muscle relaxant 2015

8/18/2019 Muscle Relaxant 2015

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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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muscle relaxant 2015

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