Yes

Antilipemic Agent (Bile Acid Seqestrant)

Adjunct in the management of primary hypercholesterolemia; pruritus associated with elevated levels of bile acids; diarrhea associated with excess fecal bile acids; binding toxicologic agents; pseudomembraneous colitis

C

Hypersensitivity of bile acid sequestering resins or any component of the products; complete biliary obstruction; bowel obstruction

Not to be taken simultaneously with many other medicines (decreased absorption). Treat any diseases contributing to hypercholesterolemia first. May interfere with fat-soluble vitamins (A, D, E, K) and folic acid. Chronic use may be associated with bleeding problems (especially in high doses). May produce or exacerbate constipation problems. Fecal impaction may occur. Hemorrhoids may be worsened.

>10%: Gastrointestinal: Constipation, heartburn, nausea, vomiting, stomach pain

1% to 10%:

Central nervous system: Headache

Gastrointestinal: Belching, bloating, diarrhea

<1% (Limited to important or life-threatening symptoms): Hyperchloremic acidosis, gallstones or pancreatitis, GI bleeding, peptic ulcer, steatorrhea or malabsorption syndrome, hypoprothrombinemia (secondary to vitamin K deficiency)

Symptoms of overdose include GI obstruction

Treatment is supportive

Cholestyramine can reduce the absorption of numerous medications when used concurrently. Give other medications 1 hour before or 4 hours after giving cholestyramine. Medications which may be affected include HMG-CoA reductase inhibitors, thiazide diuretics, propranolol (and potentially other beta-blockers), corticosteroids, thyroid hormones, digoxin, valproic acid, NSAIDs, loop diuretics, sulfonylureas, troglitazone (and potentially other agents in this class).

Warfarin and other oral anticoagulants: Hypoprothrombinemic effects may be reduced by cholestyramine. Separate administration times (as detailed above) and monitor INR closely when initiating or discontinuing.

Suspension may be used for up to 48 hours after refrigeration

Forms a nonabsorbable complex with bile acids in the intestine, releasing chloride ions in the process; inhibits enterohepatic reuptake of intestinal bile salts and thereby increases the fecal loss of bile salt-bound low density lipoprotein cholesterol

Peak effect: 21 days

Absorption: Not absorbed from the GI tract

Elimination: In feces as an insoluble complex with bile acids

Oral (dosages are expressed in terms of anhydrous resin):

Children: 240 mg/kg/day in 3 divided doses; need to titrate dose depending on indication

Adults: 4 g 1-2 times/day to a maximum of 24 g/day and 6 doses/day

Tablet: Adults: Initial: 4 g once or twice daily; maintenance: 8-16 g/day in 2 divided doses

Dialysis: Not removed by hemo- or peritoneal dialysis; supplemental doses not necessary with dialysis or continuous arteriovenous or venovenous hemofiltration effects

Cholestyramine (especially high doses or long-term therapy) may decrease the absorption of fat-soluble vitamins (vitamins A, D, E and K), folic acid, calcium, and iron; deficiencies may occur including hypoprothrombinemia and increased bleeding from vitamin K deficiency; supplementation of vitamins A, D, E, and K, folic acid, and iron may be required with high-dose, long-term therapy

prothrombin time; cholesterol (S), iron (B)

Cholestyramine alone or when combined with a statin is effective in lowering cholesterol. Cholestyramine may increase triglycerides, therefore, it should be avoided in patients with triglyceride levels greater than or equal to 200 mg/dL. Potential factors that may limit patient compliance include GI side effects and the need to space other medications at least 1 hour before or 4 hours after cholestyramine administration.

None reported

May decrease the absorption of psychotropics including TCAs, beta-blockers, valproic acid, barbiturates

No information available to require special precautions

No effects or complications reported

Take once or twice a day as directed. Do not take the powder in its dry form; mix with fluid, applesauce, pudding, or jello. Chew bars thoroughly. Take other medications 2 hours before or 4 hours after cholestyramine. Ongoing medical follow-up and laboratory tests may be required. You may experience GI effects (these should resolve after continued use); nausea and vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); constipation (increased exercise, dietary fluid, fiber, or fruit may help - consult prescriber about use of stool softener or laxative). Report unusual stomach cramping, pain or blood in stool; unresolved nausea, vomiting, or constipation. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Administer warfarin and other drugs at least 1-2 hours prior to, or 6 hours after cholestyramine because cholestyramine may bind to them, decreasing their total absorption. ( Note: Cholestyramine itself may cause hypoprothrombinemia in patients with impaired enterohepatic circulation.)

Powder: 4 g of resin/9 g of powder (9 g, 378 g)

Powder, for oral suspension, with aspartame: 4 g of resin/5 g of powder (5 g, 210 g)

Powder, for oral suspension, with phenylalanine: 4 g of resin/5.5 g of powder (60s)

Al-Mahasneh QM, Rodgers GC, and Tutinji MF, "Anion Exchange Resin "Cholestyramine" Adsorption Capabilities for Arsenic Trioxide. An In Vivo Study," Clin Toxicol, 1995, 33(5):539.

Cohn WJ, Boylan JJ, Blanke RV, et al, "Treatment of Chlordecone (Kepone) Toxicity With Cholestyramine," N Engl J Med, 1978, 298(5):243-8.

Leaf DA, "Lipid Disorders: Applying New Guidelines to Your Older Patients," Geriatrics, 1994, 49(5):35-41.

Pieroni RE and Fisher JG, "Use of Cholestyramine Resin in Digitoxin Toxicity," JAMA, 1981, 245(19):1939-40.