lappaconitine

Lappaconitine is a natural diterpene alkaloid originally isolated from Aconitum sinomontanum (sacred tower giant Chinese monkshood), a plant used in traditional Chinese medicine. It acts primarily as a voltage-gated sodium channel blocker, distinguishing it from other aconitum alkaloids like aconitine, which are sodium channel activators[1][2][6]. Lappaconitine exhibits multiple pharmacological activities including analgesic, anti-inflammatory, antiarrhythmic (class IC), antiepileptic/anticonvulsant, and antitumor effects[2][3][7]. Its analgesic effect is non-opioid in nature and has been shown to be effective for moderate to severe pain management such as cancer pain and postoperative pain[3][6]. The compound also downregulates P2X3 receptor expression in dorsal root ganglion neurons and modulates inflammatory cytokines via the NF-kB and MAPK pathways[2][3]. Clinically, lappaconitine or its hydrobromide salt has been used mainly in China for arrhythmias and as an analgesic agent; however, its development for arrhythmia was discontinued after phase II trials due to efficacy or safety concerns[4].

Brand names

allapinine

Other names

lappaconitine hydrobromideLAQG3030QG-3030QG 3030