CBDA for Pain – The Science
I have been exercising since I was young, and my knee and elbow joints are causing me a lot of pain, and preventing me from getting back to my normal routine. I need something that can help and fast.
My endometreosis feels like a throbbing pain every time my heart beats. When I have an episode it lasts for like 30 mins, and the contractions feel like i am trying to push out my insides.
In the past year, ive noticed my joints have become stiffer and more painful. It started with my feet, sometimes in the morning they are so stiff that its hard to walk. In the morning my hands are starting to get stiff and hard to flex, and this seems to be progressing to my knees as well.
Does this sound like you?
Pain is caused by many different underlying conditions, and prevents you from enjoying the activities and social events that make life so enjoyable. Finding the right pain relief can be difficult!
Pain relief is a routine, and finding support in the right routines is critical to getting back to your normal self.
Article Highlights
- Pain is associated with increased inflammation
- CBDA and other acidic cannabinoids have much higher absorption
- Studies show CBDA can inhibit critical enzymes (COX2) involved in inflammation
- In vivo research found CBDA may provide pain relief through TRPV1 on nerve cells
Legend
What is pain?
Pain comes in many forms, but fundamentally, it is a neurological signal to the brain that something is wrong in the body. We all know the feeling, and emotional pain can be just as damaging as physical pain.
Inflammation and pain
Chronic pain is often a result of chronic inflammation that leads to temporary, and sometimes permanent damage if not treated appropriately. Often, dealing with the inflammation directly, as well as what is causing the inflammation can improve symptoms.
Fundamentally, inflammation evolved as a mechanism to prevent infection from external pathogens. In modern society, inflammation is mostly a cause of chronic pain and disease, thus the many anti inflammatory drugs and treatments to decrease its long term harmful effects.
While this topic is extensive, and is the subject of a lot of research, the connection between inflammation and pain is widely accepted in the medical community.
What is CBDA and CBD oil?
The cannabis plant, which includes hemp and marijuana, has over 100 different cannabinoids. While each cannabinoid is structurally different, they all have some common properties that involve interacting with the endocannabinoid system.
Most of the cannabinoids are located in the flower, but there are minor amounts also found in the stem.
The cannabinoids in the cannabis plant are naturally in the acidic form. Below is a partial list of the different acidic cannabinoids:
- CBDA (cannabidiolic acid) & CBD (cannabidiol)
- THCA (tetrahydrocannabinolic acid) & THC (tetrahydrocannabinol)
- CBGA (cannabigerolic acid) & CBG (cannabigerol)
- CBCA (cannabichromenic acid) & CBC (cannabichromene)
- CBDVA (cannabidivarinic acid) & CBDV (cannabidivarin)
- THCVA (tetrahydrocannabivarinic acid) & THCV (tetrahydrocannabivarin)
- CBNA (cannabinolic acid) & CBN (cannabinol)
Difference between CBDA (cannabidiolic acid) and CBD (cannabidiol) oil
CBDA is the mother compound to CBD, and is naturally found in the hemp flower in large concentrations depending on the strain. CBD oil is derived from CBDA after it has been exposed to significant heat.
The raw form of cannabis plant extract contains mostly acidic cannabinoids depending on how well it is stored.
The conversion from CBDA to CBD is termed decarboxylation, and is found during conventional purification processes of extracted hemp oil. Typically, the first extraction of the hemp flower produces a low quality crude extract that requires further purification of the cannabinoids.
The benefits of CBDA and CBD oil have been studied for their potential medical benefits, and while there is some therapeutic overlap there are some significant differences.
CBDA does not need to be decarboxylated to be active
CBDA has its own properties that make it unique and different from CBD, and may have better therapeutic potential because it is not decarboxylated. This notion that a cannabinoid needs to be heated before it is active came from the marijuana field, where THCA gives less of a high than THC due to the difference in CB1 receptor activation.
Endocannabinoid system
Cannabinoids are known for their interaction with the endocannabinoid system (ECS). The ECS is found throughout the body, and with strong expression in the brain and immune system.
The ECS helps regulate many physiological processes, such as mood, sleep, inflammation, and blood pressure. While all cannabinoids interact with the ECS in some fashion, there are significant differences in how they do and what their effects are.
For example, THC is known to have psychoactive properties that confer the euphoric feeling people associate with marijuana. However, CBDA and CBD are not considered psychoactive, and do will not get you high.
These different effects are typically through the cannabinoid receptors, such as cannabinoid receptors 1 and 2 (CB1, CB2). THC may activate CB1, which elicits it euphoric feeling, whereas CBD is an allosteric inhibitor of CB2.
CBDA is known to help activate CB2, but also has other effects on different endocannabinoid receptors, such as the 5HT1A receptor. This receptor is associated with serotonin recycling in the brain, and is also a target for depression drugs in the SSRI (selective serotonin reuptake inhibitor) class.
Why do I not see more CBDA on the market?
Conventional processing requires the use of heat to purify the cannabinoids from crude extract after hemp flower harvesting. This has led to widespread use and marketing of CBD and CBG as the standard cannabinoid products.
Scientists at Natural Dos developed a new technology to isolate only the acidic cannabinoids without adding heat. This has allowed us to preserve the natural therapeutic properties of acidic cannabinoids in all our products.
CBDA has enhanced absorption
A significant difference between acidic cannabinoids like cannabidiolic acid (CBDA), is that they have much better absorption than decarboxylated cannabinoids like CBD. Multiple studies have tested the absorption levels of acidic and decarboxylated cannabinoids by ingestion to see how much is taken up by the body.
How well the body absorbs a compound is critical to how effective compounds are at exerting any potential therapeutic effects.
A recent study out of University of Sydney found that CBDA is absorbed over 100-times better than CBD. This seems incredible, but their results were significant, and follows a similar trend seen in other CBDA absorption studies.
Further, this University of Sydney study showed that CBDA absorption was enhanced by the presence of other cannabinoids, highlighting the importance of having all the cannabinoids present in a dose.
This means that to reach potent therapeutic doses of CBDA may require only low doses to be ingested.
CBDA and inflammation
Cannabidiolic acid (CBDA) is not as well studied as CBD and THC since its isolation methods are more difficult, and is only recently gaining in popularity. Many people are reporting significant benefits from taking CBDA, and may represent the new cannabis plant medicine in the space.
Most of the research on CBDA has been performed by in vitro (cell culture) and in vivo (animal) studies.
COX2, CBDA and inflammation
The cyclooxygenase (COX) class of enzymes are critical to many inflammatory processes. These enzymes produce prostaglandins which enhance the pro-inflammatory mechanisms in many cells. One of the major COX enzymes is COX 2, which is well noted for its role in promoting many inflammatory states during injury, cardiovascular disease, joint swelling, cancer, and many other pathologies.
Why is COX2 important? The NSAIDs (non-steroidal anti inflammatory) drug class is a commonly used for pain relief. These drugs, such as ibuprofen and aspirin, target the COX2 enzyme form to reduce inflammation and pain.
Some of the first studies with CBDA found that it can inhibit the activity of COX 2. In this study using breast cancer cells, CBDA inhibited COX 2 activity.
In addition to direct inhibition, other studies in breast cancer cells found that it also effects the expression of COX 2. Breast cancer cells exposed to CBDA lowered the expression of COX 2, meaning that there was less enzyme present.
NSAIDS, such as celecoxib, have been used in treatment for breast cancer, and have been associated with reduced incidence.
This data suggests that CBDA may be important in treatment of inflammation and pain relief.
CBDA and pain relief
In this study out of Canada, using an animal model of inflammatory pain management, CBDA and THC both alone and together were tested. Administration of CBDA was found to have anti inflammatory and pain relief properties.
This in vivo study suggests that CBDA pain management is through the transient receptor potential cation channel subfamily V member 1 antagonist (TRPV1). This was determined by using an inhibitor, then treatment with CBDA, which prevented the effects of CBDA.
TRPV1 is associated with the endocannabinoid system, and is also a target of capsaicin, the compound known for inducing the hot feeling in spice from peppers. Interestingly, there is considerable research into using capsaicin for its pain management properties.
Summary
Inflammation is typically considered as significant underlying contribution to pain, and is a common target for many over the counter pain management drugs. Many patients are prescribed potent pain medications, such as opioids, which can have significant complications.
Cannabis plant raw form extracts which contain high amounts of CBDA may provide an alternative to traditional therapeutics, but more research is needed.
The FDA has not approved CBDA or other cannabinoids for pain management, so please consult with your health care provider if you are currently on medication. Since CBD in high doses has been found to have some drug-drug interactions, its important to seek advice from your physician if you are on multiple medications.
FAQ – CBDA for Pain
CBDA has been studied in pre-clinical trials for its anti-pain properties, and found to have substantial benefits. This appears to be, in part, through its inhibition of COX2 (cyclooxygenase 2), which is a pro-inflammatory enzyme targeted by aspirin and ibuprofen. Inflammation is often the cause of pain, and resolving it can lower the amount of pain in a patient.
While both have been studied in pre-clinical trials for their pain relief properties, only CBDA has the bioavailability to make dosing at the human level applicable. Many of the studies need to use very high levels of CBD to reach significant pain reduction outcomes due to its poor absorption.
In addition, CBDA is much better at reducing inflammation by inhibiting the pro-inflammatory enzyme COX2 compared to CBD, which has little to no ability for direct inhibition.
Yes, the strength of a compound is dependent on its bioavailability and kinetic binding to molecular targets. Because CBDA has superior bioavailability to CBD, the compound can get into the bloodstream at much higher levels.
With respect to kinetics, it depends on what targets you are looking at, and CBDA has both similar and different targets than CBD. Many people are finding that CBDA works much better for them than CBD.
