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 17, 2023. Written by ASHP.

Introduction

Inactive endogenous steroid converted intracellularly into active androgens and/or estrogens.¹

Uses for Prasterone (Topical)

Dyspareunia

Treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, associated with menopause.^{1 2 3 4}

Prasterone (Topical) Dosage and Administration

Administration

Intravaginal

Administer intravaginally using the disposable applicator provided by manufacturer.¹

Dosage

Adults

Dyspareunia

Vaginal

6.5 mg (one insert) once daily at bedtime.¹

Special Populations

Hepatic Impairment

No specific dosage recommendations.¹

Renal Impairment

No specific dosage recommendations.¹

Geriatric Patients

No specific dosage recommendations.¹

Cautions for Prasterone (Topical)

Contraindications

• Undiagnosed abnormal genital bleeding.¹ Determine cause of undiagnosed, persistent, or recurrent genital bleeding in postmenopausal women prior to considering therapy.¹

Warnings/Precautions

Breast Cancer

Estrogen is a metabolite of prasterone.¹ Use of exogenous estrogen contraindicated in women with known or suspected history of breast cancer.¹ Not studied in women with history of breast cancer.¹

Specific Populations

Pregnancy

Not studied in pregnant women.¹ Animal reproduction studies not conducted.¹

Manufacturer states that prasterone is labeled for use only in postmenopausal women.¹

Lactation

Not known if distributed into human milk.¹ Effects of drug on breast-fed infant or milk production also unknown.¹

Pediatric Use

Safety and efficacy not established in pediatric patients; not indicated for use in children.¹

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.¹

Hepatic Impairment

Effect of hepatic impairment on pharmacokinetics not studied.¹

Renal Impairment

Effect of renal impairment on pharmacokinetics not studied.¹

Common Adverse Effects

Vaginal discharge, abnormal Papanicolaou test (Pap smear).¹

Related/similar drugs

estradiol topical, acetylcysteine, ascorbic acid, biotin, multivitamin, Dextrose, Imvexxy

Drug Interactions

Drug interaction studies not performed.¹

Prasterone (Topical) Pharmacokinetics

Absorption

Plasma Concentrations

Prasterone: Mean serum trough concentrations increased by 47% from baseline following daily intravaginal administration for 12 weeks.¹

Androgen and estrogen metabolites: Systemic concentrations within expected range for postmenopausal women.^{4 5 6 7 8} Mean serum trough concentrations of testosterone and estradiol increased by 21 and 19%, respectively, from baseline following daily intravaginal administration for 12 weeks.¹

Elimination

Metabolism

Metabolized by steroidogenic enzymes (e.g., hydroxysteroid dehydrogenase, 5α-reductases, aromatases) into androgens and estrogens.¹

Distribution

Extent

Not known whether distributed into human milk.¹

Stability

Storage

Intravaginal

Inserts

5–30°C.¹ Store at room temperature or refrigerate.¹

Actions

• Inactive endogenous steroid converted intracellularly into active androgens and/or estrogens.^{1 5 7}

• Exact mechanism of action for treatment of vulvar and vaginal atrophy in postmenopausal women not fully established.¹

• 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.^{1 2 3 4}

• No stimulatory effect on the endometrium with intravaginal administration up to 52 weeks,⁹ but increased incidence of abnormal Pap smear results has been observed in some patients.¹

Advice to Patients

• Importance of instructing patients to read the manufacturer's patient information and instructions for use prior to initiation of therapy.¹

• Importance of instructing patients to empty their bladder and wash their hands before handling vaginal insert and applicator.¹

• Importance of informing patients that vaginal discharge or abnormal Pap smear results may occur.¹

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

• Importance of informing patients of other important precautionary information.¹ (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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