LoCHOLEST, Questran, Questran Light, Prevalite
Classifications: antilipemic; bile acid sequestrant; Therapeutic: cholesterol-lowering agent; bile acid sequestrant
Pregnancy Category: C
4 g powder for suspension; 1 g tablet
Anion-exchange resin used for its cholesterol-lowering effect. Adsorbs and combines with intestinal bile acids in exchange
for chloride ions to form an insoluble, nonabsorbable complex that is excreted in the feces. As a result, bile salts are
continually (but not entirely) prevented from reentry into the enterohepatic circulation, thus increasing fecal loss of
bile acids. This leads to lowered serum total cholesterol by decreasing low-density lipoprotein (LDL) cholesterol.
The resin anion-exchange agent increases fecal loss of bile acids which leads to lowered serum total cholesterol by decreasing
(LDL) cholesterol, and reducing bile acid deposit in dermal tissues (decreasing pruritus). Serum triglyceride levels may
increase or remain unchanged.
As adjunct to diet therapy in management of patients with primary hypercholesterolemia (type IIa hyperlipidemia) with a
significant risk of atherosclerotic heart disease and MI; for relief of pruritus secondary to partial biliary stasis.
To control diarrhea caused by excess bile acids in colon; for hyperoxaluria.
Complete biliary obstruction or biliary cirrhosis, cholelithiasis; GI obstruction; hypersensitivity to bile acid sequestrants;
coagulopathy; pregnancy (category C), lactation. Safe use in children ≤6 y
Bleeding disorders; hemorrhoids; impaired GI function, decreased GI motility; peptic ulcer, malabsorption states (e.g.,
steatorrhea); phenylketonuria (Questran Light only); renal disease.
Route & Dosage
Adult: PO 4 g b.i.d. to q.i.d. a.c. and h.s., may need up to 24 g/d
Child: PO 240 mg/kg/d in 3 divided doses
Adult: PO 48 g b.i.d. to q.i.d. a.c. and h.s. (≤32 g/d)
Adult: PO 4 g b.i.d. to q.i.d. a.c. and h.s. (≤16 g/d)
- Place contents of one packet or one level scoopful on surface of at least 120 to 180 mL (46 oz) of water or other
preferred liquid. Permit drug to hydrate by standing without stirring 12 min, twirling glass occasionally, then stir
until suspension is uniform. Rinse glass with small amount of liquid and have patient drink remainder to ensure entire dose
is taken. Administer before meals.
- Always dissolve cholestyramine powder before administration; it is irritating to mucous membranes and may cause esophageal
impaction if administered dry.
- Store in tightly closed container at 15°30° C (59°86° F) unless otherwise specified.
Adverse Effects (≥1%)GI: Constipation,
fecal impaction, hemorrhoids, abdominal pain and distension, flatulence, bloating sensation, belching, nausea, vomiting,
heartburn, anorexia, diarrhea
, steatorrhea. Endocrine:
Increased libido. Metabolic:
Weight loss or gain, iron, calcium, vitamin A, D, and K deficiencies (from poor absorption); hypoprothrombinemia, hyperchloremic
acidosis, decreased erythrocyte folate levels. Skin:
Rash, irritations of skin, tongue, and perianal
areas. Special Senses:
Arcus juvenilis, uveitis.
Diagnostic Test Interference
Cholestyramine therapy may be accompanied by increased serum AST, phosphorus, chloride, and alkaline phosphatase levels; decreased serum calcium, sodium, and potassium levels.
Decreases the absorption of oral anticoagulants
, digoxin, tetracyclines
, penicillins, phenobarbital, thyroid hormones
, thiazide diuretics
, iron salts
, fat-soluble vitamins
(A, D, E, K) from the GI tractadminister cholestyramine 4 h before or 2 h after these drugs. Can bind to and affect
absorption of any drug.
Not absorbed from GI tract. Elimination:
Excreted in feces as insoluble complex.
Assessment & Drug Effects
- Monitor therapeutic effect. Serum cholesterol levels are reduced within 2448 h after treatment starts and may continue
to decline for a year. After withdrawal of cholestyramine, cholesterol levels usually return to baseline level in about 2
to 4 wk.
- Be alert to early symptoms of hypoprothrombinemia (petechiae, ecchymoses, abnormal bleeding from mucous membranes, tarry
stools) and report their occurrence promptly. Long-term use of cholestyramine resin can increase bleeding tendency.
- Preexisting constipation may be worsened in the older adult, women, and in those taking >24 g/d.
- Consult physician regarding supplemental vitamins A and D and folic acid that may be required by patient on long-term therapy.
- Lab tests: Periodic CBC, platelet count, serum electrolytes, and lipid profile.
Patient & Family Education
- Report constipation immediately to physician. High-bulk diet with adequate fluid intake is an essential adjunct to cholestyramine
treatment and generally resolves the problems of constipation and bloating sensation.
- Do not omit doses. Sudden withdrawal can promote uninhibited absorption of other drugs taken concomitantly, leading to toxicity
- GI adverse effects usually subside after the first month of drug therapy.
- The following symptoms may be drug-induced and should be reported promptly: severe gastric distress with nausea and vomiting,
unusual weight loss, black stools, severe hemorrhoids (GI bleeding), sudden back pain.