Comparative Pharmacology
Head-to-head clinical analysis: COLESTIPOL HYDROCHLORIDE versus LOCHOLEST.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COLESTIPOL HYDROCHLORIDE versus LOCHOLEST.
COLESTIPOL HYDROCHLORIDE vs LOCHOLEST
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Binds bile acids in the intestine, forming an insoluble complex that is excreted in feces, thereby reducing enterohepatic circulation and increasing hepatic conversion of cholesterol to bile acids, lowering serum LDL cholesterol.
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.
Initial: 5 g orally once daily or 2.5 g twice daily; increase gradually by 5 g/day at 1-2 month intervals; maintenance: 5-30 g/day divided once or twice daily; maximum: 30 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 colestipol is not absorbed; it acts locally in the gastrointestinal tract and has no systemic half-life.
Terminal elimination half-life is approximately 19 hours (range 14-47 hours) for patients with normal renal function; accumulation occurs with once-daily dosing.
Colestipol hydrochloride is not absorbed systemically; it is excreted entirely in the feces as the intact polymer, without undergoing metabolism. No renal or biliary elimination occurs.
Primarily fecal (biliary) as unchanged drug; renal excretion <5%.
Category C
Category C
Bile Acid Sequestrant
Bile Acid Sequestrant