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Flashcards in Oral Meds in Diabetes Deck (43):
1

All drugs except ____ used for Type 2 DM only

Insulin

2

Drugs usable during pregnancy

Glyburide (sulfonylurea) and metformin

3

Do not use in combination

Sulfonylureas and meglitinides

4

Drug of choice:

Metformin

5

Advantageous Characteristics (4)

Weight loss
No hypoglycemia
Frequency of administration
Oral pill (vs. injectable)

6

Disadvantageous (4)

Weight gain: reversal of osmotic diuresis, fluid retention of TZDs
Hypoglycemia risk
Frequency of delivery
Oral pill (vs. injectable)

7

Why would patient not be on metformin? (AKA what are AE)

GI characteristics: anorexia, nausea, diarrhea, lactic acidosis

8

Metformin: Mechanism & Effect

Activation/phosphorylation of AMPK--> reduces hepatic gluconeogenesis

Improves pre-meal glucose with modest post-prandial effect
Weight neutral (can induce weight loss)

9

Metformin other:
Requires ____ for action
How much does it

Requires presence of insulin for its action
Lowers A1c by up to 2%-->Higher A1c at start of treatment leads to greater drop

10

Metformin Contraindications (5)

Metabolic acidosis
Hypoxia
Renal failure
T1DM
Cardiac ischemia

Basically all related to ability to regulate pH

11

Sulfonylureas: Mechanism of Action

Binds to sulfonyl receptor in B cell resulting in depolarization of ATP-dependent K channel-->Stimulates insulin secretion for 12-24 hours

12

Sulfonylurea: Effect & A1c

Works mostly on pre-meal glucose

Lowers A1c by up to 1.5%

13

Sulfonylurea: metabolism

Metabolized via ____ and excreted via ______

Hepatic; excreted via kidney
(caution with renal impairment)

14

Sulfonylurea: AE (3) and CI (3)

AE: hypoglycemia, weight gain, hunger

CI: T1DM, DKA, sulfa allergy

15

Meglitinides: MOA

Stimulates insulin release by regulating ATP-sensitive K channels on B-cells-->stimulates insulin secretion for 3-4 hours

16

Sulfonylureas vs. Meglitinides: onset and duration

Meglitinides: Fast onset, but only lasts for 3-4 hours

Sulfonylureas: Last for 10-12hr

17

Meglitinides: AE (2) and CI (4)

AE: low glucose 2-4 hour after meal, weight gain

CI: T1DM, liver failure, DKA, sulfa allergy

18

Meglitinides: Metabolism
Metabolized by _____ and excreted by _____

Metabolized by Hepatic cytP450
Excreted by GI tract

19

Thiazolinediones (TZD): MOA

Binds nuclear PPARgamma receptor causing increased GLUT4 transcription-->

Decreases peripheral insulin resistance in skeletal muscle, adipose, liver

20

TZD: Effect (pre/post meal?)

Lower pre-meal and post-meal glucose

21

TZD: AE (3) and CI (4)

AE: weight gain (due to glycemic control), hepatocellular injury, increased risk of bladder cancer

CI: Liver disease, Heart failure, renal insufficiency, hx of bladder cancer

22

TZD: Effect on Cholesterol

Reduces triglycerides
Increases LDL-cholesterol, HDl

23

TZD: A1c

Lowers A1c by 1.8%

24

A-Glucosidase Inhibitors: MOA

Competitive inhibit ability of SI enzymes to break down oligosaccharides/disaccharides into monosaccharides

Delays gut carb absorption, increases GLP-1

25

A-glucosidase inhibitors: Effect (pre/post meal)

Post-prandial glucose only

26

A-glucosidase inhibitors: AE (2) and CI (1)

AE: flatulance, abdominal bloating
CI: GI disorders (inflammatory bowel disease)

27

A-glucosidase inhibitors: Metabolism
Excreted by ____ as _____

Excreted by renal as unchanged drug

28

A glucosidase inhibitor: A1c efficacy

Lowers A1c by .4%

29

Incretin effect in Diabetics is ____ compared to controls

Diminished

30

Treatment Strategies involving Incretin system (1)

GLP-1 Receptor Agonists:
Exenatide, liraglutide via SQ injection

31

Exenatide Effect (Pre/post meal?)

Lowers post-meal glucose

32

Incretin Mimetics/ GLP-1 Agonists: Actions (4)

Potentiates glucose-dependent insulin secretion
Inhibits glucagon secretion
Slows gastric emptying
Stimulates satiety

33

GLP-1 Agonists: Metabolism
Degraded by _____ and excreted by _____

DPP-4 degradation with renal excretion

Note: can enhance effect with DPP-IV inhibitors to increase duration of action for GLP-1

34

GLP-1 Agonists: AE (3) and CI (1)

AE: bloating, nausea, diarrhea
CI: gastroparesis

35

GLP-1 Effect on A1c

Lowers A1c by 1%
Weight loss too!

36

Incretin Enhancers: MOA

Inhibit DPP-IV to increase duration of action of GLP-1

37

Incretin Enhancers: Metabolism

Not metabolized, excreted via kidneys

38

Incretin Enhancers: AE (1) and CI

AE: gastrointestinal
CI: None!

39

SGL2 Inhibitors: Names

Canagliflozin, dapagliflozin, empagliflozin

40

SGLT2 Inhibitors: MOA

Inhibit SGLT2 (duh)

41

SGLT2 Inhibitors: Metabolism
Metabolized by ____ and excreted via _____

Hepatic metabolism with renal excretion

42

SGLT2: AE (4) and CI (3)

AE: vulvovaginal candiasis, vulvovaginal mycotic infection, UTI, polyuria

CI: renal impairment, ESRD, Dialysis

43

SGLT2 Inhibitors: A1c efficacy and weight loss

Lowers A1c by .7%
Weight loss of 2.2kg