Bile acid sequestrants

Background

Bile acid sequestering agents (Resins): The liver uses cholesterol to produce bile acids, which are used in the digestive process. The bile acid sequestrants bind to these acids, reducing their supply. In turn, this stimulates the liver to produce more bile acids, which uses more cholesterol. Unfortunately, the resins can increase triglyceride levels. When the statins are not sufficient to lower high cholesterol, these drugs can be added. Their use is often limited by side effects, which are primarily gastrointestinal. They can include nausea, bloating, cramping, and an increase in liver enzymes.

cholestyramine (Questran ®):

Dosing (Adults): (usual) Hypercholesterolemia/pruritis: initial: 4 grams orally qd to bid. maintenance: 8-16 g in divided doses. Maximum: 24 g daily.

colesevelam (Welchol ®):

Colesevelam is a high capacity bile acid binding molecule.
Dosing (Adults): (usual)- hypercholesterolemia: 3 tabs (1875 mg) orally bid or 6 tabs orally qd - may increase to 7 tabs (4375 mg) daily

[Supplied: 625 mg tablet ]

colestipol (Colestid ®):

Dosing (Adults): Recommended dose (Maintenance) -
(Tablets): 2 to 16 grams/day given once or in divided doses. The starting dose should be 2 grams once or twice daily. Dosage increases of 2 grams, once or twice daily should occur at 1 or 2 month intervals. If the desired therapeutic effect is not obtained at a dose of 2 to 16 grams/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered.
Adult (usual): powder: 5-30 g orally (mixed with liquid) once daily or in divided doses.

Colestipol tablets must be taken one at a time and be promptly swallowed whole, using plenty of water or other appropriate liquid. Do not cut, crush, or chew the tablets. Patients should take other drugs at least one hour before or four hours after colestipol tablets to minimize possible interference with their absorption.

[Supplied: 1 gram coated tablet. 5 grams/dose granules for oral suspension. ]

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David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc.

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