Methyltestosterone

Name: Methyltestosterone

Pharmacology

Half-Life: 10-100 min

Peak Plasma Time: 1-2 hr

Bioavailability: absorbed from GI tract & oral mucosa

Protein Bound: 98%

Metabolism: less extensively undergoes first-pass hepatic metabolism than testosterone, suitable for PO admin

Excretion

Urine: 90%

Feces: 6%

Mechanism of Action

Synthetic testosterone derivatives with anabolic & androgenic activity; promoting growth & development of male sex organs & maintaining secondary sex characteristics in androgen-deficient males

Indications

  1. Males
    Androgens are indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone:
    1. Primary hypogonadism (congenital or acquired) - testicular failure due to cryptorchidism, bilateral torsions, 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. If the above conditions occur prior to puberty, androgen replacement therapy will be needed during the adolescent years for development of secondary sexual characteristics. Prolonged androgen treatment will be required to maintain sexual characteristics in these and other males who develop testosterone deficiency after puberty.
    3. Androgens may be used to stimulate puberty in carefully selected males with clearly delayed puberty. These patients usually have a familial pattern of delayed puberty that is not secondary to a pathological disorder; puberty is expected to occur spontaneously at a relatively late date. Brief treatment with conservative doses may occasionally be justified in these patients if they do not respond to psychological support. The potential adverse effect on bone maturation should be discussed with the patient and parents prior to androgen administration. An X-ray of the hand and wrist to determine bone age should be obtained every 6 months to assess the effect of treatment on the epiphyseal centers (see WARNINGS).
  2. Females
    Androgens may be used secondarily in women with advancing inoperable metastatic (skeletal) mammary cancer who are 1 to 5 years postmenopausal. Primary goals of therapy in these women include ablation of the ovaries. Other methods of counteracting estrogen activity are adrenalectomy, hypophysectomy, and/or antiestrogen therapy. This treatment has also been used in premenopausal women with breast cancer who have benefitted from oophorectomy and are considered to have a hormone-responsive tumor. Judgment concerning androgen therapy should be made by an oncologist with expertise in this field.

Side effects

Endocrine and Urogenital

Female: The most common side effects of androgen therapy are amenorrhea and other menstrual irregularities, inhibition of gonadotropin secretion and virilization, including deepening of the voice and clitoral enlargement. The latter usually is not reversible after androgens are discontinued. When administered to a pregnant woman androgens cause virilization of external genitalia of the female fetus.

Male: Gynecomastia, and excessive frequency and duration of penile erections. Oligospermia may occur at high dosages (see CLINICAL PHARMACOLOGY).

Skin and appendages: Hirsutism, male pattern of baldness, and acne.

Fluid and Electrolyte Disturbances: Retention of sodium, chloride, water, potassium, calcium and inorganic phosphates.

Gastrointestinal: Nausea, cholestatic jaundice, alterations in liver function tests, rarely hepatocellular neoplasms and peliosis hepatis (see WARNINGS).

Hematologic: Suppression of clotting factors II, V, VII, and X, bleeding in patients on concomitant anticoagulant therapy and polycythemia.

Nervous System: Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.

Metabolic: Increased serum cholesterol.

Miscellaneous: Rarely anaphylactoid reactions.

Drug abuse and Dependence

Methyltestosterone Capsules are classified as a schedule III Controlled Substance under the Anabolic Steroids Act of 1990.

Read the entire FDA prescribing information for Testred (Methyltestosterone)

Read More »

What is the most important information I should know about methyltestosterone?

Do not use this medicine if you are pregnant.

You should not use methyltestosterone if you have prostate cancer or male breast cancer.

What should I discuss with my health care provider before taking methyltestosterone?

You should not use methyltestosterone if you are allergic to it, or if you have:

  • prostate cancer;

  • male breast cancer; or

  • if you are pregnant or may become pregnant.

To make sure methyltestosterone is safe for you, tell your doctor if you have:

  • an enlarged prostate;

  • breast cancer;

  • heart disease, congestive heart failure;

  • liver or kidney disease; or

  • if you take a blood thinner (warfarin, Coumadin, Jantoven).

FDA pregnancy category X. This medicine can harm an unborn baby or cause birth defects. Do not use methyltestosterone if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use effective birth control while you are using methyltestosterone.

It is not known whether methyltestosterone passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Methyltestosterone dosing information

Usual Adult Dose for Hypogonadism -- Male:

10 to 50 mg orally once a day.
-or-
5 to 25 mg buccal tablet once a day. Buccal administration allows direct absorption of methyltestosterone into the systemic venous system resulting in delivery of unmetabolized drug to the target tissue. Potency of buccal tablets is 2 times that of oral methyltestosterone.

Usual Adult Dose for Breast Cancer--Palliative:

50 to 200 mg orally per day in divided doses.
-or-
25 to 100 mg buccal tablet per day. Buccal administration allows direct absorption of methyltestosterone into the systemic venous system resulting in delivery of unmetabolized drug to the target tissue. Potency of buccal tablets is 2 times that of oral methyltestosterone.

Methyltestosterone is approved by the FDA for the palliation of androgen-responsive metastatic breast cancer in women who are 1 to 5 years postmenopausal or who are proven to have a hormone-dependent tumor noted by previous beneficial response to castration.

Female patients should be observed for signs of virilization. Women should be instructed to report any hoarseness, acne, changes in menstrual periods, or increase in facial hair. Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. A decision may be made by the patient and the physician that some virilization will be tolerated during the treatment for malignant disease.

Usual Adult Dose for Postpartum Breast Pain:

80 mg orally per day for 3 to 5 days.

Usual Pediatric Dose for Delayed Puberty -- Male:

10 to 50 mg orally once a day.
-or-
5 to 25 mg buccal tablet once a day. Buccal administration allows direct absorption of methyltestosterone into the systemic venous system resulting in delivery of unmetabolized drug to the target tissue. Potency of buccal tablets is 2 times that of oral methyltestosterone.

Dosages used to treat delayed puberty are generally started at the lower end of the dosing range and titrated according to patient response and tolerance. The duration of therapy should be limited to 4 to 6 months.

Wrist and hand bone age should be assessed prior to initiation of methyltestosterone therapy and every 6 months to monitor bone maturation. Exogenous androgen therapy can accelerate bone maturation without producing a compensatory gain in linear growth. Use over long periods can result in fusion of the epiphyseal growth centers and termination of the growth process.

Methyltestosterone Dosage and Administration

Prior to initiating Methyltestosterone, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least two separate days and that these serum testosterone concentrations are below the normal range. 

Methyltestosterone capsules are administered orally. The suggested dosage for androgens varies depending on the age, sex, and diagnosis of the individual patient. Dosage is adjusted according to the patient's response and the appearance of adverse reactions.

Replacement therapy in androgen-deficient males is 10 to 50 mg of Methyltestosterone daily. Various dosage regimens have been used to induce pubertal changes in hypogonadal males, some experts have advocated lower dosages initially, gradually increasing the dose as puberty progresses with or without a decrease to maintenance levels. Other experts emphasize that higher dosages are needed to induce pubertal changes and lower dosages can be used for maintenance after puberty. The chronological and skeletal ages must be taken into consideration both in determining the initial dose and in adjusting the dose.

Doses used in delayed puberty generally are in the lower range of that given above, and for a limited duration, for example 4 to 6 months.

Women with metastatic breast carcinoma must be followed closely because androgen therapy occasionally appears to accelerate the disease. Thus, many experts prefer to use the shorter acting androgen preparations rather than those with prolonged activity for treating breast carcinoma, particularly during the early stages of androgen therapy. The dosage of Methyltestosterone for androgen therapy in breast carcinoma in females is from 50 to 200 mg daily.

PRINCIPAL DISPLAY PANEL - 10 mg Bottle Label

Impax Generics

NDC 0115-1408-01

Methyltestosterone
Capsules, USP
CIII

10 mg

Rx only
100 Capsules

Methyltestosterone 
Methyltestosterone capsule
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0115-1408
Route of Administration ORAL DEA Schedule CIII    
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Methyltestosterone (Methyltestosterone) Methyltestosterone 10 mg
Inactive Ingredients
Ingredient Name Strength
STARCH, CORN  
D&C YELLOW NO. 10  
GELATIN  
FD&C BLUE NO. 1  
FD&C BLUE NO. 2  
FD&C RED NO. 40  
FERROSOFERRIC OXIDE  
MAGNESIUM STEARATE  
PROPYLENE GLYCOL  
SHELLAC  
Product Characteristics
Color RED (translucent) Score no score
Shape CAPSULE Size 18mm
Flavor Imprint Code AA1
Contains     
Packaging
# Item Code Package Description
1 NDC:0115-1408-01 100 CAPSULE in 1 BOTTLE
2 NDC:0115-1408-03 1000 CAPSULE in 1 BOTTLE
3 NDC:0115-1408-08 30 CAPSULE in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA204851 09/21/2015
Labeler - Impax Generics (079832487)
Revised: 01/2017   Impax Generics

Dosing Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied). However, patients with hepatic disease may be at an increased risk of fluid retention.

Storage

Store at 15°C and 30°C (59°F and 86°F). Protect Methitest from light, moisture, and heat.

Pregnancy Risk Factor X Pregnancy Considerations

Use is contraindicated in women who are or may become pregnant. May cause virilization of the external genitalis 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 dose related and most likely to occur when androgens are administered in the first trimester. If a patient becomes pregnant while taking androgens, she should be counseled on the potential hazard to the fetus.

For the Consumer

Applies to methyltestosterone: oral capsules, oral tablets

Side effects include:

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).

Liver Dose Adjustments

Data not available

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