Objective: Orlistat decreases the absorption of dietary triglycerides by inhibiting intestinal lipases. Orlistat therapy is associated with a greater decline in plasma low-density lipoprotein-cholesterol concentrations than that expected from weight loss alone. Therefore, we evaluated the effect of orlistat treatment on dietary cholesterol absorption as a possible mechanism for the independent effect of orlistat on plasma cholesterol concentration. Research Methods and Procedures: Cholesterol absorption from a standardized meal, containing 72 mg of cholesterol, was determined in 18 subjects with class II abdominal obesity (BMI, 35.0 to 39.9 kg/m2) by simultaneous administration of intravenous ([2H6] cholesterol) and oral ([2H5] cholesterol) cholesterol tracers. In protocol 1 (n = 9), cholesterol absorption was determined on two different occasions, 10 to 20 days apart, to assess the reproducibility of the tracer method. In protocol 2 (n = 9), cholesterol absorption was determined with and without orlistat therapy in a prospective, randomized, crossover design to assess the effect of orlistat on cholesterol absorption. Results: In protocol 1, cholesterol absorption from the test meal was the same on both occasions (53 ± 5% and 51 ± 5%). In protocol 2, orlistat treatment caused a 25% reduction in cholesterol absorption, from 59 ± 6% to 44 ± 5% (p < 0.01). Discussion: These data demonstrate that orlistat inhibits dietary cholesterol absorption, which may have beneficial effects on lipoprotein metabolism in obese subjects that are independent of weight loss itself.

Original languageEnglish
Pages (from-to)599-604
Number of pages6
JournalObesity research
Issue number10
StatePublished - Oct 2001


  • Cholesterol
  • Orlistat
  • Stable isotope
  • Weight loss


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