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Toxicological properties of Δ9-tetrahydrocannabinol and cannabidiol Cover

Toxicological properties of Δ9-tetrahydrocannabinol and cannabidiol

By: Katarina Černe  
Open Access
|Apr 2020

Figures & Tables

Recommended post-marketing studies to obtain a complete safety profile of cannabidiol (CBD)

Non-clinical toxicity studies
Toxicity studies with CBD metabolite 7-COOH-cannabidiol in rat:

- embryo-foetal developmental study

- pre- and postnatal developmental study

- juvenile animal toxicity study

- 2-year carcinogenicity study with gavage

Toxicity studies with CBD

- 2-year carcinogenicity study in mouse

- 2-year carcinogenicity study in rat with gavage

Clinical studies

- Potential for chronic liver injury

- Effect on glomerular filtration rate

- Pregnancy outcome study

- QT interval prolongation trial at the maximum tolerable dose

Drug-drug interaction trials in healthy volunteers

CBD effect on the pharmacokinetics of:

- caffeine

- sensitive CYP2B6

cytochrome P450

and CYP2C9 substrate

- sensitive UGP1A9

UDP-glucuronosyltransferase

and UGTB7 substrate

Strong CYP3A inhibitor effects on pharmacokinetics of CBD

Strong 2C9 inhibitor effects on pharmacokinetics of CBD

Rifampin effects on pharmacokinetics of CBD

Cannabidiol (CBD) abuse potential

TYPE OF STUDYRESULTS
Receptor binding studies

- cannabinoid receptorsno significant affinity

- opioid receptorsno significant affinity

Non-clinical studies evaluating general behaviour (similarity to THC)

- tetrad testno meaningful abuse related signal

- drug discrimination studyno meaningful abuse related signal

- self-administration studyno meaningful abuse related signal

Clinical studies evaluating efficacy and safety in patients with LGS

Lennox-Gastaut syndrome

or DS

Dravet syndrome


- Phase I clinical studyno euphoria or other abuse-related signals

- Phase II/III studiescould not be evaluated

concomitant use of other seizure drugs and limited capacity of patients


Phase I human abuse potential (HAP) study (N=40, with 35 completers)

randomized, double blind, placebo-controlled trial

subjects: healthy recreational poly-drug users

positive control: THC (10, 30 mg), alprazolam (2 mg)

negative control: placebo

mean DRUG LIKING SCORE

lower therapeutic dose: 750 mg/daynot significantly different

higher therapeutic dose: 1500 mg/daysignificantly different (very small increase)

supra-therapeutic dose: 4500 mg/daysignificantly different (very small increase)

Human physical dependence study following chronic administration

3 days after discontinuationno withdrawal signs and symptoms
DOI: https://doi.org/10.2478/aiht-2020-71-3301 | Journal eISSN: 1848-6312 | Journal ISSN: 0004-1254
Language: English, Croatian, Slovenian
Page range: 1 - 11
Submitted on: Jun 1, 2019
Accepted on: Mar 1, 2020
Published on: Apr 9, 2020
Published by: Institute for Medical Research and Occupational Health
In partnership with: Paradigm Publishing Services
Publication frequency: 4 issues per year

© 2020 Katarina Černe, published by Institute for Medical Research and Occupational Health
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.