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Colestipol

Class
Hypolipidemic agents
Subclass
Polyanionic resins
Substance name
Colestipol hydrochloride
Brand names
Colestid®
Common formulations
Granule for suspension
Dosage and administration
Adults patients
Treatment of primary hypercholesterolemia • Reducing total cholesterol or reducing LDL-C
•
Start at: 2 g PO q12-24h
•
Maintenance: 2-16 g PO daily, in 1-2 divided doses for 1-2 months, followed by possible uptitration
Other off-label uses
•
Treatment of generalized atherosclerosis
Indications for use
Labeled indications
Adults
•
Treatment of primary hypercholesterolemia (reducing total cholesterol or reducing LDL-C)
Off-label indications
Adults
•
Treatment of generalized atherosclerosis
Safety risks
Boxed warnings
Hemorrhoids
•
Use extreme caution with pre-existing constipation.
Metabolic acidosis
•
Use extreme caution with renal disease.
Contraindications
A serum triglyceride concentration > 400 mg/dl
Any pre-existing coagulopathy (e.g., hemophilia)
Warnings and precautions
Cholelithiasis
•
Use caution with gastrointestinal tract impairment or risk factors for biliary obstruction.
Hypothyroidism
•
Use caution with a history of thyroid disease.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
Renal replacement therapy
Any modality
•
Use acceptable. No dose adjustment required.
Hepatic impairment
Any severity
•
Use acceptable. No dose adjustment required. Monitor serum concentrations. Monitor serum aminotransferases.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B2
•
Use only if benefits outweigh potential risks. Vitamin K should be monitored during therapy. INR should be monitored during therapy. This drug is known to interfere with absorption of fat-soluble vitamins even in the presence of vitamin supplementation.
•
This drug is essentially not absorbed systemically (less than 0.17% of the dose) and is not expected to cause fetal harm when administered during pregnancy at recommended doses.
Breastfeeding
Acceptable for use during breastfeeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
Abdominal discomfort
Common 1-10%
•
Cholestasis, gastrointestinal bleeding, abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea, vomiting
Uncommon < 1%
•
Gastrointestinal bleeding, vitamin A deficiency, vitamin D deficiency, vitamin E deficiency, vitamin K deficiency
Unknown frequency
•
Folate deficiency, hemorrhoids, ↑ liver enzymes, migraine, arthralgia, back pain, chest pain, dizziness, dysphagia, dyspnea, fatigue, headache, insomnia, loss of appetite, musculoskeletal pain, skin rash, weakness, sinus tachycardia, urticaria
Interactions
Drug(s)
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