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

Summary: 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 overview summarizes 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. Read more

 

Identification of Psychoactive Degradants of Cannabidiol in Simulated Gastric and Physiological Fluid

Summary: In recent research, orally administered cannabidiol (CBD) showed a relatively high incidence of sleepiness in a pediatric population. Previous work has suggested that when CBD is exposed to an acidic environment, it degrades to THC and other psychoactive cannabinoids. To gain a better understanding of quantitative exposure, an in vitro study was completed, evaluating the formation of psychoactive cannabinoids when CBD is exposed to simulated gastric fluid (SGF). Read more