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Drugs that affect neuronal functioning by altering neuronal transmission in ways other than attaching to synaptic receptors. Drug categories Agonist - A drug that facilitates the effects of a particular neurotransmitter on the postsynaptic cell Antagonist - A drug that opposes or inhibits the effects of a particular neurotransmitter on the postsynaptic cell Type of Drug Action •Drug affects the amount of neurotransmitter stored in vesicles •If it facilitates storage (e.g., by acting as a precursor) -agonist •If it inhibits storage (e.g., by inhibiting synthesis of neurotransmitter or by blocking the storage into vesicles) - antagonist •Drug affects release of neurotransmitter •If it increases release - agonist •If it inhibits release -antagonist •Drug affects reuptake/breakdown of neurotransmitter If it facilitates reuptake/breakdown - antagonist If it inhibits reuptake/breakdown - agonist Drug effects on Dopaminergic neurons •Effects on the amount of neurotransmitter stored in vesicles •L-DOPA facilitates synthesis of DA by acting as a precursor -agonist •Deprenyl facilitates synthesis of DA by blocking the enzyme MAOagonist •Reserpine blocks the storage of DA into vesicles - antagonist •Effects on the release of neurotransmitters •Amphetamine increases release of DA- agonist •Effects on the reuptake of neurotransmitters •Cocaine and amphetamine blocks DA reuptake- agonist Drug effects on Acetylcholinergic neurons •Effects on the amount of neurotransmitter stored in vesicles •Choline facilitates synthesis of ACh by acting as a precursor -agonist •Effects on the release of neurotransmitters •Botulinum toxin blocks the release of ACh - antagonist •Black widow spider venom facilitates the release of ACh - agonist •Effects on the breakdown of neurotransmitters •Physostigmine blocks ACh breakdown by inhibiting the enzyme Acetylcholinesterase- agonist Drug effects on Serotonergic (5-HT) neurons •Effects on the amount of neurotransmitter stored in vesicles •PCPA inhibits synthesis of 5-HT - antagonist •Effects on the release of neurotransmitters •Fenfluramine facilitates the release of 5-HT - agonist •Effects on the reuptake of neurotransmitters •Fluoxetine (Prozac) blocks reuptake of 5-HT- agonist
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