Anti-addiction drug ibogaine inhibits voltage-gated ionic currents: A study to assess the drug's cardiac ion channel profile

Koenig, Xaver, Kovar, Michael, Rubi, Lena, Mike, Agnes K., Lukacs, Peter, Gawali, Vaibhavkumar S., Todt, Hannes, Hilber, Karlheinz, Sandtner, Walter · 2013 · Toxicology and Applied Pharmacology

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Ibogaine IC₅₀: hERG 4 μM, hNaᵥ1.5 142 μM, hCaᵥ1.2 163 μM. Free plasma 1–11 μM at therapeutic dose. Computer model predicts human AP prolongation despite Caᵥ1.2 counteraction. 18-MC hERG IC₅₀ 15 μM.

Dosing: IC₅₀: hERG 4 μM, hNav1.5 142 μM, hCav1.2 163 μM; 18-MC hERG 15 μM — in vitro concentrations (not-applicable)

Safety data present: QTC, HERG

Contraindications: Pre-existing cardiac conditions, Concurrent use of QT-prolonging drugs, Hypokalaemia (exacerbates hERG blockade and reduces channel surface density)