Methyltestosterone

Men with breast cancer or those with known or suspected prostate cancer. Pregnancy and women of childbearing potential.

Patient with breast cancer; diseases that may be exacerbated by fluid retention (e.g. cardiac impairment); risk factors for sleep apnoea (e.g. obesity, chronic lung disease). Not recommended for use in patients with thrombophilia, severe lower respiratory tract symptoms. Hepatic and renal impairment. Lactation.

Significant: Peliosis hepatitis, hepatic neoplasms, hepatocellular carcinoma, cholestatic hepatitis, jaundice, CV events (e.g. MI); oligospermia, polycythaemia, priapism; venous thromboembolic events (e.g. DVT, pulmonary embolism); worsened benign prostatic hyperplasia, gynaecomastia; urethral obstruction; hypercalcaemia, fluid retention, oedema with or without CHF; increased risk of prostate cancer; exacerbated sleep apnoea (male patients); virilisation (e.g. deepening of voice, menstrual irregularities, clitromegaly, hirsutism, acne) in females.
Blood and lymphatic system disorders: Clotting factors suppression.
Gastrointestinal disorders: Nausea.
Investigations: Increased serum cholesterol.
Metabolism and nutrition disorders: Retention of Ca, K, Na, NaCl.
Nervous system disorders: Headache, paraesthesia.
Psychiatric disorders: Anxiety, depression.
Reproductive system and breast disorders: Increased or decreased libido.
Skin and subcutaneous tissue disorders: Acne vulgaris, androgenetic alopecia (male).

PO: X

Monitor LFTs, lipid panel, Hb, and haematocrit (at 3-6 months and annually); urine, serum Ca, serum glucose. Monitor for signs and symptoms of CV and venous thromboembolic events, liver toxicity, and virilisation in females.

May enhance the anticoagulant effect of vitamin K antagonists (e.g. warfarin). May increase serum levels of oxyphenbutazone. May enhance the hypoglycaemic effect of blood glucose lowering agents.

May reduce thyroxine-binding globulin, causing reduced total T₄ serum levels and enhanced reuptake of T₃ and T₄.

Description:
Mechanism of Action: Methyltestosterone, a synthetic androgenic anabolic steroid, is used primarily for the substitution of diminished or absent endogenous testicular hormone.
Pharmacokinetics:
Distribution: Plasma protein binding: 98% to sex hormone-binding globulin.
Metabolism: Metabolised in the liver.
Excretion: Via urine (approx 90%); faeces (approx 6%). Elimination half-life: 10-100 minutes (may vary).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6010, Methyltestosterone. https://pubchem.ncbi.nlm.nih.gov/compound/Methyltestosterone. Accessed Nov. 25, 2024.

Store between 15-30°C. Protect from light, moisture, and heat.

Androgens & Related Synthetic Drugs / Cancer Hormone Therapy

G03BA02 - methyltestosterone ; Belongs to the class of 3-oxoandrosten (4) derivative androgens used in androgenic hormone preparations.

Anon. Methyltestosterone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/10/2024.

Brayfield A, Cadart C (eds). Methyltestosterone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/10/2024.

Methyltestosterone Capsule (Novitium Pharma LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 10/10/2024.

Methyltestosterone. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/10/2024.