Term
| acetylcholine parasympathetic system |
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Definition
| from nicotinic receptor to muscarinic receptor. |
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Term
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Definition
| some are nicotinic to muscarinic, some are cathecholamine releasing, somee dopamine releasing . |
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Term
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Definition
| 1 nictonic receptor. @ muscular endplate |
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Term
| nicotinic receptors locations |
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Definition
| within the CNS. There is neuronal type (Nn) (postganglionic cell body, presynatpic cholinergic terminals) and muscule type (Nm)(skeletal muscle neurmuscular end plates) subunits with different structural features. Both open sodium/potassium channels once ligand bound. |
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Term
| muscarinic receptors location |
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Definition
| located on the target organ examples - sweat glands, cardiac and smooth muscle . 7 transmembrane domain.- Bidnign to receptor leads to g protein association wihich then tramsits info to effectors (ac,plc)-. Second messengers (camp, calcium) ultimately leaddign to ion chanen l opening |
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Term
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Definition
| inhibits sodium depepdnatn choline transporterinto presynatpic cell which is unieque to chilnergic neurons. |
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Term
| acetylcholine in presynapatic neuron |
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Definition
| taken up by choline transporter and then added to acetyl Coa to acetylcholine, taken up by vesicles and stored until calcium influx happens. When calcium influx happens Ach is released. |
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Term
| Cholinesterase inhibitors |
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Definition
| on suraface of postsynaptic cell. Cholinesterase ihibitors asass well as cholinmimetmics potentiate the effects of acetylcholine |
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Term
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Definition
| antagonize choline by bindin to postsynaptic cholien receptors. |
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Term
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Definition
| degrades syanptobrevin which is requried for vesicale vusion to presynatpicnmembrane, induces flaccid paralysis |
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Term
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Definition
| similar to cholinergic junciton, trnaasporter brings in recpeotr which is then converted to product product is then stored in vesicle until ready for use. Calcium influx etc. Unlike acetylcholine, cathecohalamines themselves are taken up by catecholamien transporters |
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Term
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Definition
| sympathetic postganglionic (which are modulated by Ach,) and several neurons which release acetycholine are actually within ENS. ach released throughout ENS , which menas agetns that ffect cholienric recetors wil lhave side ffects from result of interacitons with ENS. |
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Term
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Definition
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Term
| effect of nictonic ach receptor |
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Definition
| depolraization of nerve cell, or neuromuscular endplate membrane. Ach bindsto a subunits, confomrational change results in hcannel opnieng- fast response. Depolarization is brief due to Ach dissociationg rapidyly from molecules and beign rapidly degraded. |
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Term
| mutations in muscle subunits. (nicotinic) |
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Definition
| myasthenia gravis: autioimmune resposne to receptors at NMJ, mutationso f neuronal subunits associated with epilepsy. |
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Term
| rule of thum regardign m3 receptors and smooth uscle |
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Definition
| lead to contraction. BUT sphincters relax! Peripheral blodo vessels dilate due to release EDRF (NO). |
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Term
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Definition
| very rapidly hydrolized by cholinesterase. IM or SQ only gives you local efefct so f acetylcholine. NO therapeutic applications |
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Term
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Definition
| muscarnic receptor agonists. Permanently charged ntirogen, so low cns penetration,used for peripheral uses . Hydolysis yb acetylcholinesterase. B- methyl group reduces binding to nictonic receptors. Methacholein and bethanacol are selective for muscarinic receptors. |
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Term
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Definition
| cholien ester: promote Gi and urinary tractm otility when non obstructive cuase. muscarinic recetpro agonist |
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Term
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Definition
| muscarinic receptor agonist (cholinomimeti c alkaloid), it is a tertiary amie so it is well absorbed, penetrates CNS, exceted by kidney, not an ester so nto hydrolyezed by cholinesterase |
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Term
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Definition
| sialogogue increase secretion) and miotic agent |
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Term
| main effects of muscarinic agonists |
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Definition
| slow down heart ,decrease output vasodilation: fall in arterial pressure, increase in GI peristaltic activity- contraciton of bladder nad bronchial smooth muscle. Stimulation of sweat, lacrimation ,salviation, bonrhcial secretion. Cotnraction fo ciliary muscle, to lower introccular presure in acute glaucoma. |
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Term
| muscarinic agonisttoxicity |
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Definition
| cutaneous vasodilation, nausea,vomitting diarrhea, bornchail cosntriction, sweating , salivation, misosis . Treat with atropine. |
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Term
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Definition
| muscarinic receptor antagonist (belladonna, beautiful women eyes wide open)- pupil dilation. Dry as abone, blind as a bat, red as a beet mad as a hatter |
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Term
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Definition
| closely related to atropine, for motion sickness. Andn ausea related to chemotherapy, greater cns efects tha natropine so sedative. |
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Term
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Definition
| inhbitison of secretions fro salivy lacrimal ,bronchial sweat glands, tachycardia (modest) , mydriasis (big eeys), inhbition of gi motikilty, relaxation of bronchial biliary , urinatry tract smooth muscle, excitatory effect s on cns . In children: hyperactivity ecitement, rise in body temperatuer excarbated by inability to sweat. |
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Term
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Definition
| muscarien posiiniing, inhibit excessive salivation during surgery, reverus sinus bradycardia, induce mydriassi for eye exam, prevent vagal reflexed induced by surgical trauma of visceral organs. |
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Term
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Definition
| muscarinic antagonist tertiary amine with good CNS penetration. Adjunct in therapy of parkingsons disease. Acute dysotnoiaas cuase d bya ntispychotics. |
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Term
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Definition
| antimuscarnic agent. quarternary amine (poor cns pen). Decreease oral secretions , GI spasms. Treatment of peptic ulcer disease. Prevent bradcyardia duirng surgical procedures |
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Term
| oxybutynin, tolterodien, darifenacin |
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Definition
| antimuscarine ttertiary amine m3 selective. Relief of bladder spasm after urolgoic surgery, urinary incontinence inadults. |
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Term
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Definition
| uaternary ammonium,sunethetic anagologue of atropine,, acts lcoally, used inhalation for asthma and COPD. |
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Term
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Definition
| tertiary amines, m1 selective. Inhiits gastric acid secretion. Little effect on smooth muscle or CNS. Use in peptic ulcer disease declining. (m2,m3 receptors found on SMC). |
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Term
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Definition
| tertiary amines, mydriatic, much shorter duration foaciton tha natropine. |
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Term
| muscarinic antagonists effects |
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Definition
| tachycardia, relaxatin of gut, bladder and bronchial smooth msucle, contraction of sphincters. Sinhbition of sweat salivation , bonrhical and gastri c aci d secretion. Mydriasis and cycloplegia (dialysis fo pupil and paralysis fo acocmodation). CnS effects inclue antiemetic and antiparkinsoism effect . |
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Term
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Definition
| muscarinic receptors found on ciliary msucleand on sphincter. This is why muscarinc agetnss causes misosis (decrease in pupil size). Ciliary msucle contraciton puts tnesion on trabecular meshowrk, facilitating outlow and reducing intracoular pressure (good for glaucoma). |
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Term
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Definition
| readily crosses blodbrain barrier avilale as transdermal patch for smoking cessation. |
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Term
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Definition
| vomotitting (limits amount absorbed0. Cns stimualtion -convulsions progresisng ot coma and repiratory paryalisis. Nueromescular end plate depolarizaiton leads to fasciculatiosn and paralysis. Hypertension and cardiac arrythmias |
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Term
| nictoinic receptor treatment |
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Definition
| symptom directed, (muscarinci excess controleld with atorpine), may reqiurie mechanical respiration. Metabolzied and excreted rapidly. |
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Term
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Definition
| ganglion blockign drug, nicotinic receptor antagonist, Hypotensive agent. Works by decreasing sympathetic tone and vasodilation. |
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Term
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Definition
| nictonic antagonist: nondepolarizing blocker neuromuscular blocking, skeltal muslce relaxant . Isoquinolien derivative |
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Term
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Definition
| non depolarizing neuromuscular blocking, skeltal muslce relaxant . Streoid derivative. |
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Term
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Definition
| nondepolarizing blocker. presynaspe relase ach to ach receptors resutls in depolarizatoin. S |
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Term
| skleletal msucle relaxsnts/ neuromuscular blocekrs |
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Definition
| used in surgery, critically ill patientts hwen enedt o contorl ventilation, attenuate convulsions. Quarternary ntirgoens prvent them from being usedi n cns |
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Term
| nictonic agonist function |
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Definition
| binding keeps channel open and depolarized |
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Term
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Definition
| keeps channel closed and unable to dpeolarize. To antaognize effects of depolarizign blocker, must increase ocncentration of acetylcholine (using cholinesterase inhibitor). |
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Term
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Definition
| keeps channel perpetually open and unblocked. This results in paralysis as well, because if Ach is in excess or if agonist such as this is in use , membrane remains depolarized, so vvoltage gated sodium channels cannot open to support futher AP . Not readily reversible, sicne adding AcH would only make mattersworse. |
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Term
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Definition
| depolarizing neurmoscular blocking drugs (nitocinitc agonist). Elimianted by plasma cholinesterase |
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Term
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Definition
| channel opens and cuses depolarization- adjacent membraens deoplrize and muscle untis contract. However depolarized membranes remaine depoalrized (since succinylcholine is not metabolized effectively ), depolarized membrane remain depoalrized and unresponsive to subsequnt impulses. Flaccid paralysis results, since repolariation needs to ucrr with repetive firing to maintain msucle tension. |
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Term
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Definition
| desensitizing block- continued exposue to drug results in densensitazion to depolarization with emmbrane becomign reporlaized. Channels now behave as though in a prologned closed state, because are desensitized toagonists. |
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Term
| moa fo acetylcholiensterase |
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Definition
| hydrolylsis of choline and acetate. |
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Term
| acetylcholiensterase inhibitors |
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Definition
| indirect-acting cholinomiemetics (don’t act on receptors) bind to and inhibit AchE which elevated AcH atsynaptic cleft. |
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Term
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Definition
| simple alchol with 4degree ammonium gorup. Revrsible inhibitor AchE. |
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Term
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Definition
| diagonistic test for myasthenia gravis (will mitigate weakness if blockaed due to competitiv ach recetpor antagonists. Also useful for neruomuscular blockade |
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Term
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Definition
| achE inhibitor- uses: myathenia gravis, reversal of neurmuscular blockade. Attracted to AchE - Hydrolysis yields carbamoylated compoudnd which hstays stuck to achE a lot longer than the acetyalted counterpart of the Ach molecule. |
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Term
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Definition
| carbamate - poor absorption from conjunctiva skin, lungs. Distribution in Cnsneglible , neurmsucular blockade reversor, as well as m |
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Term
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Definition
| carbamate - poor absorption from conjunctiva skin, lungs. Distribution in Cnsneglible. Lognest halflife of the three. MG . |
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Term
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Definition
| carbamate, used for glaucoma, reversal of muscarinic blockade . Well absorbed froma ll sites, used topically in eye, distributed into CNS . More toxic than other two carbamates |
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Term
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Definition
| used as treamtent, but lao used in cehmcial warfare and pesticides. |
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Term
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Definition
| organophosphate: Thiocholine derivate, highly polar, nto well absorbedand doenst enter cns. Very long duration of aciton. |
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Term
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Definition
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Term
| thiphopshate insecticides |
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Definition
| ianctive until conveted to phosphate derivatives. Lipid soulbe and wel laabsorbed from al lroutes, distributes to cns. Oxygen analog conversion activated it in body. |
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Term
| thiophosphate insecticides. MOA |
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Definition
| phosophoylratedby ACHE this enzyme hs halflife of hundreds of hours. Loss of alkyl groups due to aging enchances stbility of inhibitor. |
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Term
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Definition
| cholinesterase regenetor compound. Strong nucleophile. Hdryolyzed phophorylated enzyme if has not aged. Positive hcarge prevents entry itn oCNS, so inenfctie against central effects of organohposhpate. |
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Term
| toxicity of ache inhibitors |
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Definition
| DUMBBELSS : dirrhea urination miosis bornchoconrtistion bradycardia, excitation of skeletal muscle and cns, alcrimation, salivation, sweating. Exension of muscarinic and incitonic receptor effects of ACH. Muscarinc exxcesses apparent first (miosis, slaivation, sweating bronchial constricion vomting diarrhea). CNs involvement usually follows. |
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Term
| therapy from AchE inhbitor toxicity |
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Definition
| maintain vital signs, decontamination atropine to control muscarinic excess, pralidoxime. |
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Term
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Definition
| autoimmuen disease resulting in decreased nubmer of nicotnic receptors on postjuncitonal endp laetes. |
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Term
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Definition
| dipolopia, difficulty speaignand swallowing, ,extremity weakness, respriatory difficulty . Resemble tubocurarine paralysis. |
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Term
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Definition
| neostigmine, pyridostigmien . Longer-actign inhbitiors (organophosphates) don’t allow enough control . |
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Term
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Definition
| diagnostic test to ensure adequcy of treatment (with other choliensterase inhbitiors). Measure baseline msuclestrength, then administor edrophonium and measureagain, If patient has myasthenia improvmeent in msuclestrenght will be observed, so know increase dose of inhibitor.. IF too much inhibitor has been used already, patients may become weak because of nicotinic depolarizing blockade. |
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Term
| therapuetic uses of chiolinesterase inhbiitors |
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Definition
| MG, arrythmias, ileus glaucoma , reversal of neurmoscular blockade (nondepolarizing nerumoscular relaxatns)(neostimien and erophonium) . Muscarnic blockade (cuased by atropien intoxication). Physostigmien used because reversesboth epripheral and central feffects. |
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Term
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Definition
| anticholinesterase actions. uSed fo alzheimers disaease, However signiciant hepatotoxicity. |
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Term
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Definition
| occur at postganglionci cell location |
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Term
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Definition
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Term
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Definition
| ligand binding ,released IP3, DAG, and increased calcium levels |
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Term
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Definition
| lgiand binding opens poatasisum channel direcitly, inhibiting adenyl cyclase |
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Term
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Definition
| cns neurons ,sympathetic postganglionic neurons |
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Term
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Definition
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Term
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Definition
| glands, smooth muscle cells |
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Term
| parasympethatic activity on ehart |
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Definition
| deceleration, decrease contracitlity |
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Term
| parasympathetic acitivty on eye |
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Definition
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Term
| parasympathetic effect on bronchioalr smooth msucle |
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Definition
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Term
| parasympthetic effect on GI |
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Definition
| increases secretion, contracts smooth msucls, relaxes sphicnters |
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Term
| parasymapthetic effect on GU |
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Definition
| contracts wall , relaxe sphincter |
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