final frontier 2002 Flashcards

1
Q

pilocarpine

A

used to treat glaucoma

mAChR agonist

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2
Q

bethanecol

A

used to treat urinary retention

mAChR agonist

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3
Q

mAChR antagonist

A

iTOPH.
ipratropium, tropicamide, oxybutynin, pirenzepine, hyoscine

i-obstructive pulmonary disease
t-eye
o-urinary incontinence
p-peptic ulcer
h-bowel
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4
Q

a1 is inhibitory for

A

only smooth muscle intestinal, it is actually excitatory for everything else.

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5
Q

salbutamol

A

agonises beta 2 adrenoreceptors to relax bronchial smooth muscle

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6
Q

phenylephrine

A

used in nasal congestion, agonises a1 adrenoceptors to restrict blood flow

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7
Q

timolol

A

blocks beta 1 adrenoceptors to prevent heart rate and force of contraction in hypertension

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8
Q

prazosin

A

blocks a1 adrenoceptors to dilate vascular smooth muscle and reduce arterial blood pressure

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9
Q

most druggable parts of the genome

A

1)kinases 22%

GPCRs 15%

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10
Q

pD2

A

-logEC50

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11
Q

HILL PLOT

A

log (Pa/(1-Pa)) on y axis against log Xa on x axis.

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12
Q

arpriprazole

A

dopamine D2 receptor partial agonist

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13
Q

buprenorphine

A

mu opioid receptor partial agonist

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14
Q

hill langmuir equation

A

relates receptor occupancy to drug concentration

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15
Q

quantitative aspects equation

A

log (DR-1)=log (xb)-log Kb

also for schild plots

DR=ra=X’/X
where X’= ec50 agonist in presence of an antagonist
Xa=EC50 in the presence of agonist alone.

The affinity, Kb is the same as potency for the antagonist

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16
Q

what kind of antagonism is salbutamol and acetylcholine

A

physiological antagonism

acetylcholine will contract bronchial smooth muscle while salbutamol would relax it

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17
Q

example of chemical antagonism

A

TNF and infliximab

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18
Q

opioids

A

analgesia, nausea, vomiting, respiratory depression, constipation, reward, tolerance, addiction

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19
Q

pharmacokinetic curve of a drug in the body

A
absorption phase
peak concentration
disposition phase
elimination phase and half life
trough concentration
20
Q

SLC transporters

A

influx

21
Q

p glycoprotein

A

a type of ABC efflux transporter

22
Q

henderson hasselbalch

A

pH-pKa= log[A-]/[HA]

23
Q

prodrug activation example

A

codeine to morphine

24
Q

CYP2D6 expression

A

punches way above its weight

25
Q

main CYP

A

3A4, most drugs metabolised by this

26
Q

felodipine

A

grape juice inhibitor of intestinal CYP3A4

27
Q

PXR

A

the PXR forms dimers with RXR and then it transduce the genes for cyps on the nucleus

28
Q

CYP2D6 polymorphism

A

extensive, poor, intermediate and ultrarapid metabolisers

29
Q

Irinotecan

A

is a topoisomerase 1 inhibitor and used in colorectal cancer.
It is activated by hydrolysis to SN38

and deactivated by UGT1A1 into SN28G

30
Q

UGT1A1 *28

A

extral TA repeat, type of VNTR polymorphism, less SN38 conjugation

asians have *6

31
Q

glomerular filtration

A

removal of free drug not bound to plasma proteins

32
Q

active tubular secretion

A

drug is transported from blood into urine by tubular transporter proteins

33
Q

tubular reabsorption

A

passive process in which drug in urine diffuses back into blood

34
Q

ammonium chloride

A

is a weak base that can actually acidify urine

35
Q

Faecal excretion

A

drugs can appear in faeces by 2 main mechanisms:
1) by not being absorbed into the systemic circulation so drug passes along the intestine

2) by being absorbed, excreted in bile and then being deposited back into the intestine.

36
Q

sulfanilamide

A

antibacterial agent that you can pour into wounds to prevent
Can’t dissolve it
They dissolved it using diethylene glycol. It is highly toxic.
diethylene glycol- PEG
PEG can be super toxic
PEG (polyethylene glycol)

37
Q

australian ethics approval

A

all studies must have human research ethics committee approval

38
Q

regulatory authorities

A

TGA- therapeutic goods administration
ARTG-Australian register of therapeutic goods
EMA, FDA

39
Q

International regulatory bodies

A

ICH (international council for harmonisation- establishes the common technical document)

40
Q

random difficult regulation drugs

A

clostridium difficle, ginko baloba, etc, not a pure drug, printed drug

41
Q

ibrutinib

A

Bruton tyrosine kinase inhibitor

42
Q

bortzemib

A

target:ubiquitin proteosome signalling pathway

43
Q

examples of in vitro cyp inducers

A

omeprazole, lansoprazole, phenobarbital, rifampicin

44
Q

nusinersen

A

anti sense oligonucleotide

45
Q

rhematoid arthritis

A

morning stiffness, excessive, chronic inflammation of multiple joints

46
Q

TNF inhibitors

A

very effective in immunosuppression, but it eventually had declining responses over tine

47
Q

TGN412

A

rapid and unexpected cytokine storm ensured-leading to activation and proliferation of immune cells.