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Cholestyramine

 

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Cholestyramine



 
 
Cholestyramine or colestyramine (Questran, Questran Light, Cholybar) is a bile acid sequestrant
Bile acid sequestrant

The bile acid sequestrants are a group of medications used for binding certain components of bile in the gut. They disrupt the enterohepatic circulation of bile acids by sequestering them and preventing their reabsorption from the gut....
, which binds bile
Bile

Bile or gall is a bitter yellow or green fluid secreted by hepatocytes from the liver of most vertebrates. In many species, bile is stored in the gallbladder between meals and upon eating is discharged into the duodenum where the bile aids the process of digestion of lipids....
 in the gastrointestinal tract
Gastrointestinal tract

The digestive tract is the system of Organ s within multicellular animals that takes in food, digestion it to extract energy and nutrients, and expels the remaining waste....
 to prevent its reabsorption. The resin is a strong anion exchange resin, which means that 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 removes bile acids from the body by forming insoluble complexes with bile acids in the intestine, which are then excreted in feces.






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Cholestyramine or colestyramine (Questran, Questran Light, Cholybar) is a bile acid sequestrant
Bile acid sequestrant

The bile acid sequestrants are a group of medications used for binding certain components of bile in the gut. They disrupt the enterohepatic circulation of bile acids by sequestering them and preventing their reabsorption from the gut....
, which binds bile
Bile

Bile or gall is a bitter yellow or green fluid secreted by hepatocytes from the liver of most vertebrates. In many species, bile is stored in the gallbladder between meals and upon eating is discharged into the duodenum where the bile aids the process of digestion of lipids....
 in the gastrointestinal tract
Gastrointestinal tract

The digestive tract is the system of Organ s within multicellular animals that takes in food, digestion it to extract energy and nutrients, and expels the remaining waste....
 to prevent its reabsorption. The resin is a strong anion exchange resin, which means that 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 removes bile acids from the body by forming insoluble complexes with bile acids in the intestine, which are then excreted in feces. When bile acids are excreted, plasma cholesterol is converted to bile acid to normalize bile acid levels. This conversion of cholesterol into bile acids lowers plasma cholesterol concentrations. Bile acid sequestrants such as cholestyramine are primarily used to treat hypercholesterolemia
Hypercholesterolemia

Hypercholesterolemia is the presence of high levels of cholesterol in the blood . It is not a disease but a metabolism derangement that can be secondary to many diseases and can contribute to many forms of disease, most notably cardiovascular disease....
, but can also be used to treat the pruritus, or itching, that often occurs during liver failure
Liver failure

Acute liver failure is the appearance of severe complications rapidly after the first signs of liver disease , and indicates that the liver has sustained severe damage ....
 due to the liver's inability to eliminate bile.

Cholestyramine is also used to prevent diarrhea in Crohn's disease patients who have undergone post-ileal resection. The terminal portion of the small bowel (ileum) is where bile acids are reabsorbed. When this section is removed, the bile acids pass into the large bowel and attract water due to their osmotic effect, causing diarrhea. Cholestyramine prevents this increase in water by making the bile acids insoluble and osmotically inactive.

Available forms

Cholestyramine is available as powder form, in 4 gram packets, or in larger canisters. In the United States
United States

The United States of America is a Federal government constitutional republic comprising U.S. state and a federal district. The country is situated mostly in central North America, where its Contiguous United States and Washington, D.C., the Capital districts and territories, lie between the Pacific Ocean and Atlantic Oceans, Borders of the U...
, it can be purchased either as a generic medicine, or as Questran or Questran Light (Bristol-Myers Squibb
Bristol-Myers Squibb

Bristol-Myers Squibb , colloquially referred to as BMS, is a pharmaceutical corporation, formed by a 1989 merger between pharmaceutical companies Bristol-Myers Company, founded in 1887 by William McLaren Bristol and John Ripley Myers in Clinton, NY , and E.R....
).

Dosage

4 to 8 grams once or twice daily, maximum dose 24 grams a day.

Side-effects


The following side effects have been noted.

  • Most frequent: Constipation
    Constipation

    Constipation, costiveness, or irregularity, is a condition of the digestive system in which a person experiences hard feces that are difficult to expel....
  • Seldom: tooth discoloration, tooth enamel erosion, and premature tooth decay, all from prolonged oral exposure to the suspension
  • Increased risk for gallstones due to increased cholesterol content of bile.


Warnings


Patients with hypothyroidism
Hypothyroidism

Hypothyroidism is the disease state in humans and in animals caused by insufficient production of thyroid hormone by the thyroid gland. Cretinism is a form of hypothyroidism found in infants....
, diabetes, nephrotic syndrome
Nephrotic syndrome

Nephrotic syndrome is a nonspecific disorder in which the kidneys are damaged, causing them to leak large amounts of protein from the blood into the urine....
, dysproteinemia, obstructive liver disease, kidney disease, or alcoholism
Alcoholism

Alcoholism is a term with multiple and sometimes conflicting definitions to describe the detrimental effects of alcohol intake.In common and historic usage, alcoholism refers to any condition that results in the continued consumption of alcoholic beverages despite health problems and negative social consequences....
 should consult their doctor before taking this medication. Other drugs should be taken at least one hour before or four to six hours after cholestyramine to reduce possible interference with absorption.

Patients with phenylketonuria
Phenylketonuria

Phenylketonuria is an Dominance genetic disorder characterized by a deficiency in the enzyme phenylalanine hydroxylase . This enzyme is necessary to metabolize the amino acid phenylalanine to the amino acid tyrosine....
 should consult with a physician before taking Questran Light because that product contains phenylalanine
Phenylalanine

Phenylalanine is an a-amino acid with the chemical formula HO2CCHCH2C6H5, which is found naturally in the breast milk of mammals and manufactured for food and drink products and are also sold as nutritional supplements for their reputed analgesic and antidepressant effects....
.

Drug interactions

The following interactions have been noted.
  • Digitalis
    Digitalis

    Digitalis is a genus of about 20 species of herbaceous Perennial plant, shrubs, and Biennial plant that are commonly called foxgloves....
  • Estrogens and progestins
  • Oral diabetes drugs
  • Penicillin G
    Penicillin

    Penicillin is a group of antibiotics derived from Penicillium fungi. They are Beta-lactam antibiotics used in the treatment of bacterial infections caused by susceptible, usually Gram-positive, organisms....
  • Phenobarbital
    Phenobarbital

    Phenobarbital or phenobarbitone is a barbiturate, first marketed as Luminal by Bayer. It is the most widely used anticonvulsant worldwide and the oldest still commonly used....
  • Spironolactone
    Spironolactone

    Spironolactone is a diuretic and is used as an antiandrogen.It is a synthetic 17-lactone drug that is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat heart failure, ascites in patients with liver disease, low-renin hypertension, hypokalemia, and Conn's syn...
  • Tetracycline
    Tetracycline

    Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections....
  • Thiazide
    Thiazide

    File:Benzothiadiazine.pngThiazide is a term used to describe a type of molecule and a class of diuretic.The members of this class of diuretics are derived from benzothiadiazine....
    -type diuretic pills
  • Thyroid
    Thyroid

    The thyroid is one of the largest endocrine glands in the body. This gland is found in the neck inferior to the thyroid cartilage and at approximately the same level as the cricoid cartilage....
     medication
  • Warfarin
    Warfarin

    Warfarin is an anticoagulant. It was initially marketed as a pesticide against rats and mice, and is still popular for this purpose, although more potent poisons such as brodifacoum have since been developed....
  • Arava
    Arava

    Arava can refer to:*Arava, Estonia, a village in Anija Commune, Harju County, Estonia.*Arabah, a section of the Great Rift Valley between the Dead Sea and the Gulf of Aqaba in Israel and Jordan....


Most interactions are due to the risk of decreased absorption of these drugs.

Duration of treatment

The duration of treatment is not limited, but the prescribing physician should reassess at regular intervals if continued treatment is still necessary.

Overdose


Principal overdose risk is blockage of intestine or stomach.

Other remarks


Cholestyramine may interfere in the absorption of fat soluble vitamins such as vitamins A
Vitamin A

Vitamin A, a bi-polar molecule formed with bi-polar covalent bonds between carbon and hydrogen, is linked to a family of similarly shaped molecules, the retinoids, which complete the remainder of the vitamin sequence....
, D
Vitamin D

Vitamin D is a group of fat-soluble prohormones, the two major forms of which are vitamin D2 and vitamin D3 . The term vitamin D also refers to metabolites and other analogues of these substances....
, E
Vitamin E

Vitamin E is the collective name for a set of 8 related a-, ?-, ?-, and d-tocopherols and the corresponding four tocotrienols, which are fat-soluble vitamins with antioxidant properties....
, and K
Vitamin K

Vitamin K denotes a group of lipophilic, hydrophobic vitamins that are needed for the posttranslational modification of certain proteins, mostly required for blood coagulation....
. There are no special considerations regarding alcohol consumption.