At a glance
Cholestyramine is a bile acid binding agent used to lower cholesterol, treat bile acid-induced diarrhea, and relieve pruritus associated with partial biliary obstruction.
Indications
- Primary hypercholesterolemia (elevated LDL cholesterol)
- Combined hypercholesterolemia and hypertriglyceridemia
- Bile acid-induced diarrhea (short bowel syndrome)
- Pruritus associated with partial biliary obstruction
Pharmacology
Cholestyramine is an ion-exchange resin that binds with bile acids to form an insoluble complex which is excreted in the feces, resulting in increased loss of bile acid, thus increasing the oxidation of cholesterol to bile acids. It interferes with the enterohepatic circulation of bile acids and lowers cholesterol levels.
Dosage
Adult Dose:
| Indication | Dose | Schedule |
|---|---|---|
| Hyperlipidemia | 12-24 g/day | Single dose or up to 4 divided doses |
| Bile acid-induced diarrhea | 12-24 g/day | Single dose or up to 4 divided doses |
| Pruritus with partial biliary obstruction/primary biliary cirrhosis | 4-8 g/day | — |
Pediatric Dose (>6 years): 240 mg/kg/day in divided doses.
Side effects
Common Side Effects:
- Constipation (most common)
- Abdominal discomfort
- Flatulence
- Nausea
- Vomiting
- Diarrhea
- Heartburn
- Anorexia
- Dyspepsia
- Steatorrhea
Rare Side Effects: Hypoprothrombinemia (Vitamin K deficiency), Vitamin A & D deficiencies, hyperchloremic acidosis (children), osteoporosis, rash, skin irritation.
Use in pregnancy
[CONSULT YOUR DOCTOR] Cholestyramine may be unsafe to use during pregnancy. Although cholestyramine is not systemically absorbed, interference with fat-soluble vitamin absorption may be detrimental. Pregnancy Category C.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Precautions & warnings
- [SAFE] Cholestyramine does not usually affect your ability to drive.
- Always take it with food and a full glass of water.
- It may interfere with the absorption of vitamins A, D and K. Take supplements as suggested by your doctor.
- Any other medicine should be taken 1 hour before or 4 hours after taking cholestyramine.
- Constipation is usually mild and transient; reduce dosage temporarily if needed.
Overdose effects
Cholestyramine overdose may cause gastrointestinal obstruction. Treatment should be symptomatic.
Storage conditions
Store at room temperature between 15°C and 30°C. Protect from moisture. Keep out of the reach of children.