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38 Cards in this Set
- Front
- Back
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Where do you find M1, M2, and M3 receptors?
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M1 - neurons
M2 - heart (inhibitory) M3 - glands, smooth muscle, endothelium M4 - CNS (inhibitory) |
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Rate limiting step in Ach syntehsis
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Choline transport/uptake into the neuron
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In symp neurons, the major method of termination is reuptake, what about for para?
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It's acetylcholine esterase
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Hemicholinium
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inhibits transport of choline into neuron (rate limting step)
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Vasamciol
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blocks Ach storage (so it is broken down)
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Botulinium toxin
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injected form is least toxic and paralyzes muslce, prevents release of Ach
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AChE inhibitors
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major route of degradation for Ach, blocking this allows Ach to build up
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What drug blocks the rate limiting step in the PNS and SNS release pathways?
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PNS - hemicholonium (blocks choline uptake)
SNS - alpha-methyltyrosine (blocks tyrosine to L-dopa conversion) |
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What are the 2 major direct acting Cholinomimetic drugs?
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Choline esters
Alkaloids (muscarine and nicotine) |
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What are the indirect acting cholinomimetic drugs?
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neostigmine, physostigmine, edrophonium, insecticides, neurotoxins
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4 Acetylocholine esters mentioned in class.
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Acetycholine
Methacholine Carbachol Bethanechol |
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What cholinomimetic, Ach esters mentioned in class have no susceptibility to Cholinesterase?
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Carbechol
Bethanechol |
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What choline ester drugs are selelctive muscarinic stimulators?
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Methacholine and Bethanechol
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What other class of direct acting cholinomimetics (besides choline esters) are there, and what are the drugs?
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Alkaloids -
Muscarine, Pilocarpine for M receptors NIcotine, and Lobeline for N |
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What alkaloid drugs are selective to muscarinic receptors only?
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muscarine and pilocarpine
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Bethanechol
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M1, M3 agonist
Increases secretion, visceral smooth muscle contraction, decrease HR Uses: postop and neurogenic ileus and urinary retention |
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Carbachol
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cholinomimetic that is used exclusively for glaucoma
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Direct acting muscarinic alkaloids or synthetics?
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eg. pilocarpine, muscarine, Cevimeline (new drug)
- activates muscarinic recpetors Uses: glaucoma (both open and narrow angle) by increasing outflow of aqueous humor. Zerostomia, Sjogren's syndrome |
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ASE of cholinomimetics
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GI stress, sweating, bronchoconstriciton, CV depression
Contraindications: peptic ulcers, bronchial asthma, hyperthyroidism |
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Direct acting nicotinic agonist
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eg. nicotine and lobeline
Enters CNS (highly lipophillic) activates both PNS, SNS, and NMJ Clinical use: smoking cessation toxicities: increase GI activites, nausea, vomiting, increase BP and HR Interactions:additive with CNS stimulants |
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Neostigmine
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AchE inhibiitor
used for postop paralytic ileus and neurogenic bladder |
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Physostigmine
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AchE inhibitor
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Neostigmine
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AchE inhiibtor used to treat myasthenia gravis, used to terminate curare-like drugs during surgery
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Edrophonium
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AchE inhibitor that is used to diagnose myasthenia gravis
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Physostigmine
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AchE inhibitor that is antidote for atropine overdose
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AchE toxicities and ASE
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muscarinic - bronchoconstriciton, miosis, excessive secretions, diarrhea
NIcotinic - tremors, skeletal muscle fasciculations, depolarization block of skeletal muscle CNS: convulsions |
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What do you use to treat AchE inhibitor poisoning?
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Pralidoxime (regenerate active AChE)
Atropine (cholinergic receptors antagnoist) |
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Pralidoxime
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used to treat AchE inhibit poisoning,
Toxicities: muscle weakiness in overdose |
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Atropine
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cholinergic receptor antagnoist
Manditory antidoe for severe AChE poisoning toxicities: not much (see slide about atropine) |
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Non selective muscarinic receptor antagonist:
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atropine (there is a ton of info on atropine on the slide ,just look at that, i'm sick of righting
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Ipratropium
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non-selelctive muscarinic receptor antagnoist - redcues or prevents bronchospasms in asthma
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Scopolamine
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Muscarinin recpetor antagonist - treates motion sickness
Toxicities: tachycardia |
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Dicyclomine
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Used to treat irritable bowel syndrome, minor diarrhea. It's a muscarinic M1 antagnoist
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Oxybutynin
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muscarinin receptor antagonist
reduces detrusor smooth muscle tone and treates ure incontinence, |
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Toxic effects of atropine
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"red as a beet, dry as a bone, blind as a bat, hot as a firestone, mad as a hatter"
increasing dose...: 1) dryness of mouth, increase HR 2) marked dryness of mouth, rapid hear rate, blurred vision 3) hot skin, pluss all the above 4) above plus ataxia, restlessness, excitement, delirium, coma |
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Trimethaphan
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Nictonic receptor blocker used for hypertension emergency (ganglionic blocker)
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Tubocurarine
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produces msucle paralysis (during surgery) by blocking nictonici recpetors
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Succinylcholine
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Depolarizing NM blockers
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