Bile Acid Sequestrants


Serotonin 5-HT Receptor Agonists




Para-aminobenzoic Acid

Vitamin B6


Xanthine Derivatives

Bile Acid Sequestrants - Uses and Benefits

Type of Drug:

Drugs used as adjunctive therapy to diet and exercise to lower the level of LDL cholesterol and total cholesterol in the blood.

How the Drug Works:

Bile acid sequestrants increase the removal of bile acids from the body.

As the body loses bile acids, it replaces them by converting cholesterol from the blood to bile acids. This causes the blood level of cholesterol to decrease.

High blood levels of cholesterol may increase the risk of developing heart, coronary artery, or other vascular disease.


To lower high levels of cholesterol in the blood alone or in conjunction with proper diet, exercise, and possibly other lipid-lowering drugs.

Cholestyramine: To relieve itching associated with partial biliary obstruction.

Unlabeled Uses: Occasionally doctors may prescribe cholestyramine to bind the toxins produced by Clostridium edificial, the organism which causes antibiotic-induced pseudomembranous colitis. Choloslyrnrnine has also been used for treatment of chlordecone (Kopone)pesticide poisoning, bile salt-mediated and postvagotomy darrhea,and thyriod hormone overdose. Cholestyramine and colestipol ihave both been used to treat digitials toxicty.


Before treatment: Before treatment with a bile acid sequestrant, a vigorous attempt should be made to control cholesterol with appropriate diet, exercise, and weight reduction (in obese people).

Diseases that may increase cholesterol and must be treated before beginning treatment with bile acid sequestrants include:

Phenylketonuria: Some of these products contain phenylalanine. Consult your doctor or pharmacist.

Supplementation: Treatment with bile acid sequestrants may require supplementation with vitamins A, E, and D, oral vitamin K, or folic acid.

Pregnancy: Safety for use during pregnancy has not been established.

These agents are not absorbed systemically, and are not expected to cause fetal harm when administered during pregnancy in recommendod doses. Use only when clearly needed the potential benefits to the mother outweigh the possible hazards to the fetus.

Breastfeeding: Use caution when breastfeeding. The possible lack of proper vitamin absorption may have an effect on nursing infants. Consult your doctor.

Children: Dosage schedules have not been established. The effects 01 long-term use and effectiveness in maintaining lowered cholesterol levels are unknown.

Lab Tests: Lab tests will be required periodically during treatment with bile acid sequestrates. Tests may include blood counts, triglycerides, and cholesterol levels.

Drug Interactions:

Tell your doctor or pharmacist if you are taking or planning to take any over­the-counter or prescription medications or dietary supplements while taking bile acid sequestrants. Doses of one or both drugs may need to be modified or a different drug may need to be prescribed. The following drugs and drug classes interact with bile acid sequestrants:

  • Diclofenac (eg, Cataflam)

  • Dicumarol digoxin (eg, Lanoxin)

  • Divalproex sodium (eg, Depakote)

  • Furosemide (eg, Lasix)

  • Hydrocortisone (eg, Cortet)

  • Piroxicam (eg, Feldene)

  • Sulindac (eg, Clinoril)

  • Thiazide diuretics (eg, hydrochlorothiazide)

  • Thyroid hormones (eg, levo thyroxine sodium)

  • Valproic acid (eg, Depakene)

  • Warfarin (eg, Coumadin)

Side Effects:

Every drug is capable of producing side effects. Many patients experience no, or minor, side effects. The frequency and severity of side effects depend on many factors including dose, duration of therapy, and individual susceptibility. Possible side effects include:

Digestive Tract: Severe constipation or other persistent stomach problems; gastrointestinal bleeding or irritation; fatty or black stools; loose stools; occasional stomach pain; gas; indigestion; ulcer attack; bloating; belching; nausea; vomiting; heartburn; aggravated hemorrhoids; appetite loss; difficulty swallowing; diarrhea.

Nervous System: Headache; leg pain; anxiety; feeling of whirling motion; dizziness; fatigue; insomnia; drowsiness; fainting.

Respiratory System: Asthma; wheezing; shortness of breath. Skin: Rash; itching; hives; abnormal skin sensations.

Other: Unusual bruising or bleeding (eg, gums, rectum); hiccups; sour taste; weight loss or gain; difficulty swallowing; muscle pain; anemia, backache; chest pain; arthritis; ringing in the ears; blood in urine; painful urination; increased urination; burnt urine odor; fluid retention; tingling or numbness in legs and arms; swelling of hands or feet; inflammation of the uveal tract; inflammation of the pancreas or gall bladder; gallstones; increased libido; deficiencies of fat-soluble vitamins (eg, A and D).

Guidelines for Use:

  • Dosage is individualized. Take exactly as prescribed.

  • Do not stop taking or change the dose, unless instructed by your doctor.

  • Granules, powder - Mix with liquid (water or noncarbonated drinks), very liquid soups or cereals, or pulpy fruits (applesauce or crushed pineapple). Do not take the dry powder or granules alone.

  • Tablets - Take with food and liquids.

  • Cholestyramine tablets - May be taken with meals. Swallowing tab­lets is easier if you drink plenty of fluid as you swallow each tablet.

  • Cholestyramine powder - Mix the contents of 1 powder packet or 1 level scoopful with 2 to 6 fl oz water or noncarbonated beverage. Avoid accidental inhalation. Do not take dry.

  • Colestipol granules - Add the prescribed amount to a glass (3 oz or more) of liquid. Stir until completely mixed. Colestipol will not dissolve. May also mix with carbonated beverages, slowly stirred in a large glass. After taking, rinse glass with a small amount of additional beverage and swallow to ensure that all the medication is taken.

  • If a dose is missed, take it as soon as possible. If several hours have passed or it is nearing time for the next dose, do not double the dose to catch up, unless instructed by your doctor. If more than one dose is missed or it is necessary to establish a new dosage schedule, contact your doctor or pharmacist.

  • May interfere with the effects of other drugs taken at the same time. Take other drugs 1 hour before or 4 to 6 hours after bile acid sequestrants.

  • Contact your doctor if you experience unusual bleeding (eg, gums, rectum).

  • May cause constipation, gas, nausea, or heartburn. These effects usually disappear with continued use, but contact your doctor if these effects continue and are bothersome.

  • Most effective when used with a diet that decreases the intake of cholesterol and saturated fats.

  • Lab tests may be required to monitor therapy. Be sure to keep appointments.

  • Store at room temperature (59° to 86°F) in a dry place.


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