Download - K10 Opioid Analgesics
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BMS-K 10OpioidAnalgesics
Aznan Lelo
Dep. Farmakologi & Terapeutik,Fakultas KedokteranUniversitas Sumatera
Utara
1 anuari "010 KBK BMS-10 FK USU
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ANALGETIKA OPIAT
Peptida endogen opioid
FD/FK opioid
Efek samping, antidiare, antitussiva Interaksi
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Analgesics
Decrease in sensation of pain.
Classes:
Opioid.
Agonist. Antagonist.
Agonist-antagonist.
Non-opioids.
Saliclates. NSA!Ds.
Ad"uncts.
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Opioids
#eneric reference to morp$ine-likedrugs%actions
Opiate: deriatie of opium 'rototpe: morp$ine
(orp$eus: god of dreams
Act on endorp$in receptors: (u )most important*
+appa
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Actions o$ Opioid
%eceptorsResponse Mu Kappa
Analgesia
Respiratory Depression
edation
Eup!oria
P!ysi"al Dependen"e
#I motility
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Actions at Opioid
%eceptorsDrugs Mu Kappa
Pure Agonists
$morp!ine, "odeine, meperidine %Demerol&
',fentanyl %u(lima)e&', remifentanil %*ltiva&',propo+yp!ene %Darvon&', !ydro"odone%i"odin&', o+y"odone %Per"o"et&'
Agonist Agonist
Agonist$Antagonist$nal(up!ine %-u(aine&', (utorp!anol %tadol&'
Anta$
gonist
Agonist
Pure Antagonist$nalo+one %-ar"an&'
Anta$gonist
Anta$gonist
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&eneral Actions o$Opioids
Analgesia
espiratordepression
Constipation rinar retention
Coug$ suppression
mesis !ncreased !C' !ndirect t$roug$ CO/
retention
up$oria%Dsp$oria
Sedation
(iosis
'upil constriction
'reload &afterload
0atc$ for$potension1
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Opioid %eceptors
Opioid receptors
2inding sites not onl for
endogenous opiates 2ut also foropioid analgesics to reliee pain.
Seeral tpes of receptors:
(u, +appa, Delta, psilon andSigma.
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Mu %eceptors
3ocation:
CNS incl. 2rainstem, lim2ic sstem,dorsal $orn of spinal cord
(orp$ine sulfate and morp$inesulfate agonists 2ind to (u receptors
4ind to opioid receptors in 2rain andSC and een in perip$er
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'arcotic Analgesics
eliee moderate to seere pain 2
in$i2iting release of Su2stance ' incentral and perip$eral neres5
reducing t$e perception of painsensation in 2rain,
producing sedation and
decreasing emotional upsetsassociated 6it$ pain
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'arcotic Analgesics
Can 2e gien orall, !(, su2 7, !8 oreen transdermall
Orall are meta2oli9ed 2 lier,ecreted 2 kidne;caution ifcompromised
(orp$ine and meperidine producemeta2olites
0idespread e
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(ndications $or Use
4efore and during surger
4efore and during inasie diagnosticprocedures
During la2or and delier
T acute pulmonar edema
Treating seere, nonproductie coug$
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)ontraindications to Use
espirator depression
C$ronic lung disease
C$ronic lier or kidne disease 4'=
!ncreased intracranial pressure
=persensitiit reactions
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Management)onsiderations
age-speci>c considerations
(orp$ine often drug of c$oice;non-ceiling. Ot$er nonceiling drugs
include: $dromorp$one, leorp$anoland met$adone
se non-narcotic 6$en a2le
Com2inations ma 6ork 2 di
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%oute selections
Oral preferred
!8 most rapid;'CA allo6s selfadministration. 4asal dosage. (oree
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*osage
Dosages of narcotic analgesicss$ould 2e reduced for clientsreceiing ot$er CNS depressants
suc$ as ot$er sedatie-tpe drugs,anti$istamines or sedatingantianiet medications
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Sc+eduling
#ie narcotics 2efore encouragingturning, coug$ing and deep2reat$ing in post-surgical patients
Automatic stop orders after @/$
!n acute pain, narcotic analgesics aremost e
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(ndividual *rugs
Agonists $ae actiit on mu andkappa opioid receptors
Agonist%antagonists $ae agonist
actiit in some receptors5antagonists in ot$ers. =ae lo6era2use potential t$an pure agonists5
2ecause of antagonism;can produce6it$dra6al smptoms
Antagonists are antidote drugs
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Agonists
Alfenta )alfentanil*;s$ort duration Codeine Su2lima9e or Duragesic )Fentanl*;s$ort
duration
Dilaudid )$dromorp$one* Demerol )meperidine*;preferred in urinar and
2iliar colic, less resp. depression ne62orns (orp$ine OContin Daron )propop$ene* ltram )tramadol* (et$adone
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Agonists,Antagonists
=ae lo6er a2use potential t$an pureagonists
4uprene )2uprenorp$ine*
Nu2ain )nal2up$ine*
Tal6in )penta9ocine*
Stadol )2uto$anol*;also in nasalspra
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Antagonists
ee )nalmefene*;longer durationof action t$an Narcan
Narcan )naloone*
e8ia )naltreone*-used inmaintenance of opiate-free states inopiate addicts
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Narcotic )Opioid*Antagonists
urpose.eerse CNS depression andrespirator depression from ecessieopioid usage.
Action.4lock t$e e
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FARMAKOLOGI SSP
Kanal ion
.apak kera o(at dan mekanisme
modulasi transmisi sinap
E+"itatory and in!i(itory neurotransmitter
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(n+i2itor3 and Facilitator3Mec+anisms
Neurotransmitters;c$emicals t$ateert in$i2itor or ecitator actiitat post-snaptic nere cell
mem2ranes. amples include:acetlc$oline, norepine$prine,epinep$rine, dopamin, and serotonin.
Neuromodulators;endogenousopiates. =ormones in 2rain. Alp$aendorp$ins, 2eta endorp$ins andenkep$alins. =elp to reliee pain.
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4opics
Analgesics and antagonists
Anest$etics
Anti-aniet and sedatie-$pnotics Anti-sei9ure % anti-conulsants
CNS stimulators
'sc$ot$erapeutics ANS%'NS%SNS agents