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Medicinal 3 > Antiglycemic medication > Flashcards

Antiglycemic medication Flashcards

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1
Q

What is type 1 diabetes

A

Insulin dependent DM

Inability of b-islets of pancrease to produce insulin

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2
Q

What is type 2 diabetes

A

Non-insulin dependent DM

  1. reduced ability of pancreas to produce or secrete insulin
  2. reduced ability of target cells to respond to insulin (insulin resistance)
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3
Q

Mention types of DM

A

T1D
T2D
Gestational diabetes

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4
Q

What are the input sources of sugar

A
  1. Abs from diet
  2. biosynthesis in the liver
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5
Q

is insulin a first choice in t2d

A

No
last choice

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6
Q

is insulin a first choice in T1D

A

yes

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7
Q

Is insulin a biological drug

A

No
because it is SMALL in size

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8
Q

MOA of a-Glucosidase inhibitors

A

blocks a-glucosidase (which is an enzyme that hydrolyzes maltose to glucose)

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9
Q

Mention drugs that fall under the class of a-Glucosidase inhibitors

A

Acarbose
Miglitol
Voglibose (new)

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10
Q

MOA of Acarbose

A

a-Glucosidase inhibitor

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11
Q

SE of acarbose

A

Flatulence
Diarrhea
Colonic gas production from sugar fermentation
bloating
cramping

NOT well tolerated

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12
Q

CI of Acarbose

A
  1. chronic GI diseases
  2. Renal impairment
  3. Hepatic dysfunction
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13
Q

Acarbose ________ ________ state

A

mimic transition state

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14
Q

Miglitol _________ ________

A

Mimic product

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15
Q

is miglitol reversible or not

A

Reversible a-glucosidase inhibitor

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16
Q

Is miglitol well absorbed

A

Yes

but no systemic effect ( extremely hydrophilic -> renally excreted)

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17
Q

Is miglitol well tolerated

A

NO

but still better and less GI effects than a carbose

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18
Q

Why did the USFDA not approve voglibose

A

Because the studies were only done on asian individuals

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19
Q

Do a-glucosidase inhibitor work on endogenous biosynthesis pathway

A

No, only on sugars from diet

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20
Q

What is the MOA of sulfonyl ureas

A

They open potassium channel in B-cells which affect k+ balance -> open Ca+2 channel -> Insulin secretion

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21
Q

What are the generations of sulfonylureas and what are some example drugs

A

FIRST gen
- Tolbutamide
- Chlorpropamide
- Tolazamide
-Acetohexamide

SECOND gen
- Glyburide
-Glipizide

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22
Q

What are the SE of Sulfonylureas

A

Weight gain

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23
Q

SAR of sulfonylureas

A
  1. R1
  2. Aromatic ring
  3. Sulfone
  4. Urea
  5. R2 (responsible for activity)
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24
Q

Adding a high hydrophibicity group on R1 will..?

A

Increase duration of action

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25
What will happen if we add an easily metabolized group like CH3 on R1 and what will happen if we add a slow metabolized group like Cl on R1 in sulfonylureas?
Easily metabolized CH3 like in Tolbutamide FAST ONSET, SHORT DOA Slowly metabolized Cll like in CHLORPROMAIDE, GLYBURIDE,GLIMPERIDE,GLIPIZIDE SLOW ONSET, LONG T1/2 (60hr)
26
What is the minimum side chain in R1 of sulfonylureas accepted? What is the maximum
3-C side chain less than that, no action 3-6 carbons increase activity -----> the BEST 6-12 carbon, NO INCREASE activity >12 NO ACTIVITY
27
Most of sulfonylureas contain cyclic hexane not aliphatic, why
Because cyclic is more soluble and stable than aliphatic
28
In sulfonylureas, R1 increases ----- while R2 increase -------
R1 -> ACTIVITIY R2 -> PK
29
Since Sulfonylureas affect the potassium chanels, can they be given to heart patients
NO except Glimperide, doesnt affect the cardiac tissue
30
What is the main concern with sulfonylureas?
HYPOGLYCEMIA since sulfonylureas increase insulin levels regardless of its level, so we need to organize it with meals
31
Which have more protein binding, first or second generation sulfonylureas
Second generation glipizide, glimperide... have a high protein binding than first
31
Signs of HYPOGLYCEMIA
Sweating Shaking Irratibility Sonfusion Tachycardia feeling hungry
32
If sulfonylureas are taken with medication that displace sulfonylureas (LIKE SULFONAMIDE, GEMFIBROZIL, WARFARIN) from their plasma protein binding side what will happen
HIGHER RISKS OF HYPOGLYCEMIA
33
What is the DOA of chlorpropamide
60 hours! the longest
34
Do first and second generation sulfonylureas have the same MOA
YES
35
Sulfonylureas are mostly used in juvenile-onset diabetes?
NOT IN T1D but it adulthood onset T2D
36
Is tolbutamide short or long acting ?
SHORT
37
What % of tolazamide is found in the urine
85%
38
Is glyburide safe in pregnancy
CATEGORY C Studies showed that pregnant woman who took glyburide in pregnancy, their children were more likely to be diabetic not teratogenic
39
What are the safe glycemic medication in pregnancy
Insulin Metformin glyburide
40
Biguanides contain guanidine group, is it acidic, basic?
BASIC PKA = 12.5
41
Why does biguanides cause lactic acidosis?
They block the krebs cycle in mitochondira which lead to pyrovate accumulation in the cell pyruvate will be converted to lactate it is not an issue in normal kiney function, it is however a problem in kidney dysfunction
42
Does phenphormin cause lactic acidosis
YES
43
Which caused more death cases? metformin or phenformin
phenformin > metformin
44
Are biguanides only used alone? or can they be in combo
they can be either alone or with sulfonylureas
45
What is the MOA of metformin
not known but maybe increase insulin binding to its receptor (increase insulin sensitivity)
46
At physiological pH, how is the guandinium group
Positively charged -> poorly protein bound
47
What is the drug reporposing of metformin
Polycyctic ovary cancer Weight loss (NOT FDA APP)
48
What is the duration of action of metforn? short long?
Short, 1.7 - 4.5 hr
49
SE OF metformin
Lactic acidosis low B12
50
SAR of thiazolidinediones?
1. ACIDIC RING 2. LINKER phenyl alkyl 3. Lipophilic ring
51
Where does pioglitazone target
PPAR-Y PPAR-A
52
Where does rioglitazone targer
PPAR-Y
53
SE of pioglitazone
Increase risk of MI BLADDER CANCER
54
What does DPP4 break down
Incretins
55
What is the MOA of sitagliptin
DPP4i (breaks down increitn)
56
Is Sitaglitptin well tolerated
YES
57
Is Ozempic a biological peptide
NO
58
Scientific name of ozempic
Semaglutide
59
What is Ozempic
GLP1RA
60
Is ozempic approved for T2D
yes
61
What is the first GLP1RA approved by fda
Exenatide in 2005
62
What is the difference between ozempic and wegovy
Same semaglutide but wegovy has double the dose
63
Which is approved by FDA, ozempic or wegovy
only wegoey is approved
64

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