T2DM Drugs Flashcards

Pharmacology

1
Q

Name the 4 actions of T2DM drugs.

A
  1. increase insulin secretion
  2. decrease insulin resistance and reduce hepatic glucose output
  3. slow glucose absorption in GI tract
  4. enhance glucose excretion by kidney
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2
Q

name the 4 classes of drug that increase insulin secretion.

A

sulfonylureas
glinides (meglitinides)
incretic analogues
DPP-4 inhibitors

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3
Q

name the 2 classes of drug that decrease insulin resistance and hepatic glucose output

A

biguanides and thiazolidinediones (glitazones)

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4
Q

name the class of drug that slows glucose absorption from the GI tract

A

alpha-glucosidase inhibitor

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5
Q

name the class of drug that enhances glucose excretion by the kidney

A

sodium glucose type-2 (SGLT2) inhibitors

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6
Q

are alpha-glucosidase inhibitors and sodium glucose type-2 (SGLT2) inhibitors insulin dependent?

A

no

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7
Q

SUR1 subunits regulate __________ channel activity

A

SUR1 subunits regulate POTASSIUM channel activity

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8
Q

___ binding to each of the Kir6.2 subunits closes the channel causing ______________ of the ____ cell and _______ release

A

ATP binding to each of the Kir6.2 subunits closes the channel causing DEPOLARIZATION of the BETA cell and INSULIN release

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9
Q

ADP-Mg2+ binding to the SUR1 subunits ______ the channel maintaining the resting potential of the ____ cell and _________ insulin secretion

A

ADP-Mg2+ binding to the SUR1 subunits OPENS the channel maintaining the resting potential of the BETA cell and INHIBITS insulin secretion

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10
Q

sulfonylureas used in T2DM bind to SUR1 and _____ the channel causing _____________ and insulin release independent of plasma ________ concentration

A

sulfonylureas used in T2DM bind to SUR1 and CLOSE the channel causing DEPOLARIZATION and insulin release independent of plasma GLUCOSE concentration

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11
Q

what do sulfonylurea drugs end in?

A

-ide

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12
Q

give an example of a sulfonylurea

A

glipizide

gliclazide

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13
Q

SUs, in the long term, reduce what complications?

A

microvascular

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14
Q

SUs are used first line if the patient is intolerant to what?

A

metformin

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15
Q

SUs are often used in combination with what?

A

metformin

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16
Q

SUs adverse effect?

A

weight gain

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17
Q

SUs should be avoided in who?

A

elderly, pregnancy and CKD

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18
Q

what do glinides (meglitinides) end in?

A

-glinide

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19
Q

give an example of a glinide

A

repaglinide and netaglinide

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20
Q

glinides should not be used in who?

A

severe hepatic impairment, pregnancy and breast feeding

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21
Q

ingestion of food stimulates release of what?

A

glucagon peptide like-1 (GLP-1) and GIP

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22
Q

GLP-1 and GIP enhance _______ release from beta cells and ________ uptake whereas GLP-1 decreases _________ release from alpha cells

both resulting in decreased blood glucose

A

GLP-1 and GIP enhance _______ release from beta cells and ________ uptake whereas GLP-1 decreases _________ release from alpha cells

both resulting in decreased blood glucose

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23
Q

what is the other name for DPP-4 inhibitors

A

gliptins

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24
Q

what do DPP-4s end in?

A

-gliptin

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25
Q

give an example of a DPP-4 inhibitor

A

sitagliptin

26
Q

what does DPP-4 stand for?

A

dipeptidyl peptidase-4

27
Q

DPP-4s are usually prescribed in combination with what?

A

metformin or SU

28
Q

what is the main adverse effect of a gliptin?

A

DPP-4 inhibitor adverse effect = NAUSEA

29
Q

is there hypoglycaemia or weight gain in gliptins?

A

no

30
Q

can SUs cause hypoglycaemia?

A

no

31
Q

can glinides cause hypoglycaemia?

A

no

32
Q

incretin analogues are peptides that mimic the action of what?

A

GLP-1

33
Q

what do incretin analogues end in?

A

-tide

34
Q

how are incretin analogues administered?

A

SC injection

35
Q

name an incretin analogue

A

extenatide
extenatide
liraglutide

36
Q

what can incretin analogues cause loss of?

A

weight loss

37
Q

do incretin analogues cause hypoglycaemia?

A

no

38
Q

2 side effects of incretin analogues?

A

nausea

pancreatitis - rare

39
Q

name the infrequently used in the UK, brush border enzyme inhibitor that breaks down starch and disaccharides to absorbable glucose

A

alpha-glucosidase inhibitors

40
Q

name an example of a alpha-glucosidase inhibitor

A

acarbose
miglitol
voglibose

41
Q

alpha-glucosidase inhibitor adverse effects?

A
flactulence
loose stools
diarrhoea
abdominal pain
bloating
42
Q

do alpha-glucosidase inhibitors pose risk of hypoglycaemia?

A

no

43
Q

name the first line agent in the treatment of T2DM

A

metformin

unless SEVERE hepatic/renal impairment

44
Q

what does metformin reduce and increase?

A

reduce:

hepatic gluconeogenesis
carbohydrate absorption

increase:

glucose uptake by muscle
fatty acid oxidation

45
Q

metformin is what class of drug?

A

biguanide

46
Q

does metformin cause hypoglycaemia?

A

no

47
Q

does metformin cause weight gain?

A

no - weight loss

48
Q

name the 2 adverse effects of metformin

A

GI upset

lactic acidosis - rare

49
Q

thiazolidinediones are also known as what?

A

TZDs and glitazones

50
Q

do thiazolidinediones cause hypoglycaemia?

A

no

51
Q

do thiazolidinediones cause weight gain?

A

yes

52
Q

what do thiazolidinediones end in?

A

-glitazone

53
Q

name a thiazolidinedione drug

A

pioglitazone

54
Q

thiazolidinedione adverse effects?

A

weight gain
increased bone fracture risk
fluid retention

55
Q

name the new drug class that is not dependent on insulin

A

sodium-glucose cotransporter (SGLT2) inhibitors

56
Q

what do SGLT2 inhibitors end in?

A

-agliflozin

57
Q

give an example of a SGLT2 inhibitor

A

empagliflozin
canagliflozin
dapagliflozin

58
Q

do SGLT2 inhibitors cause hypoglycaemia?

A

no

59
Q

do SGLT2 inhibitors cause weight gain?

A

no - weight loss

60
Q

name the drug that can cause hypoglycaemia

A

SUs - glipizide

glinides can also cause but not as much as SUs