Drugs for Diabetes Flashcards
What are the 10 classes
1) Alpha-glucosidase inhibitors
2) Biguanides
3) sulfonylureas
4) meglitinides
5) Thiazolidinediones
6) Dipeptidyl peptidase-4 (DPP-4)
7) Glucagon-like peptide-1 GLP-1 receptor agonists
8) SGLT2 inhibitors
9) weight loss agents
10) Insulins
What is the A1C target for adults with T2D to reduce the risk of CDK and retinopathy if at low risk of hypoglycemia
<=6.5
What is the A1C target for most adults with T1D or T2D
<=7.0
What is the A1C target for the end of life
7.1-8.5
What pharmacotherapy do you give if A1C 1.5% over target
Initiate healhty behavior interventions and start metformin if not a target in 3 months or start metformin with helahty behavior interventions
What pharmacotherapy do you give if A1C >=1.5% over target
start metformin with healthy behaviour interventions and consider a second concurrent agent
I patient presents as symptomatic hyperglycemia ad or metabolic decompensation Polyuria polydipsia weight loss volume depletion
Start insulin plus or minus metformin
What are good drugs for Chronic kidney disease and Diabetes
SGLT2i and GLP1-RA
What is a good drug for Heart failure and Diabetes
SGLT2I
What is a good drug for
Atherosclerotic cardiovascular disease and Diabetes
SGT2I
What is the mechanism of action of Biguanide?
Acts on liver and decrease hepatic glucose output an decreases insulin resistance , increase glucose metabolism
decrease gluconeogenisi. drecreased glyconolysis
decreased FA oxidation
decreased insulin mediated glucose uptake
decrease NADH oxidation, ampk signalling TCA cycle flux ATP synthesis GNG
What type of drug is metformin
Beguanide
Metformin advantages
effective gluvose lowering (1.5-2.0%)
no significant hypoglycemia (rare)
durable effect
not associated with weight gain or CV sdie effects (possible benefit
Metformin disadvantages
GI side-effects nausea diarrhea metallic taste
rare lactic acidosis
What are the two types of Secretagogues
Long acting sulfonylureas
GLyburide
glicalzide
glimepiride
Short-acting secretogogues
Repaglinide
Nateglinide
What are the long-acting sulfonylureas
GLyburide
glicalzide
glimepiride
What are the short-acting sulfonylureas
Repaglinide
Nateglinide
Mechanism of action of secretagogues
work in B cell to increase insulin secretion
block the Kir6.2/SUR-1 complex on the potassium channel leads to increased caldium incflux
Secretagogues (Sulfonylurea) advantages
inexpensive
easy to administer
effective at lowering glucose (intially) (1.5-2.0%)
Secretagogues (Sulfonylurea) disadvantages
Prone to wieght gain
risks of hypoglycemia
Dipeptidyl peptidase-4 inhibitors (DPP-4) what is the last part of the name
“liptin”
alogliptin
liagliptin
saxagliptin
sitagliptin
GLP-1 receptor agonists what is the last part of the name
“natide” or “glutide”
Short acting: exenatide
lixisenatide
liraglutide
long acting
exanatide LAR
dulagluide
semaglutide
Mechanism of GLP-1 receptor agonist action
GLP-1 RA’s exerts its main effect by stimulating glucose-dependent insulin release from the pancreatic islets
Mechanism of action of DPP-4 inhibitors
DPP-4 is an enzyme that breaks down GLP-1
The mechanism of DPP-4 inhibitors is to increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.
What does GLP-1 do? (4)
It increases insulin release decreases blood glucose decreases glucagon secretion it decreases appetitive by slowing gastric emptying
Does GLP-1 help you lose weight
yes
Do DPP-4 help you lose weight
no
How do you administer GLP-1 RA
Injection
What organs do Incretins act on
the liver,stomach and pancreaus, Increase insuling secretion decrease glucose output and decrease gastric tempting
Advantages of incretin agents
Dpp-4 inhibitors- 0.5-0.9%
GLP-1 Recetor agonsits -1.0-1.5%
cardiovasucular benefit liraglutide semaglutide dulaglutide
Possible weight loss
Disadvantages of incretins
Cost and coverage
DPP-4 side effects sasal stuffiness
saxagliptin-increased risk of heart failure
GLP-1 RA’s injectable nausea cholelithiasis
What is the end part of SGLT2 inhibitors
“flozin”
Canagliflozin
dapagliflozin
empagliflozin
etrugiflozin
Mechanism of action of SGLT2 inhibitors
increase amount of glucose excreted by kidneys by inhibiting sglt2 in the proximal convoluted tubule
Advantages Of SGLT2 inhibitors
easy to admin
effective glucose lowering (1-1.5
promotes weight loss, lowers BP low risk of hypoglycemia
Cardiovascular benefit in high-risk patients -empagliflozin and canagliflozin
renal benefit reduces microalbuminuria, slows decline in kidney function ,reduces the risk of eskd or dialyssis
Disadvantages of SGLT2 inhibitors
polyuria urininary frequency volumen deplecion hyperkalemia mycotic yeast infections rare cases of euhlycemic DKA cnagliflozin-increased risk of ampuattion and bone fracutures in people at high risk
What is the mechanism of action of Thiazolidinediones(TZDs): PPAR-y activators
act on liver adipose and muscle reduces insulin resistance modifies adipocyte differentiation inhibits VEGF-induced angiogenesis reduces leptin levels leading to increased appetite
Their action, in large part, is mediated by activation of PPARϒ and involves the redistribution of surplus fatty acids to peripheral fat. This reduces fatty acid availability in the circulation as well as in the liver and muscle - thus improving insulin sensitivity
ADvantages of Thiazolidinediones
easy to administer
effective glucose lowering (1.5-2.0%)
durable
Disadvantages of TZDs
cost/coverage
sideeffects of weight gain edema worsening CHF distal bone fratures in women
alpha-glucosidase inhibitors MOA
Binds to glucosidase enzyme in the gut and competitively inhibits the breakdown of non-absorbable complex poly-saccharides
reduces monosaccharide absorption
Name of the one alpha-glucosidase inhibitor we know
Acarbose
Disadvantages Acarbose
not systemically absorbed
targets post-prandial hyperglycemia
Disadvantage of Acrabose
Modest A1C lowering (0.5%)
GI sideeffects gas bloating flatulence
multipel daily dosing
What are the 4 Basal insulins
insulin glargine
insuline glargine u300
insulin determir
insulin gludec
What are the 4 bolus insulings
Human regula insulin
analogue rapid insulins
analogue ultra-rapid insulins
