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cholestyramine (Prevalite, Questran, Questran Light, LoCholest)

 

Classes: Bile Acid Sequestrants

Dosing and uses of Prevalite, Questran (cholestyramine)

 

Adult dosage forms and strengths

powder for oral suspension

  • 4g resin/5g powder
  • 4g resin/5.5g powder
  • 4g resin/5.7g powder
  • 4g resin/6.4g powder
  • 4g resin/9g powder

 

Hyperlipidemia

4 g PO q12-24hr; not to exceed 24 g/day (4 g q4hr)

Overdose: Symptoms include gastrointestinal (GI) obstruction; treatment is supportive

 

Dosing Modifications

Renal impairment: Supplemental doses not necessary with peritoneal dialysis (PD) or hemodialysis (HD)

 

Administration

Always mix with fluids or food

Take before or with meals

 

Pediatric dosage forms and strengths

powder for oral suspension

  • 4g resin/5g powder
  • 4g resin/5.5g powder
  • 4g resin/5.7g powder
  • 4g resin/6.4g powder
  • 4g resin/9g powder

 

Hyperlipidemia

240 mg/kg/day PO divided q8-12hr; generally not to exceed 8 g/day

 

Prevalite, Questran (cholestyramine) adverse (side) effects

Frequency not defined

Belching

Constipation

Dental erosion

Diarrhea

Duodenal ulcer bleeding

Flatulence

Gallstones

Heartburn

Hypoprothrombinemia

Malabsorption of fat-soluble vitamins

Nausea and vomiting

Pancreatitis

Perianal irritation

Rectal pain

Steatorrhea

Stomach pain

Weight gain or loss

 

Warnings

Contraindications

Hypersensitivity to bile-sequestering resins

Complete biliary obstruction

 

Cautions

Use with caution in renal impairment

Volume depletion

Concomitant spironolactone therapy

Secondary causes of hyperlipidemia must be ruled out before therapy is initiated

Not to be used as monotherapy in hypertriglyceridemia

With prolonged use, increased risk of bleeding because of hypoprothrombinemia from vitamin K deficiency

May interfere with fat absorption and decrease absorption of fat-soluble vitamins (A, D, E, K)

May exacerbate preexisting constipation (initiate therapy at lower dosage in patients with history of constipation)

Special care must be taken to avoid constipation in patients with symptomatic coronary heart disease

Always mix with water or fluids; never ingest dry powder

Some formulations contain phenylalanine

Because of large quantities of chloride ion released from resin (which may lead to hyperchloremic acidosis and increase urinary calcium excretion on prolonged use), it may be advisable to reduce chloride intake

Take other drugs at least 1 hour before or 4-6 hours after taking cholestyramine to minimize possible interference with absorption

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Drug does not enter breast milk; use with caution because of potential vitamin loss in mother

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Prevalite, Questran (cholestyramine)

Mechanism of action

Forms complex with bile acids that is not absorbed through intestine; inhibits enterohepatic reuptake of intestinal bile salts, and this, in turn, increases fecal loss of bile salt-bound LDL and consequently reduces serum cholesterol in patients with primary hypercholesterolemia

 

Absorption

Not absorbed

Peak effect: 21 days

 

Metabolism

Not metabolized

 

Elimination

Excretion: Feces (insoluble complex with bile acids)