Diabete's Pharmagology Flashcards

1
Q

Cells in the pancreas that synthesize and secrete glucagon

A

alpha cells

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2
Q

Cells in the pancreas that synthesize and secrete insulin

A

Beta cells

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3
Q

Location in the pancreas where endocrine function occurs

A

Islets of Langerhons

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4
Q

4 stimuli that trigger insulin release

A
  1. Cholinergic transmission
  2. Peptide hormones
  3. AAs
  4. glucose
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5
Q

The biggest stimuli of insulin release

A

Glucose

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6
Q

Transporter that uptakes glucose into beta cells of the pancreas

A

GLUT-2

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7
Q

GTPases that hep to target insulin-containing vesicles to a specific area of the membrane

A

Rab proteins

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8
Q

Proteins located on vesicles that bind calcium and promote docking to the membrane

A

SNAREs

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9
Q

GPCR on beta cell membrane that are activated by acetylcholine released by parasympathetic nerve endings

A

M3R

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10
Q

2 amino acids that can be taken up by beta cells and metabolized via TCA/Kerb’s cycle, increasing ATP

A

Alanine and glutamine

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11
Q

The 3 primary transcription factors for the insulin gene

A
  1. PDX-1
  2. MafA
  3. Beta2/NeuroD
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12
Q

Pathway induced by oxidative stress due to glucotoxicity and causes phosphorylation of key kinases, such as PI3K, deactivating them

A

JNK

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13
Q

Location of GLUT4 (Insulin-dependent)

A

Skeletal muscle and adipose tissue

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14
Q

Receptor that allows the brain to constantly take up glucose without needing insulin

A

GLUT1

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15
Q

The most important antigen in Type I DM

A

Insulin (B chain)

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16
Q

Acute metabolic complication in type I diabetes due to cells metabolizing triglycerides and AAs for energy

A

Ketoacidosis

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17
Q

The primary function of insulin in the vasculature

A

vasodilation

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18
Q

Glucose transporter located in the vascular endothelium

A

GLUT1

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19
Q

Cell adhesion molecules present in the endothelium that are important for the recruitment of macrophages and are decreased by PI3K/AKT pathways that are activated by insulin

A

ICAM-1 and VCAM-1

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20
Q

Important inflammatory cytokines present in insulin resistance that inhibit IRS1,2, eNOS and NO production

A

TNF-alpha and IL-6

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21
Q

MOA of sulfonylureas

A

Block ATP-sensitive K channels, stimulating insulin release from beta cells

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22
Q

3 1st generation sulfonylureas

A

tolbutamide
tolazamide
chlorpropamide

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23
Q

3 2nd generation sulfonylureas

A

glyburide
glipizide
glimpiride

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24
Q

Subunit of K channel that sulfonylureas bind to

A

SUR1 (sulfonylurea receptor 1), a regulatory subunit

25
Q

2 meglitinides

A

repaglinide

nataglinide

26
Q

Major elimination route of meglitinides

A

liver

27
Q

MOA of metformin

A

inhibits mitochondrial respiratory complex-1, increasing AMP

28
Q

MOA of thiazolidinedione

A

Activate PPARs, inducing transcription of genes involved in glucose metabolism

29
Q

2 TZDs

A

rosiglitazone

pioglitazone

30
Q

TZD withdrawn from market due to increased incidence of hepatitis

A

troglitazone

31
Q

MOA of alpha-glucosidase inhibitors

A

Competitively inhibit digestion/absorption of carbs

32
Q

2 alpha-glucosidase inhibitors

A

acarbose

miglitol

33
Q

Peptide hormone that is co-secreted with insulin from pancreatic beta cells that slows gastric emptying, inhibits glucagon release and promotes satiety

A

Amylin

34
Q

Amylin analogue used in conjunction with insulin in type I and type II DM

A

Pramlintide

35
Q

Gut hormones that enhance insulin secretion in an insulin-dependent manner

A

Incretins

36
Q

2 types of incretins

A

GIP

GLP-1

37
Q

Protein that inactivates GLP-1 and GIP by cleaving N-terminal region

A

DPP4

38
Q

2 DPP4-resistant GLP-1 analogues

A

exenatide

liraglutide

39
Q

4 oral DPP4 inhibitors

A

sitagliptan
saxagliptan
linagliptan
alogliptan

40
Q

Primary carbon source of fuel for all organisms

A

Glucose

41
Q

2 main kinases that are involved in signal transduction regulated by glucose in pancreatic beta cells

A

ERK and PI3K/AKT

42
Q

portion of proinsulin that is cleaved off to make insulin

A

chain C

43
Q

Location of insulin receptor

A

ubiquitus

44
Q

Type of receptor that insulin receptor is

A

tyrosine kinase

45
Q

substrates that are recruited to the insulin receptor and activate PI3K

A

IRS1/2

46
Q

Enzyme that inhibits glycogen synthase and is inactivated by insulin, allowing glycogen synthesis

A

GSK3

47
Q

Pathways that is activated by insulin that activates protein synthesis

A

AKT/mTOR

48
Q

Pathway that is involved in increased cell survival via inhibition of apoptosis by insulin action

A

PI3K/AKT

49
Q

Pathway involved in the insulin-induced mitogenic responses (proliferation)

A

MAPK/ERK1,2

50
Q

Primary function of insulin in the brain

A

satiety and appetite regulation

51
Q

Primary function of insulin in the bone

A

stimulates bone formation and decreases osteoclast function

52
Q

Cell surface molecules that bind peptide fragments from pathogens and are presented to thymocytes in the process of positive selection

A

MHC (major histocompatability complex)

53
Q

Pathway that is responsible for increased proliferation and hypertrophy during hyperglycemia due decreased signaling through PI3K pathway

A

Ras/MAPK

54
Q

Product of PI3K signaling that causes relaxation of the vasculature and is antithrombotic

A

NO

55
Q

Potent vasoconstrictor and prothrombotic agent that is produced by RAS/MAPK signaling during hyperinsulinema

A

endothelin

56
Q

Transporter that transports metformin into cells and is highly concentrated in hepatocytes

A

OCT1 (organic cation transporter-1)

57
Q

3 affects of metformin in hepatocytes due to decreased AMP

A
  1. inhibits adenylate cyclase (alters gene expression)
  2. Inhibits FBPase (enzyme in gluconeogenesis)
  3. activates AMPK (inhibits lipid and cholesterol synthesis)
58
Q

3 key genes involved in glucose metabolism that PPAR/RXR induces

A

IRS1,2, PI3K, GLUT4

59
Q

2 mechanisms by which GLP-1 increases insulin secretion in beta-cells

A
  1. upregulates insulin gene transcription

2. increased Ca influx