The pharmacokinetic fate of cannabidiol and its relationship to barbiturate sleep time

Karler, Ralph; Sangdee, Puckprink; Turkanis, Stuart A.; Borys, Henry K.

doi:10.1016/0006-2952(79)90358-7

Cited by 23 publications

(7 citation statements)

References 8 publications

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“…The dose of CBD was chosen based on anticonvulsant effects and pharmacokinetic studies (Karler et al, 1979; Turkanis et al, 1979; Siemens et al, 1980; Consroe et al, 1982; Jones et al, 2009). Gas chromatography has used to evaluate the CBD plasma levels during the experiments and ensure CBD was present during our experiment.…”

Section: Methodsmentioning

confidence: 99%

Protective Effects of Cannabidiol against Seizures and Neuronal Death in a Rat Model of Mesial Temporal Lobe Epilepsy

et al. 2017

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The present study reports the behavioral, electrophysiological, and neuropathological effects of cannabidiol (CBD), a major non-psychotropic constituent of Cannabis sativa, in the intrahippocampal pilocarpine-induced status epilepticus (SE) rat model. CBD was administered before pilocarpine-induced SE (group SE+CBDp) or before and after SE (group SE+CBDt), and compared to rats submitted only to SE (SE group), CBD, or vehicle (VH group). Groups were evaluated during SE (behavioral and electrophysiological analysis), as well as at days one and three post-SE (exploratory activity, electrophysiological analysis, neuron density, and neuron degeneration). Compared to SE group, SE+CBD groups (SE+CBDp and SE+CBDt) had increased SE latency, diminished SE severity, increased contralateral afterdischarge latency and decreased relative powers in delta (0.5–4 Hz) and theta (4–10 Hz) bands. Only SE+CBDp had increased vertical exploratory activity 1-day post SE and decreased contralateral relative power in delta 3 days after SE, when compared to SE group. SE+CBD groups also showed decreased neurodegeneration in the hilus and CA3, and higher neuron density in granule cell layer, hilus, CA3, and CA1, when compared to SE group. Our findings demonstrate anticonvulsant and neuroprotective effects of CBD preventive treatment in the intrahippocampal pilocarpine epilepsy model, either as single or multiple administrations, reinforcing the potential role of CBD in the treatment of epileptic disorders.

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Section: Methodsmentioning

confidence: 99%

Protective Effects of Cannabidiol against Seizures and Neuronal Death in a Rat Model of Mesial Temporal Lobe Epilepsy

et al. 2017

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“…It must be noted that none of the above studies reported on the metabolic fate of CBD and no information is available on the human pharmacokinetics of the metabolites. (For an early mouse study indicating slow elimination of unidentified polar metabolites, see Karler et al 55 ).…”

Section: Human Pharmacokinetics Of Cbd Upon Various Administration Romentioning

confidence: 99%

“… 94 It has also been proposed that the observed interference with drug metabolism in vivo could be due to one or more metabolites and not to the parent CB. 55 …”

Section: Biological Activity Studies With Cbd Metabolitesmentioning

confidence: 99%

Human Metabolites of Cannabidiol: A Review on Their Formation, Biological Activity, and Relevance in Therapy

Ujváry¹,

Hanŭs

2016

Cannabis and Cannabinoid Research

228

204

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Cannabidiol (CBD), the main nonpsychoactive constituent of Cannabis sativa, has shown a wide range of therapeutically promising pharmacological effects either as a sole drug or in combination with other drugs in adjunctive therapy. However, the targets involved in the therapeutic effects of CBD appear to be elusive. Furthermore, scarce information is available on the biological activity of its human metabolites which, when formed in pharmacologically relevant concentration, might contribute to or even account for the observed therapeutic effects. The present overview summarizes our current knowledge on the pharmacokinetics and metabolic fate of CBD in humans, reviews studies on the biological activity of CBD metabolites either in vitro or in vivo, and discusses relevant drug–drug interactions. To facilitate further research in the area, the reported syntheses of CBD metabolites are also catalogued.

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“…In view of the encouraging results with CBD in in vivo experiments 4 and in clinical trials,5d it is surprising that its metabolites have not been investigated for their pharmacological properties, as the probability exists that some of the effects observed are due to active metabolites rather than to CBD. Indeed prolongation of barbiturate sleeping time caused by CBD has been shown to be due to an unidentified metabolite …”

mentioning

confidence: 99%

“…Indeed prolongation of barbiturate sleeping time caused by CBD has been shown to be due to an unidentified metabolite. 6 The metabolism of CBD is well established. In numerous species, including man, 7a,b the first step is hydroxylation, mostly on C-7, leading to 7-hydroxy-CBD 2, followed by further oxidations.…”

mentioning

confidence: 99%

Synthesis of a Primary Metabolite of Cannabidiol

Tchilibon

Mechoulam

2000

Org. Lett.

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Cannabidiol 1 is the major nonpsychotropic, neutral constituent in most cannabis preparations. It is devoid of the psychoactive properties typical of cannabis; however, it produces numerous, potentially therapeutic pharmacological effects, some of which may be due to its metabolites. We report now the first total synthesis of 7-hydroxycannabidiol 2, a primary metabolite of cannabidiol, in an eight-step procedure.

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The pharmacokinetic fate of cannabidiol and its relationship to barbiturate sleep time

Cited by 23 publications

References 8 publications

Protective Effects of Cannabidiol against Seizures and Neuronal Death in a Rat Model of Mesial Temporal Lobe Epilepsy

Protective Effects of Cannabidiol against Seizures and Neuronal Death in a Rat Model of Mesial Temporal Lobe Epilepsy

Human Metabolites of Cannabidiol: A Review on Their Formation, Biological Activity, and Relevance in Therapy

Synthesis of a Primary Metabolite of Cannabidiol

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