Comparative Pharmacology
Head-to-head clinical analysis: CHOLESTYRAMINE versus LOCHOLEST.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CHOLESTYRAMINE versus LOCHOLEST.
CHOLESTYRAMINE vs LOCHOLEST
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cholestyramine is a bile acid sequestrant that 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 conversion of cholesterol to bile acids in the liver and decreased 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.
4 g orally once or twice daily, titrated up to 24 g/day divided into 2-6 doses; usual maintenance dose 8-16 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; cholestyramine is not absorbed and does not have a systemic half-life. Its clinical effect is related to gastrointestinal transit time.
Terminal elimination half-life is approximately 19 hours (range 14-47 hours) for patients with normal renal function; accumulation occurs with once-daily dosing.
Cholestyramine is not absorbed systemically; it remains in the gastrointestinal tract and is excreted unchanged in feces. 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