Colestipol

What is Colestipol?

• Colestipol (Colestid) is a nonabsorbed bile acid sequestrant that is used to decrease the amount of fatty substances such as low-density lipoprotein (LDL) cholesterol in certain people with high cholesterol.
• It is also used to reduce stool volume and frequency, and in the treatment of chronic diarrhea.

Colestipol skeletal

Colestipol constituents

What are the uses of this medicine?

• Colestipol (Colestid) are used 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.

How does this medicine work?

• Colestipol (koe les' ti pol) is a large, highly positively charged anion exchange resin that binds to negatively charged anions such as bile acids (as well as other organic compounds and some medications).
• The binding of bile acids to colestipol creates an insoluble compound that cannot be reabsorbed and is thus excreted in the feces.
• Bile acids ordinarily undergo extensive (>95%) enterohepatic recirculation, being secreted in bile, acting as fat solubilizing compounds in the upper intestine, and then being reabsorbed in the distal small bowel.
• Chronic loss of bile acids from colestipol use results in a contraction of the total bile acid pool.
• The liver compensates for this decrease by increasing bile acid synthesis, which directly competes with cholesterol synthesis resulting in a decrease in serum levels of cholesterol.
• Some of the decrease in serum cholesterol may also result from inhibition of fat absorption by the binding of bile acids to colestipol.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have shown hypersensitivity to any of its components.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• amiodarone (Pacerone)
• antibiotics
• anticoagulants ('blood thinners') such as warfarin (Coumadin, Jantoven)
• digitoxin
• digoxin (Lanoxin)
• diuretics ('water pills')
• iron
• loperamide (Imodium)
• mycophenolate (Cellcept)
• oral diabetes medications
• phenobarbital
• phenylbutazone
• propranolol (Inderal, Innopran)
• thyroid medications

Is this medicine FDA approved?

• Colestipol was approved for use in the United States in 1977 and is one of the oldest and safest cholesterol lowering agents, but it is currently used largely as an adjunctive therapy when statins or other lipid lowering agents result in an inadequate decrease in cholesterol levels.
• Colestipol is used off-label to reduce the pruritus of chronic liver disease probably as a result of binding the “pruritogen” in the intestine (which is either a bile acid or an organic anion like a bile acid that undergoes enterohepatic circulation).

How should this medicine be used?

Recommended dosage: Colestipol hydrochloride tablets:

• 2 to 16 grams/day given once or in divided doses.
• The starting dose should be 2 grams once or twice daily.
• Dosage increases of 2 grams, once or twice daily should occur at 1- or 2-month intervals.

Colestipol granules: One dose (1 packet or 1 level teaspoon) of Colestid Granules contains 5 grams of colestipol hydrochloride. One dose (1 packet or 1 level scoopful) of FLAVORED Colestid Granules is approximately 7.5 grams powder which contains 5 grams of colestipol hydrochloride. The recommended daily adult dose is one to six packets or level scoopfuls given once or in divided doses (5 grams daily increasing to a maximum of 30 grams).

Administration:

• Colestipol comes as tablets and granules to take by mouth.
• The tablets are usually taken once or twice daily.
• The granules are usually taken one to six times daily.
• Unless otherwise instructed, take all other medications at least 1 hour before or 4 hours after you take colestipol because it can interfere with their absorption.
• Swallow the tablets whole with a glass of water or another liquid; do not chew, split, or crush them.
• Your doctor may gradually increase your dose at 1 to 2 month intervals, depending on your response.
• Do not take the granules dry.
• Add them to at least 3 ounces of a liquid (e.g., fruit juice, water, milk, or soft drink) and stir until completely mixed.
• If you use a carbonated beverage, mix it slowly in a large glass to minimize foaming.
• After taking the dose, rinse the glass with a small amount of additional liquid and drink it to be sure that you receive the entire dose.
• Colestipol also may be mixed with hot or regular breakfast cereals, thin soups, or pulpy fruit.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As tablets and granules for suspension

This medicine is available in fallowing brand namesː

• Colestid
• Colestid Flavored Granules
• Colestid Granules

What side effects can this medication cause?

The most common side effects of this medicine include:

• abdominal discomfort, indigestion, nausea, flatuence and constipation.

Less common side effects may include:

• intestinal gas (bloating and flatulence)
• indigestion and heartburn
• diarrhea and loose stools
• nausea and vomiting
• Bleeding hemorrhoids
• blood in the stool
• Peptic ulceration
• cholecystitis
• cholelithiasis
• Difficulty swallowing
• transient esophageal obstruction
• elevations of aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT) and alkaline phosphatase

Other side effects may include: Cardiovascular:

• Chest pain, angina, and tachycardia

Hypersensitivity:

• Rash, Urticaria and dermatitis

Musculoskeletal:

• Musculoskeletal pain, aches and pains in the extremities, joint pain and arthritis, and backache

Neurologic:

• Headache, migraine headache, sinus headache, dizziness, light-headedness, and insomnia

Miscellaneous:

• Anorexia, fatigue, weakness, shortness of breath, and swelling of the hands or feet

What special precautions should I follow?

• 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. This will usually respond promptly to parenteral vitamin K1 and recurrences can be prevented by oral administration of vitamin K1.
• Colestipol hydrochloride tablets may produce or severely worsen pre-existing constipation. The dosage should be increased gradually in patients to minimize the risk of developing fecal impaction. Increased fluid and fiber intake should be encouraged to alleviate constipation and a stool softener may occasionally be indicated.
• In patients with pre-existing constipation, the starting dose should be 2 grams once or twice a day. If the initial dose is well tolerated, the dose may be increased as needed by a further 2 to 4 grams/day (at monthly intervals) with periodic monitoring of serum lipoproteins. If constipation worsens or the desired therapeutic response is not achieved at 2 to 16 grams/day, combination therapy or alternate therapy should be considered.
• Since colestipol hydrochloride is a chloride form of an anion exchange resin, there is a possibility that prolonged use may lead to the development of hyperchloremic acidosis.
• Caution should be exercised when colestipol hydrochloride tablets are administered to a nursing mother. The possible lack of proper vitamin absorption described in the "Pregnancy" section may have an effect on nursing infants.
• Colestipol hydrochloride tablets may be larger than pills you have taken before. If you have had swallowing problems or choking with food, liquids or other tablets or capsules in the past, you should discuss this with your doctor before taking colestipol hydrochloride tablets.
• Swallow each tablet whole. Do not cut, crush, or chew the tablets.
• Colestipol hydrochloride tablets must be taken with water or another liquid that you prefer. Swallowing the tablets will be easier if you drink plenty of liquid as you swallow each tablet.
• Difficulty swallowing and temporary obstruction of the esophagus (the tube between your mouth and stomach) have been rarely reported in patients taking colestipol hydrochloride tablets.
• If you are taking other medications, you should take them at least one hour before or four hours after taking colestipol hydrochloride tablets.
• If you are taking gemfibrozil, take it 2 hours before or 2 hours after colestipol.
• Colestipol has not been associated with clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• The chief potential harm would be obstruction of the gastrointestinal tract.
• The location of such potential obstruction, the degree of obstruction and the presence or absence of normal gut motility would determine treatment.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Since colestipol hydrochloride is essentially not absorbed systemically, it is not expected to cause fetal harm when administered during pregnancy in recommended dosages.
• The use of colestipol hydrochloride 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.

Can this medicine be used in children?

• Safety and effectiveness in the pediatric population have not been established.

What are the active and inactive ingredients in this medicine?

Colestipol hydrochloride tablets:

Active Ingredient:

• COLESTIPOL HYDROCHLORIDE

Inactive Ingredients:

• CELLULOSE, MICROCRYSTALLINE
• COPOVIDONE K25-31
• SILICON DIOXIDE
• POLYETHYLENE GLYCOL 6000
• HYPROMELLOSE
• CELLACEFATE
• DIBUTYL SEBACATE

Who manufactures and distributes this medicine?

Colestipol hydrochloride tablets: Manufactured by:

• Amneal Pharmaceuticals Pvt. Ltd.
• Ahmedabad, INDIA

Distributed by:

• Amneal Pharmaceuticals LLC
• Bridgewater, NJ

Colestipol hydrochloride for oral suspension:

• Pharmacia & Upjohn Company LLC

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 20° to 25° C (68° to 77° F).

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Colestipol
• FDA Colestipol

Colestipol Resources
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