TYPE 2 diabetes drugs Flashcards
What are the two Thiazolidinediones
Pioglitazone and Rosiglitazone
What do thiazolidinediones do? What are their MOA?
what are the AE?
They decrease insulin resistance
MAO: they target adipocytes and activate the transcription factor PPAR gamma which will increase the reuptake of glucose in the liver and skeletal muscle.
AE: they are contraindicated in NY heart association class 3 and class 4 heart failure
What does Metformin do?
what is its MOA in the liver and skeletal muscle?
What are the AE?
It decreases insulin resistance
MAO LIVER: Metformin is transported into the liver cell and binds to complex 1 which causes and increase in AMP kinase which will block the release of glucose from the liver and decrease blood glucose levels.
MAO SKELETAL MUSCLE: Accumulation of AMP causes the activation of AMP kinase. AMPK phosphorylates TBC1D4 which promotes activity from Rab. Rab then disassociates from the GLut 4 receptor and allows for it to translocate to the membrane and increase glucose uptake in the skeletal muscle.
AE: Decrease vitamin B-12, GI discomfort,
What are the 6 Sulfonylureas drugs
Tolbutamide, Tolazamide, Chlorpropamide, Glyburide, Glipizide, Glimepiride
What do Sulfonylureas do?
What is their MOA?
What are the AE?
There will enhance insulin secretion (Glucose Independent)
MOA: Sulfonylureas will bind to the sulfonylurea receptor on the Katp channel and cause it to close. This closure will cause the depolarization of the membrane and cause the Ca channel to open which allows Ca into the cell and this increases excocytosis of granules containing insulin (Increase the release of insulin from the liver)
AE: Weight gain, long term use can result in decrease insulin secretion, hypoglycemia
What are the two Meglitinides
Nateglinide and Repaglinide
What do meglitinides do?
What is the MOA?
What are the AE?
They will increase the release of insulin (glucose independent)
MOA: Bind to Katp channel and block it. Cause depolorization of membrane and stimulate Ca channel allowing for ca in the cell and increasing insulin release.
AE: Weight gain, hypoglycemia
What are the 5 GLP-1R agonists
Exenatide, Liraglutide, Lixenatide, Dulaglutide, Semaglutide
What do GLP-1R agonists do
What is their MOA
What are the AE
These will enhance the incretin effect
MOA : These will cause amplification of glucose stimulated secretion in the gut (Increase in insulin secretion thru cAMP pathway and increase beta cell proliferation thru ERK 1/2 pathway)
AE:Nausea, Vommiting, pancreatitis, Risk of thyroid tumors
Contraindicated in patients with a family history of medullary thyroid cancer (EXCEPT Liraglutide)
What is the one GLP-1 and GIP dual agonist drug
Trizepatide
What is the action of GLP-1 and GIP dual agonist drug
reduces internalization of GLP-1 receptor to maintain GLP-1 effect
What are the 4 inhibitors of Dipeptidyl Peptidase 4
Sitagliptin, saxagliptin, linagliptin, aloglipitin
What do inhibitors of DPP-4 do
What is the MOA
What are the AE
These will inhibit DPP-4 which is the enzyme that degrades GLP-1
MOA: binds to DPP-4 and blocks its activity to reduce hyperglycemia and HgbA1C
(All are excreted in the kidneys except for saxaglipitin which is excreted in the liver (poop))
NOTE: Can cause white blood cell count to be reduces which means potential increased risk of cancer
AE: HF, joint pain, pancreatitis, Nausea, vomiting, constipation, headaches
Pramlintide (amylin analog)
Works by slowing gastric emptying, decrease food intake, and inhibits glucagon secretion
- blunts rise in blood glucose after a meal
can be used in both type 1 and 2
what are the two alpha-glucosidase inhibitors
acarbose, and miglitol