Oral Meds in Diabetes

Question 1

All drugs except ____ used for Type 2 DM only

Answer 1

Insulin

Question 2

Drugs usable during pregnancy

Answer 2

Glyburide (sulfonylurea) and metformin

Question 3

Do not use in combination

Answer 3

Sulfonylureas and meglitinides

Question 4

Drug of choice:

Answer 4

Metformin

Question 5

Advantageous Characteristics (4)

Answer 5

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

Question 6

Disadvantageous (4)

Answer 6

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

Question 7

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

Answer 7

GI characteristics: anorexia, nausea, diarrhea, lactic acidosis

Question 8

Metformin: Mechanism & Effect

Answer 8

Activation/phosphorylation of AMPK–> reduces hepatic gluconeogenesis

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

Question 9

Metformin other:
Requires ____ for action
How much does it

Answer 9

Requires presence of insulin for its action

Lowers A1c by up to 2%–>Higher A1c at start of treatment leads to greater drop

Question 10

Metformin Contraindications (5)

Answer 10

Metabolic acidosis
Hypoxia
Renal failure
T1DM
Cardiac ischemia

Basically all related to ability to regulate pH

Question 11

Sulfonylureas: Mechanism of Action

Answer 11

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

Question 12

Sulfonylurea: Effect & A1c

Answer 12

Works mostly on pre-meal glucose

Lowers A1c by up to 1.5%

Question 13

Sulfonylurea: metabolism

Metabolized via ____ and excreted via ______

Answer 13

Hepatic; excreted via kidney

caution with renal impairment

Question 14

Sulfonylurea: AE (3) and CI (3)

Answer 14

AE: hypoglycemia, weight gain, hunger

CI: T1DM, DKA, sulfa allergy

Question 15

Meglitinides: MOA

Answer 15

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

Question 16

Sulfonylureas vs. Meglitinides: onset and duration

Answer 16

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

Sulfonylureas: Last for 10-12hr

Question 17

Meglitinides: AE (2) and CI (4)

Answer 17

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

CI: T1DM, liver failure, DKA, sulfa allergy

Question 18

Meglitinides: Metabolism

Metabolized by _____ and excreted by _____

Answer 18

Metabolized by Hepatic cytP450

Excreted by GI tract

Question 19

Thiazolinediones (TZD): MOA

Answer 19

Binds nuclear PPARgamma receptor causing increased GLUT4 transcription–>

Decreases peripheral insulin resistance in skeletal muscle, adipose, liver

Question 20

TZD: Effect (pre/post meal?)

Answer 20

Lower pre-meal and post-meal glucose

Question 21

TZD: AE (3) and CI (4)

Answer 21

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

Question 22

TZD: Effect on Cholesterol

Answer 22

Reduces triglycerides

Increases LDL-cholesterol, HDl

Question 23

TZD: A1c

Answer 23

Lowers A1c by 1.8%

Question 24

A-Glucosidase Inhibitors: MOA

Answer 24

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

Delays gut carb absorption, increases GLP-1

Question 25

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

Answer 25

Post-prandial glucose only

Question 26

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

Answer 26

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

Question 27

A-glucosidase inhibitors: Metabolism | Excreted by ____ as _____

Answer 27

Excreted by renal as unchanged drug

Question 28

A glucosidase inhibitor: A1c efficacy

Answer 28

Lowers A1c by .4%

Question 29

Incretin effect in Diabetics is ____ compared to controls

Answer 29

Diminished

Question 30

Treatment Strategies involving Incretin system (1)

Answer 30

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

Question 31

Exenatide Effect (Pre/post meal?)

Answer 31

Lowers post-meal glucose

Question 32

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

Answer 32

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

Question 33

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

Answer 33

DPP-4 degradation with renal excretion Note: can enhance effect with DPP-IV inhibitors to increase duration of action for GLP-1

Question 34

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

Answer 34

AE: bloating, nausea, diarrhea CI: gastroparesis

Question 35

GLP-1 Effect on A1c

Answer 35

Lowers A1c by 1% | Weight loss too!

Question 36

Incretin Enhancers: MOA

Answer 36

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

Question 37

Incretin Enhancers: Metabolism

Answer 37

Not metabolized, excreted via kidneys

Question 38

Incretin Enhancers: AE (1) and CI

Answer 38

AE: gastrointestinal CI: None!

Question 39

SGL2 Inhibitors: Names

Answer 39

Canagliflozin, dapagliflozin, empagliflozin

Question 40

SGLT2 Inhibitors: MOA

Answer 40

Inhibit SGLT2 (duh)

Question 41

SGLT2 Inhibitors: Metabolism | Metabolized by ____ and excreted via _____

Answer 41

Hepatic metabolism with renal excretion

Question 42

SGLT2: AE (4) and CI (3)

Answer 42

AE: vulvovaginal candiasis, vulvovaginal mycotic infection, UTI, polyuria CI: renal impairment, ESRD, Dialysis

Question 43

SGLT2 Inhibitors: A1c efficacy and weight loss

Answer 43

Lowers A1c by .7% | Weight loss of 2.2kg