Pharmaco Antidiabetics Agents Flashcards

1
Q

Common feature if all type of diabetes mellitus

A

Hyperglycemia

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2
Q

Classification of diabetes mellitus

A

Insulin dependent diabetes mellitus (type I)

Non insulin dependent diabetes mellitus (type II)

Gestational diabetes

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3
Q

Clinical symptoms of type I

A

Polydipsia
Polyuria
Polyphagia

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4
Q

Clinical management

A

Diet
Exercise
Treatment

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5
Q

Treatment types

A

Exogenous insulin

Oral Hypoglycemic drugs

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6
Q

In what case if exogenous insulin used

A

Type I diabetes mellitus

Sometimes in type II

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7
Q

Goal of exogenous insulin therapies

A

Maintain glucose level close to normal

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8
Q

Why is diabetes treatment individualized

A

Spectrum of patients with diabetes

Symptoms may exist or not , may vary

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9
Q

Classification of exogenous insulin

A

Rapid acting

Short acting

Intermediate acting

Long acting

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10
Q

Onset of action of rapid acting insulin

A

5-10 min

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11
Q

Examples of rapid acting insulin

A

Lispro

Insulin aspart

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12
Q

Insulin aspart can bind to

A

Insulin receptors

IGF-1

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13
Q

Short acting / regular insulin examples

A

Humulin R

Novolin R

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14
Q

Short acting insulin onset of action.

A

30mins

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15
Q

When do you administer regular insulin

A

Administered several minutes before a meal

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16
Q

What type of diabetes is controlled by regular insulin

A

Postprandial hyperglycemia

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17
Q

When should you use regular insulin

A

Surgery
Trauma
Shock
Diabetic ketoacidosis

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18
Q

How many times do you administer rapid and short acting insulin per day

A

2/3 times a day

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19
Q

Intermediate acting insulin names

A

Isophane insulin suspension(NPH)

Insulin zinc suspension (lente insulin)

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20
Q

Onset of action of intermediate acting insulin

A

1-2h

Long duration of action too

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21
Q

What can be combined with intermediate acting insulin to prolong duration of action

A

Zinc

Protamine

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22
Q

Can you use intermediate acting insulinin case of emergency

A

No

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23
Q

How many times a day do you give intermediate acting insulin

A

Once or twice a day

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24
Q

What compound it sounds in high quantity in long acting insulin

A

Protamine and zinc

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25
Q

Examples of long acting insulin

A

Protamine zinc

extended insulin zinc suspension (ultralente)

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26
Q

Duration of action of long acting insulin

A

36 hours

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27
Q

Onset of action of long acting insulin

A

Two or more hours

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28
Q

Factors influencing insulin regimen

A
Diet 
lifestyle 
physical activity
 type of diabetes
Work schedule 
meal times
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29
Q

In insulin regimen what form of combinations of insulin preparations are made

A

Intermediates and short acting insulin combination

70:30 ratio or 50:50 for NPH/regular

70: 30 Humilin
70: 30 Novolin
50: 50 Humulin

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30
Q

Adverse effects of insulin therapy

A

Hypoglycemia with CNS Symptoms ( tremor , lethargy, sensory deficits seizures, loss of consciousness)

Weight gain ( increased caloric storage by insulin)

Allergic rxns for animal derived insulin

Hypokalemia ( Na-K-ATPase stimulation)

Local lipodystrophy (repeated insulin SC injection)

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31
Q

If Hypoglycemia due to insulin therapy what can you do

A

Oral carbohydrates (fruit juice, glucose tablets)

When severe IV glucose or IM glucagon

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32
Q

When are oral hypoglycemic agents used

A

In type two diabetes

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33
Q

Why is compliance for type two diabetes better

A

Because therapy is not injected

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34
Q

Type of drugs in oral hypoglycemic agents

A
Sulfonylureas
Biguanides
Thiazolidinediones
A-glucosidase inhibitors 
Meglitinides
35
Q

Most widely prescribed drugs in treatment of type two diabetes mellitus

A

Sulfonylureas

36
Q

Classification of sulfonylureas

A

First generation

second generation

third generation

37
Q

First generation sulfonylureas

A

Chlorpropamide

Tolbutamide

38
Q

Second generation sulfonylureas

A

Glyburide

Glipizide

39
Q

Third generation sulfonylureas

A

Glimepiride

40
Q

Why are first generation sulfonylureas not frequently used in modern management of diabetes mellitus

A

Delay in time of onset
occasional long duration of action
side effects
More drug interactions

41
Q

Chlorpropamide pk

A

Slow onset of action maximal
Hypoglycemic potential reached at one or two weeks
several weeks to be eliminated

42
Q

Chlorpropamide side effects

A

Flushing especially with alcohol intake

43
Q

Tolbutamide pk

A

Short acting compounds

good for likely to be hypoglycemic patient

44
Q

Why are second generation sulfonylureas better agent than the first

A

More predictable time of onset and duration of action

fewer side effects

45
Q

Potency of glyburide

A

150 more times potent than tolbutamide

46
Q

Duration of action of glyburide

A

24h

47
Q

MOA of sulfonylureas

A

Stimulation of insulin release from pancreatic b-cell

48
Q

Why are sulfonylureas not used in management of type one diabetes

A

Low number available B cells in that form of diabetes

49
Q

Why do obese diabetics respond poorly to sulfonylureas

A

Because Obesity must be associated with insulin resistance

50
Q

Where are sulfonylureas absorbed

A

Git

51
Q

Sulfonylureas excretion

A

Renal or biliary route

52
Q

Does of sulfonylureas

A

Low to intermediate dose at first

gradual increase until dose results in normoglycemia

53
Q

Adverse effects of sulfonylureas

A

Hypoglycemia
weight gain
cross-reactivity when sensitivity to sulfa-containing antibiotics

54
Q

Main biguanides

A

Metmorfin

55
Q

First line treatment of mild to moderate type 2 overweight diabetic’s with insulin resistance

A

Metformin

56
Q

2 formulations a metformin

A

Glucovance

Glucophage XR

57
Q

Glycovance composition

A

Metformin + glyburide

58
Q

Why is glucophage XR better tolerated in patients who are prone to GIT side effects

A

Because it’s extended release product

59
Q

Are biguanides hypoglycemic

A

Not necessarily

60
Q

Do biguanides have effects on secretion or glucagon or somatostatin

A

No

61
Q

Effects of biguanides

A

Decrease intestinal absorption of carbohydrates

Increase glucose uptake (GLUT4)

Increase glycolysis via anaerobic pathway (lactic acidosis)

Increase glucose utilization (glycogenesis)

Decrease gluconeogenesis

62
Q

What can you combine biguanides with

A

Sulfonylureas

Insulin

63
Q

Side effects of biguanides

A
20-25% of patients 
Diarrhea 
Abdominal discomfort 
Nausea
Metallic Taste 
Decreased absorption of B12
64
Q

Thiazolidinediones effect

A

Insulin sensitizing properties
Decrease insulin resistance
Enhance insulin in target tissues

65
Q

Name of Thiazolidinediones

A

Rosiglitazone

Pioglitazone

66
Q

What can you associate rosiglitazone with

A

Metformin

Can also be combined with insulin and sulfonylureas

67
Q

Rosiglitazone action

A

Modest increase in low density lipoprotein And TAGs

68
Q

Thiazolidinediones absorption.

A

From GIT

Metabolized by liver

69
Q

Plasma elimination of Thiazolidinediones

A

2-3h

Urine mostly and then stool

70
Q

Why is Thiazolidinediones dosage gradual

A

Risk of hypoglycemia because effects takes weeks to develop

71
Q

Thiazolidinediones adverse effects

A

Edema
Weight gain
Hypoglycemia (rare)

72
Q

a glucosidase inhibitors action

A

Decrease postprandial hyperglycemia
Decrease carbohydrates absorption from GIT
Inhibit a-glucosidase (glycoamylase, sucrase, maltase, dextranase)

73
Q

How can you make a glucosidase more effective

A

Take it before or with meal

74
Q

In which people are a glucosidase more effective

A

Patients with type II diabetes with 50% carbohydrates diet

75
Q

Can you use a glucosidase in type 1

A

No prohibited

76
Q

Name of a glucosidase

A

Acarbose (low systemic absorption)

Miglitol (high systemic absorption)

77
Q

Adverse effects of a glucosidase

A

GIT disturbances ( loose stool, flatulence, abdominal cramping)

78
Q

Can you have weight gain with a glucosidase inhibitors

A

No weight gain

79
Q

What can you combine a glucosidase inhibitors with

A

Metformin
Sulfonylureas
Insulin

80
Q

Meglitinides moa

A

Augment release of insulin in presence of glucose

81
Q

Name of meglitinides

A

Repaglinide

Nateglinide

82
Q

What can you associate meglitinides with

A

Metformin

83
Q

When is the only situation where meglitinides is used over sulfonylureas

A

Allergy to sulfa drugs

84
Q

Nateglinide compared to repaglinide

A

Faster onset and shorter duration