Colestipol

Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. [PubChem]

Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use.

Micronized Colestipol tablets are indicated as adjunctive therapy to diet for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet. Generally, micronized Colestipol tablets have no clinically significant effect on serum triglycerides, but with their use, triglyceride levels may be raised in some patients.

Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Treatment should begin and continue with dietary therapy. A minimum of six months of intensive dietary therapy and counseling should be carried out prior to initiation of drug therapy. Shorter periods may be considered in patients with severe elevations of LDL-C or with definite CHD.

According to the NCEP guidelines, the goal of treatment is to lower LDL-C, and LDL-C is to be used to initiate and assess treatment response. Only if LDL-C levels are not available, should the Total-C be used to monitor therapy. The NCEP treatment guidelines are shown below.

Colestipol is used to lower high cholesterol levels in the blood. This may help prevent medical problems caused by cholesterol clogging the blood vessels.

Colestipol works by attaching to certain substances in the intestine. Since Colestipol is not absorbed into the body, these substances also pass out of the body without being absorbed.

Colestipol may also be used for other conditions as determined by your doctor.

Colestipol is available only with your doctor's prescription.

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, Colestipol is used in certain patients with the following medical conditions:

• Diarrhea caused by bile acids
• Digitalis glycoside overdose
• Excess oxalate in the urine
• Itching (pruritus) associated with partial biliary obstruction

One dose (1 packet or 1 level scoopful) of Colestipol for oral suspension contains 5 gram of Colestipol. The recommended daily adult dose is one to six packets or level scoopfuls given once or in divided doses. Treatment should be started with one dose once or twice daily with an increment of one dose/day at one- or two-month intervals. Appropriate use of lipid profiles as per NCEP guidelines including LDL-cholesterol and triglycerides is advised so that optimal, but not excessive doses are used to obtain the desired therapeutic effect on LDL-cholesterol level. If the desired therapeutic effect is not obtained at one to six doses/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered.

To avoid accidental inhalation or esophageal distress, Colestipol for oral suspension should not be taken in its dry form. Colestipol for oral suspension should always be mixed with water or other fluids before ingesting. Patients should take other drugs at least one hour before or four hours after Colestipol for oral suspension to minimize possible interference with their absorption.

The scoop accompanying this product is not interchangeable with other scoops.

Before Colestipol for

Oral Suspension Administration

1. Define the type of hyperlipoproteinemia, as described in NCEP guidelines.

2. Institute a trial of diet and weight reduction.

3. Establish baseline serum total and LDL-cholesterol and triglyceride levels.

During Colestipol for

Oral Suspension Administration

1. The patient should be carefully monitored clinically, including serum cholesterol and triglyceride levels. Periodic determinations of serum cholesterol levels as outlined in the NCEP guidelines should be done to confirm a favorable initial and longer term response.

2. Failure of total or LDL-cholesterol to fall within the desired range should lead one to first examine dietary and drug compliance. If these are deemed acceptable, combined therapy or alternate treatment should be considered.

3. Significant rise in triglyceride level should be considered as indication for dose reduction, drug discontinuation, or combined or alternate therapy.

Mixing and Administration Guide

Colestipol for oral suspension should always be mixed in a liquid such as water or the beverage of your choice. It may also be taken in soups or with cereals or pulpy fruits. Colestipol for oral suspension should never be taken in its dry form.

With Beverages

1. Add the prescribed amount of Colestipol for oral suspension to a glassful (three ounces or more) of water or the beverage of your choice. A heavy or pulpy juice may minimize complaints relative to consistency.

2. Stir the mixture until the medication is completely mixed. (Colestipol for oral suspension will not dissolve in the liquid.) Colestipol for oral suspension may also be mixed with carbonated beverages, slowly stirred in a large glass; however, this mixture may be associated with GI complaints.

Rinse the glass with a small amount of additional beverage to make sure all the medication is taken.

With cereals, soups, and fruits

Colestipol for oral suspension may be taken mixed with milk in hot or regular breakfast cereals, or even mixed in soups that have a high fluid content. It may also be added to fruits that are pulpy such as crushed pineapple, pears, peaches, or fruit cocktail.

See also:
What is the most important information I should know about Colestipol?

Micronized Colestipol tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components.

Use Colestipol as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Colestipol by mouth with or without food.
• Swallow Colestipol whole. Do not cut, crush, or chew tablets.
• Always take 1 tablet at a time. Swallow the tablet right away.
• Take each dose with at least 1 full glass (8 oz [240 mL]) of water or other liquid. Swallowing the tablet will be easier if you drink plenty of liquids as you swallow each tablet.
• Take any other medicines at least 1 hour before or 4 hours after you take Colestipol.
• Drinking extra fluids and making sure you get enough fiber is recommended while you are taking Colestipol. Check with your doctor for instructions.
• Continue to take Colestipol even if you feel well. Do not miss any doses.
• If you miss a dose of Colestipol, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Colestipol.

Use: Labeled Indications

Primary hypercholesterolemia: Adjunctive therapy to diet in patients with primary hypercholesterolemia

Off Label Uses

Pruritus with primary biliary cholangitis

Based on limited and older data for cholestyramine (which is approved for relief of pruritus associated with partial biliary obstruction), as well as clinical experience, the American Association for the Study of Liver Diseases (AASLD) recommends the use of bile acid sequestrants as first-line treatment of pruritus associated with cholestasis.

See also:
What other drugs will affect Colestipol?

Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Management: Consider alternatives to this combination due to the risk of subtherapeutic amiodarone serum concentrations. If amiodarone is coadministered with colesevelam, administer amiodarone at least 4 hours before colesevelam. Consider therapy modification

Cardiac Glycosides: Bile Acid Sequestrants may decrease the absorption of Cardiac Glycosides. Monitor therapy

Chenodiol: Bile Acid Sequestrants may decrease the serum concentration of Chenodiol. Management: Administration of chenodiol 5 hours or more after bile acid sequestrants may reduce chenodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants. Consider therapy modification

Cholic Acid: Bile Acid Sequestrants may decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 to 4 hours before or 4 to 6 hours after administration of any bile acid-binding products to minimize the potential for a significant interaction. Consider therapy modification

Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Monitor therapy

Deferasirox: Bile Acid Sequestrants may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider a 50% increase in initial deferasirox dose, with monitoring of serum ferritin concentrations and clinical responses to guide further dosing. Consider therapy modification

DilTIAZem: Colestipol may decrease the absorption of DilTIAZem. Monitor therapy

Estrogen Derivatives (Contraceptive): Bile Acid Sequestrants may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer estrogen-based oral contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant. Consider therapy modification

Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Consider therapy modification

Fibric Acid Derivatives: Bile Acid Sequestrants may decrease the absorption of Fibric Acid Derivatives. Management: Separate doses by at least 2 hours to minimize this interaction; fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant. Consider therapy modification

Leflunomide: Bile Acid Sequestrants may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Consider therapy modification

Lomitapide: Bile Acid Sequestrants may decrease the absorption of Lomitapide. Management: Administer lomitapide at least 4 hours before or after administration of a bile acid sequestrant. Consider therapy modification

Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Monitor therapy

Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Monitor therapy

Methylfolate: Colestipol may decrease the serum concentration of Methylfolate. Monitor therapy

Multivitamins/Fluoride (with ADE): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Fluoride (with ADE). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, bile acid sequestrants may impair the absorption of fat-soluble vitamins. Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with AE, No Iron). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Mycophenolate: Bile Acid Sequestrants may decrease the serum concentration of Mycophenolate. Avoid combination

Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Management: Consider separating the administration times of niacin and bile acid sequestrants by a few hours in order to reduce the potential for decreased efficacy of these agents. Consider therapy modification

Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor therapy

Obeticholic Acid: Bile Acid Sequestrants may decrease the serum concentration of Obeticholic Acid. Management: Administer obeticholic acid at least 4 hours before or at least 4 hours after the administration of bile acid sequestrants. Consider therapy modification

Pravastatin: Bile Acid Sequestrants may decrease the serum concentration of Pravastatin. Management: Administer pravastatin at least 1 hour before or 4 hours after administration of bile-acid resins (eg, cholestyramine, Colestipol, colesevelam) to minimize the risk for any significant interaction. Consider therapy modification

Progestins (Contraceptive): Bile Acid Sequestrants may decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral progestin-containing contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant. Consider therapy modification

Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Monitor therapy

Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Management: Consider separating the doses of raloxifene and bile acid sequestrants by at least 4 hours. Consider therapy modification

Teriflunomide: Bile Acid Sequestrants may decrease the serum concentration of Teriflunomide. Management: Unless using this combination to intentionally enhance teriflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is unlikely to be effective at avoiding the interaction. Consider therapy modification

Tetracyclines: Bile Acid Sequestrants may decrease the absorption of Tetracyclines. Exceptions: Eravacycline. Monitor therapy

Thiazide and Thiazide-Like Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide and Thiazide-Like Diuretics. The diuretic response is likewise decreased. Management: Consider separating administraton of bile acid sequestrants and thiazide diuretics by at least 4 hours. Monitor for decreased therapeutic effects of thiazide diuretics if coadministered with a bile acid sequestrant. Consider therapy modification

Thyroid Products: Bile Acid Sequestrants may decrease the serum concentration of Thyroid Products. Management: Administer oral thyroid products at least 4 h prior to colesevelam, and at least 1 h before or 4-6 h after cholestyramine. Specific recommendations for Colestipol are not available. Monitor for decreased concentrations/effects of the thyroid product. Consider therapy modification

Ursodiol: Bile Acid Sequestrants may decrease the serum concentration of Ursodiol. Management: Administer ursodiol 2 to 4 hours before or at least 2 to 5 hours after bile acid sequestrants to minimize the potential for any significant interaction. Monitor for decreased therapeutic effects of ursodiol in patients receiving bile acid sequestrants. Consider therapy modification

Vancomycin: Bile Acid Sequestrants may diminish the therapeutic effect of Vancomycin. Management: Avoid concurrent administration of oral vancomycin and bile acid sequestrants when possible. If use of both agents is necessary, consider separating doses by at least 2 hours to minimize the significance of the interaction. Consider therapy modification

Vitamin D Analogs: Bile Acid Sequestrants may decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Management: Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Exceptions: Calcipotriene; Calcitriol (Topical); Tacalcitol. Consider therapy modification

See also:
What are the possible side effects of Colestipol?

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 granules, and are not necessarily drug related.

Difficulty swallowing and transient esophageal obstruction have been rarely reported in patients taking micronized Colestipol 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.

The following nongastrointestinal adverse reactions have been reported with generally equal frequency in patients receiving micronized Colestipol tablets, Colestipol granules, or placebo in clinical studies:

Cardiovascular

Chest pain, angina, and tachycardia have been infrequently reported.

Hypersensitivity

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

Musculoskeletal

Musculoskeletal pain, aches and pains in the extremities, joint pain and arthritis, and backache have been reported.

Neurologic

Headache, migraine headache, and sinus headache have been reported. Other infrequently reported complaints include dizziness, light-headedness, and insomnia.

Miscellaneous

Anorexia, fatigue, weakness, shortness of breath, and swelling of the hands or feet, have been infrequently reported.