type 2 diabetes Flashcards
Metformin drug class
Biguanides
metformin target
AMP-kinase
metformin moa
increase the sensitivity of peripheral tissues to insulin and inhibits gluconeogenesis in the liver
metformin effect on senses
metallic taste
critical side effect of metformin
lactic acidosis
what condition and metformin are you worried about lactic acidosis
renal impairment
metformin dosent cause …
hypoglycaemia (requires endogenous insulin to work)
name a drug that causes taste distubance
amitriptyline = metallic taste
what enzyme does metformin inhibit
glycogen phosphorylase
gliclazide drug class
Sulfonylureas
gliclazide target
block ATP-sensitive K+ channels on β islet cell plasma membranes
what dont people like about gliclazide
weight gain
gliclazide moa
Reduced K+ efflux leading to β cell depolarisation, Ca2+ entry and insulin secretion
gliclazide side effects
Hypoglycaemia
Hyponatraemia
Hepatotoxicity
Hypersensitivity
when to with hold all diabetic drugs
ketoacidosis
name two Sulfonylureas
Glimepiride
gliclazide
glimepiride drug class
Sulfonylureas
glimepiride duration
long duration of action
overall action of glimepiride
stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin
what does glimepiride bind to
ATP-sensitive potassium channel receptors on the pancreatic cell surface
glimepiride moa
potassium blocking = depolarization of the membrane = calcium ion influx through voltage-sensitive channels = secretion of insulin
repaglinide drug class
Meglitinides
repaglinide target
sulphonylurea type-1 receptor
repaglinide moa
Antagonism of this receptor prevents potassium ions from exiting the cell when intracellular ATP levels are low. potassium ions (K+) accumulate inside beta cells = depolarisation = insulin release
why are there no cardiac side effects with repaglinide
acts as an agonist at Sur-1 receptors. Thus no cardiac side effects as myocytes have Sur-2a subtype of sulphonylurea receptor
other good thing about repaglinide
prevention of beta cell apoptosis under heavy glucose load and prevention of fat accumulation in arteries
what is the sulphonylurea type-1 receptor part of
ATP-modulated potassium channel
where is sulphonylurea type-1 receptor found
beta cells of the pancreas
Glucagon-like peptide-1 analogues
Exenatide
Liraglutide
Liraglutide drug class
GLP-1 analogues
Liraglutide target
Glucagon-like peptide-1 (GLP-1) receptors
Liraglutide moa
GLP-1 analogues bind to and activate the receptors in the same way as the endogenous hormone and Increase synthesis and release of insulin by pancreatic β cells, suppress inappropriate glucagon secretion from pancreatic α cells
Liraglutide adverse effects
Severe pancreatitis
Hypoglycaemia
Antibody formation against exenatide
what to do if someone misses a dose of Liraglutide
take next one as normal
when not to take Liraglutide
after a meal
what is Liraglutide dependant on
glucose
Exenatide class
Glucagon-like peptide-1 receptor (GLP1R) agonists
where is GLP1 released from
intestinal endocrine cells
when is GLP1 released
after eating
Pioglitazone drug class
Thiazolidinediones
Pioglitazone target
PPARγ receptors
Pioglitazone moa
Causes the PPARγ-RXR complex to bind to DNA, promoting transcription of genes whose products are involved in insulin signalling e.g. lipoprotein lipase, Glut-4. This increases the sensitivity of tissues to insulin by recruiting glucose transporters to cell surface.
Pioglitazone are dependant on
presence of insulin
common side effects of Pioglitazone
weight gain
fluid retention
severe side effect of Pioglitazone
liver dysfunction
bone fractures in women
when to be careful giving Pioglitazone
people with cardiovascular probs
what are PPARγ receptors complexed with
retinoid X receptor
what are PPARγ receptors complexed with
retinoid X receptor
when should you stop Pioglitazone
if jaudice develops
why not take Pioglitazone and insulin
cardiac risks
why not take Pioglitazone and BB
might mask hypo
Sitagliptin drug class
DPP4 inhibitors
Sitagliptin moa
Inhibit degradation of incretin hormones GLP-1 and GIP by DPP4 enzymes. This increases levels of GLP-1 and GIP leading to increased synthesis and release of insulin by pancreatic β cells.
common adverse effect of Sitagliptin
Upper respiratory tract infection
Sitagliptin important side effect
Pancreatitis
caution with Sitagliptin in
heart failure
vildagliptin side effect
hepatotoxicity
Linagliptin drug class
dipeptidyl peptidase (DPP)-4 enzyme inhibitor
Linagliptin moa
slows the breakdown of insulinotropic hormone glucagon-like peptide (GLP)-1 and GIP
action of GIP and GLP
incretin hormones that increase the production and release of insulin from pancreatic beta cells
action of GIP and GLP
incretin hormones that increase the production and release of insulin from pancreatic beta cells
Acarbose drug class
alpha-glucosidase inhibitor
where is alpha-glucosidase found
gut
what is alpha-glucosidase used for
breaking down complex carbohydrates (i.e. starch) into glucose
Acarbose moa
kess gluclose is made in the gut so less glucose is released into the hepatic portal vein following a meal
Acarbose moa
kess gluclose is made in the gut so less glucose is released into the hepatic portal vein following a meal
name some Sodium-glucose co-transporter 2 (SGLT2) inhibitors
Canagliflozin
Dapagliflozin
Canagliflozin inhibits
SGLT2
Canagliflozin moa
reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion
what does Sodium-glucose co-transporter 2 do
reabsorption of filtered glucose from the tubular lumen
where is Sodium-glucose co-transporter 2 expressed
proximal renal tubule
where is Sodium-glucose co-transporter 2 expressed
proximal renal tubule
Dapagliflozin moa
blocks glucose reabsorption into the kidney, resulting in the elimination of blood glucose through the urine
