Cholestyramine (CSM) is a bile acid sequestrant, traditionally used to lower cholesterol. Now it is being used to help with other stubborn health issues. Cholestyramine does not get absorbed in the body and is a great option for helping you to bind and eliminate biotoxins.

What is Cholestyramine?

In addition to being used to lower cholesterol, cholestyramine is also being used off-label to help with other stubborn health issues including the treatment of Chronic Inflammatory Response Syndrome (CIRS) and other biotoxin-related illness.

Cholestyramine Mechanism of Action

Cholestyramine (CSM) prevents bile from being reabsorbed into the body, this is what makes it a bile acid sequestrant. Cholestyramine has been used for years without complication for lowering cholesterol levels.

Uses of Cholestyramine

1) Helps CIRS, Biotoxin Issues, and Removes Bile and LDL

Cholestyramine is helpful in a few ways. First, it can bind directly to a wide variety of toxins. Second, it can help flush bile and LDL cholesterol out of your system, both of which contain toxins.

Cholestyramine Binds Directly to Toxins

Cholestyramine (CSM) has been very successful at lowering inflammation and improving VCS scores (a test used to determine neurotoxicity) for patients with Chronic Inflammatory Response Syndrome (CIRS). There are other binders that have been used with success, but CSM is the only scientifically studied and proven way to eliminate biotoxins from the body.

CSM binds ionophores from a wide variety of biotoxins produced by fungi, cyanobacteria, Lyme, and other infections, and excrete them from the body. Some toxins include Psalmotoxin, a spider toxin [1], Caribbean ciguatoxin [2], responsible for Ciguatera fish poisoning (CFP) [3] and Brevetoxin, responsible for neurotoxic shellfish poisoning (NSP) [4].

You can see the polycyclic ethers, surrounded by several double bonds. The CSM fits between, the positive charges attracting the negative charge of the toxins.

However, the most common toxins that can be bound by CSM come from a multitude of toxins produced by mold.

Ochratoxin A, a mycotoxin found in a wide variety of raw and processed foods such as coffee, dried fruits, wine, nuts, beans, bread, and rice, is a potent neurotoxin that can cause chronic effects in kidneys. It is genotoxic (damages DNA) and teratogenic (damages the fetus), and is considered a probable carcinogen. Ochratoxin is another toxin that is bound by taking CSM [5].

Cholestyramine is almost like a “glue” for biotoxins. It is a long polystyrene chain molecule with side groups of positively charged nitrogen called quaternary ammonium (1.43 Angstroms) (Shoemaker Conference, 2016). The shape and size of the positively charged molecules on the CSM are relatively the same size as many negatively charged biotoxins (at 1.41 Angstroms), making it easy for the CSM to bind to them. Once the biotoxins are bound within the gastrointestinal tract, the CSM prevents them from being reabsorbed into the intestines, before finally being excreted in the stool.

Cholestyramine will not be able to bind to every toxin (for instance, the botulinum toxin are too large), but it can bind to a majority of toxins that are relatively similar to its size. Several of the toxins that it can bind to are in the chart below (in red).

Cholestyramine Helps Flush Bile

Cholestyramine is composed of positively charged resins that bind to bile acids in the intestine in order to be excreted from the body.

Cholestyramine forms insoluble complexes with the bile, which is then excreted from the body [6].

By lowering bile, which stores toxins, that can also help reduce the toxic burden in the body.

Cholestyramine Reduces LDL Cholesterol

Serious infections can trigger sepsis, an inflammatory response throughout the body in response to the presence of bacteria or the byproducts of bacteria (Jarisch–Herxheimer reaction) that have been killed by antibiotics.

Sepsis isn’t an active infection, it’s your body’s response to the toxic parts of an infection.

When your body responds aggressively to an infection you will see high temperatures, racing heart, and low blood pressure, which is the case in CIRS as well.

Even if you defeat the infection, your body has a memory that can trigger a response when it finds parts of the toxin in your bloodstream [7].

The parts of the infection that your body recognizes as toxic ride around almost exclusively on LDL cholesterol [7].

Researchers found that the death rate from sepsis went down when they gave people a powerful drug to flush the LDL cholesterol out of their body [7].

Because cholestyramine lowers bile levels in the body, to even out bile levels, cholesterol in the liver is converted to bile, thus lowering cholesterol levels [6].

Patients that had a daily treatment of cholestyramine had reported levels of 50-80% less cholesterol compared to average control levels [6]. 

2) Stops Diarrhea

People who suffer from diarrhea can use cholestyramine to treat it.

Bile acid can stimulate the colon and cause diarrhea. However, after cholestyramine makes bile acid insoluble, the bile acid passes through the bowels and does not stimulate the colon, preventing diarrhea from happening [8].

Cholestyramine was found to be one of the most effective drugs to treat diarrhea, with a success rate of more than 70% [8].

3) Treats Bacterial Infection

Bacteria Clostridium difficile (C. diff) can overgrow in the digestive tract and release toxins that attack the lining of the intestines. It can be treated using cholestyramine and is used in conjunction with the antibiotic vancomycin to treat diarrhea and other symptoms related to this bacteria infection [9].

Lyme disease can also be treated by using cholestyramine and atovaquone (an antifungal and anti-parasite). It reduces the symptoms of the disease [10].

Cholestyramine can also bind E. coli and its toxins to help prevent diarrhea [11].

4) May Improve Blood Sugar Control in Diabetes Patients

Cholestyramine reduced blood glucose levels in patients with type 2 diabetes [12].

5) May Combat Hyperthyroidism

Patients that do not respond well to conventional therapy for hyperthyroidism can take daily doses of cholestyramine to treat hyperthyroidism and its symptoms [13].

6) Treats Digoxin Intoxication

Digoxin is a drug used to treat heart failures. Toxic levels of digoxin can cause health problems, and cholestyramine will reduce levels and decrease the performance of digoxin [14].

7) Prevents Itching

Cholestyramine can be used to stop pruritus or severe itching of the skin, that occurs when someone has liver failure [15].

Cholestyramine used in ointments can be also used to heal diaper rashes in babies [16].

8) May Reduce Pain

When used on patients post-surgery (for patients with hemorrhoids), cholestyramine ointments helped reduce pain by 15%. They also took fewer painkillers than the average patient [17].

9) May Reduce Inflammation

Cholestyramine and mesalazine (an NSAID) treatment can be used to treat collagenous colitis, a chronic inflammatory disease of the colon [18].

10) May Treat Anemia

Cholestyramine, coupled with flunarizine (calcium antagonist, not available in the US or Japan) and pentoxifylline (a vasodilator and anti-inflammatory) can help treat spur cell anemia, which is a lack of red blood cells due to alcoholism. This treatment of 3 drugs helped patients recover from anemia and also reduced the number of spur cells in the body [19].

11) May Promote Gallbladder Health

Cholestyramine is shown to increase the emptying of the gallbladder. This prevents gallstones from forming and is good for your health [20].

Side Effects of Cholestyramine

1) Gut-Related

2) Reduced Vitamin Absorption

Cholestyramine lowers the levels of Vitamin D and K. In some cases, patients were Vitamin K deficient after long-term usage of cholestyramine [21, 22].

You need to supplement with Vitamin K2 if you’re taking cholestyramine.

3) May Decrease Mineral Levels

Magnesium, Iron, and Zinc levels were found to decrease in rats that underwent cholestyramine diets. They also had increased urinary excretion of calcium and magnesium; however, calcium levels remained normal [23].

4) Might Cause Liver Damage

High levels of alanine aminotransferase in the blood can lead to liver damage. In a study done on healthy adults, they were given a daily dose of 8g of cholestyramine and their levels of alanine aminotransferase increased by more than three times. This huge increase was also coupled with cell death in the liver, which means that cholestyramine plays a part in liver damage [24].

5) Can Lower Thyroid Hormones

Bile activates receptors that increase thyroid hormones (TGR5).

By binding to bile, your thyroid hormones will go down, which is why it’s good for hyperthyroidism.

Using Cholestyramine

Adults usually take 4 grams of the pure CSM on an empty stomach (1 hour after food) 3 to 4 times a day. It’s best to eat something with fat 30 minutes after taking CSM in order to help stimulate bile. You may also take CSM 30 minutes before a meal.

Make sure to take CSM 3-4 hours away from medication to avoid binding of the medication. For this reason, taking vitamins first thing in the morning is the most efficient.

It’s a good idea to check VCS before taking CSM so that you can monitor its decrease as you continue taking CSM. Some will also test MMP9 before taking CSM. You’ll see why in the “What to Expect” section.

Generally, it’s best to mix several binders in water for the best results, such as a scoop of Activated charcoal, clay, a few caps of Chitosan-micro, 4 grams of CSM and Magnesium (taking this mixture with magnesium calm at night helps cover the taste of CSM).

You must be able to go to the restroom in order for the binders to have an effect, and the magnesium helps to offset any constipation effect. If you have major gastrointestinal problems, work up your dosage slowly, or as tolerated. For these people, it’s best to take a break after 3 months.

Dr. Shoemaker recommends someone with CIRS take cholestyramine until their VCS test is normalized. This can sometimes take longer than 3-6 months.

However, because long-term use can occasionally cause slight problems with your liver, it’s usually best to stop at the 3 or 4 marks and continue taking other binders in order to help your liver recover if need be. But toxins in the body can cause a lot of damage to the liver in general, so it’s best to get them OUT as soon as possible.

Contraindications of Cholestyramine

Contraindicated for severe hypertriglyceridemia and complete biliary obstruction [25].

Drug Interactions of Cholestyramine

Cholestyramine can decrease the absorption and prevent the full performance of the following drugs [26]:

Because these drugs help treat heart diseases, rheumatoid arthritis, high blood pressure, and diabetes, taking cholestyramine might cause more health problems.

What to Expect

Some people can begin to see improvement in their VCS tests (a test used to determine neurotoxicity) within a month of taking Cholestyramine. There are also cases of people with CIRS taking CSM and immediately having their symptoms disappear. This is rarer and usually requires a longer length of treatment.

Others may experience what Dr. Shoemaker describes as an “intensification,” meaning a short-term rise in symptoms after taking CSM, which then usually dies down over the next day or few days. If the intensification takes a long time to resolve, it’s best to temporarily stop CSM, then add it back in at a reduced dose of 4 grams 2 times a day.

If the intensification occurs again and lasts a while, you can take an MMP9 test to see if it has increased. If so, this is another clue that treating infections is a good next step before adding CSM back into the picture again.

There is no real data on why this happens, but the theory is that perhaps this is due to an already increased MMP9, or a current Lyme infection (I believe it could also be due to other infections which cannot be targeted directly by CSM and may require treatment in addition to the CSM). In this case, CSM is potentially increasing the release of toxins, causing a temporary spike in cytokines before they are then excreted from the body.

Usually, if MMP9 has increased after an intensification, it is a good idea to take a high dose of fish oil, and stay on an anti-inflammatory, low-lectin, low-tannin diet (you should be on this diet anyway throughout treatment). After 30 days your inflammation levels should be reduced and you may begin taking CSM at the regular dose of 4 grams, 3 to 4 times a day (as tolerated) dose.

Want More Targeted Ways to Combat Inflammation?

If you’re interested in natural and more targeted ways of lowering your inflammation, we at SelfHacked recommend checking out this inflammation wellness report. It gives genetic-based diet, lifestyle and supplement tips that can help reduce inflammation levels. The recommendations are personalized based on your genes.

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