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Cholinergic Agents
agonists/antagonists
30
Pharmacology
Professional
10/01/2009

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Cards

Term
ACh
Definition
Non-selective agonist. Little use. Rapid induction of miosis.
Term
Methacholine
Definition
Mostly muscarinic agonist. Some AChE resistance. Rarely used.
Term
Carbachol
Definition
Non-selective agonist. Not AChE substrate. Tx: glaucoma.
Term
Pilocarpine
Definition
Mostly muscarinic (M1) agonist. Causes sweating. Tx: glaucoma.
Term
Bethanechol
Definition
Muscarinic agonist. Tx: post-op/post-partum non-obstructive urinary retention.
Term
Neostigmine
Definition
AChE antagonist. Tx: myasthenia gravis sxs, nondepolarizing neuromuscular blocker antidote, post-op urinary retention. Adverse: arrhythmia, inc secretions, urinary urgency & freq.
Term
Edrophonium
Definition
AChE antagonist. Tx: myasthenia gravis differential dx, non-depol neuromusc blocker antidote.
Term
Physostigmine
Definition
AChE antagonist IN CNS. Tx: reverse muscarinic antagonists & sedatives.
Term
Tacrine, donepezil, rivastigmine, galantamine
Definition
AChE antagonist--LONG ACTING. Tx: Alzheimer's.
Term
Isoflurophate (DFP)
Definition
IRREVERSIBLE AChE antagonist. Tx: glaucoma, insecticides.
Term
Atropine
Definition
Muscarinic R agonist. Tx: many uses (think anti-parasympathetics). Warning: determine intraocular press before ophthalmic use to avoid glaucoma attacks.
Term
Ipratropium
Definition
Muscarinic R antagonist on bronchial sm musc. Tx: bronchospasm
Term
Propantheline
Definition
Muscarinic R antagonist on GIT. Tx: adjunct in peptic ulcer. Warning: glaucoma, CHF.
Term
Scopolamine
Definition
Muscarinic R antagonist. Sedation & amnesia in obstetrics (no more).
Term
Pirenzepine
Definition
Muscarinic (partially M1 selective) antagonist in auto ganglia. Tx: (not-US) gastric ulcers
Term
Darifenacin**
Definition
Muscarinic (M3 SELECTIVE) antagonist. Tx: urinary urgency.
Term
Nicotine
Definition
Nicotine R agonist. Tx: smoking cessation.
Term
Varenicline
Definition
Niconine R partial agonist. Tx: smoking cessation.
Term
Hexamethonium**
Definition
Nicotinic R antagonist (partially autonomic gang selective). Tx: (not anymore) HTN
Term
Trimethaphan
Definition
Nicotinic R antagonist. Ultra-short acting gang blocker. Tx: post-op bleeding, hyperreflexia, hypertensive emergencies when B blocker contraindicated.
Term
Mecamylamine
Definition
NON-COMPETITIVE Nicotinic antagonist in CNG. Tx: same as trimethaphan, nicotine dependence?
Term
Succinylcholine**
Definition
Depolarizing/sensitizing Neuro-musc jxn antagonist. Rapid onset, short duration, metabolized by PSEUDOCHOLINESTERASE.
Term
Tubocurarine**
Definition
Non-depolarizing neuro-muscular jxn antagonist. Can partially block auto gang--> hypotension. HISTAMINE release.
Term
Doxacurium
Definition
Non-depolarizing neuro-muscular jxn antagonist. Long-acting. No CV side effects.
Term
Rocuronium
Definition
Non-depolarizing neuro-muscular jxn antagonist. Most rapid onset. High dose--> antimuscarinic.
Term
Atracurium
Definition
Non-depolarizing neuro-muscular jxn antagonist. Some histamine release. Inactivated w/o enzyme.
Term
Mivacurium
Definition
Non-depolarizing neuro-muscular jxn antagonist. Hydrolyzed by PSEUDOCHOLINESTERASE.
Term
Baclofen
Definition
Skeletal musc relaxant. GABA derivative. Tx: spasticity (from MS, trauma). Adverse: Drowsiness, weakness, w/drawl--> seizures.
Term
Diazepam
Definition
Skeletal musc relaxant. Facilitates GABA binding. tx: joint disease or muscle spasm. Adverse: sedation
Term
Dantrolene
Definition
Skeletal musc relaxant. Dec amt of Ca++ release from SR (esp in reflex). Tx: spasticity, MS, MALIGNANT HYPERTHERMIA.
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