Endocrine drugs Flashcards
Lispro, Aspart, Glulisine Action
-bind insulin receptor (tyrosine kinase activity) -increase glucose stored as glycogen in the liver -increase glyocgen, protein synthesis, and K+ uptake in muscle -increase TG storage in fat (rapid-acting)
Clinical use of lispro, aspart and glulisine
-DM1 -DM2 -GDM (postprandial glucose control)
Use of Inuslin, Regular
-DM1, DM2 -GDM -DKA -hyperkalemia -stress hyperglycemia (short acting)
NPH
intermediate acting insulin -DM1, DM2, GDM
Glargine and Detemir are…
long acting insulins for DM1, DM2, GDM (basal glucose control)
Metformin (a biguanide) acts to…
-decrease gluconeogenesis -increase glycolysis -increase peripheral glucose uptake (insulin sensitivity)
Use of Metformin
-first line therapy in type 2 DM
Toxicities of Metformin
lactic acidosis (thus contraindicated in renal failure)
First generation sulfonylureas
Tolbutamide Chlorpropamide
Second generation sulfonylureas
Glyburide Glimepiride Glipizide
MOA of Sulfonylureas
close K+ channel in beta-cell membrane so the cell depolarizes triggering insulin release via calcium influx
Use of sulfonylureas
type 2 DM (requires some islet function so useless in T1)
Toxicities of sufonlyureas
-1st gen: disulfiram-like effects -2nd gen: hypoglycemia (esp. in renal failure)
Pioglitazone and Rosiglitazone (glitazones/thiazolidinediones) MOA
increase insulin sensitivity in the peripheral tissues; binds PPAR-gamma nuclear transcription regulator
Use of Pioglitazone and Rosiglitazone
type 2 DM