pharmacopeia
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Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Androgen Receptor Agonists.

Androgen Receptor

Indications

Sourced from openFDA
  • 1. Males Androgens are indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone: Primary hypogonadism (congenita or acquired) — Testicular failure due to cryptohidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy.

Contraindications

Sourced from openFDA
  • METHITEST™ (methyltestosterone) tablets are contraindicated in men with carcinomas of the breast or with known or suspected carcinomas of the prostate, and in women who are or may become pregnant. When administered to pregnant women, androgens cause virilization of the external genitalia of the female fetus.contraindicated

Dosage & administration

Sourced from openFDA

Prior to initiating METHITEST™ (methyltestosterone) tablets, 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. Dosage must be strictly individualized. The suggested dosage for androgens varies depending on the age, sex, and diagnosis of the individual patient. Adjustments and duration of dosage will depend upon the patient’s response and the appearance of adverse reactions. Males: In the androgen-deficient male the guideline for replacement therapy indicates the usual initial dosage of 10 mg to 50 mg daily. Various dosage regimens have been used to induce pubertal changes in hypogonadel 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. Dosages used in delayed puberty generally are in the lower ranges of those given above, and are for limited duration, for example, 4 to 6 months. Females: Women with metastatic breast carcinoma must be followed closely because androgen therapy occasionally appears to accelerate the disease.

Warnings & precautions

Sourced from openFDA

In patients with breast cancer, androgen therapy may cause hypercalcemia by stimulating osteolysis. In this case, the drug should be discontinued. Prolonged use of high doses of androgens has been associated with the development of peliosis hepatis and hepatic neoplasms including hepatocellular carcinoma (see PRECAUTIONS: CARCINOGENESIS, MUTAGENESIS, IMPAIRMENT OF FERTILITY ). Peliosis hepatis can be a life-threatening or fatal complication. Cholestatic hepatitis and jaundice occur with 17-alpha-alkylandrogens (such as methyltestosterone) at a relatively low dose. If cholestatic hepatitis with jaundice appears or if liver function tests become abnormal, the androgen should be discontinued and the etiology should be determined. Drug-induced jaundice is reversible when the medication is discontinued. Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking. There have been post-marketing reports of venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), in patients using testosterone products, such as methyltestosterone. Evaluate patients who report symptoms of pain, edema, warmth and erythema in the lower extremity for DVT and those who present with acute shortness of breath for PE. If a venous thromboembolic event is suspected, discontinue treatment with methyltestosterone and initiate appropriate workup and management.

Adverse reactions

Sourced from openFDA

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 dosage (see CLINICAL PHARMACOLOGY ). Skin and Appendages: Hirsutism, male pattern of baldness, and acne. Cardiovascular Disorders: Myocardial infarction, stroke 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 neoplasma 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. Vascular Disorders: Venous thromboembolism. Miscellaneous: Rarely, anaphylactoid reactions. To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Overdosage

Sourced from openFDA

Overdose of medication may be reflected in the occurrence of the signs and symptoms associated with testosterone-anabolic drugs. Nausea and appearance of the early manifestations of edema should be looked for. However, there has been no report of acute overdosage with androgens.

Approval history

Sourced from openFDA
  • Oct 17, 1974ANDAANDA080767Impax Labs
  • Sep 21, 2015ANDAANDA204851Impax Labs Inc
  • Feb 18, 2022ANDAANDA215270Novitium Pharma

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
515 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Breast Cancer Female6913%
  2. 2Breast Cancer5511%
  3. 3Drug Ineffective448.5%
  4. 4Fatigue448.5%
  5. 5Nausea387.4%
  6. 6Headache336.4%
  7. 7Arthralgia316.0%
  8. 8Asthenia295.6%
  9. 9Dyspnoea295.6%
  10. 10Myalgia265.0%
  11. 11Pain265.0%
  12. 12Off Label Use254.9%
  13. 13Vomiting254.9%
  14. 14Anxiety244.7%
  15. 15Depression244.7%

Literature

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Recent PubMed references pinned to Methyltestosterone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 352 ClinicalTrials.gov registrations naming Methyltestosterone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Methyltestosterone work?
Mechanism-of-action class: Androgen Receptor Agonists.
What is Methyltestosterone used for?
According to FDA labeling, Methyltestosterone carries indications including: 1. Males Androgens are indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone: Primary hypogonadism (congenita or acquired) — Testicular failure due to cryptohidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Methyltestosterone?
Methyltestosterone is classified as 3-oxoandrosten (4) derivatives, Androgens and female sex hormones in combination with other drugs, Androgen, Androgen Receptor Agonists, Stimulate Penile Development.
What are the brand names for Methyltestosterone?
Methyltestosterone is marketed under brand names including Covaryx, Estratest, Methitest.
What are the contraindications for Methyltestosterone?
Methyltestosterone labeling lists contraindications including: METHITEST™ (methyltestosterone) tablets are contraindicated in men with carcinomas of the breast or with known or suspected carcinomas of the prostate, and in women who are or may become pregnant. When administered to pregnant women, androgens cause virilization of the external genitalia of the female fetus.. Always consult the full prescribing information and a clinician.
Note. Data for methyltestosterone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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