topical loperamide

Topical loperamide is a repurposed formulation of the common anti-diarrheal medication, being investigated by the University of Rochester for the treatment of localized provoked vulvodynia (LPV). Loperamide is a small molecule that acts as a peripheral mu-opioid receptor agonist. While typically administered orally to slow intestinal motility, its topical application in this context aims to leverage peripheral opioid receptors located in the vulvar vestibule to modulate pain signaling. By targeting these peripheral receptors, the formulation seeks to provide localized analgesic effects for genital pain syndromes while minimizing the systemic side effects and central nervous system activity typically associated with opioid agonists. In clinical trials, it was compounded at a 5% concentration in a Cetaphil base and evaluated in a blinded crossover study alongside other topical agents such as gabapentin and ketamine.

Other names

5% topical loperamideloperamide 5% creamloperamide 5% topical