W14 Diabetes Drugs Flashcards

1
Q

What are the 10 classes of diabetes medication

A
Biguanides 
Alpha-glucosidase inhibitors 
Sulfonylureas 
SGLT2 inhibitors 
Insulin 
meglitinides 
Thiazolidinediones 
Dipeptidyl peptidase-4 (DPP-4) inhibitors 
GLP-1 receptor agonists 
Weight loss agents
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2
Q

What are the actions of insulin on the liver ?

A

Increase glycogen synthesis
Decrease gluconeogenesis
Increase lipogenesis

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3
Q

What promotes the transport of GLUT4 ?

A

Insulin

Exercise

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4
Q

When is basal insulin used ?

A

Between meals and overnight

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5
Q

What are some short acting insulin analogues ?

A

Lispro
Aspart
Glulisine

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6
Q

What are some examples of long acting insulin analogues?

A

Glargine
Detemir
Degludec

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7
Q

What type of insulin is insulin glargine ?

A

Basal

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8
Q

What type of insulin is insulin glargine U300?

A

Basal

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9
Q

What type of insulin is insulin detemir ?

A

Basal

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10
Q

What type of insulin is insulin degludec ?

A

Basal

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11
Q

What type of insulin is regular human insulin and what are some examples ?

A

bolus
Humulin R
Novolin Toronto

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12
Q

What type of insulin are analogue rapid insulins and what are some examples ?

A

Bolus
Aspart (novorapid)
Lispro (humalog)
Glulisine (apidra)

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13
Q

What type of insulin are analogue ultra-rapid insulins and what are some examples?

A

Bolus

Ultra rapid aspart (FiAsp)

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14
Q

What is the primary site of action of biguanide ?

A

Liver

  • decrease glucose output
  • decrease insulin resistance
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15
Q

What is the primary site of action of sulfonylureas/meglitinides ?

A

Pancreas

- increase insulin secretion

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16
Q

What is the primary site of action of thiazolidinediones ?

A

Liver, stomach, adipocytes (?)

- decrease insulin secretion

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17
Q

What is the primary site of actions of DPP-4i, GLP-1 RAs

A

Pancreas, stomach, liver

  • increase insulin secretion
  • decrease glucose output
  • decrease gastric emptying
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18
Q

What is the primary site of action of SGLT2 inhibitors ?

A

Kidneys

- increase urinary glucose excretion

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19
Q

What is the primary site of action of a-glucosidase inhibitors ?

A

Intestines

- decrease carb breakdown and absorption

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20
Q

What class of diabetes medication does metformin belong to?

A

Biguanide

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21
Q

What are some examples of sulfonylureas ?

A

Glyburide
Gliclazide
Glimepiride

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22
Q

What is the mechanism of action of metformin?

A

Liver:
Decrease gluconeogenesis, glycogenolysis, fatty acid oxidation
Intestines:
- increase anaerobic glucose metabolism
Skeletal muscle:
- decrease glucose uptake, glycogenolysis, fatty acid oxidation

Anti-oxidant properties on endothelial cells

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23
Q

Advantages of metformin

A

Glucose lowering
Durable effect
No weight gain, CV side effects, hypoglycaemia

24
Q

Side effects of metformin

A

GI side effects (start low, go slow)

Rare lactic acidosis

25
Q

Metformin dose

A

250-500 mg BID

Maximum 1000 mg BID or 2500 mg in divided doses

26
Q

Examples of short acting secretogogues

A

Repaglinide

Nateglinide

27
Q

Mechanism of action of sulfonylureas

A
Block K(ATP) channel
—> stimulate insulin secretion
28
Q

Advantages of sulfonylureas ?

A

Inexpensive
Easy to administer
Effective glucose lowering

29
Q

Disadvantages of sulfonylureas ?

A

Weight gain
Hypoglycaemia
Durability ?
Effects beta cell function ?

30
Q

Examples of DPP-4 inhibitors

A

Alogliptin
Linagliptin
Saxagliptin
Sitagliptan

31
Q

Examples of short acting GLP-1 receptor agonists

A

Exenatide
Lixisenatide
Liraglutide

32
Q

Long acting GLP-1 RAs

A

Exenatide LAR
Dulaglutide
Semaglutide

33
Q

Mechanism of action of incretins

A
  • reduce gastric emptying
  • reduce appetite
  • increase insulin secretion
  • decrease glucagon secretion
  • decrease hepatic glucose output
34
Q

Advantages of DPP-4 inhibitors

A

Glucose lowering

No weight gain

35
Q

Advantages of GLP-1 RAs

A

Possible weight loss
Glucose lowering
CV benefit

36
Q

Disadvantages of GLP-1 RAs ?

A

Cost/coverage
Injectable
Nausea
Cholelithiasis

37
Q

Disadvantages of DPP-4 inhibitors

A

Cost/coverage
Nasal stuffiness
Increased risk of heart failure (saxagliptin)

38
Q

Examples of SGLT2 inhibitors

A

Canagliflozin
Dapagliflozin
Empagliflozin
Ertugiflozin

39
Q

Mechanism of action of SGLT2 inhibitors

A

Urinary glucose excretion

40
Q

Advantages of SGLT2 inhibitors

A
Easy to administer 
Effective glucose lowering 
Weight loss
Lowers BP 
Low risk of hypoglycaemia 
CV benefit in high risk patients
41
Q

Disadvantages of SGLT2 inhibitors

A
Polyuria 
Volume depletion 
Hyperkalemia 
Orthostatic hypotension 
Yeast infections
Euglycemic DKA 
Increase risk of amputation (canagliflozin)
42
Q

Mechanism of action of thiazolidinediones (TZDs)

A
  • reduce insulin resistance
  • modifies adipocyte differentiation
  • inhibits VEGF-induced angiogenesis
  • reduces lepton levels —> reduced appetite
43
Q

Advantages of TZDs?

A

Easy to administer
Effective glucose lowering
Durable

44
Q

Disadvantages of TZDs

A
Cost/coverage 
Weight gain 
Edema
Worsening CHF 
Distal bone fractures
45
Q

Examples of TZDs

A

Pioglitazone

Rosiglitazone

46
Q

Example of a-glucosidase inhibitor

A

Acarbose

47
Q

Mechanism of action of a-glucosidase inhibitors

A

Inhibits breakdown of non-absorbable complex poly-saccharides
Reduces mono-saccharide absorption

48
Q

Advantages of a-glucosidase inhibitors

A

Not systemically absorbed

Targets post prandial glucose

49
Q

Disadvantages of a-glucosidase inhibitors

A

Modest A1C lowering
GI side effects (gas, bloating, flatulence)
Multiple daily dosing

50
Q

What is first line treatment for T2D?

A

Metformin

51
Q

What are the A1C target guidelines ?

A

Adults, T2D, low risk of hypoglycaemia: <6.5%
Most adults, T1D or T2D: <7%
Frail elderly, limited life expectancy, recurrent hypoglycaemia: 7.1-8.5%

52
Q

When after diagnosis should A1C target be reached?

A

3-6 months

53
Q

Initial therapy choice if A1C <1.5% over target

A

Heathy behaviour, start metformin if not at target in 3 months
Or
Metformin + healthy behaviour

54
Q

Initial therapy if A1C>1.5% over target

A

Metformin + healthy behaviour
And
Consider second concurrent agent

55
Q

When should initial therapy for T2D include insulin +/- metformin?

A

Symptomatic
Hyperglycaemia
And/or
Metabolic decompensation