9. mdn-ketorolac akhir (no p).ppt
TRANSCRIPT
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Aznan Lelo
Dep. Farmakologi & Terapeutik,Fakultas KedokteranUniversitas Sumatera
Utara
2 A ril 2011 MEDAN A!N 2011 Medan
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Surgical Inflammatory Pain
functio
laesiarubor
calor
tumor
inflammation
acute chronic
pain
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Inflammatory mediatorand its actions
Mediator Pain Vascularpermeability
Vaso-dilatation
Chemotaxis
Histamine -
++ -
Serotonin -
+/- -
rady!inin +++
+++ -
Prosta-
glandin +
+++ +++
"eu!o-triene
-
- +++
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Classification of some ma#or
features of pain$ype %ura-
tionCharac-teristics
Cells &dapti'eresponse
(xamples
&cute Seconds Proportional
to the cause
Nociceptive Withdrawal,
escape
Contact with
hot surface
Sub-chronic
Hours todays
Hyperalgesia,Allodynia,Spontaneouspain
NociceptiveNeurogenic
Quiescence,Avoidance ofcontact withinjuredtissues
Inflaatorywound
Chronic !onths toyears
Hyperalgesia,Allodynia,SpontaneouspainAffectivecoponent
NociceptiveNeurogenic
Psychologicaland cognitive
Arthritis, CNSinjury,etastaticdisease
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)ocicepti'e Pain
" #$aples%
& Post-surgical
& etastatic 'one pain& usculos(eletal pain
& arthritic pain
" What to (now
& *esponds to )S&I%s and pioids
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,actors that modify post-
operati'e pain
)* Site, nature and duration of surgery*
+* ype and e$tent of incision*
-* Physiologic and psychologic a(eup ofthe patient*
.* Pre operative preparation of the patient*
/* Presence of coplications of surgery*
0* Anesthetic anageent*
1* Quality of perioperative care*
2* Preoperative treatent of painful stiuli *
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Pain Management
.oals of Pain Managemento 3elieve sufferingo Increase functional capacityo Iprove 4uality of life
ays to ad'ocate forPainManagement
o 5on6t use place'oso Proote pain education with all
disciplines
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Pathophysiology of acuteinflammatory pain
" Pain ediators released in acute
inflaatory pain
& 7rady(inin
& Prostaglandin
" #n8ye involved in prostaglandin
synthesis
& C9: ) ; C9:
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C0-1/C0-2 selecti'ity of )S&I%s
nonsele"tive
re#$%&'(2
%&'(2sele"tive
%&'(1sele"tive
re#$%&'(1
anti(in)ammation
anal*esi"NN+
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10/28Warner et al. PNAS1999; 96: 7563-7568
C0-1 Inhibition at $herapeutic C0-2 Inhibition
in a Human hole lood &ssay
! " 6 8 1 1!
ro#e"oi-
NS(./
etodola"meloi"am
nimesulide"ele"oi-
tomoiproldi"lo#ena"
sulinda" sulpide
piroi"amme"lo#enamate
di)unisalni)umi" a"id
sodium sali"late#enopro#en
zomepira"
indometa"intolmetin
naproeni-upro#en
amproneketopro#en
aspirin
)ur-ipro#ensupro#en
ketorola"
# $n%iition '()-1 *%en '()-! in%iite+ 8#
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Willoug% D, et al. '()-1, '()-!, an+ '()-3 an+ t%e uture
treatment o /%roni/ in0ammator +ieae. 2an/et 355: 6"6-
&' potesized "entrall involvesin in)ammator pain
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=hu :, Con(lin 53, #isenach >C*
Preoperati'e Inhibition of Cyclooxygenase-1
in the Spinal Cord *educes Postoperati'e Pain
Anesth Analg ??%)-@?
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)g &7 $emple &7 Smith .7 (membolu 8
(arly analgesic effects of parecoxib versus!etorolacfollo9ing laparoscopic sterili:ation
a randomi:ed controlled trial7ritish >ournal of Anaesthesia, @+0B%2.0
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3eu'en SS, 7uvanendran A, Droin >S, Stein'erg 37*
Postoperati'e modulation of central ner'ous system
prostaglandin (2 by cyclooxygenase inhibitors after
'ascular surgery;Anesthesiology* )?.-B%.))
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Current 'ie9 in selecting analgesic and
anti-inflammatory drugs
(fficacyindicationB Safety side effectB
)ot onlyEI to$icity
Cardiovascular to$icity 3enal to$icity 7leeding 7one healing ipairent etc
Suita'ility contra
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9
C9+H
9
acetylsalicylic acid
aspirin
H
N
9
acetainophen
ylenol
H9
C9+H
i'uprophen
!otrin, Nuprin
C9+H
(etoprophen
9rudis
9
C9+H
napro$en
Naprosyn, Alleve
(etorolac
oradol
9
!e9
HN
diclofenac
Catafla, Foltaren
Cl
Cl
C9+
N
C9+H
indoethacin
Indocin
N
9 Cl
C9+H
!e9
%emi"al stru"ture o#NSA!Ds
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3etorolac tromethamine
a e'er of the pyrrolo
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Pharmaco!inetic Parameters =Mean < S%>
po7 im and i' doses of 3etorolac $romethamine
3oute of adinistration po i IvPharaco(inetic Paraeter )? g )/ g )/ g
7ioavaila'ility e$tentB )??K )??K )??K
a$
)inB .. L -. -- L +)MM )*) L ?*1MM
Ca$
+cglBGsingle dose ?*21 L ?*++ )*). L?*-+MM
+*.1 L?*/)MM
Ca$
cglBGsteady state 4id)*?/ L?*+0MM
)*/0 L?*..MM
-*?@ L)*)1MM
Cin-cglBGsteady state 4id ?*+@ L?*?1MM ?*.1 L?*)-MM ?*0) L?*+)MM
Cavg
.cglBGsteady state 4id ?*/@ L?*+?MM
?*@. L?*+@MM
)*?@ L?*-?MM
F'eta
/(gB ?*)1/ L
?*?-@
?*)1/, Choi #D, Dil HD*
3etorolac or fentanyl continuous
infusion for post-operati'e analgesia
in children undergoing
ureteroneocystostomy*Acta Anaesthesiol Scand* +?)) >anO//)B%/.
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5aw(ins N, 7arclay CA, Eardiner 3,
Drawc8es(i C5*
Safety of intra'enous use of
!etorolac in infants follo9ing
cardiothoracic surgery;Cardiol oung* +??@ e'O)@)B%)?/
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" Detorolac is an acidic and C9: