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Sophomore - Pharm test 3 > DM3 - Pharmacology > Flashcards

DM3 - Pharmacology Flashcards

1
Q

What is the first drug we consider for monotherapy in Tx of T2DM?

A

Metformin

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2
Q

If target A1C is not achieved after _______ months on Metformin, consider adding ________.

A

3

A second agent

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3
Q

What are the first line agents for T2DM?

A
  1. Biguanides (Metformin)

2. Insulin (if A1C >10)

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4
Q

Biguanides - MOA?

A
  1. Decrease hepatic glucose production
  2. Enhance insulin sensitivity
  3. Slow intestinal absorption of sugars
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5
Q

Biguanides (Metformin) - taken when and why?

A

With the largest meal of the day to avoid stomach upset

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6
Q

How of Biguanides (Metformin) eliminated?

A

Renally

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7
Q

Biguanides (Metformin) - AE’s?

A

GI upset, lactic acidosis (rare)

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8
Q

Biguanides (Metformin) - CI’s?

A

Renal insufficiency

Anyone at risk for lactic acidosis (CHF, liver disease, alcoholics, sepsis)

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9
Q

Biguanides (Metformin) - drug interactions?

A

Iodinated contrast media

Cimetidine (Tagamet) can increase Metformin levels

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10
Q

Sulfonylureas (SU) - MOA?

A

Stimulates insulin secretion from the pancreatic beta cell (“squeezes the insulin” out of the cell)

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11
Q

In which patients do we need to exercise caution when administering Sulfonylureas?

A

Hepatic or renal dysfunction

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12
Q

Most common problem with 1st gen Sulfonylureas?

A

Failure to maintain efficacy over time

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13
Q

Sulfonylureas - AE’s?

A
  1. Hypoglycemia
  2. Weight gain
  3. GI upset
  4. Hyponatremia
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14
Q

Sulfonylureas - Drug interactions?

A
  1. Protein binding displacement
  2. CYP metabolism
  3. If pt is on GLP1 antagonists or DPP-4 inhibitors, consider decreasing SU dose by 50%
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15
Q

Chlorpropamide - class and notable features?

A

1st gen sulfonylurea

Highest hypoglycemic potenital

SIADH

Avoid in renal dysfunction and elderly

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16
Q

Tolazamide - class?

A

1st gen Sulfonylurea

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17
Q

Tolbutsmide - class?

A

1st gen Sulfonylurea

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18
Q

Glipizide - class?

A

2nd gen sulfonylurea

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19
Q

Common features of most 2nd gen sulfonylureas?

A

Caution in renal insufficiency (except Glimepiride - safer for renal insufficiency)

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20
Q

Glyburide - class and notable features?

A

Highest 2nd gen sulfonylurea rate of hypoglycemia

Pregnancy Safe

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21
Q

Glimepiride - class and notable feature?

A

Safer in renal dysfunction than the other Sulfonylureas

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22
Q

What class of drug that causes stimulation of insulin secretion is considered by the ADA to be a second-line therapy added on to Metformin if target A1C is not met?

A

1st or 2nd gen sulfonylureas

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23
Q

Meglitinides - MOA?

A

Stimulates insulin secretion from the pancreatic beta cells similarly to SU’s BUT requires the presence of glucose (taken with meals)

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24
Q

Meglitinides - useful for what kind of patient?

A

Someone who skips meals or doesn’t eat regularly

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25
Q

Meglitinides - AE’s?

A
  1. Hypoglycemia
  2. URTI
  3. Dizziness
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26
Q

Which meglitinide is better at lowering A1C - repaglinide or nateglinide?

A

Repaglinide

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27
Q

Which drug class may be used as a 1st line if patient cannot take metformin, or used in combination with metformin or other drugs?

A

Meglitinides

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28
Q

Nateglinide - class?

A

Meglitinides

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29
Q

Repaglinide - class and notable features?

A

Meglitinides

Better at lowering A1C than nateglinide

Gemfibrozil DOUBLES its effects

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30
Q

Thiazolidinediones - MOA?

A

Enhances insulin sensitivity by:

1) increasing glucose transporter expression
2. Binding PPAR-y

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31
Q

Thiazolidinediones (TZD’s) - AE’s?

A
  1. Weight gain (edema)

2. Hepatic failure

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32
Q

Thiazolidinediones (TZD’s) - increased risk for:

A
  1. MI

2. Bladder CA

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33
Q

Thiazolidinediones (TZD’s) - CI’s?

A
  1. Class III/IV heart failure (congestive HF)
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34
Q

Thiaziolidinediones (TZD’s) - drug interactions?

A

Nitrates (increased MI risk)

Insulin (increased CHF risk)

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35
Q

Thaizolidinediones (TZD’s) - monitoring?

A
  1. HbA1C - slow effects
  2. Liver - hepatotoxicity
  3. Lipids
36
Q

Pioglitazone - class and notable feature?

A

Thiazolidinedione (TZD), suspended in some European countries due to bladder CA risk

37
Q

Rosiglitazone - class?

A

Thiazolidinediones (TZD)

38
Q

What is the “incretin effect”?

A

The body produces a greater insulin response to an oral glucose than an IV glucose

39
Q

Name the two incretin hormones that contribute to increased secretion of insulin following oral glucose consumption:

A
  1. Glucose-dependent insulinotropic polypeptide (GIP)

2. Glucagon-like Peptide (GLP-1)

40
Q

What is the enzyme that rapidly degrades GIP and GLP-1? (The incretin hormones)

A

Di-peptidyl peptidase-4 (DPP-4)

41
Q

Actions of GLP-1?

A

Glucagon-like peptide-1

Secreted from L-cells in distal intestine

Stimulated by glucose

Suppresses glucagon secretion, slows gastric emptying, increased satiety

42
Q

What is the preferred incretin hormone target in T2DM?

A

GLP-1, because it is deficient is T2DM

43
Q

Actions of GIP?

A

Secreted by K cells in the intestine

Does NOT affect glucagon secretion, gastric motility, or satiety

Augments insulin secretion

44
Q

Depeptidyl Peptidase-4 (DPP-4) Inhibitors - MOA?

A

Inhibits the enzyme DPP4

Prevents degradation of endogenous incretins (GLP-1 and GIP)

Increased insulin secretion

Decreased glucagon secretion

45
Q

DPP4 Inhibitors - AE’s?

A
  1. Pancreatitis
  2. Infection risk
  3. May worsen existing HF
  4. Must dose-adjust for renal/hepatic impairment
46
Q

DDP4 inhibitors - drug interactions?

A

Consider decreasing the dose of sulfonylureas by 50% if using

47
Q

Which drug class names are “-gliptin”’s?

A

Dipeptidyl Peptidade-4 Inhibitors (DPP4 Inhibitors)

48
Q

Saxagliptin and Linagliptin are both ______ substrates

A

CYP3A4

49
Q

Which DPP4 inhibitor does NOT require dose adjustment for renal or hepatic impairment?

A

Linagliptin

50
Q

Glucagon-like Peptide 1 Agonists (GLP-1 Agonists) - MOA?

A

Stimulate GLP-1 receptors

GLP1:

  • slows gastric emptying
  • increases satiety
  • reduces post-prandial glucagon secretion
  • increases insulin-secretion
51
Q

GLP-1 agonists - AE’s?

A
  1. Hypoglycemia
  2. HA/nausea/diarrhea/constipation
  3. Pancreatitis
52
Q

GLP-1 agonists - CI’s?

A

Type 1 diabetics

Pt’s with personal or familial hx thyroid CA

53
Q

GLP-1 agonists - drug interactions?

A
  1. May delay absorption of other drugs (due to delayed gastric emptying)
  2. Consider reducing sulfonylurea dose by 50%
54
Q

GLP-1 agonists - route of administration?

A

SubQ

55
Q

DPP4 inhibitors - route of administration?

A

Oral

56
Q

Exenatide - class?

A

GLP-1 agonist

57
Q

Liraglutide - class?

A

GLP-1 agonist

58
Q

Liraglutide - notable features?

A

GLP-1 agonist

Indicated for weight management

59
Q

Albiglutide - class?

A

GLP-1 agonist

60
Q

Dulaglutide - class?

A

GLP-1 agonist

61
Q

Synthetic Amylin Analogue - MOA?

A

Suppresses inappropriately high postprandial glucagon secretion

Increases satiety

Slows gastric emptying

62
Q

Synthetic Amylin analogue - clinical use?

A

Adjunct to mealtime insulin therapy in T1DM and T2DM

63
Q

What medication can be considered as an adjunct to mealtime insulin therapy in Type 1 diabetics?

A

Synthetic Amylin Analogues

64
Q

Three main effects of Synthetic Amylin Analogues?

A
  1. Slows gastric emptying
  2. Suppresses post-prandial glucagon secretion
  3. Increases satiety
65
Q

Synthetic Amylin Analogues - AE’s?

A
  1. Hypoglycemia

2. N/V

66
Q

Synthetic Amylin Analogues - CI’s?

A
  1. Pt’s with gastroparesis
  2. HbA1c >9
  3. Pt’s generally noncompliant with insulin regimen
67
Q

Synthetic Amylin analogues - drug interactions?

A

2-fold increase in hypoglycemia in T1DM patients (decrease bolus insulin 50%)

68
Q

Pramlintide - class?

A

Synthetic Amylin Analogue

69
Q

Alpha-Glucosidase Inhibitors - MOA?

A

Competitively inhibit alpha-glucosidase enzymes, delaying breakdown of sucrose and complex carbs

Reduction in blood sugar spike after eating

ABSORPTION OF GLUCOSE, LACTOSE, FRUCTOSE UNAFFECTED

70
Q

Alpha-glucosidase inhibitors - clinical use?

A

THIRD LINE T2DM

71
Q

Biggest issue with alpha-glucosidase inhibitors?

A

GI side effects - gas, bloating, abdominal discomfort, diarrhea

72
Q

Alpha-glucosidase inhibitors - CI’s?

A

Pt’s with GI issues - short-bowel syndrome, IBS

Cirrhosis

73
Q

Arcabose - class?

A

Alpha-glucosidase inhibitor

74
Q

Miglitol - class?

A

Alpha-glucosidase inihibitor

75
Q

Considerations with alpha-glucosidase inhibitors?

A

Renal insuffiency

76
Q

Selective Sodium Dependent Glucose CoTransporter-2 Inhibitors (SGLT2) - MOA?

A

Inhibits the sodium glucose cotransporter-2 transporter, which reduces reabsorption of filtered glucose, leading to increased urinary glucose excretion

77
Q

SGLT2 inhibitors - use?

A

THIRD LINE T2DM

78
Q

Suffix for SGLT2 inhibitors?

A

-flozin

79
Q

SGLT2 inhibitors - AE’s

A
  1. Weight loss
  2. Polyuria
  3. Genital fungal infections
  4. UTI’s
80
Q

SGLT2 inhibitors - precautions?

A
  1. Increased risk of stroke

2. Increased risk of bladder CA

81
Q

SGLT2 inhibitors - CI’s?

A

Bladder CA

Renal dysfunction

82
Q

Suflonylureas (Glimepiride, Glipizide) - MOA?

A

Stimulate insulin secretion

83
Q

Sulfonylureas - caution when combined with?

A

Insulin

84
Q

Second-line T2DM drugs?

A
  1. Sufonylureas (SU’s)
  2. Thiazolidinediones (TZD’s)
  3. Dipeptidyl Peptidase-4 Inhibitors (DPP4-I)
  4. Insulin
  5. Glucagon-like Peptide-1 agonists (GLP-1 agonists)
85
Q

Third-line T2DM drugs?

A
  1. Meglitinides
  2. Synthetic Amylin Analogues
  3. Sodium-Glucose CoTransporter-2 Inhibitors (SGLT2 Inhibitors)
  4. Alpha-glucosidase inhibitors (AGI)
86
Q

Other T2DM drugs?

A
  1. Bile acid sequestrants

2. Dopamine Agonists

87
Q

Examples of drugs non-DM drugs that can raise blood glucose?

A
  1. Beta blockers
  2. Corticosteroids
  3. Niacin
  4. Diuretics

Sophomore - Pharm test 3 (7 decks)

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