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Pharmacology > Diabetes Pharm > Flashcards

Diabetes Pharm Flashcards

1
Q

what is the MOA of metformin?

A

activates AMPK in hepatocyte mitochondria, inhibiting ATP production
blocks gluconeogenesis and subsequent glucose output
also blocks adenylate cyclase so promotes fat oxidation

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2
Q

what is the drug target of metformin

A

5’-AMPK in hepatocyte mitochondria

and adenylate cyclase

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3
Q

what are the main side effects of metformin?

A

GI side effects - abdo pain, reduced appetite, diarrhoea, vomiting

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4
Q

why does metformin accumulate in the liver (therapeutic effect) and GI tract (side effect)?

A

as it is highly polar, requires organic cation transporter-1 (OCT-1) to access tissues (present in these places)

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5
Q

when is metformin most effective?

A

in patients with remaining functional pancreatic islet cells

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6
Q

what is the MOA for dipeptidyl-peptidase 4 inhibitors? (DPP-4)
sitagliptin

A

inhibits action of DPP-4 in vascular endothelium which normally breaks down incretins in the plasma
therefore limits breakdown of incretins and prolongs their effects

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7
Q

what are incretins?

A

secreted by enteroendocrine cells, stimulate production of insulin when needed and reduce glucagon.
also slow down digestion and decrease appetite

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8
Q

give examples of incretins?

A

GLP-1

GIP

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9
Q

what is the drug target for DPP-4 inhibitors? (sitagliptin)

A

DPP-4 enzyme in vascular endothelium

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10
Q

what are the main side effects of DPP-4 inhibitors?(sitagliptin)

A

upper respiratory tract infections, flu like symptoms

less commonly - severe allergy

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11
Q

what are the contraindications for DPP-4? (sitagliptin)

A

pancreatitis

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12
Q

what is the MOA of sulphonylureas? (gliclazide)

A

inhibits ATP-sensitive K+ channel on pancreatic beta cell
inhibition causes depolarisation of beta cell which stimulates Ca2+ influx
subsequent insulin vesicle exocytosis

aka causes increased release of insulin

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13
Q

what is the drug target for sulphonylureas? (gliclazide)

A

ATP-sensitive potassium channel on pancreatic beta cells

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14
Q

what are the main side effects of sulphonylureas? (gliclazide)

A

weight gain

hypoglycaemia

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15
Q

what is the MOA of SGLT2 inhibitors? (dapaglifozin)

A

reversibly inhibits sodium-glucose cotransporter 2 in PCT

reduces glucose reabsorption and increases urinary glucose excretion

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16
Q

what is the drug target for SGLT2 inhibitors? (dapaglifozin)

A

sodium-glucose cotransporter 2 in proximal convoluted tubule

17
Q

what are the main side effects of SGLT2 inhibitors? (dapaglifozin)

A

urogenital infections
slight decrease in bone formation
can worsen diabetic ketoacidosis
weight loss
BP reduction

18
Q

what are SGLT2 inhibitors dependent on and therefore its contraindications? (dapaglifozin)

A

renal function

therefore less effective in patients with renal impairment

19
Q

when should metformin be prescribed in patients with T2DM?

A

HbA1c above 48mmol/mol even with lifestyle intervention

20
Q

when is the first intensification of metformin treatment for T2DM?

A

HbA1c 58mmol/mol despite on metformin

dual therapy with 2 of DPP4i, SGLT2i, gliclazide, pioglitazone

21
Q

first line treatment for HbA1c over 48 when already given lifestyle advice

A

Metformin

22
Q

first line treatment for HbA1c over 58

A

Metformin

23
Q

why may you not choose to prescribe sulphonylureas (gliclazide)

A

can cause weight gain - not for people with already high BMI

hypoglycaemia risk

24
Q

what patients would you choose to prescribe GLP-1 agonists and SGLT-2 inhibitors to?

A

patients with CVD risk - prevention

25
Q

when are thiazolidinediones contraindicated (pioglitazone)

A

heart failure

26
Q

what diabetes drug is most tolerable

A

DPP-4 inhibitors

moderately effective

27
Q

example of DPP-4 inhibitor

A

sitagliptin

28
Q

example of GLP-1 agonist

A

liraglutide

29
Q

example of sulphonylurea

A

gliclazide

30
Q

example of SGLT-2 inhibitor

A

empagliflozin

31
Q

example of thiazolidinedione

A

pioglitazone

Pharmacology (9 decks)

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