Crotamiton is an ectoparasiticide and antipruritic agent.1,2,3 It blocks the mouse transient receptor potential vanilloid 4 (TRPV4) channel expressed in HEK293 cells in a calcium-dependent manner (IC50s = 223.5 and 15.5 μM in buffer containing 0 and 2 mM calcium, respectively).2 It inhibits scratching behavior in mice induced by the TRPV4 agonist GSK1016790A . Topical application of crotamiton (0.025 g of a 10% ointment) also inhibits scratching behavior in mice induced by histamine, serotonin , and the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 .3 Formulations containing crotamiton have been used to eradicate scabies and in the treatment of symptomatic pruritic skin.
1.Goldust, M., Rezaee, E., and Raghiafar, R.Topical ivermectin versus crotamiton cream 10% for the treatment of scabiesInt. J. Dermatol.53(7)904-908(2014) 2.Kittaka, H., Yamanoi, Y., and Tominaga, M.Transient receptor potential vanilloid 4 (TRPV4) channel as a target of crotamiton and its bimodal effectsPflugers Arch.469(10)1313-1323(2017) 3.Sekine, R., Satoh, T., Takaoka, A., et al.Anti pruritic effects of topical crotamiton, capsaicin, and a corticosteroid on pruritogen-induced scratching behaviorExp. Dermatol.21(3)201-204(2012)