Cholestyramine

What is Cholestyramine?

• Cholestyramine or Colestyramine (Locholest; Locholest Light; Prevalite; Questran; Questran Light) is the chloride salt of a basic anion exchange resin, a cholesterol lowering agent, is intended for oral administration.
• Cholestyramine resin is quite hydrophilic, but insoluble in water.
• The cholestyramine resin in Cholestyramine is not absorbed from the digestive tract.
• Cholestyramine is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption.
• It is a strong ion exchange resin, which means it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix.
• The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer.

Cholestyramine resin

What are the uses of this medicine?

• Cholestyramine for Oral Suspension is used as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet.
• Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body.
• Cholestyramine for oral suspension is also used for the relief of pruritus associated with partial biliary obstruction.

How does this medicine work?

• Cholestyramine (koe" le stye' ra meen) 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 cholestyramine 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 cholestyramine 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.
• In addition, cholestyramine may also decrease in serum cholesterol by direct inhibition of fat absorption caused by its binding to bile acids in the intestine.

Use in pruritus of chronic liver disease:

• Cholestyramine is also effective in reducing the pruritus of chronic liver disease, probably as a function 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).
• Because cholestyramine binds to negatively charged molecules, it can also be used to reduce absorption of medications taken in toxic overdoses and has multiple drug-drug interactions.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• complete biliary obstruction where bile is not secreted into the intestine.
• hypersensitivity to any of its components.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

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

Is this medicine FDA approved?

• Cholestyramine was approved for use in the United States in 1973 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.

How should this medicine be used?

Recommended dosage:

• The recommended starting adult dose for all cholestyramine for oral suspension powdered products (Cholestyramine for Oral Suspension USP and Cholestyramine for Oral Suspension USP, Light) is one packet or one level scoopful once or twice a day.
• The recommended maintenance dose for all cholestyramine for oral suspension powdered products is 2 to 4 packets or scoopfuls daily (8-16 grams anhydrous cholestyramine resin) divided into two doses.
• It is recommended that increases in dose be gradual with periodic assessment of lipid/lipoprotein levels at intervals of not less than 4 weeks.
• The maximum recommended daily dose is six packets or scoopfuls of cholestyramine for oral suspension (24 grams of anhydrous cholestyramine resin).

Administration:

• Cholestyramine comes in a chewable bar and in a powder that must be mixed with fluids or food.
• It usually is taken two to four times a day.
• Take this medication before a meal and/or at bedtime, and try to take any other medications at least 1 hour before or 4 hours after you take cholestyramine because cholestyramine can interfere with their absorption.
• Continue to take cholestyramine even if you feel well.
• Do not stop taking cholestyramine without talking to your doctor.
• This precaution is especially important if you also take other drugs; changing your cholestyramine dose may change their effects.
• Cholestyramine is unpalatable and can be difficult to swallow.
• Place the contents of one single-dose packet or one level scoopful of Cholestyramine in a glass or cup. Add an amount of water or other noncarbonated beverage of your choice depending on the product being used.
• Stir to a uniform consistency and drink.
• Cholestyramine may also be mixed with highly fluid soups or pulpy fruits with a high moisture content such as applesauce or crushed pineapple.

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

This medicine is available in fallowing doasage form:

• As Oral Suspension

This medicine is available in fallowing brand namesː

• Locholest; Locholest Light; Prevalite; Questran; Questran Light

What side effects can this medication cause?

The most common side effects of this medicine include:

• constipation
• abdominal discomfort
• indigestion
• nausea
• flatulence

Less common side effects may include:

• nausea, vomiting, diarrhea, eructation, anorexia, and steatorrhea, bleeding tendencies due to hypoprothrombinemia (Vitamin K deficiency) as well as Vitamin A (one case of night blindness reported) and D deficiencies, hyperchloremic acidosis in children, osteoporosis, rash and irritation of the skin, tongue and perianal area.

Other side effects reported in patients taking cholestyramine resin include:

• Gastrointestinal: GI-rectal bleeding, black stools, hemorrhoidal bleeding, bleeding from known duodenal ulcer, dysphagia, hiccups, ulcer attack, sour taste, pancreatitis, rectal pain, diverticulitis.
• Laboratory test changes: Liver function abnormalities.
• Hematologic: Prolonged prothrombin time, ecchymosis, anemia
• Hypersensitivity: Urticaria, asthma, wheezing, shortness of breath.
• Musculoskeletal: Backache, muscle and joint pains, arthritis.
• Neurologic: Headache, anxiety, vertigo, dizziness, fatigue, tinnitus, syncope, drowsiness, femoral nerve pain, paresthesia.
• Eye: Uveitis.
• Renal: Hematuria, dysuria, burnt odor to urine, diuresis.
• Miscellaneous: Weight loss, weight gain, increased libido, swollen glands, edema, dental bleeding, dental caries, erosion of tooth enamel, tooth discoloration.

What special precautions should I follow?

• Chronic use of cholestyramine resin may be associated with increased bleeding tendency due to hypoprothrombinemia associated with Vitamin K deficiency. This will usually respond promptly to parenteral Vitamin K1 and recurrences can be prevented by oral administration of Vitamin K1.
• Reduction of serum or red cell folate has been reported over long term administration of cholestyramine resin. Supplementation with folic acid should be considered in these cases.
• There is a possibility that prolonged use of cholestyramine resin, since it is a chloride form of anion exchange resin, may produce hyperchloremic acidosis. Caution should also be exercised in patients with renal insufficiency or volume depletion, and in patients receiving concomitant spironolactone.
• Cholestyramine resin may produce or worsen pre-existing constipation. The dosage should be increased gradually in patients to minimize the risk of developing fecal impaction.
• In patients with pre-existing constipation, the starting dose should be 1 packet or 1 scoop once daily for 5–7 days, increasing to twice daily with monitoring of constipation and of serum lipoproteins, at least twice, 4–6 weeks apart.
• Increased fluid intake and fiber intake should be encouraged to alleviate constipation and a stool softener may occasionally be indicated.
• Inform your physician if you are pregnant or plan to become pregnant or are breastfeeding.
• Drink plenty of fluids and mix each 9 gram dose of Cholestyramine for Oral Suspension USP in at least 2 to 6 ounces of fluid. Mix each 5 gram dose of Cholestyramine for Oral Suspension USP, Light in at least 2 to 6 ounces of fluid before taking.
• Sipping or holding the resin suspension in the mouth for prolonged periods may lead to changes in the surface of the teeth resulting in discoloration, erosion of enamel or decay; good oral hygiene should be maintained.
• Cholestyramine has been associated with mild and transient serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent liver injury with jaundice.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• No ill effects were reported.

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.
• 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.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well controlled studies in pregnant women.
• The use of Cholestyramine in pregnancy or lactation or by women of childbearing age requires that the potential benefits of drug therapy be weighed against the possible hazards to the mother and child.

Can this medicine be used in children?

• The safety and efficacy of fluvastatin sodium in children have been evaluated.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• CHOLESTYRAMINE

Inactive Ingredients:

• ACACIA
• CITRIC ACID ANHYDROUS
• D&C YELLOW NO. 10
• FD&C YELLOW NO. 6
• POLYSORBATE 80
• PROPYLENE GLYCOL ALGINATE
• SUCROSE

Who manufactures and distributes this medicine?

Distributed by:

• PAR PHARMACEUTICAL COMPANIES, INC.
• Spring Valley, NY

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

• Store between 20º-25ºC (68º-77ºF).
• Excursions permitted to 15º-30ºC (59º-86ºF).

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 Cholestyramine
• FDA Cholestyramine

Cholestyramine Resources
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