Pharmacology: Type 2 Diabetes Drugs Flashcards

1
Q

Name an example of a first generation sulphonylurea.

A

Tolbutamide

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2
Q

Name two examples of a second generation sulphonylurea

A

Glibenclamide

Glipizide.

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3
Q

What is the difference between 1st and 2nd generation sulphonylureas.

A

Second generation are more potent and longer acting.

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4
Q

What is the mechanism of action of sulphonylureas

A

The bind to SUR1 in the Katp channel- closing it and causing depolarisation of pancreatic beta cell- results in insulin release.

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5
Q

What are the side effects of sulphonylureas

A

Weight gain

Hypoglycaemia (particularly in elderly, long acting agents or patients with reduced hepatic or renal function)

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6
Q

What are glinides.

A

Similar to sulphonylureas -same mechanism of action (also close Katp channel)

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7
Q

What is the main difference between glinides and sulphonylureas

A

Glinides are less likely to cause hypo

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8
Q

Name two examples of glinides

A

Repaglinide

Nateglinide

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9
Q

When are glinides usually used therapeutically.

A

To be taken right before a meal to reduce post prandial glucose increase

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10
Q

What is the mechanism of action of incretin analogues.

A

They mimic the action of GLP 1 but are longer lasting

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11
Q

What are the side effects of incretin analogues

A

Weight loss
Nausea
Hypoglycaemia
Pancreatitis

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12
Q

How are incretins administered

A

Subcutaneously

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13
Q

Name two incretins

A

Exenatide (twice daily)

Liraglutide (once daily)- longer acting

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14
Q

What is the mechanism of action of DDP 4 inhibitors

A

Inhibit the enzyme dipeptidyl peptidase 4 which usually inhibits the actions of GLP1 and GIP - thus prolonging the action of GLP1 and GIP

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15
Q

Name three examples of DDP 4 inhibitors

A

Sitagliptin
Saxigliptin
Vildagliptin

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16
Q

What do alpha glucosidase inhibitors (acarbose) do?

A

Inhibit the enzyme alpha glucosidase which breaks down starch and disaccharides in the gut- thus slowing gluscose absorption in the gut

17
Q

When is acarbose used

A

In T2DM patients who are not adequately controlled by lifestyle or other drugs

18
Q

What are the main side effects of acarbose

A

GI side effects- diarrhoea, flatulence, bloating

19
Q

Name a biguanide

A

Metformin

20
Q

Give the effects of metformin

A

Reduces hepatic gluconeogenesis.
Increases glucose uptake and utilization by skeletal muscle
Decreases carbohydrate absorption
Increases fatty acid oxidation

21
Q

Why is metformin desirable

A

Oral administration
Does not cause hypo
Causes weight loss
Can be combined with other drugs

22
Q

What are the adverse effects of metformin

A

GI upset
Lactic acidosis- avoid in patients with hepatic or renal impairment
Can interfere with vitamin B12 and folic acid absorption although anaemia is rare
Rash
Liver failure

23
Q

How do thiazolidinediones work to enhance the action of insulin

A

They are agonists of PPAPy nucleur receptors which increase the transcription of genes that code for proteins that are involved in insulin signalling eg GLUT4

24
Q

What are the adverse effects of TZDs

A

Weight gain
Fluid retention
Hepatotoxicity
Increased incidence of bone fractures

25
Q

What TZD should be used as it doesn’t cause hepatotoxiciy

A

Pioglitazone

26
Q

What is the mechanism of action of SGLT2 inhibitors

A

Prevent reabsorption of glucose in the proximal tubule of the kidney - glucosurea

27
Q

Give an example of a SGLT2 inhibitor.

A

Dapaglitlozin

28
Q

What other effects can SGLT2 inhibitors cause

A

weight loss

unlikely to cause hypo

29
Q

Is metformin safe to use in pregnancy

A

yes

30
Q

What is the first line agent for type 2 diabetes

A

Metformin