Insulin Sensitisers And GLP agonists Flashcards
What is an insulin sensitiser?
Improve insulin sensitivity in tissues
Decrease insulin resistance
They DO NOT induce insulin secretion
What is the mechanism of action for metformin?
Inhibits mitochondrial complex 1 of respiratory chain
Decreases ATP = increases AMP:ATP ratio
Decreases NAD+
Overall less gluconeogenesis and less glucagon action
Function of metformin
Decrease hepatic glucose production
Decrease intestine absorption of glucose
Improves insulin sensitivity by increasing peripheral glucose uptake and utilisation
Role of metformin in liver
Decrease : gluconeogenesis, lipogenesis, glycolysis
Increase: glucose uptake, fatty acid oxidation
Role of metformin in muscle
Decrease lipogenesis
Increase: glucose uptake, fatty acid oxidation
Role of metformin in adipocytes
Decrease: lipolysis, lipogenesis, glycolysis
Increases: glucose uptake, fatty acid oxidation
Role of metformin in liver, muscle, adipocytes? Increasing only
Increase glucose uptake, fatty acid oxidation
Role of metformin in pancreas
Decrease lipotoxicity (insulin secretion and apoptosis)
Increase GLP-1 receptor
Role of metformin in gut
Decrease glucose absorption
Increase GLP-1 secretion
Advantages of metformin
Water soluble so can be taken orally
Generally effective and well operated
Disadvantages of metformin
Cause lactic acidosis, diarrhoea, nausea, vomiting, flactulence (gas)
Maximum dose of metformin
2000 mg/ day
mg of metformin for immediate-release
500mg twice a day or 850 mg once a day
Mg for metformin for extended-release
500 - 1000 mg once a day
TZD
Thiazolidinediones
