Endocrine drugs Flashcards Preview

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Flashcards in Endocrine drugs Deck (36):
1

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)

2

Clinical use of lispro, aspart and glulisine

-DM1 -DM2 -GDM (postprandial glucose control)

3

Use of Inuslin, Regular

-DM1, DM2 -GDM -DKA -hyperkalemia -stress hyperglycemia (short acting)

4

NPH

intermediate acting insulin -DM1, DM2, GDM

5

Glargine and Detemir are...

long acting insulins for DM1, DM2, GDM (basal glucose control)

6

Metformin (a biguanide) acts to...

-decrease gluconeogenesis -increase glycolysis -increase peripheral glucose uptake (insulin sensitivity)

7

Use of Metformin

-first line therapy in type 2 DM

8

Toxicities of Metformin

lactic acidosis (thus contraindicated in renal failure)

9

First generation sulfonylureas

Tolbutamide Chlorpropamide

10

Second generation sulfonylureas

Glyburide Glimepiride Glipizide

11

MOA of Sulfonylureas

close K+ channel in beta-cell membrane so the cell depolarizes triggering insulin release via calcium influx

12

Use of sulfonylureas

type 2 DM (requires some islet function so useless in T1)

13

Toxicities of sufonlyureas

-1st gen: disulfiram-like effects -2nd gen: hypoglycemia (esp. in renal failure)

14

Pioglitazone and Rosiglitazone (glitazones/thiazolidinediones) MOA

increase insulin sensitivity in the peripheral tissues; binds PPAR-gamma nuclear transcription regulator

15

Use of Pioglitazone and Rosiglitazone

type 2 DM

16

Toxicities of Pioglitazone and Rosiglitazone

-weight gain -edema -hepatotoxicity -HEART FAILURE

17

Acarbose and Miglitol (alpha-glucosidase inhibitors) MOA

-inhibit intestinal brush-border alpha-glucosidases -delayed sugar hydrolysis and glucose absorption leading to decreased postprandial hyperglycemia

18

Acarbose and Miglitol uses

type 2 DM

19

Pramlintide is an amylin analog that...

decreases gastric emptying and decreases glucagon. Used in T1 and T2 DM.

20

Exenatide and Liraglutide are...

GLP-1 analogs that increase insulin and decrease glucagon release. Used in T2 diabetes.

21

Toxicity of exenatide and liraglutide

pancreatitis

22

Linagliptin, Saxagliptin and Sitagliptin are..

DPP-4 inhibitors that increase insulin and decrease glucagon release used in T2DM.

23

Genes activated by PPAR-gamma regulate...

fatty acid storage and glucose metabolism. Activation of PPAR-gamma increase insulin sensitivty and levels of adiponectin.

24

Propylthiouracil and Methimazole MOA

block thyroid peroxidase, inhibiting the oxidation of iodide and organification of iodine leading to inhibition of thyroid hormone synthesis.

25

PTU also blocks...

5'-deiodinase which decreases peripheral conversion of T4 to T3. (used in pregnancy)

26

Use of Methimazole and PTU

Hyperthyroidism

27

Toxicity of PTU and Methimazole

-skin rash -agranulocytosis -aplastic anemia -teratogen (Methimazole can cause aplasia cutis)

28

Levothryoxine and Triiodothyronine are used for...

hypothyroidism and myxedema.

29

GH is used in...

GH deficiency and Turner syndrome.

30

Somatostatin (octreotide) is used in...

acromegaly, carcinoid, gastinoma, glucagonoma and esophageal varices.

31

Oxytocin stimulates...

labor, uterine contractions and milk letdown; it controls uterine hemorrhage too.

32

ADH (DDAVP) is used for...

pituitary DI.

33

Glucocorticoids (6)

1. hydrocortisone 2. prednisone 3. triamcinolone 4. dexamethasone 5. beclomethasone 6. fludrocortisone

34

Mechanism of glucocorticoids

metabolic, catabolic, anti-inflammatory, and immmunosuppressive effects are mediated by interactions with the glucocorticoid response elements and inhibition of transcription factors such as NF-kappaB.

35

Use of glucocorticoids

-addison disease -inflammation -immune suppression -asthma

36

Toxicity of Glucocorticoids

-iatrogenic Cushings -adrenal insufficiency when drugs are stopped abruptly after chronic use