ARTHRITIS

BY MATT JACKSON, PHD

There are over 100 different types of arthritis that target bone joints. Osteoarthritis is the most common, affecting 27 million people in theU.S. who experience limited range of motion, swelling, stiffness, and chronic pain. 1 It’s easy to take our joints for granted, but when the protective, slippery cartilage wears down, bone-on-bone contact can be intensely painful. It can affect all aspects of everyday life—simply moving in the night can wake you with pain.

Osteoarthritis can damage nerves, inflame the joint, and cause physical damage and bone spurs, which are bony projections on the edges of bones. The spurs can break off from the bone and float into the synovial fluid that lubricates the joint, acting like shrapnel.

The chronic pain caused by osteoarthritis is difficult to treat. The first medication recommended by most professional medical organizations is acetaminophen, but some 50% of osteoarthritis patients don’t respond to it. Nonsteroidal anti inflammatory drugs (NSAIDs) and the selective serotonin norepinephrine reuptake inhibitor (SSNRI) duloxetine are often tried next—but again, not all patients respond. 2 And let’s just not talk about opioids, which are addictive and have their own set of serious problems.

Considering 63% of osteoarthritis patients are unsatisfied with their current pain medication regimen, 3 some are turning to medical cannabis for baseline pain management or to relieve the acute pains that “break through” their current medications. Cannabis might seem like a new alternative treatment, but cannabinoids are not. We have been treating chronic pain with cannabinoids for over 130 years. We just didn’t know it.

The story goes like this. Acetaminophen was first prescribed in1887. Its widespread usage initially was put on hold by a competitor, which ended up causing kidney failure and cancer. Acetaminophen was mass produced in the 1950s and, despite safety concerns, became widely accepted as an over-the-counter medication by the 1970s. 4 It may surprise you, but until recently, no one knew how acetaminophen worked.

Then in 1991, a scientist in Israel, Dr. Raphael Mechoulam, discovered the first two endocannabinoids, AEA and 2-AG. It took almost two decades until we connected the dots and realized how acetaminophen truly works, and it’s an indirect action. When our bodies metabolize acetaminophen, it ends up amplifying our levels of the AEA and 2-AG. Those elevated endocannabinoids cause an ECS response, which is what is truly responsible for relieving pain and reducing inflammation. 4

So, what's the big problem with using acetaminophen to activate the ECS? Osteoarthritis patients are treated with the maximum recommended dose, 4 grams per day. 2 Acetaminophen, which is available over-the-counter, is also the most common cause of poisoning in the United States. A single dose of 4–10 grams can damage the liver, and acetaminophen is the leading cause of acute liver failure. 5 Osteoarthritis patients who take acetaminophen have to be careful not to consume over-the-counter cold medicines or alcohol, for example, for fear of accidental liver damage, 2 and many are still not satisfied with their pain management. 2 So, if it were you, how would you feel about trying medical cannabis?

Over 80% of clinical studies have reported significant pain relief using cannabinoids. In two studies of patients with chronic and diabetic nerve pain, increasing concentrations of THC in cannabis provided progressively better pain relief, improved sleep quality, and caused only mild to moderate side effects. 3 But studies that specifically focus on arthritis are few and far between. One such study from 2006, treated patients with rheumatoid arthritis, an autoimmune disease, with Sativex, a pharmaceutical grade extract from whole cannabis plants that contains a 1:1 ratio of THC and CBD. Sativex significantly improved movement pain, pain at rest, and sleep quality in these patients, 6 but Sativex remains an investigational product in the U.S. and doesn’t have FDA approval.

Despite not fully understanding its mechanism of action, acetaminophen has been well-studied for treating chronic arthritic pain, and it has been helping relieve pain and inflammation via the ECS for decades. Acetaminophen has also been responsible for many poisonings, liver failures, and liver transplants. 5 We should question why it remains approved for over-thecounter use by the FDA. Meanwhile, U.S. regulations surrounding medical cannabis are so constrained that researchers are all but prohibited from studying real-world cultivars, each with a unique blend of cannabinoids and terpenes. For more on this, see the Research Corner on page 14.

63% OF OSTEOARTHRITIS PATIENTS ARE UNSATISFIED WITH THEIR CURRENT PAIN MEDICATION REGIMEN.

Perhaps if cannabis plants produced pills instead of flowers, history would be different, and I would be able to recommend specific cannabis cultivars for osteoarthritis, rheumatoid arthritis, and the like. But instead, I can recommend only this: talk to your doctor, and if you want to try CBD or medical cannabis for arthritis pain or breakthrough pain, remember that more is not always better. Try different doses, perhaps topical ointments too, and certainly different cultivars if you plan to use cannabis. You may find some cultivars provide better pain relief, or you prefer different cognitive effects. Some cultivars might be more appropriate for working in the morning; others might be better for sleep quality. Arthritis pain can stem from many sources—inflamed joints, damaged bones, and nerves—so I wouldn’t be surprised if someone with arthritis used multiple cultivars of cannabis, ointments, and other medications to ease their pain as effectively as possible.

References 1Madden, K., George, A., van der Hoek, N., Borim, F., Mammen, G., and Bhandari, M. "Cannabis for pain in orthopedics: a systematic review focusing on study methodology." Canadian Journal of Surgery 62, no. 6 (2019): 001018. https://www.ncbi.nlm.nih.gov/pubmed/31545565. 2Brown, J. and Boulay, L. "Clinical experience with duloxetine in the management of chronic musculoskeletal pain. A focus on osteoarthritis of the knee." Therapeutic Advances in Musculoskeletal Disease 5, no. 6 (2013): 291-304. https://doi.org/10.1177/1759720X13508508. 3O'Brien, M. and McDougall, J. "Cannabisand joints: scientificevidenceforthealleviation ofosteoarthritispain bycannabinoids." CurrentOpinion in Pharmacology40 (2018): 104-109. https://doi. org/10.1016/j.coph.2018.03.012. 4Bertolini, A., Ferrari, A., Ottani, A., Guerzoni, S., Tacchi, R., and Leone, S. "Paracetamol: new vistas of an old drug." CNS Drug Reviews 12, no. 3-4 (2006): 250-275. https://doi.org/10.1111/j.1527- 3458.2006.00250.x. 5Dimitropoulos, E. and Ambizas, E. "Acetaminophen toxicity: what pharmacists need to know." U.S. Pharmacist 39, no. 3 (2014): HS2-HS8. https://www.uspharmacist.com/article/acetaminophentoxicity-what-pharmacists-need-to-know 6Blake, D., Robson, P., Ho, M., Jubb, R., and McCabe, C. "Preliminaryassessmentoftheefficacy, tolerabilityand safetyofacannabis-based medicine(Sativex) in thetreatmentofpain caused by rheumatoid arthritis." Rheumatology 45, no. 1 (2006): 50-52. https://doi.org/10.1093/rheumatology/kei183.