prasterone: clinical use

Prescribing considerations

• Confirm that symptoms are postmenopausal and materially affect quality of life.
• Take relevant personal and family history; tailor pelvic and breast examination to risks and symptoms.
• Treat vaginal infection before initiation.
• Use closer supervision with fibroids, endometriosis, thromboembolic or oestrogen-dependent tumour risk factors, hypertension, liver disease, diabetes, gallstones, migraine, systemic lupus erythematosus, epilepsy, asthma or otosclerosis.
• Prasterone is a Class C, Schedule 4 Part 2 controlled drug in the UK.

Contraindications and cautions

• Hypersensitivity to prasterone or hard fat
• Undiagnosed genital bleeding
• Known, previous or suspected breast cancer
• Known or suspected oestrogen-dependent malignancy
• Untreated endometrial hyperplasia
• Acute liver disease, or previous liver disease with persistently abnormal liver function
• Previous or current venous thromboembolism
• Known thrombophilia
• Active or recent arterial thromboembolic disease
• Porphyria

Monitoring

• Periodically reassess symptom benefit and ongoing risks.
• Investigate bleeding or spotting during treatment.
• Advise reporting of breast changes and maintain usual breast and cervical screening.
• Monitor clinically relevant blood pressure, liver or thromboembolic concerns according to individual risk.
• Long-term endometrial safety beyond one year has not been established.

Clinical pharmacology

Prasterone is an inactive endogenous steroid precursor converted intracellularly in vaginal tissue into small, cell-specific amounts of oestrogens and androgens. Distribution is mainly local, although limited systemic exposure occurs; measured metabolite concentrations remained within usual postmenopausal ranges in the pharmacokinetic study.

Formulation and product differences

• The selected product is a vaginal pessary containing prasterone in a hard-fat base.
• It may be inserted digitally or with the supplied reusable applicator.
• The hard-fat base can melt and cause vaginal discharge, and may damage latex barrier devices.

Pessary

Route: Vaginal

Strengths: 6.5 mg