The bile acid sequestrants
(BAS) target bile acids and are mainly used to treat diarrhea.
Bile acid sequestrants
(cholestyramine [Questran[R]], colestipol [Colestid[R]], colesevelam [WelChol[R]]) inhibit the intestinal reabsorption of bile, thus increasing the amount excreted in the stool (Durstine et al., 2003).
Unfortunately, the older bile acid sequestrants
have multiple drug interactions (ie, warfarin, digitalis, phenobarbital), and patients dislike them, since they must remember to take other medications >1 hour before or >4 hours later (these problems are not seen with colesevelam, a newer drug).
Agents such as bile acid sequestrants
, niacin, and fibric acid compounds are commonly added to the statin drug regimen to further cholesterol reduction.
Drug Dosage Cost/Day * atorvastatin 5-80 mg/day $1.16 (5 mg) (Lipitor) fluvastatin 20-80 mg/day $1.48 (Lescol) (40 mg) lovastatin 20-80 mg/day $2.39 (20 mg) pravastatin 10-40 mg/day $2.78 (20 mg) (Pravachol) simvastatin 5-80 mg/day $2.53 (Zocor) (10 mg) NIACIN niacin, extended- 1-2.5 g/day $1.41 (1 g) release (Niaspan) BILE ACID SEQUESTRANTS
cholestyramine 4-16 g/day $2.96 (8 g) colesevelam 2.5-3.75 $4.74 (WelChol) g/day (3.75 g) colestipol 5-20 g/day $2.40 (5 g) (Colestid) FIBRATES gemfibrozil 600 mg b.i.d $1.98 fenofibrate 200 mg/day $2.58 (Tricor) Drug Comment ** atorvastatin Most widely prescribed statin, most (Lipitor) potent LDL reducer, and the sole statin not backed by a larger clinical trial demonstrating reductions in acute Ml, mortality, and other key end points.
Three subsequent clinical trials reported in 2008 evaluated the glucose and lipid-lowering effects of colesevelam HC1, which is a specifically engineered bile acid sequestrant
developed in the 1990s as a high-affinity, high-capacity bile acid-binding molecule.
Weitzman, an endocrinologist at Stony Brook University, New York, examined the interaction of levothyroxine with two relatively new drugs--colesevelam (Welchol), the newest bile acid sequestrant
approved for hyperlipidemia and diabetes; and lanthanum carbonate (Fosrenol), a new phosphate binder used in end-stage renal disease.
The bile acid sequestrant
colesevelam HCl, sold under the name WelChol, has been approved in the United States for LDL cholesterol lowering since 2000.
Budesonide is a locally acting corticosteroid that Puma believes targets the inflammation identified in a preclinical model of neratinib-induced diarrhea and colestipol is a bile acid sequestrant
that Puma believes targets potential bile acid malabsorption that could result from such inflammation.
One new drug that is expected to be approved in the coming year is a variant of a bile acid sequestrant
that can be taken as a capsule or a tablet.
In the past, niacin, fenofibrates, bile acid sequestrants
and fish oil were widely used to help normalize blood lipid levels.
The weight loss drugs Orlistat or Olestra, and the cholesterol-lowering bile acid sequestrants
Choletryamine, Colestipol, and Colsevelam can block fat absorption, creating a potential for vitamin K deficiency since it is fat-soluble.