Pharmacology: Endocrine drugs

Question 1

Lispro

Answer 1

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

Question 2

Aspart

Answer 2

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

Question 3

Regular insulin

Answer 3

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

Question 4

NPH

Answer 4

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

Question 5

Detemir

Answer 5

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

Question 6

Glargine

Answer 6

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

Question 7

Tolbutamide

Answer 7

First generation sulfonylurea

• Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
• Disulfiram-like effects

Question 8

Chlorpropamide

Answer 8

First generation sulfonylurea

• Close K+ATP channel => cell depolarization => Ca2+ influx => insulin release
• Disulfiram-like effects

Question 9

Glyburide

Answer 9

Second generation sulfonylurea

• Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
• Hypoglycemia

Question 10

Glimepiride

Answer 10

Second generation sulfonylurea

• Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
• Hypoglycemia

Question 11

Glipizide

Answer 11

Second generation sulfonylurea

• Close K+ATP channel on pancreatic beta cells => cell depolarization => Ca2+ influx => insulin release
• Hypoglycemia

Question 12

Metformin

Answer 12

Biguanide

• Unk mechanism: DECR gluconeogenesis, incr glycolysis and peripheral glucose uptake/insulin sensitivity
• Lactic acidosis! *Don’t give in RF, check BUN/Cr

Question 13

Pioglitazone

Answer 13

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

Question 14

Rosiglitazone

Answer 14

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

Question 15

Acarbose

Answer 15

alpha-glucosidase inhibitor

• Inhibits intestinal brush border alpha-glucosidases
• Decreases post-prandial hypergly

Question 16

Miglitol

Answer 16

alpha-glucosidase inhibitor

• Inhibits intestinal brush border alpha-glucosidases
• Decreases post-prandial hypergly

Question 17

Pramlintide

Answer 17

Mimetic

- Mimics amylin (secreted with insulin): decr glucagon and inh gastric mobility

Question 18

Exenatide

Answer 18

GLP-1 analog
- Incr insulin, decr glucagon release

GLP-1 (cAMP-coupled R)

• incretin hormone secreted by intestinal L cells in response to food intake
• decreases blood glucose by incr satiety, decr gastric emptying, incr insulin release from pancreatic beta cells

Question 19

Repaglinide

Answer 19

Meglitinide

- Similar to sulfonylureas; bind to different spot on K+ channel

Question 20

Nateglinide

Answer 20

Meglitinide

- Similar to sulfonylureas; bind to different spot on K+ channel

Question 21

Sitagliptine

Answer 21

DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)

Question 22

Vildagliptine

Answer 22

DD4 inhibitor
- DD4 normally degrades GLP-1 (an incretin hormone secreted by intestinal L cells in response to food intake–incr insulin and decr gastric motility and glucagon)

Question 23

PTU vs. Methimazole

Answer 23

PTU: inhibits both peroxidase (thyroid) and 5’-deiodinase (peripheral T4 to T3 conversion), heptatotoxic
Methimazole: inhibits peroxidase only, possible teratogen

Question 24

Levothyroxine

Answer 24

Hypothyroid

Question 25

Perchlorate

Answer 25

Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells - Tx: Hyperthyroid

Question 26

Pertechnetate

Answer 26

Anion, competitively inhibits basolateral Na-I symporter on thyroid follicular cells - Tx: Hyperthyroid

Question 27

Which diabetic drug requires some islet cell function?

Answer 27

Sulfonylureas, because they increase endogenous insulin secretion from beta cells

Question 28

GH

Answer 28

Tx: GH deficiency, Turner's

Question 29

SST

Answer 29

AKA Octreotide | Tx: Acromegaly, carcinoid, gastrinoma, glucaconoma

Question 30

Oxytocin

Answer 30

Stimulates labor, uterine contractions, milk let down; controls uterine hemorrhage

Question 31

ADH (desmopressin)

Answer 31

Pituitary/central DI

Question 32

Demeclocycline

Answer 32

A tetracycline, used to treat SIADH but can cause nephrogenic DI, photosensitivity, bone and teeth abnormalities

Question 33

Hydroxycortisone

Answer 33

Glucocorticoid Indications: Addison's disease, immunosuppression, inflammation, asthma SE: Iatrogenic Cushing's; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

Question 34

Prednisone

Answer 34

Glucocorticoid Indications: Addison's disease, immunosuppression, inflammation, asthma SE: Iatrogenic Cushing's; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

Question 35

Triamcinolone

Answer 35

Glucocorticoid Indications: Addison's disease, immunosuppression, inflammation, asthma SE: Iatrogenic Cushing's; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

Question 36

Dexamethasone

Answer 36

Glucocorticoid Indications: Addison's disease, immunosuppression, inflammation, asthma SE: Iatrogenic Cushing's; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c

Question 37

Beclomethasone

Answer 37

Glucocorticoid Indications: Addison's disease, immunosuppression, inflammation, asthma SE: Iatrogenic Cushing's; adrenal insufficiency, >3 weeks of use/more potent GCs increase risk of insufficiency after d/c