not known
    anxiety / Delayed / Incidence not known
    paresthesias / Delayed / Incidence not known

    DRUG INTERACTIONS

    Abarelix: (Major) Concomitant use of androgens or estrogens with abarelix is relatively contraindicated, as both could counteract the therapeutic effect of abarelix.
    Acarbose: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Alogliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Alogliptin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Alogliptin; Pioglitazone: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Alpha-glucosidase Inhibitors: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Anticoagulants: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Antithrombin III: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Apixaban: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Argatroban: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Betrixaban: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Bivalirudin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Canagliflozin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Canagliflozin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Cyclosporine: (Moderate) Androgens may increase concentrations of cyclosporine, potentially increasing the risk of nephrotoxicity. Until further data are available, close monitoring of cyclosporine serum concentrations is prudent during coadministration with androgens.
    Dabigatran: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Dalteparin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Danaparoid: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Dapagliflozin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Dapagliflozin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Dapagliflozin; Saxagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Darbepoetin Alfa: (Moderate) Androgens are known to stimulate erythropoiesis. Concurrent administration of androgens can increase the patient's response to darbepoetin alfa, reducing the amount required to treat anemia.
    Degarelix: (Major) Concomitant use of androgens with degarelix is relatively contraindicated, as androgens could counteract the therapeutic effect of degarelix.
    Desirudin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Dipeptidyl Peptidase-4 Inhibitors: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Edoxaban: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Empagliflozin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Empagliflozin; Linagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Empagliflozin; Linagliptin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Empagliflozin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Enoxaparin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Epoetin Alfa: (Moderate) Androgens are known to stimulate erythropoiesis. Concurrent administration of androgens can increase the patient's response to epoetin alfa, reducing the amount required to treat anemia. Because adverse reactions have been associated with an abrupt increase in blood viscosity, this drug combination should be avoided, if possible. Further evaluation of this combination needs to be made.
    Ertugliflozin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Ertugliflozin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Ertugliflozin; Sitagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Fondaparinux: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Glipizide; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Glyburide; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Goserelin: (Major) Avoid concurrent use of androgens with gonadotropin releasing hormone (GnRH) agonists such as goserelin. Goserelin inhibits steroidogenesis; concomitant use with androgens may counteract this therapeutic effect.
    Heparin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Histrelin: (Major) Avoid concurrent use of androgens with gonadotropin releasing hormone (GnRH) agonists such as histrelin. Histrelin inhibits steroidogenesis; concomitant use with androgens may counteract this therapeutic effect.
    Imipramine: (Minor) Coadministration of methyltestosterone with imipramine has led to dramatic paranoia in a limited number of patients.
    Incretin Mimetics: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Insulins: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Lepirudin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Leuprolide: (Major) Leuprolide inhibits steroidogenesis. While no drug interactions have been reported with leuprolide, therapy with androgens would be relatively contraindicated and would counteract the therapeutic effect of leuprolide.
    Leuprolide; Norethindrone: (Major) Leuprolide inhibits steroidogenesis. While no drug interactions have been reported with leuprolide, therapy with androgens would be relatively contraindicated and would counteract the therapeutic effect of leuprolide.
    Linagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Linagliptin; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Meglitinides: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Metformin; Repaglinide: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Metformin; Rosiglitazone: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Metformin; Saxagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Metformin; Sitagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Methotrexate: (Moderate) Methyltestosterone has been associated with hepatotoxicity; caution is recommended in combining 17-alpha-alkylated androgens in combination with other medications that have potential hepatotoxic effects (e.g., methotrexate). Monitor liver function periodically; if liver function becomes abnormal or clinical symptoms (e.g., jaundice) develop, discontinue the androgen and determine the etiology. Androgen-induced jaundice is reversible whtih medication discontinuation.
    Methoxy polyethylene glycol-epoetin beta: (Moderate) Androgens are known to stimulate erythropoiesis. Despite the fact that endogenous generation of erythropoietin is depressed in patients with chronic renal failure, other tissues besides the kidney can synthesize erythropoietin, albeit in small amounts. Concurrent administration of androgens can increase the patient's response to MPG-epoetin beta, reducing the amount required to treat anemia. Because adverse reactions have been associated with an abrupt increase in blood viscosity, this drug combination should be avoided, if possible. Further evaluation of this combination needs to be made.
    Miglitol: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Nafarelin: (Major) Gonadotropin releasing hormone (GnRH) agonists (i.e.,nafarelin) inhibit steroidogenesis, therefore the concomitant use of these agents with androgens may counteract this therapeutic effect. Avoid concurrent use of androgens with GnRH agonists.
    Pentosan: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Pioglitazone; Metformin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Pramlintide: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Rivaroxaban: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Saw Palmetto, Serenoa repens: (Major) Drug interactions with Saw palmetto, Serenoa repens have not been specifically studied or reported. Saw palmetto extracts appear to have antiandrogenic effects. The antiandrogenic effects of Saw palmetto, Serenoa repens would be expected to antagonize the actions of androgens; it would seem illogical for patients taking androgens to use this herbal supplement.
    Saxagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    SGLT2 Inhibitors: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Simvastatin; Sitagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Sitagliptin: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Sulfonylureas: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Thiazolidinediones: (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, may decrease antidiabetic agent dosage requirements. Monitor blood glucose and HbA1C when these drugs are used together.
    Tinzaparin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.
    Triptorelin: (Major) Gonadotropin releasing hormone (GnRH) agonists (i.e.,triptorelin) inhibit steroidogenesis, therefore the concomitant use of these agents with androgens may counteract this therapeutic effect. Avoid concurrent use of androgens with GnRH agonists.
    Warfarin: (Moderate) Methyltestosterone can increase the effects of anticoagulants through reduction of procoagulant factor. Patients receiving oral anticoagulant therapy should be closely monitored, especially when methyltestosterone treatment is initiated or discontinued.

    PREGNANCY AND LACTATION

    Pregnancy

    Methyltestosterone is classified as FDA pregnancy category X; its use is absolutely contraindicated during pregnancy because of probable adverse effects on the fetus. Androgens have caused virilization of the external genitalia of the female fetus, including clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is dependent on the amount of drug given and the age of the fetus; these effects are most likely to occur in the female fetus when the drugs are given in the first trimester. Females of childbearing potential should use adequate methods of contraception, and should commence therapy during menstruation to ensure a nonpregnant state. If pregnancy occurs, the drug should be immediately discontinued and the patient should be counseled concerning the potential risks to the fetus.

    Methyltestosterone distribution into breast milk has not been determined, but exposure to this androgen via breast-feeding may have adverse androgenic effects on the infant and the drug may also interfere with proper establishment of lactation in the mother. Because methyltestosterone is both structurally and mechanistically similar to testosterone, and testosterone products are to be avoided in lactating women, methyltestosterone should also be avoided in lactating women. Alternative methods to breast-feeding are recommended if methyltestosterone therapy is necessary. Historically, testosterone/androgens have been used adjunctively for lactation suppression.

    MECHANISM OF ACTION

    Mechanism of Action: The function of androgens in male development begins in the fetus, is crucial during puberty, and continues to play an important role in the adult male. Women also secrete small amounts of androgen from the ovaries. The secretion of androgens from the adrenal cortex is insufficient to maintain male sexuality.Normally, endogenous androgens stimulate RNA polymerase, increasing protein production. These proteins are responsible for normal male sexual development, including the growth and maturation of the prostate, seminal vesicle, penis, and scrotum. During puberty, androgens cause a sudden increase in growth and development of muscle, with a redistribution of body fat. Changes associated with endogenous androgens also take place in the larynx and vocal cords, deepening the voice. Puberty is completed with beard development and growth of body hair. Fusion of the epiphyses and termination of growth is governed by the androgens, as is the maintenance of spermatogenesis. Androgens have a high lipid solubility, enabling them to rapidly enter cells of target tissues. Increased androgen plasma levels suppress gonadotropin-releasing hormone, reducing endogenous testosterone, luteinizing hormone, and follicle-stimulating hormone through a negative-feedback mechanism. Exogenous replacement therapy stimulates the above process when endogenous supply is inadequate.

    PHARMACOKINETICS

    Methyltestosterone is administered orally or via the buccal cavity. Methyltestosterone has an elimination half-life of 2.5—3.5 hours, somewhat longer than that of testosterone. Excretion of glucuronide and sulfate conjugates is primarily renal; there is little excretion of unchanged drug. Small amounts are eliminated in the feces.

    Oral Route

    Bioavailability is roughly 50% after oral administration. Peak serum concentrations are achieved about 2 hours after tablet administration.

    Other Route(s)

    Buccal Route
    After administration of methyltestosterone via the buccal cavity, first-pass hepatic metabolism is bypassed.