Comparative Pharmacology
Head-to-head clinical analysis: FLAVORED COLESTID versus LOCHOLEST.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FLAVORED COLESTID versus LOCHOLEST.
FLAVORED COLESTID vs LOCHOLEST
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Colestid (colestipol) is a bile acid sequestrant. It binds bile acids in the intestine, forming an insoluble complex that is excreted in feces. This reduces enterohepatic circulation of bile acids, leading to increased hepatic conversion of cholesterol to bile acids, thereby lowering serum low-density lipoprotein (LDL) cholesterol levels.
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.
5-30 grams orally daily, divided into 2-4 doses, starting at 5 grams once daily and increasing by 5 grams every 4-7 days as tolerated; taken with meals and mixed with at least 4-8 oz of liquid per dose.
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 due to non-absorbable resin; systemic absorption is negligible. Terminal half-life not defined.
Terminal elimination half-life is approximately 19 hours (range 14-47 hours) for patients with normal renal function; accumulation occurs with once-daily dosing.
Primarily fecal as insoluble complex (90-95%); <5% renal as glucuronide conjugate; minimal biliary elimination.
Primarily fecal (biliary) as unchanged drug; renal excretion <5%.
Category C
Category C
Bile Acid Sequestrant
Bile Acid Sequestrant