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USMLE Step 1 Web Prep Cholinergic Receptors Antagonists

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Muscarinic Receptor Antagonists (Parasympatholytics)


Atropine -- prototype, tertiary amine (enters CNS) Low dose decreases H ! moderate dose increases H decreased secretions (sa"i#ary, $ronc%io"ar, sweat) mydriasis & cyc"op"e'ia %ypert%ermia wit% res("tin' #asodi"ation decreased )* moti"ity de"(sions & %a""(cinations +dry as a $one, red as a $eet, %ot as a pisto", $"ind as a $at & mad as a %atter, -o.icity mana'ement: "ar'e"y symptomatic /0- p%ysosti'mine
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!linical "ses # !haracteristics of M$%loc&ers


Drug atropine tropicamide ipratropi(m scopo"amine '"ycopyrro"ate $en9tropine
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!linical "ses an'(or !haracteristics antispasmodic, antisecretory, AC%3 in%i$itor 45, antidiarr%ea" op%t%a"mo"o'y (topica") ast%ma & C465 (in%a"ationa") 7 no CNS entry antimotion sic8ness, ca(ses sedation & s%ort-term memory $"oc8 antispasmodic antisecretory, anti-("cer 7 no CNS entry 6ar8insonism & dr('-ind(ced e.trapyramida" dys:(nction
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*anglion %loc&ing Agents


Competiti#e anta'onists at NN receptors in ANS 'an'"ia 3::ects depend on inner#ation to e::ectors and ANS dominance <or tiss(es wit% d(a" inner#ation 6ANS is dominant 7 inc"(de SA & A= nodes, p(pi", )*0)> m(sc"es & sp%incters SANS is dominant on"y in terms o: #asc("ar tone & sweat '"ands )an'"ion $"oc8ers red(ce t%e dominant tone (-a$"e **-5?) He.amet%oni(m (prototype), mecamy"amine, trimet%ap%an
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*anglion %loc&ers Pre,ent A-S Refle.es/


@"oc8 $radycardia or tac%ycardia e"icited $y c%an'es in mean @6 C%aracteristic (se:(" in A(estions on dr(' *5 7 %e"ps determine i: a dr(' action (e', on %eart rate) is direct, or d(e to ANS re:"e. response 3.amp"e: %e.amet%oni(m $"oc8s re:"e. $radycardia t%at occ(rs w%en p%eny"ep%rine ca(ses #asoconstriction! it does not $"oc8 $radycardia :rom direct acti#ation $y AC% o: cardiac B-receptors
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S&eletal -M0 %loc&ers


-on'epolari1ing Competiti#e anta'onists at NB receptor o: m(sc"e endp"ate e#ersi$"e $y AC%3 in%i$itors *nc"(de t($oc(rarine, atrac(ri(m & panc(roni(m Depolari1ing A'onist at NB receptors (s(cciny"c%o"ine) *nitia" :ascic("ation, t%en para"ysis t%ro('% persistent mem$rane depo"ari9ation Not re#ersed $y AC%3 in%i$itors

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