final frontier 2002 Flashcards
pilocarpine
used to treat glaucoma
mAChR agonist
bethanecol
used to treat urinary retention
mAChR agonist
mAChR antagonist
iTOPH.
ipratropium, tropicamide, oxybutynin, pirenzepine, hyoscine
i-obstructive pulmonary disease t-eye o-urinary incontinence p-peptic ulcer h-bowel
a1 is inhibitory for
only smooth muscle intestinal, it is actually excitatory for everything else.
salbutamol
agonises beta 2 adrenoreceptors to relax bronchial smooth muscle
phenylephrine
used in nasal congestion, agonises a1 adrenoceptors to restrict blood flow
timolol
blocks beta 1 adrenoceptors to prevent heart rate and force of contraction in hypertension
prazosin
blocks a1 adrenoceptors to dilate vascular smooth muscle and reduce arterial blood pressure
most druggable parts of the genome
1)kinases 22%
GPCRs 15%
pD2
-logEC50
HILL PLOT
log (Pa/(1-Pa)) on y axis against log Xa on x axis.
arpriprazole
dopamine D2 receptor partial agonist
buprenorphine
mu opioid receptor partial agonist
hill langmuir equation
relates receptor occupancy to drug concentration
quantitative aspects equation
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
what kind of antagonism is salbutamol and acetylcholine
physiological antagonism
acetylcholine will contract bronchial smooth muscle while salbutamol would relax it
example of chemical antagonism
TNF and infliximab
opioids
analgesia, nausea, vomiting, respiratory depression, constipation, reward, tolerance, addiction