Exam 4: Diabetes Pharmacology Flashcards Preview

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Flashcards in Exam 4: Diabetes Pharmacology Deck (86):
1

Two reasons for hyperglycemia in DMII:

Lack of insulin production once β cells fail
Cells resistant to insulin action

2

Insulin produced by:

β cells in islets of Langerhans

3

β cells secrete insulin in response to:

↑ circulating glucose

4

Insulin released as:

Proinsulin (precursor)

5

Structure of insulin:

Small protein chain of 21 amino acids linked by two disulfide bridges to a β chain of 30 amino acids

6

Effects of insulin:

Glucose into cells
Glycogen creation
Uptake of amino acids, Phos, K, Mg
Protein synthesis/inhibited proteolysis
Fatty acid/TG synthesis
↓ lipolysis
DNA/gene regulation

7

Portal circulation receives basal insulin rate of:

1U/hr

8

With meals, insulin secretion increases:

5-10x

9

Average daily requirement of insulin:

40U

10

ANS influence on insulin secretion:

α stimulation ↓ insulin
β and PSNS stimulation ↑ insulin

11

History of making insulin:

Stage 1: insulin extracted from pigs/cows
Stage 2: replaced one 'wrong' amino acid to make it identical to human
Stage 3: Make yeast or e.coli produce it instead

12

Rapid-acting forms of insulin:

Lispro (Humalog)
Aspart (Novalog)
Glulisine (Apidra)

13

Short-acting form of insulin:

Regular (Humulin R/Novolin R)

14

Intermediate-acting form of insulin:

NPH (Humulin N/Novolin N)

15

Long-acting forms of insulin:

Glargine (Lantus)
Detemir (Levemir)
Ultralente

16

Delivery forms for insulin:

SQ
IV
Inhaled

17

Insulin mixtures available:

R/NPH
Rapid/NPH

18

Long-acting insulin used to mimic:

Basal insulin rate

19

Insulin mixture incompatibilities:

Do not mix glargine with others

20

PK of IV regular insulin:

E1/2t of IV bolus: 5-10 min
Duration: 30-60 minutes
Metabolized in liver/kidneys by proteolytic enzyme

21

Insulin's relatively long duration is due to:

Tightly binding to receptors

22

Formulation to use IV:

U-100 (100 units/ml)

23

Onset/peak/duration of rapid-acting insulin (lispro):

Onset: 10-15 min
Peak: 30-60 min
Duration: 3-5 hrs

24

Onset/peak/duration of short-acting insulin (regular):

Onset: 30-60 min
Peak: 1-5 hrs
Duration: 5-8 hrs

25

Onset/peak/duration of intermediate-acting insulin (NPH):

Onset: 1-2 hrs
Peak: 6-10 hrs
Duration: 16-20 hrs

26

Onset/peak/duration of long-acting insulin (glargine):

Onset: 2-6 hrs
Peak: none
Duration: 24 hrs

27

Delivery methods for insulin:

Syringe
Pens
Jet injectors
Insulin pumps

28

A/E of insulin injection:

Site rxns
Lipodystrophy at site
Protamine allergy
Weight gain
Hypoglycemia!!

29

S/s of hypoglycemia:

Diaphoresis
Tachycardia
HTN
CNS agitation
Seizures
Coma

30

Drugs that oppose the hypoglycemic effects of insulin:

ACTH
Glugacon
Estrogens

31

Drug that decreases insulin release/mobilizes glucose:

Epinephrine

32

Drugs that prolong insulin duration:

Tetracycline
Chloramphenicol
Salicylates

33

Drugs that increase hypoglycemic effects of insulin:

MAOIs

34

In a type I diabetic 1 U will ↓ BG by:

40-50 mg/dL

35

In a type II diabetic 1 U will ↓ BG by:

30-40 mg/dL

36

Advantages of tight periop BG control:

↑ healing
↓ infection, diuresis, DKA

37

Disadvantages of tight periop BG control:

Hypoglycemia risk without labor intensive monitoring/adjustments

38

Nontight periop managment of diabetes:

D5W @ 100-125cc/hr in 2nd IV
30-50% of normal AM intermediate insulin
Check BG q1-2hr, adjust D5W
SS insulin for BG > 200-250

39

Tight periop management of diabetes:

D5W @ 100-150cc/hr in 2nd IV
50U regular insulin in 250cc NS piggybacked
Insulin rate: (last BG/150)/hr
** BG/100 for steroids, obese, infection
Add 20mEq K+ for each liter of glucose infused

40

Tx of hyperkalemia:

10U regular insulin IV
25g glucose
1 amp D50
Over 5 minutes

41

Tx of hypoglycemia:

Conscious: Fast acting oral sugar
Anesthetized: 25-50ml D50

42

MoA of sulfonylureas:

Stimulates release of insulin from β cells (binds to ATP sensitive K+ channels that allow depolarization)

Enhances β cell sensitivity to glucose
Enhances tissue sensitivity to insulin
Normalizes hepatic glucose production

43

FBG, A1c reduction with sulfonylureas:

60-70 mg/dL
Up to 2%

44

1st generation sulfonylureas:

Tolbutamide
Chlorpropamide

45

2nd generation sulfonylureas:

Glipizide
Glyburide
Glimepiride

46

1st vs 2nd generation sulfonylureas:

1st has more drug interactions/SE than 2nd

2nd 100x more potent but no more effective

47

PK of sulfonylureas:

90-98% protein bound
Hepatic metabolism

48

Renal impairment best served by these sulfonylureas:

Glipizide or tolbutamide

49

A/E of sulfonylureas:

GI: nausea, fullness, cholestasis, LFTs, appetite stim
GU: ADH-like effect
Derm: pruritis, rash
Hypoglycemia

50

Pre-op mgmt of sulfonylureas:

Hold 24-48 hrs preop

51

MoA of sulfonylureas:

**Stimulates release of insulin from β cells (binds to ATP sensitive K+ channels that allow depolarization)**

Enhances β cell sensitivity to glucose
Enhances tissue sensitivity to insulin
Normalizes hepatic glucose production

52

Class and MoA of metformin:

Biguanide

**Decreases hepatic and renal glucose production**

Enhances insulin receptor binding
Increases glucose utilization, decreases insulin resistance
Requires insulin to work!

53

Clearance of metformin:

Excreted unchanged by kidneys

54

FPG change from metformin:

60 mg/dL
More with sulfonylureas

55

Benefits of metformin:

No weight gain
May ↑ HDL, ↓ LDL/TG
Hypoglycemia rare

56

A/E of metformin:

GI: diarrhea, metallic taste, nausea
Lactic acidosis
Rash

57

Contraindications for metformin:

ESRD: ♀ Cr > 1.4, ♂ Cr > 1.5
Hepatic dysfunction
CHF, shock, hypoxic pulm disease

58

Examples of thiazolidinediones:

Pioglitazone (Actos)
Rosglitazone (Avandia)

59

MoA of thiazolidinediones:

**Improves insulin sensitivity/decreases insulin resistance**

Reduces hepatic glucose production

60

FBG/A1c changes with thiazolidinediones:

FBG ↓ 50 mg/dL
A1c ↓ 1-2%

61

Clearance of thiazolidinediones:

Hepatic metabolism

62

Unique advantage of thiazolidinediones:

Will restore ovulation in women who had stopped due to insulin resistance

63

A/E of thiazolidinediones:

Edema
Weight gain
Hepatotoxicity

64

Black box warnings for thiazolidinediones:

CHF - cause or exacerbate
Possible MI with rosiglitazone

65

Examples of alpha-glucosidase inhibitors:

Acarbose (Precose)
Miglitol (Glyset)

66

MoA of alpha-glucosidase inhibitors:

Antagonizes enzymes in brush border that digest complex carbs to delay glucose absorption and lower post-prandial hyperglycemia

67

FBG/PPG/A1c changes with alpha-glucosidase inhibitors:

FBG ↓ 25-30
PPG ↓ 60-70
A1c ↓ 0.7 - 0.9%

68

Clearance of alpha-glucosidase inhibitors:

Excreted in stool

69

A/E of alpha-glucosidase inhibitors:

Abdominal pain/distention
Diarrhea
Flatulence

70

Considerations with alpha-glucosidase inhibitors:

Take with first bite of meal
Caution with IBD, colon ulceration, obstruction

71

Examples of meglitinides:

Repaglinide (Prandin)
Nateglinide (Starlix)

72

MoA of meglitinides:

Stimulates insulin secretion from β cells

73

PK of meglitinides:

Onset and peak: 1 hr
Duration: 4 hrs

74

Administration of meglitinides:

Take 15-30 min before meals
Skip meal - skip dose
Add meal - add dose

75

A/E of meglitinides:

Hypoglycemia
N/V/C/D, heartburn
Headache

76

MoA of gliptins:

Inhibit DPP-4, which stimulates GLP-1, which enhances glucose-dependent insulin secretion

77

Example of gliptins:

Sitagliptan (Januvia)

78

PK of sitagliptan:

E1/2t: 12 hours

79

Efficacy of gliptins:

Modest; third-line drug

80

A/E of gliptins:

Rare fatal pancreatitis, anaphylaxis

81

MoA of exenatide:

GLP-1 analog; identical MoA to gliptins

82

A/E of exenatide:

N/V
Antibody development
Pancreatitis (can be fatal)
Transplant-requiring renal failure
Hypersensitivity
Delayed gastric emptying

83

MoA of pramlintide:

Analog of amylin that ↓ gastric emptying, glucagon secretion, and ↑ feeling of satiety

84

PK of pramlintide:

Peak: 20 min post-SC injection
E1/2t: 49 minutes
Metabolized in kidneys

85

Indications for pramlintide:

Enhance insulin effects in DM I/II patients who cannot control well with insulin

86

A/E of pramlintide:

Hypoglycemia
Nausea
Site rxns
Decreased absorption of drugs