From the Guidelines
Colestid (colestipol) is a bile acid sequestrant medication that should be used to lower cholesterol levels in patients with hyperlipidemia, with a typical starting dose of 2-16 g/day orally, given once or in divided doses, as it can reduce LDL-C levels by 10.4% to 27.2% depending on the dose and combination with other therapies 1.
Mechanism of Action and Indications
Colestid works by binding to bile acids in the intestines, preventing their reabsorption and forcing the liver to use cholesterol to make more bile acids, which ultimately reduces cholesterol levels in the bloodstream. It is FDA-approved for use as an adjunct to diet to decrease LDL-C with primary hyperlipidemia.
Dosage and Administration
The dose and route of administration for Colestid are 2-16 g/day orally, given once or in divided doses. It comes as granules that should be mixed with liquids or soft foods before consumption, or as tablets that should be taken with plenty of water.
Efficacy and Safety
Colestid can reduce LDL-C levels by 10.4% to 27.2% depending on the dose and combination with other therapies. Common side effects include constipation, bloating, gas, and stomach pain. Colestid may decrease absorption of other medications, so they should be taken at least 1 hour before or 4 hours after Colestid.
Clinical Considerations
This medication is particularly useful for patients who cannot tolerate statins or need additional cholesterol-lowering therapy. It's especially effective at reducing LDL (bad) cholesterol but has minimal effect on HDL (good) cholesterol or triglycerides. Patients should maintain a low-cholesterol diet and regular exercise while taking this medication for optimal results.
- Key points to consider when prescribing Colestid include:
- Pill burden and inconvenience in preparation of oral suspension preparations
- GI side effects and potential for exacerbating hypertriglyceridemia
- Potential for drug interactions, particularly with medications that should be taken at least 1 hour before or 4 hours after Colestid
- Importance of monitoring triglyceride levels and discontinuing the medication if signs and symptoms of acute pancreatitis occur
- Consideration of alternative therapies if the patient has a history of tendon disorder or rupture, as Colestid may increase the risk of tendon rupture 1.
From the FDA Drug Label
PRECAUTIONS Prior to initiating therapy with colestipol hydrochloride for oral suspension, secondary causes of hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism), should be excluded, and a lipid profile performed to assess Total cholesterol, HDL-C, and triglycerides (TG).
Because it sequesters bile acids, colestipol hydrochloride may interfere with normal fat absorption and thus may reduce absorption of folic acid and fat soluble vitamins such as A, D, and K
Chronic use of colestipol hydrochloride may be associated with an increased bleeding tendency due to hypoprothrombinemia from vitamin K deficiency.
Colestid (Colestipol) is a medication used to lower cholesterol levels. It works by binding to bile acids in the gut and removing them from the body, which in turn lowers cholesterol production in the liver.
- Main uses:
- Lowering LDL-C (bad cholesterol) and total cholesterol levels
- Raising HDL-C (good cholesterol) levels
- Common side effects:
From the Research
Colestid Overview
- Colestid, also known as colestipol, is a bile acid sequestrant used to lower plasma lipid levels 3, 4, 5, 6.
- It is an anion exchange resin with properties similar to cholestyramine, another lipid-lowering binding resin 3.
Mechanism of Action and Efficacy
- Colestid reduces total plasma cholesterol concentrations, primarily low-density lipoprotein (LDL) cholesterol, by about 15-30% 3.
- It is effective in patients with primary hypercholesterolaemia without associated hypertriglyceridaemia (type IIa hyperlipoproteinaemia) 3, 6.
- Long-term colestipol therapy may reduce xanthoma size, arrest progression of coronary artery atherosclerosis, and reduce mortality from coronary heart disease 5.
Side Effects and Interactions
- Side effects of colestipol treatment are primarily gastrointestinal in nature, as the drug is essentially unabsorbed 3, 6.
- Colestipol may bind with other concomitantly administered drugs, reducing their absorption or enterohepatic recirculation 3.
- Dosage intervals of other concurrent medications should be adjusted to minimize potential interactions 3.
Clinical Applications
- Bile acid sequestrants, including colestipol, are used to treat primary hypercholesterolemia and hypercholesterolemia associated with mild hypertriglyceridemia 7.
- They may also be used as a second-line treatment for pruritus associated with cholestatic disease and in patients with incomplete biliary obstruction 7.
- Modulation of bile acid homeostasis may have a good clinical effect in managing diabetes mellitus and diarrhea from bile acid malabsorption 7.