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77 Cards in this Set

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Drug Name
Mechanism
Metyrosine
Comp inhibitor of Tyr-hydroxylase -> depletes catecholamine stores in CNS & PNS
Carbidopa
Comp inhibitor of peripheral DOPA-decarboxylase (similar structure to L-DOPA)
Reserpine
Irreversibly inhibits H+ -amine exchanger in CNS/PNS neurons (ie. catechols can't enter the vessicles)
Guanethidine (Ismelin)
blocks catechol transport into vesicles (also blocks vesicle release & re-uptake)
Guanedrel (Hylorel)
similar to guanethidine - inhibs norepi release & reuptake into vesicle)
Adrenergic Displacers

Tyramine
Comp inhibitor of neuronal uptake (mimic dopamine); Dopamine b-hydroxylase substrate; displaces norepi into synx cleft.
Amphetamines
Competitive catechol uptake inhibitor & displaced norepi into synx cleft (out via Uptake I channel!)
Adrenergic Reuptake Inhibitor

Cocaine
Blocks uptake 1 (esp. dopamine)
(e.g. Imipramine)"
Blocks uptake 1
COMT Inhibitor

Nitecapone & Tolcapone
COMT inhibitos; prevents metabolism of L-DOPA in periphery
MAO Inhibitor

Clorgyline
MAO-A inhibitor (norepi and 5-HT)
Pargyline
MAO-B inhibitor (phenylethylamines and dopamine)
Deprenyl (sergiline)
MAO-B inhibitor - may prevent metabolic activation of MPTP-like chemicals
Alpha Agonists

(Neosynephrine)"
direct acting agonists; alpha-1
(Vasoxyl)"
direct acting agonists; alpha-1 agonist
Clonidine
direct acting agonists; alpha-2 agonist
Alpha-methyl-norepi
direct acting agonists; alpha-2 agonist
Norepinephrine
"endogenous neurotransmitter
Epinephrine
"endogenous neurotransmitter
Beta Agonists

Dobutamine
direct acting agonists; beta-1
Dopamine
direct acting agonists; beta-1
Albuterol (Ventolin)
direct acting agonists; beta-2
Terbutaline (Brethine)
direct acting agonists; beta-2
Isoproterenol
direct acting agonists of beta-1 & -2 (powerful!)
Alpha Antagonist

Prazosin
direct acting a-1 antagonist
Yohimbine
direct acting a-2 antagonist
Phenoxybenzamine
Irreversibly binds (covalently) alpha receptors, uptake 1 & 2
Phentolamine
Reversible, non-selective alpha blockage
Beta Antagnists

Atenolol
direct acting b-1 antagonist
Metoprolol
direct acting b-1 antagonist
Propanolol
reversible, direct-acting B1, B2 antagonist
Hemicholinium-3
blocks choline uptake into nerve terminal (like cocaine, but acts on cholinergic nerves)
Cholinergic Potientiator

3-4 diaminopyridine
potentiates ACh vesicular release
Adrenergic Vesicle Destroyers

b-Bungarotoxin
"destroys vesicles in cholingeric nerves, pre-synpatically
Latrotoxin
destroys vesicles in cholingeric nerves
Adrenergic Vesicle Uptake Inhibitors

AH5183 (vesamicol)
inhibits loading of vesicles (analogous to reserpine)
Adenergic Vesicle Release Inhibitor

Botulinum toxin
irreversible ADP-ribosylation of synaptobrevin (vesicles can not be released); enters cholinergic nerves
Reversible Acetylcholinesterase Inhibitors

Physostigmine (eserine)
" ""Reversible"" inhibitors of acetylcholinesterases
Neostigmine & Pyridostigmine
"Reversible" inhibitors of acetylcholinesterases; carbamylates the active site - recovers in minutes;
Edrophonium (Tensilon)
"truly reversible" non-covalent comp inhib at anionic site of acetylcholinesterases
Irreversible Acetylcholinesterase Inhibitors

di-isopropyl fluorophosphates (DFP) & Soman
phosphorylates the esteratic sites of Ach-esterase; "Irreversible" inhibitors of acetylcholinesterases (organophosphates: insecticides & nerve agents!)
Parathion & Malathion
phosphorylates the esteratic sites of Ach-esterase; "Irreversible" inhibitors of acetylcholinesterases (organophosphates: insecticides & nerve agents!)
Chlorpyrifos (Dursban)
phosphorylates the esteratic sites of Ach-esterase; "Irreversible" inhibitors of acetylcholinesterases (organophosphates: insecticides & nerve agents!)
Echothiophate
phosphorylates the esteratic sites of Ach-esterase; "Irreversible" inhibitors of acetylcholinesterases (organophosphates: insecticides & nerve agents!)
Cholinesterase Restorer

Pralidoxime
site-directed nucleophile; can restore activity to "aging" cholinesterase
Muscaranic Agonists

Pilocarpine
muscarinic agonist
Bethanecol
muscarinic agonist
carbachol
muscarinic & nicotinic properties
Muscarinic Antagonists

Atropine
classic muscarinic antagonist; blocks all muscarininc receptors
Pirenzipine
atropine analog; preferentially blocks m1; muscarinic
Scopolamine
muscarinic antagonist
Nicotinic Antagonists

Curare (tubocurarine)
Post-synaptic ganglion block of nAChR
Alpha-bungarotoxin
Post-synaptic ganglion block of nAChR
Trimethaphan
Selectively blocks ganglionic receptors (N1 preganglionic receptors); nicotinic
Acetylcholine
Proto-typical direct cholinergic agonist
Muscarine
proto-typical direct muscarinic agonist
Nicotine
Proto-typical direct nicotinic cholinergic agonist
Succinylcholine
Depolarizing block of neuro-muscular junction (N); a pseudocholinesterase substrate