Page last updated: 2024-12-08

ibogaine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

Ibogaine: One of several indole alkaloids extracted from Tabernanthe iboga, Baill. It has a complex pharmacological profile, and interacts with multiple systems of neurotransmission. Ibogaine has psychoactive properties and appears to modulate tolerance to opiates. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ibogaine : An organic heteropentacyclic compound that is ibogamine in which the indole hydrogen para to the indole nitrogen has been replaced by a methoxy group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
Tabernanthegenus[no description available]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]
Tabernanthe ibogaspecies[no description available]ApocynaceaeThe dogbane family of the order Gentianales. Members of the family have milky, often poisonous juice, smooth-margined leaves, and flowers in clusters.[MeSH]

Cross-References

ID SourceID
PubMed CID317505
MeSH IDM0010963

Synonyms (6)

Synonym
ibogamine, 12-methoxy-
nsc249764
nsc-249764
(-)-ibogaine
ibogaine
83-74-9

Research Excerpts

Toxicity

The use of ibogaine often occurs with no medical supervision in uncontrolled settings, and its use has been associated with several reports of severe adverse events. Single oral doses of noribogaine 3-60 mg were safe and well tolerated in healthy volunteers. That a lesion of the inferior olive almost completely prevents the neurotoxicity demonstrates that ibogane is not directly toxic to Purkinje cells.

ExcerptReferenceRelevance
" That a lesion of the inferior olive almost completely prevents the neurotoxicity demonstrates that ibogaine is not directly toxic to Purkinje cells, but that the toxicity is indirect and dependent on integrity of the olivocerebellar projection."( The olivocerebellar projection mediates ibogaine-induced degeneration of Purkinje cells: a model of indirect, trans-synaptic excitotoxicity.
Molliver, ME; O'Hearn, E, 1997
)
0.3
"To evaluate acute toxic effect of ibogaine and noribogaine on the survival of mice and determine median lethal doses of the substances mentioned."( Acute toxicity of ibogaine and noribogaine.
Ivanov, L; Kazlauskas, S; Kubiliene, A; Marksiene, R; Razukas, A; Sadauskiene, I, 2008
)
0.35
" Single oral doses of noribogaine 3-60 mg were safe and well tolerated in healthy volunteers."( Ascending-dose study of noribogaine in healthy volunteers: pharmacokinetics, pharmacodynamics, safety, and tolerability.
Friedhoff, L; Glue, P; Hung, CT; Hung, N; Lam, F; Lockhart, M, 2015
)
0.42
"Its pharmacokinetics in toxic states is not well understood."( Internet-purchased ibogaine toxicity confirmed with serum, urine, and product content levels.
Friesen, MW; Gerona, RR; Ly, BT; O'Connell, CW, 2015
)
0.42
" The most frequent treatment-emergent non-OWS adverse events were headache, nausea, constipation, and neck pain."( Switching Opioid-Dependent Patients From Methadone to Morphine: Safety, Tolerability, and Methadone Pharmacokinetics.
Cape, G; Devane, J; Friedhoff, L; Glue, P; Gray, A; Harland, S; Howes, J; Hung, CT; Hung, N; Lam, F; Lockhart, M; Tunnicliff, D; Weis, H, 2016
)
0.43
" In the current study, a noribogaine dose of 320mg/kg was considered to be the EEG no observed adverse effect level (NOAEL) in conscious freely moving cynomolgus monkeys."( Functional neurotoxicity evaluation of noribogaine using video-EEG in cynomolgus monkeys.
Accardi, MV; Arezzo, J; Authier, S; Friedhoff, LT; Gerson, RJ; Paquette, D; Pouliot, M; Stubbs, RJ; Weis, H,
)
0.13
" 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)."( Ibogaine for treating drug dependence. What is a safe dose?
Galea, S; Newcombe, D; Schep, LJ; Slaughter, RJ, 2016
)
0.43
" Despite the potential therapeutic effects, several cases of fatalities and serious adverse events related to ibogaine/noribogaine use can be found in the literature."( The adverse events of ibogaine in humans: an updated systematic review of the literature (2015-2020).
Borràs, T; Bouso, JC; Colomina, MT; Dos Santos, RG; Hallak, JEC; Ona, G; Rocha, JM, 2022
)
0.72
"To update (2015-2020) the literature on the adverse events and fatalities associated with ibogaine/noribogaine administration."( The adverse events of ibogaine in humans: an updated systematic review of the literature (2015-2020).
Borràs, T; Bouso, JC; Colomina, MT; Dos Santos, RG; Hallak, JEC; Ona, G; Rocha, JM, 2022
)
0.72
" The adverse events were classified in acute effects (< 24 h), mainly cardiac (the most common was QTc prolongation), gastrointestinal, neurological, and clinical alterations, and long-lasting effects (> 24 h), mainly persistent cardiac alterations, psychiatric, and neurological signs."( The adverse events of ibogaine in humans: an updated systematic review of the literature (2015-2020).
Borràs, T; Bouso, JC; Colomina, MT; Dos Santos, RG; Hallak, JEC; Ona, G; Rocha, JM, 2022
)
0.72
" The use of ibogaine often occurs with no medical supervision in uncontrolled settings, and its use has been associated with several reports of severe adverse events."( Identifying setting factors associated with improved ibogaine safety: a systematic review of clinical studies.
Bouso, JC; Dos Santos, RG; Hallak, JEC; Reis, JAS; Rocha, JM, 2023
)
0.91

Pharmacokinetics

The objectives of this Phase I study were to assess the safety, tolerability, pharmacokinetic, and pharmacodynamic profiles of noribogaine. Blood concentration-time effect profiles of ibogaine and noribogsaine obtained for individual subjects after single oral dose administrations demonstrate complex pharmacokinetics profiles.

ExcerptReferenceRelevance
" Blood concentration-time effect profiles of ibogaine and noribogaine obtained for individual subjects after single oral dose administrations demonstrate complex pharmacokinetic profiles."( Ibogaine: complex pharmacokinetics, concerns for safety, and preliminary efficacy measures.
Ervin, FD; Kovera, CA; Mash, DC; Mayor, M; Pablo, J; Singleton, EG; Tyndale, RF; Williams, IC, 2000
)
0.31
" The objectives of this Phase I study were to assess the safety, tolerability, pharmacokinetic, and pharmacodynamic profiles of noribogaine."( Ascending-dose study of noribogaine in healthy volunteers: pharmacokinetics, pharmacodynamics, safety, and tolerability.
Friedhoff, L; Glue, P; Hung, CT; Hung, N; Lam, F; Lockhart, M, 2015
)
0.42
" We compared 168 hours pharmacokinetic profiles of both analytes after a single oral 20 mg dose of ibogaine in 21 healthy subjects who had been pretreated for 6 days with placebo or the CYP2D6 inhibitor paroxetine."( Influence of CYP2D6 activity on the pharmacokinetics and pharmacodynamics of a single 20 mg dose of ibogaine in healthy volunteers.
Garbe, K; Glue, P; Hung, CT; Jakobi, H; Lenagh-Glue, Z; Lyudin, A; Winter, H, 2015
)
0.42
" Pharmacokinetic evaluation showed that 91% of methadone was cleared during this time, with a mean elimination half-life of 59 hours."( Switching Opioid-Dependent Patients From Methadone to Morphine: Safety, Tolerability, and Methadone Pharmacokinetics.
Cape, G; Devane, J; Friedhoff, L; Glue, P; Gray, A; Harland, S; Howes, J; Hung, CT; Hung, N; Lam, F; Lockhart, M; Tunnicliff, D; Weis, H, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" These data show that there are sex differences in the effects of ibogaine and that this may be due to decreased bioavailability of ibogaine in males as compared to females."( Sex differences in ibogaine antagonism of morphine-induced locomotor activity and in ibogaine brain levels and metabolism.
Boyd, DL; Glick, SD; Hough, LB; Pearl, SM, 1997
)
0.3
" The absolute bioavailability of voacangine was determined to be 11-13 %."( Pharmacokinetics of hERG Channel Blocking Voacangine in Wistar Rats Applying a Validated LC-ESI-MS/MS Method.
Carreño, F; Dalla Costa, T; de Araújo, BV; de Miranda Silva, C; Grienke, U; Kratz, JM; Mair, CE; Rollinger, JM; Zimmermann, ES, 2016
)
0.43

Dosage Studied

Ibogaine (IBO), and a synthetic iboga alkaloid congener, 18-methoxycoronaridine (18-MC), increase the potency of cocaine to elicit behavioral sensitization. Local perfusion with ibogaine via microdialysis probes in the nucleus accumbens or striatum of rats produced a biphasic dose-response effect on extracellular dopamine levels. In chronic cocaine but not in acute cocaine rats, Ibogaine pretreatment enhanced the locomotor response to 5 and 10 mg/kg cocaine.

ExcerptRelevanceReference
" Tremorolytic potency (ED50) was calculated from dose-response curves."( Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. A comparison with prolyl-leucylglycine amide (MIF), anti-Parkinsonian drugs and clonazepam.
Zetler, G, 1983
)
0.27
" Once trained, these rats were used to investigate the dose-response effects to ibogaine from each of the three suppliers."( Comparison of the behavioral effects of ibogaine from three sources: mediation of discriminative activity.
Gordon, TL; Schechter, MD, 1993
)
0.29
" One hr after ip dosing (40 mg/kg), drug levels ranged from 106 ng/ml (plasma) to 11,308 ng/g (fat), with significantly higher values after sc administration of the same dose."( Tissue distribution of ibogaine after intraperitoneal and subcutaneous administration.
Glick, SD; Hough, LB; Pearl, SM, 1996
)
0.29
" Together, the data indicate that IBG damages areas of the brain outside the cerebellum and that the sites damaged are dependent on sex and dosage regimen."( Acute and chronic administration of ibogaine to the rat results in astrogliosis that is not confined to the cerebellar vermis.
O'Callaghan, JP; Page, JG; Rodman, LE; Rogers, TS, 1996
)
0.29
"Local perfusion with ibogaine (10(-6) M-10(-3) M) via microdialysis probes in the nucleus accumbens or striatum of rats produced a biphasic dose-response effect on extracellular dopamine levels."( Neuropharmacological characterization of local ibogaine effects on dopamine release.
Berger, SP; Broderick, PA; Hsu, K; Reid, MS; Souza, KH, 1996
)
0.29
" Lu 28-179 and BD 1008 potentiated dose-dependently the NMDA response and generated bell-shaped dose-response curves."( Modulation of the neuronal response to N-methyl-D-aspartate by selective sigma2 ligands.
Couture, S; Debonnel, G, 1998
)
0.3
" Furthermore, due to the shape of the dose-response curve, in chronic cocaine but not in acute cocaine rats, ibogaine pretreatment enhanced the locomotor response to 5 and 10 mg/kg cocaine while decreasing the locomotor response to 40 mg/kg cocaine."( Pretreatment with the putative anti-addictive drug, ibogaine, increases the potency of cocaine to elicit locomotor responding: a study with acute and chronic cocaine-treated rats.
Glick, SD; Maisonneuve, IM; Szumlinski, KK, 1999
)
0.3
" 18-Methoxycoronaridine produced a downward shift in the entire morphine dose-response curve without any displacement to the left or right."( Attenuation of the reinforcing efficacy of morphine by 18-methoxycoronaridine.
Glick, SD; Maisonneuve, IM, 1999
)
0.3
" Compared to vehicle pretreated controls, 18-MC increased the potency of morphine, shifting the dose-response curve to the left, in acute morphine treated rats; however, 18-MC did not alter the potency of morphine in rats treated repeatedly with morphine."( The potential anti-addictive agent, 18-methoxycoronaridine, blocks the sensitized locomotor and dopamine responses produced by repeated morphine treatment.
Glick, SD; Maisonneuve, IM; Szumlinski, KK, 2000
)
0.31
" Recent dose-response studies demonstrated that pretreatment with the putative antiaddictive agent, ibogaine (IBO), and a synthetic iboga alkaloid congener, 18-methoxycoronaridine (18-MC), increase the potency of cocaine to elicit behavioral sensitization, an effect proposed to contribute, in part, to their ability to attenuate drug self-administration."( Interactions between iboga agents and methamphetamine sensitization: studies of locomotion and stereotypy in rats.
Balogun, MY; Glick, SD; Maisonneuve, IM; Szumlinski, KK, 2000
)
0.31
" Dose-response curves for nicotine (0."( The development and expression of locomotor sensitization to nicotine in the presence of ibogaine.
Shoaib, M; Stolerman, IP; Zubaran, C, 2000
)
0.31
" Subjects established on daily methadone OST (mean dose 60 mg/day) were switched to morphine slow-release capsules, dosed at 4× the previous total daily methadone dose, for 6 days, then given morphine syrup dosed q3h."( Switching Opioid-Dependent Patients From Methadone to Morphine: Safety, Tolerability, and Methadone Pharmacokinetics.
Cape, G; Devane, J; Friedhoff, L; Glue, P; Gray, A; Harland, S; Howes, J; Hung, CT; Hung, N; Lam, F; Lockhart, M; Tunnicliff, D; Weis, H, 2016
)
0.43
", 160 and 320mg/kg, PO) with an interval between dosing of at least 6days, and the resulting behavioral and EEG effects were evaluated."( Functional neurotoxicity evaluation of noribogaine using video-EEG in cynomolgus monkeys.
Accardi, MV; Arezzo, J; Authier, S; Friedhoff, LT; Gerson, RJ; Paquette, D; Pouliot, M; Stubbs, RJ; Weis, H,
)
0.13
" dosing and a one-compartmental model with two first-order absorption rates for oral dosing."( Pharmacokinetics of hERG Channel Blocking Voacangine in Wistar Rats Applying a Validated LC-ESI-MS/MS Method.
Carreño, F; Dalla Costa, T; de Araújo, BV; de Miranda Silva, C; Grienke, U; Kratz, JM; Mair, CE; Rollinger, JM; Zimmermann, ES, 2016
)
0.43
" However oral dosing is the preferred route clinically."( Acute oral 18-methoxycoronaridine (18-MC) decreases both alcohol intake and IV nicotine self-administration in rats.
Cauley, MC; Glick, S; Levin, ED; Rezvani, AH; Rose, JE; Slade, S; Wells, C,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (426)

TimeframeStudies, This Drug (%)All Drugs %
pre-199040 (9.39)18.7374
1990's135 (31.69)18.2507
2000's105 (24.65)29.6817
2010's117 (27.46)24.3611
2020's29 (6.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (1.80%)5.53%
Reviews54 (12.13%)6.00%
Case Studies22 (4.94%)4.05%
Observational4 (0.90%)0.25%
Other357 (80.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Tolerability and Efficacy of Ibogaine in the Treatment of Alcoholism: the First Randomized, Double-blind, Placebo-controlled, Escalating-dose, Phase 2 Trial [NCT03380728]Phase 212 participants (Anticipated)Interventional2022-10-30Enrolling by invitation
Ibogaine to Determine Maximum Tolerated Dose (MTD) or Treat-to-Target Dose (TTD) for the Evaluation of Efficacy and Safety [NCT05029401]Phase 1/Phase 2116 participants (Anticipated)Interventional2021-04-01Recruiting
Preliminar Efficacy and Safety of Ibogaine in the Treatment of Methadone [NCT04003948]Phase 220 participants (Anticipated)Interventional2020-10-28Recruiting
A Pre-post Study Evaluating the Safety and Efficacy of Ibogaine-Magnesium Therapy in Veterans With Sequelae of Repeated Blast Exposure [NCT04313712]30 participants (Anticipated)Observational2021-11-15Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]