EXAM 4 Drugs Pt2 Dr. Hess Flashcards
MOA of DPP-4 inhibitors
blocking Dipeptidyl peptidase-4
-> DPP-4 is enzyme that degrades endogeounes GLP-1 and GIP
GLP-1 works on the pancreas an increases insulin release and decreases glucagon release
How is the endogenous GLP-1 different from GLP-1 receptor agonists?
the GLP-1 receptor agonist also decreases and suppresses appetite and increases satiety
Which drug should not be used together with DPP-4 inhibitors?
GLP-1 receptor agonists -> overlay in the MOA
-no synergistic effect
-also insulin and Sulfonylurea -> increase the risk for hypoglycemia (despite alone having a low risk of hypoglycemia)
What is the efficacy of DPP-4-i?
0.5 - 0.8% (moderate)
Low hypoglycemia risk (glucose-dependent activity of endogenous GLP-1)
ADE of DPP-4-i
not many
in rare cases:
-upper respiratory infection
-skin reactions
-joint pain
How are DPP-4 inhibitors dosed?
-daily dose
-no titration
-may need dose adjustment (except from Tradjenta (linagliptin))
Which DPP-4 inhibitor does not require any renal dose adjustments?
Tradjenta
Which DPP 4 inhibitors increase the risk for HF hospitalization?
Onglyza (Saxagliptin)
Nesina
MOA of TZDs
activating nuclear transcription factor PPARγ -> increases the synthesis of GLUT4 transporter
-> enhances insulin sensitivity
On which cell do TZDs work?
not in the pancreas
-Muscle cells
-Adipose tissue
-Liver cell (like metformin)
How long does it take for TZDs to reach their effect?
6-8 weeks
can be used with metformin (both insulin sensitizers)
What are the precautions for Pioglitazone?
in patients with NYHF class III & IV
-hx of HF
-LFT > 2.5x ULN
What is the BBW for Pioglitazone?
can cause exercabtion of HF
Side effects of TZDs
-edema, weight gain
-macular edema
-HF
-bone fractures
-bladder cancer
MOA for Sulfonylureas
closes ATP-K channels on ß-cells -> leading to glucose INDEPENDENT insulin secretion