Drugs that affect synaptic transmissions are categorised as
Antagonists: A drug that opposes or inhibits the effects of a particular neurotransmitter on the postsynaptic cell.
Agonists: A drug that facilitates the effects of a particular neurotransmitter on the postsynaptic cell.
Drugs can influence synaptic transmission by
- Inhibiting the synthesis of a neurotransmitter
Drugs serve as precursor
Drug inhibits NT synthesis
Effects on storage and release of neurotransmitters
Antagonist action (step 3)
Agonist action (step 4)
Antagonist action (step 5)
Drug effects on receptors
6) Drugs can stimulate postsynaptic receptors
7) Drugs can block postsynaptic receptors
8) Drugs can stimulate autoreceptors and inhibit neurotransmitter synthesis/release
9) Drugs can block autoreceptors and stimulate neurotransmitter synthesis/release
Competitive binding
Drugs act directly on the neurotransmitter binding site on opening of the ion channel.
1) Direct agonist - Binds with a receptor site that a neurotransmitter would normally bind with- causes postsynaptic potentials (PSPs - Step 6)
2) Receptor blocker (direct antagonist) - Binds with a receptor site that a neurotransmitter would normally bind with - does not cause PSPs (Step 7)
Noncompetitive binding
Drugs act on an alternative binding site and modify the effects of the neurotransmitter on opening of the ion channel.
3) Indirect agonist - Binds with a site on a receptor that a neurotransmitter does not bind with, but facilitates the action of the receptor (Step 6)
4) Indirect antagonist - Binds with a site on a receptor that a neurotransmitter does not bind with, but interferes with the action of the receptor (Step 7)
Autoreceptor stimulation - and drug effects
Stimulation of autoreceptors normally cause less neurotransmitter to be released
5) Antagonist drugs stimulate autoreceptors and inhibit the synthesis/release of neurotransmitter (Step 8)
6) Agonist drugs block autoreceptors and increases synthesis/release of neurotransmitters (Step 9)
Drug effects on Reuptake and destruction of neurotransmitters
10) Drugs can block reuptake of neurotransmitter from the synaptic cleft
11) Drugs can inactive enzymes involved in enzymatic deactivation of a neurotransmitter
Reuptake
Molecules of neurotransmitter are taken back into terminal button
Enzymatic deactivation
Destruction of a neurotransmitter in synaptic cleft by an enzyme
Drugs impact synaptic transmission by influencing neurotransmitter reuptake
Molecules of the drug attach to transporter molecules which are responsible for neurotransmitter reuptake and inactivate them.
This means that neurotransmitters can’t bind and be taken back into the cell (Step 10).
Drugs impact synaptic transmission by influencing neurotransmitter deactivation
Molecules of the drug bind to enzymes that normally deactivate the neurotransmitter – stopping enzyme action (Step 11).