Methyltestosterone


Generic Medicine Info
Indications and Dosage
Oral
Male hypogonadism
Adult: 10-50 mg daily.

Oral
Metastatic breast carcinoma in postmenopausal women
Adult: 50-200 mg daily.
Contraindications
Men with breast cancer, known or suspected prostate cancer. Pregnancy.
Special Precautions
Patient with CV disease, benign prostatic hyperplasia, chronic lung disease; obesity. Renal and hepatic impairment. Lactation.
Adverse Reactions
Significant: Peliosis hepatis, hepatic neoplasms, hepatocellular carcinoma, cholestatic hepatitis, jaundice, MI, stroke, DVT, pulmonary embolism, polycythaemia, oligospermia, reduced ejaculatory volume, priapism, benign prostatic hypertrophy, sleep apnoea.
Blood and lymphatic system disorders: Clotting factors suppression.
Endocrine disorders: Hirsutism.
Gastrointestinal disorders: Nausea, vomiting.
Immune system disorders: Anaphylactic reactions.
Investigations: Change in libido.
Metabolism and nutrition disorders: Hypercholesterolaemia.
Nervous system disorders: Headache, paraesthesia.
Psychiatric disorders: Depression, anxiety.
Reproductive system and breast disorders: Amenorrhoea, impotence, mastalgia, testicular atrophy.
Skin and subcutaneous tissue disorders: Acne vulgaris, androgenetic alopecia.
Monitoring Parameters
Monitor LFTs, lipid profile, haemoglobin and haematocrit (at 3-6 months and annually thereafter); urine, and serum Ca. Monitor serum glucose in diabetic patients; prostate specific antigen if clinically indicated. Assess for signs of virilisation in women. Perform radiologic examination of the wrist and hand for prepubertal patients every 6 months.
Drug Interactions
Enhanced effect of anticoagulants and hypoglycaemic agent. Increased hepatotoxicity of ciclosporin. Increased plasma concentrations of oxyphenbutazone.
Lab Interference
May decrease thyroxine-binding globulin concentrations.
Action
Description:
Mechanism of Action: Methyltestosterone is a synthetic anabolic steroid hormone which promotes growth and development of male sex organs. It also aids in the maintenance of secondary sex characteristics in androgen-deficient men.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract.
Distribution: Plasma protein binding: 98% mainly to sex hormone-binding globulin.
Metabolism: Metabolised in the liver.
Excretion: Mainly via urine (approx 90%); faeces (approx 6%). Elimination half-life: 10-100 minutes.
Chemical Structure

Chemical Structure Image
Methyltestosterone_01

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6010, Methyltestosterone. https://pubchem.ncbi.nlm.nih.gov/compound/Methyltestosterone. Accessed Oct. 27, 2020.

Storage
Store between 15-30°C. Protect from light, moisture, and heat.
MIMS Class
Androgens & Related Synthetic Drugs / Cancer Hormone Therapy
ATC Classification
G03BA02 - methyltestosterone ; Belongs to the class of 3-oxoandrosten (4) derivative androgens used in androgenic hormone preparations.
References
Anon. Methyltestosterone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/09/2020.

Anon. Methyltestosterone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/09/2020.

Buckingham R (ed). Methyltestosterone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2020.

Methitest Tablets (Amneal Pharmaceuticals of New York LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/09/2020.

Methyltestosterone Capsule (Amneal Pharmaceuticals of New York LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/09/2020.

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