Diabetic pharmacology Flashcards
Name the insulin analogues
Lispro
Aspart
Glulisine
What is the onset of Lispro, Aspart and Glulisine
15 min
What is the Peak of Lispro, Aspart and Glulisine
0.5- 1.5 hrs
What is the Duration of Lispro, Aspart and Glulisine
3-5 hrs.
What is the onset of human insulin
0.5-1 hr
What is the Peak of human insulin
2-3 hrs
What is the duration of human insulin
5-8 hrs
What is the onset human NPH/Lente
1-3 hrs
What is the peak of human NPH/Lente
4-8 hrs
What is the duration of human NPH/Lente
8-20 hrs
What is the onset of human ultralente
4-8 hrs
What is the Peak of ultralente
8-12 hrs
What is the duration of ultralente
18-36 hrs
What is the onset of glargine, determir
1-2 hrs
What is the peak of glargine, determir
Flat
What is the duration of glargine, determir
24 hrs
Name the 2nd generation sulfonylureas
Glyburide
Glipizide
Glimepiride
What is the MOA of the sulfonylureas
stimulates insulin secretion from pancreatic islet beta cells
- Inhibits SUR1 ATP-sensitive potassium channels on beta cells
- Does NOT decrease insulin resistance
Thiazide diuretics have what effect on sulfonylureas
excretes it from blood
*Must increase the dose of sulfonylurea
Renal disease has what effect on sulfonylureas
decreases elimination
Meglitinides are the newer oral diabetic agents and include which drugs
“NIDEs”
Repaglinide
Netaglinide
Miglitinide
What is the MOA of Meglitinides
Stimulates insulin secretion from beta cell
*Same MOA as sulfonylurea but peaks in 1 hour and shorter DOA of 4 hours
Meglitinides are active ONLY
in the presence of glucose
*less risk of hypoglycemic episodes
What is the major Biguanides
Metformin
What is the MOA of metformin
Decrease hepatic glucose production
Decreases absorption from gut
Increases insulin sensitivity in skeletal muscles and adipose tissue
*Does NOT stimulate insulin secretion
What are the adverse effects associated with metformin
Hypoglycemia (rare)
Diarrhea (20%)
Lactic acidosis
Why does metformin cause lactic acidosis
Blocks mitochondrial membranes preventing mitochondria from converting pyruvate to acetyl-CoA and oxidation
What are alpha glucosidase
enzymes that breakdown starch and dissacharides into glucose
What are the a-Glucosidase inhibitors
Acarbose
Miglitol
Voglibose
Where do a-Glucosidase inhibitors exert their effects in the body
On the enzymes in intestinal brush border
What are a-glucosidase inhibitors used for
to prevent post-prandial hyperglycemia
What are the PPAR gama-agonists
“litazones”
Why were the PPAR gama-agonists pulled off the market
Cause CHF, MI
What is amylin
a polypeptide cosecreted with insulin from the pancreatic beta cells responsible for slowing gastric emptying, suppressing glucagon, and promoting satiety
What drug mimics amylin
Pramlintide
Amylin is —— in diabetics
deficient
What are incretins
a group of GI hormones that stimulate insulin release and inhibits glucagon release with net effect of lowering blood glucose
*Glucagon-like polypeptide-1 (GLP-1)
What inactivates incretins
DPP-4
What are the drugs designed to MIMIC incretins
Liraglutide
Exenatide
Taspoglutide
GLP-1 activity is similar to amylin activity in what three ways
Suppresses glucagon secretion from pancreatic alpha cells
slows gastric emptying
Promotes satiety
What are the two additional MOA of GLP-1 that distinguishes it from the amylins
Improves insulin sensitivity
Stimulates insulin secretion from pancreatic beta cells
Exenatide does what to the hemoglobin A1c levels
decreases it by 1%
Exenatide does what for weight
decreases by 2.5 kg or 5 lbs
exenatide is associated with what disease
acute pancreatitis
*don’t give to patients with severe abdominal pain radiating to back and vomiting
What is DPP-4
The enzyme that inactivates incretins
What are the DPP-4 inhibitors
“…gliptins”
What are the concerns with Vildagliptin
Skin lesions
Bowel CA
Lung CA
What is Sodium Glucose Transporter 2 (SGLT-2)
Receptors found on proximal kidney tubules that reabsorb glucose from ultrafiltrate regardless of hyperglycemia
What are the SGLT-2 inhibitors
“…liflozin”
