Formulary
Colesevelam hydrochloride: 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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Colesevelam hydrochloride: 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
**Primary hypercholesterolaemia as an adjunct to dietary measures [monotherapy]**
- **Adult** (By Mouth): 3.75 g daily in 1-2 divided doses; maximum 4.375 g per day.
**Primary hypercholesterolaemia as an adjunct to dietary measures [in combination with a statin],Primary and familial hypercholesterolaemia [in combination with ezetimibe, either with or without a statin]**
- **Adult** (By Mouth): 2.5-3.75 g daily in 1-2 divided doses, may be taken at the same time as the statin and ezetimibe.
**Bile acid malabsorption**
- **Adult** (By Mouth): 1.25-3.75 g daily in 2-3 divided doses.
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). Cautions For colesevelam hydrochloride Gastro-intestinal motility disorders; inflammatory bowel disease; major gastro-intestinal surgery
Contraindications
Biliary obstruction; bowel obstruction
Side effects
For all bile acid sequestrants Common or very common Constipation; dyspepsia; nausea; vomiting Rare or very rare Intestinal obstruction Side-effects For colesevelam hydrochloride Common or very common Faeces abnormal; gastrointestinal discomfort; headache Uncommon Dysphagia; myalgia Rare or very rare Pancreatitis
Interactions
**Severe interactions:**
- Ciclosporin In an interaction study in healthy volunteers, co-administration of Cholestagel/Colesevelam and ciclosporin significantly reduced the AUC 0-inf and C max of ciclosporin by 34% by 44%,...
- Other forms of interaction Cholestagel/Colesevelam did not induce any clinically significant reduction in the absorption of vitamins A, D, E or K during clinical studies of up to one year.
**Other interactions (29):**
- In general Cholestagel/Colesevelam may affect the bioavailability of other medicinal products.
- Therefore when a drug interaction cannot be excluded with a concomitant medicinal product for which minor variations in the therapeutic level would be clinically important, Cholestagel/Colesevelam...
- For concomitant medications which require administration via divided doses, it should be noted that the required dose of Cholestagel/Colesevelam can be taken once a day.
- In interaction studies in healthy volunteers, Cholestagel/Colesevelam had no effect on the bioavailability of digoxin, metoprolol, quinidine, valproic acid, and warfarin.
- Cholestagel/Colesevelam decreased the C max and AUC of sustained-release verapamil by approximately 31% and 11%, respectively.
- There have been very rare reports of reduced phenytoin levels in patients who have received Cholestagel/Colesevelam administered with phenytoin.
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.
Hepatic impairment
Manufacturer advises caution in hepatic failure (no information available).
Medicinal forms
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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