Cholybar
Cholybar - General Information
Cholybar or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholybar resin is quite hydrophilic, but insoluble in water.
Pharmacology of Cholybar
Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Cholybar resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption.
Cholybar for patients
Inform your physician if you are pregnant or plan to become pregnant or are breast-feeding. Drink plenty of fluids and mix each 9 gram dose of Cholestyramine for Oral Suspension 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.
Cholybar Interactions
Cholestyramine resin may delay or reduce the absorption of concomitant oral medication such as phenylbutazone, warfarin, thiazide diuretics (acidic) or propranolol (basic), as well as tetracycline penicillin G, phenobarbital, thyroid and thyroxine preparations, estrogens and progestins, and digitalis. Interference with the absorption of oral phosphate supplements has been observed with another positively-charged bile acid sequestrant. Cholestyramine resin may interfere with the pharmacokinetics of drugs that undergo enterohepatic circulation, The discontinuance of cholestyramine resin could pose a hazard to health if a potentially toxic drug such as digitalis has been filtrated to a maintenance level while the patient was taking cholestyramine resin.
Because cholestyramine binds bile acids, cholestyramine resin may interfere with normal fat digestion and absorption and thus may prevent absorption of fat soluble vitamins such as A, D, E, and K. When cholestyramine resin is given for long periods of time, concomitant supplementation with water-miscible (or parenteral) forms of fat-soluble vitamins should be considered.
SINCE CHOLESTYRAMINE RESIN MAY BIND OTHER DRUGS GIVEN CONCURRENTLY, IT IS RECOMMENDED THAT PATIENTS TAKE OTHER DRUGS AT LEAST 1 HOUR BEFORE OR 4 TO 6 HOURS AFTER CHOLESTYRAMINE RESIN (OR AT AS GREAT AN INTERVAL AS POSSIBLE) TO AVOID IMPEDING THEIR ABSORPTION.
Cholybar Contraindications
Cholestyramine for Oral Suspension, USP powder is contraindicated in patients with complete biliary obstruction where bile is not secreted into the intestine and in those individuals who have shown hypersensitivity to any of its components.
Additional information about Cholybar
Cholybar Indication: Indicated 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. Also for the relief of pruritus associated with partial biliary obstruction.
Mechanism Of Action: Cholybar 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.
Drug Interactions: Methotrexate Decreased levels of methotrexate
Anisindione The gastro-intestinal binding agent decreases the anticoagulant effect
Dicumarol The gastro-intestinal binding agent decreases the anticoagulant effect
Acenocoumarol The gastro-intestinal binding agent decreases the anticoagulant effect
Warfarin The gastro-intestinal binding agent decreases the anticoagulant effect
Digoxin The resin decreases the effect of digoxin
Ezetimibe Decreases the levels of ezetimibe
Fluvastatin Increased/decreased effect according to spacing
Hydrocortisone Decreases the effect of hydrocortisone
Levothyroxine The resin decreases the absorption of thyroid hormones
Liothyronine The resin decreases the absorption of thyroid hormones
Raloxifene The resin decreases the effect of raloxifene
Spironolactone Increased risk of acidosis and hyperkaliemia
Troglitazone Decreases the effect of troglitazone
Liotrix The resin decreases the absorption of thyroid hormones
Thyroglobulin (Tg) The resin decreases the absorption of thyroid hormones
Ursodeoxycholic acid The resin decreases the effect of ursodiol
Acenocoumarol The gastro-intestinal binding agent decreases the anticoagulant effect
Food Interactions: Take with food, do not mix with soft drinks.
Generic Name: Cholestyramine
Synonyms: Colestyramine
Drug Category: Cholesterol Absorption Inhibitors; Anticholesteremic Agents; Antihyperlipidemics
Drug Type: Small Molecule; Approved
Other Brand Names containing Cholestyramine: Questran; Questran Light; Cholybar; Locholest; Locholest light; Novo-Cholamine; Novo-Cholamine Light; PMS Cholestyramine; Prevalite;
Absorption: Not absorbed from the gastrointestinal tract following oral administration.
Toxicity (Overdose): Overdose may result in blockage of intestine or stomach.
Protein Binding: Not Available
Biotransformation: Bile acids
Half Life: 6 minutes
Dosage Forms of Cholybar: Powder, for solution Oral
Powder Oral
Powder, for suspension Oral
Chemical IUPAC Name: Not Available
Chemical Formula: Not Available
Cholestyramine on Wikipedia: https://en.wikipedia.org/wiki/Cholestyramine
Organisms Affected: Humans and other mammals
