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Flashcards in Pharm Exam 3 MOA Only Deck (22):
1

a Glucosidase Inhibitors

- Are carbohydrate analogs that bind reversibly and with much greater affinity than carbs to GS
- Delays the absorption of carbohydrates making it effective in decreasing the after meal glucose spike
- Metabolism occurs within the GI tract
- generally considered to be additive to other antidiabetics

2

Biguanides

- Reduced gluconeogenesis by activating AMPK
- Increase insulin action in muscle and fat through AMPK
- Delayed glucose absorption in the GI tract
- Direct stimulation of glycolysis in tissue with increased removal of glucose from blood
- Reduced plasma glucagon

3

Incretins

- GLP-1 and GIP stimulate insulin release in response to elevated blood glucose
- GLP-1 lowers glucagon secretion, slows gastric emptying and regulates beta cell growth
- DPP-4 inactivates GLP-1 and GIP
- Gliptins inhibit DDP-4
- Incretin Mimetics cannot be broken down by DPP-4
- Incretin effect - Oral glucose is more effective at stimulating insulin release than IV administered because GLP-1 and GIP are secreted in the bowel

4

Insulin

- Mobilizes GLUT-4 transporters on fat and muscle cells
- Increased glycogen synthesis in liver and muscle
- Inhibits gluconeogenesis in the liver
- Muscle it increases the uptake of amino acids for protein synthesis
- Adipose it promotes the synthesis of triglycerides and inhibits lipolysis

5

Meglitinides

- Stimulate the release of insulin
- Bind to beta cells at the SUR-1 receptor
- Opening of the ATP sensitive K channel
- Depolarizes the cell resulting in Ca++ release
- Ca++ initiates exocytosis of insulin
- Relies on functioning beta cells so it is not used in DM1
- Short onset allows it to be used before meals to decrease glucose spike

6

Sulfonylureas

- Stimulate the release of insulin
- Bind to beta cells at the SUR-1 receptor
- Opening of the ATP sensitive K channel
- Depolarizes the cell resulting in Ca++ release
- Ca++ initiates exocytosis of insulin
- Relies on functioning beta cells so it is not used in DM1

7

Thiazolidinediones

- Peroxisome proliferator activated receptor- gamma agonists (PPAR-y)
- PPAR-y receptors are found in the nucleus of muscle, fat and liver cells
- PPAR-y recdeptors are responsible for lipid and protein metabolism, insulin signal transduction, tissue differentiation
- Promote uptake and storage of FFA's
- Promote expression and translocation of glucose transporters
- Stimulation of adiponectin which increases glucose uptake, inhibits atherosclerosis and endothelial apoptosis, stabilizes plaques

8

Glucagon

- Secretion is controlled by the Sympathetic NS
- Works through cAMP
- Increases glycogenolysis
- Decreased glycogen synthesis
- Increased glycolysis
- Increased ketogenesis

9

Somatostatin analogs

- Acts on the somatostatin Receptors s1-S5
- Secreted by the delta cells
- Reduces secretion of GH. Insulin, Glucagon, Gastrin, VIP and pancreatic enzymes
- Lowers portal BP by vasoconstriction leading to decreased blood flow to the liver

10

GH Antagonists

- Block the action of GH at the liver
- Blocks the release of IGF-1 which works on bone, and soft tissues
- GH is an Insulin antagonist

11

ACTH

- Acts though cAMP activation to produce cortisol in the ZF

12

Thyroid replacements

- Replacement of T4

13

Antithyroids

Thioamides
- Inhibit thyroid perioxidase
- Block iodine oxidation
- Block the coupling of iodinated tyrosines
- Inhibit peripheral iodination of T3 and T4
- Do not block the uptake of iodine
Radioactive Iodine 131I
- Destroys the thyroid gland through radiation

14

Steroids as Immune Modifiers

- Decreasing the number of white blood cells
- reduce the function of macrophages and lymphocytes
- Reduced function on phospholipase A2 resulting in reduced mediators of inflamation

15

B Cell biologics

- Either destroy the B Cell or decrease its function
- Blockage of CD20 results in apoptosis
- Blocking of the cytokines which stimulate B Cell activity will decrease the function of B Cells
- CD20 is expressed only of B Cells

16

T Cell Biologics

- CD3 is expressed on all T cells, targeting it will nonspecifically inhibit all T cells
- CD25 is the IL-2 receptor. Decreased IL-2 leads to decreased inflammation.
* Expressed on Treg cells which suppress Autoreactive T cells so the benefit must out weigh the cost
- CTLA-4 is a costimulator of T cells, its inhibition will decrease the activation of T cells

17

Mixed Biologics

- CD52 located on both T and B cells. Targeting of it by mAbs results in prolonged T and B cell Depletion.
- IL6 - Receptor. Targeting this does not destroy lymphocytes but can inhibit them

18

TNF-a

- Reduces the inflammatory process and releases cytotoxic agents

19

Antimetabolites

- Act in several ways but the end result is reduced DNA and RNA synthesis
- T and B cells are highly sensitive because they must produce their own (de novo) purines

20

Calcineurin Inhibitors

- Act on T cells
- Calcineurin binds to NFAT to dephosporalate it which allows it to bind to T cell DNA resulting in production of IL-2 which matures the T cell
- Calcineurin inhibitors prevent this process

21

mTOR Inhibitors

- Binds to FKBP-12 in the cytoplasm, this complex then inhibits mTOR
- Impede VGEF
- Block the action of IL-2

22

Glatiramoids

- Binds to MHC class II
- Induces T helper 2 suppressive cells