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Colesevelam Hydrochloride

Pronunciation: KOE-le-SEV-e-lam HYE-droe-KLOR-ide
Class: Anti-hyperlipidemic agent, Bile acid sequestrant

Trade Names

- Tablets 625 mg


Increases removal of bile acids from the body by binding bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the conversion of cholesterol to bile acids is increased, which decreases serum cholesterol.

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Not absorbed.


Maximum reduction in serum cholesterol is achieved within 2 wk.

Indications and Usage

Adjunctive therapy to diet and exercise given alone or with an HMG-CoA reductase inhibitor for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson type IIa). Adjunctive therapy to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.


History of bowel obstruction; history of hypertriglyceridemia-induced pancreatitis; serum triglyceride concentration greater than 500 mg/dL.

Dosage and Administration


PO 1,875 mg (3 tablets) twice daily with meals or 3,750 mg (6 tablets) once daily.

General Advice

  • Administer with liquid and a meal.
  • Caution patient to swallow tablets whole and not to crush, chew, or break tablets.


Store at controlled room temperature (59° to 86°F). Protect from moisture.

Drug Interactions

Glyburide, hormonal contraceptives (containing ethinyl estradiol and norethindrone), levothyroxine, oral supplements containing fat-soluble vitamins (ie, vitamins A, D, E, and K), phenytoin

Administer at least 4 h prior to colesevelam.


Reduced INR has been reported. Monitor INR when before starting colesevelam and frequently during concurrent treatment.

Laboratory Test Interactions

None well documented.

Adverse Reactions


CV reactions (including arterial stenosis, bradycardia, MI), hypertension (3%).


Asthenia (4%); increased seizure activity (postmarketing).


Nasopharyngitis (4%); pharyngitis, rhinitis (3%).


Constipation (11%); dyspepsia (8%); nausea (4%); abdominal distension, bowel obstruction, dysphagia, esophageal obstruction, exacerbation of hemorrhoids, fecal impaction, pancreatitis (postmarketing).


Increased transaminases (postmarketing).


Triglyceride concentrations of 500 mg/dL or more (4%); hypoglycemia (3%).


Myalgia (2%).


Accidental injury (4%); flu syndrome (3%).



After initiation of treatment, assess lipid levels within 4 to 6 wk.


Category B .




Safety and efficacy not established.


No special considerations.

Renal Function

No differences in safety and efficacy between patients with CrCl less than 50 mL/min and those with CrCl of 50 mL/min or more.

Hepatic Function

No special considerations or dosage adjustments are recommended.

GI disorders

Use with caution in patients with dysphagia, major GI tract surgery, severe GI motility disorders, or swallowing disorders.


Use caution when treating patients with triglyceride levels higher than 300 mg/dL.

Secondary causes of hypercholesterolemia

Ensure that secondary causes of hyperlipidemia (eg, alcoholism, dysproteinemias, hypothyroidism, nephritic syndrome, obstructive liver disease, other drug therapy, poorly controlled diabetes) have been excluded before starting therapy.



Because colesevelam is not absorbed, the risk of toxicity is low.

Patient Information

  • Advise patient to read patient information leaflet before using the first time and to reread and check for new information with each refill.
  • Advise patient to drink plenty of fluids and maintain a high fiber intake to minimize risk of constipation.
  • Advise patient to take each dose with liquid and a meal.
  • Caution patient to swallow tablets whole and not to crush, chew, or break tablets.
  • Inform patient that constipation, gas, heartburn, and nausea may occur but usually go away with continued therapy. Advise patient to notify health care provider if these effects become bothersome, or if bleeding or unusual bruising occurs.
  • Inform patient that drug helps control, but does not cure, lipid abnormality and to continue taking drug as prescribed when lipid levels are lowered.
  • Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
  • Emphasize to patient importance of other modalities on cholesterol control such as dietary changes (increased soluble fiber intake, reduced saturated fat intake), regular exercise, smoking cessation, and weight control.
  • Instruct patients to discontinue colesevelam and seek immediate medical attention if symptoms of pancreatitis (eg, severe abdominal pain with or without nausea and vomiting) occur.

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