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13/Aug/2022

Cannabinoid therapy for sleep

I have noticed consistently good results using cannabinoids for sleep disorders. I am often asked what are the top indications for cannabis therapy in my practice and insomnia would always be in the top three.

I first started to gain an interest in cannabis and cannabinoids back in 2015. One of the most common reasons that my patients were using cannabis was for various types of insomnia. Most of these patients were having very good results. That really peaked my interest because I too suffered from insomnia for a large part of my life.

I had used various natural sleep aids but needed a change as my current medication was producing some inconvenient side effects. After receiving my medical cannabis prescription I started using a balanced THC:CBD oil which improved my sleep latency and nighttime wakeup’s within a few days. Cannabinoid therapy is now one of my most recommended treatments for various types of insomnia as it is safe, inexpensive, fast acting and effective.

Cannabis can have calming or stimulating effects depending on the preparation, dose and mode of administration. I really wanted to find out what made cannabis effective for sleep and what would be the optimal way to use it for sleep. My research pointed towards a few mechanisms through which cannabinoids likely have sleep promoting effects: GABA, Serotonin and Endocannabinoid modulation.

GABA

GABA is an inhibitory neurotransmitter that generally promotes a relaxation response in the central and peripheral nervous system. It is well established that activation of GABA receptors favours sleep and many pharmaceutical drug classes, including benzodiazepines, act on GABA receptors.

Both animal and human studies have demonstrated that cannabidiol (CBD) has a modulatory effect on GABA activity. CBD can both increase and decrease GABA activity depending on neurotransmitter activity levels (if there’s too little it increases, if there is too much it decreases). This makes CBD useful for sleep disorders resulting from too little GABA activity (think of the overactive brain) without the addictive potential of GABA stimulating pharmaceutical preparations.

Serotonin

Serotonin is a neurotransmitter that is involved in mood and sleep/wake responses. Many antidepressant medications specifically target serotonin activity. Research from the early 2000’s by Bambico et al demonstrated that cannabinoid receptor agonists (things that stimulate cannabinoid receptors) have the ability to modulate serotonin activity. Low doses seemingly to raise serotonin activity while high doses have little effect.

Both endogenous cannabinoids (cannabinoids we make ourselves) and phytocannabinoids (THC, CBD etc..) seem to have the ability to modulate serotonin activity via stimulation of our cannabinoid receptors. This may explain some of the physiology involved in the sleep promotion and anti-anxiety effects of cannabis preparations. CBD seems to be particularly useful through its interplay with our endocannabinoid system.

The Endocannabinoid System

All species, with the exception of insects, have an endocannabinoid system. The endocannabinoid system is our bodies harm reduction system, keeping chemical and electrical singling in balance. Overall, stimulation of the endocannabinoid system has a calming effect and a known modulator of our sleep/wake cycle.

Many chronic diseases that have been linked to disruption in the endocannabinoid system (Fibromyalgia, Migraine, Inflammatory Bowel Disorder) have a sleep disruption comorbidity. This sleep disruption can usually be helped with a prescription of cannabinoids such as CBD. It is certainly plausible and empirical evidence supports the theory that patients with sleep disorders have endocannabinoid disruption. Therefore, phystocannabinoids like CBD can be helpful to restore endocannabinoid tone and subsequently better sleep.

Dosing Considerations

Cannabis is a unique medicine as it cannot be prescribed based on age and weight. Everyone has an individual response to cannabinoids due to the fact that everyone has unique  endocannabinoid tone and metabolism.

Cannabinoids like CBD and THC can interact with particular medications and preexisting conditions. Some preparations of cannabis are very different in their effect and duration. Smoked cannabis has a very fast acting effect but a short duration. Edible cannabis can have a slow onset of effect but last for a long time.

Therefore it is highly recommended to have a healthcare professional knowledgeable in cannabinoid therapy work with you for the initial stages of treatment. This will ensure a safe and effective dosing strategy with minimal chance for adverse effects. With that being said cannabis is a very safe medication and when prescribed correctly can make a significant difference in those suffering from sleep disorders. Check out the Cannabis Therapy page for more information.

References

Pretzsch CM, Freyberg J, Voinescu B, Lythgoe D, Horder J, Mendez MA, Wichers R, Ajram L, Ivin G, Heasman M, Edden RAE, Williams S, Murphy DGM, Daly E, McAlonan GM. Effects of cannabidiol on brain excitation and inhibition systems; a randomised placebo-controlled single dose trial during magnetic resonance spectroscopy in adults with and without autism spectrum disorder. Neuropsychopharmacology. 2019 Jul;44(8):1398-1405. doi: 10.1038/s41386-019-0333-8. Epub 2019 Feb 6. PMID: 30758329; PMCID: PMC6784992.

Gottesmann C. GABA mechanisms and sleep. Neuroscience. 2002;111(2):231-9. doi: 10.1016/s0306-4522(02)00034-9. PMID: 11983310.

Moreira FA. Serotonin, the prefrontal cortex, and the antidepressant-like effect of cannabinoids. J Neurosci. 2007 Dec 5;27(49):13369-70. doi: 10.1523/JNEUROSCI.4867-07.2007. PMID: 18057193; PMCID: PMC6673093.

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21/Nov/2019

It was my hope to find an effective alternative to Cannabidiol (CBD) that wouldn’t land me in jail when I travel; so is PEA the new CBD?

PEA stands for Palmitoylethanolamide. It is a fatty acid that is found in Eggs, Cheese, Meats and Peanuts.  We also make PEA during stress, infections, inflammation, trauma, allergies, pain, cardiac disease, kidney disease and obesity. Much like our endocannabinoids, PEA is responsible for maintaining cellular homeostasis.

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How does it work?

While PEA does not have a direct effect on Cannabinoid receptor (CB1 and CB2) it does have similar mechanisms of action to our endocannabinoids and cannabidiol (CBD). PEA looks very similar to our body’s own endocannabinoids (AEA and 2-AG). These similarities allow PEA to exert effects similar to our AEA and 2-AG.

PEA down regulates mast cells, which are responsible for the release of histamine and other inflammatory mediators. PEA can therefore be a powerful molecule for immune heath, inflammation, pain, neuro-protection and allergies. PEA has direct action on receptors GPCR55 and GPR119, which produce effects similar to activation of CB1 and CB2 by endocannabinoids, THC and CBD.  PEA also acts similarly to CBD by affecting the breakdown of endocannabinoids via inhibition of the enzymes FAAH and MAGL. 

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The Research

Several studies have shown that when PEA is used with opioid type drugs for low back pain, the dose of the opioids could be reduced significantly. PEA was found to exert pain relief animal models of inflammation and neuropathic pain. These analgesic effects are thought to be due to increasing endocannabinoid levels similarly to how CBD works. All in all many studies have revealed that PEA exerts similar effects to CBD.  So I thought I would give this supplement a whirl, as a alternative to CBD (especially for travel) would be an important option for patients using CBD. 

My 5-day Trial with PEA

I took the supplement P.E.A. Activate from AOR , which contains 600mg PEA per lozenge.  My daily dose was two lozenges per day and I did that for 5 days. I noticed a strange light-headed feeling about 5 minutes after chewing my first lozenge. The feeling lasted for a bout 30min. I was excited that I actually felt a bit different after that fist dose by unfortunately each dose produced a similar effect (a light relaxing feeling) that only lasted between 30-60min. There didn’t seem to be much carry over from one dose to another. The effects were always pretty fast acting but short-lived. Furthermore I had a return of some muscle soreness that was absent for most of the time that I was taking my CBD supplement.  So, it seemed like, for me, the PEA was not having the same effect that I had experienced while on CBD.

In summary, the effects that I experienced during my PEA trial were fast acting but short-lived. PEA may therefore be a useful tool for acute episodes of anxiety, pain etc… but it did not have the same accumulative and long term effects that I experienced with CBD. The research on PEA is compelling and it is possible that this supplement warrants a more long-term trial. According to the research PEA seems to be a potential alternative to CBD but from my experience it falls a bit short.  Check out my video review of PEA here. 

https://youtu.be/Yfr-Ma19gGk

dr_shawn

Patient focused integrative health care. Utilizing effective natural approaches designed to be used alone or to compliment conventional medical care.


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