Pharmacology: SGLT2 inhibitors Flashcards
what does SGLT2 stand for
sodium glucose transporter
what is the physiological role of SGLT 2
to reabsorb glucose(90%) in the renal tubules so it doesn’t come out in urine
what effect do SGLT 2 inhibitors have on sugar/glucose uptake in the kidneys
they decrease it by about 1/4
what effect do SGLT 2 inhibitors have on urine
they make you urinate sugar
what direct systemic effects are seen with the use of SGLT 2
reduction in HF, increased urate excretion(= decreased urate in blood plasma) and renal protection
describe why SGLT 2 inhibitors reduce HF
glucose loss results in osmotic diuresis, inhibition of SGLT2 reduced Na absorption
Both of these have mild diuretics effect, may explain reduction in HF
what indirect effect do SGLT2 inhibitors have by reducing glucose
decreased insulin and increase in glucagon
what indirect effect of SGLT2 inhibitors is due to a decrease in lipolysis(due to decreased insulin which inhibits it)
increase in free fatty acids, which increase ketone body production
what is the benefit of increased FFA and ketone body production
they are fuel to cardiac myocytes and improve cardiac bioenergetics(cardiac benefit)
what is the bad effect of increased FFA and ketone body production
can increase ketosis and risk of ketoacidosis
describe the effect SGLT2 inhibitors have on weight
result in weight loss because glucose is excreted, so loss of calories and therefore weight loss(significant weight loss)
what does the glucose reducing effect of SGLT2 inhibitors rely on
the renal glucose filtration, no glucose benefit if eGFR <45ml/min and decrease benefit if <90ml/min
describe the potency of SGLT2 inhibitors
moderate, HbAC1 reduction of ~11mmol/mol.
more then DPP4i, same as GLP-1RA, less than SUs and metformin
what are the 3 commonly used SGLT2 inhibitors
Dapagliflozin, Canagliflozin, Empagliflozin
what effect do SGLT2 inhibitors have on BP and on lipids
BP = slight reduction Lipids = slight increased in LDL and HDL cholesterol
