Cannabidiol (CBD) Dosing: Plasma Pharmacokinetics and Effects on Accumulation in Skeletal Muscle, Liver and Adipose Tissue

Child, Robert B.; Tallon, Mark J

doi:10.3390/nu14102101

Cited by 27 publications

(18 citation statements)

References 49 publications

(67 reference statements)

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Section: Resultsmentioning

confidence: 99%

“…One study examined sex differences in CBD pharmacokinetics after acute and repeated dosing in adult rats [ 57 ]. Child and Tallon (2022) administered 30, 115, or 230 mg/kg CBD daily by oral gavage for 28 days and assessed CBD pharmacokinetics on day 1 and day 28 [ 57 ]. At the 115 mg/kg dose, there was a significantly higher day 28 AUC 0–24h in females (50,561 ± 15,090) compared to males (28,602 ± 8486).…”

Section: Resultsmentioning

confidence: 99%

“…In mice, higher embryonic brain CBD concentrations were found in females compared to males after gestational exposure to CBD, which the authors suggested could be due to enzymatic differences driving sexual differentiation [ 50 ]. In adult rats, CBD concentrations were significantly higher in females compared to males (after 28 days of dosing, but not after the first day of dosing), and there was a tissue-specific sex difference in distribution, with greater liver CBD concentrations in females compared to males [ 57 ]. In a single-dose trial with healthy human volunteers, there was a significant sex difference in CBD concentrations with at least one formulation, with greater AUC in females compared to males [ 61 ].…”

Section: Discussionmentioning

confidence: 99%

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Sex Differences in the Neuropsychiatric Effects and Pharmacokinetics of Cannabidiol: A Scoping Review

2022

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Cannabidiol (CBD) is a non-intoxicating cannabinoid compound with diverse molecular targets and potential therapeutic effects, including effects relevant to the treatment of psychiatric disorders. In this scoping review, we sought to determine the extent to which sex and gender have been considered as potential moderators of the neuropsychiatric effects and pharmacokinetics of CBD. In this case, 300 articles were screened, retrieved from searches in PubMed/Medline, Scopus, Google Scholar, PsycInfo and CINAHL, though only 12 met our eligibility criteria: eight studies in preclinical models and four studies in humans. Among the preclinical studies, three suggested that sex may influence long-term effects of gestational or adolescent exposure to CBD; two found no impact of sex on CBD modulation of addiction-relevant effects of Δ⁹-tetrahydrocannabinol (THC); two found antidepressant-like effects of CBD in males only; and one found greater plasma and liver CBD concentrations in females compared to males. Among the human studies, two found no sex difference in CBD pharmacokinetics in patient samples, one found greater plasma CBD concentrations in healthy females compared to males, and one found no evidence of sex differences in the effects of CBD on responses to trauma recall in patients with post-traumatic stress disorder (PTSD). No studies were identified that considered the role of gender in CBD treatment effects. We discuss potential implications and current limitations of the existing literature.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Sex Differences in the Neuropsychiatric Effects and Pharmacokinetics of Cannabidiol: A Scoping Review

2022

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“…Comparison of a single oral dose of CBD (115mg/kg) given to male and female rats shows that females reach a peak plasma concentration after 7:45 hrs, while males reach a peak concentration at 8:25 hrs 27 . While accumulation of CBD in tissue was not evaluated after acute administration, after 28 days of chronic treatment, males and females did not significantly differ in CBD levels in adipose or muscle tissue, but females had significantly higher levels of CBD than males in liver 27 . A more comprehensive evaluation of plasma THC and CBD over time and at multiple doses in both males and females would help determine which variables account for these differences in THC accumulation across studies and clarify the pharmacokinetics of CBD in both sexes.…”

Section: Discussionmentioning

confidence: 99%

Plasma and Liver Lipids are Differentially Regulated After Cannabinoid Treatments in Male and Female Mice

Johnson

Bosquez-Berger

Bentz

et al. 2023

Preprint

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Cannabinoids (CBs) have sex-dependent behavioral and physiological effects and modulate lipids across the body. To understand how some of these sex differences may be due to differences how both phyto- and endocannabinoids are regulated in the liver and plasma, male and female CD1 mice were administered 10 mg/kg i.p. of cannabidiol (CBD), ∆9-tetrahydrocannabinol (THC), or THC+CBD then core blood and liver tissue were collected after 2 hours. Lipids were extracted from both liver and plasma, and samples were screened via HPLC/MS/MS for ∆9-tetrahydrocannabinol (THC), metabolites 11-OH-THC and 11-COOH-THC, cannabidiol (CBD), metabolites 7-OH-CBD and 7-COOH-CBD, ~70 endolipids including the endocannabinoids, N-arachidonoyl ethanolamine (Anandamide; AEA) and 2-sn-arachidonoyl glycerol (2-AG). Structural analogs to AEA (e.g. lipoamino acids, lipoamines) and 2-acyl glycerols) as well as free fatty acids and prostaglandins were also evaluated. Results show that at 2 hours post injection levels of CBs demonstrate key differences between males and females in both plasma and liver, and that these differences vary when co-administered as opposed to administered alone. Illustrating a link between liver and plasma, directionality of CB differences are similar between the two tissue types as a function of both sex and CB treatment. By contrast, endolipids had very different profiles as a function of sex, CB administration, and tissue type. Importantly, there are baseline differences between male and female mice in endocannabinoids and related lipids, which likely impact how CB administration modulates these endolipids. These data illustrate the complexity of outcomes of CB treatment between males and females on circulating CBs and endolipids and highlight the need to consider these factors when evaluating efficacy of CB drug treatments or usage.

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“…In an earlier study, it has been shown that perfusion of isolated rat hearts with buffer containing [ 3 H]-CBD results in strong accumulation of radioactivity in the tissue ( Smiley et al, 1976 ). Recently, chronic (28 days) administration of CBD (230 mg/kg) was shown to reach CBD concentrations of 2.7 µM and 3.3 µM in muscle and liver tissue, respectively ( Child and Tallon, 2022 ). Therefore, the membrane concentrations of cannabinoids are likely to reach to pharmacologically relevant ranges to exert their effects on the functional properties of LGICs described in this review.…”

Section: Discussionmentioning

confidence: 99%

Effects of cannabinoids on ligand-gated ion channels

2022

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Phytocannabinoids such as Δ9-tetrahydrocannabinol and cannabidiol, endocannabinoids such as N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol, and synthetic cannabinoids such as CP47,497 and JWH-018 constitute major groups of structurally diverse cannabinoids. Along with these cannabinoids, CB1 and CB2 cannabinoid receptors and enzymes involved in synthesis and degradation of endocannabinoids comprise the major components of the cannabinoid system. Although, cannabinoid receptors are known to be involved in anti-convulsant, anti-nociceptive, anti-psychotic, anti-emetic, and anti-oxidant effects of cannabinoids, in recent years, an increasing number of studies suggest that, at pharmacologically relevant concentrations, these compounds interact with several molecular targets including G-protein coupled receptors, ion channels, and enzymes in a cannabinoid-receptor independent manner. In this report, the direct actions of endo-, phyto-, and synthetic cannabinoids on the functional properties of ligand-gated ion channels and the plausible mechanisms mediating these effects were reviewed and discussed.

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Cannabidiol (CBD) Dosing: Plasma Pharmacokinetics and Effects on Accumulation in Skeletal Muscle, Liver and Adipose Tissue

Cited by 27 publications

References 49 publications

Sex Differences in the Neuropsychiatric Effects and Pharmacokinetics of Cannabidiol: A Scoping Review

Sex Differences in the Neuropsychiatric Effects and Pharmacokinetics of Cannabidiol: A Scoping Review

Plasma and Liver Lipids are Differentially Regulated After Cannabinoid Treatments in Male and Female Mice

Effects of cannabinoids on ligand-gated ion channels

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