Cholestyramine

385.66878

331.206665

234-270-8

White to buff-colored, fine powder

3914002000

1

Insoluble in water, in methylene chloride and in ethanol (96 per cent).Hygroscopic [Merck.]

Commercially available cholestyramine resin powder should be stored in tight containers at a temperature less than 40 °C, preferably at 15-30 °C.

Odorless or not more than a slight amine-like odor

Hygroscopic

NONH for all modes of transport

2

22-24/25

FZ9310000

Xi

SRP: The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl cholestyramine resin, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Cholestyramine/

Cholestyramine was among the many drugs tested for to establish the nature and amount of pharmacologically active substances which come into landfills as a result of throwing away old drugs(1).

There is little evidence that cholestyramine causes significant liver injury. However, mild elevations in serum aminotransferase levels occur in a proportion of patients on cholestyramine. The elevations have been mild, transient and without accompanying symptoms or jaundice. In one prospective study, cholestyramine therapy was associated with serum ALT elevations above 3 times the upper limit of normal in 11% of subjects. In all cases, the abnormalities were asymptomatic and resolved rapidly upon stopping cholestyramine. Serum alkaline phosphatase levels are usually normal. A single case report of marked serum aminotransferase elevations on bile acid sequestrant therapy with rapid resolution on stopping has been published. However, there have been no reports of clinically apparent liver injury with jaundice attributed to cholestyramine or the other bile acid sequestrants. Cholestyramine is used in patients with liver disease to treat pruritus, and has little or no effect on serum enzyme or bilirubin levels.

Concurrent use /of oral thiazide diuretics, oral penicillin G, phenylbutazone, oral propranolol, oral tetracyclines/ with cholestyramine may result in binding of these medications, thus decreasing their absorption; an interval of several hours between administration of cholestyramine and any of these medications is recommended.|Cholestyramine may reduce the half-life of these medications /digitalis glycosides, especially digitoxin/ by decreasing intestinal reabsorption and enterohepatic circulation; caution is recommended, especially when cholestyramine is withdrawn from a patient who was stabilized on the digitalis glycoside while receiving cholestyramine, because of the potential for serious toxicity; some clinicians recommend administration of cholestyramine approximately 8 hours after the digitalis glycoside.|Effect may be decreased when chenodiol or ursodiol is used concurrently with cholestyramine, which binds these medications and decrease their absorption and also tends to increase cholesterol saturation of bile.|Concurrent use may significantly increase the anticoagulant effects as a result of depletion of vitamin K, but cholestyramine may also bind with oral anticoagulants in the gastrointestinal tract and reduce their effects; administration at least 6 hours before cholestyramine and adjustment of anticoagulant dosage based on frequent prothrombin-time determinations are recommended.|For more Interactions (Complete) data for CHOLESTYRAMINE RESIN (8 total), please visit the HSDB record page.

Cholestyramine is a nonabsorbed bile acid sequestrant that is used a therapy of hyperlipidemia and for the pruritus of chronic liver disease and biliary obstruction. 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.

Antilipemic Agents

Ion exchange resin (bile salts); antihyperlipoproteinemic|Cholestyramine is indicated for use in patients with primary hypercholesterolemia (type IIa hyperlipidemia) and a significant risk of coronary artery disease who have not responded to diet and other measures alone. Cholestyramine reduces plasma total cholesterol and low density lipoprotein (LDL) concentrations, but causes no change or a slight increase in serum triglyceride concentrations, and so is not useful in patients with elevated triglyceride concentrations alone. Its use is limited in other types of hyperlipidemia (including type IIb) because it may cause further elevation of triglycerides. /Included in US product labeling/|Cholestyramine is indicated to reduce the risks of atherosclerotic heart disease and myocardial infarctions. /Included in US product labeling/|Cholestyramine is indicated for the relief of pruritus associated with partial biliary obstruction (including primary biliary cirrhosis and various other forms of bile stasis). It is not useful in patients with complete biliary obstruction or the pruritus due to other causes. /Included in US product labeling/|For more Therapeutic Uses (Complete) data for CHOLESTYRAMINE RESIN (8 total), please visit the HSDB record page.

The most common adverse effects of cholestyramine involved the GI tract, especially after high doses (more than 24 g daily) and in patients older than 60 years of age. The most frequent adverse effect of cholestyramine resin is constipation, which occurs in about 20% of patients receiving the drug; cholestyramine resin may also increase the severity of preexisting constipation. Fecal impaction and/or hemorrhoids with or without bleeding have been reported rarely in association with constipation, most often when high dose of cholestyramine have been used in children and in the elderly.|Other less common adverse GI effects of cholestyramine are abdominal pain and distention, bloating, flatulence, nausea, vomiting, diarrhea, anorexia, dyspepsia, heartburn, biliary colic, and indigestion. Bloating and flatulence often disappear with continued therapy. Other reported adverse Gi effects include dysphagia, hiccups, ulcer attack, rectal bleeding, black stools, sour taste, pancreatitis, bleeding from know duodenal ulcer, rectal pain, and diverticulitis; however, a direct relationship of these effects to drug therapy has not been established.|Large quantities of chloride, which are liberated from cholestyramine resin, may be absorbed in place of intestinal bicarbonate and can lead to hyperchloremic acidosis and increased urinary calcium excretion. This effect is prevalent mainly with high dose of usual dose in small patients or children and may be partially offset by decreasing chloride intake.|Adverse dermatologic effects of cholestyramine have included rash and irritation of the skin, tongue, and perianal area.|For more Drug Warnings (Complete) data for CHOLESTYRAMINE RESIN (14 total), please visit the HSDB record page.

High-molecular-weight insoluble polymers that contain functional cationic groups capable of undergoing exchange reactions with anions. (See all compounds classified as Anion Exchange Resins.)|Substances used to lower plasma cholesterol levels. (See all compounds classified as Anticholesteremic Agents.)

Previous studies performed on excised gastric tissue and in healthy volunteers revealed that the ion exchange resin, cholestyramine, exhibits mucoadherent behaviour. This study was designed to elucidate whether surface charge affected this behaviour. Gamma scintigraphy was performed on fasted normal subjects following oral administration of cholestyramine or the cationic exchanger Amberlite(R) IRP-69, either uncoated or polymer-coated to mask their charge. Subjects were fed after 4 h. The initial gastric emptying of all formulations was similar (T(50) values (mean+/-S.E.M.): cholestyramine=85.86+/-9.16 min; IRP-69=76.09+/-9.23 min; polymer-coated cholestyramine=72.0+/-12.64 min; polymer-coated IRP-69=70.25+/-10.57 min: P=0.724). However, after 3 h the emptying pattern of cholestyramine was slower than that of IRP-69. This resulted in greater retention times than IRP-69 (AUC(0-6) values (relative units)=15,200+/-1093 versus 9452+/-811; cholestyramine versus IRP-69: P=0.0004). This effect was reduced by polymer-coating the cholestyramine. Serial images showed that cholestyramine was trapped in the oropharyngeal region and subsequently displaced by the meal, resulting in higher levels of activity remaining at 6 h. Thus, cholestyramine exhibited prolonged gastric residence via mucoadhesion and was distributed throughout the stomach. The surface charge of the resin was found to have a contributory role. These materials may have potential for the delivery of drugs in the topical treatment of the gastric mucosa, for example in the eradication of Helicobacter pylori.|Not absorbed from the gastrointestinal tract.

Cholestyramine binds with bile acids in the intestine, preventing their reabsorption and producing an insoluble complex, which is excreted in the feces.

Cholestyramine

Oral: For suspension: 4 g (of dried cholestyramine resin) per 9 g Cholestyramine (Eon, Sandoz, Major, Teva), Locholest (Warner Chilcott), Questran (with propylene glycol alginate) (Par); 4 g (of dried cholestyramine resin) per 5 g Cholestyramine Light (Eon, Sandoz, Major, Teva) Locholest Light (Warner Chilcott) Questran Light (With aspartame) (Par).

Analyte: cholestyramine resin; matrix: chemical identification; procedure: infrared absorption spectrophotometry with comparison to standards|Analyte: cholestyramine resin; matrix: chemical purity (exchange capacity); procedure: liquid chromatography with detection at 214 nm and comparison to standards|Analyte: cholestyramine resin; matrix: pharmaceutical preparation (oral suspension); procedure: infrared absorption spectrophotometry with comparison to standards (chemical identification)|Analyte: cholestyramine resin; matrix: pharmaceutical preparation (oral suspension); procedure: liquid chromatography with detection at 214 nm and comparison to standards (chemical purity (exchange capacity))