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 ®):	colesevelam (Welchol ®):
colestipol (Colestid ®):

cholestyramine (Questran ®):

Mechanism of Action
Forms a nonabsorbable complex with bile acids in the intestine, releasing chloride ions in the process; inhibits enterohepatic reuptake of intestinal bile salts and thereby increases the fecal loss of bile salt-bound low density lipoprotein cholesterol.

Use
Adjunct in the management of primary hypercholesterolemia; pruritus associated with elevated levels of bile acids; diarrhea associated with excess fecal bile acids; binding toxicologic agents; pseudomembraneous colitis

Dosage
Oral (dosages are expressed in terms of anhydrous resin):
Children: 240 mg/kg/day in 3 divided doses; need to titrate dose depending on indication

Adults: 4 g 1-2 times/day to a maximum of 24 g/day and 6 doses/day

Administration
Mix powder with water or other fluid prior to administration; not to be taken in dry form. Suspension should not be sipped or held in mouth for prolonged periods (may cause tooth discoloration or enamel decay).

Supplied
Powder for oral suspension: 4 g of resin/5.7 g of powder (5.7 g packets, 240 g can) [light formulation]; 4 g of resin/9 g of powder (9 g packets, 378 g can)

Prevalite®: 4 g of resin/5.5 g of powder (5.5 g packets, 231 g can) [contains phenylalanine 14.1 mg/5.5 g; orange flavor]

Questran®: 4 g of resin/9 g of powder (9 g packets, 378 g can)

Questran® Light: 4 g of resin/5 g of powder (5 g packets, 210 g can) [contains phenylalanine 16.8 g/5 g]

colesevelam (Welchol ®):

Colesevelam is a high capacity bile acid binding molecule.
Use
Adjunctive therapy to diet and exercise in the management of elevated LDL in primary hypercholesterolemia (Fredrickson type IIa) when used alone or in combination with an HMG-CoA reductase inhibitor

Mechanism of Action
Colesevelam binds bile acids including glycocholic acid in the intestine, impeding their reabsorption. Increases the fecal loss of bile salt-bound LDL-C

Dosing (Adults): (usual): Oral:
Monotherapy: 3 tablets twice daily with meals or 6 tablets once daily with a meal; maximum dose: 7 tablets/day

Combination therapy with an HMG-CoA reductase inhibitor: 4 to 6 tablets daily; maximum dose: 6 tablets/day

[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. ]

Disclaimer

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

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