Pharmacology: Endocrine drugs Flashcards
1
Q
Lispro
A
Rapid-acting insulin
- Binds insulin R (cell surface receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
2
Q
Aspart
A
Rapid-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
3
Q
Regular insulin
A
Short-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
4
Q
NPH
A
Intermediate-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
5
Q
Detemir
A
Long-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
6
Q
Glargine
A
Long-acting insulin
- Binds insulin R (receptor tyrosine kinase with intrinsic activity, MAP kinase)
- Liver: incr glycogen storage
- Muscle: incr glycogen and protein synthesis, K+ uptake (**Shift K* IN!)
- Fat: incr TG storage
7
Q
Tolbutamide
A
First generation sulfonylurea
- Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
- Disulfiram-like effects
8
Q
Chlorpropamide
A
First generation sulfonylurea
- Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
- Disulfiram-like effects
9
Q
Glyburide
A
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
10
Q
Glimepiride
A
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
11
Q
Glipizide
A
Second generation sulfonylurea
- Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
- Hypoglycemia
12
Q
Metformin
A
Biguanide
- Unk mechanism: DECR gluconeogenesis, incr glycolysis and peripheral glucose uptake/insulin sensitivity
- Lactic acidosis! *Don’t give in RF, check BUN/Cr
13
Q
Pioglitazone
A
Glitazone/thiazolidinedione
- Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
- Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
- SEs: weight gain (from fluid), edema (caution in CHF), hepatotoxity (check LFTs!), heart failure.
- NO hypoglycemia
14
Q
Rosiglitazone
A
Glitazone/thiazolidinedione
- Bind to nuclear PPAR-gamma (peroxisome proliferator-activated receptor), in family of steroid and thyroid nuclear receptors, affects transcription
- Effects: 1) incr adiponectin, 2) incr FA transport protein, 3) incr insulin R substrate, 4) incr Glut4
- SEs: weight gain, edema, hepatotoxity, heart failure.
- NO hypoglycemia
15
Q
Acarbose
A
alpha-glucosidase inhibitor
- Inhibits intestinal brush border alpha-glucosidases
- Decreases post-prandial hypergly