DM3 - Pharmacology Flashcards

(87 cards)

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
Meglitinides - AE’s?
1. Hypoglycemia 2. URTI 3. Dizziness
26
Which meglitinide is better at lowering A1C - repaglinide or nateglinide?
Repaglinide
27
Which drug class may be used as a 1st line if patient cannot take metformin, or used in combination with metformin or other drugs?
Meglitinides
28
Nateglinide - class?
Meglitinides
29
Repaglinide - class and notable features?
Meglitinides Better at lowering A1C than nateglinide Gemfibrozil DOUBLES its effects
30
Thiazolidinediones - MOA?
Enhances insulin sensitivity by: 1) increasing glucose transporter expression 2. Binding PPAR-y
31
Thiazolidinediones (TZD’s) - AE’s?
1. Weight gain (edema) | 2. Hepatic failure
32
Thiazolidinediones (TZD’s) - increased risk for:
1. MI | 2. Bladder CA
33
Thiazolidinediones (TZD’s) - CI’s?
1. Class III/IV heart failure (congestive HF)
34
Thiaziolidinediones (TZD’s) - drug interactions?
Nitrates (increased MI risk) | Insulin (increased CHF risk)
35
Thaizolidinediones (TZD’s) - monitoring?
1. HbA1C - slow effects 2. Liver - hepatotoxicity 3. Lipids
36
Pioglitazone - class and notable feature?
Thiazolidinedione (TZD), suspended in some European countries due to bladder CA risk
37
Rosiglitazone - class?
Thiazolidinediones (TZD)
38
What is the “incretin effect”?
The body produces a greater insulin response to an oral glucose than an IV glucose
39
Name the two incretin hormones that contribute to increased secretion of insulin following oral glucose consumption:
1. Glucose-dependent insulinotropic polypeptide (GIP) | 2. Glucagon-like Peptide (GLP-1)
40
What is the enzyme that rapidly degrades GIP and GLP-1? (The incretin hormones)
Di-peptidyl peptidase-4 (DPP-4)
41
Actions of GLP-1?
Glucagon-like peptide-1 Secreted from L-cells in distal intestine Stimulated by glucose Suppresses glucagon secretion, slows gastric emptying, increased satiety
42
What is the preferred incretin hormone target in T2DM?
GLP-1, because it is deficient is T2DM
43
Actions of GIP?
Secreted by K cells in the intestine Does NOT affect glucagon secretion, gastric motility, or satiety Augments insulin secretion
44
Depeptidyl Peptidase-4 (DPP-4) Inhibitors - MOA?
Inhibits the enzyme DPP4 Prevents degradation of endogenous incretins (GLP-1 and GIP) Increased insulin secretion Decreased glucagon secretion
45
DPP4 Inhibitors - AE’s?
1. Pancreatitis 2. Infection risk 3. May worsen existing HF 4. Must dose-adjust for renal/hepatic impairment
46
DDP4 inhibitors - drug interactions?
Consider decreasing the dose of sulfonylureas by 50% if using
47
Which drug class names are “-gliptin”’s?
Dipeptidyl Peptidade-4 Inhibitors (DPP4 Inhibitors)
48
Saxagliptin and Linagliptin are both ______ substrates
CYP3A4
49
Which DPP4 inhibitor does NOT require dose adjustment for renal or hepatic impairment?
Linagliptin
50
Glucagon-like Peptide 1 Agonists (GLP-1 Agonists) - MOA?
Stimulate GLP-1 receptors GLP1: - slows gastric emptying - increases satiety - reduces post-prandial glucagon secretion - increases insulin-secretion
51
GLP-1 agonists - AE’s?
1. Hypoglycemia 2. HA/nausea/diarrhea/constipation 3. Pancreatitis
52
GLP-1 agonists - CI’s?
Type 1 diabetics Pt’s with personal or familial hx thyroid CA
53
GLP-1 agonists - drug interactions?
1. May delay absorption of other drugs (due to delayed gastric emptying) 2. Consider reducing sulfonylurea dose by 50%
54
GLP-1 agonists - route of administration?
SubQ
55
DPP4 inhibitors - route of administration?
Oral
56
Exenatide - class?
GLP-1 agonist
57
Liraglutide - class?
GLP-1 agonist
58
Liraglutide - notable features?
GLP-1 agonist Indicated for weight management
59
Albiglutide - class?
GLP-1 agonist
60
Dulaglutide - class?
GLP-1 agonist
61
Synthetic Amylin Analogue - MOA?
Suppresses inappropriately high postprandial glucagon secretion Increases satiety Slows gastric emptying
62
Synthetic Amylin analogue - clinical use?
Adjunct to mealtime insulin therapy in T1DM and T2DM
63
What medication can be considered as an adjunct to mealtime insulin therapy in Type 1 diabetics?
Synthetic Amylin Analogues
64
Three main effects of Synthetic Amylin Analogues?
1. Slows gastric emptying 2. Suppresses post-prandial glucagon secretion 3. Increases satiety
65
Synthetic Amylin Analogues - AE’s?
1. Hypoglycemia | 2. N/V
66
Synthetic Amylin Analogues - CI’s?
1. Pt’s with gastroparesis 2. HbA1c >9 3. Pt’s generally noncompliant with insulin regimen
67
Synthetic Amylin analogues - drug interactions?
2-fold increase in hypoglycemia in T1DM patients (decrease bolus insulin 50%)
68
Pramlintide - class?
Synthetic Amylin Analogue
69
Alpha-Glucosidase Inhibitors - MOA?
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
Alpha-glucosidase inhibitors - clinical use?
THIRD LINE T2DM
71
Biggest issue with alpha-glucosidase inhibitors?
GI side effects - gas, bloating, abdominal discomfort, diarrhea
72
Alpha-glucosidase inhibitors - CI’s?
Pt’s with GI issues - short-bowel syndrome, IBS Cirrhosis
73
Arcabose - class?
Alpha-glucosidase inhibitor
74
Miglitol - class?
Alpha-glucosidase inihibitor
75
Considerations with alpha-glucosidase inhibitors?
Renal insuffiency
76
Selective Sodium Dependent Glucose CoTransporter-2 Inhibitors (SGLT2) - MOA?
Inhibits the sodium glucose cotransporter-2 transporter, which reduces reabsorption of filtered glucose, leading to increased urinary glucose excretion
77
SGLT2 inhibitors - use?
THIRD LINE T2DM
78
Suffix for SGLT2 inhibitors?
-flozin
79
SGLT2 inhibitors - AE’s
1. Weight loss 2. Polyuria 3. Genital fungal infections 4. UTI’s
80
SGLT2 inhibitors - precautions?
1. Increased risk of stroke | 2. Increased risk of bladder CA
81
SGLT2 inhibitors - CI’s?
Bladder CA | Renal dysfunction
82
Suflonylureas (Glimepiride, Glipizide) - MOA?
Stimulate insulin secretion
83
Sulfonylureas - caution when combined with?
Insulin
84
Second-line T2DM drugs?
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
Third-line T2DM drugs?
1. Meglitinides 2. Synthetic Amylin Analogues 3. Sodium-Glucose CoTransporter-2 Inhibitors (SGLT2 Inhibitors) 4. Alpha-glucosidase inhibitors (AGI)
86
Other T2DM drugs?
1. Bile acid sequestrants | 2. Dopamine Agonists
87
Examples of drugs non-DM drugs that can raise blood glucose?
1. Beta blockers 2. Corticosteroids 3. Niacin 4. Diuretics