Does rimonabant independently affect free fatty acid and glucose metabolism?

J Clin Endocrinol Metab. 2012 Mar;97(3):819-27. doi: 10.1210/jc.2011-2486. Epub 2011 Dec 14.

Abstract

Context: Endocannabinoid receptor 1 blockade is proposed to improve metabolic complications of obesity via central and peripheral effects.

Objective: Our objective was to test whether rimonabant improves insulin regulation of free fatty acid and glucose metabolism after controlling for fat loss.

Design: This was a double-blind, placebo-controlled substudy of the visceral fat reduction assessed by computed tomography scan on rimonabant (VICTORIA) trial.

Participants and setting: Sixty-seven abdominally obese, metabolic syndrome volunteers age 35-70 yr participated at academic medical center general clinical research centers.

Intervention: Intervention included a 12-month lifestyle weight management program plus rimonabant 20 mg/d or placebo.

Main outcome measures: Body composition and two-step euglycemic, hyperinsulinemic clamp before and after intervention were performed. Insulin sensitivity was assessed as insulin concentration needed to suppress by 50% palmitate concentration [IC50(palmitate)], flux [IC50(palmitate)f], and hepatic glucose output [IC50(HGO)] and as insulin-stimulated glucose disposal (Δ glucose disappearance per Δ insulin concentration--glucose slope).

Results: Body fat decreased by 4.5±2.9% (SD) in the rimonabant and 1.9±4.5% in the placebo group (P<0.005). The primary [improvement in IC50(palmitate) and IC50(palmitate)f] and secondary [improvement in IC50(HGO) and glucose slope] outcomes were not significantly different between the rimonabant and placebo groups. Post hoc analyses revealed that 1) changes in body mass index (BMI) and IC50(palmitate) were correlated (P=0.005) in the rimonabant group; this relationship was not significantly different from placebo when controlling for greater BMI loss (P=0.5); 2) insulin-regulated glucose disposal improved in both groups (P=0.002) and correlated with changes in BMI.

Conclusions: Improvements observed in insulin regulation of free fatty acid and glucose metabolism with rimonabant treatment in humans was not greater than that predicted by weight loss alone.

Publication types

  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Behavior Therapy
  • Body Composition / drug effects
  • Cannabinoid Receptor Antagonists
  • Diet, Reducing
  • Double-Blind Method
  • Fatty Acids, Nonesterified / metabolism*
  • Female
  • Glucose / metabolism*
  • Glucose Clamp Technique
  • Humans
  • Insulin / metabolism
  • Intra-Abdominal Fat / drug effects*
  • Intra-Abdominal Fat / metabolism
  • Life Style
  • Male
  • Metabolic Syndrome / drug therapy
  • Metabolic Syndrome / metabolism*
  • Metabolic Syndrome / therapy*
  • Middle Aged
  • Obesity / drug therapy
  • Obesity / metabolism*
  • Obesity / therapy*
  • Piperidines / pharmacology
  • Piperidines / therapeutic use*
  • Pyrazoles / pharmacology
  • Pyrazoles / therapeutic use*
  • Rimonabant
  • Treatment Outcome
  • Weight Loss / drug effects

Substances

  • Cannabinoid Receptor Antagonists
  • Fatty Acids, Nonesterified
  • Insulin
  • Piperidines
  • Pyrazoles
  • Glucose
  • Rimonabant