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14-September-2008 10:43:22 - Cholestyramine Cholestyramine Systematic IUPAC name ? Identifiers CAS number 11041-12-6 ATC code C10AC01 PubChem ? Chemical data Formula ? Mol. mass Average MW exceeds 106 Daltons Pharmacokinetic data Bioavailability ? Metabolism bile acids Half life .1 hr Excretion feces Therapeutic considerations Pregnancy cat. CUS Legal status Routes gastrointestinal Cholestyramine or colestyramine Questran, Questran Light, Cholybar is a bile acid sequestrant, which binds bile in the gastrointestinal tract 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, but can also be used to treat the pruritus, or itching, that often occurs during liver failure 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. Contents 1 Available forms 2 Dosage 3 Side-effects 4 Warnings 5 Drug interactions 6 Duration of treatment 7 Overdose 8 Other remarks 9 References Available forms Cholestyramine is available as powder form, in 4 gram packets, or in larger canisters. In the United States, it can be purchased either as a generic medicine, or as Questran or Questran Light Bristol-Myers Squibb. Dosage 4 to 8 grams once or twice daily, maximum dose 24 grams a day. Side-effects The following side effects have been noted.1 Most frequent: Constipation 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, diabetes, nephrotic syndrome, dysproteinemia, obstructive liver disease, kidney disease, or alcoholism should consult their doctor before taking this medication.2 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 should consult with a physician before taking Questran Light because that product contains phenylalanine. Drug interactions The following interactions have been noted.3 Digitalis Estrogens and progestins Oral diabetes drugs Penicillin G Phenobarbital Spironolactone Tetracycline Thiazide-type diuretic pills Thyroid medication Warfarin Arava 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, D, E, and K. There are no special considerations regarding alcohol consumption. 4 References The Merck Index, 12th ion. 2257 v d e Lipid modifying agents C10 Statins HMG-CoA reductase Atorvastatin Cerivastatin‡ Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin Fibrates PPAR Clofibrate‡ Bezafibrate Aluminium clofibrate Gemfibrozil Fenofibrate Simfibrate Ronifibrate Ciprofibrate Etofibrate Clofibride Clinofibrate Bile acid sequestrants Colestyramine Colestipol Colestilan Colextran Colesevelam Niacin and derivatives Niceritrol Niacin Nicofuranose Aluminium nicotinate Nicotinyl alcohol Acipimox CETP inhibitors Anacetrapib† Torcetrapib§ Combinations Niacin/lovastatin Niacin/simvastatin Ezetimibe/simvastatin Other Dextrothyroxine Probucol Tiadenol Benfluorex Meglutol Omega-3-triglycerides Magnesium pyridoxal 5-phosphate glutamate Policosanol Ezetimibe Lapaquistat§ †Undergoing clinical trials. ‡Withdrawn from market. §Development terminated. Retrieved from http://en..org/wiki/Cholestyramine Categories: Hypolipidemic agents | Hepatology Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Polski This page was last modified on 17 July 2008, at 04:0
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