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

@article{Mash2000IbogaineCP,
  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 Ervin and I. C. Williams and Edward G. Singleton and M. Mayor},
  journal={Annals of the New York Academy of Sciences},
  year={2000},
  volume={914}
}
  • D. Mash, C. Kovera, +5 authors M. Mayor
  • Published 1 September 2000
  • Psychology, Medicine
  • 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… Expand
Ibogaine for treating drug dependence. What is a safe dose?
TLDR
To consider an appropriate and safe initial dose for humans, necessary safety factors need to be applied to the animal data; these would include factors such as intra- and inter-species variability and for susceptible people in a population (such as drug users). Expand
Ibogaine as a treatment for substance misuse: Potential benefits and practical dangers.
TLDR
There is a need to develop better opiate detoxification treatment against a background of increasing opioid-related fatalities, and a congener of ibogaine, 18-MC, appears to be safer and is to undergo clinical trials. Expand
Comparative neuropharmacology of ibogaine and its O-desmethyl metabolite, noribogaine.
TLDR
Ibogaine and noribogaine are equipotent in their ability to evoke a transient stimulation of dopamine metabolism that is characterized by profound depletion of tissue DA in mesolimbic, mesocortical, and mesostriatal terminal projection areas. Expand
Breaking the cycle of opioid use disorder with Ibogaine
  • Deborah C Mash
  • Medicine
  • The American journal of drug and alcohol abuse
  • 2018
TLDR
Two studies demonstrate that ibogaine may have significant pharmacological effects that include blockade of the acute signs and symptoms of opioid withdrawal (SOWS) and the post-acute withdrawal syndrome (cravings and depression). Expand
DARK Classics in Chemical Neuroscience: Ibogaine.
TLDR
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. Expand
Ibogaine in the treatment of substance dependence.
TLDR
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. Expand
Ibogaine, an anti-addictive drug: pharmacology and time to go further in development. A narrative review
TLDR
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. Expand
Detoxification from methadone using low, repeated, and increasing doses of ibogaine: A case report
TLDR
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. Expand
The Anti-Addiction Drug Ibogaine and the Heart: A Delicate Relation
TLDR
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. Expand
A Single Administration of the Atypical Psychedelic Ibogaine or its Metabolite Noribogaine Induces an Antidepressant-like Effect in Rats.
TLDR
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. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 24 REFERENCES
Medication development of ibogaine as a pharmacotherapy for drug dependence.
TLDR
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. Expand
A preliminary investigation of ibogaine: case reports and recommendations for further study.
TLDR
Ibogaine, an alkaloid with psychotropic effects at doses of 200-300 mg and above, was taken by seven individuals who were addicted to opiates and may serve as a model for the development of improved agents for the treatment of substance abuse in the future. Expand
Identification of a primary metabolite of ibogaine that targets serotonin transporters and elevates serotonin.
TLDR
It is reported here that 12-hydroxyibogamine, a primary metabolite of ibogaine, displays high affinity for the 5-HT transporter and elevates extracellular 5- HT and may heighten mood and attenuate drug craving. Expand
Noribogaine stimulates naloxone‐sensitive [35S]GTPγS binding
NORIBOGAINE is formed in vivo by the O-demethylation of the indole alkaloid ibogaine. We report here that noribogaine acts as a full agonist at the μ-opioid receptor. Noribogaine-stimulated guanylylExpand
Cytochrome P4502D6 catalyzes the O-demethylation of the psychoactive alkaloid ibogaine to 12-hydroxyibogamine.
  • R. Obach, J. Pablo, D. Mash
  • Chemistry, Medicine
  • Drug metabolism and disposition: the biological fate of chemicals
  • 1998
TLDR
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. Expand
Research issues related to development of medications for treatment of cocaine addiction.
  • M. Klein
  • Medicine
  • 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 ofExpand
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-ibogamineExpand
Neurobiological Similarities in Depression and Drug Dependence: A Self-Medication Hypothesis
TLDR
It is concluded that drug dependence and depression may be associated with alterations in some of the same neurotransmitter systems and, in particular, with alterations of neurotransmitter function in limbic-related brain structures, and may be linked by some shared neurobiology. Expand
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
  • Chemistry, Medicine
  • Drug metabolism and disposition: the biological fate of chemicals
  • 1997
TLDR
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. Expand
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 immediateExpand
...
1
2
3
...