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Flashcards in Oral Medications in Diabetes Deck (38):
1

T/F all glucose lowering agents are only used for t2d

T

2

T/F all glucose lowering agents are contraindicated in pregnancy

F --> all except sulfonylurea and metformin

3

T/F all glucose lowering agents can be used in any combination

F --> any combination except sulfonylurea and meglitinides should not be mixed

4

T2D first drug of choice

metformin

5

Metformin/diguanide action and mechanism

activation of ampk -->

1. increase muscle glucose tranport
2. reduces hepatic glucose production
3. sensitizes insulin (via reduced ACC and SREBP expression and consequent reduced hepatic FA production)

-->improves pre meal glucose and modestly affects post-prandial glucose

6

Thiazolidinendiones (TZD)/PPARgamma agonists MOA/Action

binds nuclear ppar gamma receptor --> increases GLUT4 transporter--> decreases peripheral insulin resistance in skeletal muscle, adipose, liver --> lowers premeal/post meal glucose

7

Insulin secretagogues

Induce beta cell secretion of insulin (short and long acting) --> suflonylureas and meglitinides

8

alpha glucosidase inhibitors MOA/action

competitively inhibit enzymes in brush border to breakdown carbohydrates --> delay carbohydrate absorption in gut --> reduce post prandial glucose only

9

GLP1 agonist

slows gut motility, induces satiety, increased insulin/lower glucagon

10

Incretin enhancers (DPP-4 inhibitors)

increase duration of action of GLP1 via 80% inhibition of DPP4 --> mostly on post-meal glucose

11

Advantageous characteristics of a good drug for t2d

weight loss/neutral, no hypoglycemia, oral, frequency of delivery

12

Disadvantageous characteristics of a good drug for t2d

weight gain (reversal of osmotic diuresis, reversal of relative starvation/normalization, fluid retention), hypoglycemia, frequency of delivery, injectable

13

T/F metformin is weight neutral and can induce weight loss

T

14

T/F metformin is metabolized at the liver

F --> renally excreted unexchanged and can accumulate if pt has renal insufficiency

15

Adverse effects of metformin

anorexia, nausea, diarrhea, lactic acidosis

16

T/F metformin does not cause hypoglycemia

T

17

Contraindications of metformin

prone to metabolic acidosis, hypoxic states, renal failure, t1d, cardiac ischemia

18

T/F metformin requires presence of insulin for its action

T

19

Sulfonylurea action and MOA

binds to sulfonyl receptor in beta cell --> depolarization of ATP K channels --> pancreatic insulin secretion for 12-24 hours --> mostly premeal glucose effect

20

T/F Sulfonylurea does not get metabolised

F --> hepatic and excreted in kidney

21

Contraindications of sulfonylurea

T1d, DKA, sulfa allergy

22

Adverse effects of sulfonylurea

hypoglycemia, weight gain, hunger

23

K+ channel in the beta cell

induces calcium current which causes insulin release --> sulfonylurea and meglitinide binding sites

24

Meglitinide action/MOA

stimualtes K+ channel on beta cells --> pancreatic insulin for 3-4 hours

25

T/F Meglitinide is fast onset

T

26

Adverse effects of meglitinide

low glucose after meal, weight gain

27

Contraindications of meglitinide

T1d, liver failure, DKA, sulfa allergy

28

T/F meglitinide is metabolized in the kidney

F --> in liver by p450 --> excreted mostly in GI tract

29

Adverse effects of TZD

weight gain, hepatocellular injury

30

Contraindications of TZD

active liver disease, heart failure, renal insufficiency

31

T/F TZD has slow onset of action

T

32

T/F TZD can induce low blood glucose

F --> no insulin secretory effect

33

Adverse effects of alpha glucosidase inhibitors

flatulence, abdominal bloating

34

T/F alpha glucosidase inhibitors are metabolized in the liver

F--> renally excreted unchanged

35

T/F alpha glucosidase inhibitors can cause low glucose

F

36

Metabolism of GLP agonists

rapidly degraded by DPP4 in blood

37

SGLT2

major transporter of glucose in kidney, low affinity/high capacity- -> 90 % of renal glucose reabsorption in proximal tubule

38

SGLT2 inhibitors

inhibit reabsorption of glucose --> excretion by kidney