T2DM drugs Flashcards

1
Q

where does insulin induce glucose uptake mainly

A

muscle and liver

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2
Q

in adipose tissue what is glucose converted to with insulin

A

fat

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3
Q

what does insulin do to amino acids

A

stimulated amino acids –> proteins

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4
Q

what are first-line lifestyle modifications in T2DM

A

stop smoking, diet, lower BMI, exercise

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5
Q

what drug types are dependent upon insulin

A

increase secretion of insulin (SURs, incretin mimics - meglitinides, DPP4 - gliptins), decrease insulin resistance and reduce hepatic glucose output (metformin, thiazolidinediones)

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6
Q

what drug types are independent of insulin

A

slow glucose absorption fro GI tract (alpha-glucosidase inhibitors), enhance glucose excretion via kidneys (SGLT2)

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7
Q

describe insulin release in beta cells (briefly)

A

enters via GLUT2 –> phosphorylated –> ATP by glucokinase, ATP/K channels shut –> increased K –> depolarisation –> ca channels open –> insulin secretion

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8
Q

what is first line drug

A

metformin

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9
Q

what type of drug is metformin

A

biguanides

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10
Q

how does metformin work (4)

A

reduces gluconeogenesis, increases glucose uptake in muscle, reduces carb absorption, increases fatty acid oxidation

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11
Q

what side effects of metformin are there

A

GI upset, rarely acidosis (DKA)

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12
Q

what is a positive side effect of metformin

A

weight loss

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13
Q

what type of drug are sulfonylureas (SURs)

A

insulin secretagogues so need functional beta cells

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14
Q

name 3 SURs

A

gliclazide, glipizide, tolbutamide (-ide)

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15
Q

how do SURs work

A

close K/ATP channels –> depolarisation –> insulin release

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16
Q

when are SURs used first line

A

metformin intolerant or osmotic symptoms

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17
Q

what are side effects of SURs

A

hypoglycaemia, weight gain

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18
Q

what are contraindications for hypoglycaemia ie SURs

A

elderly, renal impairment, pregnant, professional drivers (DVLA strict rules)

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19
Q

what is a positive side effect of SURs

A

good for heart

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20
Q

when do SURs peak

A

after 1-2 hours

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21
Q

name 2 glinides/ meglinitides

A

repaglinide, mateglinide, - glinide

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22
Q

how do glinides work

A

similar to SURs but augmented by glycaemia, close KATP channels (not really used)

23
Q

when do glinides kick in

A

fast onset 30-60 mins

24
Q

what are contraindications of glinides

A

severe hepatic impairment, pregnancy and breast feeding

25
name a thiazolidinediones/ TZDs/ glitazones
pioglitazone only one used now
26
how do glitazones work
enhance insulin action at target (no effect on secretion), agonist of TF that promotes insulin signalling
27
what effects do glitazones have
fatty acid uptake to apidocytes, reduce hepatic output
28
what are adverse affects of glitazones
weight gain, fluid retention, bone fractures
29
what peptides are released from the intestine in the incretin effect
glucagon like peptide-1 (GLP1) and glucose dependent insulinotropic peptide (GIP)
30
describe the incretin effect
GLP1 and GIP released from intestine into blood, GLP1 and GIP enhance insulin release, GLP1 decreases glucagon release
31
what breaks down GLP1 and GIP
DPP4
32
what are incretin analogues. GLP1 agonists
peptides that miic action of GLP1 but resist breakdown by DPP4
33
give an example of an incretin mimic/ GLP1 agonist
exenatide
34
how are incretin analogues. GLP1 agonists given
subcut injections
35
what are side effects of incretin analogues/ GLP1 agonists
nausea, pancreatitis, very short half life - not long acting
36
name a DPP4 inhibitors/ gliptins
sitagliptin, -gliptin
37
how do DPP4is/ gliptins work
competitively inhibit DPP4 which therefore increases GLP1 and GIP
38
what are downsides of gliptins
not very effective, can cause nausea
39
how do SGLT2 inhibitors work
selectively blocks reabsorption by SGLT2 deliberately causing glucosuria
40
name and SGLT2 inhibitor
dapagliflozin
41
name a side effect of SGLT2i's
UTIs
42
how do alpha glucosidase inhibitors work
breaks down starch to absorbable glucose, inhibitors stop this happening in intestines
43
name 2 alpha glucosidase inhibitors
acarbose, voglibose, -bose
44
what are side effects of alpha glucosidase
GI symptoms, not very effective
45
what drugs cause weight gain
SUR's and piogliazatone
46
what drugs cause weight loss
metformin, SGLT2i, GLP1 agonists
47
what drugs are good for the heart
metformin, SGLT2i
48
what drugs cause hypoglycaemic risk
SURs, insulin
49
what drugs are safest in CDK
pioglitazone, GLP1 agonists, insulin (NOT SLGT2i)
50
what drug causes fractures and oedema
pioglitazone
51
what is orlistat
inhibits lipases and stops absorption of fat
52
which bariatric surgery is most malapsorptive
route en Y
53
which bariatric surgery can slip
adjustable bands