How should I start colestipol (colestipol nitrate) in an adult patient who needs additional LDL‑cholesterol lowering after diet, exercise, and possibly a statin?

How to Order Colestipol

Start colestipol at 2–16 g/day orally, given once daily or in divided doses, always mixed with water or other fluids and taken with meals, with other medications administered at least 1 hour before or 4 hours after colestipol to avoid absorption interference. 1, 2

Initial Dosing Strategy

• Begin with 5 g once or twice daily (one packet or one level scoopful), then increase by one dose increment every 1–2 months based on LDL-cholesterol response 2
• The typical effective dose range is 15–30 g/day, which produces approximately 15–30% reduction in LDL-cholesterol 3, 4
• Lower doses (10 g/day) can be effective in moderate hypercholesterolemia, reducing LDL by 17–19% with better tolerability 5

Preparation and Administration Requirements

Critical preparation steps 2:

• Never give colestipol in dry form to avoid accidental inhalation or esophageal distress 2
• Mix each 5 g dose with at least 3 ounces of water, juice, or other beverage 2
• Stir until completely mixed (the powder will not dissolve) 2
• Rinse the glass with additional liquid to ensure complete dose administration 2

Alternative administration methods 2:

• Can be mixed with milk in hot or cold breakfast cereals 2
• Can be added to high-fluid soups 2
• Can be mixed with pulpy fruits (crushed pineapple, pears, peaches, fruit cocktail) 2
• May use carbonated beverages, but stir slowly in a large glass as this may increase GI complaints 2

Timing with Meals and Other Medications

Meal timing 6, 2:

• Always take with meals to maximize bile acid binding during digestion 6
• Schedule with breakfast and/or dinner for once or twice daily dosing 6

Critical drug interaction timing 1, 6, 2:

• All other medications must be taken at least 1 hour before or 4 hours after colestipol 2
• This is particularly critical for medications with narrow therapeutic windows including thyroid hormone, warfarin, phenytoin, and oral contraceptives 6
• Practical approach: take other medications first thing in the morning (1+ hours before colestipol) or at bedtime (4+ hours after) 6

Dosing Schedules and Flexibility

Flexible dosing options 5:

• 5 g twice daily (morning and evening with meals) 5
• 10 g once daily in the morning with breakfast 5
• 10 g once daily in the evening with dinner 5
• All three schedules produce similar LDL reductions (17–19%) with 10 g total daily dose 5

Dose escalation for higher-risk patients 4, 7:

• Can increase from 15 g/day to 30 g/day after 12 months if additional LDL lowering is needed 4
• The 30 g/day dose produces mean cholesterol decrease of 69 mg/dL versus 42 mg/dL with 15 g/day 4

Expected Efficacy

LDL-cholesterol reduction 1:

• Monotherapy at 5 g: 16.3% reduction 1
• Monotherapy at 10 g: 22.8% reduction 1
• Monotherapy at 15 g: 27.2% reduction 1

Combination therapy with statins 8, 7:

• Colestipol 20 g/day plus lovastatin produces 52% LDL reduction 8
• Colestipol plus niacin can achieve 55% LDL reduction and normalize LDL levels in familial hypercholesterolemia 7

Monitoring Requirements

Before starting colestipol 2:

• Define the type of hyperlipoproteinemia per NCEP guidelines 2
• Establish baseline serum total cholesterol, LDL-cholesterol, and triglyceride levels 2
• Institute trial of diet and weight reduction 2

During treatment 2:

• Monitor serum cholesterol and triglyceride levels periodically 2
• Significant rise in triglycerides should prompt dose reduction, discontinuation, or alternative therapy 2
• If LDL-cholesterol fails to reach goal, first examine dietary and drug compliance before considering combination or alternate therapy 2

Common Pitfalls and Adverse Effects

Gastrointestinal effects 1, 6, 4:

• Constipation, dyspepsia, and nausea are most common 6
• These are usually transitory and mild 4
• Taking with adequate liquid may help mitigate GI symptoms 6
• Constipation, nausea, and bloating may lead to discontinuation in some patients 4

Metabolic considerations 4:

• Serum uric acid may increase significantly during treatment 4
• Triglycerides may increase or remain unchanged 1

Vitamin supplementation 6:

• Patients requiring oral vitamins should take them at least 4 hours before colestipol to avoid impaired absorption 6