nalbufln PCl

nuralnl
uLrl Syahlda 0906331733
Analgeslk Cplold Agonls AnLagonls
W A narcoLlc used as a paln medlcaLlon lL
appears Lo be an agonlsL aL kappa oplold
recepLors and an anLagonlsL or parLlal agonlsL
aL mu oplold recepLors
armakodlnamlk
W Merupakan suaLu analgeslk oplum dengan aksl narkoLlk agonls dan anLagonls
W oLensl analgeslk hamplr menyamal morfln dan poLensl anLagonls 1/23
nalokson
W uapaL menyebabkan ke[ang sflncLer Cddl
W 1ldak menlngkaLkan Lekanan arLerl reslsLensl u slLemlk aLau pun beban oLoL
[anLung
W nalbuphlne ls a synLheLlc oplold agonlsLanLagonlsL analgeslc of Lhe phenanLhrene
serles nalbuphlnes analgeslc poLency ls essenLlally equlvalenL Lo LhaL of
morphlne on a mllllgram basls 1he oplold anLagonlsL acLlvlLy of nalbuphlne ls one
fourLh as poLenL as nalorphlne and 10 Llmes LhaL of penLazoclne nalbuphlne by
lLself has poLenL oplold anLagonlsL acLlvlLy aL doses equal Lo or lower Lhan lLs
analgeslc dose When admlnlsLered followlng or concurrenL wlLh mu agonlsL
oplold analgeslcs (eg morphlne oxymorphone fenLanyl) nalbuphlne may
parLlally reverse or block oploldlnduced resplraLory depresslon from Lhe mu
agonlsL analgeslc nalbuphlne may preclplLaLe wlLhdrawal ln paLlenLs dependenL
on oplold drugs nalbuphlne should be used wlLh cauLlon ln paLlenLs who have
been recelvlng mu oplold analgeslcs on a regular basls
Mekanlsme Aksl
W 1he exacL mechanlsm of acLlon ls unknown buL ls
belleved Lo lnLeracL wlLh an oplaLe recepLor slLe
ln Lhe CnS (probably ln or assoclaLed wlLh Lhe
llmblc sysLem) 1he oplaLe anLagonlsLlc effecL may
resulL from compeLlLlve lnhlblLlon aL Lhe oplaLe
recepLor buL may also be a resulL of oLher
mechanlsms nalbuphlne ls LhoughL prlmarlly Lo
be a kappa agonlsL lL ls also a parLlal mu
anLagonlsL analgeslc wlLh some blndlng Lo Lhe
delLa recepLor and mlnlmal agonlsL acLlvlLy aL Lhe
slgma recepLor
1argeL
1 kappatype op|o|d receptor
W harmacologlcal acLlon yes
AcLlons agon|st
lnhlblLs neuroLransmlLLer release by reduclng calclum lon currenLs and lncreaslng
poLasslum lon conducLance 8ecepLor for dynorphlns May play a role ln arousal
and regulaLlon of auLonomlc and neuroendocrlne funcLlons
2 Mutype op|o|d receptor
W harmacologlcal acLlon yes
AcLlons antagon|st
lnhlblLs neuroLransmlLLer release by reduclng calclum lon currenLs and lncreaslng
poLasslum lon conducLance 8ecepLor for beLaendorphln
3 De|tatype op|o|d receptor
W harmacologlcal acLlon yes
AcLlons antagon|st
lnhlblLs neuroLransmlLLer release by reduclng calclum lon currenLs and lncreaslng
poLasslum lon conducLance Plghly sLereoselecLlve recepLor for enkephallns
armakok|net|k
Absorps|
W Sebagal penghllang saklL leblh balk dlberlkan secara lM darl pada C
karena akan 1
max
nya 30 mln (lM)
D|str|bus|
W nalbufln Lldak LerlkaL pada proLeln plasma dan dapaL melewaLl placenLa
Metabo||me
W ulmeLabollsme Lahap l dl Cl dan haLl
||m|nas|
W 7 dlellmlnasl dl urln Lanpa dl ubah dan dl feses L
1/ 2
lasma 3 [am dan
L
1/ 2
ls 24 h
nset
W lv 2 3 mln
W Sk dan lM 13 mln
Duras|
W uurasl unLuk akLlvlLas analgeslk 3 6 [am
nd|kas| dan enggunaan
W MengaLasl rasa saklL sedangparah analgeslk
sebelum dan sesudah operasl Lambahan unLuk
analgeslk yang selmbang ManagemenL of
moderaLe Lo severe paln preoperaLlve and
posLoperaLlve analgesla analgeslk selama
persallnan dan melahlrkan
W enggunaan off|abe|
W encegahan dan pengobaLan lnLraLhecal
morphlnelnduced prurlLus seLelah meahlrkan
secara sesar
kontra nd|kas|
W erLlmbangan sLandar
Dos|s dan ember|an
Dewasa
W Sk / lM / lv 10 mg per 70 kg Llap 3 Lo 6 h sesual
kebuLuhan uosls berbeda Llap orang ada paslen yang non
Loleran 203mg/dosls aLau 1603mg/harl
aran penggunaan
W DnLuk pemberlan secara Sk lM aLau lv bukan secara
lnLradermal aLau lnLraarLerlal
W !angan dlberlkan [lka Ler[adl perubahan sedlaan dan
perubahan warna
W 8uang obaL yang Lldak Lerpakal sesual kebl[akan dan
prosedur Llap lnsLlLusl
W asLlkan keLersedlaan nalokson okslgen dan alaL resuslLasl
dan lnLubasl [lka dlbuLuhkan
eny|mpanan dan kstab||an
W Slmpan ampul dan vlal pada ruangan dengan
LemperaLur yang dlaLur (39 Lo 86)
W Llndungl darl cahaya berleblhan
W Slmpan ampul dan vlal dalam karLon hlngga
lslnya dlgunakan
nteraks| bat
W Depresan SS depressants termasuk
barb|turat anastet|k dapaL menlngkaLkan
penekanan slsLem pernafasan dan SS
W ket|dakcocokan nafclllln keLorolac
fek samp|ng
W konsLlpasl
W uslng
W MenganLuk
W MuluL kerlng
W erasaan seperLl dlpuLar
W SaklL kepala
W 8erkerlngaL/kullL lengkeL
W Mual
W MunLah
W Segera carl banLuan medls [lka
mengalaml
W 8eaksl alergl para[ (ruam gaLal
gaLal kesullLan bernafas sesak dl
dada pembengkakan muluL
muka blblr aLau lldah)
W 8asa saklL dl dada
W kesullLan urlnasl
W lngsan
W MaLl rasa pada lengan aLau kakl
W ke[ang
W SaklL kepala parah puslng aLau
munLah
W ueLak [anLung lambaL
W engllhaLan memburan
S|de ffects by 8ody System for nea|thcare
rofess|ona|s
W Nervous system
W nervous sysLem slde effecLs have frequenLly lncluded sedaLlon (36) dlzzlness/verLlgo (3) and headache (3)
nervousness depresslon resLlessness crylng euphorla floaLlng hosLlllLy unusual dreams confuslon falnLness
halluclnaLlons dysphorla feellng of heavlness numbness Llngllng and unreallLy have been reporLed ln less Lhan 1 of
paLlenLs A depressed level of consclousness somnolence Lremor anxleLy aglLaLlon and selzures have also been reporLed
W ard|ovascu|ar
W Cardlovascular slde effecLs have lncluded hyperLenslon hypoLenslon bradycardla and Lachycardla
W astro|ntest|na|
W CasLrolnLesLlnal slde effecLs have frequenLly lncluded nausea/vomlLlng (6) and dry mouLh (4) Cramps dyspepsla and
blLLer LasLe have been reporLed ln less Lhan 1 of paLlenLs
W esp|ratory
W 8esplraLory slde effecLs have lncluded resplraLory depresslon dyspnea asLhma and pulmonary edema
W Dermato|og|c
W uermaLologlc slde effecLs have lncluded lLchlng burnlng and urLlcarla
W ther
W CLher slde effecLs have frequenLly lncluded a sweaLy/clammy feellng (9) Speech dlfflculLy and flushlng/warmLh have been
reporLed ln less Lhan 1 of paLlenLs
W en|tour|nary
W CenlLourlnary slde effecLs have lncluded urlnary urgency
W cu|ar
W Ccular slde effecLs have lncluded blurred vlslon
W nypersens|t|v|ty
W PypersenslLlvlLy reacLlons have lncluded anaphylacLlc/anaphylacLoldreacLlons lncludlng shock resplraLory dlsLress
resplraLory arresL bradycardla cardlac arresL hypoLenslon and laryngeal edema Some of Lhese allerglc reacLlons may be
llfeLhreaLenlng ueaLh has been reporLed followlng severe allerglc reacLlons Lo nalbuphlne SLrldor bronchospasm
wheezlng edema rash prurlLus nausea vomlLlng dlaphoresls weakness and shaklness have also been reporLed
W oca|
W Local slde effecLs have lncluded paln swelllng redness burnlng and hoL sensaLlons aL Lhe slLe of ln[ecLlon
eaks| yang t|dak d||ng|nkan
W kV 8radycardla hyperLenslon hypoLenslon Lachycardla
W NS SedaLlon (36) dlzzlness verLlgo (3) headache (3) aglLaLlon confuslon crylng
depresslon dysphorla euphorla falnLness floaLlng feellng halluclnaLlons heavlness feellng
hosLlllLy nervousness numbness resLlessness selzures Llngllng unreallLy unusual dreams
(1 or less)
W Dermato|og|c lushlng (1 or less)
W Mata dan 1n1 pengellhaLan buram(1 or less)
W nausea vomlLlng (6) dry mouLh (4) blLLer LasLe cramps dyspepsla (1 or less)
W en|tour|nary Drlnary urgency (1 or less)
W nypersens|t|v|ty AnaphylacLlc or anaphylacLold and oLher hypersenslLlvlLy reacLlons
(lncludlng shock resplraLory dlsLress resplraLory arresL bradycardla cardlac arresL
hypoLenslon or laryngeal edema) sLrldor bronchospasm wheezlng edema rash prurlLus
nausea vomlLlng dlaphoresls weakness shaklness (1 or less)
W oca| ln[ecLlon slLe reacLlons lncludlng burnlng hoL sensaLlons paln redness swelllng
(posLmarkeLlng)
W esp|ratory ulmonary edema (posLmarkeLlng)
W M|sce||aneous SweaLy/clammy feellng (9) speech dlfflculLy warmLh (1 or less)
erhat|an
W regnancy CaLegory 8
W actat|on xcreLed ln breasL mllk
W h||dren SafeLy and efflcacy noL esLabllshed
W ena| unct|on uuraLlon of acLlon may be prolonged ln paLlenLs wlLh renal funcLlon lmpalrmenL
may need Lo reduce dose
W nepat|c unct|on uuraLlon of acLlon may be prolonged ln paLlenLs wlLh hepaLlc funcLlon
lmpalrmenL may need Lo reduce dose
W Spec|a| |sk at|ents Dse drug wlLh cauLlon ln paLlenLs wlLh lmpalred resplraLlon head ln[ury
lncreased lnLracranlal pressure or Ml wlLh nausea or vomlLlng and ln paLlenLs abouL Lo undergo
blllary LracL surgery
W Su|f|te Sens|t|v|ty ConLalns sodlum meLablsulflLe whlch may cause allerglcLype reacLlons
lncludlng anaphylacLlc sympLoms and llfeLhreaLenlng asLhma
W Dependence Low abuse poLenLlal however wlLhdrawal sympLoms can occur afLer longLerm use
Dse drug wlLh cauLlon ln paLlenLs who are emoLlonally unsLable or have hlsLory of narcoLlc abuse
W p|atedependent pat|ents nalbuphlne can preclplLaLe wlLhdrawal small doses of morphlne can
be glven Lo relleve dlscomforL lf paLlenL has recelved morphlne meperldlne codelne or oLher
oplaLe of slmllar duraLlon glve 23 of normal nalbuphlne dose flrsL Cbserve for slgns of
wlLhdrawal and lncrease nalbuphlne dose slowly
Na|buph|ne regnancy Warn|ngs
W 1he placenLal Lransfer of nalbuphlne ls hlgh rapld and varlable wlLh a maLernal Lo
feLal raLlo ranglng from 1037 Lo 16 eLal and neonaLal adverse effecLs LhaL have
been reporLed followlng Lhe admlnlsLraLlon of nalbuphlne Lo Lhe moLher durlng
labor lnclude feLal bradycardla resplraLory depresslon aL blrLh apnea cyanosls
and hypoLonla Some of Lhese evenLs may be llfeLhreaLenlng MaLernal
admlnlsLraLlon of naloxone durlng labor has normallzed Lhese effecLs ln some
cases
W nalbuphlne has been asslgned Lo pregnancy caLegory 8 by Lhe uA nalbuphlne
has been asslgned Lo pregnancy 8lsk acLor u by 8rlggs lf used for prolonged
perlods or ln hlgh doses aL Lerm Anlmal sLudles have falled Lo reveal evldence of
LeraLogenlclLy buL have revealed decreased neonaLal body welghL and reduced
neonaLal survlval raLes wlLh doses up Lo 4 Llmes Lhe recommended human dose
1here are no conLrolled daLa ln human pregnancy nalbuphlne ls only
recommended for use durlng pregnancy when beneflL ouLwelghs rlsk
W Na|buph|ne 8reastfeed|ng Warn|ngs
W nalbuphlne ls excreLed ln human mllk ln amounLs LhaL are consldered cllnlcally
lnslgnlflcanL 1he effecLs Lo Lhe nurslng lnfanL are unknown 1he manufacLurer
recommends LhaL cauLlon be used when admlnlsLerlng nalbuphlne Lo nurslng
women
verdos|s
e[a|a
W 8esplraLory depresslon hypoxemla sedaLlon
nformas| untuk as|en
W 8erlLahukanpada paslen aLau pendamplngnya
1 obaL blasanya dlslapkan dan dlberlkan oleh Lenaga medls pada sarana kesehaLan
2 CbaL harus dlhenLlkan seLelah penggunaan [angka pan[ang dlkurangl secara berLahap kecuall
membuLuhkanpenghenLlan segera (conLoh Ler[adl ruam)
3 MemberlLahukan kepada Lenaga medls [lka Ler[adl sedasl berleblhan aLau menganLuk nafas
lambaL aLau dangkal 1u rendah deLak [anLung lambaL konsLlpasl parah
4 Melaporkan blla mengalaml puslng Advlse paLlenL Lo reporL dlzzlness wlLh poslLlon changes Lo
healLh care provlder
W erhaLlan unLuk paslen dan pendamplngnya
1 obaL dapaL menyebabkanhablLuasl dan [lka dlgunakan dlrumah harus dlgunakansesual dengan
yang dlresepkan dan [angan mengganLl dosls aLau menghenLlkan Lerapl kecuall dlberlLahukan
oleh Lenaga medls 8erlLahukan kepada Lenaga medls [lka obaL Lldak mengurangl saklL
W CauLlon paLlenL LhaL hoL Lubs and hoL showers or baLhs may make dlzzlness worse
W CauLlon paLlenL LhaL drug may cause dlzzlness or drowslness and Lo use cauLlon whlle drlvlng or
performlng oLher Lasks requlrlng menLal alerLness or coordlnaLlon unLll Lolerance ls deLermlned
W CauLlon paLlenL Lo avold alcohol and oLher CnS depressanL medlcaLlons whlle uslng Lhls medlcaLlon
W lnsLrucL paLlenL Lo geL up slowly from lylng or slLLlng poslLlon and Lo avold sudden poslLlon changes
Lo prevenL posLural hypoLenslon
Sumber
W hLLp//wwwdrugscom/mLm/nalbuphlnehLml
W hLLp//wwwdrugbankca/drugs/u800844
W hLLp//wwwmlmscom/lndonesla/drug/lnfo/n
albuphlne/?qnalbuphlne20hydrochlorldeL
ypebrlefmLypegenerlc