ArticleToxicology and applied pharmacology2013
Anti-addiction drug ibogaine inhibits voltage-gated ionic currents: a study to assess the drug's cardiac ion channel profile.
Article in Toxicology and applied pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 44 citations in OpenAlex.
- A Pharmacological Perspective on Plant-derived Bioactive Molecules for Epilepsy.Neurochemical research · 2021Pooled it
- Rare but relevant: Ibogaine and cardiovascular complications-prolonged QT interval and ventricular arrhythmias.Addiction (Abingdon, England) · 2026Review
- Development of Bioisosteres of Iboga Alkaloids: A Step-Economical Synthesis to Enhance the Antinociceptive and Anxiolytic Activity with Neuroprotective Effects.ACS pharmacology & translational science · 2026Article
- The science of psychedelic medicine.Nature medicine · 2026Review
- Cardiovascular effects and safety of classic psychedelics.Nature cardiovascular research · 2025Review
- Natural L-type calcium channels antagonists from Chinese medicine.Chinese medicine · 2024Article
- The pharmacokinetics and pharmacodynamics of ibogaine in opioid use disorder patients.Journal of psychopharmacology (Oxford, England) · 2024Article
- Psilocybin Therapy of Psychiatric Disorders Is Not Hampered by hERG Potassium Channel-Mediated Cardiotoxicity.The international journal of neuropsychopharmacology · 2022Article
- Safety of ibogaine administration in detoxification of opioid-dependent individuals: a descriptive open-label observational study.Addiction (Abingdon, England) · 2022Observational
- Genetic and Molecular Aspects of Drug-Induced QT Interval Prolongation.International journal of molecular sciences · 2021Review
- Plants with Anti-Addictive Potential.Advances in experimental medicine and biology · 2021Article
- Cardiac hERG KHandbook of experimental pharmacology · 2021Article
- Allicin disrupts cardiac Cav1.2 channels via trafficking.Pharmaceutical biology · 2019Article
- Modulation of the heart's electrical properties by the anticonvulsant drug retigabine.Toxicology and applied pharmacology · 2017Article
- Anti-addiction Drug Ibogaine Prolongs the Action Potential in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes.Cardiovascular toxicology · 2017Article
- Ibogaine-associated cardiac arrest and death: case report and review of the literature.Therapeutic advances in psychopharmacology · 2016Review
- The anti-addiction drug ibogaine and the heart: a delicate relation.Molecules (Basel, Switzerland) · 2015Review
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9 authors at 1 institution in 1 country.
Funding
Abstract
The plant alkaloid ibogaine has promising anti-addictive properties. Albeit not licensed as a therapeutic drug, and despite hints that ibogaine may perturb the heart rhythm, this alkaloid is used to treat drug addicts. We have recently reported that ibogaine inhibits human ERG (hERG) potassium channels at concentrations similar to the drugs affinity for several of its known brain targets. Thereby the drug may disturb the heart's electrophysiology. Here, to assess the drug's cardiac ion channel profile in more detail, we studied the effects of ibogaine and its congener 18-Methoxycoronaridine (18-MC) on various cardiac voltage-gated ion channels. We confirmed that heterologously expressed hERG currents are reduced by ibogaine in low micromolar concentrations. Moreover, at higher concentrations, the drug also reduced human Nav1.5 sodium and Cav1.2 calcium currents. Ion currents were as well reduced by 18-MC, yet with diminished potency. Unexpectedly, although blocking hERG channels, ibogaine did not prolong the action potential (AP) in guinea pig cardiomyocytes at low micromolar concentrations. Higher concentrations (≥ 10 μM) even shortened the AP. These findings can be explained by the drug's calcium channel inhibition, which counteracts the AP-prolonging effect generated by hERG blockade. Implementation of ibogaine's inhibitory effects on human ion channels in a computer model of a ventricular cardiomyocyte, on the other hand, suggested that ibogaine does prolong the AP in the human heart. We conclude that therapeutic concentrations of ibogaine have the propensity to prolong the QT interval of the electrocardiogram in humans. In some cases this may lead to cardiac arrhythmias.
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