Colestipol
Bile acid sequestrants
Bile acid sequestrants
A non-absorbed resin that binds bile acids in the gut, forcing the liver to use cholesterol to make more and lowering LDL.
Also called: colestipol hydrochloride
Quick facts
- Group
- Bile acid sequestrants
- Target
- Bile acids in the intestinal lumen (anion-exchange resin)
- Used for
- Primary high LDL cholesterol
- Key effects
- Constipation · Bloating · Nausea
- Monitor
- LDL cholesterol and triglycerides · Bowel habits
- ATC
- C10AC02
No doses: the clinician sets them by the current guideline.
Mechanism of action
Colestipol is an insoluble anion-exchange resin that stays in the gut. It binds bile acids and carries them out in the stool, breaking their enterohepatic circulation. The liver turns more cholesterol into new bile acids, makes more LDL receptors and takes up more LDL from the blood. Triglycerides may rise in some patients.
- Binds bile acids in the intestine
- Bile acids leave in the stool instead of returning to the liver
- Liver converts more cholesterol into bile acids
- More LDL receptors; LDL falls in the blood
Indications
- Primary high LDL cholesterol, as an adjunct to diet, when diet alone is not enough Atherosclerosis and dyslipidaemia →
Adverse effects
Common
- Constipation (the main complaint, sometimes severe)
- Bloating, belching, gas
- Nausea, vomiting, indigestion
- Haemorrhoids made worse
Contraindications
- Hypersensitivity to any component
Key interactions
- Many oral drugs (digoxin, thiazides, furosemide, tetracycline, penicillin G, gemfibrozil, propranolol)
- Their absorption may fall; other drugs are taken at least one hour before or four hours after colestipol.
- Fat-soluble vitamins (A, D, E, K) and folate
- Absorption reduced with long-term use.
- Mycophenolate
- Colestipol may lower mycophenolic acid exposure.
What is monitored
- LDL cholesterol and triglycerides
- Bowel habits
- Signs of bleeding (vitamin K) on long-term use
- Levels or effect of narrow-margin drugs taken with it (e.g. digoxin)
Administration and safety
- Tablets are swallowed whole, one at a time, with plenty of water; granules are mixed with liquid before use.
- Other medicines are taken at least one hour before or four hours after.
- More fluid and fibre help prevent constipation.
Pregnancy and breastfeeding
Not absorbed, but long-term use can reduce fat-soluble vitamin absorption, which may matter for the fetus; vitamin status is considered.
Nursing care
- Before: bowel habits, haemorrhoids, list of other oral medicines and their timing.
- During: constipation and abdominal distension; triglycerides.
- Teach the timing gap with other medicines.
- Teach to report bleeding gums or rectal bleeding.
Pharmacokinetics
- Absorption
- Not absorbed; it acts entirely inside the gut.
- Elimination
- In the stool, together with the bound bile acids.
Test yourself
Think of the answer, then tap the question to see it.
Why must other drugs be separated from colestipol?
The resin binds many drugs in the gut and reduces their absorption, so they are given one hour before or four hours after.
What happens to triglycerides with bile acid sequestrants?
They may rise, so these drugs are avoided when triglycerides are very high.
What is the most common adverse effect of colestipol?
Constipation.
Connections
← Back to the class: Bile acid sequestrants
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Colestipol: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - COLESTIPOL HYDROCHLORIDE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.