Mesterolone: Indication, Dosage, Side Effect, Precaution

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

Generic Medicine Info

Indications and Dosage

Oral
Androgen deficiency, Infertility due to hypogonadism

Adult: Male: Initially, 75-100 mg daily in 3 or 4 divided doses for several mth. Maintenance: 50-75 mg daily in divided doses.

Administration

May be taken with or without food.

Contraindications

Current or history of hepatic tumours. Prostatic carcinoma.

Special Precautions

Not suitable for increasing muscular development and physical ability.

Adverse Reactions

Significant: Frequent or persistent erections.

Monitoring Parameters

Regularly monitor prostate status.

Action

Description: Mesterolone supplements endogenous androgens w/ less inhibitory effect on intrinsic testicular function than testosterone and its derivatives.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the GI tract. Absolute bioavailability: Approx 3%. Time to peak plasma concentration: Approx 1.6 hr.
Distribution: Plasma protein binding: 98% (40% to albumin, 58% to sex hormone binding globulin).
Metabolism: Rapidly metabolised to 1α-methyl-androsterone, 1α-methyl-5α-androstane-3α, 17β-diol and other metabolites.
Excretion: Via urine (approx 77% as metabolites) and faeces (approx 13% as metabolites). Terminal half-life: 12-13 hr.

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 26/07/2017.

Buckingham R (ed). Mesterolone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/07/2017.

Joint Formulary Committee. Mesterolone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/07/2017.

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