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GI cancers > pharmacology > Flashcards

pharmacology Flashcards

1
Q

what trasnporter does metformin need to get across body compartments?

A

OCT 1

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2
Q

where is oct 1 expressed

A

liver
enterocytes
proximal tubules

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3
Q

why must kindye function be measured on metformin?

A

lactic acidosis risk due to impaired clearance

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4
Q

what is the mechanism of action of metformin

A

activates AMPK in mitochondria of hepatocytes, inhibiting ATP prodution, blocking hgo

also blocks enylate cyclase, promoting fat metabolism

increases insulin sensitivity

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5
Q

met formin drug target?

A

AMPK in hepatocyte mitochondria

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6
Q

side effects of metformin?

A

GI side effects

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7
Q

when is metformin most effective?

A

in presence of endogenous insulin

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8
Q

example of DPP-4 inhibitor?

A

sitagliptin

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9
Q

mechanism of DPP-4 inhibitors?

A 
inhibit action of DPP-4 
less incretin metabolism
more insulin production
slows digestion 
decreases appetite
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10
Q

drug target od dpp-4 inhibitors

A

dpp4

vascular endothelium

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11
Q

side effects of dpp4 inhibitors

A

upper rt infections
avoid in pancreatitis

no weight gain

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12
Q

when is dpp 4 effective

A

when there is b cell activity

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13
Q

example of sulphonylure?

A

gliclazide

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14
Q

how do sulphonylures work?

A

inhibit atp sensitive k channels in beta cells

this causes depolarisatino, more ca in, insulin release

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15
Q

side effects of sulphonylures

A

wieght gain

hypoglycaemia

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16
Q

example of sgl2 inhibitor

A

dapaglitozin

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17
Q

mechanism of sgl2 inhibitors

A

reversibly inhibitos sgl2 in prox tubule

reduces gluc reabsorption

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18
Q

side effects of sglt 2?

A

worsen dka
utis
less bone formation

help with weight loss and lower bp

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19
Q

what is the firt line treatment for diabetes?

A

metformin

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20
Q

why isnt valpropate given to women of childbearing potential?

A

can cause neural tube defects, lower iq and autism

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21
Q

what effect does the COP have on lamotrigine levels?

A

lowers level

COC increases UDPGA which converts it to LTG-gluc

lamotragine prescription increased if on COC

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22
Q

how are siezures treated in hospital?

A

IV benzodiazepines

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23
Q

how does lamotrigine work

A

Blocks voltage gated Na+ channels preventing Na+ influx.

Prevents depolarisation of glutamatergic neurones and reduces glutamate excitotoxicity.

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24
Q

drug target of lamotrigiine

A

voltage gated sodium channels

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25
Q

side effects of lamotrigine

A

rash, drowsiness

introduce gradually to decrease skin issues

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26
Q

mechanism of sodium valproate?

A

inhibits GABA transaminase

less breakdown of GABA

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27
Q

target of valproate?

A

GABA transaminase

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28
Q

side effects of valproate?

A

common: stomach pain and diarrhoea, drowsiness, weight gain, hair loss

less common: hepatotoxicity, teratogenicity, pancreatitis, brith defects

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29
Q

why does valproate increase the serum concentration of many drugs

A

CYP enxyme inhibitor

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30
Q

how does diazepam work?

A

upregulates gaba - increases chlorine ion infux when gaba binds

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31
Q

drug target of diazepam

A

benzo site on GABA A receptor

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32
Q

side effects of diazepam?

A

common: drowsiness, respiratory depression if IV
addiction

less common: haemolytic anaemia, jaundice

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33
Q

why isnt diazepam used routinely?

A

become tolerant

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34
Q

how does levetiracetam work?

A

inhibition of synaptic vesicle protein SV2A

prevents exocytosis

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35
Q

side effects of levetiracetam

A

dizziness
somnolence
fatigue
headache

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36
Q

what scoring system is used to screen depression

A

PHQ-9

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37
Q

what is the drug interaction of erythromycin and citalopram

A

prolong the QT interval. use of both not advised

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38
Q

why is there a plateau of mood improvement on ssris after a point

A

5-htt transporters are fully blocked

maxxed out

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39
Q

what does mirtazapine preferentially block at low concs

A

the H2 receptor

causes sleepiness

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40
Q

at higher doses, what does mirtazapine target?

A

alpha 2
5HT2
5HT3 (anti emetic)

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41
Q

why is the sedative effect of mirtazapine offset in higher doses?

A

due to increased noradrenergic transmission

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42
Q

what happens if venflaxine doses increase over 300 mg

A

increase in BP and HR

due to adrenergic effects

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43
Q

primary mechanism of action of sertraline, citalopram and fluoxetine?

A

inhibition of serotinin reuptake via the serotonin transporter

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44
Q

side effects of ssris?

A

gi effects
sexual dysfunction
anxiety
insomnia

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45
Q

what other targets does sertraline have?

A

mild inhibition of dopamine transporter

inhibits CYP2D6 at high doses so less drug metabolism

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46
Q

what other things does citalopram target?

A

mild antagonism of muscarininc and histamine receptors

47
Q

what other targets does fluoxetine habe?

A

mild antagonism of 5HT2A and 5HT2C

complyetely inhibits CYP2D6 and others so caution with warfarin

48
Q

mechanism of venlafaxine?

A

more potent SSRI

also inhibits NA uptake

49
Q

2 drug targets of venlafaxine?

A

serotinin transporter

noradrenaline transporter

50
Q

mechanims of action of mirtazapine?

A

increases release of serotonin and noradrenaline

antagonises 5HT2 receptors, leaving 5HT1 unopposed causing antidepressant effects

51
Q

targets of mirtazapine

A

antagonises presynaptic alpha 2 adrenergic receptors

antagonises central 5HT2 r

52
Q

side effects of mirtazapine

A

weight gain
sedation
may exacerbate rem sleep disorder

low probability of sexual dysfunction

53
Q

what is the management for bp under 135/85

A

moniter every 5 years

54
Q

management for bp 135-149

A

start drug treatment if diabetes, organ damage etc

55
Q

first line for under 55s/non black people for bp

56
Q

first line for black ppl/over 55

A

ccb (amlodopine or felodipine)

57
Q

what is the mechanism of ccbs

A

less muscular contraction, less resistance, less cardiac output

58
Q

why doesnt amolodpine cause a refle increase in heart rate but felodipine does?

A

amplodipine has loger half life

59
Q

when are aceis contraindicated?

A

bilateral renal artery stenosis

60
Q

why do thiazides not sustain their kidney effects?

A

tolerance. after, continuing antihypertensive effect based on vasodilation

61
Q

examples of aceis

62
Q

side effects of aceis

A 
cough 
hypotension 
hyperkalaemia 
foetal injury 
renal failure 
uticaria 
oedema
63
Q

what do most ace inhibitors require

A

hepatic activation as they are pro drugs

64
Q

what must be checked when using aceis

A

eGFR snd k

65
Q

what are ccbs

66
Q

Mechanism of ccbs

A

block l type calcium channels on vascular smooth muscle. less contraction.
inhibition of myosin light kinase, no cross bridge formation

67
Q

side effects of ccbs

A

ankle oedema
constipation
palpitations
flushing

68
Q

which type of ccbs are more selevtive?

A

dihydropyridine

69
Q

how do thiazides work

A

block na/cl contransporter in dct

70
Q

side efects of thiazides?

A 
hypokalaemia 
hyponatraemia
metabolic acidosis (more h excretion)
hypercalcaemia
hyperglycaemia
71
Q

arbs examples

A

losartan
irbesartan
candesartan

72
Q

how do arbs work

A

act as non competative inhibitors od the at1 receptor in kidneys and vasculatrue , preventing a2 taking effect

73
Q

target of arbs

A

angiotensin receptor

74
Q

side effects of arbs

A

hypotension
hyperkalaemia
foetal injury
rena failure

75
Q

why for salbutamol is inhalation the prefferd route

A

reach more receptors quicker

76
Q

how can nsaids cause asthma exacerbations

A

block cox
less prostaglandins
pushed down other pathway producing leukotriens

77
Q

mechanism of salbutamol

A

Agonist at the β2 receptor on airway smooth muscle cells.

Activation reduces Ca2+ entry and this prevents smooth muscle contraction

78
Q

drug target for salbutamol

A

b-2 adrenergic receptor on airway smooth muscle cells

79
Q

side effects of salbutamol

A

palpitation
arrythmia
hypokalaema

80
Q

what type of beta agonist is salbutamol

A

short acting

81
Q

what can exacerbate hypokalaemia with salbutamol use

A

corticosteroids

82
Q

how can salbutamol cause an increase in cardiac contractility?

A

beta 1 receptor

83
Q

how do fluticasone, mometasome and budesonide work

A

directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells.

and reduce number of cytokines they produce

84
Q

target of fluticasone, mometasone and budesonide?

A

glucocorticoid receptor

85
Q

side effects of the glucocortocid receptor targeting drugs?

A

horse voice, oral infection

growth retardation in children
gyperglycaemia 
less bone density 
immunosuppression 
mood issues
86
Q

which of the 3 glucocortocoid receptors drugs may be taken orally

A

budesonide as oral bioavailability above 10%

87
Q

Mechanism of monteleukast?

A

Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells

decreases eosinophil migration, broncho-constriction and inflammation induced oedema

88
Q

drug target of monteleukast

A

cyslt1 leukotriene receptor

89
Q

side effects of monteleukast

A

diarrhoea, fever, headaches, nausea, vomiting, mood changes, anaphylaxis

90
Q

what do prostaglandins do?

A

sensitize peripheral nociceptor mediators which cause pain

91
Q

how do nsaids cause stomach ache

A

pgs inhibit gastrin, leading to less acid.

92
Q

what is the treatment for gastric ulcer disease?

A

full dose ppi for 4-8 weeks

93
Q

what should someone with osteoporosis be given instead of a ppi?

A

histamine receptor agonist.

ppis increase risk of fracture

94
Q

what is naproxen an example of

95
Q

what is the mechanism of nsaids?

A

inhibit COX, reduce production of prostaglandins from arachdonic acid.

prostaglandins cause pain and inflammation

96
Q

what are most of the analgesic and antipyretic actions of nsaids linked to?

A

inhibition of cox 2

97
Q

side effects of nsaids?

A

gastric irritation, ulceration
reduced creatinine clearance
contraindicated in asthma due to bronchoconstriction
prolonged use may increase risk of cv effects
aspirin linked to reyes syndrome in kids

98
Q

what are examples of ppis?

A

omeprazole, lansoprazole

99
Q

how do ppis work

A

irreversable inhibitors of h+k+ atpase in parietal cells

100
Q

what is the drug target of ppis

A

h+/k+ atpase

101
Q

side effects of ppis

A

headache, diarrhoea, bloating, abdo pain

102
Q

why does omeprazole reduce the activity of clopidogrel

A

inhibits cytochrome p2c19

103
Q

how do ppis go from pro drugs to active?

A

at low ph convert to 2 reactive basic species

react with sulphydryl groups in the transporter

104
Q

example of histamine receptor antagonist

A

ranitidine

105
Q

mechanism of histamine receptor antagnoistms

A

competetive antagonism of h2
ingibit stimulation by histamine from enterochromaffin like cells

inhibit gastrrx acid production

106
Q

drug target of histamine receptor antagnosits?

A

h2 receptros

107
Q

what h2 aonist inhibits p450?

A

cimetidine

108
Q

what is the mechanism of action of paracetamol

A

unclear

may involve cox 3 isoform, cannabinoid recepros

109
Q

side effects of paracetamol

A

hapatotoxicity in very high doses

allergigic skin reaction

109
Q

side effects of paracetamol

A

hapatotoxicity in very high doses

allergigic skin reaction

110
Q

first line treatemnt for hypertension

A

amlodopine (or ccb)

111
Q

treatment for proteinuria?

A

acei/arbs
sglt2 inhibitors

stop amlodipine if reduces bp too much

112
Q

why can the antibiotic trimethoprim derange gfr

A

inhibits active secretion of creartine

GI cancers (18 decks)

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