muscle relaxant 2015
TRANSCRIPT
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Muscle
Relaxantsdr. Boby Suryawan
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Triad of Anaesthesia
• Analgesia
• Pain control w/ opioid and non-opioid analgesics• Hypnosis
• Drug induced sleep
• Muscle Relaxation
• To minimize patient movement and/or facilitate
ventilation
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Muscle Relaxation
Relasasi !tot dapat dicapai dengan"
• Mendalaman anestesia umum
in#alasi
• Melauan $loade saraf regional
• Pem$erian pelumpu# otot
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Muscle Relaxants
• Depolarizing Muscle Relaxants
• Non-depolarizing Muscle
Relaxants
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What is a Muscle Relaxer?
• A muscle relaxer, alsonown as a musclerelaxant, is a dru!which a"ects seletalmuscle function anddecreases the muscle
tone. #t may be used toalle$iate sym%tomssuch as muscle s%asms,%ain.
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&istory of Muscle Relaxers
The earliest nown use of muscle relaxant dru!s dates bacto the '(th century, when )uro%ean ex%lorers encounterednati$es of the Ama*on were usin! %oison+ti%%ed arrows that%roduced death by seletal muscle %aralysis. By '-,neuromuscular blocin! dru!s became established asmuscle relaxants in the %ractice of anesthesia and sur!ery.
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Muscle Relaxers and the
/er$ous System
• Muscle
relaxers referto two ma0orthera%eutic
!rou%s1neuromuscular blockersand spasmolyt
ics
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Neuromuscular BlockersSpasmolytics
/euromuscular blocers act by interferin! withtransmission at the neuromuscular end %late andha$e no central ner$ous system acti$ity. They areoften used durin! sur!ical %rocedures andin intensi$e care and emer!ency medicine to cause
tem%orary %aralysis.
S%asmolytics, also nown as 2centrally actin!2 musclerelaxants, are used to alle$iate musculoseletal %ain ands%asms and to reduce s%asticity in a $ariety of neurolo!icalconditions.
Two Thera%eutic Muscle
Relaxers
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/euromuscular BlocersMost neuromuscular $locers function $y $locing transmission at t#e end
plate of t#e neuromuscular %unction&
'ormal end plate function can $e $loced $y two mec#anisms& 'on
depolarizing agents( suc# as tu$ocurarine( $loc t#e agonist( acetylc#oline(
from $inding to nicotinic receptors and activating t#em( t#ere$y preventing
depolarization&
Alternatively( depolarizing agents( suc# as succinylc#oline( are nicotinic
receptor agonists w#ic# mimic Ac#( $loc muscle contraction $y depolarizing
to suc# an extent t#at it desensitizes t#e receptor and it can no longer initiatean action potential and cause muscle contraction&
)ot# of t#ese classes of neuromuscular $locing drugs are structurally similar
to acetylc#oline( t#e endogenous ligand( in many cases containing two
acetylc#oline molecules lined end-to-end $y a rigid car$on ring system( as
in pancuronium *a nondepolarizing agent+&
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Depolarizing Muscle Relaxants
• Depolarizing Muscle Relaxants $eer%a seperti acetylcholine( tetapi tida dapat
dirusa ole# cholinesterase di cela# saraf&
• Depolarizing Muscle Relaxants menye$a$an depolarisasi yang ditandai ole#
fasiulasi yang disusul ole# relasasi otot luri&
•Termasu golongan pelumpu# otot depolarisasi adala# succinylcholine dan
decamethonium&
•Durasi er%a succinylcholine sangat pende
•,uccinylcholine dimeta$olisme ole# enzim plasma cholinesterase
* pseudocholinesterase+ di pem$ulu# dara#&
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Depolarizing Muscle Relaxants
fe samping succinylcholine adala#"
• 'yeri otot( ter%adi pada .0 asus( dapat diurangi dengan mem$erian
pelumpu# otot non-depolarisasi dosis ecil se$elumnya&
• Peningatan teanan intraoular
• Peningatan teanan intraranial
• Peningatan teanan intragastri
•
Peningatan adar alium plasma *#iperalemia+• Aritmia %antung
• ,alivasi
• Alergi( anafilasis
• Malignant hyperthermia
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Non-depolarizing Muscle Relaxants
• Non-depolarizing muscle relaxants
beriatan den!an muscarinic
cholinergic receptors, seba!ai inhibitor
acetylcholine, sehin!!a acetylcholine
tida da%at beer0a dan tida ter0adi
de%olarisasi.
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)erdasaran susunan moleul( non-depolarizing muscle relaxants digolongan
men%adi"
)enzyliso1uinol
inium
" tu$ocurarine( metocurine( atracurium(
doxacurium( mivacurium
,teroid " pancuronium( vecuronium( pipecuronium(
rapacuronium( rocuronium
P#enol et#ers " 2allamine
'ortoxiferine " Alcuronium
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Dosis
awal
(mg/kg)
Dosis
rumatan
(mg/kg)
Duras
i
(meni
t)
Efek Samping
Nondepol long-acting! "ubocurarine
(tubarin)
#! $ancuronium
%! &etocurine
'! $ipecuronium
! Doacurium
*! +lcuronium
(alloferin)
3.-3+3.(3
3.34+3.'5
3.53+3.-3
3.36+3.'5
3.35+3.34
3.'6+3.3
3.'3
3.3'6+3.353
3.36
3.3'+3.3'6
3.336+3.3'3
3.36
3+(3
3+(3
-3+(3
-3+(3
-6+(3
-3+(3
&istamin 7, hi%otensi
8a!oliti, taiardi,
tensi 9
&istamin +, hi%otensi
:ardio$asular stabil
:ardio$asular stabil
8a!oliti, taiardia
Nondepol intermediate acting! ,allamine (aedil)
#! +tracurium
(tracrium)
%! .ecuronium
(norcuron)
'! ocuronium
(esmeron)
! 0istacuronium
-+(
3.6+3.(
3.'+3.5
3.(+'.3
3.'6+3.53
3.6
3.'
3.3'6+3.35
3.'3+3.'6
3.35
3+(3
53+-6
56+-6
3+(3
3+-6
&istamin ;, hi%otensi
Aman untu he%ar,
!in0al
#somer atraurium
Nondepol s1ort acting! &i2acurium
(mi2acron)
#! opacuronium
3.53+3.56
'.6+5.3
3.36
3.+3.6
'3+'6
'6+3
&istamin 7, hi%otensi
Depol s1ort acting+
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Muscle Relaxants
• hiccup
• @indin! %erut au
• Ada tahanan %ada inasi %aru
'. an!!uan faal
!in0al
5. an!!uan faal hati
. Miastenia !ra$is
-. Bedah sin!at
6. :asus obstetri
1
1
1
1
1
Atracurium, $ecuronium
Atracurium
Cia dibutuhan, dosis 'D'3 atracurium
Atracurium, rocuronium, mi$acuronium
Semua da%at di!unaan ecuali !allamine
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Antidotum/euromuscular Blocer
• Penawar pelumpu# otot atau acetylcholinesterase inhibitor *anti-cholinesterase+
$eer%a pada neuro-muscular junction untu mencega# acetylcholinesterase&
• Anti-cholinesterase yang paling sering digunaan adala# neostigmine
*prostigmin+( piridostigmin( dan edrop#onium&
• Penawar pelumpu# otot $ersifat muscarinic se#ingga menye$a$an #ipersalivasi(
eringatan( $radiardia( e%ang $ronus( #ipermotilitas usus( dan pandangan
a$ur&
• Pem$erian o$at penawar pelumpu# otot #arus disertai ole# o$at
vagolytic
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Antidotum/euromuscular Blocer
• Dosis o$at-o$atan penawar muscle relaxants
• neostigmine adala# (3-(4 mg/g5
• pyridostigmine (6-(3 mg/g5
• edrophonium (7-6( mg/g5
• dan physostigmine (6-(8 mg/g&
• Dosis o$at-o$atan vagolytic
• atropine dosis (6-(9 mg/g atau
• glycopyrrolate dosis (7-(6 mg/g sampai (9-(8 mg pada dewasa&
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S%asmolytics,pasmolytic agents generally wor $y eit#er en#ancing t#e level of
in#i$ition( or reducing t#e level of excitation&
:n#i$ition is en#anced $y mimicing or en#ancing t#e actions ofendogenous in#i$itory su$stances( suc# as gamma-Amino$utyric acid
*2A)A+&
2A)A is t#e c#ief in#i$itory neurotransmitter in t#e mammalian central
nervous system& :t plays a role in regulating neuronal excita$ility
t#roug#out t#e nervous system& :n #umans( 2A)A is also directlyresponsi$le for t#e regulation of muscle tone&
,pasmolytics are referred to as ;centrally acting muscle relaxants<
$ecause t#ey can $e used to target specific regions of t#e $ody suc# as
low $ac and nec&
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S%asmolytics
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S%asmolytic dru!s
De3nition of muscle spasm
(spasticity)4'. #ncreased muscle tone5. to!ether with muscle weaness#t is often associated with cerebral %alsy,
multi%le sclerosis, and stroe.
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=entrally actin!s%asmolytic dru!s
Drug &ec1anism
'+ @ia*e%am ABA rece%tor
5+ Baclofen ABA rece%tors causin!hy%er%olari*ation by increasin!%otassium conductance
Ad$erse e"ects1 drowsiness andincreased sei*ure acti$ity
+ Ti*anidine E5 adrenorece%tor a!onist-+ aba%entin
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DIAZEPAM
• Benzodiazepines facilitate the action of γ-aminobutyric acid (GABA) in the central nervoussystem.
• Diazepam acts at GABA A synapses, and its actionin reducin spasticity is at least partly mediated inthe spinal cord
• Althouh diazepam can be used in patients !ith
muscle spasm of almost any oriin (includinlocal muscle trauma), it produces sedation at thedoses re"uired to reduce muscle tone.
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BACLOFEN • Baclofen (p-chlorophenyl-GABA) was es!"ne
#o $e an orally ac#!%e GABA-&!&e#!c a"en#' !#sspas&oly#!c ac#!%!#y a# GABA B recep#ors' #h!sresl# !n• hyperpolar!*a#!on' pro$a$ly $y !ncrease +,
conc#ance• !nh!$!#!on of rec!n" calc!& !n./• 0h!s w!ll rece e/c!#a#!on of sp!nal cors an
rece pa!n !n pa#!en#s w!#h spas#!c!#y'
perhaps $y !nh!$!#!n" #he release of s$s#ance P (nero1!n!n-2) !n #he sp!nal cor• Baclofen !s a# leas# as e3ec#!%e as !a*epa& !n
rec!n" spas#!c!#y wh!le proc!n" lesssea#!on In a!#!on' $aclofen oes no# receo%erall &scle s#ren"#h as &ch as an#rolene
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• A%erse e3ec#s
•
Drows!ness' #oleran# #o #he sea#!%ee3ec# w!#h chron!c a&!n!s#ra#!on
• Increase se!*re ac#!%!#y has $eenrepor#e !n ep!lep#!c pa#!en#s
• 0herefore' w!#hrawal fro& $aclofen
&s# $e one %ery slowly
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0IZANIDINE
• A%erse e3ec#s' !ncl!n"
rows!ness' hypo#ens!on' ry &o#h'an as#hen!a
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O04E5 CEN05ALL6 AC0ING7PA7MOL60IC D58G7
• ,abapentin
• I# !s an an#!ep!lep#!c r" #ha# has shown cons!era$lepro&!se as a spas&oly#!c a"en# !n se%eral s#!es!n%ol%!n" pa#!en#s w!#h &l#!ple scleros!s
• Pre"a$al!n
• !s a new analo" of "a$apen#!n #ha# &ay also pro%e
sefl Pro"a$!e an "lyc!ne ha%e also $een fon !nprel!&!nary s#!es #o rece spas#!c!#y Pro"a$!e !s aGABA A an GABA B a"on!s# an has ac#!%e &e#a$ol!#es'!ncl!n" GABA !#self Glyc!ne !s ano#her !nh!$!#orya&!no ac! nero#rans&!##er I# appears #o possessphar&acolo"!c ac#!%!#y when "!%en orally an rea!lypasses #he $loo-$ra!n $arr!er
• Iroc!la&!e an r!l*ole• 0hey are newer r"s for #he #rea#&en# of a&yo#roph!c
la#eral scleros!s #ha# appear #o ha%e spas&-rec!n"e3ec#s' poss!$ly #hro"h !nh!$!#!on of "l#a&a#er"!c#rans&!ss!on !n #he cen#ral ner%os sys#e&
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Dantrolene4
5ndications4
'+ Muscle s%asticity
5+ Mali!nant hy%erthermia1o !eneralanesthetics or succinylcholine there is a sudden and %rolon!edrelease of calcium, with massi$e muscle contraction, lactic acid
%roduction, and increased body tem%erature.Treatment of mali!nant hy%erthermia1
'. control acidosis and body tem%erature5. Reduce calcium release with intra$enous dantrolene•. Ma9or a%erse e3ec#s
• are "eneral!*e &scle wea1ness' sea#!on' an occas!onally hepa#!#!s
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T&A/:S