Mesterolone: Indication, Dosage, Side Effect, Precaution

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Androgen deficiency, Infertility due to hypogonadism

Adult: Initially, 75-100 mg daily in 3-4 divided doses for several months. Maintenance: 50-75 mg daily. Treatment recommendations may vary between countries (refer to specific product guidelines).

Administration

May be taken with or without food.

Contraindications

Prostatic carcinoma, current or history of liver tumours.

Special Precautions

Patient with a history of MI or CAD; conditions influenced by oedema (e.g. CV disease, seizure, migraine), polycythaemia. Not indicated for use in women. Not indicated for enhancing muscular development or physical ability in healthy individuals. Renal and hepatic impairment.

Adverse Reactions

Significant: Frequent or persistent erections, excessive sexual stimulation; increased risk of prostate cancer; VTE.
Potentially Fatal: Rarely, benign or malignant liver tumours, intra-abdominal haemorrhage.

Monitoring Parameters

Monitor lipid profile. Perform prostate examination prior to starting therapy and routinely during therapy.

Lab Interference

May interfere with thyroid function test and glucose tolerance test.

Action

Description: Mesterolone is an orally active androgen with less inhibitory effect on intrinsic testicular function than testosterone. It stimulates receptors in tissues and organs to promote the growth and development of male sex organs and to maintain secondary sex characteristics in androgen-deficient males.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed. Bioavailability: 3%. Time to peak plasma concentration: 1.6 ± 0.6 hours.
Distribution: Plasma protein binding: 98% (40% to albumin and 58% to sex hormone binding globulin).
Metabolism: Rapidly metabolised in the liver into metabolites including 1α-methylandrosterone and 1α-methyl-5α-androstane-3α, 17β-diol.
Excretion: Via urine (80% as metabolites); faeces (13% as metabolites). Elimination half-life: 12-13 hours.

Chemical Structure

Storage

Store below 30°C.

MIMS Class

Androgens & Related Synthetic Drugs

ATC Classification

G03BB01 - mesterolone ; Belongs to the class of 5-androstanon (3) derivative androgens used in androgenic hormone preparations.

References

Anon. Mesterolone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/11/2022.

Buckingham R (ed). Mesterolone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/11/2022.

Pro-viron (Bayer PLC). MHRA. https://products.mhra.gov.uk. Accessed 16/11/2022.

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