pharm 2
Terms
undefined, object
copy deck
- 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