Generic
Cholestyramine
1 brands available in the market
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.
Description
Cholestyramine is used to lower cholesterol and to reduce the risk of heart disease. Cholesterol is a fatty substance that builds up in your blood vessels and causes narrowing, which may lead to a heart attack or stroke. Cholestyramine may also be used to treat itching seen in certain types of liver disease and to relieve some types of diarrhea. This medicine may be used alone or in combination with other medicines. It may be taken with a meal or on an empty stomach. You can take it at any time of day but try to take it at the same time each day. Most people with high cholesterol do not feel ill, but if you stop taking this medicine, your condition could get worse. This may lead to your cholesterol levels creeping up again and increase your risk of heart disease and stroke. It is important to have your cholesterol levels checked regularly. This medicine is only one part of a treatment program which should also include a healthy diet, regular exercise, smoking cessation, moderation of alcohol intake and weight reduction.
Cholestyramine is a bile acid binding agent. It removes bile acids from the body. The liver then produce more bile acids using cholesterol, as a result, the levels of cholesterol in the body is lowered.
Indications
- Primary hypercholesterolemia (elevated LDL cholesterol)
- Combined hypercholesterolemia and hypertriglyceridemia
- Bile acid-induced diarrhea (short bowel syndrome)
- Pruritus associated with partial biliary obstruction
Therapeutic class
Bile acid sequestrants
Pharmacological class
Bile Acid Binding Agent (Ion-Exchange Resin)
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.
Mechanism of action
Cholestyramine 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.
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.
Administration
Take this medicine in the dose and duration as advised by your doctor. Check the label for directions before use. Empty the granules in a glass of water/milk, stir it and consume immediately. Cholestyramine may be taken with or without food, but it is better to take it at a fixed time.
Missed dose
If you miss a dose of Cholestyramine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.
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.
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.
Contraindications
- Complete biliary obstruction
- Hypersensitivity
Drug interactions
Delayed or reduced absorption of folic acid, thiazide diuretics, propranolol, digoxin and related glycosides, loperamide, phenylbutazone, barbiturates, oestrogens, progestogens, thyroid hormones, warfarin and other coumarin-derivative anticoagulants, iron salts, deferasirox, tetracycline, penicillin G. May prevent absorption of fat-soluble vitamins.
Food interactions
[CAUTION] Caution is advised when consuming alcohol with Cholestyramine. Please consult your doctor.
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.
Use in lactation
[SAFE IF PRESCRIBED] Cholestyramine is probably safe to use during breastfeeding. Limited human data suggests that the drug does not represent any significant risk to the baby. However, consider the potential for interference with vitamin absorption.
Pediatric use
Pediatric dose (>6 years): 240 mg/kg/day in divided doses. A pediatric dosage schedule has not been fully established.
Geriatric use
Elderly patients (>60 years) may be more likely to experience gastrointestinal side effects.
Renal / hepatic impairment
[SAFE IF PRESCRIBED] Cholestyramine is safe to use in patients with kidney disease. No dose adjustment is recommended. However, talk to your doctor if you have any underlying kidney disease.
[CONSULT YOUR DOCTOR] There is limited information available on the use of Cholestyramine in patients with liver disease. Please consult your doctor.
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.
Chemical structure
Cholestyramine Resin