Trifluoperazine is a phenothiazine antipsychotic that is clinically used to treat schizophrenia and anxiety. Trifluoperazine also exhibits anxiolytic, anti-parasitic, anticancer, and anesthetic activities. This compound inhibits α1-adrenergic receptors, calmodulin, and D1/2 receptors. In Plasmodium, trifluoperazine inhibits Ca2+-dependent protein kinase 4 (CDPK4). In lung adenocarcinoma cells, trifluoperazine downregulates expression of F-actin and Bcl-2, upregulates expression of Bax and phosphorylation of ERK and JNK, induces apoptosis, and inhibits cellular proliferation. Additionally, this compound inhibits Nav1.4/SCNA4 and Nav1.7/SCN9A Na+ channels, causing sensory and motor blockade in vivo.