‘’ The bioavailability of cannabinoids is lower when taken on an empty stomach or more accurately an empty liver.” <- so there it is! If you get nothing else from this please get that 📷
🙂 Consuming a teaspoon of healthy fat rich coconut oil gives those liver enzymes something else to work on. Having a light meal before oral dosing helps keep our digestive acids busy as well. The result is that most of the cannabis oil goodness gets to where we intended it to go and used the way we intended it to be.’
Dominic Le Prevost : When swallowed on an empty stomach surprisingly few cannabinoids avoid “first pass metabolism” by the liver and enter circulation unaltered. Studies indicate swallowed THC has a bioavailability of 4-20%. This low bioavailability is in direct contrast to the strong wave of psychoactivity often felt. The reason for this contradiction is that the metabolism of THC, into 11-OH-THC produces a molecule many times more psychoactive but with key medical benefits deactivated. Highly psychoactive metabolites are the reason that a cannabis high can have two distinct phases
People mistakenly take an intense high as indication their medicine has successfully absorbed and so believe they are healing themselves efficiently but sadly they are often mistaken. Counter intuitively the height of the high a person experiences can be a relatively poor indicator as to the amount of unmetabolised THC that is circulating and healing the body.
Due to the low and varied bioavailability of oral THC formulations, alternative routes of drug administration, including oromucosal (through the mouth lining), sublingual (under the tongue), vaporization and inhalation, and rectal administration, have been developed by pharmaceutical companies to improve the amount of delivered cannabinoids in their products. All medical user should take note of their measures. This is an industry that would much prefer to produce a usable cannabis pill. That they don’t is for good reason.
The bioavailability of cannabinoids is lower when taken on an empty stomach or more accurately an empty liver. Oils are metabolised mostly in the liver and by eating fat 30 minutes before administering cannabis oil the liver will be otherwise occupied when the medicine starts to circulate. A tablespoon of coconut oil is widely considered to be a healthy and effective option. Other supplements can be taken with or mixed into this coconut oil.. The eating of the coconut oil is to otherwise occupy the liver. Coconut oil is easily absorbed by the small intestine and transported to the liver. This makes coconut and cannabis infusions/mixes particularly inefficient.
For a liver problem it would be a very efficient delivery method however it’s perhaps still not always the best as vasodilation might be an issue. Your blood vessels (especially in the digestive system) become larger, allowing for increased blood flow, which is normally ok. However for people with gallbladder/liver problems, this means immediate inflammation and potentiall pain, despite any anti-inflammatory effects. Just because a cannabinoid has found it’s way to the liver does not however mean that it will remain there to successfully treat any disease there.
As mentioned before the enzymes that metabolise cannabinoids are mainly found in the liver. A cannabinoid entering the liver is more likely to connect with an enzyme and be metabolised than to connect with a cancerous cell. This makes liver cancer a trickier one to treat without additional supplements.
Beneficially certain plant molecules are metabolised by the same enzymes that metabolise most THC molecules. The enzyme is called CYP2C9 and the molecules are apigenin and amentoflavone. Apinenin can be found in tablets and certain foods and amentoflavone is available in supplements for weightlifters such as Amentomax. These molecules, as well as having additional benefits, will give the enzymes “busy work” allowing the cannabinoids greater opportunity to circulate, connect with and destroy mutated cells both in the liver and throughout the body.
This enzyme busying effect is called competitive inhibiton. A well known example of this is the grapefruit effect. A molecule in grapefruit called bergamottin competitively inhibits an enzyme called CYP3A4 that metabolises many pharmaceuticals causing a risk of build up and overdose. Bergamottin slows drug removal by 50-80% categorising it as a moderate inhibitor. Apigenin and Amentoflavone reduce “clearance” by >80%, a strong inhibitor. As one cannot overdose on cannabis we can safely harness this strong competitive inhibiton. This will allow cannabinoids greater chance to heal and maximise the benefits of an often expensive and limited supply. Amentoflavone is also among the more powerful inhibitors of 3A4.
Slowing metabolism does not however result in a stronger high. The main metabolite of THC is called 11-OH-THC. This metabolite is more psychoactive than THC. This is the reason that a cannabis high can have two distinct phases. Slowing metabolism of THC to 11-OH-THC means the more psychoactive metabolite’s entry into the body is spread out over a longer period. Consequently a person is less likely be made uneasy by a strong more condensed wave of psychoactivity.
It’s counter intuitive but the amount of healing occuring cannot easily be judged by the height of the high. THC will be long gone by the time the effects of the 11-OH-THC have stopped being felt. Additional oil should be administered whilst still feeling the effects of the 11-OH-THC if a constant pressure is to be placed on a disease.
To place a disease under constant pressure oil should be taken more than a couple of times a day. If apigenin and amentoflavone are being used perhaps 4-5 suppositories/doses in 24 hours. 50mg of apigenin and twice a day 200mg of Amentoflavone taken 30-40 minutes before each suppository should over a few days. A daily dose of 250mg of apigenin and 400mg amentoflavone is not excesse more might safely be used.
Apigenin ad amentoflavone will interact with certain pharmaceuticals. Such interactions are well understood researched and documented and so can be checked. Ask your pharmacist and/or check online. This effect will last for perhaps a few days after their use is discontinued. Their usage should be emphasised to and noted by any doctors who might be administering pharmaceuticals. Apigenin and amentoflavone are also MAOIs. MAOIs block an enzyme called monoamine oxidase, which breaks down excess tyramine in the body. Blocking this enzyme helps relieve depression. However, tyramine can quickly reach dangerous levels if you eat high tyramine foods, which may cause a spike in blood pressure and require emergency treatment. Tyramine is not tricky to avoid and many people take MAOIs. Tyramine is naturally found in small amounts in protein-containing foods. As these foods age, the tyramine level increases. Some foods high in tyramine include: Aged cheeses, such as aged cheddar and Swiss; blue cheeses such as Stilton and Gorgonzola; and Camembert. Cheeses made from pasteurized milk are less likely to contain high levels of tyramine, including American cheese, cottage cheese, ricotta, farm cheese and cream cheese. Cured meats, which are meats treated with salt and nitrate or nitrite, such as dry-type summer sausages, pepperoni and salami. Fermented cabbage, such as sauerkraut and kimchee. Soy sauce, fish sauce and shrimp sauce. Yeast-extract spreads, such as Marmite. Improperly stored foods or spoiled foods. Broad bean pods such as fava beans.
Observations from Larry Bright
‘These are some interesting ideas about increasing bioavailability of cannabis oils while treating liver disease during “first pass metabolism.”
My first conversation with Brewster James was by inbox some 6 months ago about this very topic. I understood his concept of keeping the liver busy because this is just so logical, but it’s not so easy to explain for someone like me with no real medical background. To articulate this document in a way that everyone can digest took some thought. I’ve ran into and appreciated these concepts discussed in other places as well, but this is the first time I’ve seen them detailed in one place.
Please note that loading our bodies up with the internet’s version of a “dose” isn’t a good plan. Our bodies are too different for any kind of generalizations about how much THC or CBD is needed to be effective. This paper discusses staging out our personalized dosing throughout a 24 hour period to get more out of our meds while using less of them.
The condensed takeaway here is that our liver does a great job of getting us schwacked out of our gourd on THC while denying us the healing effects we’re trying to achieve (more on that in a moment). Avoiding the hydrochloric acid in our stomachs, and keeping the P450 liver enzymes busy while ingesting cannabis oil will result in a greater bioavailability of our cannabinoids and terpenes while … again … needing less of them.
The bioavailability of cannabinoids is lower when taken on an empty stomach or more accurately an empty liver.” <- so there it is! If you get nothing else from this please get that ! Consuming a teaspoon of healthy fat rich coconut oil gives those liver enzymes something else to work on. Having a light meal before oral dosing helps keep our digestive acids busy as well. The result is that most of the cannabis oil goodness gets to where we intended it to go and used the way we intended it to be.
If our stomach acids are not busy digesting food then some of the various cannabinoids and terpenes get destroyed on the way in. If our liver is not busy processing fats and converting them into energy the P450 liver enzymes convert our delta-9-tetrahydrocannabinol (Δ9-THC) into 11-Hydroxy-Δ9-tetrahydrocannabinol (11-OH-THC) giving us sleepy high while leaving us very little THC left to kill cancer.
BTW, what this paper does not note is that CBD is also converted to 7-hydroxy-cannabidiol making it less effective as well. Keeping liver enzymes busy is crucial in making use of A L L of the cannabinoids and terpenes in our medication.
This paper explains of a few other things we can do to increase the bioavailability of our cannabinoids and terpenes. It includes advice on the use the monoamine oxidase inhibitors called apigenin and amentoflavone to temporarily block liver enzyme production to some degree.
If we’re fighting a disease we already have medical professionals on our team. We are well advised to consult them to keep a handle on the side effects of MAOIs. They’re used to battle depression by altering some of the enzymes going from the liver to the brain and are mostly harmless, but too much of anything can cause us harm.
Caution is the way.