Combination drug therapy with HMG CoA reductase inhibitors and bile acid sequestrants for hypercholesterolemia.

Single-drug therapy is often not sufficient to lower total and low-density lipoprotein (LDL) cholesterol levels in patients with familial hypercholesterolemia to desirable or target levels. Therefore, combination drug therapy is often necessary. The most potent therapy to achieve this goal is a combination of a 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitor, which reduces cholesterol synthesis, and a bile acid sequestrant, which indirectly depletes the intrahepatic cholesterol pool. LDL cholesterol reductions reportedly vary between 52 and 54% in short-term trials. Combining a bile acid sequestrant with nicotinic acid reduces LDL cholesterol 34-55%, and with a fibrate, 12-42%. The triple-drug regimen of bile acid sequestrant, an HMG CoA reductase inhibitor, and nicotinic acid is even more effective, achieving reductions of 59-67%. All these regimens elevate high-density lipoprotein cholesterol levels concomitantly by 2-37%.