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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

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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
How often are intermediate acting insulins administered?
2x/day
26
When are ultra-long-acting insulins used?
Basal (fasting) control
27
Why do ultra-long-acting insulins not produce hypoglycemia?
Because there is no peak activity, unlike shorter acting rugs
28
Do ultra long acting insulin produce hypoglycaemia?
No
29
How often are ultra-long acting insulins administered?
1x/day (given at the same time daily).
30
Name the incretins
GLP-1 | GIP
31
Where is GLP1 produced?
produced in the ileum and colon upon ingestion of food
32
Where is GIP produced?
produced in the duodenum and jejunum
33
What is the effect of GLP1?
Increase release of insulin | Decrease release of glucagon
34
What is the effect of GIP?
Increase release of insulin
35
In DM2, what happens to GIP and GLP1?
GIP - effect on insulin is lost | GLP1 - the effect is kept
36
Name the agents acting on the GLP1 receptors?
``` Exenatide Lixisenatide Liruaglutide Albiglutide Dulaglutide ```
37
What are the clinical indications of agents acting on the GLP1 receptor?
Adjuvant treatment in DM2.
38
What is the mechanism of action of GLP1 analogues?
- Glucose mediated insulin release - Delaying gastric emptying - Decreased post prandial glucagon release - Decreased appetite
39
What are the advantages of agents acting on GLP1 receptor?
- The effect is glucose-dependent and thus there is no hypoglycemia - There is no weight gain
40
What are the adverse effects of agents acting on the GLP1 receptor?
``` N/V Diarrhea Constipation Pancreatitis (Exenatide and Liraglutide) Decreased appetite can lead to weight loss Hypoglycemia when administered with SU Local reactions ```
41
How is Exenatide administered?
SC 2X/day | Retarded preparation is possible
42
How is Lixisenatide administered?
SC 1x/day | Long acting
43
How is Albiglutide administered?
SC 1x/week ultra long acting fusion to human albumin
44
How is Dulaglutide administered?
SC 1x/week | Ultra-long-acting
45
Name the amylin analogue?
Pramlinitide
46
What is the action of Pramlinitide?
- Decrease in post-prandial glucagon release - Decreased gastric emptying - Decreased appetite
47
What are the clinical indications of Pramlinitide?
DM type 1 and 2 (because it does not require functioning beta cells).
48
How is Pramlinitide administered?
Preprandial SC
49
What is the adverse effect of Pramlinitide?
Relatively high risk of hypoglycemia
50
What is pramlinitide?
It is a synthetic version of amylin which slows the rate at which food is absorbed from the intestine.
51
In what position is the AA altered in ultra-short acting insulin analogues?
B28 position
52
What AA is altered in lispro?
B28 - PROLINE AND LYSIN
53
What AA is altered in aspart?
Aspartate
54
What AA is altered in glulisine?
Glutamate
55
What other clinical use is protamine?
anti-heparin
56
What is the isoelectric point of human insulin?
pH 5.4
57
What is the isoelectric point of glargin insulin?
pH 7.0
58
What is the chemical structure of determir?
The threonine in position B30 has been omitted and myristic acid replaces it
59
What is the duration of action of degludec?
40h
60
What is the chemical structure of degludec?
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
What are the parenteral anti-diabetics?
Amylin analogue | Agents acting on the GLP1 receptor

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