K10 Opioid Analgesics

7/26/2019 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

K10 Opioid Analgesics

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