The Ultimate Guide to Use CBD for Pain

A Guide To Using Cannabidiol (CBD) For Pain

By Dr. Victor Chou

Disclaimer
All content in this article was created for informational purposes only. The content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition.

In the heated battle of CBD vs. Pharma regarding pain relief drugs, more and more people start to explore their options and rely on the benefits of CBD, a natural, non-psychoactive compound derived from the hemp plant.The most common doctor’s advice on treating pain usually revolves around the combination of toxic medications and a healthy, active lifestyle.

However, if used in the long-run, over-the-counter medications present a serious health hazard for the patient.

Which means that, unfortunately, there is little to no, effective, lasting medications for people experiencing chronic pain on a day-to-day basis. Until now.

Although in its early stages of research, CBD offers promising results in pain relief because of its various therapeutic benefits. But, being in the spotlight also brings lots of misconceptions. [1]

Read on to find out how exactly CBD works for pain relief and how to get the most out of it by choosing the right type of product and dosing.

What is CBD?

CBD, short for cannabidiol, is an all-natural, non-psychoactive compound derived from the hemp plant. The hemp plant and marijuana are different species from the same cannabis family. CBD is the second most abundant compound in cannabis, representing up to 40% of its extracts.

After THC, CBD has become the second most popular of more than 60 cannabinoids found in marijuana and the hemp plant, for one major reason — it doesn’t cause the usual high.

Hemp is high in cannabidiol (CBD), which also acts as THC’s antagonist, protecting against THC’s adverse psychological effects. Various studies examining the protective effects of CBD have shown that CBD can counteract the negative effects of THC. [2]

On the other hand, marijuana is rich in THC, containing anywhere from 5-20%, even as high as 25-30% THC in premium marijuana.

Good news is, CBD studies show that even if used in high dosages, the substance is safe for the patient, feeding the body with its powerful analgesic, pain-relieving, and anti-inflammatory properties. [3]

More on the difference between hemp and marijuana, THC and CBD later on.

Psychoactive Effects and The Endocannabinoid System

It all comes down to the endocannabinoid system (ECS) and its immense regulatory roles in neuronal, metabolic, vascular, immune and reproductive systems. [4]

Naturally present in the human body, the endocannabinoid system is responsible for receiving and translating the signals from cannabinoids – which can be produced by the body itself, known as the endocannabinoids, or introduced from outside agents (diet or smoking) like CBD and THC.

Although we don’t have a complete understanding of the functions of the endocannabinoid system, we know that it is widely distributed in the brain, the peripheral system, and most glands and organs in the body. The two primary and well-documented endocannabinoids are arachidonylethanolamine, nicknamed anandamide (AEA) and 2-arachidonylglycerol (2-AG). Anandamide is also known as the “bliss molecule”.

These two endocannabinoids work as agonists (chemicals that bind to a receptor and produces a biological response) to the essential CB1 and CB2 receptors. AEA is a high-affinity, partial agonist of CB1 receptor, and almost inactive at CB2 receptor, while 2-AG acts as a full agonist at both CBRs with moderate-to-low affinity [5]

This is important because THC and CBD affect the cannabinoid 1 (CB1) and 2 (CB2) receptors in a different way. Namely, THC directly activates both receptors, particularly the CB1 receptor mostly found in the brain. The CB1 receptors deal with coordination of movement, pain, emotions, thinking, appetite and memories, and most importantly, are guilty for getting someone “stoned”. The mechanisms and actions of CBD are not completely clear yet, but the compound does not bind to the CB1 receptor or the CB2 receptor. [6]

In fact, CBD is not only bad at activating the CB1 receptor, but also interferes with its activity. Meaning, if taken together, THC and CBD work in activating the CB1 receptor as polar opposites, making the patient feel a more mellow high with much lower chances of experiencing paranoia. If CBD is absent, no other component inhibits the activation of the CB1 receptor, leaving the path open for THC to trigger its regular “high.” [7][/vc_column_text][vc_column_text]

How CBD Affects The Endocannabinoid System In Reducing Pain

Both CB receptors communicate with each other, with the difference that one is more commonly found in the brain, while the other — CB2 — is more common in the body, particularly in the immune system, affecting inflammation and pain.

While THC directly activates both CB1 and CB2 receptors, there is a misconception that CBD affects only the CB2 receptors. In fact, CBD ( let’s say in the form of oil) doesn’t directly affect these receptors at all.

What it does instead, it influences the body to utilize more of its occurring endocannabinoids naturally. It’s interesting that the endocannabinoids can be created by the human body and consumed through food. But for the body to use more of the endocannabinoids that are already existing, it needs the help of the CBD oil. CBD oil enhances the body’s mechanism of using other receptors, such as the vanilloid receptor, where THC shows no activity. These activities reinforce the conception of CBD as an endocannabinoid modulator. [8]

It is believed that the result of a CBD oil consumption for treating pain lies in its mediation with various receptors such as the Vanilloid receptors, directly correlated to the endocannabinoid receptors in the body. [9]Vanilloid receptors are connected to body temperature, with higher body temperature affecting inflammation and causing higher pain.

It is proven that CBD enhances the effects of anandamide (AEA), one of the two primary endocannabinoids in the body. Cannabidiol enhances the anandamide signaling. By inhibiting the FAAH enzyme responsible for breaking down anandamide in the body. Less FAAH means more anandamide in the body. [10] What’s even more fascinating is that a 2010 study found that anandamide suppresses pain initiation in the body through a peripheral endocannabinoid mechanism. [11]

Moreover, the only reasonably well-characterized, non-cannabinoid site of action for AEA is the vanilloid receptor type 1 (VR1). The VR1 channel is gated by protons and heat and is considered that under certain conditions, mediates effects ranging from vasodilation, smooth muscle tone modulation, inhibition of tumor cell growth and induction of apoptosis (death of cells). [12]

Another explanation of the inflammatory and analgesic effects of CBD has recently come to light with the discovery that it is able to promote signaling of the adenosine receptor A2A by inhibiting the adenosine transporter. [13]

CBD increases the effect of the adenosine receptor (opposite of caffeine) giving a more relaxed, a calming effect, but not a sleepy one. Caffeine, on the other hand, blocks the adenosine receptors, making the person consuming it, more excited.

Eight Proven Benefits of Using CBD For Pain

Over the years, it was thought that THC was the compound that may help with pain, nausea, loss of appetite while CBD was considered as biologically inactive in humans. In the last decade however, studies have shown that CBD is effective in treating epilepsy and other illnesses, such as anxiety, cancer, and schizophrenia, among many other ailments. [14]

The number of people using CBD products is on the rise. In fact, 42% of CBD users have left traditional medications behind and use only medical marijuana, while the major portion of 57% of the surveyed continues to use both CBD and their regular medication. [15]

What is even more fascinating is that almost 66% of CBD users claim that CBD products are more effective in relieving medical conditions than their regular over-the-counter medications.

Pre-clinical research shows CBD to have a variety of therapeutic effects, including anti-seizure, anti-inflammatory, antioxidant, neuroprotective, analgesic, anti-tumor, anti-anxiety and anti-psychotic. Read on for the scientifically proven eight benefits of CBD:

RELIEVES NEUROPATHIC PAIN AND INFLAMMATION

According to a 2012 study published in the Journal of Experimental Medicine, CBD significantly suppressed neuropathic pain and chronic inflammation in rodents, without causing tolerance. This suggests that CBD may be useful in pain modulation, representing a novel class of therapeutic solution for chronic pain treatment. [16]

A newer study found that the endocannabinoid system demonstrates a significant interface with pain homeostasis. Plant-based cannabinoids “have been demonstrated to be effective in a range of experimental neuropathic pain models, and there is mounting evidence for therapeutic use in human neuropathic pain conditions.” [17]

These claims are supported by another 2014 study that found analgesia to be a principal therapeutic target of the cannabinoid system, providing effective treatment of neuropathic pain. [18]

Antipsychotic Effects

As previously stated, the THC found in medical marijuana may produce acute psychotic episodes — if used in high doses — which can be mitigated by CBD. Studies show results that support the idea of CBD as a future therapeutic option in psychosis in patients with schizophrenia. [19]

Reduces Anxiety

CBD reduces anxiety in patients with social anxiety disorder, and are effective for patients struggling with panic disorder, OCD, and PTSD. [20]

An interesting 2011 study conducted between 24 never-treated patients with social anxiety disorder found that CBD significantly reduces anxiety, cognitive impairment and alertness in speech anticipation. The researchers divided the group into a placebo group and a CBD group, both given suitable treatment before a speech. Contrary to the calm CBD group, the placebo group showed higher anxiety, discomfort, and cognitive impairment. [21]

HELPS CANCER PATIENTS

A 2006 study revealed that CBD was the most potent inhibitor of cancer cell growth of different breast tumor cell lines, with significant lower potency in non-cancer cells. [22]

A 2012 review of cannabidiol as potential anticancer drug stated that cannabinoids possess antiproliferative, pro-apoptotic effect that interferes with tumor adhesion, invasion, and metastization. [23]

Extremely important findings show that CBD can be used for prolonged treatment because it doesn’t show toxicity in humans. Aside from proven effective in fighting breast cancer cells, CBD can inhibit the invasion of lung and colon cancer, as well as leukemia. [24]

A 2017 study published in The New England Journal of Medicine found that CBD drastically cut down seizure frequency of most patients — paving the way for the FDA approved Epidiolex, a drug used to treat two rare forms of childhood epilepsy. After just three months of treatment in doses up to 25 milligrams per kilogram of body weight, 39% of the 23 patients showed a 50% reduction in seizures. [25]

For centuries, both THC and CBD has helped patients suppress nausea and vomiting. A study found that CBD has anti-nausea and antiemetic benefits, acting in a diphasic manner. This means that in low doses, CBD suppresses vomiting, while in high doses it either increases nausea or passes without an effect. [26]

A 2013 British Journal of Clinical Pharmacology study, reports that CBD prevented vascular damage caused by a high glucose environment, induction of type 2 diabetes, as well as reduced the vascular permeability. [27]

LOWERS INCIDENCE OF DIABETES

A 2006 study found that CBD treatment “significantly reduced the incidence of diabetes in non-obese mice from an incidence of 86% in non-treated control mice to an incidence of 30% in CBD-treated mice.” Another benefit of the experiment was a significant reduction of pancreatic islets and reduced insulins of the CBD-treated mice. [28]

A newer, 2013 American Journal of Medicine study on the impact of medical marijuana use on glucose, insulin, and insulin resistance among US adults showed that unlike past marijuana users, current medical marijuana use was associated with 16% lower fasting insulin levels. [29]

Therapeutic Benefits of CBD for Pain Relief

Natural pain relief is one of the most significant benefits of CBD. Most diseases listed below unfortunately, can’t be cured by CBD, but this powerful cannabinoid may help manage or eliminate pain and other symptoms.

In just four days of application of CBD topical gel to rats with arthritis, researchers found a significant drop in inflammation and pain, without side effects. [30] However, more human studies are needed to confirm or debunk the results.

The degenerative joint disease causes articular cartilage degradation. Unfortunately, patients are offered limited therapeutic approaches regarding drugs and analgesics that can control the disease. A 2014 study on the involvement of the endocannabinoid system in osteoarthritis pain, based on promising preclinical data, summarizes the therapeutic value of cannabinoids for osteoarthritis management. Pharmacological studies have supported the anti-nociceptive effects of cannabinoids in different types of osteoarthritis. [31]

Multiple Sclerosis (MS)

This autoimmune disease attacks the body’s nerves and brain, causing muscle spasms that cause constant pain. It was found that short-term use of CBD oil can help reduce the symptoms (spasms), but the results are modest. [32]

Sativex is a multiple sclerosis drug approved in Canada and the United Kingdom to treat MS pain, but more clinical trials are necessary to determine the efficiency of the drug for pain management.

A 2007 study found that both THC and CBD are effective in treating neuropathic pain in MS. [33]

General Chronic Pain

Aside from MS, the previously mentioned report studied the effect of CBD on general chronic pain. The research compiled results of multiple systematic reviews of trials and studies and concluded that there is evidence that medical marijuana is effective in treating chronic pain in adults.

Another study published in the Journal of Experimental Medicine suggests that CBD can reduce pain and inflammation. When it comes to building up tolerance to CBD, the researchers found that the subjects were not likely to build up tolerance. [34]

As studies show, CBD interacts with the receptors in the brain and the immune system. The receptors are proteins attached to the cells that respond when receiving chemical signals from different stimuli. Due to the anti-inflammatory effects of CBD, the CBD oil is believed to use that mechanism in the body to help with pain management, such as chronic back pain.

Myalgia is a widespread condition that causes discomfort in the muscles of the patient. It can be caused by fibromyalgia, infections, autoimmune diseases, use of certain medications, etc. The most common medicine for treating excruciating muscle pain, as the muscle tissue is located nearly anywhere in the body, is ibuprofen.

The problem with this over-the-counter, anti-inflammatory, but toxic drug is that over the years, causes serious health issues, such as increasing the risk of peptic ulcer, acute renal failure, and even stroke. Luckily, many people suffering from muscle pain have found pain relief with CBD. Experts believe that ibuprofen offers pain-relieving properties because it increases the anandamide levels in the bloodstream, an endocannabinoid that attenuates pain perception and inflammation. Fortunately, CBD naturally increases the levels of anandamide in the body. By combining physical therapy, stretching and exercising, as well as staying hydrated, the patient can achieve optimal results.

The symptoms of fibromyalgia vary with time, regardless of what treatment the person is undertaking. Patients suffering from this condition find that a combination of remedies works best to reduce or eliminate the symptoms. As a safe and natural remedy, a 2013 review shows that CBD helps to relieve pain caused by fibromyalgia.

A newer study suggested that lack of endocannabinoids may be the root cause of chronic pain syndromes, including fibromyalgia. [35] So far, it is determined that CBD works best if combined with THC (also because it reduces the side effects of THC). [36]

It is unknown why CBD works better for some people with fibromyalgia and not in others, as well as the actual mechanism that the body uses to reduce the symptoms of fibromyalgia.

Another win for medical marijuana research was the study that found the effectiveness of the active compounds on cannabis at reducing migraine pain, compared to the prescription migraine meds, who show higher side effects. The study showed that a cannabis-based medication given to the participants — combining two active compounds, THC and CBD — provides therapeutic benefits, such as relieving seizures in epileptic patients. [37]

A newer, 2017 study found that CBD has an effective analgesic role for headache-related conditions. [38]

There is evidence that the endocannabinoid system, digestion, and CBD interact in various ways. It is believed that CBD can help with digestive pain. [39]

According to the National Cancer Institute, CBD may alleviate not only the symptoms of cancer by preventing cancer cell growth but the side effects of draining cancer treatment. Although it is not a fully endorsed form of cancer treatment, CBD and medical marijuana are showing promising results in moderating the inflammation and change the way the cells reproduce, reducing the ability for tumor cells to reproduce. [40]

A 2014 study found that CBD may be a safe way to prevent chemotherapy-induced neuropathic pain. [41]

CBD vs NSAIDS for Pain Relief

Over-the-counter pain relievers known as NSAIDs are a go-to pain relieving source for many adults. But, regardless of the recommended lowest dosage for the shortest amount of time, people tend to take NSAIDs chronically. Which is unfortunate because these drugs are extremely toxic, each year causing an estimated 41,000 hospitalizations and 3,300 deaths among older adults. [42]

CBD is a much safer, natural alternative to NSAIDs, showing promising results in effectively reducing pain and inflammation. Both types of drugs are believed to potentially increase the levels of anandamide — an endocannabinoid responsible for pain perception and inflammation.

For more on the relationship between CBD vs. NSAIDs click here.

CBD Dosing Guidelines: How Much Should You Take

Important: The information presented in the article is for informational purposes only – it should never be considered as individualized medical advice. That being said, there is no universally prescribed dosage for the diseases treated with CBD. The following advice is based on current best practices.

CBD is not regulated, so there are no official guidelines for dosages appropriate for pain or other issues. It is safe to say that CBD dosage depends on other factors, such as weight, age, metabolism, genetics, type and severity of pain.

At the beginning, it is very likely that you’ll experiment before finding the dosage that works best for you. Some patients benefit from 0.25 milligrams of CBD, while others need 50 to 100 milligrams or more.

A tip: Start low and increase as you start noticing an effect.

The daily recommendations for various illnesses according to Mayo Clinic research-based CBD dosage:

Chronic Pain:5-20mg of CBD for 25 days [with or without THC] (orally). [43]
Loss of Appetite in Cancer Patients:5mg of THC (orally), with or without 1mg of CBD for six weeks. [44]
Epilepsy: 200-300mg of CBD (orally) daily, up to 4.5 months. [45]
Multiple Sclerosis (MS) symptoms: Cannabis plant extracts containing 2.5-120 milligrams of a THC/CBD combination daily for 2-15 weeks. Patients typically use eight sprays within any three hours, with a maximum of 48 sprays in any 24-hour period. [46]
Migraine and chronic headaches: 10-50 mg; oral
Schizophrenia: 40-1,280mg oral CBD daily. [47]

Which CBD Product Is The Most Effective For Your Pain?

It is important to understand that, once formulated, a recommended CBD regimen for pain management should be used regularly for maximum pain relief.

It is recommended to start with 5-10 mg per day of pure cannabidiol for treating chronic pain. If you don’t feel relief, increase the dose by 5-10 mg per day, until achieving desired results.

For pain caused by headaches, arthritis and osteoarthritis, depending on the severity try taking cannabidiolorally using tinctures. Typically, people use the 300 mg’s for mild pain, 600mg for moderate pain, or 1800mg or more for severe pain. Another option is CBD Gum. It contains 10 mg of cannabidiol per piece and is a great choice for chronic pain issues caused by inflammatory diseases. The best thing is, you are constantly absorbing the cannabidiol as you chew.

All of the Ways to Take CBD – Which One is Right for You?

Choosing the right brand is important. But, after choosing a brand, you might get confused by how each CBD product works and which one would be the best type to buy. Here are advantages and disadvantages of the top six ways to take and use CBD oil:

Without a doubt, the most commonly used cannabidiol product on the market, especially for chronic pain. The reason: they typically contain the purest form of cannabidiol, can be manufactured at high potencies and dosing is simple and accurate. It is used by simply dropping a couple drops under the tongue. Dosage of tinctures varies from 300mg to 4000mg. Sublingual application is one of the quickest ways to feel the effects of cannabidiol.

If you are looking for a no-brainer method of taking CBD, try capsules. This daily supplement comes a dose of 10-50 mg of pure CBD.

Gummies and Edibles

Always look for cannabidiol infused gummies, with no artificial ingredients, like those offered by Every Day Optimal. These types of products contain anywhere from 10mg–25mg of CBD and are known for their long-lasting effect. With digestibles, you are slowly absorbing the cannabidiol into the bloodstream.

Lotions, lip balms, and other CBD topicals are used for pain caused by arthritis, and other skin conditions. The offer an advantage to treating pain because of their direct, local effect on the affected areas, which makes them most suitable for skin, muscle, and joint issues.

Definitely one of the most popular ways of taking cannabidiol is “vaping” . Smoking or vaporizing the oil is done with a device where you add, heat, and inhale the appropriate amount of vape oil, such as a vape pen, an e-cigarette or vaporizer. Not recommended for people struggling with asthma and other related conditions.

How CBD Bioavailability Affects the Effectiveness of CBD for Pain Relief?

Now that we’ve talked about proper dosage and various forms of consuming CBD, it’s time to address an important topic: bioavailability.

Shortly, bioavailability is “the degree and rate at which a substance (such a drug) is absorbed into a living system or is made available at the site of physiological activity.”

For example, a substance delivered intravenously is likely to have 100% bioavailability. Other routes of administration of CBD include oral, inhalation, sublingual, and rectal. How effective is each of these routes?

The oral consumption is one of the most common routes of administration, but the overall results of its bioavailability rate are not the most optimistic. One study showed a bioavailability rate of 6%, while another one between 4% and 20%. By consuming an edible of 100mg, only 20mg reach the bloodstream. In conclusion, oral administration is most effective in treating symptoms that require small concentrations of CBD. [48] [49][

Sublingual Consumption

The sublingual gland — the vein located under the tongue — gets CBD oil absorbed directly into the bloodstream. The most common sublingual administration is through CBD tinctures and sprays, with a bioavailability that ranges from 12% to 35%. After the inhalation route, the sublingual route is the second most efficient in delivering CBD to the bloodstream. [50]

Through vaporized consumption, CBD is directly inhaled into the lungs, quickly after, enters the bloodstream. The bioavailability rates of inhalation are between 34-46%. Higher bioavailability means more effective CBD for treating pain.[51]

THC vs. CBD and Hemp vs. Marijuana

Choosing between THC and CBD for your pain relief is quite the dilemma. Most people go to CBD purely for its non-psychoactive effect, which is not the best criteria. Depending on your pain treatment, sometimes, it is best to use both THC and CBD oil because these two natural components work in synergy.

In practice, doctors and patients prefer CBD over THC because of the lack of side effects. Although temporary, THC’s side effects include increased heart rate, dry mouth and red eyes, memory loss, coordination problems, and slower reaction times.

THC offers essential health benefits such as: an antispasmodic, analgesic, anti-tremor, anti-inflammatory, appetite-stimulating, and anti-emetic properties. However, because of its psychotic influence, CBD has gained more popularity in patients looking for a somewhat “normal” way to reduce pain.

Aside from its anti-inflammatory, anticonvulsant, antipsychotic, antioxidant, neuroprotective, and immunomodulatory effects, CBD reduces the intoxicating effects produced by THC, such as paranoia and memory impairment. [52]

It is interesting how both CBD and THC have the exact molecular structure and are chemically similar to the body’s endocannabinoids. The biggest difference between these two components also causes different interpretations in the legal system. Considered more of a recreational drug, THC is on the list of controlled substances. But, in the US, 20 states have passed marijuana related laws to legalize the use of medical marijuana, at the same time legalizing CBD.

Hemp Plant vs. Marijuana

Hemp plant and marijuana differ in their function, application, and cultivation. Marijuana is widely used for its recreational purposes, while hemp is used in the production of clothing, accessories, healthy dietary supplements, and skin products.

They even look different. Marijuana is usually with broad leaves, while hemp has skinnier leaves concentrated at the top. The difference between hemp and marijuana is also a legal one. According to law regulations, the hemp plant contains less than 0.3% THC, while marijuana has more than 0.3% THC.

End Thoughts

Chronic pain is becoming a serious issue for patients around the world. The official opioid crisis showcases a severe problem affecting the US.

I hope that I have put together enough proof to get you on board to try CBD oil to treat pain and testify for its benefits. Of course, it’s always recommended to speak with a doctor before starting any new regiment. If you want to get in touch with me, Dr. Chou, you can do so by contacting me via the links below!

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CHOUAUTHOR

Dr. Victor H Chou, M.D. is the Founder and Medical Director of the Medical Marijuana Clinic of Louisiana, the first medical marijuana specialty clinic in Louisiana. He can be reached through his official website, MarijuanaClinicLa

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