Prasterone (Topical) (Monograph)

Brand name: Intrarosa
Drug class: Adrenals
Chemical name: (3S,8R,9S,10R,13S,14S)-3-hydroxy-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-one
Molecular formula: C₁₉H₂₈O₂
CAS number: 105597-37-3

Medically reviewed by Drugs.com on Nov 18, 2024. Written by ASHP.

Introduction

Inactive endogenous steroid converted intracellularly into active androgens and/or estrogens.

Uses for Prasterone (Topical)

Dyspareunia

Treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, associated with menopause.

Prasterone (Topical) Dosage and Administration

Administration

Intravaginal

Administer intravaginally using the disposable applicator provided by manufacturer.

Dosage

Adults

Dyspareunia

Vaginal

6.5 mg (one insert) once daily at bedtime.

Special Populations

Hepatic Impairment

No specific dosage recommendations.

Renal Impairment

No specific dosage recommendations.

Geriatric Patients

No specific dosage recommendations.

Cautions for Prasterone (Topical)

Contraindications

• Undiagnosed abnormal genital bleeding. Determine cause of undiagnosed, persistent, or recurrent genital bleeding in postmenopausal women prior to considering therapy.

Warnings/Precautions

Breast Cancer

Estrogen is a metabolite of prasterone. Use of exogenous estrogen contraindicated in women with known or suspected history of breast cancer. Not studied in women with history of breast cancer.

Specific Populations

Pregnancy

Not studied in pregnant women. Animal reproduction studies not conducted.

Manufacturer states that prasterone is labeled for use only in postmenopausal women.

Lactation

Not known if distributed into human milk. Effects of drug on breast-fed infant or milk production also unknown.

Pediatric Use

Safety and efficacy not established in pediatric patients; not indicated for use in children.

Geriatric Use

In placebo-controlled 12-week studies and open-label 52-week clinical trial, 19 and 11% of patients, respectively, were ≥65 years of age.

Hepatic Impairment

Effect of hepatic impairment on pharmacokinetics not studied.

Renal Impairment

Effect of renal impairment on pharmacokinetics not studied.

Common Adverse Effects

Vaginal discharge, abnormal Papanicolaou test (Pap smear).

Drug Interactions

Drug interaction studies not performed.

Prasterone (Topical) Pharmacokinetics

Absorption

Plasma Concentrations

Prasterone: Mean serum trough concentrations increased by 47% from baseline following daily intravaginal administration for 12 weeks.

Androgen and estrogen metabolites: Systemic concentrations within expected range for postmenopausal women. Mean serum trough concentrations of testosterone and estradiol increased by 21 and 19%, respectively, from baseline following daily intravaginal administration for 12 weeks.

Elimination

Metabolism

Metabolized by steroidogenic enzymes (e.g., hydroxysteroid dehydrogenase, 5α-reductases, aromatases) into androgens and estrogens.

Distribution

Extent

Not known whether distributed into human milk.

Stability

Storage

Intravaginal

Inserts

5–30°C. Store at room temperature or refrigerate.

Actions

• Inactive endogenous steroid converted intracellularly into active androgens and/or estrogens.

• Exact mechanism of action for treatment of vulvar and vaginal atrophy in postmenopausal women not fully established.

• Exhibits both estrogenic and androgenic effects on vaginal epithelium resulting in improvements in symptoms of menopause (e.g., dyspareunia, vaginal dryness), cell maturation, vaginal pH.

• No stimulatory effect on the endometrium with intravaginal administration up to 52 weeks, but increased incidence of abnormal Pap smear results has been observed in some patients.

Advice to Patients

• Importance of instructing patients to read the manufacturer's patient information and instructions for use prior to initiation of therapy.

• Importance of instructing patients to empty their bladder and wash their hands before handling vaginal insert and applicator.

• Importance of informing patients that vaginal discharge or abnormal Pap smear results may occur.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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