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Med Chem 7 > Antidiabetics I > Flashcards

Antidiabetics I Flashcards

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1
Q

What type of disorder is diabetes?

A

metabolic

hyperglycemia

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2
Q

Diabetes occurs when what 2 things happen?

A
  1. pancreas does not produce enough insulin

2. body cannot effectively use insulin it produces

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3
Q

4 types of diabetes

A
  1. T1D
  2. T2D
  3. gestational diabetes
    other: impaired glucose tolerance and impaired fasting glycemia
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4
Q

What type of diabetes is insulin dependent?

A

T1D

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5
Q

What can cause T1D?

A

B cells destroyed
autoimmune
viral

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6
Q

What type of diabetes is characterized by insulin resistance?

A

T2D

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7
Q

In normal population insulin secretion is _____ to insulin sensitivity

A

inversely proportional

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8
Q

Genetic defects of B cell function could be what?

A

MODY (maturity onset diabetes of young)

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9
Q

What is MODY?

A

several hereditary forms of diabetes caused by mutations in autosomal dominant gene

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10
Q

Gestational diabetes can cause increased risk of

A

pre-eclampsia
depression
require C section

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11
Q

What is the current rate of diabetes in America and what is it predicted to be in 2050?

A

1/10

1/3

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12
Q

T/f diabetes is related to low income

A

true

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13
Q

t/f India has about 1/3 of the world’s diabetes

A

false

China

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14
Q

significant complications from diabetes

A
  • CVD
  • nerve damage
  • kidney damage
  • foot damage
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15
Q

insulin brings glucose where?

A
  • liver
  • fat
  • muscle cells
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16
Q

4 treatments of hyperglycemia

A
  1. insulin and its analogs
  2. insulinotropic agents
  3. insulin sensitizing agents
  4. a-glucosidase inhibitors
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17
Q

t/f insulin administration is the only effective treatment for T2D

A

false

T1D

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18
Q

When is insulin useful for T2D?

A

when poor B cell function limits efficacy of oral meds

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19
Q

2 major side effects of insulin

A

hypoglycemia

weight gain

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20
Q

What is the major limiting factor of glycemic management

A

hypoglycemia

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21
Q

t/f the frequency of hypoglycemia increases with intensive conventional regiments

A

true

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22
Q

What type of hormone is insulin?

A

polypeptide

23
Q

Insulin is formed after elimination of what?

A

c peptide by hydrolysis

24
Q

Insulin is recreated by what cells?

A

B cells of islets of langherans of pancreas

25
Q

What type of peptides does insulin belong to?

A

IGF

26
Q

Insulin structure

A

A chain: 21AA
B chain: 30AA

connected by 2 disulfide bridges

27
Q

Human insulin has close homology with _____ and ____

A

pig (1AA)

cow (3AA)

28
Q

How are the chains of insulin assembled?

A

post-translational modification

with disulfide bridge formation

29
Q

What two forms can insulin be in?

A

dimer

hexamer

30
Q

How does insulin form dimers?

A

H bonding

31
Q

How does insulin form hexameters?

A

zinc ions

32
Q

The design of insulin analogs has emphasized _______ or ______ of structural elements according to established principles of _______

A

stabilization or destabilization

protein folding

33
Q

(SAR) What are good sites of modification of insulin?

A

solvent exposed side chain extrinsic to receptor binding surface

34
Q

(SAR) What has been studied to assess it ability to form dimers or hexameters and activate insulin receptors?

A

different sequences

35
Q

(SAR) Modify insulin to change what?

A

ADME

Fast or slow insulin analogs

36
Q

What type of interactions are in insulin?

A

dimer dimer contacts

monomer monomer interactions

37
Q

T/f residues involved in interaction with receptor of insulin cannot be modified

A

true

38
Q

Non-hexomeric insulins

A

NPH
Lisper
Aspart
Glulisine

39
Q

Shifted isoelectric point insulins

A

glargine

detemir

40
Q

Which insulin has a suspension of crystalline zinc porcine insulin?

A

NPH (non-hexomeric)

41
Q

Which insulin has a high affinity for serum albumin?

A

detemir

42
Q

New long acting insulins

A

Toujeo
Tresiba
Ryzodeg

43
Q

How long do new long acting insulins last?

A

up to 42 hours

44
Q

What was the 1st fast acting insulin analog engineered by recombinant DNA tech?

A

lispro

45
Q

Which insulin enhances hexamer formation without Zn in formula?

A

glargine

46
Q

Why are shifted isoelectric point insulins used for?

A

replace basal level of insulin

may be effective over period of 24h

47
Q

How do smart insulins work?

A

circulates in blood, turns on when BG is high

Turns back off when in safe zone

48
Q

Smart insulins are chemically attached to a _____ polymer with sticky sugar groups. This is mixed with a ____ binding molecule.

A

biodegradable

sugar

49
Q

The insulin polypeptides in smart insulin comprise a ____ motif that enables the _____ expression of glycosylated insulin polypeptides

A

N linked glycan

recombinant

50
Q

The glycosylated insulin conjugates of smart insulin will be sensitive to ______

A

serum concentrations of glucose

51
Q

What is important to know about smart insulin pump?

A

automatically adjusts insulin levels

- users need to manually adjust when high carb meal

52
Q

What are biosimilars?

A

generic copy of biologics

53
Q

Current biosimilar products

A
  • EPO products
  • growth factors
  • insulins Biocon

Med Chem 7 (9 decks)

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