Mesterolone

Indications
 Oral
Androgen deficiency, Infertility due to hypogonadism
Adult: Initially, 75-100 mg daily in divided doses. Maintenance: 50-75 mg daily in divided doses.
Contraindications
 Prostatic or breast carcinoma. Previous or existing hepatic tumours. Pregnancy and lactation.
Warnings / Precautions
 Regularly examine the prostate and breast during treatment. CV disorders, renal or hepatic impairment, epilepsy, migraine, DM or other conditions that may be exacerbated by the possible fluid retention or oedema. Skeletal metastases (risk of hypercalcaemia). Children. Monitor skeletal maturation during therapy.
Adverse Reactions
 Frequent or persistent erections.
Potentially Fatal: Malignant liver tumours.
Drug Interactions
 Enhances effects of ciclosporin, antidiabetics, levothyroxine, anticoagulants e.g. warfarin. Resistance to the effects of neuromuscular blockers may occur.
See Below for More mesterolone Drug Interactions
Lab Interactions
 May Interfere with glucose tolerance and thyroid function tests.
Mechanism of Actions
 Mesterolone is an androgen with less inhibitory effects on intrinsic testicular function compared to testosterone.
Absorption: Rapidly and almost completely absorbed (oral); peak serum levels in about 1.6 hr.
Distribution: Protein-binding: About 40% to albumin and 58% to sex-hormone binding globulin.
Metabolism: Rapidly metabolised; absolute bioavailability: 3% of the oral dose. Not metabolised to oestrogenic compounds.
Excretion: Via urine (approx 77% of the metabolites); via faeces (approx 13%); 12-13 hr (terminal half-life).
Administration
 May be taken with or without food.
ATC Classification
 G03BB01 - mesterolone ; Belongs to the class of 5-androstanon (3) derivative androgens used in androgenic hormone preparations.
Available As
  • Mesterolone 0.1 mg
  • Mesterolone 25 mg

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