week 4 Flashcards
potency
an index of the concentration required for a given effect = EC50 = mix function of both affinity & efficacy
drugs that are highly potent only require ___ doses
small dose (concentration) to achieve their effects
what are the four protein targets
- receptors
- ion channels
- enzymes
- transporters
define agonists
drugs that occupy receptors & activate them
define antagonists
drugs that occupy receptors but do not activate them, they block receptor activation by agonist
two types of antagonists
irreversible antagonist
competitive antagonist
three types of agonists
partial vs full agonist & inverse agonist
define partial compared to full agonist
full agonist has a higher efficacy (produces a full response) whilst not fully occupying all the receptors. partial agonist has a lower efficacy whilst occupying all receptors still cannot produce maximum response (despite concentration).
define inverse agonist
produce effect opposite to agonist & binds to same binding site = negative efficacy
define efficacy
the capacity of a drug to activate a receptor & generate a response = maximal response a drug can produce
define ec50
concentration needed to produce a 50% max response
if curve B has the same efficacy as curve A but is more the the right then what is the difference
Curve B has a lower potency
define competitive antagonist
competes with agonist for binding site = zero efficacy
what does competitive antagonist do to the curve if it is added with the agonist
shift of the curve to the right without affecting the slope or max response
what looks similar to competitive antagonist
a partial agonist with a full agonist also cause a shift to the right but look for the initial response
what does full agonist mixed with partial agonist look like on concentration curve
it competes with the full agonist for binding site therefore, it delays the efficacy but eventually reaches the efficacy
what does the partial agonist look like by self
starts from zero but reaches half the efficacy of the full agonist and slightly more to the right because it is slower
define irreversible antagonist & affect on concentration curve
drug forms covalent bonds with the receptor
shift of the curve to the right & also affect slope & max response
can the concentration curve be used to calculate affinity if there are spare receptors
no
define allosteric modulation & the two types
drugs that bind to an alternate site to the orthosteric site, they can be antagonism (lower the efficacy) = negative allosteric modulator or potentiation (increase the efficacy) = postive allosteric modulator
define pharmacokinetics
the study of how the body handles drugs
define pharmacodynamics
what the drugs do to the body & how they do it
what is studied in pharmacodynamics
the association of a drug molecule with its target leads to a physiological response
are most drug targets proteins
yes
