With medical Cannabis approved in half the country plus  states for legalized adult (or recreational) use, the Cannabis industry is growing at an astounding rate in the US and around the globe. Cannabis has therapeutic application for various conditions such as seizure management, inflammatory pain relief, insomnia, and anxiety. To help you make an informed decision about how and when to incorporate Cannabis into a health and wellness plan, it is essential first to dispel misconceptions and gain basic knowledge about the interplay between cannabinoids, terpenoids and the Endocannabinoid System. Once you have basic understanding of THC and CBD, as well as the other constituents of Cannabis, the numerous products on the market will be easier to evaluate.
Perhaps the most widespread and misleading myth surrounding the uses and effects of Cannabis lies in whether the plant is a sativa or an indica. A wide-spread belief about the effects of Cannabis is that Cannabis sativa produces more of a head-trip effect (mind racing, heart pounding) and that Cannabis indica results in a more sedating effect (chill on the couch, relax). Products in the marketplace perpetuate this myth.
In actuality, it is the mixture of phytocannabinoids and terpenoids, which interact with our endo-cannabinoid system, creating these sensations. These mixtures vary widely across both species, and there is an ongoing discussion among medical researchers and botanists about whether the distinction between Sativa and Indica is relevant. To make intelligent recommendations to your clients, you must move beyond these broad and disputed categories and develop an understanding of the underlying chemovars and the effects they have on our endocannabinoid system (ECS).
There are several chemovars found in Cannabis: the primary phytocannabinoids are tetrahydrocannabinol (THC) and cannabidiol (CBD). The Federal assignment of Cannabis as a Schedule 1 drug has made research in the US difficult, so researching these compounds and their complex interactions with each other and with our ECS has been challenging. Until more is known, be aware that products claiming to have specific effects based on their cannabinoid profiles may be based on testimonial experience.
Delta-9-tetrahydrocannabinol acid (THCa) is the component in Cannabis that upon decarboxylation via heating converts to THC, eliciting the well-known psychotropic effect. Besides conferring a “high” effect, THC may offer health benefits such as bronchodilation, neuroprotective antioxidant stimulation for brain injuries and strokes, anti-inflammation without COX-1 or COX-2 inhibition, muscle relaxation, anti-emetic uses, and the reduction of the b-amyloid plaques found in Alzheimer’s.
The appetite-stimulating effects of THC were confirmed in a long-term study of 94 AIDS patients. Of the patients who completed the trial, 25% achieved a weight gain of 2 kg or more during a 12-month period (Beal et al., 1995). Oral THC has been found to be effective against cancer pain in doses of 15 mg and 20 mg in two clinical trials, although some participants reported intolerable side effects such as dizziness, confused thinking, and panic (Regelson et al., 1976). A clinical trial of inhaled Cannabis for neuropathic pain showed that low potency (3.5% THC) and high potency (7% THC) Cannabis had equivalent analgesic properties (Wilsey et al., 2013). The discovery that higher THC percentages are not necessary for pain reduction is significant because some individuals do not welcome its psychotropic effects.
Despite these early and encouraging results, there is a lot of controversy surrounding the laboratory testing of THC. To date, there is no standard for testing, and there are large differences in THC percentages from lab to lab. The desire for high-THC varieties in adult, or recreational, use has spilled over into the medical field. There’s market pressure for dispensaries and edible-product producers to offer products with high percentages of THC. As we examine the synergy of cannabinoids and terpenoids, we will see that THC is only one of the key Cannabis constituents.
Cannabidiol (CBD) is the other primary constituent in Cannabis. Unlike THC, it does not have any psychoactive properties. Research has shown its medical uses to be quite varied. It has been found to be effective against methicillin-resistant Staphylococcus aureus (MRSA) (Appendino et al., 2008); as an anticonvulsant (Jones et al., 2010); and as an analgesic (Costa et al., 2007). It has been shown to reduce anxiety (Russo et al., 2005) and it is cytotoxic against certain breast cancers (Ligresti et al., 2006).
Its neuroprotective antioxidant properties are well established and have been found to be more potent than ascorbate (vitamin C) or tocopherol (vitamin E) (Hampson et al., 1998). In fact, US Health and Human Services have a patent on cannabinoids as antioxidants and neuroprotectants (US 6630507 B1; 2001). This is in direct contradiction to the illegal status of Cannabis as a Schedule I drug, which are drugs with no medicinal value and a high potential for abuse.
CBD has also been shown to help reduce the occurrence of seizures in infants. Research has also discovered anti-seizure properties in vitro and in vivo, as well as anti-convulsant effects in animal models for temporal lobe and partial seizures (Jones et al., 2010).
Other properties have been attributed to CBD including bone growth stimulation and the reduction and prevention of the spread of pain. As an autoimmune protectant, CBD antagonizes tumor necrosis factor, which is present in autoimmune disorders such as rheumatoid arthritis. It has also been found to inhibit the activity of THC (Russo and Guy, 2006), which can modulate the psychotropic effects.
Optimal dosing and the proper application of Cannabis products is an emerging topic. Early indications have produced a recommendation of beginning with 0.1 mg/kg/day, gradually increasing the dosage until the desired impact is achieved. Further research and experimentation will help us determine optimal dosage.
CBG, CBN, CBDV, and THCV
Though less studied than CBD or THC, several other phytocannabinoids have also been identified. Cannabigerol (CBG) has been found to antagonize prostate cancer and work as an analgesic (De Petrocellis and Di Marzo, 2010). It is a GABA-uptake inhibitor (Banerjee et al., 1975) with possible antidepressant properties. Cannabinol (CBN) is an oxidative byproduct of THC that has been shown to have sedative and anticonvulsant properties (Turner et al., 1980). It is effective against MRSA (Appendino et al., 2008), and can be useful for treating burns. Cannabidivarin (CBDV), too, is a potential anticonvulsant (Jones et al., 2010), as is tetrahydrocannabivarin (THCV), which has been shown to be effective in treating metabolic syndrome (Cawthorne et al., 2007; Riedel et al., 2009). Again, further research into these compounds and their interactions promises great potential effects.
The Endogenous Cannabinoid System
The Endocannabinoid System (ECS), present in all vertebrates, is a network of neuro-modulation receptors within our brains, immune systems, and other parts of the body. Our ECS is a hemostatic regulatory system essential for key processes such as pain, appetite, memory, and mood and pain regulation. It plays a hand in regulating mitochondrial activity and in neurogenesis. Three components of ECS are known: endogenous cannabinoids (endocannabinoids); cannabinoid receptors (CB1, CB2, TRPV1); and the enzymes that synthesize and degrade endocannabinoids.
Endocannabinoids are ligands that bind to cannabinoid receptors to stimulate and regulate various functions. The two most significant endocannabinoids to date are arachidonylethanolamide (anandamide) and 2-arachidonoylglycerol. Anandamide is a fatty acid neurotransmitter, referred to as the “bliss molecule” because of its pleasurable effects. Notably, anandamide has been shown to inhibit breast cancer cell proliferation by inhibiting DNA synthesis (De Petrocellis et al., 2011).
Cannabinoid receptors are neuro-modulating receptors that halt neurotransmitter release upon binding with an endocannabinoid. CB1 receptors, which are psychoactive, are the most abundant receptors in the brain. Most CB1 receptors are found in the limbic system, cerebellum, and cerebral cortex. Nonpsychoactive CB2 receptors are found in immune tissues such as leukocytes, the spleen, and tonsils, and in the heart, bones, and muscles. They are expressed in the brain when injury or disease occurs, such as multiple sclerosis. As immuno-modulatory receptors, they are important in reducing pain and inflammation. CB2 agonist drugs have been shown to be effective for hepatic fibrosis and other fibrotic conditions.
CB1 and CB2 receptors are also in the gut, where they help modulate propulsion and secretion and are distributed along the skin where they modulate pain and inflammation. TRPV1 receptors mediate pain signals, and therapeutic agents that work on this receptor may reduce neuropathic pain.
The ECS is triggered by various external sources, including herbs, foods, and even exercise. What was once believed to be endorphins producing the feel-good effects post-exercise is the ECS at work. Other activities including meditation and orgasm impact the ECS. Metabolism and digestion are also factors in the functioning of ECS, as cannabinoid receptors affect the digestive system.
Phytocannabinoids and the ECS
The various phytocannabinoids interact with the ECS at the cannabinoid receptor sites to induce various biological and psychoactive effects. THC, THCV (at higher doses), and anandamide are all CB1 agonists and elicit the euphoric effects of Cannabis. CBD has the opposite effect – it antagonizes the CB1 receptors, reducing the psychoactive effects of THC. CBG has also been shown to have agonist effects on both CB1 and CB2 receptors, though its effect is weaker than THC’s. This self-balancing regulatory system provided by the Cannabis plant is one reason why using whole plant medicine is more beneficial than standardized extracts of phytocannabinoids.
Knowledge of the ECS and the effects phytocannabinoids have upon it can quickly help you separate fact from fiction in an unregulated marketplace where manufacturers often make dubious claims or tout measurements that have little basis in science. As you make decisions about how to incorporate Cannabis products into your practice, it is important to know the correct phytocannabinoid profiles to ensure consistency in treating specific conditions. Not only is the source important, but as with any other botanical product, each harvest can yield a slightly different profile due to environmental conditions. The more information you can acquire, the better equipped you will be to help your clients.
Beyond the phytocannabinoids, Cannabis also contains terpenoids – over 200 have been discovered. We are already familiar with the therapeutic properties of common constituents such as α-pinene in Pine (Pinus spp.) needles, d-limonene in citrus, and β-caryophyllene in Carrot (Daucus carota) seeds. These are among the many constituents also found in Cannabis. Research into these and into how Cannabis interacts with other oils and terpenoids could well yield dramatic results. According to neurologist and Cannabis researcher Ethan Russo (2011), some of these phytocannabinoid-terpenoid entourage effects could well come from the interaction of Cannabis with Frankincense (Boswellia carterii), citrus oil, Lavender (Lavandula angustifolia), Spearmint (Mentha spicata), Pine, Black Pepper (Piper nigrum), Rosemary (Rosmarinus Officinalis ), Sage (Salvia office -nails), and others. Because terpenoids are already an area of expertise for the Aromatherapist, adding Cannabis terpenoids into the mix can be a logical and natural extension of a care plan.
There are countless Cannabis products on the market today. Many of these are unregulated, and the manufacturers behind them may have limited experience or education in phytochemical interactions. Until there is greater understanding about the benefits and entourage effects of phytocannabinoids, it is wise to purchase only Cannabis-extract products that have undergone rigorous third-party testing and provide a certificate of analysis.
CBD oil has been promoted for children and young adults with seizure disorders. Many of the claims attributed to CBD oil are not unfounded, yet it is important to remember that it is not a panacea and common sense should be applied when working with these oils. As with all herbal products, it is important to know your source and ask about growing practices, pesticide use, and application and extraction methods.
Not only are many of the claims about cannabinoid profiles spurious, but there are also significant health concerns with ingestion. Cannabis is effective phytoremediation, which means it draws heavy metals and other toxins out of the soil. Tests have shown that THC may concentrate these heavy metals, so it is very important to know the source of the Cannabis in the products you purchase.
The lack of regulation of Cannabis has allowed producers of Cannabis oil to sell medical and retail Cannabis products with solvent and pesticide residue, adulterants, and contaminants. Edible Cannabis products are usually made with solvent-extracted hash oil. Besides the residual solvent and pesticides, they may also contain GMO ingredients, refined flours or sugar, and other inflammatory ingredients.
It is also important to remember that flavored Cannabis products often contain hexane-extracted terpenoids that were added after the fact, as is popular within the food industry. A better approach would be to breed Cannabis for specific terpenoid profiles instead of adding them.
Inhaled Cannabis oil products such as vape pen cartridges often contain propylene glycol as an additive and the Cannabis oil itself is often solvent- or CO2-extracted. Residual solvent left in the product is always a concern, as inexperienced people are making the extractions in unregulated laboratories. With CO2 extraction, it is important to know what pesticides were used to avoid contamination in the products.
As our understanding about phytocannabinoids and their potential interactions with other plant compounds and with our endocannabinoid system evolves, so will the need for Aromatherapists and other practitioners to help guide their clients. The success of Cannabis as a healing tool lies in its integration with other holistic nutrition, and modalities such as Aromatherapy, nutrition, and massage. Thus, it’s critical that health practitioners become Cannabis competent in this rapidly evolving area of healthcare. Aromatherapist incorporates Cannabis guidance into their practices once they gain education about the science and the appropriate application of this plant. In doing so, can set themselves apart as the forward-thinking appropriate application of this plant. In doing so, can set themselves apart as forward-thinking professionals by adding this ancient healing plant into their existing botanical toolbox.
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Previously published in the International Journal of Professional Holistic Aromatherapy, (Volume 5, Issue 4, Spring 2017).
Special Thanks to:
Laura Lagano and Donna Shields of Holistic Cannabis Network