final frontier 2002

Question 1

pilocarpine

Answer 1

used to treat glaucoma

mAChR agonist

Question 2

bethanecol

Answer 2

used to treat urinary retention

mAChR agonist

Question 3

mAChR antagonist

Answer 3

iTOPH.
ipratropium, tropicamide, oxybutynin, pirenzepine, hyoscine

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

Question 4

a1 is inhibitory for

Answer 4

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

Question 5

salbutamol

Answer 5

agonises beta 2 adrenoreceptors to relax bronchial smooth muscle

Question 6

phenylephrine

Answer 6

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

Question 7

timolol

Answer 7

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

Question 8

prazosin

Answer 8

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

Question 9

most druggable parts of the genome

Answer 9

1)kinases 22%

GPCRs 15%

Question 10

pD2

Answer 10

-logEC50

Question 11

HILL PLOT

Answer 11

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

Question 12

arpriprazole

Answer 12

dopamine D2 receptor partial agonist

Question 13

buprenorphine

Answer 13

mu opioid receptor partial agonist

Question 14

hill langmuir equation

Answer 14

relates receptor occupancy to drug concentration

Question 15

quantitative aspects equation

Answer 15

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

Question 16

what kind of antagonism is salbutamol and acetylcholine

Answer 16

physiological antagonism

acetylcholine will contract bronchial smooth muscle while salbutamol would relax it

Question 17

example of chemical antagonism

Answer 17

TNF and infliximab

Question 18

opioids

Answer 18

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

Question 19

pharmacokinetic curve of a drug in the body

Answer 19

absorption phase
peak concentration
disposition phase
elimination phase and half life
trough concentration

Question 20

SLC transporters

Answer 20

influx

Question 21

p glycoprotein

Answer 21

a type of ABC efflux transporter

Question 22

henderson hasselbalch

Answer 22

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

Question 23

prodrug activation example

Answer 23

codeine to morphine

Question 24

CYP2D6 expression

Answer 24

punches way above its weight

Question 25

main CYP

Answer 25

3A4, most drugs metabolised by this

Question 26

felodipine

Answer 26

grape juice inhibitor of intestinal CYP3A4

Question 27

PXR

Answer 27

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

Question 28

CYP2D6 polymorphism

Answer 28

extensive, poor, intermediate and ultrarapid metabolisers

Question 29

Irinotecan

Answer 29

is a topoisomerase 1 inhibitor and used in colorectal cancer. It is activated by hydrolysis to SN38 and deactivated by UGT1A1 into SN28G

Question 30

UGT1A1 *28

Answer 30

extral TA repeat, type of VNTR polymorphism, less SN38 conjugation asians have *6

Question 31

glomerular filtration

Answer 31

removal of free drug not bound to plasma proteins

Question 32

active tubular secretion

Answer 32

drug is transported from blood into urine by tubular transporter proteins

Question 33

tubular reabsorption

Answer 33

passive process in which drug in urine diffuses back into blood

Question 34

ammonium chloride

Answer 34

is a weak base that can actually acidify urine

Question 35

Faecal excretion

Answer 35

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.

Question 36

sulfanilamide

Answer 36

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)

Question 37

australian ethics approval

Answer 37

all studies must have human research ethics committee approval

Question 38

regulatory authorities

Answer 38

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

Question 39

International regulatory bodies

Answer 39

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

Question 40

random difficult regulation drugs

Answer 40

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

Question 41

ibrutinib

Answer 41

Bruton tyrosine kinase inhibitor

Question 42

bortzemib

Answer 42

target:ubiquitin proteosome signalling pathway

Question 43

examples of in vitro cyp inducers

Answer 43

omeprazole, lansoprazole, phenobarbital, rifampicin

Question 44

nusinersen

Answer 44

anti sense oligonucleotide

Question 45

rhematoid arthritis

Answer 45

morning stiffness, excessive, chronic inflammation of multiple joints

Question 46

TNF inhibitors

Answer 46

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

Question 47

TGN412

Answer 47

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