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Med Chem 7 > Antidiabetics (2) > Flashcards

Antidiabetics (2) Flashcards

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1
Q

Insulintropic agents

A

sulfonylureas

glinides

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2
Q

3 isoforms of SUR

A

SUR1

SUR2A

SUR2B

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3
Q

SUR1

A

regulatory subunit of K ATP channels in B cells

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4
Q

SUR2A

A

represent sulphonylurea receptor in heart and skeletal muscle

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5
Q

SUR2B

A

sulphonylurea receptor in smooth muscle

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6
Q

K ATP channels in pancreas

A

Open and bound to ADP at baseline

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7
Q

K ATP channels in pancreas with sulfonylureas

A

Activate SUR1

Close ATP sensitive channels –> depolarization

Open Ca2 channels –> exocytosis of insulin

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8
Q

Which SUR is in B cells?

A

SUR1

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9
Q

Which SUR is in heart and skeletal muscle?

A

SUR2A

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10
Q

Which SUR is in smooth muscle?

A

SUR2B

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11
Q

In the heart or endothelial cells are the K ATP channels open or closed?

What effect does sulphonylureas have?

A

closed

Open channels

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12
Q

What type of drug is this?

Is it 1st or 2nd gen?

A

Sulfonylurea

1st gen

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13
Q

What type of drug is this?

Is it 1st gen or 2nd gen

A

Sulfonylurea

2nd gen

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14
Q

When are sulfonylureas given?

A

after meal

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15
Q

When are glinides given?

A

before meals

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16
Q

glinide MOA

A

activate SUR1

close pancreatic B cell K ATP channels

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17
Q

What type of drug is this?

A

Glinide

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18
Q

Common features of insulinotropic activity drugs

A
  1. aromatic tail with ortho substituent
  2. acidic group
  3. pnehyl ring
  4. pendant lipophilic group
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19
Q

Does A or B have higher selectivity for specific SUR receptors?

A

A

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20
Q

What shape do sulfonylureas have?

A

U shaped conformation (right angle)

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21
Q

Which site is SUR1 selective?

A

i. of A site

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22
Q

What bonds could form at the arrows?

A

H bonds

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23
Q

What is critical?

A

spacing between anionic group and amide nitrogen

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24
Q

Side effects of sulfonylureas

A

Hypoglycemia

body weight gain

**generally well tolerated

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25
Q

Glinide side effects

A

weight gain

**less long term side effects

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26
Q

First gen insulinotropic drugs metabolism

A

extensively metabolized

primarily excreted by kidney

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27
Q

Describe the possible metabolism sites

A
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28
Q

Is this first gen or second gen?

A

first gen

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29
Q

is this first gen or second gen?

A

2nd gen

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30
Q

Describe the possible metabolism sites

A
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31
Q

Insulin sensitizing agents

A

biguanidines

thiazolidinediones

32
Q

Metforming is what type of drug?

A

biguanidine: insulin sensitizing agent

33
Q

What type of drug is this?

A

biguanidines: insulin sensitizing agent

34
Q

T/F biguanidines can be used for T1D

A

False! T2D only!

35
Q

How do biguanidines work?

A

activate AMPK –> GLUT4 translocation

**insulin independent glucose uptake

36
Q

AMPK

A

liver enzyme

important role in insulin signiling, whole body energy balance and metabolism of glucose and fats

37
Q

What is the only oral med approved for T2D in children?

A

biguanidines: Metformin

38
Q

What drug was removed from the market for causing lactic acidosis?

A

biguanidines

39
Q

Side effects of biguanidines

A

GI: N/D/anorexia

Lactic acidosis

40
Q

Metformin metabolism

A

excreted unchanged by tubular secretion

41
Q

Phenformin metabolism

A

aromatic hydroxylation

42
Q

Which part is required for activity?

A

guanidine

43
Q

(SAR) R1

A

arylaklyl most potent

increase activity to n-pentyl

decrease with long length, branching or cyclic

44
Q

(SAR) R2

A

H

CH3: highest potency

45
Q

What drugs are known as insulin enhancers?

A

thiazolidinediones (glitazones)

46
Q

Glitazones MOA

A

PPARy agonists:

increase insulin sensitivity

Decrease BG

Decrease FFA

Decrease TG levels

47
Q

What is the key component?

A
48
Q

T/F glitazones are for T2D

A

True

49
Q

What type of drug is this?

A

glitazone

50
Q

Why was troglitazone withdrawn from the market?

A

increased hepatoxicity

51
Q

What 2 studies did EMEA do in rosiglitazone?

A
  1. chronic heart failure
  2. cardiovascular effects
52
Q

What drugs did the DREAM trial study?

A

glitazones

prediabetic on Avandia

53
Q

DREAM study conclusion

A

Avandia prevented diabetes

**not the case afterwards

* didn’t rejuvenate B cells

54
Q

What other things did the DREAM study find?

A

Avandia had increase heart attacks, strokes and deaths from cardiovascular problems

55
Q

Meta-anlysis of glitazones initial report

A

avandia increase cardiac risks

BBW for heart failure

56
Q

Meta-analysis of glitazones final conclusion

A

Duke found no incrase in heart attacks

57
Q

How is pioglitazone used?

A

alone or combo with sulfonylurea, metformin or insulin

58
Q

T/f pioglitazone is associated with increased irk of heart attacks, stroke or death

A

False!

not associated

59
Q

What is another use for pioglitazone?

A

depression

60
Q

What drug has a link to bladder cancer?

A

pioglitazone

61
Q

T/F diabetics already have an increased risk of bladder cancer and actos adds to that risk

A

true

62
Q

structure of PPAR

A

PPARa

PPARy

PPARd

63
Q

____% of the 34 residues of PPAR are conserved

A

80%

64
Q

Side effects of glitazones

A

weight gain

minor edema

65
Q

Who is not recommended to take glitazones?

A

those with moderate to severe heart failure

66
Q

Describe the metabolism that can occur

A
67
Q

Describe the metabolism that can occur

A
68
Q

Which part is more flexible?

A

Left side

69
Q

Glitazars MOA

A

Dual alpha/gamma PPAR activator

70
Q

t/f glitazars are approved for use

A

false

71
Q

What groups of drugs are insulin sensitizers?

A

biguanidines

thiazolidines

glitazars

72
Q

What groups of drugs are insulin secretagogues?

A

sulfonylureas

glinides

GLP-1 analogs incretins

DDP-4 inhibitors

73
Q

What drugs are thiazolidines?

A

pioglitazone

rosiglitazone

74
Q

What drugs are sulfonylureas?

A

glipizide

gilburide

tolbutamide

75
Q

what drugs are glinides?

A

nateglinide

repaglinide

Med Chem 7 (9 decks)

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