Ibogaine: Complex Pharmacokinetics, Concerns for Safety, and Preliminary Efficacy Measures

  title={Ibogaine: Complex Pharmacokinetics, Concerns for Safety, and Preliminary Efficacy Measures},
  author={Deborah C. Mash and Craig A. Kovera and John Pablo and Rachel F. Tyndale and FRANK D. Ervin and IZBEN C. Williams and Edward G. Singleton and Manny Mayor},
  journal={Annals of the New York Academy of Sciences},
Ibogaine is an indole alkaloid found in the roots of Tabernanthe Iboga (Apocynaceae family), a rain forest shrub that is native to western Africa. Ibogaine is used by indigenous peoples in low doses to combat fatigue, hunger and thirst, and in higher doses as a sacrament in religious rituals. Members of American and European addict self‐help groups have claimed that ibogaine promotes long‐term drug abstinence from addictive substances, including psychostimulants and opiates. Anecdotal reports… 

DARK Classics in Chemical Neuroscience: Ibogaine.

Structural-activity studies led to the isolation of the ibogaine analog 18-methoxycoronaridine (18-MC), an α3β4 nicotinic receptor modulator that retains ibogane's anticraving properties with few or no adverse effects.

Ibogaine in the treatment of substance dependence.

Concerns about ibogaine's safety, as well as a dearth of solid data from human studies, have hampered progress in its development as an approved medication, and major findings from preclinical studies are outlined.

Ibogaine, an anti-addictive drug: pharmacology and time to go further in development. A narrative review

The purpose of this article was to review data from the literature concerning physicochemical properties, bio-analytical methods, and pharmacology of ibogaine; this article will be focused on the use of this drug as anti-addictive agent.

Detoxification from methadone using low, repeated, and increasing doses of ibogaine: A case report

It is not clear if ibogaine at low doses could be used therapeutically in people on methadone maintenance treatments (MMT), but a case report of a female on MMT for 17 years who performed a self-treatment with several low and cumulative doses of ibogance over a 6-week period successfully eliminated her withdrawal symptoms.

The Anti-Addiction Drug Ibogaine and the Heart: A Delicate Relation

The aim of this review is to recapitulate the current knowledge about ibogaine’s effects on the heart and the cardiovascular system, and to assess the cardiac risks associated with the use of this drug in anti- addiction therapy.

A Single Administration of the Atypical Psychedelic Ibogaine or its Metabolite Noribogaine Induces an Antidepressant-like Effect in Rats.

It is found that ibogaine and noribogaine induced a dose- and time-dependent antidepressant-like effect without significant changes of animal locomotor activity, which suggests a polypharmacological mechanism underpinning the antidepressant- like effects of ibogane and norIBogaine.

hERG Blockade by Iboga Alkaloids

Results may relate to observations of persistent QT prolongation and cardiac arrhythmia at delayed intervals of days following ibogaine ingestion, and suggest that the iboga alkaloids might provide an informative paradigm for investigation of the structural biology of the hERG channel.



Medication development of ibogaine as a pharmacotherapy for drug dependence.

A rising tolerance study using single administration of ibogaine for treatment of cocaine dependency is initiated to determine safety, pharmacokinetics and dose effects, and to identify relevant parameters of efficacy in cocaine-dependent patients.

Noribogaine stimulates naloxone‐sensitive [35S]GTPγS binding

The efficacy of noribogaine as a full μ-opioid agonist may explain ibogaine's ability to block the acute signs of opiate withdrawal and its suppressive effects on morphine self-administration.

Cytochrome P4502D6 catalyzes the O-demethylation of the psychoactive alkaloid ibogaine to 12-hydroxyibogamine.

Evidence is presented that the O-demethylation of ibogaine observed in human hepatic microsomes is catalyzed primarily by the polymorphically expressed cytochrome P-4502D 6 (CYP2D6) and that this isoform is the predominant enzyme of ib Bogaine O- Demethylation in humans.

Research issues related to development of medications for treatment of cocaine addiction.

  • M. Klein
  • Medicine, Psychology
    Annals of the New York Academy of Sciences
  • 1998
Draft guidelines for the study of medications for treatment of drug addiction have been developed by the Food and Drug Administration's (FDA's) Center for Drug Evaluation and Research, Division of

Identification and quantitation of ibogaine and an o-demethylated metabolite in brain and biological fluids using gas chromatography-mass spectrometry.

This report describes a sensitive method for quantitating ibogaine and a single major metabolite in biological fluids and brain tissue. We identified the metabolite as 12-hydroxy-ibogamine

Nonspecific binding to microsomes: impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine, and propranolol.

  • R. Obach
  • Biology, Chemistry
    Drug metabolism and disposition: the biological fate of chemicals
  • 1997
The nonspecific, noncovalent binding of three drugs, imipramine, warfarin, and propranolol, to pooled human and animal liver microsomes has been determined using equilibrium dialysis in conditions where no cofactor (NADPH) was included in the incubation, and the parameter fu(mic) is suggested to obtain when attempting to relate in vitro intrinsic clearance to in vivo clearance.

Cellular and molecular mechanisms of drug dependence.

The molecular and cellular actions of three classes of abused drugs--opiates, psychostimulants, and ethanol--are reviewed in the context of behavioral studies of drug dependence. The immediate