FDA Approved Sexual & Reproductive Health

Alprostadil

also known as: Prostaglandin E1, PGE1, Caverject, Edex, MUSE, Prostin VR

A synthetic prostaglandin E1 vasodilator FDA-approved for intracavernosal use in erectile dysfunction and for maintaining ductus arteriosus patency in neonatal congenital heart disease.

A vasodilator and smooth-muscle relaxant that binds prostaglandin EP2/EP4 receptors to raise intracellular cAMP; used for decades as a first-line intracavernosal injectable for erectile dysfunction and as a life-saving bridge therapy in ductus-dependent neonatal cardiac conditions.

Mechanism of action

Binds prostaglandin EP2 and EP4 receptors on smooth-muscle cells, activating adenylate cyclase to increase intracellular cAMP. Elevated cAMP causes smooth-muscle relaxation and arterial dilation. In the corpus cavernosum, this engorges the penis with blood to produce an erection without requiring intact nerve supply. In neonatal cardiac use, the same vasodilation keeps the ductus arteriosus patent. Also exhibits antiplatelet and anti-atherosclerotic effects via cAMP elevation in vascular tissue.

Primary uses

Erectile dysfunction (intracavernosal injection or intraurethral pellet)
Maintenance of ductus arteriosus in neonatal congenital heart disease
Peripheral arterial occlusive disease (approved in Europe)
Raynaud phenomenon (off-label, mixed evidence)

Typical dosing

5–40 mcg as needed; typically ≤ 3x weekly (intracavernosal injection or intraurethral pellet)

Intracavernosal ED dosing individually titrated starting at 2.5–5 mcg. Intraurethral MUSE pellets supplied as 125–1000 mcg. Neonatal IV dosing is weight-based (0.01–0.1 mcg/kg/min continuous infusion).

Regulatory status

FDA-approved as Caverject and Edex (intracavernosal injection for ED), MUSE (intraurethral pellet for ED), and Prostin VR Pediatric (IV for ductus-dependent neonatal congenital heart disease). Also approved in Europe since 1984 for peripheral arterial occlusive disease of the lower limbs.

References

[review] Linet OI, Ogrinc FG. "Efficacy and safety of intracavernosal alprostadil in men with erectile dysfunction." N Engl J Med, 1996;334(14):873-877.
[review] Porst H. "The rationale for prostaglandin E1 in erectile failure: a survey of worldwide experience." J Urol, 1996;155(3):802-815. PMID: 8583582.
[fda-label] FDA Prescribing Information: edex (alprostadil for injection) — Endo Pharmaceuticals, revised 2015.

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Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.