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EndocrineJaz > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

lispro is a ___ insulin

A

ultra-fast/short-acting

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2
Q

glargine = ___ insulin

give a single bedtime dose

A

ultra-long acting

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3
Q

a biguanide

A

metformin

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4
Q

insulin sensitiser =

A

metformin/biguanides

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5
Q

usual dose of metformin

A

500mg od/bd

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6
Q 
metformin:
decreases HbA1c by:
hypo risk?
weight?
complications?
pregnancy?
A 
15-20mmol/mol
no hypo risk
stays same or lose wt
decreases micro+macrovasc complications
safe in pregnancy
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7
Q

adverse affects of metformin

A 
nausea, vom, abdo pain
vitB12 and folic acid absorption interference
lactic acidosis
liver failure 
rash
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8
Q

insulin secretagogues =

A

sulfonylureas

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9
Q

sulfonylurea examples

A

glipizide
glicazide
glimepiride
glibenclamide/glyburide

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10
Q

adverse affects of sulfonylureas

A

hypoglycaemia

weight gain

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11
Q

PPAR gamma agonists =

A

thiazolidenediones (TZDs)

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12
Q

TZD example

A

pioglitazone

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13
Q

PPAR-RXR receptor in nucleus turns on genes for (4)

A

lipoprotein lipase
FA transport protein
FA CoA synthase
GLUT4

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14
Q

TZD- hypo risk? wt?

A

no hypo risk unless taken with SU

increases weight due to S/C fat and fluid retention

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15
Q

drugs that increase intestinal secretion of insulin =

A

incretins

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16
Q

GLP-1 receptor agonists examples

A

exenatide
exendin LAR
liraglutide
lixisenatide

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17
Q

benefits of GLP-1 receptor agonists

A

promote insulin secretion without hypos
suppress glucagon (which is raised in T2D)
early satiety

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18
Q

adverse affects of GLP-1 receptor agonists

A

nausea (resolves in 6-8wks)

pancreatitis

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19
Q

route of delivery of exenatide

A

S/C injection

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20
Q

DPP4 inhibitors

A

vildagliptin
sitagliptin
saxagliptin
linagliptin

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21
Q

DPP4 inhibitors are less/more potent than GLP-1 receptor agonists?

A

less

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22
Q

GLP-1 is secreted by:

GIP is secreted by:

A 
GLP-1 = L cells
GIP = K cells
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23
Q

benefits of DPP4 inhibitors

A

promote insulin secretion without hypos
decrease glucagon
weight neutral

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24
Q

adverse affect of DPP4 inhibitors

A

pancreatitis

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25
Q

SGLT2 inhibitors

A

dapagliflozin
canagliflozin
empagliflozin

26
Q

diabetic drug than causes you to pee out 80g sugar each day

A

SGLT2 inhibitors

27
Q

SGLT2 inhibitor benefit and adverse affect

A 
benefit = weight loss
adverse = increase risk of thrush and UTI
28
Q

low levels of ___ increase appetite and thermogenesis but high levels dont do the reverse

A

leptin

29
Q

drugs with insulin dependent action that cause an increase in insulin secretion

A

SUs
incretin mimics
glinides
DPP4 inhibitors

30
Q

insulin dependent drugs that decrease insulin resistance and decrease hepatic glucose output

A

biguanides

TZDs

31
Q

insulin independent drugs that slow glucose absorption from the gut

A

alpha-glucosidase inhibitors

32
Q

insulin independent drugs that enhance glucose excretion from the kidney

A

SGLT2 inhibitors

33
Q

increased blood glucose cause increased diffusion of ___ into beta cell by ____ > ___ phosphorylates glucose > increase ATP and ___ close > depolarisation and __ open >insulin secreted

A 
glutamate
GLUT2 facilitated transport
glucokinase
KATP channels close
Ca2+ channels open
34
Q

ATP binds to KIR6.2 = KATP channel ___

A

closes

35
Q

ADP-Mg2+ binds to SUR1 = KATP channel ___

A

opens

36
Q

SUs have a risk of hypoglycaemia because

A

bind to SUR1 and close KATP causing insulin release independent of bg

37
Q

1st generation SU=

A

tolbutamide

38
Q

2nd generation SU are __potent and have a ___ duration of action so a higher risk of___ than 1st generation SUs

A

more
longer
hypos

39
Q

SUs usually given in combo with __/__

A

metformin

TZDs

40
Q

Examples of glinides

A

repaglinide and nateglinide

41
Q

mechanism of glinides

A

similar to SUs - bind to SUR1 at a benzamido site and close KATP channel

42
Q

glinides have ____ which causes a reduced risk of hypos when compared to SUs

A

a quick onset and offset of action

43
Q

when are glinides taken and by what route

A

PO before meals to decrease post prandial bg rise

44
Q

glinides are usually in combo with __/__

A

metformin

TZDs

45
Q

L cells that secrete ___ are found in the __+__

A

GLP-1

ileum and colon

46
Q

K cells that secrete __ are found in the __+__

A

GIP

jejunum and duodenum

47
Q

GLP-1 and GIP ___ insulin release and delay ___ causing ___ glucose uptake and use

A

increase
gastric emptying
increased

48
Q

GLP-1 decreases ___ release and so decreases ___ production

A

glucagon

glucose

49
Q

GLP-1 analogues give S/C od = and S/C bd =

A 
od = liraglutide
bd = exenatide
50
Q

GLP-1 analogues bind to ___ receptors that increase ___ causing increased __ secretion, decreased __ secretion and decreased__+__

A

GPCR GLP1
cAMP and insulin secretion
glucagon secretion, gastric emptying and appetite

51
Q

DPP4 antagonists usually in combo with __/__

A

TZD

metformin

52
Q

mechanism of action of DPP4 antagonists

A

stop DPP4 terminating GLP1/GIP action = prolong their action

53
Q

alpha glucosidase inhibitor example

A

acarbose

54
Q

alpha glucosidase inhibitor mechanism of action

A

inhibit alph glucosidase (brush border enzyme) to stop starch and disaccharide being converted to glucose = delay glucose absorption and decrease postprandial bg rise

55
Q

hypo risk with alpha glucosidase inhibitor ?

A

no

56
Q

adverse effects of alpha glucosidase inhibitor

A 
flatulence
loose stools
diarrhoea
abdo pain
bloating
57
Q

metformin decreases hepatic ___ (stimulates __), increases skeletal muscle __+__ by increasing ___
decreases __ absorption
increases __ oxidation

A

gluconeogenesis (AMPK)
glucose uptake and use ; insulin signalling
carbohydrate absorption
FA oxidation

58
Q

lactic acidosis is a rare but serious side effect of this drug

A

metformin

59
Q

TZDs mechanism of action

A

agonise PPAR gamma - largely confined to adipocytes
= a TF that promotes gene expression of proteins involved in insulin signalling, lipoprotein lipase, FA transport protein and GLUT4
promote FA uptake and storage in adipocytes over muscle and liver
decrease hepatic glucose output

60
Q

TZDs cause fluid retention because

A

increase Na reabsorption in the kidney

61
Q

SGLT2 inhibitors block ___ in ___ of nephron

decrease ___ and cause glycosuria

A

SGLT2
proximal tubule
glucose reabsorption

EndocrineJaz (15 decks)

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