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Pharmacokinetic characterization of the indole alkaloid ibogaine in rats.

L B Hough, A A Bagal, Stanley D Glick

Methods and findings in experimental and clinical pharmacology March 1, 2000 DOI: 10.1358/mf.2000.22.2.796066 (opens in new tab)

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Study at a glance

AI-extracted from the abstract
Characteristics Observational pharmacokinetic study Peer reviewed
Sample size 7
Population Rats
Intervention ibogaine
Dose 20 mg/kg
Duration Up to 3 h following i.v. infusion
Topics Ibogaine
Keywords Alkaloid Compound Pharmacokinetics Body processes Clearance Redistribution Duration Adipose tissue accumulation Fat tissue Concentration Prolonged presence
Citations 7
Key findings Ibogaine accumulates in adipose tissue at much higher concentrations than in other tissues, suggesting a prolonged presence in the body that may be underestimated by the measured terminal half-life.

Abstract

To investigate the pharmacokinetic properties of ibogaine, a putatively anti-addictive alkaloid, levels of this drug were quantified in plasma and tissues for up to 3 h following i.v. infusion in rats. Immediately following a 31-35 min infusion (20 mg/kg), mean plasma ibogaine levels were 373 ng/ml; these values declined rapidly thereafter in a biexponential manner. The plasma time course in 5 of 7 animals demonstrated an excellent fit to a two-compartment pharmacokinetic model, with alpha and beta half-lives of 7.3 min and 3.3 h, respectively. Drug clearance was estimated to be 5.9 l/h (n = 7). Ibogaine levels in brain, liver and kidney 3 h after the end of drug infusion were 143-170 ng/g, close to simulated values for the peripheral pharmacokinetic compartment. However, 3-h drug levels in adipose tissue were much higher (3,328 ng/g), implying the need for a more complex pharmacokinetic model. Mechanisms for the initial, rapid disappearance of plasma ibogaine are thought to include metabolic demethylation as well as redistribution to body stores. The sequestration of ibogaine by adipose tissue probably contributes to a protracted persistence of drug in the body. This persistence may be underestimated by the beta half-life reported in the present study.

Comparable studies

Other preclinical and animal studies on ibogaine, most cited first.

Study Year Design Participants
Noncompetitive Functional Inhibition at Diverse, Human Nicotinic Acetylcholine Receptor Subtypes by Bupropion, Phencyclidine, and Ibogaine TE671/RD cells (human muscle-type nAChR) and SH-SY5Y neuroblastoma cells (human... 1999 In vitro study
Degeneration of Purkinje cells in parasagittal zones of the cerebellar vermis after treatment with ibogaine or harmaline. Ibogaine- or harmaline-treated rats 1993 Experimental animal study
Effects and aftereffects of ibogaine on morphine self-administration in rats. Rats 1991 Preclinical experimental study
Effects of iboga alkaloids on morphine and cocaine self-administration in rats: relationship to tremorigenic effects and to effects on dopamine release in nucleus accumbens and striatum. Rats 1994 Experimental study
Glial Cell Line-Derived Neurotrophic Factor Mediates the Desirable Actions of the Anti-Addiction Drug Ibogaine against Alcohol Consumption Rats 2005 Experimental study

Citations in the library

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