Comparative Pharmacology
Head-to-head clinical analysis: COLESEVELAM HYDROCHLORIDE versus COLESTID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COLESEVELAM HYDROCHLORIDE versus COLESTID.
COLESEVELAM HYDROCHLORIDE vs COLESTID
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Colesevelam hydrochloride is a bile acid sequestrant that binds bile acids in the intestine, forming an insoluble complex excreted in feces. This reduces enterohepatic circulation of bile acids, leading to increased conversion of cholesterol to bile acids in the liver and upregulation of LDL receptors, resulting in decreased serum LDL cholesterol. In diabetes, it improves glycemic control possibly by altering bile acid signaling via FXR and TGR5 receptors, affecting hepatic glucose production and incretin release.
Binds bile acids in the intestine, forming an insoluble complex that is excreted in the feces, thereby increasing fecal loss of bile acids and reducing enterohepatic circulation of bile salts. This leads to increased hepatic conversion of cholesterol to bile acids, reduction in hepatic cholesterol stores, and decreased plasma LDL cholesterol levels.
3.75 g orally once daily or divided as 1.875 g twice daily with meals and liquid; maximum 4.375 g/day.
5-10 g orally once or twice daily, maximum 30 g/day.
None Documented
None Documented
Not applicable as colesevelam is not absorbed; it acts locally in the gastrointestinal tract.
Not applicable due to non-systemic action; local gastrointestinal half-life not clinically defined
Colesevelam is not absorbed systemically; it is excreted unchanged in the feces via biliary elimination. No renal excretion occurs.
Primarily fecal (≥95%) as unchanged drug; minimal renal excretion (<5%)
Category A/B
Category C
Bile Acid Sequestrant
Bile Acid Sequestrant