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80 Cards in this Set
- Front
- Back
What are the ingredients for making ACh, and what enzyme makes it?
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-Choline
-AcCoA -Choline-Acetyl Transferase |
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What has to happen first for ACh synthesis? What can inhibit it?
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Choline uptake by transporter
Hemocholinium inhibits it |
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What happens after ACh is made in the presynaptic vesicle? What inhibits this?
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-Packing in secretory vesicles
-Vesamicol inhibits the transporter |
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What stimulates ACh NT release?
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Calcium
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What inhibits ACh release?
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Botulinum toxin
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What 2 enzymes break down ACh after its release?
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-Tissue Acetylcholinesterase
-Plasma Butyrylcholinesterase (pseudo) |
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How DON'T we administer ACh? Why?
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Parenterally - it would be broken dow instantaneously by the plasma butyrylcholinesterase
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What is the first step in Norepinephrine synthesis? What inhibits it?
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Uptake of Tyrosine - inhibited by alpha-methyl-tyrosine
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What happens to Tyrosine? What inhibits it?
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Conversion to DOPA
Inhibited by Metatyrosine |
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What happens after Dopa is converted to Dopamine? What inhibits this step?
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Packaging into vesicles via the transmitter VMAT - Reserpine inhibits VMAT
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What stimulates NE release after conversion from Dopamine in the vesicle by Dopamine B-hydroxylase?
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Calcium
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What inhibits release of the vesicle storage pool of NE?
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Guanethidine and Bretylium
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What stimulates the NONvesicular cytoplasmic storage pool of NE?
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Indirect acting sympathomimetics
-Ephedrine -Amphetamine -Tyramine This is NOT calcium stimulated! |
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What is the major mechanism for terminating NE's actions after release? What inhibits this?
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Active Reuptake by Uptake-1
-Inhibited by Cocaine and TCA's (Imipramine) |
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What happens to NE after reuptake?
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Transport into storage vesicles by another carrier system
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What are 2 other ways that catecholamine action is terminated?
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-Diffusion away
-Enzyme degradation |
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What enzymes metabolize catecholamines?
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MAO-A/B - oxidative deamination
COMT - methylation |
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What is the metabolite of COMT breakdown of catecholamines?
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VMA
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What are 3 major things that modulate the release of NE from sympathetic nerve endings?
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-NE itself on autoreceptors (a2)
-Ang II -Acetylcholine |
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What effect does Ang II have on SNS release of NE?
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Stimulatory
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What effect does ACh have on NE release, and by what ACh receptor does this work?
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Inhibitory - M1 receptor
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What are 2 types of cholinomimetics?
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-Direct agonists
-Indirect agonists |
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Difference btwn Direct and Indirect cholinomimetics?
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Direct - mimic ACh
Indirect - inhibit AChesterase |
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What are the 4 DIRECT cholinomimetics?
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-Bethanechol
-Carbachol -Pilocarpine -Methacholine |
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What is Bethanechol's CLINICAL APPLICATION?
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Post-op or neurogenic ileus and urinary retention
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How does Bethanechol act?
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-Bowel and Bladder smooth muscle activation
-RESISTs AChesterase |
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What is Carbachol's CLINICAL APPLICATION?
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-Glaucoma - open/closed angle
-Pupillary contraction -Release IOP -Stimulate Sweat/Tears/Saliva |
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How does Carbachol act?
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-Contracts ciliary muscle to treat open angle glaucoma
-Contracts pupillary sphincter to treat narrow angle glaucoma -Resists ACHesterase |
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What is Pilocarpine's CLINICAL APPLICATION?
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Same as Carbachol!
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What is the CLINICAL APPLICATION of Methacholine?
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Challenge test for diagnosis of Asthma
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How does Methacholine work?
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Stimulates muscarinic receptors in airway when inhaled - bronchoconstriction
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What are the 5 INDIRECT cholinomimetics?
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EPNPE
-Edrophonium -Pyridostigmine -Neostigmine -Physostigmine -Echothiophate |
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What is the mechanism of all the indirect cholinomimetics?
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Increase endogenous ACh by inhibiting Acetylcholinesterase
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Which one does NOT cross the BBB?
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Neostigmine
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So what is Neostigmine used for clinically?
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-Postop and Neurogenic ileus and urinary retention
-Myasthenia gravis -Postop reversal of NMJ blockade (succinylcholine) |
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What is Pyridostigmine used for clinically?
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Increasing strength in Myasthenia gravis - it does cross into the CNS
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What is the CLINICAL APPLICATION of Edrophonium?
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Diagnosis of Myasthenia gravis
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Why is Edrophonium only used for M. gravis DIAGNOSIS?
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Extremely short acting
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What is the CLINICAL APPLICATION of Physostigmine?
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-Glaucoma
-Atropine overdose |
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What is the CLINICAL APPLICATION of Echothiophate?
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Glaucoma
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What are the symptoms of ACholinesterase inhibitor POISONING? (What drugs are known for this?)
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DUMBBLESS
-parathion/sarin -organopesticides |
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DUMBBLESS
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-Diarrhea
-Urination -Miosis -Bronchospasm -Bradycardia -Lacrimation -Excitation of CNS/sk muscle -Salivation -Sweating |
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What are the 2 things to give to TREAT ACHe inhibitor overdose?
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-Atropine to blockade
-Pralidoxime to reactivate ACHesterase |
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And what is given to treat an ATROPINE overdose?
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Physostigmine
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And what is given to reverse NMJ blockade after surgery due to Succinylcholine?
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Neostigmine
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What are the 5 main ANTICholinergic BLOCKERS?
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-Atropine
-Scopalamine -Ipratropium -Benztropine -Methscopalamine, Oxybutin, Glycopyrrolate |
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What are 2 Atropine analogs?
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-Homatropine
-Tropicamide |
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What is the main organ system Atropine is used for? What does it do?
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-Eye
-Reverses miosis to cause mydriasis -Cycloplegia |
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And what are the 2 atropine analogs?
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Homatropine
Tropicamide |
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Where does Benztropine act? Application?
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CNS - Parkinson's (also Trihexyphenidyl)
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Where does Scopolamine act? Application?
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CNS - motion sickness
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Where does Ipratropium work, application?
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-Respiratory
-Asthma/COPD |
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Where do Methscopolamine, Oxybutin, and Glycopyrrolate work? Application?
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-Genitourinary
-REDUCE urgency in mild cystitis, reduce bladder spasms |
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So what are 5 classes of drugs that treat Glaucoma?
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-alpha agonists
-Beta blockers -Cholinomimetics -Diuretics -Prostaglandin |
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What 2 alpha agonists are used for treating glaucoma and what effect does each have?
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Epinephrine - increases Aq humor OUTFLOW
Brimonidine - decreases Aq humor SYNTHESIS |
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What are 2 side effects and a contraindication to giving EPINEPHRINE for glaucoma?
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SE's: burning/stinging
DON'T give in CLOSED angle glaucoma! |
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What are 3 beta blockers for Glaucoma treatment?
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-Timolol
-Betaxolol -Carteolol |
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What is the mechanism of the B-blockers for treating Glaucoma?
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Decrease Aq humor SECRETION
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What cholinomimetics are given for glaucoma?
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Pilocarpine (direct)
Echothiophate (indirect) Physostigmine (indirect) Carbachol (direct) |
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What are the 3 things that cholinomimetics do in their mechanism of treating glaucoma?
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-Increase Aq humor OUTFLOW
-Contract ciliary muscle -Open up Trabecular meshwork |
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What cholinomimetic is given in emergencies? Why?
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Pilocarpine - it is VERY effective at opening the canal of schlemm!
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What are 2 side effects of the cholinomimetics when given for glaucoma however?
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Miosis
Cyclospasm |
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What diuretic is used for treating glaucoma? What is its mechanism?
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ACETAZOLAMIDE
-Decreases Aq humor SECRETION due to decreasing Bicarb |
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What prostaglandin is used for treating glaucoma? What is it an analog of and what is its mechanism?
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Latanoprost
PGF2alpha analog Increases Aq humor OUTFLOW |
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What is a side effect of Latanoprost?
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It colors the iris dark brown!
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So what 3 drugs increase Aqueous humor OUTFLOW?
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-Epinephrine
-Cholinomimetics -Latanoprost |
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What 3 drugs decrease Aqueous humor SYNTHESIS/SECRETION?
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Brimonidine - inhibs synthesis
B-blockers - inhibit secretion Acetazolamide - inhib secretion |
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What is Atropine again?
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A muscarinic ANTAGONIST
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What are 5 organ systems Atropine affects and how?
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Eye: mydriasis/cycloplegia
Airway: decreased secretions Bladder: decreases urgency Gut: decreases motility Stomach: decreases acid secretion |
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So what are the 4 effects of Atropine in a nutshell?
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BLOCKS SLUD
-Less salivation -Less lacrimation -Less urination -Less Defecation |
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What are 5 side effects of Atropine TOXICITY?
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-Hot as a hare
-Dry as a bone -Mad as a hatter -Red as a beet -Blind as a bat |
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What can Atropine cause in elderly?
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Acute closed angle glaucoma
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What can Atropine cause in men with prostatic hypertrophy?
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Urinary retention
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What can Atropine cause in infants?
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Hyperthermia
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What is Hexamethonium?
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A NICOTINIC ACh blocker!
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What is Hexamethonium NOT to be confused with?
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Hemicholinium, the choline uptake blocker
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Where are there nicotinic ACh receptors?
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-Neuroneuronal in ganglia
-Adrenal medulla -Skeletal muscle |
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Where does Hexamethonium work? How?
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At the Ganglia - it is a Ganglionic Blocker
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What is Hexamethonium used FOR and what does it do?
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Experimental models - PREVENTS vagal reflex responses to bp changes
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What is a clinical application of Hexamethonium?
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Prevents reflex bradycardia when you give things like Norepi to increase blood pressure!
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