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Endocrinology > Oral Meds in Diabetes > Flashcards

Oral Meds in Diabetes Flashcards

1
Q

All drugs except ____ used for Type 2 DM only

A

Insulin

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2
Q

Drugs usable during pregnancy

A

Glyburide (sulfonylurea) and metformin

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3
Q

Do not use in combination

A

Sulfonylureas and meglitinides

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4
Q

Drug of choice:

A

Metformin

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5
Q

Advantageous Characteristics (4)

A

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

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6
Q

Disadvantageous (4)

A

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

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7
Q

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

A

GI characteristics: anorexia, nausea, diarrhea, lactic acidosis

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8
Q

Metformin: Mechanism & Effect

A

Activation/phosphorylation of AMPK–> reduces hepatic gluconeogenesis

Improves pre-meal glucose with modest post-prandial effect
Weight neutral (can induce weight loss)
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9
Q

Metformin other:
Requires ____ for action
How much does it

A

Requires presence of insulin for its action

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

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10
Q

Metformin Contraindications (5)

A 
Metabolic acidosis
Hypoxia
Renal failure
T1DM
Cardiac ischemia

Basically all related to ability to regulate pH

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11
Q

Sulfonylureas: Mechanism of Action

A

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

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12
Q

Sulfonylurea: Effect & A1c

A

Works mostly on pre-meal glucose

Lowers A1c by up to 1.5%

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13
Q

Sulfonylurea: metabolism

Metabolized via ____ and excreted via ______

A

Hepatic; excreted via kidney

caution with renal impairment

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14
Q

Sulfonylurea: AE (3) and CI (3)

A

AE: hypoglycemia, weight gain, hunger

CI: T1DM, DKA, sulfa allergy

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15
Q

Meglitinides: MOA

A

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

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16
Q

Sulfonylureas vs. Meglitinides: onset and duration

A

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

Sulfonylureas: Last for 10-12hr

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17
Q

Meglitinides: AE (2) and CI (4)

A

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

CI: T1DM, liver failure, DKA, sulfa allergy

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18
Q

Meglitinides: Metabolism

Metabolized by _____ and excreted by _____

A

Metabolized by Hepatic cytP450

Excreted by GI tract

19
Q

Thiazolinediones (TZD): MOA

A

Binds nuclear PPARgamma receptor causing increased GLUT4 transcription–>

Decreases peripheral insulin resistance in skeletal muscle, adipose, liver

20
Q

TZD: Effect (pre/post meal?)

A

Lower pre-meal and post-meal glucose

21
Q

TZD: AE (3) and CI (4)

A

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
Q

TZD: Effect on Cholesterol

A

Reduces triglycerides

Increases LDL-cholesterol, HDl

23
Q

TZD: A1c

A

Lowers A1c by 1.8%

24
Q

A-Glucosidase Inhibitors: MOA

A

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

Delays gut carb absorption, increases GLP-1

25
Q

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

A

Post-prandial glucose only

26
Q

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

A

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

27
Q

A-glucosidase inhibitors: Metabolism

Excreted by ____ as _____

A

Excreted by renal as unchanged drug

28
Q

A glucosidase inhibitor: A1c efficacy

A

Lowers A1c by .4%

29
Q

Incretin effect in Diabetics is ____ compared to controls

A

Diminished

30
Q

Treatment Strategies involving Incretin system (1)

A

GLP-1 Receptor Agonists:

Exenatide, liraglutide via SQ injection

31
Q

Exenatide Effect (Pre/post meal?)

A

Lowers post-meal glucose

32
Q

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

A

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

33
Q

GLP-1 Agonists: Metabolism

Degraded by _____ and excreted by _____

A

DPP-4 degradation with renal excretion

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

34
Q

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

A

AE: bloating, nausea, diarrhea
CI: gastroparesis

35
Q

GLP-1 Effect on A1c

A

Lowers A1c by 1%

Weight loss too!

36
Q

Incretin Enhancers: MOA

A

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

37
Q

Incretin Enhancers: Metabolism

A

Not metabolized, excreted via kidneys

38
Q

Incretin Enhancers: AE (1) and CI

A

AE: gastrointestinal
CI: None!

39
Q

SGL2 Inhibitors: Names

A

Canagliflozin, dapagliflozin, empagliflozin

40
Q

SGLT2 Inhibitors: MOA

A

Inhibit SGLT2 (duh)

41
Q

SGLT2 Inhibitors: Metabolism

Metabolized by ____ and excreted via _____

A

Hepatic metabolism with renal excretion

42
Q

SGLT2: AE (4) and CI (3)

A

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

CI: renal impairment, ESRD, Dialysis

43
Q

SGLT2 Inhibitors: A1c efficacy and weight loss

A

Lowers A1c by .7%

Weight loss of 2.2kg

Endocrinology (26 decks)

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