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Med Chem 7 > Antidiabetics (2) > Flashcards

Antidiabetics (2) Flashcards

(75 cards)

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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
Glinide side effects
weight gain \*\*less long term side effects
26
First gen insulinotropic drugs metabolism
extensively metabolized primarily excreted by kidney
27
Describe the possible metabolism sites
28
Is this first gen or second gen?
first gen
29
is this first gen or second gen?
2nd gen
30
Describe the possible metabolism sites
31
Insulin sensitizing agents
biguanidines thiazolidinediones
32
Metforming is what type of drug?
biguanidine: insulin sensitizing agent
33
What type of drug is this?
biguanidines: insulin sensitizing agent
34
T/F biguanidines can be used for T1D
False! T2D only!
35
How do biguanidines work?
activate AMPK --\> GLUT4 translocation \*\*insulin independent glucose uptake
36
AMPK
liver enzyme important role in insulin signiling, whole body energy balance and metabolism of glucose and fats
37
What is the only oral med approved for T2D in children?
biguanidines: Metformin
38
What drug was removed from the market for causing lactic acidosis?
biguanidines
39
Side effects of biguanidines
GI: N/D/anorexia Lactic acidosis
40
Metformin metabolism
excreted unchanged by tubular secretion
41
Phenformin metabolism
aromatic hydroxylation
42
Which part is required for activity?
guanidine
43
(SAR) R1
arylaklyl most potent increase activity to n-pentyl decrease with long length, branching or cyclic
44
(SAR) R2
H CH3: highest potency
45
What drugs are known as insulin enhancers?
thiazolidinediones (glitazones)
46
Glitazones MOA
PPARy agonists: increase insulin sensitivity Decrease BG Decrease FFA Decrease TG levels
47
What is the key component?
48
T/F glitazones are for T2D
True
49
What type of drug is this?
glitazone
50
Why was troglitazone withdrawn from the market?
increased hepatoxicity
51
What 2 studies did EMEA do in rosiglitazone?
1. chronic heart failure 2. cardiovascular effects
52
What drugs did the DREAM trial study?
glitazones prediabetic on Avandia
53
DREAM study conclusion
Avandia prevented diabetes \*\*not the case afterwards \* didn't rejuvenate B cells
54
What other things did the DREAM study find?
Avandia had increase heart attacks, strokes and deaths from cardiovascular problems
55
Meta-anlysis of glitazones initial report
avandia increase cardiac risks BBW for heart failure
56
Meta-analysis of glitazones final conclusion
Duke found no incrase in heart attacks
57
How is pioglitazone used?
alone or combo with sulfonylurea, metformin or insulin
58
T/f pioglitazone is associated with increased irk of heart attacks, stroke or death
False! not associated
59
What is another use for pioglitazone?
depression
60
What drug has a link to bladder cancer?
pioglitazone
61
T/F diabetics already have an increased risk of bladder cancer and actos adds to that risk
true
62
structure of PPAR
PPARa PPARy PPARd
63
\_\_\_\_% of the 34 residues of PPAR are conserved
80%
64
Side effects of glitazones
weight gain minor edema
65
Who is not recommended to take glitazones?
those with moderate to severe heart failure
66
Describe the metabolism that can occur
67
Describe the metabolism that can occur
68
Which part is more flexible?
Left side
69
Glitazars MOA
Dual alpha/gamma PPAR activator
70
t/f glitazars are approved for use
false
71
What groups of drugs are insulin sensitizers?
biguanidines thiazolidines glitazars
72
What groups of drugs are insulin secretagogues?
sulfonylureas glinides GLP-1 analogs incretins DDP-4 inhibitors
73
What drugs are thiazolidines?
pioglitazone rosiglitazone
74
What drugs are sulfonylureas?
glipizide gilburide tolbutamide
75
what drugs are glinides?
nateglinide repaglinide

Med Chem 7 (9 decks)

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