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Can Cholestyramine Effectively Manage Hyperthyroidism?

When it comes to managing the symptoms of hyperthyroidism, many people rely on antithyroid medication such as methimazole [1] or PTU.  But some people are unable to take antithyroid medication due to the side effects.  Others can tolerate antithyroid medication fine, but it might not be effective in lowering their thyroid hormone levels.  Bugleweed [2] is an antithyroid herb that can help many people who experience side effects from antithyroid medication, but in some cases this herb isn’t effective either.  And when someone is unable to lower their thyroid hormone levels, the person’s endocrinologist is very likely to recommend radioactive iodine or thyroid surgery as the only option.

Of course the ultimate goal should be to address the cause of the underlying condition.  Although this is true, it takes time to accomplish this, and in the meantime it’s important to manage the hyperthyroid symptoms.  After all, there are numerous risks associated with uncontrolled hyperthyroidism, including arrhythmias, atrial fibrillation [3], and thyroid storm.

Some people who are unable to tolerate antithyroid medication will take beta blockers.  And while beta blockers can help to manage the cardiovascular symptoms commonly experienced by those with hyperthyroidism and Graves’ disease, they don’t lower thyroid hormone levels (although some beta blockers can affect the conversion of T4 to T3).  So while beta blockers decrease the risk of developing arrhythmias and atrial fibrillation, there still is a risk of thyroid storm, and elevated thyroid hormone levels can also lead to decreased muscle mass and bone density [4].  The point I’m trying to make is that while it’s important to manage the cardiac symptoms associated with hyperthyroidism, it’s also important to lower the thyroid hormone levels.

What Is Cholestyramine?                                                                                       

Cholestyramine is a bile acid sequestrant.  It binds to certain components of bile, which in turn disrupts the enterohepatic circulation of bile acids.  Bile acid sequestrants are commonly used for lowering cholesterol or for the treatment of chronic diarrhea [5] (when the cause is due to bile acid malabsorption).  Cholestyramine can also bind to mycotoxins [6], and thus can be used as a treatment for toxic mold, although it of course is also important to remove the source of the mold.

How Can Cholestyramine Help With Hyperthyroidism?

Cholestyramine has been shown to interfere with the enterohepatic circulation of endogenous thyroid hormones, which is increased in hyperthyroidism (1) [7].  Simply put, it binds to thyroid hormones and then the hormones are excreted by the body.  In fact, this is why those people with hypothyroidism and Hashimoto’s don’t want to take cholestyramine around the same time they take thyroid hormone replacement (i.e. levothyroxine).

 What Does The Research Show?

One study evaluated the efficacy and safety of high-dose cholestyramine added to antithyroid medication in order to control hyperthyroidism (2) [8].  This was a small study, involving only five patients, all who took at least 30 mg of methimazole.  They were put on 4 grams of cholestyramine three times a day for four weeks.  When compared to a control group consisting of patients who only took methimazole, the group who took both the methimazole and cholestyramine showed a more rapid reduction of the T3 and T4 levels in nearly all subjects.

In another study, this one a randomized, double-blind, placebo-controlled trial involving 45 patients newly diagnosed with Graves’ disease, the patients were randomly assigned into three treatment protocols (3) [9].  Group one took 2 grams of cholestyramine twice per day, group two took one gram of cholestyramine twice per day, and group three took a placebo powder.  All three groups took 30 mg of methimazole and 40 mg of propranolol each day.  The length of the study was 4 weeks, and the thyroid hormone levels decreased more rapidly and to a greater extent in the cholestyramine-treated groups.  In addition, all of the patients in group one had normal thyroid hormone levels at the end of the study.

These studies, along with a few case reports (4) [10] (5) [7], showed that cholestyramine can decrease thyroid hormone levels more rapidly when combined with methimazole.  But how about if cholestyramine is taken without any antithyroid medication?  I was able to find a case report involving a 36-year old woman who was diagnosed with Graves’disease, and was unable to take antithyroid medication due to side effects (6) [11].  Four grams of cholestyramine was given every six hours, and while unfortunately the woman ended up receiving radioactive iodine, prior to receiving this treatment her free T4 levels improved significantly within five days.  Although this is only a single case study, it did provide some evidence that cholestyramine might be an effective monotherapy for those with hyperthyroidism who are unable to take antithyroid medication.

Can Cholestyramine Be Effective When Combined With Bugleweed?

As of writing this blog post I haven’t had any patients take cholestyramine along with bugleweed, and so I honestly don’t know if it would be effective when combined with this antithyroid herb.  However, earlier I did mention a case study that showed that cholestyramine was effective when taken without any antithyroid medication.  So it’s possible that you might not need to take either antithyroid medication or antithyroid herbs in combination with cholestyramine, but my guess is that combining it with bugleweed might help to lower the thyroid hormone levels quicker than just taking cholestyramine alone.

What Dosage Is Commonly Used?

In most cases the dosage of cholestyramine used was 4 grams three times per day.  This was the case when both antithyroid medication was used, as well as in the study where cholestyramine was taken without antithyroid meds.  However, another study involved taking either 1 or 2 grams of cholestyramine, and all of the patients who took 2 grams of it achieved a euthyroid state (normal thyroid hormone levels) by the end of the study.  It’s worth mentioning that the patients in the study also took 30 mg/day of methimazole, along with 40 mg/day of propranolol.

What Are The Side Effects of Cholestyramine?

There are a few downsides of cholestyramine.  First of all, it is only available in a powder form and doesn’t taste too good.  This of course isn’t a side effect, but I did want to mention it, as compliance might be an issue in some cases.  This is especially true with children and teenagers, but with some adults as well.  The main side effects of cholestyramine include constipation and abdominal discomfort.  One of the main concerns with antithyroid medication is that it can put stress on the liver and lead to elevated liver enzymes [12].  Although I’m not aware of evidence which shows that cholestyramine causes significant liver damage, mild elevations in the liver enzymes sometimes will occur (7) [13].

How Can You Convince Your Doctor To Prescribe Cholestyramine?

I have been working with hyperthyroid patients since 2009, and I have never had an endocrinologist recommend cholestyramine to their patients.  My guess is that many aren’t even aware that it can be an effective treatment for hyperthyroidism, and as a result, it might be challenging to get a doctor to write a prescription for this.  Keep in mind that an endocrinologist doesn’t need to write a prescription, as any medical doctor can do this, and it usually is easier to find an open-minded primary care physician than an open-minded endocrinologist.

Either way, if your doctor has never heard of cholestyramine as a treatment for hyperthyroidism, then I would suggest showing them the research presented in this blog post.  Make sure you let them know that the research is from published journal articles, and they of course can access the studies by clicking on the links in this blog post.  If your doctor is strongly opposed to natural treatment options you can choose not to present the entire blog post but just show them the research.  After all, cholestyramine isn’t a natural treatment option, but is just a different option than antithyroid medication.

For those who are able to tolerate methimazole but find it to be ineffective in managing hyperthyroidism, you also might want to let the endocrinologist know that you would be willing to take the cholestyramine in combination with the antithyroid medication.  The reason I bring this up is because they might be more likely to prescribe cholestyramine if they know that you will continue taking the methimazole.  If anyone reading this is successful in getting a prescription for cholestyramine to help manage their hyperthyroidism, I ask you to please come back to this blog post to share your experience in the comments section below.

In summary, cholestyramine is a bile acid sequestrant, and it might be a treatment option in some people with hyperthyroidism and Graves’ disease.  This is especially true when antithyroid medication isn’t effective in lowering the thyroid hormone levels, although cholestyramine might also be effective when used as a monotherapy.  The main side effects of cholestyramine include constipation, abdominal discomfort, and in some cases it can cause mild elevations of the liver enzymes.  But everything comes down to risks vs. benefits, and if taking cholestyramine can help someone to avoid radioactive iodine or thyroid surgery then in my opinion the minor side effects would definitely be worth it, although while taking it you of course would want to continue to address the cause of your condition.