psychopharmacology - part 2 Flashcards
different types of drug action
agonism
antagonism
allosteric modulation
agonism - direct and indirect
direct - mimics the effect of a neurotransmitter by binding the postsynaptic receptors in a similar way and producing a similar response in the postsynaptic neuron
indirect - enhances the action of a natural neurotransmitter
agonism - full, partial, inverse
full - generate a maximal response at a receptor
partial - generate a fraction of the possible response at a receptor
inverse - cause a decrease in signalling at a receptor
agonism
enhances natural action
antagonism - direct and indirect
direct - binds to receptor but has no physiological effect at receptor
indirect - involves inactivation of the enzymes that synthesises neurotransmitters pr inhibiton of release
antagonism - reversible and irreversible
reversibe competitive - competes for binding site (blocks)
irreversible competitve - form a stable bond with an agonists binding site
allosteric modulation
a substance that indirectly influences neurotransmission by acting at a site distinct from the primary binding site to modify receptor structure
many increase/decrease likelihood an agonist will bind
enhance/reduce effects of agonist
drug efficiency
= the extent to which a drug activates a receptor
dose response curve –> smallest dose w/ same effect = more efficient
drug efficiency - antagonist
have no efficiency because they dont induce a response
drug efficiency - full agonist
induce maximal response
drug efficiency - full inverse agonist
induce maximal response in the opposite direction
drug efficiency - partial agonist
depend upon the background level of neurotransmitter activity
- useful when stabilisation is needed (eg, bring back to normal levels)
do drugs have selective responses
even if a drug is selective for a particular receptor it is likely to have more than one effect on behaviour
the therapeutic index
= the relationship between toxic and therapeutic dose
determines the safety of the drug
large therapeutic index preferred
the therapeutic index
how to calculate
calculated as the dose of the drug that elicts a lethal response in 50% of samples (LD50) divided by the dose that elicits a desired response in 50% of a sample (ED50)
LD50 / ED50
if above 100 a drug is safe