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PHARMACOLOGY > [PF] INSULIN AND OHA > Flashcards

[PF] INSULIN AND OHA Flashcards

1
Q

Fasting plasma glucose criteria for the diagnosis of diabetes:

A

> 7.0 mM (126 mg/dL)

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2
Q

Drugs that promote hypoglycemia:

A

“BTS meets BAPEL”

Beta adrenergic antagonists
Theophylline
Salicylates, NSAIDs
Bromocriptine
ACE inhibitors
Pentamidine
LiCl
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3
Q

Goal for A1C

A

<7.0%

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4
Q

Blood pressure

A

<140/90

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5
Q

Mainstay for treatment of virtually all type 1 and many type 2 diabetes patients.

A

Insulin therapy

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6
Q

Insulin may be administered:

A

IV, IM or SQ

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7
Q

For long term treatment

A

SQ Insulin

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8
Q

Short acting insulin:

A

“GLAR”

Glulisine
Lispro
Aspart
Regular

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9
Q

Long acting insulin:

A

Detemir
Glargine
Degludec
NPH

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10
Q

Short acting regular insulin should be injected _______ minutes BEFORE a meal.

A

30-45 minutes

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11
Q

IV or IM

A

Regular, unbuffered, 100 units/mL insulin

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12
Q

Only subcutaenous

A

Regular, unbuffered, 500 units/mL insulin

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13
Q

Absorbed more rapidly from subcutaneous sites than regular insulin

A

Short-acting insulin analogue

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14
Q

Short acting insulin analogue should be injected ______ or less before a meal.

A

15 minutes

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15
Q

Identical to human insulin except at positions B28 and B29.

A

Insulin Lispro

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16
Q

Rapid absorption and shorter duration of action.

A

Insulin Lispro

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17
Q

Insulin aspart is formed by the replacement of ______ at B28 with aspartic acid.

A

proline

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18
Q

Dissociates rapidly into monomers following injection.

A

Insulin aspart

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19
Q

Formed when glutamic acid replaces lysine at B29 and lysine replaces asparagine at B3

A

Insulin glulisine

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20
Q

Mixed with short-acting insulin

A

Insulin glargine

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21
Q

Lower risk of hypoglycemia

A

Insulin glargine

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22
Q

Administered at any time during the day

A

Insulin glargine

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23
Q

In patients with type 1 diabetes, insulin DETEMIR is administered ______ a day.

A

twice

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24
Q

Has a smoother time action profile and produces a reduced prevalence of hypoglycemia than NPH insulin.

A

Insulin Detemir

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25
Q

Forms multihexamers after injection subcutaneously.

A

Insulin degludec

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26
Q

It has less severe hypoglycemia than glargine

A

Insulin degludec

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27
Q

Insulin dosing and regimens

A
  1. Site of injection
  2. The type of insulin
  3. Subcutaneous blood flow
  4. Smoking
  5. Regional muscular activity at the site of the injection
  6. The volume and concentration of the injected insulin
  7. Depth of injection
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28
Q

In a mixed population of patients with type 1 diabetes, the average dose of insulin is usually _______ with a range of 0.4 - 1 units/kg/d.

A

0.6 - 0.7 units/kg body weight per day

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29
Q

Obese patients generally and pubertal adolescents may require more ________ because of resistance of peripheral tissues to insulin.

A

About 1-2 units/kg/d

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30
Q

Patients who require less insulin than others

A

0.5 units/kg/d

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31
Q

The major risk that must be weighed against benefits of efforts to normalize glucose control.

A

Hypoglycemia

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32
Q

(Enlargement of subcutaneous fat depots) has been ascribed to the lipogenic action of high local concentrations of insulin.

A

Lipohypertrophy

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33
Q

Sulfonylureas:

A
  1. Glimepiride
  2. Glipizide
  3. Glipizide (extended release)
  4. Glyburide
  5. Glyburide (micronized)
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34
Q

Nonsulfonylureas (Meglitinides):

A
  1. Nateglinide

2. Repaglinide

35
Q

GLP-1 Agonists:

A
  1. Albiglutide
  2. Dulaglutide
  3. Exenatide
  4. Liraglutide
  5. Lixisenatide
36
Q

Dipeptidyl peptidase-4 inhibitors:

A
  1. Alogliptin
  2. Linagliptin
  3. Saxagliptin
  4. Sitagliptin
  5. Vildagliptin
37
Q

Sulfonylureas are all effectively absorbed from the ________.

A

GI tract

38
Q

_____ and ________ can reduce absoprtion of sufonylureas.

A

Food and hyperglycemia

39
Q

_____ of Sulfonylureas are bound to protein.

A

90-99%

40
Q

Hypoglycemic effects of Sulfonylureas are evident for _______.`

A

12-24

41
Q

Sulfonylureas are metabolized in the ______ and metabolites are excreted in the urine.

A

Liver

42
Q

Adverse effects of sulfonylureas:

A

Hypoglycemia which can lead to coma

Weight gain

43
Q

Less frequent side effects of sulfonylureas:

A
  1. Nausea and vomiting
  2. Cholestatic jaundice
  3. Agranulocytosis
  4. Aplastic and hemolytic anemias
  5. Generalized hypersensitivity reactions
  6. Dermatological reactions
44
Q

Displace the sulfonylureas from binding proteins thereby transiently increasing the concentration of free drug.

A

Sulfonamides
Clofibrate
Salicylates

45
Q

May enhance the action of SU and cause hypoglycemia.

A

Ethanol

46
Q

Therapeutic uses of Sulfonylureas

A

Diabetes mellitus type 2

47
Q

Non-sulfonylureas:

A

Repaglinide

Nateglinide

48
Q

Repaglinide is absorbed rapidly from the _________.

A

GI tract

49
Q

Repaglinide peak blood levels are obtained within ______

A

1 hour

50
Q

The half life of repaglinide is about _______

A

1 hour

51
Q

Metabolized primarily by the liver (CYP3A4) to inactive derivatives.

A

Repaglinide

52
Q

The major side effect of repaglinide is _______.

A

Hypoglycemia

53
Q

Is associated with a decline in efficacy (secondary failure) after initially improving glycemic control.

A

Repaglinide

54
Q

Certain drugs may potentiate the action of repaglinide by displacing it from plasma protein-binding sites

A
  1. Beta blockers
  2. Chloramphenicol
  3. Coumarin
  4. Maois
  5. NSAIDs
  6. Probenecid
  7. Salicylates
  8. Sulfonamide
55
Q

Certain drugs may potentiate the action of repaglinide by altering it metabolism:

A
  1. Gemfibrozil
  2. Itraconazole
  3. Trimethoprim
  4. Cyclosporine
  5. Simvastatin
  6. Clarithromycin
56
Q

The drug’s major therapeutic effect is reducing postprandial glycemic elevations in patients with type 2 diabetes.

A

Nateglinide

57
Q

Nateglinide is most effective when administered at a dose of ______, 875 three times daily, 1-10 mins before a meal.

A

120 mg

58
Q

It is metabolized primarily by hepatic CYPs (2C(, 70%; 3A4, 30%) and should be used cautiously in patients with hepatic insufficiency

A

Nateglinide

59
Q

About 16% of an administered dose is excreted by the ______ as unchanged drug.

A

kidney

60
Q

The only member of the biguanide class of oral hypoglycemic drugs available for use today.

A

Metformin

61
Q

Metformin MOA activation of AMP-dependent protein kinase (AMPK) by metformin in the ________.

A

Mitochondria

62
Q

Metformin is recommended twice-daily administration at doses of ______.

A

0.5-1.0 g

63
Q

The maximum dose of metformin is ________ but therapeutic benefit starts to plateau at ______.

A

2550 mg

2000 mg

64
Q

A sustained-release preparation of Metformin is available for once-daily dosing starting at ______ DAILY with titration up to 2000 mg as necessary.

A

500 mg

65
Q

Metformin is absorbed primarily from the ________.

A

small intestine

66
Q

Stable, does not bind to plasma proteins

A

Metformin

67
Q

Metformin is excreted unchanged in the ______.

A

urine

68
Q

Half - life of metformin in the circulation of _______

A

2 hours

69
Q

Therapeutic uses of metformin:

A

DM type 2

70
Q

Thiazolidinediones:

A
  1. Rosiglitazone

2. Pioglitazone

71
Q

Thiazolidinediones activates ____________.

A

Peroxisome proliferator-activated receptor-y (PPARy)

72
Q

Regulates the transcription of several insulin responsive genes

A

Thiazolidinediones

73
Q

Increased insulin sensitivity

A

Thiazolidinediones

74
Q

Rosiglitazone and Pioglitazone are absorbed within _______.

A

2-3 hours

75
Q

Bioavailability does not seem to be affected by food.

A

Rosiglitazone and Pioglitazone

76
Q

Rosiglitazone and Pioglitazone is metabolized by the ______.

A

Liver

77
Q

Maybe administered to patients with renal insufficiency.

A

Rosiglitazone and Pioglitazone

78
Q

Not be used if there is active hepatic disease or significant elevations of serum liver transaminases.

A

Rosiglitazone and Pioglitazone

79
Q

GLP-1 receptor agonists:

A
  1. Exenatide
  2. Liraglutide
  3. Albiglutide
  4. Dulaglutide
  5. Lixisinatide
80
Q

DPP4 - inhibitor

A
  1. Sitagliptin (Januvia)
  2. Saxagliptin (Onglyza)
  3. Vildagliptin
  4. Alogliptin
81
Q

DPP4 - inhibitors are absorbed effectively from the ________.

A

Small intestine

82
Q

DPP4 - inhibitors circulate in primarily in unbound form excreted mostly unchanged in the ______.

A

Urine

83
Q

Agents used to treat hypoglycemia

A

Glucagon

Diazoxide

PHARMACOLOGY (6 decks)

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