pharma Flashcards
(22 cards)
antagonist
prevents something
agonist
initiates something
competitive antagonist
bind to the same receptor as agonist but do not activate it
non competitive agonist
binds to allosteric site to prevent it
irreversible antagonist
covalently bonded and cannot be removed
inhibitor
binds to a protein to decrease its activity
overcome reversible agonist
administer more agonist
reaching steady state concentration for oral drug
3-5x half life
partial agonist
lower efficacy and cannot produce maximal response
EH
proportion of the drug that is cleared by the liver
fH
proportion of the drug that is absorbed from GI that actually enters systemic circulation
rate of absorption factors
lipophilicity, charged, size, gastric emptying
bioavailability equation
F= fg x fH
fg is proportion absorbed from the gut
unbound drugs
only unbound can distribute
volume of distribution
fluid that would be required to distribute the full dose of a drug at the concentration it is observed in the blood
determinants of half life
proportional to volume of distribution
inversely proportional to systemic clearance
functionalisation reaction
Cytochrome P450
conjugation reaction
UGT
renal elimination
filtration in the glomerulus, only unbound drugs
clearance
volume of blood cleared irreversibly of a drug
low hepatic clearance
less than 300mL
high hepatic clearance
over 1000mL