Antidiabetic agents

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Information about Antidiabetic agents

Management and treatment of diabetes usually begins with advice on diet and exercise. Insulin is the therapeutic mainstay of therapy of type 1 diabetes, whereas agents that increase insulin secretion or activity are the primary approaches to therapy of type 2 diabetes.

Type 2 diabetes management

  • First line conventional therapies for type 2 diabetes include biguanides (metformin) and sulfonylureas. Metformin increases insulin sensitivity whereas the sulfonylureas increase insulin secretion. More recently developed agents include alpha glucosidase inhibitors, thiazolidinediones, metiglidine analogues and drugs that affect the incretin system.
  • Alpha glucosidase inhibitors act in the gastrointestinal tract to decrease glucose absorption.
  • The thiazolidinediones affect multiple intracellular metabolic pathways that increase insulin actions and improve insulin sensitivity. Metiglidines, like the sulfonylureas, increase insulin secretion.
  • Finally, drugs that affect the incretin system include analogues of glucagon-like peptide-1 (GLP-1) that promote early insulin release from the pancreas and inhibitors of dipeptiyl peptidases 4 (DPP-4) that prolong the activity of GLP-1 in the serum.

New diabetes drugs

A relatively new category of antidiabetic agents are inhibitors of the sodium glucose cotransporter-2 (SGLT-2), which is responsible for reabsorption of glucose in the kidney; inhibition of this transporter causes glucosuria and can reduce hyperglycemia in patients with diabetes. The first commercially available SGLT-2 inhibitors (canagliflozin and dapagliflozin) were approved for use in the United States in 2013.

Liver safety of Antidiabetic agents

Most antidiabetic agents have minimal adverse effects on the liver and have only rarely been linked to instances of clinically apparent acute liver injury.


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