Mod 3 - Site of Drug Action Flashcards
two categories of drugs that affect synaptic transmission
antagonists and agonists
drugs that block or inhibit the postsynaptic effects
antagonists
drugs that facilitate postsynaptic effects
agonists
how do some psychoactive drugs produce their affects?
by altering the production of neurotransmitters
most neurotransmitters are produced from -
precursors
how do some drugs act as precursors
increase the amount of neurotransmitter a cell can synthesize and release into the synapse
precursor drugs are considered -, because administering them increases activity of the neurotransmitter system
agonists
a precursor for dopamine; involved in Parkinson’s disease treatment
L-DOPA
neurotransmitter synthesis is controlled by -
enzymes
how does a drug affect enzymes?
if a drug deactivates one of the enzymes that synthesize neurotransmitters, it will prevent the neurotransmitter from being produced; decreases amount of neurotransmitter
drugs that deactivate enzymes are -
antagonists
- inhibits an enzyme necessary for the synthesis of serotonin
p-chlorophenylalanine (PCPA)
- pump molecules of the neurotransmitter across the vesicle membrane, filling the vesicles
vesicle transporters
true or false. the vesicle transporters are not different from the transporters found on the terminal membrane
false. it is different
how are terminal membrane transporters and vesicle transporters different?
terminal membrane transporters move the molecules form the synapse into the cytoplasm of the presynaptic cell; the vesicle transporters then move the molecules into the vesicles
how do drugs act as antagonists in terms of vesicle transporters
they block them, binding with a particular site on the transporter and inactivating it; because the synaptic vesicles remain empty, nothing is released when the vesicles eventually release their contents into the synapse
ex. of a drug that blocks vesicle transporters for monoamine neurotransmitter systems; sometimes used to reduce blood pressure
reserpine
how do drugs act as antagonists in terms of the proteins at terminal buttons?
by preventing the release of neurotransmitters from the terminal button; deactivate the proteins that cause docked synaptic vesicles to fuse with the presynaptic membrane and expel their contents into the synaptic cleft
ex. of drugs that act as antagonists at the terminal button; prevents the release of acetylcholine
botulinum toxin (botox)
effects on receptors depend on -
- where the receptor is located
- what its normal effects are
- whether the drug activates the receptor or blocks its actions
a drug that mimics the effects of a neurotransmitter act as -
direct agonists
drugs that bind with receptors and block their activation act as -
direct antagonists/receptor blockers
how do drugs act as direct antagonists/receptor blockers?
they occupy the the receptor’s binding site, preventing the neurotransmitter from activating the receptor
some receptors have multiple binding sites… binding of a molecule with an alternative site is referred to as -
noncompetitive binding
if a drug attaches to an alternative site and prevents the ion channel from opening, it’s called a -
indirect antagonist
if a drug attaches to an alternative site and facilitates the opening of the ion channel, it is called a -
indirect agonist
drugs that selectively activate presynaptic receptors act as -
antagonists
drugs that bock presynaptic autoreceptors, increasing the release of the neurotransmitters, act as -
agonists
how do drugs affect reuptake?
some drug molecules attach to the terminal membrane transporter molecules responsible for reuptake and inactivate them; blocking reuptake
how do drugs affect deactivation of enzymes?
bind the with the enzymes that normally destroy the neurotransmitter and prevent them from working
drugs that affect either reuptake and enzymatic deactivation are -
agonists, because they both prolong the presence of molecules of the neurotransmitter in the synaptic cleft
effects of drugs on storage of neurotransmitters in the synaptic vesicles? (antagonist)
block vesicle transporters, decreasing neurotransmitters available
how do drugs affect the release of neurotransmitters through vesicles (antagonist)
bind to and deactivate the proteins that allow the fusion of vesicles to the membrane
when drugs mimic neurotransmitters, they act as
direct agonists
when drugs bind to the same site at neurotransmitter and blocks the receptor from being activated, it acts as
a direct antagonist
when drugs bind to different site on receptor than neurotransmitter and prevent ion channels from opening, they act as
indirect antagonist
when drugs bind to different site on receptor than neurotransmitter and causes ion channels to open, they act as
indirect agonist
drugs that activate autoreceptors are
antagonists; because they stimulate the decrease of neurotransmitters released
drugs that block autoreceptors are
agonists; because they block the regulation of neurotransmitters produced, producing more