Cholestyramine: What It Is, How It Works, and What You Need to Know
When your body makes too much cholesterol or can’t clear bile properly, cholestyramine, a bile acid sequestrant that binds to bile acids in the gut to lower cholesterol and relieve itching. Also known as Questran, it’s one of the oldest cholesterol-lowering drugs still in use today. Unlike statins that block cholesterol production in the liver, cholestyramine works in your intestines. It grabs bile acids — which your liver makes from cholesterol — and pulls them out of your system before they can be reused. That forces your liver to pull more cholesterol from your blood to make new bile, lowering your overall levels.
This same mechanism helps with liver function, a condition where bile builds up and causes severe itching, often due to gallbladder disease or primary biliary cholangitis. When bile backs up into the bloodstream, it triggers that constant, frustrating itch. Cholestyramine traps those bile acids before they reach your skin, giving relief without touching your liver directly. It’s not a cure, but for many, it’s the only thing that stops the itching.
But it’s not without trade-offs. Because it binds to everything in your gut — not just bile — it can interfere with how your body absorbs other drugs. If you’re on thyroid meds, warfarin, or even some antibiotics, timing matters. Take cholestyramine at least 4 hours before or after other pills, or you risk making them useless. It also causes constipation, bloating, and gas in most users. That gritty powder mixed with water or juice? It’s not the most pleasant thing to swallow, but for many, the relief outweighs the hassle.
It’s not used for weight loss, diabetes, or heart disease directly — but it does help people who can’t take statins or need extra cholesterol control. You’ll often see it paired with other meds in patients with familial hypercholesterolemia or those who’ve had gallbladder surgery. And while newer drugs exist, cholestyramine remains a go-to because it’s cheap, well-studied, and doesn’t get absorbed into your bloodstream.
What you won’t find in most doctor’s offices is how it interacts with your gut microbiome. Some studies suggest long-term use changes gut bacteria, which might explain why some people report digestive shifts over time. It’s also not for everyone — if you have bowel obstructions, severe constipation, or trouble swallowing, your doctor will skip it.
Below, you’ll find real-world guides on how cholestyramine fits into broader medication safety, liver health, and drug interactions. From spotting side effects to understanding how it stacks up against other cholesterol tools, these posts give you the no-fluff details you won’t get from a pill bottle.
Pruritus in Cholestasis: Bile Acid Resins and New Treatment Options
Cholestatic pruritus is a severe, persistent itch caused by liver disease. Bile acid resins like cholestyramine are first-line, but new drugs like maralixibat offer better tolerance and effectiveness. Learn what works, what doesn’t, and what’s coming next.