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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

International Brand Names:

WelChol® (CA)

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.

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