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How Does Colesevelam Work?

Colesevelam is part of a class of drugs known as bile acid sequestrants. It works by binding to bile acids in the intestines, preventing them from being reabsorbed into the body. Bile acids are made in the liver from broken-down cholesterol. Therefore, removing these substances helps lower your blood cholesterol.
This medicine can lower total and LDL cholesterol levels, while slightly raising HDL cholesterol ("good" cholesterol).
It is not yet known how colesevelam works to help control blood sugar in people with type 2 diabetes. However, it is clear that the drug works within the digestive tract, since it is not absorbed into the rest of the body.

Clinical Effects

Colesevelam has been evaluated in several different studies for cholesterol and diabetes.
Effects on Cholesterol
Since this medication can lower total and LDL cholesterol levels (along with raising HDL), a person can decrease his or her risk of developing certain health problems by taking it.
In clinical research studies, people taking colesevelam 3800 mg to 4500 mg daily were able to:
  • Reduce LDL cholesterol by 15 to 18 percent
  • Reduce total cholesterol by 7 to 10 percent
  • Raise HDL cholesterol by 3 percent.
The combination of colesevelam with an HMG-CoA reductase inhibitor (known more commonly as a statin) can further lower cholesterol levels.
Effects on Diabetes
Studies have shown that colesevelam can help lower blood sugar in people with type 2 diabetes. These studies used it in combination with other diabetes medications, such as metformin, sulfonylureas, and insulin. These studies showed that adding colesevelam to this regimen can help lower fasting blood sugar and hemoglobin A1c (HbA1c), a measure of long-term blood sugar control.
Written by/reviewed by:
Last reviewed by: Kristi Monson, PharmD;
Last updated/reviewed:
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