Formulary
Colestyramine: Indications, Dosing, Side Effects and Interactions
For all bile acid sequestrants Bile acid sequestrants act by binding bile acids, preventing their reabsorption; this promotes hepatic conversion of...
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Colestyramine: Indications, Dosing, Side Effects and Interactions
For all bile acid sequestrants Bile acid sequestrants act by binding bile acids, preventing their reabsorption; this promotes hepatic conversion of...
Drug action
For all bile acid sequestrants Bile acid sequestrants act by binding bile acids, preventing their reabsorption; this promotes hepatic conversion of cholesterol into bile acids; the resultant increased LDL-receptor activity of liver cells increases the clearance of LDL-cholesterol from the plasma.
Indications and dose
**Hyperlipidaemias, particularly type IIa, in patients who have not responded adequately to diet and other appropriate measures,Primary prevention of coronary heart disease in men aged 35-59 years with primary hypercholesterolaemia who have not responded to diet and other appropriate measures**
- **Adult** (By Mouth): Initially 4 g daily, increased in steps of 4 g every week; increased to 12-24 g daily in 1-4 divided doses, adjusted according to response; maximum 36 g per day.
**Pruritus associated with partial biliary obstruction and primary biliary cirrhosis**
- **Adult** (By Mouth): 4-8 g once daily.
**Diarrhoea associated with Crohn's disease, ileal resection, vagotomy, diabetic vagal neuropathy, and radiation**
- **Adult** (By Mouth): Initially 4 g daily, increased in steps of 4 g every week; increased to 12-24 g daily in 1-4 divided doses, adjusted according to response, if no response within 3 days an alternative therapy should be initiated; maximum 36 g per day.
**Accelerated elimination of teriflunomide**
- **Adult** (By Mouth): 8 g 3 times a day for 11 days; reduced to 4 g 3 times a day, dose should only be reduced if not tolerated.
**Accelerated elimination of leflunomide (washout procedure)**
- **Adult** (By Mouth): 8 g 3 times a day for 11 days.
**Familial hypercholesterolaemia for colestyramine**
- **Child 6-11 years** (By mouth): Initially 4 g once daily, then increased to 4 g up to 3 times a day, adjusted according to response.
- **Child 12-17 years** (By mouth): Initially 4 g once daily, then increased in steps of 4 g every week; increased to 12-24 g daily in 1-4 divided doses, adjusted according to response; maximum 36 g per day.
**Pruritus associated with partial biliary obstruction and primary biliary cirrhosis for colestyramine**
- **Child 1-11 months** (By mouth): 1 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses; maximum 9 g per day.
- **Child 1-5 years** (By mouth): 2 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses; maximum 18 g per day.
- **Child 6-11 years** (By mouth): 4 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses; maximum 24 g per day.
- **Child 12-17 years** (By mouth): 4-8 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses; maximum 36 g per day.
**Diarrhoea associated with Crohn's disease, ileal resection, vagotomy, diabetic vagal neuropathy, and radiation for colestyramine**
- **Child 1-11 months** (By mouth): 1 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses, if no response within 3 days an alternative therapy should be initiated; maximum 9 g per day.
- **Child 1-5 years** (By mouth): 2 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses, if no response within 3 days an alternative therapy should be initiated; maximum 18 g per day.
- **Child 6-11 years** (By mouth): 4 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses, if no response within 3 days an alternative therapy should be initiated; maximum 24 g per day.
- **Child 12-17 years** (By mouth): 4-8 g once daily, adjusted according to response, total daily dose may alternatively be given in 2-4 divided doses, if no response within 3 days an alternative therapy should be initiated; maximum 36 g per day.
Cautions
For all bile acid sequestrants Interference with the absorption of fat-soluble vitamins (supplements of vitamins A, D, K, and folic acid may be required when treatment is prolonged).
Contraindications
Complete biliary obstruction (not likely to be effective)
Side effects
For all bile acid sequestrants Common or very common Constipation; dyspepsia; nausea; vomiting Rare or very rare Intestinal obstruction Side-effects For colestyramine Uncommon Appetite decreased; bleeding tendency; diarrhoea; gastrointestinal discomfort; gastrointestinal disorders; hypoprothrombinaemia; night blindness; osteoporosis; skin reactions; tongue irritation; vitamin deficiencies
Interactions
**Severe interactions:**
- There was no clinically significant decrease in bioavailability or therapeutic effect when pravastatin was administered one hour before or four hours after colestyramine or one hour before...
- Effect of other medicinal products on leflunomide: Cholestyramine or activated charcoal It is recommended that patients receiving leflunomide are not treated with colestyramine or activated powdered...
**Other interactions (21):**
- Colestyramine Concomitant colestyramine administration decreased the mean area under the curve (AUC) of total ezetimibe (ezetimibe + ezetimibe glucuronide) approximately 55%.
- The incremental low-density lipoprotein cholesterol (LDL-C) reduction due to adding Ezetimibe to colestyramine may be lessened by this interaction (see section 4.2).
- Concomitant use of torasemide and colestyramine has not been studied in humans, but in an animal study co-administration of cholestyramine decreased absorption of oral torasemide.
- Colestyramine/Colestipol: concomitant administration resulted in approximately 40 to 50% decrease in the bioavailability of pravastatin .
- Pharmacokinetic interactions: An inhibition of the absorption of trospium chloride with drugs like guar, colestyramine and colestipol cannot be excluded.
- The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by colestyramine.
Pregnancy
For all bile acid sequestrants Bile acid sequestrants should be used with caution as although the drugs are not absorbed, they may cause fat-soluble vitamin deficiency on prolonged use.
Breast feeding
For all bile acid sequestrants Bile acid sequestrants should be used with caution as although the drugs are not absorbed, they may cause fat-soluble vitamin deficiency on prolonged use.
Medicinal forms
Solution
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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