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Management of GI and Endocrine Conditions > Lecture 21 - Chemistry of Oral Antidiabetics > Flashcards

Lecture 21 - Chemistry of Oral Antidiabetics Flashcards

1
Q

What are the classes of oral antidiabetics?

A 
biguanides 
sulfonylureas
glitazone 
gliptins 
GLP-1 agonists (not oral)
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2
Q

What are the biguanides?

A

metformin

buformin

phenformin

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3
Q

Structure of biguanides?

A

highly charged, highly hydrophilic and very basic

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4
Q

Effect of metformin?

A

mainly due to the inhibition of hepatic glucose output

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5
Q

What is the presumed site of metformin function?

A

the liver

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6
Q

Metabolism of metformin?

A

not metabolised and is unchanged throughout the journey in the body

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7
Q

What is most used to treat T2D?

A

Metformin

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8
Q

Why were buformin and phenformin withdrawn?

A

they had toxicity associated and caused acidosis

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9
Q

What is the high basic pKa of biguanides due to?

A

resonance forms of biguanide stabilising the conjugate acid positive charge so the equilibrium lies to the left

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10
Q

Route of metformin?

A

orally active so must be active uptake mechanism

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11
Q

1st generation sulfonylureas?

A

chlopromide

tolbutamide

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12
Q

2nd generation sulfonylureas?

A

gliquidone

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13
Q

What is the NH attached to sulphur and carbonyl in sulfornylureas?

A

weakly acidic

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14
Q

Other sulfonylureas?

A

glibenclamide and glimepiride

gliclazide and glipizide

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15
Q

What are the oldest hypoglycaemia agents?

A

sulfonylureas

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16
Q

How do sulfonylureas work?

A

stimulate insulin secretion by binding to sulfonylurea receptor 1 (SUR-1) sub unit of the ATP sensitive K channels in the beta cell plasma membrane

17
Q

How are sulfonylureas classes?

A

first and second generation

18
Q

What are sulfonylureas associated with?

A

weight gain and hypoglycaemia

19
Q

Can sulfonylureas be used with metformin?

A

yes

20
Q

Meglitinides?

A

nateglinide

repaglinide

21
Q

How do meglitinides work?

A

in a similar manner to sulfonylureas

stimulate insulin secretion by binding to sulfonylurea receptor 1 (SUR-1) sub unit of the ATP sensitive K channels in the beta cell plasma membrane

22
Q

What do meglitinides have?

A

weaker binding and dissociation from the SUR-1 binding site of the ATP sensitive K channel

23
Q

Glitazones?

A

rosiglitazone

pioglitazone

24
Q

What do glitazones posses?

A

the thiazolidinedione moiety

25
Q

How to glitazones work?

A

activate the gamma isoform of the peroxisome proliferator-activated receptor PPAR gamma

26
Q

What does activation of PPAR gamma do?

A

improve insulin sensitivity

27
Q

GLP-1 agonists?

A

exenatide

not oral

28
Q

Why are GLP-1 agonists not oral?

A

huge molecular weight, pKa etc
it is a large polypeptide

do not satisfy Lipinski’s rule of 5

29
Q

What is exenatide?

A

a synthetic mimic for GLP-1

30
Q

What is exenatide classed as?

A

an incretin mimic

31
Q

What breaks down GLP-1?

A

DPP4

32
Q

Why does DPP4 not break down exenatide?

A

it is slightly different so is not broken down as fast but stimulates insulin release

33
Q

How is exenatide given?

A

as a subcutaneous injection

34
Q

Gliptins?

A

DPP4 inhibitors

sitagliptin
vildagliptin

35
Q

What are gliptins?

A

DPP4 inhibitors

36
Q

What does DPP4 do?

A

acts on GLP-1 and GIP to inactivate the

37
Q

When are GLP-1 and GIP released?

A

after food intake in the intestine and stimulate insulin production

38
Q

What does inhibition of DPP4 do?

A

stimulates insulin secretion

39
Q

What did the SIPBS drug cause?

A

weight loss and uptake of glucose in mice

possible interaction with phosphatases in beta cells

some toxicity in mice

Management of GI and Endocrine Conditions (24 decks)

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