Antilipemic Agent (Bile Acid Seqestrant)

Adjunctive therapy to diet and exercise in the management of elevated LDL in primary hypercholesterolemia (Fredrickson type lla) when used alone or in combination with an HMG-CoA reductase inhibitor

B

Use only in pregnancy if clearly needed. No breast-feeding recommendations.

Hypersensitivity to colesevelam or any component; bowel obstruction

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.

>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

Systemic toxicity is low since the drug is not absorbed.

Sustained-release verapamil AUC and C_max 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.

Store at room temperature. Protect from moisture.

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

Absorption: Not significantly absorbed

Elimination: 0.05% was excreted in the urine after 1 month of chronic dosing

Peak effect: Maximal therapeutic response seen within 2 weeks

Adult: Oral:

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

Take with meal(s). Follow dietary guidelines.

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

Take once or twice daily with meals. Follow diet and exercise plan as recommended by healthcare provider. Tell healthcare provider if you are pregnant, plan on getting pregnant, or are breast-feeding.

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

Tablet: 625 mg

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.