What is the recommended dosing for colestipol (bile acid sequestrant)?

Colestipol Dosing

For hyperlipidemia, start colestipol at 2-16 g/day orally given once or in divided doses, with gradual titration recommended to minimize gastrointestinal side effects. 1

Standard Dosing Regimens

Initial and Maintenance Dosing

• Starting dose: Begin with 5 g (granules) once or twice daily, or 2 g (tablets) once or twice daily 2
• Titration schedule: Increase by 5 g/day (granules) or 2 g once or twice daily (tablets), but no more frequently than at one- or two-month intervals 2
• Maintenance range: 2-16 g/day given once or in divided doses 1
• Maximum dose: 30 g/day for granules; 16 g/day for tablets 1, 2

Dose-Response Relationship

• 5 g daily: Produces approximately 16.3% LDL-C reduction 1
• 10 g daily: Produces approximately 22.8% LDL-C reduction 1
• 15 g daily: Produces approximately 27.2% LDL-C reduction 1

Administration Guidelines

Preparation and Timing

• Never take in dry form to avoid accidental inhalation or esophageal distress 2
• Mix with fluids: Always combine with water or other beverages (at least 3 ounces), or incorporate into soups, cereals, or pulpy fruits 2
• Meal timing: Take with meals for optimal tolerability 1
• Dosing frequency: Can be administered once daily or divided into twice-daily dosing; both regimens show similar efficacy 3

Drug Interaction Management

• Critical timing rule: Other medications must be taken at least 1 hour before or 4 hours after colestipol to avoid impaired absorption 1, 2
• High-risk medications requiring separation: Cyclosporine, oral contraceptives (ethinyl estradiol/norethindrone), olmesartan, phenytoin, sulfonylureas, thyroid replacement therapy, and warfarin 1
• Warfarin-specific monitoring: Check INR frequently during colestipol initiation, then periodically 1

Special Populations and Indications

Bile Acid Diarrhea

• Starting dose: 1 g twice daily 1
• Titration: Increase by 1 g/day every other day based on clinical response 1
• Gradual titration rationale: Reduces side effects, increases compliance, and potentially reduces costs 1

Contraindication in Crohn's Disease

• Avoid in extensive ileal resection: Do not use colestipol in patients with Crohn's disease with extensive ileal involvement (particularly >100 cm resection) or resection, as it may worsen steatorrhea and cause substantial caloric loss 1

Safety Considerations

Contraindications

• Complete biliary obstruction 1
• History of serious hypersensitivity to colestipol 1

Common Adverse Effects

• Gastrointestinal: Constipation, dyspepsia, and nausea are most frequent 1
• Metabolic: May increase triglyceride levels or cause acute pancreatitis; monitor triglycerides and discontinue if pancreatitis develops 1
• Nutritional: May cause vitamin K or fat-soluble vitamin deficiencies; administer oral vitamins at least 4 hours before colestipol 1

Monitoring Parameters

• Baseline and periodic serum total cholesterol, LDL-C, and triglyceride levels per NCEP guidelines 2
• Assess for gastrointestinal symptoms throughout treatment 1
• If LDL-C fails to reach target, first examine dietary and drug compliance before considering dose escalation or combination therapy 2
• Significant triglyceride elevation warrants dose reduction, discontinuation, or alternative therapy 2

Clinical Pearls

Gradual titration is essential: Starting low and increasing slowly minimizes the high frequency of gastrointestinal side effects that commonly lead to discontinuation 1

Formulation considerations: Colestipol is available as granules (powder) and tablets; tablets may improve compliance compared to granules, though both are effective 4

Pregnancy safety: Colestipol is considered safe during pregnancy and lactation as it is not systemically absorbed 1