Does Colestid (colestipol) cause side effects?

Colestid (colestipol) is an oral cholesterol-lowering drug used together with dietary modifications to treat high blood cholesterol levels

Other less common uses of Colestid include treatment of diarrhea due to increased intestinal bile acids after some types of intestinal surgery and treatment of itching associated with partial obstruction to the flow of bile due to liver disease

The itching is believed to be due to the accumulation of bile acids in the body. Colestid is not absorbed from the intestine into the body. Rather, it works by binding to bile acids in the intestine and promoting the elimination of bile acids in the stool

Bile acids are formed in the liver from cholesterol, secreted into bile and with the bile enter the intestine. Most of the bile acids are reabsorbed from the intestine back into the body to be cycled again through the liver and bile. 

By promoting the elimination of bile acids, Colestid forces the liver to convert more cholesterol into bile acids in order to replace the lost bile acids. This reduces the levels of cholesterol within the body. Colestid works similarly to cholestyramine (Questran).

Common side effects of Colestid include

Serious side effects of Colestid include

  • ulcers,
  • reduced absorption of nutrients,
  • fatty stools, and stomach or intestinal bleeding,
  • fecal impaction,
  • esophageal obstruction,
  • gallbladder inflammation, and
  • gallstones.

Drug interactions of Colestid include carbamazepine, diuretics such as hydrochlorothiazide and furosemide, propranolol, tetracyclines, and fat-soluble vitamins (vitamins A, D, and K), because Colestid binds many different compounds in the gastrointestinal tract, thereby inhibiting their absorption into the body.

  • Colestid can bind with and inhibit the absorption of thyroid hormones. Colestid also can bind with ursodiol.
  • Separating the doses of Colestid and these other compounds by several hours should prevent binding with Colestid.
  • Generally, other drugs should be administered one hour before Colestid or 4 hours after Colestid is administered.
  • Colestid binds to vitamin K, a vitamin which is required by the liver to make the factors that allow blood to clot.
  • Colestid, by reducing the action of vitamin K, may exaggerate the effect of warfarin, reducing the body's ability to form blood clots. This interaction could lead to abnormal bleeding. On the other hand, Colestid can bind with warfarin directly and inhibit the absorption of warfarin. To avoid this interaction, doses of warfarin and Colestid should be separated by at least 4-6 hours. Colestid is closely related to cholestyramine.
  • Cholestyramine has been more extensively studied than Colestid. Therefore, there are several drug interactions that have been described with cholestyramine for which data is lacking with Colestid. It would be prudent to assume that similar interactions exist for both drugs and to separate ingestion of Colestid from the other drugs by several hours. These interactions with cholestyramine include

Since Colestid is essentially not absorbed systemically, it is not expected to cause fetal harm when administered during pregnancy in recommended dosages.

  • There are no adequate and well-controlled studies in pregnant women, and the known interference with absorption of fat-soluble vitamins may be detrimental even in the presence of supplementation.
  • The use of Colestid tablets in pregnancy or by women of childbearing potential requires that the potential benefits of drug therapy be weighed against possible hazards to the mother or child. 

Caution should be exercised when Colestid is administered to a nursing mother. The possible lack of proper vitamin absorption may have an effect on nursing infants. Consult your doctor before breastfeeding.

What are the important side effects of Colestid (colestipol)?

The most common adverse effect is constipation. Other less frequent side effects are:

Rarely, ulcers, reduced absorption of nutrients, fatty stools, and stomach or intestinal bleeding may occur.

Other serious side effects of colestipol include:

  • Fecal impaction
  • Esophageal obstruction
  • Gallbladder inflammation
  • Ulcers
  • Gallstones

Colestid (colestipol) side effects list for healthcare professionals

Gastrointestinal

  • The most common adverse reactions are confined to the gastrointestinal tract.
  • To achieve minimal GI disturbance with an optimal LDL-C lowering effect, a gradual increase of dosage starting with 2 grams, once or twice daily is recommended.
  • Constipation is the major single complaint and at times is severe.
  • Most instances of constipation are mild, transient, and controlled with standard treatment.
  • Increased fluid intake and inclusion of additional dietary fiber should be the first step; a stool softener may be added if needed.
  • Some patients require decreased dosage or discontinuation of therapy.
  • Hemorrhoids may be aggravated.
  • Other, less frequent gastrointestinal complaints consist of abdominal discomfort (abdominal pain and cramping), intestinal gas (bloating and flatulence), indigestion and heartburn, diarrhea and loose stools, and nausea and vomiting.
  • Bleeding hemorrhoids and blood in the stool have been infrequently reported.
  • Peptic ulceration, cholecystitis, and cholelithiasis have been rarely reported in patients receiving colestipol hydrochloride granules, and are not necessarily drug related.
  • Difficulty swallowing and transient esophageal obstruction have been rarely reported in patients taking Colestid Tablets.
  • Transient and modest elevations of aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT) and alkaline phosphatase were observed on one or more occasions in various patients treated with colestipol hydrochloride.

The following nongastrointestinal adverse reactions have been reported with generally equal frequency in patients receiving Colestid Tablets, colestipol granules, or placebo in clinical studies:

Cardiovascular

Hypersensitivity

  • Rash has been infrequently reported. Urticaria and dermatitis have been rarely noted in patients receiving colestipol hydrochloride granules.

Musculoskeletal

Neurologic

Miscellaneous

What drugs interact with Colestid (colestipol)?

  • Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids. In vitro studies have indicated that colestipol hydrochloride binds a number of drugs.
  • Therefore, Colestid Tablets may delay or reduce the absorption of concomitant oral medication.
  • The interval between the administration of Colestid Tablets and any other medication should be as long as possible.
  • Patients should take other drugs at least one hour before or four hours after Colestid Tablets to avoid impeding their absorption.
  • Repeated doses of colestipol hydrochloride given prior to a single dose of propranolol in human trials have been reported to decrease propranolol absorption.
  • However, in a follow-up study in normal subjects, single-dose administration of colestipol hydrochloride and propranolol and twice-a-day administration for 5 days of both agents did not affect the extent of propranolol absorption, but had a small yet statistically significant effect on its rate of absorption; the time to reach maximum concentration was delayed approximately 30 minutes.
  • Effects on the absorption of other beta-blockers have not been determined. Therefore, patients on propranolol should be observed when Colestid Tablets are either added or deleted from a therapeutic regimen.
  • Studies in humans show that the absorption of chlorothiazide as reflected in urinary excretion is markedly decreased even when administered one hour before colestipol hydrochloride.
  • The absorption of tetracycline, furosemide, penicillin G, hydrochlorothiazide, and gemfibrozil was significantly decreased when given simultaneously with colestipol hydrochloride; these drugs were not tested to determine the effect of administration one hour before colestipol hydrochloride.
  • No depressant effect on blood levels in humans was noted when colestipol hydrochloride was administered with any of the following drugs:
  • Particular caution should be observed with digitalis preparations since there are conflicting results for the effect of colestipol hydrochloride on the availability of digoxin and digitoxin.
  • The potential for binding of these drugs if given concomitantly is present.
  • Discontinuing colestipol hydrochloride could pose a hazard to health if a potentially toxic drug that is significantly bound to the resin has been titrated to a maintenance level while the patient was taking colestipol hydrochloride.
  • Bile acid binding resins may also interfere with the absorption of oral phosphate supplements and hydrocortisone.
  • A study has shown that cholestyramine binds bile acids and reduces mycophenolic acid exposure.
  • As colestipol also binds bile acids, colestipol may reduce mycophenolic acid exposure and potentially reduce efficacy of mycophenolate mofetil.

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Medically Reviewed on 2/5/2021
References
FDA Prescribing Information

Professional side effects and drug interactions sections courtesy of the U.S. Food and Drug Administration.