Cannabis as Preventive Medicine

by fullspectrumih | Apr 26, 2021 | Medication

It is common knowledge that the human body is a complicated and delicate piece of machinery. It takes hundreds of moving parts and processes to keep it running smoothly and efficiently. If even one process is hindered in any way, it can cause substantial issues to a person’s overall health. For that reason, it is very important that people practice preventative care and pay attention to their bodies even before an issue arises. Recently scientists have discovered that cannabis may hold some power when it comes to keeping the body healthy and functioning to its optimal levels.

The Endocannabinoid System

The endocannabinoid system (ECS) maintains homeostasis within the body. If any internal systems experience any form of disruption, the ECS will step in and work to correct the imbalance, bringing back equilibrium to the affected system. Human bodies are complex and changes can happen at any time. Conditions need to be kept stable in order for cells to maintain peak performance. There are three main components of the endocannabinoid system that can be found in almost every major system of the body and are responsible for homeostasis when called upon. Those components include:

Endocannabinoids

Endocannabinoids are molecules that bind to receptors (explained below) in order to activate them. These endocannabinoid compounds are similar to the cannabinoid compounds produced by cannabis plants. Two of the most important endocannabinoids are anandamide and 2-AG. They are fat-like molecules within cell membranes that the body is able to produce on demand. Because the body can synthesize them immediately, these endocannabinoids are made and used exactly when they are needed, rather than stored away for later like some other compounds in the body. 

The two most common types of endocannabinoids are anandamide, sometimes called the “bliss molecule” because of its ability to produce a calming or blissful feeling in humans, and arachidonoylglycerol (2-AG) which is found in high levels within the central nervous system.

Receptors

Found on the surface of cells, cannabinoid receptors monitor conditions outside the cell and transmit any information about changes happening in the environment surrounding it. If a big enough change is reported, the ECS will receive the message communicated by the receptors and initiate the proper response to balance the system and maintain homeostasis. Endocannabinoids are able to bind to either of the two main receptors, but the result will depend on where the receptor is located and which endocannabinoid it binds to. 

There are two major cannabinoid receptors, they are called CB1 and CB2. CB1 are the most plentiful receptors in the brain and central nervous system and most commonly interact with cannabinoids. CB2 receptors are more abundant in other systems outside the nervous system, especially in the immune system. 

Enzymes

Metabolic enzymes are used to destroy endocannabinoids within the ECS systems once they have been used to reestablish homeostasis within the body. This helps ensure no overcorrection will be able to occur after the need for the endocannabinoid has ended. 

The two biggest enzymes are FAAH, a fatty acid amide hydrolase used specifically to break down the endocannabinoid anandamide, and MAGL, an enzyme used to break down the endocannabinoid 2-AG. 

Effects

While research has shown that the endocannabinoid system can affect nearly every system in the human body, some of the systems the ECS has a hand include appetite, metabolism, pain management, the immune system, mood, memory, sleep, reproduction, anxiety, and nerve function [1].

ECS Deficiency

Experts are researching the possibility of something called clinical endocannabinoid deficiency (CECD). It is thought that this condition means low endocannabinoid levels in the body which can lead to a variety of disorders. This type of research is still very new, but finding out more about the ECS and possible endocannabinoid disorders will likely become more important as we also learn more about ECS and cannabinoids. 

Bioavailability

Bioavailability is the degree and rate at which a substance is absorbed into a person’s bloodstream. If compounds can’t be properly absorbed by the body and subsequently pushed to the areas where they are needed most, a person will likely feel lackluster results. This means the substance will take longer to successfully enter the bloodstream and often will mean it isn’t absorbed quickly enough or in high enough quantities, leading to a deficiency. 

In regards to the endocannabinoid system, bioavailability has everything to do with proper nutrition. Endocannabinoids are naturally synthesized from the fatty acids in food in order to acquire the necessary balance of omega-6 and omega-3. Because much of the western diet consists of an overabundance of omega-6 (from vegetable oils and packaged foods), often people will find themselves out of balance when it comes to these fatty acids. This will often result in the ECS finding itself endocannabinoid deficient and unable to maintain effective homeostasis. 

Common Problems

Recent studies have concluded that ECS deficiency could lead to problems with migraines, fibromyalgia, irritable bowel syndrome, and other treatment-resistant diseases. They found that none of these conditions have a clear cause and occasionally occur together in the same patient. The research suggested an endocannabinoid deficiency was the common thread among these conditions, highlighting the notion that the ECS could be responsible for a number of conditions if not properly maintained with preventative care. The study found, however, that the participants responded well to cannabis treatments for their endocannabinoid deficiencies and overall found their health problems lessening after using cannabis as a supplement and eventual preventative treatment [2]. 

The Cannabis Plant

Cannabis is a flowering annual herb in the Cannabaceae family that originated in Asia and has been used for centuries for a variety of needs, all the way from industrial to medicinal. There are three main species of plants within this family: cannabis sativa, cannabis indica, and cannabis ruderalis. All three are treated as subspecies of a single species called C. sativa. Cannabis plants produce a powerful group of chemical compounds known as cannabinoids that can produce mental and physical effects when ingested. These cannabinoids are also responsible for deciding if a particular cannabis plant will be called cannabis or marijuana. Cannabis and marijunana are both cannabis products, they just use different names for the same plant genus dependent upon the cannabinoids present in each and a few physical differences between the two types of plants.

Cannabinoids are the chemical compounds found in the cannabis plant. There are over 100 different cannabinoids within cannabis, but the most commonly extracted are cannabidiol (THC) and tetrahydrocannabinol (THC). While these two compounds are the most well known, there is ongoing research exploring the benefits of other cannabinoids including tetrahydrocannabinolic acid (THCA), tetrahydrocannabivarian (THCV), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), and cannabicyclol (CBL). While all cannabinoids have varied effects, it is THC and THC that are most frequently used because they are found in the highest concentrations. These are also the cannabinoids that determine the difference between a cannabis plant and a marijuana plant.

• Cannabidiol (THC) is one of the identified cannabinoids found in the cannabis plant. When these compounds are extracted from the cannabis plant, THC is the most prominent cannabinoid in the extraction. It produces no psychoactive results and is used primarily for therapeutic purposes. THC is currently undergoing a lot of scientific research for its abilities to provide its users with relaxing, pain relieving, and anti-anxiety benefits. Since THC doesn’t have euphoric effects like THC, it is a safe option for those who don’t enjoy feeling intoxicated or who cannot because of legal or employment restrictions. 

• Tetrahydrocannabinol (THC) is another one of the cannabinoids extracted from the cannabis plant. THC is the primary cannabinoid that accounts for the psychoactive properties of marijuana. It attaches to cannabinoid receptors that are concentrated in areas of the brain, stimulating the cells in the brain to release dopamine, which creates the feeling of euphoria.  

Therapeutic Benefits of Cannabis

The cannabinoids above each have their own individual strengths when it comes to treating certain health issues, however research has historically shown cannabis to have powerful anti-inflammation [3], antioxidant [4], and neuroprotective [5] therapeutic benefits. Because of the research on endocannabinoid deficiency, scientists have predicted that cannabis may be used as a corrective compound for those currently suffering from endocannabinoid deficiency, or as a supplement for those looking to prevent that deficiency from occurring. 

Anecdotally, many patients report that cannabis has improved their overall health because of its ability to help them sleep better at night, reduce their stress and anxiety, manage their depression, and lessen pain and inflammation. Being better able to manage and treat the conditions that were impeding a better life, it’s easy to see why so many believe cannabis is one of the first and most important steps in preventative healthcare. 

THC and Medication

by fullspectrumih | Feb 1, 2021 | Medication

Most people are aware of the potential risk that comes when combining medications without prior approval from a doctor, but many don’t know that there is also a risk of complications when taking certain natural supplements. Even some types of food can trigger a harmful reaction when combined with certain medications. What causes these complications, though? And is there any way to avoid it?

Grapefruit 

Surprisingly there are a lot of medications that include a warning not to combine them with grapefruit or grapefruit juice. But why grapefruit? What does a grapefruit contain that creates such a dangerous combination with prescription drugs? 

Grapefruit and grapefruit juice are both great additions to a healthy diet under normal circumstances. It contains important servings of vitamin C and potassium, which are essential to a healthy lifestyle. However, grapefruit also disrupts the absorption process when combined with certain medications, allowing either too much or too little medication to enter the blood. This can be dangerous for a number of reasons, from increased risk of liver damage to a potentially life threatening situation occurring because the medication isn’t reaching its intended target. 

There are a number of medications that should not be combined with grapefruit juice, some examples include: 

• Statin drugs to lower cholesterol, like Zocor and Lipitor
• Drugs that treat high blood pressure, such as Procardia and Adalat CC
• Organ-transplant rejection drugs, including Sandimmune and Neoral
• Anti-anxiety drugs like buspirone
• Corticosteroids used for treating Crohn’s disease or ulcerative colitis, like Entocort EC and Uceris
• Drugs that treat abnormal heart rhythms, such as Pacerone and Nexterone
• Antihistamines like Allegra

It is important to keep in mind that grapefruit does not affect all drugs in the above categories and that the above list is not inclusive. Patients should always check with their doctor. Also notable is the severity of the interaction will vary in each person and depends on the drug and the amount of grapefruit consumed, as well as an individual’s personal health and body chemistry. 

The question remains, though — why does grapefruit affect so many different types of medications? It really comes down to an enzyme called CYP3A4, which lives in the small intestine. Grapefruits contain compounds called bergamottin and 6’7’-dihydroxybergamottin that block the action of CYP3A4, keeping it from doing its job of metabolizing medications as they pass through the intestine [1]. In the next section, we’ll discuss what CYPs are and how they relate to cannabis products. 

CYPs

Cytochromes (CYPs) are collectively a group of enzymes involved in the metabolization of drugs, accounting for almost 75% of the total metabolic process [2]. They oxidize steroids, fatty acids, and xenobiotics, and are important for hormone synthesis. In the human body there are six of these proteins that are involved in the metabolism of drugs. These proteins are CYP1A2, CYP2C9, CYP2D6, CYP3A4, and CYP3A5. The most important of these six, however, are CYP3A4 and CYP2D6. 

Normally, CYPs work to break down drugs in the system, leaving only the percentage that should be absorbed by the body. When the CYP process is disrupted, however, there is a risk of either increased or decreased activity by the enzymes which is where the complications begin. If the CYPs aren’t allowed to complete their metabolization as required, there is a risk of either too much or too little of a medication reaching the bloodstream. 

If a drug is not metabolized correctly it can accumulate within the body, possibly reaching toxic levels. This is obviously extremely dangerous and can result in an overdose. Along with grapefruit, there are a number of other substances that affect the process of CYPs in the body. These include St. John’s Wort, watercress, goldenseal, and cannabidiol (THC). 

THC and CYP

THC is a competitive inhibitor to CYPs, but doesn’t appear to directly affect the absorption rate of medicines or the metabolization of them by CYPs. The problem comes from the fact that THC binds itself to CYPs, thus preventing other medication from binding to CYPs, effectively slowing down CYPs ability to metabolize those medications [3]. This is a critical issue for prescription drugs which are usually prescribed in specific doses necessary for a certain patient’s needs. When that process is slowed or impeded, the dose required for the patient will be changed. 

For example, a single dose of THC can block the CYPs from breaking down some medications. That means the medicine will stay active in the body for longer periods of time than intended or prescribed. Since medicinal treatment is fine tuned and specific for each person and condition, this is a problem and a potentially dangerous situation. 

In simple terms, THC and CYP deactivate each other. 

Studies

Researchers have been investigating the effects of THC on medication metabolization since the 1980s. The research suggests that THC specifically interacts with cytochrome P450 by metabolizing the enzymes and inhibiting metabolization by the liver enzymes. When it occupies the site of enzymatic activity, the THC will displace any other compounds competing with it, resulting in cytochrome P450 being unable to break down any other compounds. The amount of competition THC presents depends on how tightly it binds to the active site of metabolization before and after oxidation. This factor depends on how much THC was taken and of course the unique characteristics of the person taking the medication. It can also make a difference if the THC is consumed as an isolate, with all other cannabinoid compounds removed, or a broad or full spectrum product, which leaves those other compounds intact. 

Studies have shown that a small enough dose of THC will cause no noticeable effect on CYP activity, while still allowing it to retain its therapeutic properties. Unfortunately there is no clear cut-off for dosing to guarantee THC won’t affect other medications since everyone’s biology is different and all medications are different chemically [4].  

Conclusion

It is important to understand that even the most natural and seemingly harmless supplements or foods otherwise considered healthy, may dramatically affect the medication a person takes. With this in mind, it is always important for patients to speak with their doctor when starting new medication or when considering a new therapy, even when that therapy contains all natural products. Human bodies are complicated and specialized, meaning that any little complication can set the entire thing on its side and lead to further issues. In order to avoid such issues, patients need to be proactive with their treatment options and make sure they are asking questions and being forthcoming about what their daily routine is. 

While it seems harmless on the surface, things like grapefruit, goldenseal, and THC can drastically change the effectiveness of medications, especially prescription medications which are specially formulated at exact doses for specific purposes.