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Pronunciation: METH-ill-tess-TAHS-ter-ohn
Class: Androgen

Trade Names

- Capsules 10 mg

- Tablets 10 mg

- Tablets, buccal 10 mg
- Tablets 25 mg

- Capsules 10 mg


Promotes growth and development of male reproductive organs, maintains secondary sex characteristics, increases protein anabolism, and decreases protein catabolism.

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Because methyltestosterone is less extensively metabolized by the liver and has a longer t ½ than testosterone, methyltestosterone is more suitable than testosterone for oral administration.

Indications and Usage

Replacement therapy in the following conditions associated with a deficiency or absence of endogenous testosterone: primary hypogonadism (congenital or acquired); hypogonadotropic hypogonadism (congenital or acquired); delayed puberty (males); used secondarily in advancing inoperable metastatic (skeletal) mammary cancer (females).


Men with carcinoma of the breast; men with known or suspected carcinoma of the prostate gland; women known or suspected to be pregnant; hypersensitivity to any component of the product.

Dosage and Administration

Congenital or Acquired Primary Hypogonadism, Hypogonadotropic Hypogonadism
Adults (men)

PO 10 to 50 mg/day.

Delayed Puberty
Adults (men)

PO Doses are generally in the lower range of the doses for hypogonadism and for a limited duration (eg, 4 to 6 mo).

Metastatic Breast Carcinoma
Adults (women)

PO 50 to 200 mg/day.


Store tablets and capsules at ambient room temperature (59° to 86°F). Protect from light, moisture, and heat.

Drug Interactions


Blood glucose levels may be reduced by methyltestosterone, decreasing insulin requirements.

Oral anticoagulants (eg, warfarin)

Effects of oral anticoagulant may be increased. Dosage reduction may be required.

Laboratory Test Interactions

Thyroxine-binding globulin levels may be decreased; however, thyroid hormone levels remain unchanged and there is no clinical evidence of thyroid dysfunction.

Adverse Reactions


Increased and decreased libido; headache; anxiety; depression; generalized paresthesia.


Hirsutism; male pattern baldness; acne.


Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates.




Amenorrhea, menstrual irregularities, inhibition of gonadotropin secretion, virilization (including deepening of voice and clitoral enlargement for women); gynecomastia, excessive frequency and duration of penile erection, oligospermia (men).


Suppression of clotting factors II, V, VII, and X; bleeding in patients with polycythemia.


Cholestatic jaundice; alterations in LFTs; hepatocellular neoplasms; peliosis hepatitis.


Increased serum cholesterol.


Anaphylactoid reactions.



Category X .




Use with caution and only by specialists aware of the adverse effects on bone maturation.


Elderly men may be at increased risk of developing prostatic hypertrophy or carcinoma.

Athletic performance

Abuse of this agent to enhance athletic performance has potential risk of serious adverse reactions.

Delayed puberty

Because bone maturation without producing compensatory linear growth can occur, use with caution in males with delayed puberty.


Use with caution in patients with conditions that might be affected by fluid retention (eg, renal, hepatic, cardiac disease).


May occur and persist in patients being treated for hypogonadism.

Hepatic effects

Cholestatic hepatitis and jaundice may occur. Prolonged use of high doses may result in hepatic adenomas, hepatocellular carcinoma, and peliosis hepatitis.


May cause hypercalcemia when used in patients with breast cancer.

Oligospermia and reduced ejaculatory volume

May occur after prolonged use.


May be indicative of excessive dosage.


May occur in women using high-dose androgens.

Patient Information

  • Advise patient to review the patient information leaflet before starting therapy and with each refill.
  • Instruct patient to take as prescribed and not to change dose or stop taking unless advised by health care provider.
  • Advise patient taking tablets or capsules that medication can be taken without regard to meals, but to take with food if GI upset occurs.
  • Advise patient using buccal tablets to place buccal tablet between the cheek and gum and allow to dissolve. Caution patient not to chew or swallow tablet and avoid eating or drinking anything while the tablet is in the mouth.
  • Advise patient to regularly inspect gum region where buccal system is applied and to report any abnormality (including gum tenderness or irritation) to health care provider.
  • Advise women to immediately report any of the following to health care provider: deepening of voice, unusual hair growth, acne, enlargement of clitoris, menstrual irregularity.
  • Advise men to report any of the following to health care provider: frequent, persistent erections, difficult or painful urination, urinary hesitancy, inability to urinate.
  • Advise patient to report any of the following to health care provider: persistent nausea or vomiting, yellowing of skin or eyes, ankle swelling, any other unusual symptom.
  • Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
  • Caution patient that medication has not been shown to be safe or effective for the enhancement of athletic performance and not to use for this purpose.
  • Advise women of childbearing potential to use effective contraception during therapy.

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