Newer Approaches in Diabetes

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Chapter: Essential pharmacology : Insulin, Oral Hypoglycaemic Drugs and Glucagon

Exenatide : The glucagonlike peptide1 (GLP1) is an important incretin that is released from the gut in response to oral glucose. It is difficult to use clinically because of rapid degradation by the enzyme dipeptidyl peptidase4 (DPP4).


NEWER APPROACHES IN DIABETES

 

Exenatide

 

The glucagonlike peptide1 (GLP1) is an important incretin that is released from the gut in response to oral glucose. It is difficult to use clinically because of rapid degradation by the enzyme dipeptidyl peptidase4 (DPP4). Exenatide is a synthetic GLP1 analogue, resistant to DPP4, but with similar actions, viz. enhancement of postprandial insulin release, suppression of glucagon release and appetite as well as slowing of gastric emptying. It has been marketed in the USA to be used as an additional drug with metformin and/or sulfonylureas in type 2 diabetics who have inadequate response to the oral hypoglycaemics. Exenatide is injected s.c. twice daily 1 hour before meals; acts for 6–10 hours. Nausea is an important side effect.

 

Sitagliptin

 

This orally active inhibitor of DPP4 prevents degradation of endogenous GLP1 and other incretins, potentiating their action, resulting in limitation of postprandial hyperglycaemia. It is undergoing clinical evaluation as an addon drug to sufonylurea/ metformin/ thiazolidinediones in type 2 DM.

 

Pramlintide

 

This synthetic amylin (a polypeptide produced by pancreatic β cells which reduces glucagon secretion from α cells and delays gastric emptying) analogue attenuates postprandial hyperglycaemia when injected s.c. just before a meal, and exerts a centrally mediated anorectic action. The duration of action is 2–3 hours. It has been marketed as an adjuvant to insulin/ sulfonylureas/metformin for control of mealtime glycaemia in both type1 and type2 diabetes.

 

 

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