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Role of Bile Acid Sequestration in Glucose Homeostasis

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Dr Prabha Adhikari, Mangalore    26 November 2018

  1. Bile acids have a role in lipid, glucose homeostasis and energy expenditure. They regulate glucose through their effect on maintenance of normal gut microbiota which in turn regulates glucose through action on GLP-1.
  2. Novel receptors of bile acids of one nuclear receptor named FXR and cytoplasmic receptor named TGR5 regulate bile acid synthesis and participate in gluconeogenesis, insulin sensitivity, glycogen synthesis and GLP-1 – the very pathophysiology of diabetes. New drugs are being developed in preclinical studies. However, human studies have not yet been successful.
  3. Novel targets for treatment are under development as bile acid sequestrants, which regulate both lipids and glucose. Cholestyramine, colestipol, colestimide and colesevelam are bile sequestrants that are positively charged and bind to bile acids to form an insoluble complex that is excreted in the feces.
  4. Colesevelam has been approved for treatment of diabetes with an HbA1c reduction of 0.54%. Colestimide has been known to reduce cholesterol and postprandial glucose and increase GLP-1.

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