EXAMPLE OF DRUGS AND EFFECTS Flashcards
PA : Action potential propagation
Site: Nerve axons
Action: Block voltage-gated sodium channels; block conduction
Local anesthetics, tetrodotoxin, saxitoxin
PA: Transmitter synthesis
Site: cholinergic nerve terminals: membrane
Action: Block uptake of choline and slow ACh synthesis
Hemicholiniums
PA: Transmitter synthesis
Site: Adrenergic nerve terminals and adrenal medulla: cytoplasm
Action: Inhibits tyrosine hydroxylase and blocks synthesis of catecholamines
α-Methyltyrosine (metyrosine)
PA: Transmitter storage
Site: Cholinergic terminals: VAT on vesicles
Action: Prevents storage, depletes
Vesamicol
PA: Transmitter storage
Site: Cholinergic terminals: VAT on vesicles
Action: Prevents storage, depletes
Vesamicol
PA: transmitter storage
Site: Adrenergic terminals: VMAT on vesicles
Action: Prevents storage, depletes
Reserpine, tetrabenazine
PA: Transmitter release
Site: Nerve terminal calcium channels
Action: Reduces transmitter release
ω-Conotoxin GVIA4
PA: Transmitter release
Site: Nerve terminal kainate receptors (primarily CNS)
Action: Modulates transmitter release by altering calcium influx/release
Domoic acid
PA: Transmittee release
Site: Cholinergic vesicles
Action: Prevents ACh release
Botulinum toxin
PA: transmitter release
Site: Cholinergic and adrenergic vesicles
Action: Causes explosive transmitter release
α-Latrotoxin
PA: transmitter release
Site: Adrenergic nerve terminals
Action: Promote transmitter release
Tyramine, amphetamine
PA:Transmitter reuptake after release
Site: Adrenergic nerve terminals, NET
Action: Inhibit uptake; increase transmitter effect on postsynaptic receptor
Cocaine, tricyclic antidepressants, SNRI antidepressants
PA: Receptor activation or blockade
Site: Receptors at adrenergic junctions
Action: Binds and activates α receptors; causes contraction
Norepinephrine
PA: Receptor activation or blockade
Site: Receptors at adrenergic junctions
Action: Binds α receptors; prevents activation
Phentolamine
PA: Receptor activation or blockade
Site: Receptors at adrenergic junctions
Action: Binds β receptors; activates adenylyl cyclase
Isoproterenol
PA: Receptor activation or blockade
Site: Receptors at adrenergic junctions
Action: Binds β receptors; prevents activation
Propranolol
PA: Receptor activation or blockade
Site : Receptors at nicotinic cholinergic junctions (autonomic ganglia, neuromuscular end plates)
Action: Binds nicotinic receptors; opens ion channel in postsynaptic membrane
Nicotine
PA: Receptor activation or blockade
Site: Neuromuscular end plates
Action: Prevents activation of nicotinic receptors
Tubocurarine
PA: Receptor activation or blockade
Site: Receptors, parasympathetic
effector cells (smooth muscle, glands)
Action: Binds and activates muscarinic receptors
Bethanechol
PA: Receptor activation or blockade
Site: Receptors, parasympathetic effector cells
Action: Binds muscarinic receptors; prevents activation
Atropine
PA: Enzymatic inactivation of transmitter
Site: Cholinergic synapses (acetylcholinesterase)
Action: Inhibits enzyme; prolongs and intensifies transmitter action after release
Neostigmine
PA: Enzymatic inactivation of transmitter
Site: Adrenergic nerve terminals (monoamine oxidase)
Action: Inhibits enzyme; increases stored transmitter pool
Tranylcypromine
