USMLE Step 1 Web Prep Antiarrhymic Drugs

145295 >>> 0:00:01

SLIDE 1 of 11

ANS Regulation of Heart Rate

SA & AV nodes are innervated by both PANS & SANS fibers activating 2 & 1 rece!tors res!ective"y# Phase 4 s"o!e increased by cA P $1 activation% & s"o&ed by cA P $ 2 activation%# cA P ca'ses: o '!stro(e ve"ocity in !ace)a(ers by *+a,- ty!e o Action Potentia" .'ration by */ o 01 by *f th's increasing s"o!e of !hase 4 cA P o does the o!!osite2 !"'s !rod'ces a / 3 c'rrent $ */4Ach% &hich s"o&s diasto"ic de!o"ari5ation and th's decreases 01#
SLIDE 2 of 11

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Fig III-2-1. Drugs & Cardiac Action otentials

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Na" C#annel $loc%ers - Class IA

V)a8 via b"oc( of fast Na channe"s $*Na% , 9state,de!endent: AP. & ;ffective 1efractory Period $;1P% via b"oc( of / 3 channe"s $ */2 de"ayed rectifier c'rrent%

&uinidine

,b"oc( , 01 & AV cond'ction< ora""y effective Adverse: na'sea & vo)iting2 cinchonis) $=*2 tinnit's2 oc'"ar dysf'nction2 +NS e8citation%2 hy!otension $a"!ha b"oc(ade%2 >1S & >? interva", synco!e $torsades%# *nteractions: hy!er(a"e)ia increases to8icity< enhances digo8in to8icity< effects of A+h; inhibitors in )yasthenia#
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rocaina(ide )class IA*

-ess ,b"oc( & no a"!ha b"oc(2 b't )ore cardiode!ressant Ara""y effective2 )etabo"i5ed via N,acety"transferase $genoty!ic variation% to NAPA2 an active )etabo"ite &hich !ro"ongs AP. Adverse: S-;,"i(e syndro)e $60B incidence% )ore "i(e"y in s"o& acety"ators2 he)atoto8icity $thro)bocyto!enia2 agran'"ocytosis%2 +NS effects $di55iness2 ha""'cinations%2 +V effects $torsades%#
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Na" C#annel $loc%ers - Class I$

V)a8 $in tachyarrhyth)ias% , b"oc( fast Na3 channe"s $ *Na% , !reference for tiss'es !art"y de!o"ari5ed AP. , b"oc( of s"o& Na3 9&indo&: c'rrents# *V in arrhyth)ias !ost, *2 in heart s'rgery2 or d'e to digita"is & .A+ $.r'g Af +hoice% for arrhyth)ias fo""o&ing atte)!ted cardioversion# 1a!id first !ass effects !rec"'de ora" 'se# Adverse effects: +NS to8icity c'")inating in sei5'res in severe A.# -east cardioto8ic of conventiona" antiarrhyth)ics#
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Lidocaine

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Na C#annel $loc%ers - Class IC

"

V)a8 , b"oc( fast Na3 channe"s $*Na% es!ecia""y 0is,P'r(inCe tiss'e No effect on AP. No ANS effects

Flecainide & Encainide

-i)ited 'se d'e to !ro,arrhyth)ogenic effects "eading to * and &hen 'sed !ro!hy"actica""y in V?#

s'dden death !ost,

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SLIDE - of 11

Class II )$eta $loc%ers*

SA & AV noda" activity s"o!e of !hase 4 $diasto"ic c'rrents% of AP in !ace)a(ers !revent 1 adrenoce!tor activation &hich &o'"d nor)a""y cA P Pro!rano"o" $non,se"ective% & cardiose"ective dr'gs , aceb'to"o"2 )eto!ro"o" & es)o"o" 18 'ses: !ro!hy"a8is !ost, * & in SV?s< es)o"o" $*V% is 'sed in ac'te SV?s & in theo!hy""ine A.#
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Class III )/ C#annel $loc%ers*

"

AP. & ;1P es!ecia""y in P'r(inCe & ventric'"ar tiss'es */ $de"ayed rectifier c'rrent% s"o&ing !hase 6 of AP# *V 'se $bac('!% in "ife,threatening ventric'"ar arrhyth)ias 1e"eases a)ines & is !ro,arrhyth)ogenic $torsades%#

$ret0liu(

Sotalol

2 enantio)ers2 both AP. & ;1P $ */ , de"ayed rectifier c'rrent% and one acts as a 1b"oc(er Adverse: "assit'de2 i)!otence2 de!ression2 torsades2 AV b"oc(#
SLIDE 1 of 11

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A(iodarone

Activity )i)ics a"" antiarrhyth)ic dr'g c"asses $*2 **2*** & *V%, b"oc(s Na 32 +a23 & /3 channe"s and beta adrenoce!tors AP. & ;1P in a"" cardiac tiss'es ;ffective in &ide range of atria" & ventric'"ar arrhyth)ias# Adverse: !'")onary fibrosis2 cornea" de!osits2 !ig)entation $9s)'rf: s(in%2 !hototo8icity2 thyroid dysf'nction2 -.-,+2 torsades2 he!atic necrosis# .r'g interactions: c"earance of digo8in2 !henytoin2 E'inidine2 theo!hy""ine & &arfarin#
SLIDE 12 of 11

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Class I3 )Ca C#annel $loc%ers*

2"

SA & AV noda" activity s"o!e of !hase 4 $diasto"ic c'rrents% of AP in !ace)a(ers Prototy!e +a23 channe" b"oc(er , cardiose"ective2 b't a"so b"oc(s vasc'"ar +a 23 channe"s hy!otension & !ossib"e ref"e8 tachycardia $b"'nted%# .i"tia5e) is si)i"ar# Pro!hy"a8is in reentrant noda" & atria" tachycardias F not GPG# Avoid in V? as )ay !rogress to VH< in digita"is to8icity can de"ayed after, de!o"ari5ation#

3era4a(il

Adverse: =* distress2 di55iness2 f"'shing2 hy!otension2 AV b"oc(

SLIDE 11 of 11

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5nclassified Antiarr#0t#(ics
Adenosine

SA & AV noda" activity and

AV noda" refractory !eriod /3 eff"'8

Activates A,rece!tors ca'ses =i co'!"ed decrease in cA P ca'sing )e)brane hy!er!o"ari5ation# .A+ for PSV?s & AV noda" arrhyth)ias#*V2 ha"f,"ife I 60s Possib"e f"'shing2 sedation & dys!nea Antagoni5ed by theo!hy""ine#

6agnesiu( Possib"e 'se in torsades# N.$.7 Antiarr#0t#(ic drugs t#at 8loc% /" c#annels torsade arr#0t#(ias.