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BRS YEAR 2 > Pharm - Diabetets > Flashcards

Pharm - Diabetets Flashcards

1
Q

What are the 4 classes of diabetes drugs?

A

Metformin
Dipeptidyl-peptidase 4 inhibitors
Sulphonylurea
Sodium-glucose co-transporter inhibitors

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2
Q

What is the primary effect of metformin?

A
  • Inactivates AMPK in hepatocyte mitochondria
  • Stops ATP production
  • Blocks gluconeogenesis and HGO
  • Blocks adenylate cyclase which promotes fat oxidation
  • Therefore restores insulin sensitivity
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3
Q

Where is the target for metformin?

A

5’-AMPK activated protein kinase

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4
Q

Where does metformin act?

A

Hepatocyte mitchondria

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5
Q

What are the main side effects of metformin?

A

GI:

  • Abdominal pain
  • Decreased appetite
  • Diarrhoea
  • Vomiting
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6
Q

How common are metformin side effects?

A

20-30% of patients

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7
Q

What affects tolerability of metformin?

A

When a slow increase in dose is given there is better tolerability - a very high dose causes side effects

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8
Q

What explains metformin accumulating in the liver and GIT?

A

Metformin is highly polar and requires organic cation transporter 1 (OCT-1) to access tissues

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9
Q

When is metformin most effective?

A

In the presence of endogenous insulin therefore in residual functioning pancreatic islet cells

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10
Q

What is an example of a DPP-4 inhibitor?

A

Sitagliptin

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11
Q

What is the primary effect of DPP-4 inhibitors?

A

Inhibit DPP4

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12
Q

What does DPP-4 do?

A

Metabolises incretins in the plasma

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13
Q

What do incretins e.g. GLP-1 do?

A
  • Secreted by enterendocrine cells and help stimulate the production of insulin when it is needed
  • Reduce production of glucagon by the liver when it is not needed
  • Slow down digestion and decrease appetite
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14
Q

What is the target for DPP4 inhibitors?

A

DPP-4

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15
Q

Where is the effect of DPP4 inhibitors?

A

DPP-4 is found in the vascular endothelium

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16
Q

What are the common side effects of DPP4 inhibitors?

A 
Upper respiratory tract infections 
Flu-like symptoms:
-Runny nose
-Sore throat
-Headache
17
Q

What are the uncommon effects of DPP4 inhibitors?

A

Serious allergic reactions - avoid in patients with pancreatitis

DPP4 = Don’t with Pancreatitis Patients

18
Q

Do DPP4 inhibitors cause weight gain?

A

No

(DPP = Doesn’t Pig People)??

19
Q

When are DPP4 inhibitors only really effective?

A

When some residual pancreatic beta-cell activity is present, as they work by augmenting insulin production

20
Q

What is an example of sulphonylurea?

A

Gliclazide

21
Q

What is the primary effect of sulphonylurea?

A

Inhibits ATP sensitive potassium channel (KATP)

22
Q

What is the role of KATP?

A

Controls beta cell membrane potential - therefore sulphonylurea causes depolarisation stimulating calcium ion influx to beta cells and thus insulin vesicle exocytosis

23
Q

What is the target of sulphonylurea?

A

ATP- sensitive potassium channel

24
Q

Where does sulphonylurea act?

A

Pancreatic beta cells

25
Q

What are the side effects of sulphonylurea?

A

Weight gain

Hypoglycaemia

26
Q

When are sulphonylureas only really active?

A

When some residual pancreatic beta-cell activity is present, as they work by augmenting insulin production

27
Q

How do we mitigate weight gain from sulphonylurea?

A

Concurrent administration with metformin

28
Q

What is an example of SGLT2 inhibitors?

A

Dapaglizofin

29
Q

What is the primary effect of SGLT2 inhibitors?

A

Reversibly inhibits SGLT-2 in the kidney to reduce glucose reabsorption and increase its excretion in the urine

30
Q

What is the target of SGLT2 inhibitors?

A

SGLT-2

31
Q

Where is the effect of SGLT2 inhibitors?

A

Renal proximal convoluted tubule

32
Q

What are the side effects of SGLT2 inhibitors?

A

Uro-genital infections due to increased glucose load

Slight decrease in bone formation

33
Q

What can be worsened by SGLT2 inhibitors?

A

Diabetic ketoacidosis

34
Q

What can SGLT2 inhibitors cause?

A

Weight loss and reduction in blood pressure

35
Q

What influences SGLT2 inhibitors?

A

Normal renal function is needed for SGLT-2 action therefore less effective in patients with renal impairment

BRS YEAR 2 (37 decks)

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