EXAM #5: ANTIDIABETIC AGENTS Flashcards Preview

Pharmacology > EXAM #5: ANTIDIABETIC AGENTS > Flashcards

Flashcards in EXAM #5: ANTIDIABETIC AGENTS Deck (64):
1

What is the product of alpha cells in the pancreas?

Glucagon

2

What is the product of beta cells in the pancreas?

Insulin and amylin

3

What is the product of delta cells in the pancreas?

Somatostatin

4

What is the product of G cells in the pancreas?

Gastrin

5

What is the product of F cells in the pancreas?

Pancreatic polypeptide

6

What type of hormone is insulin? What are the implications?

- Peptide hormone that can bind EXTRCELLULAR receptors

*Note that from a therapeutic standpoint, oral insulin is not a viable option

7

List the factors that will upregulate insulin release?

Glucose
Amino acids
Incretins
Epi/ B-2 adrenergic
Vagus

8

List the factors that will downregulate insulin release?

NE/a-2 adrenergic
Amylin

9

Outline the response of the pancreatic beta-cell to glucose.

1) Glucose comes into the cell via the glucose transporter (GLUT-2)
2) Intracellular ATP increases
3) High levels of intracellular ATP cause ATP-sensitive K+ channels to CLOSE
4) Depolarization follows, opening voltage-gated Ca++ channels
5) Ca++ dependent Ca++ release of insulin packaged in secretory vesicles= insulin release

10

What is the major metabolic response to insulin?

Translocation of GLUT-4 transporters from the cytoplasmic compartment to the membrane

*Especially in skeletal muscle and adipose tissue

11

What is the major function of GLUT-4 transporters?

Insulin mediated uptake of glucose

12

Generally, what is the function of insulin action on: 1) fatty acids, 2) glucose, 3) amino acids?

Insulin promotes conversion of smaller molecules to their storage to the storage forms i.e:
1) Fatty acids to TAG
2) Glucose to glycogen
3) Amino acids to protein

13

What metabolic processes are favored in the absence of insulin?

1) Gluconeogenesis
2) Glycogenolysis

14

What is the key difference between Type I and Type II DM?

I= IDDM
II= NIDDM

15

What is the key pathologic characteristic of Type I DM?

Autoimmune Beta cell destruction leading to absolute insulin deficiency

16

What is the key pathologic characteristic of Type II DM?

Insulin resistance i.e. increased insulin needed for same effect

17

What are the signs/sx of Type I DM?

- Polyuria
- Polydipsia
- Polyphagia

*Remember the 3 P's of Type I DM

18

What are the signs/sx of Type II DM?

- Infection
- Neuropathy
- Obesity/ metabolic syndrome

19

What is normal fasting blood glucose level?

Less than 100 mg/dL

20

What is a diabetic fasting blood glucose level?

Roughly 140 mg/dL

21

What plasma blood glucose level should one be at an hour or so after a meal?

Less than 200 mg/dL

22

What is the mainstay treatment for Type I DM?

Insulin

23

What is the one route that insulin cannot be administrated?

Oral

*Note that SQ is most common

24

What is the purpose of altering amino acids in the beta chain of insulin?

- Alters the "stickiness" of the insulin
- Will complex with other insulin or not

*Implications for duration of action/onset

25

What has been done to make rapid acting insulin?

Amino acid change so that insulin peptide complexes DO NOT occur

26

What are the examples of rapid-acting insulin?

Insulin lispro
Insulin aspart
Insulin glulisine

27

What is the onset of rapid acting insulin?

10-30 min

28

What is the duration of action of rapid-acting insulin?

3-5 hours

29

What is an example of short-acting insulin?

Regular insulin

*Forms complexes*

30

What is the duration of action for short-acting insulin?

4-12 hours

31

What is an example of intermediate acting insulin?

NPH

*Forms protamine-insulin complexes

32

What is the duration of action of intermediate acting insulin?

10-20 hours

33

What are examples of long-acting insulin?

Glargine
Detemir

34

How is insulin formulated to be long-acting?

Forms a precipitate at neutral pH

35

What is the duration of action for long-acting insulin?

12-20 or 22-24 hours

36

What type of insulin is used in an insulin pump vs. SQ injection?

Pump= rapid only

SQ= rapid and long-acting

37

How would you manage eating a meal with insulin?

Rapid-short acting

38

How are basal levels of insulin maintained?

Long-acting insulin

39

What is intermediate duration insulin typically used for?

Overnight/ sleeping

40

What is the most common adverse effect of insulin? What are other adverse effects seen with insulin theray?

Hypoglycemia*

*Also, injection site reactions--lipohypertrophy or lipoatrophy-- that require changing sites*

41

What are the signs/sx. of hypoglycemia?

SNS:
- Tachycardia
- Diaphoresis
- Tremors
- Nausea
- Hunger
- Confusion
- Coma

42

How is hypoglycemia treated?

Glucose or glucagon

43

What is the first line agent to treat DM-II?

Metformin

44

What is the MOA of Metformin?

- Decreased hepatic glucose output
- Increased utilization in the peripheral tissue

*Not really understood, but NOT dependent on B-cell function*

45

What is the key adverse effect with Metformin?

GI disturbances

46

List the sulfonylureas and meglitinides.

Glimepiride
Glipizide
Glyburide

Repaglinide
Nateglinide

47

What is the MOA of the sulfonylureas and meglitinides?

Inhibit ATP-sensitive potassium channel of the Beta-cell resulting in insulin release

48

What adverse effects are seen with the sulfonylureas and meglitinides?

Weight gain
Hypoglycemia

49

What are the Glucosidase inhibitors?

Acarbose
Miglitol

50

What is the MOA of the Glucosidase inhibitors?

Inhibit the brush border glucosidase enzyme the prevent absorption of glucose

51

What adverse effects are seen with Glucosidase inhibitors?

GI disturbances

52

When are Glucosidase inhibitors contraindicated?

Patients with pre-existing GI disorder e.g. Lactose intolerance

53

What are the Thiazolindinediones?

Pioglitazone
Rosiglitazone

54

What is the MOA of the Thiazolindinediones?

Generally, increase the expression of GLUT-4

*Increases peripheral glucose uptake

55

What key adverse effects are associated with Thiazolindinediones?

Cardiovascular
Hepatotoxicity

56

What is the amylinomimetic drug?

Pramlintide

57

What is the MOA of Pramlintide?

- Inhibit glucagon release
- Inhibit gastric emptying
- Anorectic effect

58

What are the adverse effects of Pramlintide?

- Anorexia
- Hypoglycemia
- Delayed drug absorption

59

What are the incretins?

Exenatide
Liraglutide

60

What is the MOA of the incretins?

Increased insulin secretion by binding to incretin receptors on beta-cells

61

What adverse effects are associated with the incretins?

Acute pancreatitis

62

What is the normal function of DPP?

Breakdown of incretins

*Incretins normally stimulate insulin release

63

What are the DPP inhibitors?

Sitagliptin
Saxagliptin
Linagliptin

64

What are the adverse effects of DPP inhibitors?

- Acute pancreatitis
- Hemorrhagic/ necrotizing pancreatitis

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