Diabetes drugs Flashcards

1
Q

What class of drug is metformin?

A

Biguanide

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2
Q

Give examples of sulphonylureas

A

Gliclazide

Glibenclamide

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3
Q

Name a GLP - 1 agonist

A

Exenatide

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4
Q

Give an example of a DDP - 4 inhibitor

A

Sitagliptin

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5
Q

Give an example of a thiazolidinedione (TZD)

A

Pioglitazone

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6
Q

What’s the first line drug for T2DM?

A

Metformin

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7
Q

Is metformin safe in pregnancy?

A

Yes!

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8
Q

What effect does metformin have on weight?

A

Weight loss

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9
Q

How does metformin work?

A

INCREASE INSULIN SIGNALLING:

Decreases hepatic gluconeogenesis by stimulating AMP-activated protein kinases

Increases glucose uptake by skeletal muscle (by increasing insulin signalling)

Increase fatty acid oxidation

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10
Q

Side effects of metformin?

A

GI upset

Lactic acidosis

Liver damage and renal toxicity IF GFR IS ALREADY <30ml/min

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11
Q

What’s the risk of using metformin in kidney disease?

A

lactic acidosis

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12
Q

Can metformin cause hypoglycaemia?

A

No!

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13
Q

How do sulphonylureas work?

A

They bind to the SUR1 part of K+ ATP channels in pancreatic beta cells and cause depolarisation.

This results in Ca2+ influx and insulin release

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14
Q

Why can’t SUs be used in T1DM?

A

They require good beta cell function to work

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15
Q

Can SUs cause hypoglycaemia? Why / why not?

A

Yes! They close K ATP channels regardless of blood glucose levels

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16
Q

Briefly describe the physiology of insulin release

A
  1. Glucose enters beta cells via GLUT2
  2. It is metabolised by glycolysis / Krebs cycle to form ATP
  3. An increase ATP:ADP ratio within the cell causes K+ ATP channels to close, resulting in depolarisation (due to increased intracellular K+)
  4. This allows voltage activated Ca2+ channels to open, causing an influx of calcium into the cell
  5. Calcium mediated exocytosis of insulin follows
17
Q

Side effects of sulphonylureas?

A

HYPOGLYCAEMIA

Weight gain

Headaches

GI upset

18
Q

Effect of SUs on weight?

A

Cause weight GAIN

19
Q

What’s the “reverse tick” effect and which drug class is it associated with?

A

SUs

They work effectively initially, but efficacy decreases over time

20
Q

What does GLP stand for (as in GLP1 agonists)? Give another example of an incretin

A

Glucagon like peptide

Other incretins include GIP

21
Q

Physiologically, what do incretins (like GLP) do?

Based on that, how do GLP-1 agonists work?

A

Incretins are released from cells in the small intestine after a meal and stimulate insulin.

This increases cell uptake of glucose and lowers blood sugar.

GLP1 agonists (e.g exenadite) mimic incretins to enhance insulin secretion

22
Q

Side effects of GLP-1 agonists?

A

Nausea

Decreased appetite

Very rarely pancreatitis (? and pancreatic cancer)

23
Q

Effect of GLP-1 agonists on weight?

A

Weight loss due to decreased appetite

24
Q

Can GLP-1 agonists cause hypoglycaemia?

A

No

25
Q

Physiologically, what does DPP4 do?

Based on this, how do DPP4 inhibitors work?

A

DPP4 breaks down incretins (such as GLP and GIP).

DPP4 inhibitors prolong the glucose-lowering actions of GLP-1 and GIP.

26
Q

Side effects of DPP4 inhibitors?

A

Nausea

Pancreatitis (rare)

Much less potent than GLP-1 agonists - They only work prolonging the action of incretins that are present (and levels are low in T2DM)

27
Q

Do DPP4 inhibitors (sitaglipin) cause weight loss?

A

No

28
Q

How are GLP-1 agonists administered?

A

SC injection

29
Q

How do TZDs work?

A

Enhance the action of insulin at target sites (by acting as exogenous agonists of nuclear receptors)

Act on PPARgamma receptors

(They’re insulin sensitisers)

30
Q

Side effects of TZDs?

A

Weight gain

Fluid retention

Increased incidence of bone fractures

(avoid if heart failure, obese or osteoporotic)

31
Q

Can TZDs cause hypoglycaemia?

A

Only if used with SUs

32
Q

How do SGLT2 inhibitors work?

A

Selectively block reabsoption of glucose by Na / glucose transporters in the proximal tubule, deliberately causing glucosuria and lowering blood sugar

33
Q

Side effects of SGLT2 inhibitors?

A

Thrush

UTI

34
Q

Effect of SGLT2 inhibitors on weight? Risk of hypo?

A

Weight loss (pee out glucose)

Little risk of hypo

35
Q

From the following list, which drugs cause weight loss?

Metformin

SUs (gliclazide)

GLP-1 agonists (exenatide)

DPP4 inhibitor (sitigliptin)

PTZ (pioglitazone)

SGLT2 inhibitor (dapagliflozin)

A

Metformin

GLP-1 agonist

SGLT2 inhibitors

36
Q

Which of the following cause weight gain?

Metformin

SUs (gliclazide)

GLP-1 agonists (exenatide)

DPP4 inhibitor (sitigliptin)

PTZ (pioglitazone)

SGLT2 inhibitor (dapagliflozin)

A

SUs

PTZ

37
Q

Which of the following may cause hypoglycaemia?

Metformin

SUs (gliclazide)

GLP-1 agonists (exenatide)

DPP4 inhibitor (sitigliptin)

PTZ (pioglitazone)

SGLT2 inhibitor (dapagliflozin)

A

SUs