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54 Cards in this Set
- Front
- Back
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Varenicline
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Nicotinic partial agonist
First agent to be approved in its class may help smoking cessastio, reduces pleasurable effects mostly eliminated in urine negative psychiatric effects? |
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tiotropium
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Anticholinergic: muscarinic
Bronchodilator (COPD) Minimizes block of feedback inhibition (selective) reversible |
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Pilocarpine
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Direct Ach agonist
Primarily muscarinic Opens up Canal of Schlemm Glaucoma Tert amine orally: stimulate salvation/sweating (think CATERPILLERS coming out of pores) |
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Methacholine
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Direct Ach agonist
Primarily muscarinic quat amine diagnose bronchial airway hyper-reactivity |
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Bethanecol
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direct Ach agonist
primarily muscarinic quat amine GI tract/bladder (Tx for stasis) Contraindicated w/ mechanical obstruction |
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carbachol
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direct ach agonist
nicotinic and muscarinic "carbon copy" quat amine only applied topically miotic agent |
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acetylcholine
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direct ach agonist
nicotinic and muscarinic given IV for vasodilation via EDRF/NO release |
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nicotine
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direct ach agonist
all nicotinic receptors tert amine |
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black widow spider venom
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Acts presynaptically to promote the continuous release of Ach
not used therapeutically |
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physostigmine
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anticholinesterase
reversible tert amine topically to treat glaucoma metabolized by plama |
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rivastigmine
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anticholinesterase
reversible slowly metablozed less drug interactions? |
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neostigmine
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anticholinesterase
reversible selective for detrusser stimulation, GI tract Tx for Myasthenthia Gravis some select action at nAChR quat amine Poor absorption |
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pyridostigmine
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anticholinesterase
reversible Tx of choice: myasth. gravis |
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edrophonium
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anticholinesterase
inhibit ach binding to active site reversible acts directly at nicotinic receptors (primarily sk. muscle effect) diagnostic in myasthenthia gravis short duration |
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tacrine
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anticholesterase
inhibit ach binding to active site: simple, competitive inhibitor reversible was tx for Alzheimers: peripheral effects intolerable hepatotoxic |
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donepezil
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anticholinesterase
inhibit ach binding to active site: simple competitive inhibitor reversible less peripheral SEs that tacrine & w/o hepatotoxicity |
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galantamine
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anticholinesterase
inhibit ach binding to active site: simple, competitive inhibitor reversible tert |
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echothiophate
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anticholinesterase
irreversible stable covalent bond to active site organophosphate, atypical (polar) sustained miosis |
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sarin
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anticholinesterase
irreversible stable covalent bond to active site |
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malathion
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anticholinesterase
irreversible stable covalent bond to active site topical: tx lice |
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parathion
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anticholinesterase
irreversible binds to receptor binding site covalently insecticide: farms |
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atropine
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AchR antagonist
reversible anti-muscarinic tertiary amine: well absorbed in all forms metabolized in liver mushroom poisioning, but toxic (red as a beet, dry as a bone, blind as a bat, mad as a hatter) cycloplegia, mydriasis Eye surgery, contraindicated in glaucoma Tx for sinus bradycardia Tx for mild GI hypermotility Tx in organophosphate posioning |
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scopolamine
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AchR antagonist
reversible anti-muscarinic very similar to atropine anti-motion sickness (transdermal patch) cycloplegia, mydriasis Eye surgery, contraindicated in glaucoma |
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tolterodine
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AchR antagonist
reversible anti-muscarinic tert amine admin orally selective for bladder metabolized: liver |
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oxybutynin
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AchR antagonist
reversible anti-muscarinic tert amine relieves bladder spasm post-op |
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tropicamide
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AchR antagonist
reversible anti-muscarinic Topical, shorter duration (routine eye exam) |
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ipratropium
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AchR antagonist
reversible anti-muscarinic Tx. COPD aerosol |
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propantheline
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AchR antagonist
reversible anti-muscarinic anti-hypermotility, GI quat amine |
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d-tubocurarine
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AchR antagonist
reversible anti-nicotinic SE: BP drop (autonomic blockade reduces symp. tone & promotes release of histamine) |
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atracurium
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AchR antagonist
reversible anti-nicotinic |
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pancuronium
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AchR antagonist
reversible anti-nicotinic long duration, eliminated by kidneys, possible tachycardia Sometimes combined with other drugs for lethal injection |
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Vecuronium
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AchR antagonist
reversible anti-nicotinic NM blockade good selectivity at NM junction (little effect on CV syst: no histamine, no cardiac muscle cells) Intermediate duration eliminated unchanged |
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rocuronium
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AchR antagonist
reversible anti-nicotinic fast acting (rock stars live fast) can prevent fasiculations when give prior to SuCh |
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mecamylamine
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AchR antagonist
reversible anti-nicotinic secondary amine ganglionic blockade |
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hemicholinium 3
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blacks synthesis of Ach presynaptically
blocks active transport of choline into nerve terminal |
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Botulinum toxin A
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prevents release of Ach from nerve terminals
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AG antibiotics
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reduce Ach release
inhibit Ca++ movement through nerve terminals |
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High serum Mg++
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reduce Ach release
probably due to competitive inhibition of Ca++ through channels |
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Succinylcholine
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excessive cholinergic agonist
nicotinic depolarizes motor endplate (depolarizing blockade) NOT METABOLIZED AT ENDPLATE (but metabolized in plasma) very rapid onset, short duration liberates histamine,POTASSIUM; exacerbated by burns, trauma, CHF... only used in children in emergency relax larngeal muscles sk muscle relaxation |
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benztropine
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muscarinic antagonist
used in parkinson pts, works on CNS PARK my BENZ |
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solifenacin
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new muscarinic antagonist
Tx overactive bladder |
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trospium
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new muscarinic antagonist
Tx overactive bladder |
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darifenacin
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new muscarinic antagonist
Tx overactive bladder |
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cevimeline
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new direct-acting muscarinic
xerostomia selective M1/M3? metabolized by liver |
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cisatracurium
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antagonist, nicotinic
20 minute 1/2 life used safely in renal pts/liver fail Atracurium replacaement |
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doxacurium
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nicotinic antagonist
production ceased |
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mivacurium
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nicotinic antagonist, production ceased
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symptoms of nicotine poisoning:
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1. autonomic stimulation through the ganglia
2. CNS excitation: convulsion --> depression 3. skeletal muscle paralysis |
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Competitive NM blocking agents are potentiated by:
(reduce dosing levels) |
1. AG Abx
2. Mg++, elect. imbalance 3. polypeptide Abx: polymixins, colistin, lincomycin 4. advanced age |
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dantrolene
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unique mech of action
skeletal muscle relaxant blocks CA++ release from SR (intracellular) treat malignant hyperthermia |
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hexamethonium
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ganglionic blocker: blocks parasymp and symp transmission
reduce BP tone shut down JH clin trial |
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memantine
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Alzhemiers
may slow rate of deterioration limited SE glutamate rec antagomist |
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pralidoxime
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promotes regeneration of Ach esterase
used after atropine in organophosphate poisoning |
