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Pharma > Pancreatic hormones and parenterally applied anti-diabetic drugs. Pharmacotherapy of IDDM. > Flashcards

Pancreatic hormones and parenterally applied anti-diabetic drugs. Pharmacotherapy of IDDM. Flashcards

1
Q

What are the indications of insulin?

A

DM
Gestational DM
Diabeti critical states: DKA and hyperosmolar hyperglycaemic states.
Hyperkalemia

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2
Q

What are the sites of degeneration of insulin?

A

Liver
Kidney
Muscle

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3
Q

How is insulin degraded in the liver?

A

50% is destroyed in a single passage before reaching the general circulation. In severe impairment, insulin metabolism decreases and thus there is longer half life

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4
Q

How is insulin degraded in the kidney?

A

Filtrated by glomeruli, reabsorption by tubules, degradation in tubule. In severe impairment, insulin metabolism decreases and thus there is longer half life

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5
Q

How is insulin degraded in the muscle?

A

Minor significance

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6
Q

What are the adverse effects of insulin?

A 
Lipoatrphy or lipohypertrophy 
Edema
Allergic skin reactions
Anaphylaxis (rare)
Hypokalemia 
Hypoglycemia 
Acute bronchospasm
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7
Q

Why does insulin cause hypokalaemia?

A

because insulin enhances K+ influx into cells.

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8
Q

What are the duration of action of insulin’s?

A

Ultrashort acting
short acting
intermediate acting
ultra-long-acting

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9
Q

Name the ultra-short-acting insulins?

A

Insulin lispro
Insulin aspart
Insulin glulisine

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10
Q

Name the short-acting insulins?

A

Regular human insulin

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11
Q

Name the intermediate acting insulins?

A

Neutral protamine

Hagedorn insulin

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12
Q

Name the ultra-long-acting insulins?

A

Insulin glargin
Insulin determir
Insulin degludec

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13
Q

What is the onset of action of ultra short acting insulins?

A

20-30 mins

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14
Q

What is the duration of action of ultra-short-acting insulins?

A

3-4h

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15
Q

What is the onset of action of short acting insulins?

A

1h

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16
Q

What is the duration of action of short acting insulins?

A

5-6h

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17
Q

What is the onset of action of intermediate acting insulin?

A

4-5h

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18
Q

What is the duration of action of intermediate acting insulins?

A

12-14h

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19
Q

When are ultra short acting insulins used?

A

They control the post-prandial glucose spine.

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20
Q

When are ultra-short-acting insulin taken?

A

Given with the meal 3x/day

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21
Q

When are short-acting insulin used?

A

1h pre-prandial SC injection for ordinary maintenance regimes.
They are also used in emergencies (DKA) - administered IV

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22
Q

When are short acting insulins administered IV?

A

In emergencies such as DKA

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23
Q

How are short acting insulins administered in ordinary maintenance regimes?

A

SC

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24
Q

What is the use of intermediate acting insulin?

A

Basal (fasting) control in DM1 and 2

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25
Q

How often are intermediate acting insulins administered?

26
Q

When are ultra-long-acting insulins used?

A

Basal (fasting) control

27
Q

Why do ultra-long-acting insulins not produce hypoglycemia?

A

Because there is no peak activity, unlike shorter acting rugs

28
Q

Do ultra long acting insulin produce hypoglycaemia?

29
Q

How often are ultra-long acting insulins administered?

A

1x/day (given at the same time daily).

30
Q

Name the incretins

31
Q

Where is GLP1 produced?

A

produced in the ileum and colon upon ingestion of food

32
Q

Where is GIP produced?

A

produced in the duodenum and jejunum

33
Q

What is the effect of GLP1?

A

Increase release of insulin

Decrease release of glucagon

34
Q

What is the effect of GIP?

A

Increase release of insulin

35
Q

In DM2, what happens to GIP and GLP1?

A

GIP - effect on insulin is lost

GLP1 - the effect is kept

36
Q

Name the agents acting on the GLP1 receptors?

A 
Exenatide
Lixisenatide
Liruaglutide 
Albiglutide
Dulaglutide
37
Q

What are the clinical indications of agents acting on the GLP1 receptor?

A

Adjuvant treatment in DM2.

38
Q

What is the mechanism of action of GLP1 analogues?

A
  • Glucose mediated insulin release
  • Delaying gastric emptying
  • Decreased post prandial glucagon release
  • Decreased appetite
39
Q

What are the advantages of agents acting on GLP1 receptor?

A
  • The effect is glucose-dependent and thus there is no hypoglycemia
  • There is no weight gain
40
Q

What are the adverse effects of agents acting on the GLP1 receptor?

A 
N/V
Diarrhea
Constipation 
Pancreatitis (Exenatide and Liraglutide)
Decreased appetite can lead to weight loss
Hypoglycemia when administered with SU
Local reactions
41
Q

How is Exenatide administered?

A

SC 2X/day

Retarded preparation is possible

42
Q

How is Lixisenatide administered?

A

SC 1x/day

Long acting

43
Q

How is Albiglutide administered?

A

SC 1x/week
ultra long acting
fusion to human albumin

44
Q

How is Dulaglutide administered?

A

SC 1x/week

Ultra-long-acting

45
Q

Name the amylin analogue?

A

Pramlinitide

46
Q

What is the action of Pramlinitide?

A
  • Decrease in post-prandial glucagon release
  • Decreased gastric emptying
  • Decreased appetite
47
Q

What are the clinical indications of Pramlinitide?

A

DM type 1 and 2 (because it does not require functioning beta cells).

48
Q

How is Pramlinitide administered?

A

Preprandial SC

49
Q

What is the adverse effect of Pramlinitide?

A

Relatively high risk of hypoglycemia

50
Q

What is pramlinitide?

A

It is a synthetic version of amylin which slows the rate at which food is absorbed from the intestine.

51
Q

In what position is the AA altered in ultra-short acting insulin analogues?

A

B28 position

52
Q

What AA is altered in lispro?

A

B28 - PROLINE AND LYSIN

53
Q

What AA is altered in aspart?

54
Q

What AA is altered in glulisine?

55
Q

What other clinical use is protamine?

A

anti-heparin

56
Q

What is the isoelectric point of human insulin?

57
Q

What is the isoelectric point of glargin insulin?

58
Q

What is the chemical structure of determir?

A

The threonine in position B30 has been omitted and myristic acid replaces it

59
Q

What is the duration of action of degludec?

60
Q

What is the chemical structure of degludec?

A

The amino acid residue threonine in position B30 of human insulin has been omitted and the lysine in position B29 has been coupled to hexadepanedioic acid via a glutamic acid linking molecule.

61
Q

What are the parenteral anti-diabetics?

A

Amylin analogue

Agents acting on the GLP1 receptor

Pharma (23 decks)

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