Antidiabetics I Flashcards

(53 cards)

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?

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
What type of peptides does insulin belong to?
IGF
26
Insulin structure
A chain: 21AA B chain: 30AA connected by 2 disulfide bridges
27
Human insulin has close homology with _____ and ____
pig (1AA) | cow (3AA)
28
How are the chains of insulin assembled?
post-translational modification | with disulfide bridge formation
29
What two forms can insulin be in?
dimer | hexamer
30
How does insulin form dimers?
H bonding
31
How does insulin form hexameters?
zinc ions
32
The design of insulin analogs has emphasized _______ or ______ of structural elements according to established principles of _______
stabilization or destabilization | protein folding
33
(SAR) What are good sites of modification of insulin?
solvent exposed side chain extrinsic to receptor binding surface
34
(SAR) What has been studied to assess it ability to form dimers or hexameters and activate insulin receptors?
different sequences
35
(SAR) Modify insulin to change what?
ADME | Fast or slow insulin analogs
36
What type of interactions are in insulin?
dimer dimer contacts | monomer monomer interactions
37
T/f residues involved in interaction with receptor of insulin cannot be modified
true
38
Non-hexomeric insulins
NPH Lisper Aspart Glulisine
39
Shifted isoelectric point insulins
glargine | detemir
40
Which insulin has a suspension of crystalline zinc porcine insulin?
NPH (non-hexomeric)
41
Which insulin has a high affinity for serum albumin?
detemir
42
New long acting insulins
Toujeo Tresiba Ryzodeg
43
How long do new long acting insulins last?
up to 42 hours
44
What was the 1st fast acting insulin analog engineered by recombinant DNA tech?
lispro
45
Which insulin enhances hexamer formation without Zn in formula?
glargine
46
Why are shifted isoelectric point insulins used for?
replace basal level of insulin | may be effective over period of 24h
47
How do smart insulins work?
circulates in blood, turns on when BG is high | Turns back off when in safe zone
48
Smart insulins are chemically attached to a _____ polymer with sticky sugar groups. This is mixed with a ____ binding molecule.
biodegradable | sugar
49
The insulin polypeptides in smart insulin comprise a ____ motif that enables the _____ expression of glycosylated insulin polypeptides
N linked glycan | recombinant
50
The glycosylated insulin conjugates of smart insulin will be sensitive to ______
serum concentrations of glucose
51
What is important to know about smart insulin pump?
automatically adjusts insulin levels | - users need to manually adjust when high carb meal
52
What are biosimilars?
generic copy of biologics
53
Current biosimilar products
- EPO products - growth factors - insulins Biocon