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SGU Pharmacology
ANS - Cholinergic Antagonists
16
Medical
Professional
09/01/2010

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Term
Atropine
Definition
Tertiary amine, competitively binds to M Rs, among other things is used as an enuresis in kids (however alpha-agonists maybe more effective w/ fewer A/Es), NB that parasym stimulate the dilation of coronary A. & sym cholinergic N.s vasodilate the MM vasculature, these are blocked by atropine. Also note that at toxic or even normal levels this antimuscarinics cause cutaneous flushing of upper body via unknown MOA. Used as an antidote for excess Ach via indirect means and helps bring it down in the CNS
Term
Scopolamine
Definition
Similar peripheral effects to atropine, but gr8er axn & duration on CNS, anti-motion sickness with an unusual effect of blocking short-term memory, sedation but at higher conc. -> excitement, used in Tx of iridocyclitis (via mydriasis & cycloplegia)
Term
Ipratropium
Definition
Quaternary ammonium derivative of atropine, used to Tx asthma and COPD for pts that cant take adrenergic agonists
Term
Tiotropium
Definition
Better then Ipratropium as a bronchodilator for COPD but not FDA for asthma
Term
Homatropine, Cyclopentolate, Tropicamide
Definition
Mydriasis and cycloplegia, prefered over atropine as its shorter acting
Term
Benztropine & Trihexyphenidyl
Definition
Tertiary amine that enters the CNS to Tx parkinsonism & extrapyramidal effects of antipsychotic Rxs
Term
Glycopyrrolate
Definition
Quaternary ammonium, taken orally to prevent GI motility but taken parenterally to prevent bradycardia during surgery
Term
Tolterodine
Definition
Tertiary amine used in overactive bladder
Term
Mecamylamine
Definition
Only one available in USA, used to Tx moderate to severe essential hypertension & uncomplicated cases of malignant hypertension
Term
Trimetaphan
Definition
Along w/ mecamylamine is the only other ganglion blocker in use in the world
Term
Hexamethonium (C6)
Definition
Quaternary ammonium, was developed to replace TEA which had a shorter T 1/2, came out as the first Rx to Tx hypertension, minimum Nm or M R activity, not used anymore (NB that Decamethonium "C10" an analog of hexamethonium is an Nm depolarizing blocking agent)
Term
Tubocurarine
Definition
Competitive antagonist (non-depolarising), are used in conjunction w/ anaesthetics (less of it is needed now thus safer to use), overcome via AceEIs such as neostigmine or edrophonium complimented w/ atropine so that u dont have unwanted muscarinic Rs activated nah!!!
Term
Succinylcholine
Definition
Depolarizing blocker -> flaccid paralysis, not easily broken down, given IV contineously (cause rapidly broken down by plasma cholinesterase), short acting, blocks ganglion at high conc., has a weak histamine-release axn, used when u need to do a rapid endotracheal intubation or ECT, A/Es: malignant hyperthermia (AD) of MM cause of stimulus-elicited excessive release of Ca2+ from SR (MCC of halogenated anesthetic related death when given w/ this Rx - Tx w/ DANTROLENE which blocks release -> reduction of heat and relaxes muscle tone)
Term
Hemicholinium
Definition
Blocks the high-affinity transporter for choline and thus prevents Ach syn, only used as a research tool
Term
Vesamicol
Definition
Blocks Ach-H+ antiporter used by vesicles, used only as a research tool
Term
Botulinum Toxin
Definition
Protein produced by Clostridium botulinum, potent neurotoxin that degrades synaptobrevin, thus injected in pts muscle that suffer from torticollis, achalasia, strabismus, blepharospasm, & other focal dystonias
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