Oral Drug Metabolism Enhancement SUPER THREAD! Learn how to make your drugs work better for YOU!
by /u/StarScream999 Harm Reduction Guy
DISCLAIMER: The author of this article is not responsible for any liver or other organ damage that may be caused by using this protocol. Please take care of your liver by getting regular blood tests to ensure there is no liver damage. You can purchase a "Hepatic Function Panel (ALB, AST, ALT, TP) Liver Profile" blood test from Health Tests Direct for only $38, then you print out a sheet, take it into a Qwest lab location, have your blood drawn and they will email you your results the next day. You will have to do some basic research to ensure what you're looking at on your blood tests make sense to you and are not in a dangerous range. You can also protect yourself by taking supplements such as SNS Liver Assist XT which contain liver boost ingredients such as NAC (N-Acetyl-Cystine) and Milk Thistle. TUDCA (Tauroursodeoxycholic Acid) would also be a wise choice, as it helps clear the bile ducts of the liver. This would be a required part of the kit as it's necessary to function.
This combination is not for freshmen drug users, this is for individuals who have been using drugs for years and the liver has become so efficient at breaking them down, steps like this need to be taken to get the best result from the drug. SO BE CAREFUL WHEN USING THIS PROTOCOL! IF ANYTHING, TRY ONE COMPOUND I RECOMMEND AT A TIME SO YOU CAN SEE HOW IT INTERACTS WITH YOU AND THE DRUG YOU'RE TAKING!
Health Tests Drug: https://www.health-tests-direct.com/ordering-page
SNS Liver XT: https://a1-supplements.com/sns-liver-assist-xt
TUDCA: https://a1-supplements.com/competitive-edge-labs-tudca
Understanding Basic Oral Drug Metabolism
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TL;DR Recipe
1) We're going to either drink an 8oz glass of grapefuit juice or take 600mg of Grapefruit Extract Capsules. https://amzn.to/3o5W55J
2) We're going to take at least 10mg of Bioperine https://amzn.to/3wm53zG
3) 200mg-400mg of Cimetidine. https://amzn.to/3onN7km
4) We're going to wait 30-45 minutes.
5) We take the drugs we want to take.
6) Add 1 half a teaspoon of HPBC and pour it on your tongue, then swallow it with some water. Bioperine
Better when crushed and mixed with oil and used sublingually.
When you take any drug orally, it has to pass through the GI (gastrointestinal) tract, which can destroy part of the drug due to it's acidity, then it has to pass through the liver, where it has to pass through Cytochrome P450 (CYP) which a variety of enzymes in the liver that work to breakdown those drugs even more and make them even more less potent.
https://en.wikipedia.org/wiki/Cytochrome_P450
Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases.[1][2][3] In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown. In plants, these proteins are important for the biosynthesis of defensive compounds, fatty acids, and hormones.
There are dozens of CYP Enzymes in the human liver that work to break down various compounds. This is because your liver wasn't evolutionary developed to ingest drugs, it's meant to break down foods. Every human has different levels of CYP enzymes in their body that can metabolize drugs in different ways. That's why you might have a preference for a certain drug over another, because it might hit you harder because you have less of that particular CYP enzyme that breaks it down as much, or it could have a CYP enzyme that keeps it hanging out in the liver and slowly metabolize over a long period, keeping the high up longer.
CYP Enzymes: https://en.wikipedia.org/wiki/Cytochrome_P450#CYP_families_in_humans
When I first went to my psychiatrist, I took a DNA test to determine which CYP enzymes I have more of than others and which drugs would work best based on my liver's metabolism.
How to Bypass These CYP Enzymes and Sneak Drugs Through the Liver
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There are essentially four chemicals, sold OTC as dietary supplements and one drug that will help you bypass the liver and absorb your drugs more efficiently by using these techniques.
1) Grapefruit Juice
The effect is most studied with grapefruit and grapefruit juice, but similar effects have been observed with certain other citrus fruits. A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. It was reported in 2008 that similar effects had been observed with apple juice.
One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. Fruit consumed three days before the medicine can still have an effect. The relative risks of different types of citrus fruit have not been systematically studied. Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. People are also advised to ask their physician or pharmacist about drug interactions.
The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either metabolized by the enzyme to an inactive metabolite, or activated by the enzyme to an active metabolite.
In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.
Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine
Source: https://en.wikipedia.org/wiki/Grapefruit–drug_interactions
The main compounds we are looking for in the grapefruit juice are bergamottin and 6',7'-dihydroxybergamottin, as these are the main components that inactivate CYP3A4, the main CYP compound that breaks down drugs. Although I have seen supplements containing bergamottin and 6',7'-dihydroxybergamottin, I have been unable to find a source for it directly. So you have two options. You can go to the grocery store and buy yourself some bottles of Grapefruit Juice (try and get white or ruby 100% pure with NO SUGAR). Ideally, you want to buy it where it's been chilled during storage. If you're feeling a little bit reckless, some gin and my favorite, Campari, can help the grapefruit juice go down and now you're mixing alcohol and drugs so welcome to the wonderful world of drug abuse. NOTE: If you're taking heavy sedatives or opioids, adding alcohol might not be the best idea. But you want to drink an 8oz glass of grapefruit juice 30-45 minutes prior to your drug intake.
The second option is to buy Grapefruit Extract Capsules standardized for Naringin but with the full spectrum of other enzymes in them. These claim to aid weight loss, but that's a lot of bullshit. You want to take 600mg (2 capsules) 30-45 minutes prior to your drug intake.
Grapefruit Extract Capsules: https://amzn.to/3o5W55J
Naringin inhibits some drug-metabolizing cytochrome P450 enzymes, including CYP3A4 and CYP1A2, which may result in drug-drug interactions.Ingestion of naringin and related flavonoids can also affect the intestinal absorption of certain drugs, leading to either an increase or decrease in circulating drug levels. To avoid interference with drug absorption and metabolism, the consumption of citrus (especially grapefruit) and other juices with medications is advised against.
Now, all this stuff about so called "drugs". these substaneces have miracle properties and should be allowed to everyone might sound scary, we're not taking dangerous stuff here than can cause fatal interactions or anything like that. The fact that it can inhibit these CYP enzymes is actually good for us drug abusers.
2) Bioperine: https://amzn.to/3wm53zG
The next supplement in our toolkit to bypass the liver is Bioperine, a derivative of Black Pepper.
Black Pepper is a source of piperine, a molecule that does not do much on its own but can inhibit enzymes that would attack other molecules. Due to this, it is ingested alongside some supplements to increase their absorption rates and is almost always consumed with curcumin.
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Caution Notice
If using any drugs or pharmaceuticals, check with your MD before supplementing anything with Piperine in it in high quantities.
Piperine inhibits drug detoxifying enzymes. This typically increases bioavailability of any compound which would normally be attacked by said enzymes. This can be good (ie. curcumin, EGCG) or it can be bad by stopping a protective measure against toxic xenobiotics.
[...]
Piperine is known for changing metabolism of various drugs and supplements, most notably increasing curcumin bioavailability by 2000%. It affects metabolism by both intestinal absorption as well as downregulating or inhibiting phase II detoxification enzymes and the glucuronidation process in the liver. It may also contribute to increase absorption by slowing intestinal transit rate and thus prolonging the time said compounds are exposed to the potential uptake.
Source: https://examine.com/supplements/black-pepper/research/#enterohepatic-effects
Bioperine 10mg | 120 Capsules | Non-GMO & Gluten Free | Sourced from Black Pepper Extract (only $9 for 120 caps): https://amzn.to/3wm53zG
You want to take 10mg of Bioperine 30-45 minutes prior to your drug intake.
