T2DM Drugs Flashcards
Pharmacology
Name the 4 actions of T2DM drugs.
- increase insulin secretion
- decrease insulin resistance and reduce hepatic glucose output
- slow glucose absorption in GI tract
- enhance glucose excretion by kidney
name the 4 classes of drug that increase insulin secretion.
sulfonylureas
glinides (meglitinides)
incretic analogues
DPP-4 inhibitors
name the 2 classes of drug that decrease insulin resistance and hepatic glucose output
biguanides and thiazolidinediones (glitazones)
name the class of drug that slows glucose absorption from the GI tract
alpha-glucosidase inhibitor
name the class of drug that enhances glucose excretion by the kidney
sodium glucose type-2 (SGLT2) inhibitors
are alpha-glucosidase inhibitors and sodium glucose type-2 (SGLT2) inhibitors insulin dependent?
no
SUR1 subunits regulate __________ channel activity
SUR1 subunits regulate POTASSIUM channel activity
___ binding to each of the Kir6.2 subunits closes the channel causing ______________ of the ____ cell and _______ release
ATP binding to each of the Kir6.2 subunits closes the channel causing DEPOLARIZATION of the BETA cell and INSULIN release
ADP-Mg2+ binding to the SUR1 subunits ______ the channel maintaining the resting potential of the ____ cell and _________ insulin secretion
ADP-Mg2+ binding to the SUR1 subunits OPENS the channel maintaining the resting potential of the BETA cell and INHIBITS insulin secretion
sulfonylureas used in T2DM bind to SUR1 and _____ the channel causing _____________ and insulin release independent of plasma ________ concentration
sulfonylureas used in T2DM bind to SUR1 and CLOSE the channel causing DEPOLARIZATION and insulin release independent of plasma GLUCOSE concentration
what do sulfonylurea drugs end in?
-ide
give an example of a sulfonylurea
glipizide
gliclazide
SUs, in the long term, reduce what complications?
microvascular
SUs are used first line if the patient is intolerant to what?
metformin
SUs are often used in combination with what?
metformin
SUs adverse effect?
weight gain
SUs should be avoided in who?
elderly, pregnancy and CKD
what do glinides (meglitinides) end in?
-glinide
give an example of a glinide
repaglinide and netaglinide
glinides should not be used in who?
severe hepatic impairment, pregnancy and breast feeding
ingestion of food stimulates release of what?
glucagon peptide like-1 (GLP-1) and GIP
GLP-1 and GIP enhance _______ release from beta cells and ________ uptake whereas GLP-1 decreases _________ release from alpha cells
both resulting in decreased blood glucose
GLP-1 and GIP enhance _______ release from beta cells and ________ uptake whereas GLP-1 decreases _________ release from alpha cells
both resulting in decreased blood glucose
what is the other name for DPP-4 inhibitors
gliptins
what do DPP-4s end in?
-gliptin
give an example of a DPP-4 inhibitor
sitagliptin
what does DPP-4 stand for?
dipeptidyl peptidase-4
DPP-4s are usually prescribed in combination with what?
metformin or SU
what is the main adverse effect of a gliptin?
DPP-4 inhibitor adverse effect = NAUSEA
is there hypoglycaemia or weight gain in gliptins?
no
can SUs cause hypoglycaemia?
no
can glinides cause hypoglycaemia?
no
incretin analogues are peptides that mimic the action of what?
GLP-1
what do incretin analogues end in?
-tide
how are incretin analogues administered?
SC injection
name an incretin analogue
extenatide
extenatide
liraglutide
what can incretin analogues cause loss of?
weight loss
do incretin analogues cause hypoglycaemia?
no
2 side effects of incretin analogues?
nausea
pancreatitis - rare
name the infrequently used in the UK, brush border enzyme inhibitor that breaks down starch and disaccharides to absorbable glucose
alpha-glucosidase inhibitors
name an example of a alpha-glucosidase inhibitor
acarbose
miglitol
voglibose
alpha-glucosidase inhibitor adverse effects?
flactulence loose stools diarrhoea abdominal pain bloating
do alpha-glucosidase inhibitors pose risk of hypoglycaemia?
no
name the first line agent in the treatment of T2DM
metformin
unless SEVERE hepatic/renal impairment
what does metformin reduce and increase?
reduce:
hepatic gluconeogenesis
carbohydrate absorption
increase:
glucose uptake by muscle
fatty acid oxidation
metformin is what class of drug?
biguanide
does metformin cause hypoglycaemia?
no
does metformin cause weight gain?
no - weight loss
name the 2 adverse effects of metformin
GI upset
lactic acidosis - rare
thiazolidinediones are also known as what?
TZDs and glitazones
do thiazolidinediones cause hypoglycaemia?
no
do thiazolidinediones cause weight gain?
yes
what do thiazolidinediones end in?
-glitazone
name a thiazolidinedione drug
pioglitazone
thiazolidinedione adverse effects?
weight gain
increased bone fracture risk
fluid retention
name the new drug class that is not dependent on insulin
sodium-glucose cotransporter (SGLT2) inhibitors
what do SGLT2 inhibitors end in?
-agliflozin
give an example of a SGLT2 inhibitor
empagliflozin
canagliflozin
dapagliflozin
do SGLT2 inhibitors cause hypoglycaemia?
no
do SGLT2 inhibitors cause weight gain?
no - weight loss
name the drug that can cause hypoglycaemia
SUs - glipizide
glinides can also cause but not as much as SUs