Drug reference

prasterone

Endogenous adrenal steroid (DHEA) — vaginal preparation · Gynecological Agent

START

6.5 mg (1 ovule) intravaginally once daily at bedtime

TYPICAL MAX

6.5 mg intravaginally once daily

STOP IF

Unexplained vaginal bleeding, new breast lesion, or thromboembolism

WATCH

Symptomatic improvement over 6–12 weeks; gynaecologic surveillance

CDSCO approvedATC G03XX01

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 2h · absorption
PEAK: 8h · local steroid
t½: 12h · DHEA t½
DURATION: 1d · once-daily

EXCRETION

Renal / biliary — steroid conjugates

route + CYP

INTERACTIONS

—

none in our sources

PREGNANCY

Not applicable (postmenopausal indication).

FDA category + note

Mechanism

Dehydroepiandrosterone (DHEA) is converted intracellularly to androgens and oestrogens via vaginal cell steroidogenesis (intracrinology), restoring local hormonal environment for vulvovaginal atrophy of menopause — minimal systemic hormonal exposure.

Indications

Moderate-to-severe vulvovaginal atrophy due to menopause / dyspareunia

Dosing

Adult: 6.5 mg (one ovule) intravaginally once daily at bedtime.
Pediatric: Not applicable.
Renal adjustment: No adjustment (minimal systemic).
Hepatic adjustment: Avoid in severe hepatic impairment.
Geriatric: Primary population; standard dose.
Max dose: 6.5 mg intravaginally once daily

Pharmacokinetics

Onset

Symptomatic improvement over 6–12 weeks

Peak effect

Local — sustained while in regular use

Duration

Daily dosing for chronic maintenance

Half-life

DHEA ~12 h (systemic, minimal)

Bioavailability

Low systemic; locally active

Protein binding

Bound to sulfatase / steroidogenic enzymes locally

Metabolism

Local intracrine steroidogenesis (androgens / oestrogens in vaginal cells)

Excretion

Renal / biliary (steroid conjugates)

Contraindications

Undiagnosed abnormal genital bleeding
Known or suspected breast cancer / oestrogen-dependent malignancy
Active thrombotic disease
Severe hepatic impairment
Hypersensitivity

Side effects

Common

Vaginal dischargeAbnormal pap smear (cells changes)Local pruritus / discomfort

Serious

Endometrial / breast effects (theoretical — minimal at recommended doses)
Thromboembolism (very rare given low systemic exposure)

Pregnancy & lactation

Pregnancy

Not applicable (postmenopausal indication).

Lactation

Not applicable.

Drug interactions

Aromatase Inhibitors

Moderate

Database

Possible interference with oestrogen suppression

Avoid in patients on AIs