Colesevelam

INTRODUCTION

Indications

Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol in patients with primary hypercholesterolemia; may be used alone or in combination with hepatic hydroxymethylglutaryl coenzyme A (HMG CoA) reductase inhibitor. Adjunctive therapy to diet and exercise to improve glycemic control in patients with type 2 diabetes.

Action

Binds bile acids in the GI tract. Result in increased clearance of cholesterol. Mechanism for lowering blood glucose unknown. Therapeutic Effects: Decreased cholesterol and blood glucose.

Adverse Reactions/Side Effects

GI: constipation, dyspepsia.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Monitor any untoward GI responses such as constipation and indigestion. Notify physician if these responses become problematic.

Interventions

• Design and implement aerobic exercise and endurance training programs to improve cardiovascular function and glycemic control and help to reduce the risk of coronary heart disease.

Patient/Client-Related Instruction

• Remind patients to take medication as directed to control hyperlipidemia even though they are asymptomatic.

• Counsel patients about additional interventions to help control lipid disorders and improve cardiovascular health, including dietary modification, regular exercise, moderation of alcohol consumption, and smoking cessation.

Pharmacokinetics

Absorption: Not absorbed; action is primarily local in the GI tract.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: Unknown.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Bowel obstruction; Triglycerides >500 mg/dL; History of pancreatitis due to hypertriglyceridemia.

Use Cautiously in: Triglycerides >300 mg/dL; Dysphagia, swallowing disorders, severe GI motility disorders, or major GI tract surgery; Pregnancy, lactation, or children (safety not established).

Interactions

Drug-Drug: May ↓ absorption of glyburide, levothyroxine, phenytoin, estrogen-containing oral contraceptives (give ≥4 hr before colesevelam).

Route/Dosage

PO (Adults): 3 tablets twice daily or 6 tablets once daily.

Availability

Tablets: 625 mg.