colesevelam hydrochloride: clinical use

Prescribing considerations

• Exclude and manage secondary causes of hypercholesterolaemia before initiation.
• Use caution with raised triglycerides, dysphagia, severe gastrointestinal motility disorders, inflammatory bowel disease, liver failure, major gastrointestinal surgery or significant constipation.
• Safety and efficacy have not been established in children and adolescents.
• Consider whether the tablet size and need to swallow it whole are suitable for the patient.

Contraindications and cautions

• Hypersensitivity to colesevelam hydrochloride or an excipient
• Bowel obstruction
• Biliary obstruction

Monitoring

• Check total cholesterol, LDL cholesterol and triglycerides to assess response and detect triglyceride elevation.
• Monitor anticoagulation closely with warfarin or similar agents.
• Monitor ciclosporin concentrations when colesevelam is started or stopped.
• For patients susceptible to malabsorption or deficiency, consider vitamins A, D and E and vitamin K status through coagulation parameters.

Clinical pharmacology

Colesevelam is a non-absorbed polymeric bile acid sequestrant. Interruption of enterohepatic bile acid recycling increases hepatic conversion of cholesterol to bile acids and LDL-receptor activity, increasing LDL clearance; triglycerides may rise.

Formulation and product differences

• The selected product is an off-white to light-yellow, capsule-shaped film-coated tablet.
• The tablets must remain intact and are supplied in a moisture-protective bottle containing an oxygen-absorber sachet.

Tablet

Route: Oral

Strengths: 625 mg