Metformin Flashcards
what flower does metformin come from?
french lilac, goats rue
what is the active component of French lilac?
guanidine
what is biguanide?
2 guanidine stuck together
what is the formulation of metformin?
dimethylbiguanide
what is metformin said to be?
weak cellular poison
how does metformin work?
inhibits complex 1 of the mitochondrial respiration chain (electoral transport chain)
what does the inhibition of the mitochondrial respiratory chain result in?
fall in cellular ATP (increase in ADP/ATP ratio), rise in AMP:ATP, activation of AMPK, reduction in gluconeogenesis (glucose production by liver)
what causes the reduction in gluconeogenesis?
could be mediated by rise in AMP kinase but probably secondary due to rise in AMP
what does the effects of metformin depend on?
where in the body it gets to
is metformin hydrophobic or hydrophilic?
hydrophilic
what does the hydrophilic nature of metformin mean?
it is not readily taken up by cells, only taken into cells that readily actively transport
what transporters does metformin require?
organic cation transporters (OCT’s)
what tissues is metformin present in?
intestines, liver and kidney (rarely gets into other tissues)
how is metformin excreted?
unchanged in the urine (metformin is not metabolised)
what is the main physiological mechanism of metformin?
lowers hepatic glucose production and increases gut glucose utilisation and metabolism
