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Cholestyramine resin
Cholestyramine resin (Questran)
Cholestyramine resin
(koh-less-TEER-ah-meen) Alti-Cholestyramine Light LoCholest Novo-Cholaine Light PMS-Cholestyramine Prevalite Questran Questran Light (Rx)

Classification: Hypocholesterolemic agent, bile acid sequestrant

Action/Kinetics: Binds sodium cholate (bile salts) in the intestine; thus, the principal precursor of cholesterol is not absorbed due to formation of an insoluble complex, which is excreted in the feces. Decreases cholesterol and LDL and either has no effect or increases triglycerides, VLDL, and HDL. Also, itching is relieved as a result of removing irritating bile salts. The antidiarrheal effect results from the binding and removal of bile acids. Onset, to reduce plasma cholesterol: Within 24-48 hr, but levels may continue to fall for 1 yr; to relieve pruritus: 1-3 weeks; relief of diarrhea associated with bile acids: 24 hr. Cholesterol levels return to pretreatment levels 2-4 weeks after discontinuance. Fat-soluble vitamins (A, D, K) and possibly folic acid may have to be administered IM during long-term therapy because cholestyramine binds these vitamins in the intestine.

Uses: Adjunct to reduce elevated serum cholesterol in primary hypercholesterolemia in those who do not respond adequately to diet. Pruritus associated with partial biliary obstruction. Diarrhea due to bile acids. Investigational: Antibiotic-induced pseudomembranous colitis (i.e., due to toxin produced by Clostridium difficile), digitalis toxicity, treatment of chlordecone (Kepone) poisoning, treatment of thyroid hormone overdose.

Contraindications: Complete obstruction or atresia of bile duct.

Special Concerns: Use during pregnancy only if benefits outweigh risks. Use with caution during lactation and in children. Long-term effects and efficacy in decreasing cholesterol levels in pediatric clients are not known. Geriatric clients may be more likely to manifest GI side effects as well as adverse nutritional effects. Exercise caution in phenylketonurics as Prevalite contains 14.1 mg phenylalanine per 5.5-g dose.

Side Effects: GI: Constipation (may be severe), N&V;, diarrhea, heartburn, GI bleeding, anorexia, flatulence, belching, abdominal distention, abdominal pain or cramping, loose stools, indigestion, aggravation of hemorrhoids, rectal bleeding or pain, black stools, bleeding duodenal ulcer, peptic ulceration, GI irritation, dysphagia, dental bleeding, hiccoughs, sour taste, pancreatitis, diverticulitis, cholescystitis, cholelithiasis. Fecal impaction in elderly clients. Large doses may cause steatorrhea. CNS: Migraine or sinus headaches, dizziness, anxiety, vertigo, insomnia, fatigue, lightheadedness, syncope, drowsiness, femoral nerve pain, paresthesia. Hypersensitivity: Urticaria, dermatitis, asthma, wheezing, rash. Hematologic: Increased PT, ecchymosis, anemia. Musculoskeletal: Muscle or joint pain, backache, arthritis, osteoporosis. GU: Hematuria, dysuria, burnt odor to urine, diuresis. Other: Bleeding tendencies (due to hypoprothrombinemia). Deficiencies of vitamins A and D. Uveitis, weight loss or gain, osteoporosis, swollen glands, increased libido, weakness, SOB, edema, swelling of hands/feet; hyperchloremic acidosis in children, rash and irritation of the skin, tongue, and perianal area.

Laboratory Test Alterations: Liver function abnormalities.

Overdose Management: Symptoms: GI tract obstruction.

Drug Interactions: Anticoagulants, PO / Anticoagulant effect R/T GI tract absorption Aspirin / Aspirin absorption from GI tract Clindamycin / Clindamycin absorption from GI tract Clofibrate / Clofibrate absorption from GI tract Digitalis glycosides / Digitalis effect R/T GI tract absorption Furosemide / Furosemide absorption from GI tract Gemfibrozil / Gemfibrozil bioavailability Glipizide / Serum glipizide levels Hydrocortisone / Hydrocortisone effect R/T GI tract absorption Imipramine / Imipramine absorption from GI tract Iopanoic acid / Results in abnormal cholecystography Lovastatin / Effects may be additive Methyldopa / Methyldopa absorption from GI tract Nicotinic acid / Nicotinic acid absorption from GI tract Penicillin G / Penicillin G effect R/T GI tract absorption Phenytoin / Phenytoin absorption from GI tract Phosphate supplements / Phosphate absorption from GI tract Piroxicam / Elimination Propranolol / Propranolol effect R/T GI tract absorption Tetracyclines / Tetracycline effects R/T GI tract absorption Thiazide diuretics / Thiazide effects R/T GI tract absorption Thyroid hormones / Thyroid effects R/T GI tract absorption Tolbutamide / Tolbutamide absorption from GI tract Troglitazone / Troglitazone absorption from the GI tract Ursodiol / Ursodiol effects R/T GI tract absorption Vitamins A, D, E, K / Malabsorption of fat-soluble vitamins
NOTE: These drug interactions may also be observed with colestipol.

How Supplied: Powder for Reconstitution: 4 g/5 g, 4 g/5.5 g, 4 g/5.7 g, 4 g/9 g

Dosage
•Powder
Adults, initial: 1 g 1-2 times/day. Dose is individualized. For Prevalite, give 1 packet or 1 level scoopful (5.5 g Prevalite: 4 g anhydrous cholestyramine). Maintenance: 2-4 packets or scoopfuls/day (8-16 g anhydrous cholestyramine resin) mixed with 60-180 mL water or noncarbonated beverage. The recommended dosing schedule is b.i.d. but it can be given in one to six doses/day. Maximum daily dose: 6 packets or scoopsful (equivalent to 24 g cholestyramine).