Comparative Pharmacology
Head-to-head clinical analysis: COLESEVELAM HYDROCHLORIDE versus LOCHOLEST.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COLESEVELAM HYDROCHLORIDE versus LOCHOLEST.
COLESEVELAM HYDROCHLORIDE vs LOCHOLEST
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.
Locholest is a bile acid sequestrant that binds bile acids in the intestine, preventing their reabsorption and promoting fecal excretion. This leads to increased hepatic conversion of cholesterol to bile acids, reducing serum LDL cholesterol.
3.75 g orally once daily or divided as 1.875 g twice daily with meals and liquid; maximum 4.375 g/day.
Initial dose: 10-20 mg orally once daily, taken in the evening. Titrate as tolerated every 4 weeks to a maximum of 80 mg once daily.
None Documented
None Documented
Not applicable as colesevelam is not absorbed; it acts locally in the gastrointestinal tract.
Terminal elimination half-life is approximately 19 hours (range 14-47 hours) for patients with normal renal function; accumulation occurs with once-daily dosing.
Colesevelam is not absorbed systemically; it is excreted unchanged in the feces via biliary elimination. No renal excretion occurs.
Primarily fecal (biliary) as unchanged drug; renal excretion <5%.
Category A/B
Category C
Bile Acid Sequestrant
Bile Acid Sequestrant