“In Switzerland, medical cannabinoids can be prescribed under compassionate use after special authorization in justified indications such as refractory pain. Evidence of efficacy in pain is limited and the clinical benefit seems to be modest. Their drug-drug interactions (DDI) profile is poorly documented. Cytochromes P450 (CYP) 2C9 and 3A4 are involved in the metabolism of tetrahydrocannabinol and cannabidiol, which implies possible DDI with CYP450 inhibitor and inducer, such as anticonvulsivants and HIV protease inhibitors, which may be prescribed in patients with neuropathic pain.”
Tag Archives: cannabidiol
HU-446 and HU-465, derivatives of the non-psychoactive cannabinoid cannabidiol, decrease the activation of encephalitogenic T cells.
“Cannabidiol (CBD), the non-psychoactive cannabinoid, has been previously shown by us to decrease peripheral inflammation and neuroinflammation in mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis (MS).
Here we have studied the anti-inflammatory effects of newly synthesized derivatives of natural (-)-CBD ((-)-8,9-dihydro-7-hydroxy-CBD; HU-446) and of synthetic (+)-CBD ((+)-8,9-dihydro-7-hydroxy-CBD; HU-465)…
These results suggest that HU-446 and HU-465 have anti-inflammatory potential in inflammatory and autoimmune diseases. ”
Cannabidiol is a negative allosteric modulator of the type 1 cannabinoid receptor.
“Cannabidiol has been reported to act as an antagonist of cannabinoid agonists at type 1 cannabinoid receptors (CB1 ).
We hypothesized that cannabidiol can inhibit cannabinoid agonist activity through negative allosteric modulation of CB1…
Cannabidiol behaved as a non-competitive negative allosteric modulator of CB1 .
Allosteric modulation, in conjunction with non-CB1 effects, may explain the in vivo effects of cannabidiol.
Allosteric modulators of CB1 have the potential to treat central nervous system and peripheral disorders while avoiding the adverse effects associated with orthosteric agonism or antagonism of CB1.”
Drug-drug interaction between clobazam and cannabidiol in children with refractory epilepsy.
“Under an expanded access investigational new drug (IND) trial, cannabidiol (CBD) is being studied as a possible adjuvant treatment of refractory epilepsy in children.
Of the 25 subjects in the trial, 13 were being treated with clobazam (CLB). Because CLB and CBD are both metabolized in the cytochrome P450 (CYP) pathway, we predicted a drug-drug interaction, which we evaluate in this article…
Monitoring of CLB and nCLB levels is necessary for clinical care of patients concomitantly on CLB and CBD.
Nonetheless, CBD is a safe and effective treatment of refractory epilepsy in patients receiving CLB treatment.”
Evaluation of Serum Cytokines Levels and the Role of Cannabidiol Treatment in Animal Model of Asthma.
“Asthma represents a public health problem and traditionally is classified as an atopic disease, where the allergen can induce clinical airway inflammation, bronchial hyperresponsiveness, and reversible obstruction of airways.
Studies have demonstrated the presence of T-helper 2 lymphocytes in the lung of patients with asthma. These cells are involved in cytokine production that regulates immunoglobulin synthesis.
Recognizing that T cell interaction with antigens/allergens is key to the development of inflammatory diseases, the aim of this study is to evaluate the anti-inflammatory potential of cannabidiol (CBD) in this setting.
CBD treatment was able to decrease the serum levels of all analyzed cytokines except for IL-10 levels.
CBD seems to be a potential new drug to modulate inflammatory response in asthma.” http://www.ncbi.nlm.nih.gov/pubmed/26101464
“In conclusion, we here demonstrate that the administration of CBD in an animal model of asthma could blunt the serum cytokine response to OVA in sensitized animals. These effects suggest a potential for a new asthma treatment since CBD controls the exaggerated inflammatory response observed in this model.” https://www.hindawi.com/journals/mi/2015/538670/
Cardioprotective effect of cannabidiol in rats exposed to doxorubicin toxicity.
“The potential protective effect of cannabidiol, the major non-psychotropic Cannabis constituent, was investigated against doxorubicin cardiotoxicity in rats.
Histopathological examination showed that cannabidiol ameliorated doxorubicin-induced cardiac injury.
Immunohistochemical analysis revealed that cannabidiol significantly reduced the expression of inducible nitric oxide synthase, nuclear factor-κB, Fas ligand and caspase-3, and increased the expression of survivin in cardiac tissue of doxorubicin-treated rats.
These results indicate that cannabidiol represents a potential protective agent against doxorubicin cardiac injury.”
Cannabidiol, a nonpsychoactive Cannabis constituent, protects against myocardial ischemic reperfusion injury
“CANNABINOIDS ARE NATURAL and synthetic compounds structurally or pharmacologically related to the constituents of the plant Cannabis sativa or to the endogenous agonists (endocannabinoids) of the cannabinoid CB1 and CB2 receptors.
Cannabidiol (CBD) is a major cannabinoid constituent of Cannabis.
In contrast to tetrahydrocannabinol, CBD binds very weakly to CB1 and CB2 receptors. Contrary to most cannabinoids, CBD does not induce psychoactive or cognitive effects.
CBD has been shown to have anti-inflammatory properties. CBD (together with tetrahydrocannabinol) has been successfully tested in a few preliminary human trials related to autoimmune diseases…
Cannabidiol (CBD) is a major, nonpsychoactive Cannabis constituent with anti-inflammatory activity mediated by enhancing adenosine signaling.
Inasmuch as adenosine receptors are promising pharmaceutical targets for ischemic heart diseases, we tested the effect of CBD on ischemic rat hearts.
Our study shows that CBD induces a substantial in vivo cardioprotective effect from ischemia that is not observed ex vivo.
Inasmuch as CBD has previously been administered to humans without causing side effects, it may represent a promising novel treatment for myocardial ischemia.”
Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
“The protective effects of cannabidiol (CBD) have been widely shown in preclinical models and have translated into medicines for the treatment of multiple sclerosis and epilepsy. However, the direct vascular effects of CBD in humans are unknown.
CONCLUSION:
This study shows, for the first time, that CBD causes vasorelaxation of human mesenteric arteries via activation of CB1 and TRP channels, and is endothelium- and nitric oxide-dependent.”
Pharmacologic effects of cannabidiol on acute reperfused myocardial infarction in rabbits: evaluated with 3.0T cardiac magnetic resonance imaging and histopathology.
“Cannabidiol (CBD) has anti-inflammatory effects.
We explored its therapeutic effects on cardiac ischemia-reperfusion injury with an experimental imaging platform…
Compared to controls, CBD treatment improved systolic wall thickening, significantly increased blood flow in the AAR, significantly decreased microvascular obstruction, increased the PDR by 1.7-fold, lowered the AMI-core/AAR ratio, and increased the MSI.
These improvements were associated with reductions in serum cTnI, cardiac leukocyte infiltration, and myocellular apoptosis.
Thus, CBD therapy reduced AMI size and facilitated restoration of LV function.
We demonstrated that this experimental platform has potential theragnostic utility.”
Cannabidiol as an Intervention for Addictive Behaviors: A Systematic Review of the Evidence.
“Drug addiction is a chronically relapsing disorder characterized by the compulsive desire to use drugs and a loss of control over consumption.
Cannabidiol (CBD), the second most abundant component of cannabis, is thought to modulate various neuronal circuits involved in drug addiction.
The goal of this systematic review is to summarize the available preclinical and clinical data on the impact of CBD on addictive behaviors.
MEDLINE and PubMed were searched for English and French language articles published before 2015. In all, 14 studies were found, 9 of which were conducted on animals and the remaining 5 on humans.
A limited number of preclinical studies suggest that CBD may have therapeutic properties on opioid, cocaine, and psychostimulant addiction, and some preliminary data suggest that it may be beneficial in cannabis and tobacco addiction in humans.
Further studies are clearly necessary to fully evaluate the potential of CBD as an intervention for addictive disorders.”
http://www.ncbi.nlm.nih.gov/pubmed/26056464
“CBD is an exogenous cannabinoid that acts on several neurotransmission systems involved in addiction. Animal studies have shown the possible effects of CBD on opioid and psychostimulant addiction, while human studies presented some preliminary evidence of a beneficial impact of CBD on cannabis and tobacco dependence. CBD has several therapeutic properties on its own that could indirectly be useful in the treatment of addiction disorders, such as its protective effect on stress vulnerability and neurotoxicity… The dreadful burden of substance-use disorder worldwide, combined with the clear need for new medication in the addiction field, justifies the requirement of further studies to evaluate the potential of CBD as a new intervention for addictive behaviors.” http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4444130/