FDA-Approved (Bremelanotide, Flibanserin) and Off-Label Medications (Testosterone, Sildenafil) to Enhance Sexual Desire/Function in Women

Bremelanotide has been available off-label through compounding pharmacies for many years for men and women seeking to improve libido. In 2019, the FDA approved use of bremelanotide (Vyleesi) for premenopausal women with hypoactive sexual desire disorder (HSDD), the second medication approved for this purpose. The first was flibanserin (Addyi), a pill to be taken daily at bedtime, and not within 2 hours of consuming alcohol. Though HSDD is highly prevalent and affects nearly six million premenopausal women, the availability of approved pharmaceuticals to treat it is relatively recent. Bremelanotide activates melanocortin receptors and pathways in the brain involved in the sexual response. Studies have shown that it improves sexual desire and lowers distress surrounding sexual interaction. Though not approved for men, bremelanotide has the potential to benefit men with low libido and erectile difficulties. As with many medications, bremelanotide is associated with adverse effects, which include nausea, flushing, injection site reactions, headache, vomiting, hypertension, and irreversible hyper-pigmentation. In addition, the offlabel prescription of testosterone in women is widespread and been used to improve libido, genitourinary symptoms, and vitality, particularly in the anti-aging community. Other pharmaceuticals that are prescribed off-label to aid female sexual function include the PDE5 inhibitors sildenafil, vardenafil and tadalafil. Non-pharmacologic interventions for improving sexual function include sex-positive vitamins, minerals, PDE5, herbs, and lifestyle changes. Combinations the above pharmaceuticals and natural therapies may enhance efficacy while minimizing side effects. The recent approval of bremelanotide is significant as it should advance knowledge and research on female sexual dysfunction, which is a relatively neglected area. The prescription of off- label and/or compounded medications for sexual dysfunction is generally considered within the domain of integrative, functional, or complementary and alternative medicine.

Keywords:Bremelanotide; Flibanserin, libido; Hypoactive sexual desire disorder (HSDD); Sexual disorders; Sildenafil; PDE5; Women’s sexuality; Off- label; Compounding; Testosterone; Integrative complementary and alternative medicine

Abbreviations: HSDD: Hypoactive Sexual Desire Disorder; FDA: Food and Drug Administration; ICD10: International Statistical Classification of Diseases and Related Health Problems; WHO: World Health Organization; PDE5: Phosphodiesterase type 5