Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

GI cancers > pharmacology > Flashcards

pharmacology Flashcards

(113 cards)

Start Studying
1
Q

what trasnporter does metformin need to get across body compartments?

A

OCT 1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

where is oct 1 expressed

A

liver
enterocytes
proximal tubules

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

why must kindye function be measured on metformin?

A

lactic acidosis risk due to impaired clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

met formin drug target?

A

AMPK in hepatocyte mitochondria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

side effects of metformin?

A

GI side effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

when is metformin most effective?

A

in presence of endogenous insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

example of DPP-4 inhibitor?

A

sitagliptin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

mechanism of DPP-4 inhibitors?

A 
inhibit action of DPP-4 
less incretin metabolism
more insulin production
slows digestion 
decreases appetite
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

drug target od dpp-4 inhibitors

A

dpp4

vascular endothelium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

side effects of dpp4 inhibitors

A

upper rt infections
avoid in pancreatitis

no weight gain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

when is dpp 4 effective

A

when there is b cell activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

example of sulphonylure?

A

gliclazide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

how do sulphonylures work?

A

inhibit atp sensitive k channels in beta cells

this causes depolarisatino, more ca in, insulin release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

side effects of sulphonylures

A

wieght gain

hypoglycaemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

example of sgl2 inhibitor

A

dapaglitozin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

mechanism of sgl2 inhibitors

A

reversibly inhibitos sgl2 in prox tubule

reduces gluc reabsorption

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

side effects of sglt 2?

A

worsen dka
utis
less bone formation

help with weight loss and lower bp

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what is the firt line treatment for diabetes?

A

metformin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

why isnt valpropate given to women of childbearing potential?

A

can cause neural tube defects, lower iq and autism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

how are siezures treated in hospital?

A

IV benzodiazepines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

how does lamotrigine work

A

Blocks voltage gated Na+ channels preventing Na+ influx.

Prevents depolarisation of glutamatergic neurones and reduces glutamate excitotoxicity.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

drug target of lamotrigiine

A

voltage gated sodium channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
side effects of lamotrigine
rash, drowsiness introduce gradually to decrease skin issues
26
mechanism of sodium valproate?
inhibits GABA transaminase | less breakdown of GABA
27
target of valproate?
GABA transaminase
28
side effects of valproate?
common: stomach pain and diarrhoea, drowsiness, weight gain, hair loss less common: hepatotoxicity, teratogenicity, pancreatitis, brith defects
29
why does valproate increase the serum concentration of many drugs
CYP enxyme inhibitor
30
how does diazepam work?
upregulates gaba - increases chlorine ion infux when gaba binds
31
drug target of diazepam
benzo site on GABA A receptor
32
side effects of diazepam?
common: drowsiness, respiratory depression if IV addiction less common: haemolytic anaemia, jaundice
33
why isnt diazepam used routinely?
become tolerant
34
how does levetiracetam work?
inhibition of synaptic vesicle protein SV2A prevents exocytosis
35
side effects of levetiracetam
dizziness somnolence fatigue headache
36
what scoring system is used to screen depression
PHQ-9
37
what is the drug interaction of erythromycin and citalopram
prolong the QT interval. use of both not advised
38
why is there a plateau of mood improvement on ssris after a point
5-htt transporters are fully blocked | maxxed out
39
what does mirtazapine preferentially block at low concs
the H2 receptor causes sleepiness
40
at higher doses, what does mirtazapine target?
alpha 2 5HT2 5HT3 (anti emetic)
41
why is the sedative effect of mirtazapine offset in higher doses?
due to increased noradrenergic transmission
42
what happens if venflaxine doses increase over 300 mg
increase in BP and HR due to adrenergic effects
43
primary mechanism of action of sertraline, citalopram and fluoxetine?
inhibition of serotinin reuptake via the serotonin transporter
44
side effects of ssris?
gi effects sexual dysfunction anxiety insomnia
45
what other targets does sertraline have?
mild inhibition of dopamine transporter inhibits CYP2D6 at high doses so less drug metabolism
46
what other things does citalopram target?
mild antagonism of muscarininc and histamine receptors
47
what other targets does fluoxetine habe?
mild antagonism of 5HT2A and 5HT2C complyetely inhibits CYP2D6 and others so caution with warfarin
48
mechanism of venlafaxine?
more potent SSRI also inhibits NA uptake
49
2 drug targets of venlafaxine?
serotinin transporter | noradrenaline transporter
50
mechanims of action of mirtazapine?
increases release of serotonin and noradrenaline antagonises 5HT2 receptors, leaving 5HT1 unopposed causing antidepressant effects
51
targets of mirtazapine
antagonises presynaptic alpha 2 adrenergic receptors antagonises central 5HT2 r
52
side effects of mirtazapine
weight gain sedation may exacerbate rem sleep disorder low probability of sexual dysfunction
53
what is the management for bp under 135/85
moniter every 5 years
54
management for bp 135-149
start drug treatment if diabetes, organ damage etc
55
first line for under 55s/non black people for bp
ACE i
56
first line for black ppl/over 55
ccb (amlodopine or felodipine)
57
what is the mechanism of ccbs
less muscular contraction, less resistance, less cardiac output
58
why doesnt amolodpine cause a refle increase in heart rate but felodipine does?
amplodipine has loger half life
59
when are aceis contraindicated?
bilateral renal artery stenosis
60
why do thiazides not sustain their kidney effects?
tolerance. after, continuing antihypertensive effect based on vasodilation
61
examples of aceis
-PRIL
62
side effects of aceis
``` cough hypotension hyperkalaemia foetal injury renal failure uticaria oedema ```
63
what do most ace inhibitors require
hepatic activation as they are pro drugs
64
what must be checked when using aceis
eGFR snd k
65
what are ccbs
-DIPINE
66
Mechanism of ccbs
block l type calcium channels on vascular smooth muscle. less contraction. inhibition of myosin light kinase, no cross bridge formation
67
side effects of ccbs
ankle oedema constipation palpitations flushing
68
which type of ccbs are more selevtive?
dihydropyridine
69
how do thiazides work
block na/cl contransporter in dct
70
side efects of thiazides?
``` hypokalaemia hyponatraemia metabolic acidosis (more h excretion) hypercalcaemia hyperglycaemia ```
71
arbs examples
losartan irbesartan candesartan
72
how do arbs work
act as non competative inhibitors od the at1 receptor in kidneys and vasculatrue , preventing a2 taking effect
73
target of arbs
angiotensin receptor
74
side effects of arbs
hypotension hyperkalaemia foetal injury rena failure
75
why for salbutamol is inhalation the prefferd route
reach more receptors quicker
76
how can nsaids cause asthma exacerbations
block cox less prostaglandins pushed down other pathway producing leukotriens
77
mechanism of salbutamol
Agonist at the β2 receptor on airway smooth muscle cells. | Activation reduces Ca2+ entry and this prevents smooth muscle contraction
78
drug target for salbutamol
b-2 adrenergic receptor on airway smooth muscle cells
79
side effects of salbutamol
palpitation arrythmia hypokalaema
80
what type of beta agonist is salbutamol
short acting
81
what can exacerbate hypokalaemia with salbutamol use
corticosteroids
82
how can salbutamol cause an increase in cardiac contractility?
beta 1 receptor
83
how do fluticasone, mometasome and budesonide work
directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. and reduce number of cytokines they produce
84
target of fluticasone, mometasone and budesonide?
glucocorticoid receptor
85
side effects of the glucocortocid receptor targeting drugs?
horse voice, oral infection ``` growth retardation in children gyperglycaemia less bone density immunosuppression mood issues ```
86
which of the 3 glucocortocoid receptors drugs may be taken orally
budesonide as oral bioavailability above 10%
87
Mechanism of monteleukast?
Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells decreases eosinophil migration, broncho-constriction and inflammation induced oedema
88
drug target of monteleukast
cyslt1 leukotriene receptor
89
side effects of monteleukast
diarrhoea, fever, headaches, nausea, vomiting, mood changes, anaphylaxis
90
what do prostaglandins do?
sensitize peripheral nociceptor mediators which cause pain
91
how do nsaids cause stomach ache
pgs inhibit gastrin, leading to less acid.
92
what is the treatment for gastric ulcer disease?
full dose ppi for 4-8 weeks
93
what should someone with osteoporosis be given instead of a ppi?
histamine receptor agonist. ppis increase risk of fracture
94
what is naproxen an example of
nsaid
95
what is the mechanism of nsaids?
inhibit COX, reduce production of prostaglandins from arachdonic acid. prostaglandins cause pain and inflammation
96
what are most of the analgesic and antipyretic actions of nsaids linked to?
inhibition of cox 2
97
side effects of nsaids?
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
what are examples of ppis?
omeprazole, lansoprazole
99
how do ppis work
irreversable inhibitors of h+k+ atpase in parietal cells
100
what is the drug target of ppis
h+/k+ atpase
101
side effects of ppis
headache, diarrhoea, bloating, abdo pain
102
why does omeprazole reduce the activity of clopidogrel
inhibits cytochrome p2c19
103
how do ppis go from pro drugs to active?
at low ph convert to 2 reactive basic species react with sulphydryl groups in the transporter
104
example of histamine receptor antagonist
ranitidine
105
mechanism of histamine receptor antagnoistms
competetive antagonism of h2 ingibit stimulation by histamine from enterochromaffin like cells inhibit gastrrx acid production
106
drug target of histamine receptor antagnosits?
h2 receptros
107
what h2 aonist inhibits p450?
cimetidine
108
what is the mechanism of action of paracetamol
unclear | may involve cox 3 isoform, cannabinoid recepros
109
side effects of paracetamol
hapatotoxicity in very high doses allergigic skin reaction
109
side effects of paracetamol
hapatotoxicity in very high doses allergigic skin reaction
110
first line treatemnt for hypertension
amlodopine (or ccb)
111
treatment for proteinuria?
acei/arbs sglt2 inhibitors stop amlodipine if reduces bp too much
112
why can the antibiotic trimethoprim derange gfr
inhibits active secretion of creartine

GI cancers (18 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions