THE CBD ENTOURAGE EFFECT & PAIN MANAGEMENT
Chronic pain is a public health issue of massive proportions, with more than 100 million Americans and more than 1.5 billion people globally suffering from pain lasting more than 24 hours.
In fact, chronic pain affects more Americans than diabetes, heart disease and cancer combined.
The Cost Of Pain In America
As a society, the cost of pain is estimated in recent studies published by the Institute of Medicine to be “at least $560-$635 billion annually, an amount equal to about $2,000.00 for everyone living in the U.S.”
Prescription painkillers have only made the problem much worse.
According to an article on CNN Health, “every day, 91 Americans die from an opioid overdose.”
“Drug overdoses overall — most of them from opioid painkillers and heroin — are the leading cause of accidental death in the US, killing more people than guns or car accidents.
In fact, while Americans represent only about 5% of the global population, they consume about 80% of the world’s opioid painkillers.<”
New Discoveries With Ancient Roots
Cannabis has been used for more than twelve thousand years and for many different purposes (i.e. fiber, medicinal, recreational).
“The ability of extracts of the hemp plant (Cannabis sativa) to cause a variety of medicinal effects unrelated to its psychoactive properties had been recognized as early as the third millennium BC, when Chinese texts described its usefulness in the relief of pain and cramps (Mechoulam, 1986).”
“In ancient India, the anxiety-relieving effect of bhang (the Indian term for marijuana ingested as food) had been recorded more than 3000 years ago.”
During the 19th Century “cannabis extracts gained widespread use for medicinal purposes until 1937” when marijuana was banned by the US Federal Government.
With overwhelming public support and more states legalizing recreational and/or medical marijuana, cannabis has once again “recently been the focus of medical research and considered a potential therapeutic target [1–3].“
Endocannabinoids Regulate Analgesia & Inflammation
Groundbreaking discoveries about the “endocannabinoid system” or ECS and the potential implications of the “Entourage Effect” for pain mitigation without side effects are one of the most significant developments in medical neuroscience as it relates to human homeostasis and pain management.
According to the U.S. Department Of Health & Human Services (HHS), “the therapeutic potential of cannabinoids has been the topic of extensive investigation following the discovery of cannabinoid receptors and their endogenous ligands which are present at supraspinal, spinal and peripheral levels.
More significantly for the purposes of the present review, they are found at central and peripheral levels of the pain pathways [28–32].”
Endocannabinoid receptors are in fact the most abundant receptors in the mammalian brain and are also found throughout the peripheral central nervous system and in muscles, bones, tissues and organs.
According to HHS, these receptors or “endocannabinoids” are “the brain’s own cannabis-like substances which serve as synaptic circuit breakers and regulate multiple physiological and pathological conditions including food intake regulation, immunomodulation, inflammation, analgesia (pain), cancer, addictive behavior, epilepsy and others.”
Since the relatively recent discovery of endocannabinoids through the study of medical cannabis, the entire natural complex came to be called the “endogenous cannabinoid system,” or “endocannabinoid system” (ECS).
Topical Application of Cannabidiol (CBD)
Considering the fact that there are cannabinoid receptors throughout the peripheral CNS, it only makes sense that applying cannabinoids directly to the affected area with a salve, gel or balm would have therapeutic benefits.
This therapeutic benefit has been confirmed by clinical research published by the NIH National Library of Medicine: “These studies demonstrate transdermal administration of CBD has long-lasting therapeutic effects without psychoactive side-effects.”
Topical application of CBD has even shown great potential in these same studies as a treatment for chronic pain issues such as arthritis: “Topical CBD application has therapeutic potential for relief of arthritis pain-related behaviours and inflammation without evident side-effects.”
“Thus, use of topical CBD has potential as effective treatment of arthritic symptomatology. At present, one in five (21%) adults worldwide are diagnosed with some form of arthritis by their physicians (Helmick et al., 2008). The data presented suggest transdermal CBD is a good candidate for developing improved therapies for these debilitating disease.”
“Transdermal CBD gel significantly reduced joint swelling, limb posture scores as a rating of spontaneous pain, immune cell infiltration and thickening of the synovial membrane in a dose-dependent manner. “
“These studies suggest that manipulation of peripheral endocannabinoids may be promising strategy for the management of pain.”
Normalized Sleep With CBD Helps Pain
According to the US Department of Health & Human Services, National Institute of Health “Cannabinoids may have another therapeutic benefit in managing chronic pain, with regard to sleep. – It has been reported that cannabinoids suppress sleep-related apnea.”
Opioid painkillers can also lead to more serious problems when taken in conjunction with other medications, especially benzodiazepines like Xanax.
Not only does normalized sleep improve pain relief and mood disorders associated with both poor pain control and poor sleep patterns, but there is significant risk of sleep-disordered breathing associated with central nervous system (CNS) drugs used to treat chronic pain.111 “
“Opioid analgesics are most problematic, especially if combined with other CNS depressants such as benzodiazepines. “
Improving Efficacy With Adjunctive Therapies
These studies also indicate that when intractable pain requires the use of opioid painkillers, cannabinoid treatment can be effectively used as an adjunctive treatment to improve the efficacy of the opioids while limiting the negative side effects.
“Adjunctive approaches show strong promise for improving the efficacy of existing pharmacotherapies for pain and limiting unwanted side-effect profiles.”
A Mountain Of Evidence
The scientific evidence supporting the efficacy of cannabinoids to regulate pain is overwhelming and backed by more than a decade of research.
Reports published by the U.S. National Institutes of Health’s National Library of Medicine find that “Endocannabinoids modulate pain under physiological conditions.” and “Cannabidiol (CBD) attenuates inflammation and pain without side-effects.”
CBD and other plant derived cannabinoids have unlimited potential for new treatment options to help people with neuropathic and chronic pain conditions.
“The phytocannabinoids have efficacy in the treatment of various chronic pain conditions with greatest promise as a therapeutic adjunct in treating peripheral and central neuropathic pain and inflammation-mediated chronic pain.”
In addition to chronic pain relief, cannabinoids have also shown efficacy in treatment of acute pain as well.
“Exogenous administration of endocannabinoids or their modulation via inhibition of endocannabinoid deactivation or uptake can produce antinociception in acute pain models.”
The Entourage Effect – Cannabinoid/Terpene Synergy
Research has revealed that the holistic benefit and therapeutic results of cannabinoid related treatments can be greatly improved by “Entourage Effect” derived from nature’s divine integration of unique blends of terpenes and cannabinoids in cannabis plants.
According to the US National Institute of Health “A chemical class known as the terpenes shares a precursor molecule with phytocannabinoids; they are all flavor and fragrance components common to human diets.”
“Terpenes have been designated “generally recognized as safe” (GRAS) by the US Food and Drug Administration and other regulatory agencies.”
”The entourage effect is the term used to describe enhancement of efficacy, with related improvement in overall therapeutic effectiveness, derived from combining phytocannabinoids and other plant-derived molecules.”
“Common cannabis-derived terpenes include limonene, myrcene, α-pinene, linalool, β-caryophyllene, caryophyllene oxide, nerolidol, and phytol.105 These terpenes are also found in many other plants.”
“Terpenes are quite potent and affect animal and even human behavior when inhaled in very low concentrations.”
“They display unique therapeutic effects that may contribute meaningfully to the entourage effects of Cannabis-based medicinal extracts.”
“Of particular interest are the phytocannabinoid–terpene interactions that could produce synergy with respect to treatment of pain and inflammation.“
“Phytocannabinoid–terpene synergy increases the likelihood that an extensive pipeline of new therapeutic products is possible from this age-old plant.”
“The terpene β-caryophyllene is found in a number of commonly available plants, including black pepper, cinnamon, clove, and other spices. It selectively binds to the CB2 receptor at nanomolar concentrations and acts as a full agonist.”
“β-Caryophyllene and cannabidiol occur abundantly in Cannabis sativa.”
“So this plant species produces at least two entirely different chemical substances able to target CB2 receptors differentially.”
“While studies on the pharmacokinetics of β-caryophyllene are still on-going, it is already clear that this terpene is readily bioavailable.“
“Orally administered β-caryophyllene (<5 mg·kg−1) produces strong anti-inflammatory and analgesic effects”107
“On-going studies show that β-caryophyllene is effective at reducing neuropathic pain in a CB2 receptor-dependent manner.”108
“Like other CB2 ligands β-caryophyllene inhibits the pathways – of pro-inflammatory cytokines and promotes a Th1 immune response that plays a critical role in neuroinflammation, sensitization, and pain.”109
“Therefore, the FDA-approved food additive β-caryophyllene seems an attractive candidate for clinical trials targeting the CB2 receptor.“
The NIH Studies also state that if using an opioid pain-killer for intractable pain, the use of non-psychoactive cannabinoids like CBD may offset some of of the undesirable side-effects of the opioids, while obtaining far greater analgesic results.
“Indeed, in cases of intractable or difficult-to-control pain, combination therapy with small doses of opioid and non-psychoactive cannabinoid receptor agonists may be an alternative way to circumvent the undesirable side effects of opioids yet obtain far greater analgesic efficacy than achieved with cannabinoids alone.” 56,110
Conclusion – A Powerful Entourage For Pain Management
Nature’s divine synergy of plant Terpenes and Cannabinoids have worked together for thousands of years to form a powerful entourage of holistic healing and now science has backed it up with real data.
“Putting these pharmacologic, clinical, and societal issues together, the direction for the future resides in the development of orally administered, highly bioavailable, non-psychoactive phytocannabinoid products that also take advantage of the entourage effect, to provide the millions of people living with debilitating pain a comparatively safe and effective form of relief.”
The science of cannabinoids and terpene synergy is continuing to expand rapidly, but decades of research have led to a clear conclusion from the U.S. National institute of Health that endocannabinoids play a critical role in pain management.
We also know that exogenous cannabinoids offer a safe and effective alternative for pain relief and that is good news for the millions of people around the world suffering from chronic pain.