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colestipol

Bile Acid Sequestrant · Antihyperlipidemic

Bile Acid SequestrantAntihyperlipidemic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
5 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • Mycophenolate MofetilSevereDatabaseDDInter
  • Mycophenolic AcidSevereDatabaseDDInter
  • TeriflunomideSevereDatabaseDDInter
  • ThyroxineSevereDatabase

Mechanism

Colestipol is highly positively charged and binds negatively charged bile acids in the intestine, preventing their reabsorption and promoting excretion in stool. This depletes the bile acid pool, stimulating hepatic bile acid synthesis and increasing LDL receptor production, which enhances LDL-C clearance from plasma. This effect is partially offset by enhanced cholesterol synthesis.

Indications

HyperlipidemiaSecond-line agent if statin therapy insufficient or in statin intolerancePatients 11-20 years of ageRetard atherosclerosis

Dosing

Adult
10 to 15 g daily (divided doses), starting with 1 scoop or packet twice daily and increasing dosage as needed and tolerated. Maximal dose up to 30 g daily.

Pharmacokinetics

Metabolism
Neither digested nor absorbed in the gut.

Contraindications

  • Severe hypertriglyceridemia (>250 mg/dL baseline)

Side effects

Common
Gritty sensation when drinking slurryBloatingDyspepsiaConstipationFlatulenceGastrointestinal symptoms
Serious
  • Hyperchloremic acidosis (rare)

Drug interactions

Mycophenolate Mofetil
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Mycophenolic Acid
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Teriflunomide
Severe
Database

Drug interaction classified as: absorption, metabolism

Source: DDInter

Thyroxine
Severe
Database

Significantly decreased thyroxine efficacy, leading to severe hypothyroidism symptoms or increased TSH levels

Administer thyroxine at least 4-5 hours before or after colestipol. Monitor TSH levels closely and adjust thyroxine dose as needed.

Ursodeoxycholic Acid
Severe
Database

Decreased efficacy of ursodeoxycholic acid.

Administer ursodeoxycholic acid at least 2 hours before or 4-6 hours after colestipol. Monitor for therapeutic effect.

Alirocumab
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Atorvastatin + Aspirin
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Evolocumab
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

L Thyroxine
Moderate
Textbook

Reduced efficacy of l-thyroxine.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Lovastatin
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Methyclothiazide
Moderate
Textbook

Reduced efficacy of thiazides.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Mevastatin
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of colestipol.

Source: G&G 14e · p738

Related guidelines

Other Bile Acid Sequestrant drugs

Ask House about colestipol

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Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team