Drug intelligence / Profile preview

hypaconitine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Hypaconitine is a highly toxic diterpene alkaloid derived from *Aconitum* species, most notably *Aconitum carmichaelii* (known as Fuzi in Traditional Chinese Medicine). It is one of the primary active components used for its analgesic and anti-inflammatory properties in treating conditions such as rheumatoid arthritis and joint pain. Mechanistically, hypaconitine acts as a potent activator of voltage-gated sodium channels, leading to persistent membrane depolarization, which contributes to both its therapeutic effects and its significant cardiotoxicity and neurotoxicity. The compound has a very narrow therapeutic window and is primarily metabolized by the cytochrome P450 enzyme CYP3A4 and transported by P-glycoprotein (P-gp). Due to its toxicity, plant materials containing hypaconitine are typically subjected to rigorous processing (detoxification) before medicinal use.

Other names
HA
02

Targets

CYP3A4 (Cytochrome P450 3A4)NaV (Voltage-gated sodium channels)

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