Colesevelam

Pronunciation

(koh le SEV a lam)

U.S. Brand Names

WelChol®

Generic Available

Canadian Brand Names

WelChol®

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

Pregnancy Risk Factor

Pregnancy Implications

Use only in pregnancy if clearly needed.

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to colesevelam or any component of the formulation; bowel obstruction

Warnings/Precautions

Use caution in treating patients with serum triglyceride levels >300 mg/dL (excluded from trials). Safety and efficacy has not been established in pediatric patients. Use caution in dysphagia, swallowing disorders, severe GI motility disorders, major GI tract surgery, and in patients susceptible to fat-soluble vitamin deficiencies. Minimal effects are seen on HDL-C and triglyceride levels. Secondary causes of hypercholesterolemia should be excluded before initiation.

Adverse Reactions

>10%: Gastrointestinal: Constipation (11%)

2% to 10%:

Gastrointestinal: Dyspepsia (8%)

Neuromuscular & skeletal: Weakness (4%), myalgia (2%)

Respiratory: Pharyngitis (3%)

Incidence less than or equal to placebo: Infection, headache, pain, back pain, abdominal pain, flu syndrome, flatulence, diarrhea, nausea, sinusitis, rhinitis, cough

Overdosage/Toxicology

Systemic toxicity low since it is not absorbed.

Drug Interactions

Sustained-release verapamil AUC and Cmax were reduced. Clinical significance unknown.

Digoxin, lovastatin, metoprolol, quinidine, valproic acid, or warfarin absorption was not significantly affected with concurrent administration.

Clinical effects of atorvastatin, lovastatin, and simvastatin were not changed by concurrent administration.

Stability

Store at room temperature. Protect from moisture.

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

Pharmacodynamics/Kinetics

Onset of action: Peak effect: Therapeutic: ~2 weeks

Absorption: Insignificant

Excretion: Urine (0.05%) after 1 month of chronic dosing

Dosage

Adult: 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: 4-6 tablets daily; maximum dose: 6 tablets/day

Dosage adjustment in renal impairment: No recommendations made

Dosage adjustment in hepatic impairment: No recommendations made

Elderly: No recommendations made

Administration

Administer with meal(s). Make sure patient understands dietary guidelines.

Monitoring Parameters

Serum cholesterol, LDL, and triglyceride levels should be obtained before initiating treatment and periodically thereafter (in accordance with NCEP guidelines)

Dietary Considerations

Should be taken with meal(s). Follow dietary guidelines.

Patient Education

Take medication exactly as directed; do not alter dosage without consulting prescriber. Other medications should be taken 1 hour before or 2 hours after colesevelam. You may experience constipation (increased exercise, increased exercise, fluids, fruit, fiber, or stool softener may help). Report persistent GI upset, skeletal or muscle pain or weakness, or respiratory difficulties. Breast-feeding precaution: Inform prescriber if breast-feeding.

Anesthesia and Critical Care Concerns/Other Considerations

Colesevelam alone or when combined with a statin is effective in lowering cholesterol. Colesevelam may increase triglycerides; therefore, it should be used with caution or avoided in patients with triglyceride levels

200 mg/dL. Systemic toxicity is low since the drug is not absorbed.

Cardiovascular Considerations

Colesevelam may be 4-6 times as potent as traditional bile acid sequestrants, perhaps because of its greater binding affinity for glycocholic acid (Steinmetz, 2002). Unlike cholestyramine and colestipol, colesevelam appears to reduce LDL cholesterol in a dose-dependent manner. Bile acid sequestrants can cause an undesirable increase in serum triglycerides. No trials are available comparing colesevelam to cholestyramine or colestipol. Colesevelam does not interfere with intestinal absorption of fat-soluble vitamins. Can be taken concurrently with a HMG-CoA reductase inhibitor.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

None reported

Mental Health: Effects on Psychiatric Treatment

Constipation is common, concurrent use with psychotropic agents may exacerbate this effect

Dosage Forms

Tablet, as hydrochloride [film coated]: 625 mg

References

Davidson MH, Dillon MA, Gordon B, et al, "Colesevelam Hydrochloride (Cholestagel): A New, Potent Bile Acid Sequestrant Associated With a Low Incidence of Gastrointestinal Side Effects," Arch Intern Med , 1999, 159(16):1893-900.

"Executive Summary of The Third Report of The National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, And Treatment of High Blood Cholesterol In Adults (Adult Treatment Panel III)," JAMA , 2001, 285(19):2486-97.

Steinmetz KL, "Colesevelam Hydrochloride," Am J Health Sys Pharm , 2002, 59:932-9.

International Brand Names

WelChol® (CA)

A.D.A.M., Inc. is accredited by URAC, also known as the American Accreditation HealthCare Commission (www.urac.org). URAC's accreditation program is the first of its kind, requiring compliance with 53 standards of quality and accountability, verified by independent audit. A.D.A.M. is among the first to achieve this important distinction for online health information and services. Learn more about A.D.A.M.'s editorial process . A.D.A.M. is also a founding member of Hi-Ethics (www.hiethics.com) and subscribes to the principles of the Health on the Net Foundation (www.hon.ch).

The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites. © 1997-2007 A.D.A.M., Inc. Any duplication or distribution of the information contained herein is strictly prohibited.

Home > Medical Reference > Complementary Medicine