Ome pr a z o l ea da l a ho b aty a n gd i g ol o ng k a ns e b ag aip en gh amb atp omp ap r o t o n/ p r o t o np u mpi mp n hi b i t o r( PPI ) . Omep r a zo l eb er f un gs is eb ag aiob atu nt u kp en y ak i t p en y ak i ty a ngd i s eb ab ka no l e hk e l e bi h anp r od uk s ia sam l a mb mb un g.Ob ati n ime ne k a ns e k r e s ia s a ml a mb mb un gd en ga nc a r ame me ng ha mb mb ats e c a r as pe s i fi kd ani r r e v e r s i b e l si st em pomp mpaasam dal am muk osal amb mbung.
I ndi kasi
Ke gu na anome pr a zo l ead al ahun t u kpe ng oba t ank on di s i k o nd i s i b er i k u t: •
Omepr azol edi gunakandal am pengobat angast r oesophagealr efluxdi sease( GERD) .GERD adal ah p en y a k i td i ma nape nd er i t ame ng al a mis mi e ns a s it e r b ak a rd ia r e ad ad ad ank er o ng k on ga nk a r e naas a m l ambungnai kk ek er ongk ongandant er j adi i r i t as i .
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Unt ukmengobat it ukakl amb mbung dan t ukakususbesar .Tukakl amb mbung bi asanyadi sebabkan ol eh i n f e k si b ak t e r i He l i c ob ac t e rp y l o r i d anp ema ka i ano ba t o ba tNSAI Dda l am j a ng kawa kt upa nj a ng .Un t u k t uj ua ni n io me me pr a zo l ebi a sa ny adi b er i k and al am k o mbi mb na si d en ga n amox i c i l l i ndanCl ar i t hr omy ci n.
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o ba ti n ij u ga b er g un au nt u k me na ng an ie r o s i fe s o ph ag i t i ss u a t uk o n di s id i ma na k e r o ng k o ng an ( e s op ha gu s )me me ng al a mip mi er a da ng an k a r e na i r i t a s ia s am l a mb mb un g,i n f e k s iv i r u sa t a uj a mu mu r ,d an pen ggunaanal k ohol s er t aobat obat ant er t ant u.
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Be r man f a atj u ga un t u kp en go ba t a nz ol l i ng ere l l i s on s y nd r ome ,s u at up en y ak i tl a ng ka y a ng t e r j a di k a r e nat u mo mo rp an k r e asa t a uu s u sb es a rme l e pa s k a nh or mo ny a n gme n y e ba bk a nt e r j a di n y ak e l e bi h an pr oduksi asam l amb mbung.
Kont r ai ndi k as i •
j anganmenggunak anomepr az ol eunt ukpas i eny angmemi l i k i r i way athi per s ens i t i f .
Ef eksamp mpi ng
Se car aumu mo me me pr a zo l eb i s ad i t ol er a ns id en ga nba i k ,s el a madi ma b er i k anpad ado si sy a ngdi a nj ur k an .Be r i k u t a da l a hb eb er a paef e ks amp i n gy a ngmu mu ng k i nt e r j a di : •
Ef e ks amp i n gr i n ga npa das al ur a np en ce r na anmi s al n y adi ar e,n y er i p er u t ,s embe l i t ,mu al da nmu nt a h. Po l i pl a mbu mb ngda nh i p er pl a si ad i l a po r k ant e r j a di p ad ap en ggu na anj an gk ap an j a ng .
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Ef eks ampi ngpadao r g anhat i adal aht e r j adi n y apeni ngk at ans er um t r ans ami nas e,a l k al i f os f at as e,dan bi l i r ubi n.Kej adi ank ej adi ans eper t i hepat i t i s ,e ns ef al opat i hat i ,gagal hat i f ul mi nans angatj ar angt er j adi .
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Ef e ks a mp i n gp ad ag i n j a lr e l a t i fj a r a ng .Na mu np ad ap e ng gu na anj a ng k ap a nj a ngd and os i sy a n g be sa r ,o me pr a zo l ed apa tme ni n gk at k ank r e at i n i ns er um d anr e si k ok e r u sa ka ng i n j a l ,t e r ma su kg ag al gi nj al ak ut .
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Ome pr a z ol eme ny e ba bk a np us i n g,s a k i tk e pa l ad anv e r t i g op ad ab eb er a pao r a ngy a ngs e ns i t i f .
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Ef e ks a mp i n gp ad as a l u r a np er n af a s any a ngd i k e t a hu ia da l a hb at u k .
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T el ah ad a l a po r a nl a po r an t e r j a di n y a a ne mi a h emo l i t i k ,t r omb os i t o pen i a ,a gr a nu l o si t o si sd an l e uk o si t o si sp ad ap ema ka i a nj a ng kapa nj a ng .
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Reak s ihi per s ens i t i v i t asak i batpemak ai anobati ni s angatj ar ang,namunj i k at er j adiper t ol onganmedi s ha r u ss eg er ad i b er i k anka r en ab i s ame ny e bab ka ns y o ka na fil a k s i sy an gbe r a ki b atf a t al
Per ha t i a n
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Pemak ai anome pr az ol ehar usd i he nt i k anj i k at andat andaa walr eak s ial er gis eper t ir uam,gat al ,s ak i t t enggor ok an,demam,ar t hr al gi a,puc at ,at au t andat anda l ai nn y a munc ul ,k ar ena j i k at er j adibi s a ber ak i batf at al .
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o me pr a z ol ed i k e t a hu ii k u tk e l u arb e r s a ma a i rs u s ui b u( ASI )me s k i p un d al a m j u ml a hy a n gk e c i l t e r u t a mas e t e l a h 3j a mp ema k a i a n.Na mu no ba ti n id i d eg r a da s id en g ans a ng atc e p ato l e hk o n di s i a s am,s e h i n gg as e j u ml a hk e c i lo ba ty a n gma s u kk ea i rs u s ui b ud ant e r mi n um o l e hb a y ia k a nr u s a k s ebe l um d i a bs or p si .Na mu nj i k aan dar a gu,b er k o ns ul t a si l a hd en ga nd ok t e ran da .
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Ob at o ba tg ol on ga np omp ap r o t o ni n hi b i t or( PPI )t e r ma su ko me pr a zo l e,h ar u sd i b er i k ans ec ar aha t i hat i padapas i enpender i t ahi pok al s emi aat auhi popar at i r oi d i s me.
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Ome pr a z ol eme ny e ba bk a nt e r j a di n y ad i fi s i e ns iv i t a mi nB1 2d anma l a bs o r p s iz a tb es i ,t e r u t a map ad a p ema k ai a nj a ng k ap an j a ng .Ad ab ai k n y aj i k ap ema k ai a no ba ti n id i l a k uk a ns e c ar aj a ng k ap an j a ng d i b ar e ng id en ga ns u pl e me nv i t a mi nB1 2.
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Ob at o ba tPPIs ep er t io me pr a zo l ed i k e t ah uime ni n gk at k an r e si k ot e r j a di n y ap at a ht u l an gk ar e na o st eo por o si st e r u t a mapa dap i n gg ul ,p er ge l a ng ant an ga n,a t a ut u l a ngb el a kan g.Re si k oi n is ema ki n me ni n gk atp adap ema ka i a nj a ng kap an j a ngd and os i sy an gl e bi ht i n gg ida r iy a ngdi an j u r k an .Pa si en y angmemi l i k ir es i k oi ni ,har usdi ber i k andos i st er endahdar i omepr az ol e.
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Ke aman anda ne f e kt i v i t a so ba ti n ip ad aa na ku si ak u r a ngd ar i 1t ah unma si hb el u md i k e t ah ui .
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Ha t i h at i me ng gu na ka nob ati ni pa dap as i e nd en ga ng an gg ua nf u ng si ha t i d ang i n j a l .
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obati nibi samenyebabkanpusi ng.Janganmengemudiat aumenyal akanmesi nsel amamenggunakan obati ni .
T ol e r a ns it e r ha da pk e ha mi l a n
Pe ne l i t i a np ad ar e pr o du k s ih ewa nt e l a hme nu nj u k k anef e kb ur u kpa daj a ni nda nt i d akad as t u di y a ngme ma da i d ant e r k e n da l id en ga nb ai kp ad ama nu s i a ,n amu nj i k ap ot e ns ik e u nt u ng and ap atd i j a mi n ,p en gg un aa no ba t pa dai b uha mi l d ap atd i l a k uk anme sk i p unpo t e ns i r e si k os an ga tbe sa r .
i nt e r a ksioba t
Ber i k utadal ahi nt er ak s iomepr az ol edenganobat obatl ai n: •
Omep r a zo l emen ur u nk anef e kf a r ma k ol o gi sc l op i do gr e lj i k adi b er i k anse c ar abe r s amaa n.
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Ome pr a z o l eme ng ha mb atk e r j ae nz i m CYP3 A4 ,o l e hk a r e nai t uo ba t o ba ty a n gd i me t a bo l i s meo l e h en zi m CYP3 A4s ep er t i b en zo di a ze pi n ,e s ci t a l o pr a m,war f a r i n ,o x y c od on e,t r a ma dol ,d anox y mo r p ho ne k o n s en t r a s i n y ad al a mp l a s maa k a nme ni n gk a t .
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Ob at o ba ty a ngk e r j an y at e r g ant u ngo l e ha sam l a mb ungs ep er t ik e t o k on az ol e ,a t a zan av i r ,d ane st e r amp i c i l l i n ,p en y er a pa nn y aa ka nme nu r uns eh i n gg ame ng ur a ng ie f e kt i v i t a sn y a.
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Sed an gk ano ba t o ba ty a ngl ab i ld al a mk o ndi s ia sa ms ep er t ier y t hr omy c i n,d andi g ox i npen y er a pann y a a k anme ni n gk a t .
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Ob at o ba ty an g di me t a bo l i s meo l e hp r o se so k si d as id id al a mh at is epe r t idi a ze pa m,wa r f ar i n ,d an f e ni t o i ne l i mi n as i n y ad i p er p an j a ng j i k ad i b er i k a ns e c ar ab er s a ma an d en ga no mp r a z ol es e hi n gg a men i ng kat k anef ekf ar mak ol ogi obat obatt er s ebut .
Dosi s omepr az ol e
ome pr a zol ed i be r i k and en ga ndo si ss eba ga ib er i k u t: •
Dosi sl azi m dewasaunt ukt ukakususbesar .
2 0mgo r a ls e k a l i s e h ar i s e b el u m ma k a n.Ke ba n y a k anp as i e ns emb uhd al a m4 8mi n gg u. •
Dos i sl a z i m de wa saunt uki nf e ks iH.py l or i .
Ko mb i n as i d en ga nc l a r i t h r o my c i n:o me pr a z ol e4 0mg1xs eh ar i+c l a r i t h r o my c i n5 00mg3xs eh ar i s e l a ma1 4 ha r i .Pad ah ar i k e1 52 8,ome pr a zol e2 0mg1xs eh ar i .Ob atdi b er i k ans ec ar ao r a l .
Ko mb i n as id en ga nc l a r i t h r o my c i n+a mo x i c i l l i n:o me pr a zo l e2 0mg+c l a r i t h r omy c i n5 00mg++a mo x i c i l l i n 1 00 0mg ,2xs e ha r is e l a ma1 0h ar i .J i k ad i s e r t a ima ag ,t e r u s k anome pr a z ol ed en ga nd os i s20mg1xs e ha r i u nt u k18ha r i k ede pa n. •
Dosi sl az i m dewasaunt ukt ukakl ambungat aumaag
4 0mg1xs e ha r i s e l a ma4 8mi n gg u.Ob atd i b er i k a ns e c a r ao r a ls e b el u m ma k a n. •
Dos i sl a z i m de wa saunt uke r os i fe sof a gi t i s
20mg1xs eh ar i .Da pa tdi t i n gk at k ansamp ai 4 0mg / h ar i .Ob atd i be r i k ans ec ar aor a ls eb el u m ma ka n. Pengobat anbi s adi l ak uk anhi ngga12bul ant er gant unghas i l y angdi per ol ehber das ar k anev al uas i dok t er . •
Dosi sl azi m dewasaunt ukZol l i nger El l i sonSyndr ome
dos i sawa l:6 0mg1xs ehar i .Obatdi ber i k ans ec ar aor al . Pe me l i h ar aa n:8 0mg / ha r i d i ba gi d al a m2 3xdo si s . •
Dosi sl azi m dewasaunt ukgast r oesophagealr efluxdi sease( GERD)
d os i sa wa l:2 0mg1xs e ha r i s e l a ma48mi n gg u.Ob atd i b er i k a ns e c ar aor a ls e be l u m ma k an .Do s i sda pa t di n ai k k ans amp ai 40mg / ha r i . •
Dosi sl azi m dewasaunt ukdi spepsi a
2 0mg1xs e ha r i s e l a ma14ha r i .Ob atd i b er i k a ns e c ar aor a ls e be l u m ma k an . •
Dosi sl az i m
anak
Anak anak ber at
badan
10
k g
unt uk
dan 5 –
k g
er osi fesof agi t i s
Remaj a –
20
10
k g
k g :
116 :
10
5 mg
b er a tb ad an>2 0k g:2 0mg1xs e h ar i . •
Dos i sl a z i ma na kunt uki nf e ks iH.py l or i .
Be r a tb ad an15 3 0k g:1 0mg2xs e ha r i . Be r a tb ad an>3 0k g:2 0mg2xs e h ar i . 1 5s a mp ai 3 0k g :1 0mgdu ak a l i s e ha r i . Le bi hbe sa rd ar i 3 0k g :20mgdu ak al i s eh ar i •
Dosi sl azi m anakunt ukgast r oesophagealr efluxdi sease( GERD) .
mg
t ahun: 1
1
x x
s ehar i . s ehar i .
Be r a tb ad an51 0k g:5mg1xs e ha r i . Be r a tb ad an10 2 0k g:1 0mg1xs e ha r i . Be r a tb ad an>2 0k g:2 0mg1xs e h ar i .
Maj orSi deEffect s I fa nyoft hef ol l owi ngs i dee ffe ct soc curwhi l et a ki ngome pr a z ol e ,c he ckwi t hy ourdoc t or i mme di a t e l y : Rar e •
Bac k ,l eg,ors t omac hpai n
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bl eedi ngorc r us t i ngs or esont hel i ps
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bl i s t er s
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bl oodyorc l oudyur i ne
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c hi l l s
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c ont i nui ngul c er sors or esi nt hemout h
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di ffic ul t ,bur ni ng,orpai nf ul ur i nat i on
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f ev er
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f r equentur get our i nat e
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gener al f eel i ngofdi s comf or tori l l nes s
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j oi ntpai n
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l os sofappet i t e
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muscl eachesorcr amps
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pai n
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r edori r r i t at edey es
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r ednes s,t ender nes s,i t c hi ng,bur ni ng,orpeel i ngoft hes ki n
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s k i nr as hori t c hi ng
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s or et hr oat
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s or es ,ul c er s,orwhi t es pot sont hel i ps ,i nt hemout h,oront hegeni t al s
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unus ual bl eedi ngorbr ui s i ng
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un us u al t i r e dne ssorwe ak nes s
I nci dencenotknown: •
Dr o ws i n es s
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f as t ,r ac i ng,orunev enhear t beat
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moodorment alchanges
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mus c l es pas ms( t et an y)ort wi t c hi ngs ei z ur es
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naus eaorv omi t i ng
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t r embl i ng
I fa nyoft hef ol l owi ngs ympt omsofov er dos eoc curwhi l et a ki ngome pr a z ol e ,ge t emer gencyhel pi mmedi at el y: Sympt omsofover dose: •
Bl ur r edv i s i on
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c onf us i on
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dr y nes soft hemo ut h
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fl us hi ng
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headache
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i nc r eas eds weat i ng
Mi norSi deEffect s So meo me pr a z ol es i d ee ffe c t sma yno tn ee da nyme di c a la t t e nt i o n.Asy o urb od yge t sus e dt o t hemedi c i net hes es i deeff ec t sma ydi s appear .Yourheal t hc ar epr of es s i onal ma ybeabl et ohel p y oupr ev entorr educ et hes es i deeff ec t s ,butdoc hec kwi t ht hem i fanyoft hef ol l owi ngs i de eff ec t sc ont i nue,ori fy ouar ec onc er nedaboutt hem: Lessc ommon: •
Bo dya che sorp ai n
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c hes tpai n
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c ons t i pat i on
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cough
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di ar r heaorl oos es t ool s
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di ffic ul t ywi t hbr eat hi ng
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di z zi nes s
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earc onges t i on
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gas
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hear t bur n
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l os sofv oi c e
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mu sc l epai n
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nas al c onges t i on
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r u nn yno s e
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s nee z i n g
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un us u al dr o ws i ne ss
Obat Generik : Omeprazole
Obat Bermerek : Contral, Dudencer, Inhipump, Lokev, Loklor, Losec, Meisec, Norsec, Omevell, OMZ, Onic, Opm, Oprezol, Ozid, Prilos, Prohibit, Promezol, Protop, Pumpitor, Redusec, Reasec, Rocer, !ocid, !tomacer, "lzol, Zepral, Zollocid#
KOMPOSISI Omeprazole 20 mg : $iap kapsul menandun Omeprazole %& m# Omeprazole 10 mg : $iap kapsul menandun Omeprazole '& m#
FARMAKOLOGI Omeprazole beker(a menhambat sekresi asam lambun denan cara berikatan pada pompa )*+*$Pase -pompa proton. dan menakti/kann0a sehina ter(adi pertukaran ion kalium dan ion h0droen dalam lumen sel# Omeprazole berikatan pada enzim ini secara irreversibel, tetapi reseptor1)% tidak dipenaruhi# !ecara klinis, tidak terdapat e/ek /armakodinamik 0an berarti selain e/ek obat ini terhadap sekresi asam# Pemberian melalui oral dari obat ini menhambat sekresi asam lambun dan stimulasi pentaastrik#
ARA K!R"A : Omeprazol menhambat sekresi asam lambun denan cara berikatan pada pompa ) * + * $Pase dan menakti/kann0a sehina ter(adi pertukaran ion kalium dan ion h0droen dalam lumen sel# Omeprazole berikatan pada enzim ini secara irreversibel, tetapi reseptor1)% tidak dipenaruhi# !ecara klinis, tidak terdapat e/ek /armakodinamik 0an berarti selain e/ek obat ini terhadap sekresi asam# Pemberian melalui oral dari obat ini menhambat basal dan sekresi asam 0an distimulasi oleh pentaastrin#IndikasiOmeprazol diindikasikan untuk penobatan (anka pendek tukak lambun, tukak duodenum dan re2uks eso/aitis3 penobatan sindroma Zolliner1 4llison#
I#$IKASI •
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Penobatan (anka pendek tukak duodenal dan 0an tidak responsi/ terhadap obat1obat antaonis reseptor )%# Penobatan (anka pendek tukak lambun# Penobatan re2uks eso/aitis erosi/ 5 ulserati/ 0an telah didianosa melalui endoskopi# Penobatan (anka lama pada sindroma Zolliner 4llison#
KO#%RAI#$IKASI Omeprazole sebaikn0a tidak diberikan pada penderita hipersensiti/ terhadap omeprazole#
$OSIS $A# A%&RA# PAKAI Dosis 0an dian(urkan %& m atau 6& m, sekali sehari# •
Penderita denan e(ala tukak duodenal 7 lama penobatan memerlukan 8aktu % minu, dan dapat diperpan(an sampai % minu lai#
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Penderita denan e(ala tukak lambun atau re2uks eso/aitis erosi/5ulserati/ 7 lama
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penobatan memerlukan 8aktu 6 mimu, dan dapat diperpan(an sampai 6 minu lai# Penderita 0an sukar disembuhkan denan penobatan lain, diperlukan 6& m sekali sehari# Penderita sindroma Zolliner 4llison dosis a8al %&1'9& m sekali sehari, dosis ini harus
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disesuaikan untuk masin1masin penderita# "ntuk dosis lebih dari :& m sehari, dosis harus •
dibai % kali sehari# +apsul harus ditelan utuh denan air -kapsul tidak dibuka, dikun0ah, atau dihancurkan.# !ebaikn0a diminum sebelum makan#
$OSIS : De8asa7 •
$ukak lambun dan tukak duodenum -termasuk 0an komplikasi terapi IN!., %& m satu kali sehari selama 6 minu pada tukak duodenum atau : minu pada tukak lambun3 pada kasus
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0an berat atau kambuh tinkatkan men(adi 6& m sehari3 Pemeliharaan untuk tukak duodenum 0an kambuh, %& m sehari3 penceahan kambuh tukak
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duodenum, '& m sehari dan tinkatkan sampai %& m sehari bila e(ala muncul kembali# $ukak lambun atau tukak duodenum karena IN! dan erosi astroduodenum, %& m sehari
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selama 6 minu, diikuti 6 minu berikutn0a bila tidak sepenuhn0a sembuh3 Pro;laksis pada pasien denan ri8a0at tukak lambun atau tukak duodenum, lesi astroduodenum, atau e(ala dispepsia karena IN! 0an memerlukan penobatan IN! 0an
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berkesinambunan, %& m sehari# $ukak duodenum karena )# P0lori menunakan reimen eradikasi# !indrom Zolliner 4llison, dosis a8al 9& m sekali sehari3 kisaran lazim %&1'%& m sehari -di
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atas :& m dalam % dosis terbai.# Penuranan asam lambun selama anestesi umum -pro;laksis aspirasi asam., 6& m pada
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sore hari, satu hari sebelum operasi kemudian 6& m %19 (am sebelum operasi# Pen0akit re2uks astroeso/aal, %& m sehari selama 6 minu diikuti 61: minu berikutn0a
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(ika tidak sepenuhn0a sembuh3 6& m sekali sehari telah diberikan selama : minu pada pen0akit re2uks astroeso/aal 0an tidak dapat disembuhkan denan terapi lain3 dosis •
• •
pemeliharaan %& m sekalis sehari# Pen0akit re2uks asam -Penatalaksanaan (an
N+7 •
Neonatus >&& mc5k bb satu kali sehari, ditinkatkan (ika perlu setelah >1'6 hari men(adi ',6
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m5k bb, beberapa neonatus memerlukan hina %,: m5k bb satu kali sehari3 "sia ' bulan ? % tahun7 >&& mc5k bb satu kali sehari, ditinkatkan (ika perlu men(adi @ m5k
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bb -maks# %& m. satu kali sehari3 =erat badan '&1%& k, '& m satu kali sehari ditinkatkan (ika perlu men(adi %& m satu kali
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sehari -pada kasus re2uks eso/aitis ulserati/ 0an parah, maks# '% minu denan dosis lebih tini.3 =erat badan A %& k, %& m satu kali sehari ditinkatkan (ika perlu men(adi 6& m satu kali
• • •
sehari -pada kasus re2uks eso/aitis ulserati/, maks# '% minu denan dosis lebih tini. 4radikasi )#p0lori pada anak -dalam kombinasi denan antibakteri7 "sia '1'% tahun, '1% m5k bb -maks# 6& m. satu kali sehari3 "sia '%1': tahun7 6& m satu kali sehari#
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In(eksi intravena diberikan selama B menit atau melalui in/us intravena3 pro;laksis aspirasi
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asam, 6& m harus telah diberikan seluruhn0a, ' (am sebelum operasi# Re2uks astroeso/aal, tukak duodenum dan tukak lambun, 6& m sekali sehari hina
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pemberian oral dimunkinkan# N+# In(eksi intravena selama B menit atau denan in/us intravena7 "sia ' bulan?'% tahun7 dosis a8al B&& mikroram5k bb -maks# %& m. satu kali sehari, ditinkatkan men(adi % m5k
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bb -maks# 6& m. (ika diperlukan#3 "sia '%1': tahun, 6& m satu kali sehari# !aran7 $elan seluruh kapsul, larutkan tablet dalam air atau campur isi kapsul denan sari buah
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atau 0ohurt# Pemberian pada anak7 Oral, sama denan de8asa#
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4nteral7 =uka kapsul omeprazol, larutkan omeprazol dalam se(umlah air secukupn0a atau dalam '& mL Natrium bikarbonat :,6 -'mmol Na*5mL.# =iarkan selama '& menit sebelum diberikan.# In/us intermiten intravena, encerkan larutan rekonstitusi pada kadar 6&& mikroram5mL denan lukosa B atau natrium klorida &,, berikan selama %&1@& menit#
!F!K SAMPI#G •
Diare, mual, sakit kepala, sembelit dan perut kembun pernah dilaporkan tetapi (aran# Pada
•
se(umlah pasien, ruam kulit munkin ter(adi# 4/ek sampin 0an ter(adi biasan0a rinan# Omeprazole umumn0a dapat ditoleransi denan baik# Pada dosis besar dan penunaan 0an lama, kemunkinan dapat menstimulasi pertumbuhan
•
sel 4CL -enterochromaEn1likecells.# Pada penunaan (anka pan(an perlu diperhatikan adan0a pertumbuhan bakteri 0an berlebihan di saluran pencernaan#
P!RI#GA%A# $A# P!R'A%IA# •
+emunkinan malinansi sebaikn0a dihindarkan sebelum penunaan Omeprazole pada
•
pasien tukak lambun karena dapat menutupi e(ala1e(alan0a dan menhambat dianosis# =elum ada penalaman penunaan Omeprazol untuk anak1anak# Obat ini sebaikn0a tidak diunakan selama kehamilan dan men0usui kecuali meman
•
dianap pentin#
I#%!RAKSI OBA% •
Omeprazol menhambat metabolisme obat1obat 0an dimetabolisme oleh sistem enzim
•
sitokrom P6B& hati dan memperpan(an 8aktu paruh diazepam, 8ar/arin dan /enitoin# Pada 8anita hamil, 8anita men0usui dan anak?anak sebaikn0a dihindari bila penunaann0a dianap tidak cukup pentin#
K!MASA# • •
Omeprazole %& m, boF, @ strip F '& kapsul# Omeprazole '& m#
Epidemiological data do not show an increased risk of major birth defects after maternal use of omeprazole during pregnancy.[20] No clinical trials hae deeply ealuated the potential conse!uences of the use of omeprazole in breastfeeding. "oweer# the pharmacokinetics of omeprazole molecule strongly suggest the safety of omeprazole use during breastfeeding$ •
%meprazole has a high plasma protein binding rate &'()*#[2+] indicating that little amount of drug is transferred to the milk duct during breast milk formation.
•
%meprazole needs to be administrated in an enteric,coated formulation due to its rapid degradation in the acidic conditions of the stomach. -his suggests that most of the free molecules ingested by the infant are likely degraded before being absorbed.[citation needed ]
%meprazole at normal doses is likely safe during breastfeeding lthough the potential for drug interactions is high# clinically important drug interactions are rare.[2/][2] "oweer# the most significant major drug interaction concern is the decreased actiation of clopidogrel when taken together with omeprazole.[2(] lthough still controersial#[21]this may increase the risk of stroke or heart attack in people taking clopidogrel to preent these eents. -he mechanism by which this potential interaction occurs is because omeprazole is an inhibitor of the enzymes 342+' and 34/.[25] lopidogrel is an inactie prodrug that partially depends on 342+' for conersion to its actie form. 6nhibition of 342+' may block the actiation of clopidogrel# which could reduce its effects.[27][2'] lmost all benzodiazepines are metabolised by the 34/ and 34281 pathway# and inhibition of these enzymes results in a higher 9 &i.e. the total effect oer time of a gien dose*. %ther e:amples of drugs dependent on 34/ for their metabolism are escitalopram#[/0] warfarin#[/+] o:ycodone# tramadol# and o:ymorphone. -he concentrations of these drugs may increase if they are used concomitantly with omeprazole.[/2] %meprazole is also a competitie inhibitor of p,glycoprotein# as are other 446s.[//] 8rugs that depend on an acidic stomach enironment &such as ketoconazole or atazanair * may be poorly absorbed# whereas acid,labile antibiotics &such as erythromycin which is a ery strong 34/ inhibitor* may be absorbed to a greater e:tent than normal due to the more alkaline enironment of the stomach.[/2] ;t.
Pharmacology [edit] Pharmacodynamics [edit] Mechanism of action [edit] %meprazole is a selectie and irreersible proton p ump inhibitor. 6t suppresses stomach acid secretion by specific inhibition of the ">?@>,-4ase system found at the secretory surface of gastric parietal cells. Aecause this enzyme system is regarded as the acid &proton# or ">* pump within the gastric mucosa# omeprazole inhibits the final step of acid production.[citation needed ] %meprazole also inhibits both basal a nd stimulated acid secretion irrespectie of the stimulus.[/1] -he inhibitory effect of omeprazole occurs within + hour after oral administration. -he ma:imum effect occurs within 2 hours. -he duration of inhibition is up to 52 hours. Bhen omeprazole is stopped# baseline stomach
acid secretory actiity returns after / to ( days. -he inhibitory effect of omeprazole on acid secretion will plateau after days of repeated daily dosing.[/5]
Pharmacokinetics [edit] -he absorption of omeprazole takes place in the small intestine and is usually completed within / to 1 hours. -he systemic bioaailability of omeprazole after repeated dose is about 10).[citation needed ] %meprazole# as well as other 446s# are only effectie on actie ">?@>,-4ase pumps. -hese pumps are stimulated in the presence of food to aid in digestion. Cor this reason# patients should be adised to take omeprazole with a glass of water on an empty stomach.[/7][/'] dditionally# most sources recommend that after taking omeprazole# at least /0 minutes should be allowed to elapse before eating[0][+] &at least 10 minutes for immediate,release omeprazole plus sodium bicarbonate products# such as Degerid*#[2] though some sources say that with delayed,release forms of omeprazole# waiting before eating after taking the medication is not necessary.[/] %meprazole is completely metabolized by the cytochrome 4(0 system# mainly in the lier. 6dentified metabolites are the sulfone# the sulfide# and hydro:y,omeprazole# which e:ert no s ignificant effect on acid secretion. bout 70) of an orally gien dose is e:creted as metabolites in the urine# and the remainder is found in the feces# primarily originating from bile secretion. [citation needed ]
Chemistry [edit]
&S*,&* and &R *,&>*,enantiomers of omeprazole# aracemate &+$+ mi:ture of both enantiomers*
%meprazole contains a tricoordinated sulfinyl sulfur in a pyramidal structure and therefore can e:ist as either the &S*, or &R *,enantiomers. %meprazole is a racemate# an e!ual mi:ture of the two. 6n the acidic conditions of the canaliculi of parietal cells# both enantiomers are conerted to achiral products &sulfenic acid and sulfenamide configurations* which react with a cysteine group in "> ?@ > -4ase# thereby inhibiting the ability of the parietal cells to produce gastric acid.[citation needed ]
straDeneca has also deeloped esomeprazole &Ne:ium* which is a eutomer # purely the &S*,enantiomer# rather than a racemate like omeprazole. %meprazole undergoes a chiral shift in vivo which conerts the inactie &R *,enantiomer to the actie &S*, enantiomer# doubling the concentration of the actie form.[] -his chiral shift is accomplished by the 342+' isozyme of cytochrome 4(0# which is not found e!ually in all human populations. -hose who do not metabolize the drug effectiely are called Fpoor metabolizersF. -he proportion of the poor metabolizer phenotype aries widely between populations# from 2.0G2.( ) in frican mericans and white mericans to H20) in siansI seeral pharmacogenomics studies hae suggested that 446 treatment should be tailored according to 342+' metabolism status. [(]
Measurement in body fluids [edit] %meprazole may be !uantified in plasma or serum to monitor therapy or to confirm a diagnosis of poisoning in hospitalized patients. 4lasma omeprazole concentrations are usually in a range of 0.2G +.2 mg?l in persons receiing the drug therapeutically by the oral route and +G1 mg?l in ictims of acute oerdose. Enantiomeric chromatographic methods are aailable t o distinguish esomeprazole from racemic omeprazole.[1]
History [edit] %meprazole was first marketed in the 9nited ;tates in +'7' by stra A# now straDeneca# under the brand name Josec. 6n +''0# at the re!uest of the 9.;. Cood and 8rug dministration# the brand name Josec was changed to 4rilosec to aoid confusion with the diuretic Jasi: &furosemide*.[5] -he new name led to confusion between omeprazole &4rilosec* and fluo:etine &4rozac*# an antidepressant.[5] Bhen 4rilosec=s 9.;. patent e:pired in pril 200+# straDeneca introduced esomeprazole &Ne:ium* as a patented replacement drug.[7] Kany companies introduced generics as straDeneca=s patents e:pired worldwide# which are aailable under many brand names.
Dosage forms[edit]
%meprazole +0,mg# from 9@
%meprazole is aailable as tablets and capsules &containing omeprazole or omeprazole magnesium* in strengths of +0# 20# 0# and in some markets 70 mgI and as a powder &omeprazole sodium* for intraenous injection. Kost oral omeprazole preparations are enteric,coated# due to the rapid degradation of the drug in the acidic conditions of the stomach. -his is most commonly achieed by formulating enteric,coated granules within capsules# enteric,coated tablets# and the multiple,unit pellet system &K94;*. ['] n immediate release formulation was approed by the C8 in the 9nited ;tates# which does not re!uire enteric coating.
[(0]
6t is also aailable for use in injectable form &6L* in Europe# but not in the 9.;. -he injection pack is a combination pack consisting of a ial and a separate ampule of reconstituting solution. Each +0,ml clear glass ial contains a white to off,white lyophilised powder consisting of omeprazole sodium 2.1 mg# e!uialent to 0 mg of omeprazole. %meprazole is also aailable as an oral suspension of enteric,coated beads in the 9@ as an unlicensed product. %ral suspensions are predominantly used for children# but can also be used by those with difficulty swallowing or those using a feeding tu be.
M!%OLOPRAMI$! ( I#$&!$ !)%RAP*RAMI+$AL SIG#S A#$ S*MP%OMS ( BRI!F R!,I!- OF LI%!RA%&R! A#$ AS! R!POR%. Mirena Galkova', =o0ko !tamenov', Dora Pe0chinska', Ivanka Geleva%, Pepa Dimitrova%, Pavlina Radeva%# 1) Clinic of Neurology, UMHAT “Dr G. Stranski, !le"en, #ulgaria $) !syc%iatric De&art'ent, Me(ical Uni"ersity !le"en, #ulgaria
"o/rnal o IMAB - Annual Proceeding (Scientifc Papers) 201 3ol. 20 i44/e 5
"o/rnal o IMAB I!!N7 '@'%1>>@H http755888#(ournal1imab1b#or
ABS%RA%: Intro6/7tion: Metoclopramide is a dopamine receptor aonist and 8ell kno8n antiemetic and astrok0netic aent# Its usae has been restricted b0 4uro1pean Medicines enc0 -4M., because o/ acute and chronic neuroloical adverse events# 4Ftrap0ramidal s0n1dromes, includin parkinsonism, tardive d0skinesia, akathisia and acute d0stonias, are the most reported and most o/ten dru side eects# ontingent an6 met8o64: Je present a case o/ %@ 0ears old 8oman 8ith a @10ear histor0 o/ Metoclopramide1induced recurrent oculo0ric crises# Re4/lt4: $he patient suered /rom eFaminophobia, 8ith minimal benzodiazepine s0mptoms relie/# !he 8ill/ull0 took small dosaes o/ oral Metoclopramide /or nausea relie/ be/ore her eFaminations, 8hich lead to recur1rent oculo0ric crises, short a/ter the dru intake# /ter a detailed eFplanation o/ dru side eects and medicine dis1continuation, the0 disappeared# !he had no sini;cant medical and /amil0 histor0 o/ neuroloical and ps0chiat1ric conditions# Laborator0 data 8ere normal# on7l/4ion4: Metoclopramide could induce acute or chronic neuroloical conditions and its usae should be restricted in eneral population to some speci;c conditions# !ome o/ its adverse reactions are o/ten misdianosed and improperl0 treated# Critical dru anamnesis 8ith a /ocus on Metoclopramide usae in some cases could enhance di1anosis# Ke9 or64: Metoclopramide side eects, dopamine antaonist, oculo0ric crises# I#%RO$&%IO#: Metoclopramide is 8ell kno8n antiemetic and astrok0netic aent, used /or treatment o/ nausea, vomit1in, astroparesis, astro1esophaeal re2uF disease and miraine K', %, @, 6# It is a dopamine -D%. receptor an1taonist 8ith short li/e and miFed B)$ @ receptor antao1nist and B)$6 receptor aonist KB, 9, ># lthouh its si1ni;cant eect on nausea and vomitin and 8idel0 usae in practice, on %6 October %&'@ 4uropean Medicines enc0s Committee on Medical Products /or
)uman "se recommended chanes o/ metoclopramide containin medicines use, due to the potential risk o/ serious neuro1loical side eects# K: 4Ftrap0ramidal side eects due to metoclopamide are the most common ones# Reported incidence is approFi1matel0 &#%, but in aed and 0oun patients this incidence increases up to as hih as %B, the risk in children is 9 times hiher than in adults K:, # $he0 ma0 occur earlier a/ter treatment -most o/ten 8ithin the ;rst %61>% hours., but most likel0 a/ter several dosaes K:, , '&# Risk /actors /or serious neuroloical events are hih dosaes, lon treatment period, and treat1ment o/ children or elderl0 patients K:, , '&# $ardive d0s1kinesia and Parkinsonism are enerall0 seen a/ter lon1term use, 8hereas d0stonia and akathisia can occur a/ter a sin1le dose o/ metoclopramide K'&# lthouh the possible reason o/ eFtrap0ramidal side eects presentation is a blockae o/ striatal D% receptor, their eFact mechanism remains unclear K# $he most o/ten t0pes o/ eFtrap0ramidal side eects due to Metoclopramide usae are parkinsonism, tardive d0skinesia, acute d0stonias and akathisia# Metoclopramide1induced parkinsonism is not uncommon, risk /actors are lon1term usae, /emale seF, advanced ae, diabetes mellitus and pol0pharmac0 K'&, ''# $ardive d0skinesia is a s0ndrome characterized b0 persistent, potentiall0 irrevers1ible involuntar0 movements# Metoclopramide tardive d0s1kinesia incidence is likel0 to be '# K'%, '@# Risk /ac1tors are lon term use o/ the medicine, increased ae, /e1male ender, pre1 eFistin abnormal movements, diabetes mellitus, oranic brain d0s/unction and atroph0, ps0chi1 atric disorders, /amil0 histor0 o/ tardive d0skinesia, pol0pramasia K'@# 4arl0 s0ndrome reconition ma0 im1prove the likelihood o/ remission K'63 ho8ever the treat1ment in some cases ma0 be unsuccess/ul# !everal medicines, thouh 8ith variable eects could be used /or the s0mp1toms relie/3 the0 are mantadine, $etrabenazine, =enzo1diazepines -limited results., Melatonin -hih dosaes at lon treatment period could be eective., Gitamine 4 -lim1ited results. K'6# !urical interventions and Deep brain stimulation ma0 be used in treatment resistant cases K'6# Incidence o/ acute d0stonias due to metoclopramide is about &#% 8ith /emale preponderance K'B# $he0 are usuall0 presented as buccolinual, torticollic, oculo0ric and opisthotonic /orms K'B# Risk /actors are unclear, al1thouh parenteral usae and hih dosaes are believed to be more likel0 associated 8ith acute d0stonias K'B# $he mechanism o/ their development remains unclear, but theduration o/ these s0mptoms corresponds to $'5% o/ the dru K'B# Intravenous diphenh0dramine ma0 be used /or d0s1tonia reversion K'B, '9# !ometimes the clinical picture ma0 imitate acute encephalitis or other brain diseases K'B# $he incidence o/ metoclopramide ? induced akathisia is unkno8n, because o/ under reconition, al1thouh it is believed to be about %&1%B K'>, ':# It ma0 present 8ith var0in rades o/ severit0 K'>, ':# =enzodia1zepines, betablockers, Q%1aonists, opioids, and anti1cholinerics ma0 be used /or treatin s0ndrome K'>, ':# O#%I#G!#% A#$ M!%'O$S: Je present a case o/ %@ 0ears old 8oman 8ith Meto1clopramide1induced oculo0ric crises misdianosed as panic attacks# )istor0 o/ disease, eneral, neuroloical and ps0choloical eFaminations, laborator0 data are applied# R!S&L%S: $he patient -%@ 0ears old student. 8as presented at our department 8ith a @1 0ear histor0 o/ uneFplained ocu1lo0ric crises durin some o/ her eFaminations# !he su/1/ered /rom lon term eFaminophobia 8ith anFiet0 and mod1erate autonomic sins, includin nausea and vomitin, tach0cardia and pallor# !mall dosae o/ benzodiazepine -Rivotril. /or acute s0mptom prevention 8as prescribed 8ith minimal eect and she 8ill/ull0 stopped it# t ;rst she complained o/ uneFpected oculo0ric crises 8ith short duration -% minutes., durin her eFamination @ 0ears ao# $his sin troubled her and she visited her outpatient ps01chiatrist, 8ho dianosed severe panic attack and sent her to ps0choloist# Ps0chotherap0 8as not conducted, because o/ patients re/usal# $he same s0ndrome she had man0 times, irreularl0, durin some o/ her eFaminations, ho8ever the s0ndrome 8orsened 8ith ever0 appearance ? the duration and severit0 o/ sins increased and she 8as unable to sit /or her eFams# !he had no s0mptoms bet8een eFaminations, no other sini;cant medical or /amil0 histor0# t ;rst she denied substance abuse and unprescribed medicine usae# Laborator0 data 8ere normal# !he 8as kindl0 asked aain /or usin unprescribed medications o/ all kinds, 8ith a /o1cus on dopamine1aonists# $he patient con/essed that she had taken ' or % tablets -'&1%& m. Metoclopramide be1/ore eFaminations /or nausea suppression# Metoclopramide side eects 8ere eFplained to the patient and the medica1tion 8as discontinued# Proton1pump inhibitor 8as pre1 scribedpre1scribed /or her nausea3 she re/used benzodiapine treatment and ps0chotherap0# $he patient had no more oculo0ric cri1ses a/ter the previousl0 mentioned corrections and she passed her eFams session 8ith success# $IS&SSIO#:
Oculo0ric crisis is an acute d0stonic reaction K'B, characterized b0 proloned involuntar0 up8ard deviation o/ the e0es, 8hich can be associated 8ith some drus us1ae 1 neuroleptics and other dopamine antaonist -includ1in Metoclopramide., carbamazepine, chlorouine, cisplatin, lithium, domperidone, ni/edipine, pemoline, phenc0clidine, etc# or 8ith brain diseases# It could be re1current and triered b0 dierent /actors -includin stress and dru eFposure.# $he s0ndrome is o/ten misdisnosed# In man0 cases it can mimic some neuroloical and ps0chi1atric diseases, particularl0 in cases 8ith short duration and mild severit0, it is underdianosed K'B# Our patient had lon histor0 o/ recurrent acute Metoclopramide1induced oculo0ric crises, misdianosed as panic attacks, 8ith 8ors1 enin o/ sins that lead to severe, althouh short1time /unc1tional disabilities and ps0choloical distress# $he sins occurred earl0 a/ter takin medication and disappeared 8ithout treatment, similarl0 to that noti;ed b0 rumuam K'B# Our patient had other ps0chiatric illness ? eFaminophobia, but no histor0 o/ co1morbid neuroloical and ps0chiatric conditions, no /amil0 histor0 o/ d0skinesia or other neuroloical diseases and no pol0pramasia# $he eFplanation o/ dru1side eects to the patient appeared to be o/ reat importance, because, because she obviousl0 took and stopped medications hersel/, 8ithout visitin ph01sician or readin dru instructions# In this clinical case 8e dianosed the Metoclopramide ? induced adverse dru re1action a/ter a %1 month clear period and no oculo0ric cri1ses durin the 8hole eFams session# $he patient remained under medical observation and accordin to us should un1dero a ps0choloical treatment# O#L&SIO#S: Metoclopramide induces acute or chronic neuroloi1cal side eects and its usae in eneral population should be restricted to some speci;c conditions# !ome o/ its ad1verse reactions are o/ten misdianosed and improperl0 treated# In some cases the thorouh dru histor0 8ith a /o1cus on Metoclopramide usae enhances dianosis# '# Jallenborn S, Telbrich T, =ulst D, =ehrends +, Jallenborn ), Rohrbach , et al# Prevention o/ post1operative nausea and vomitin b0 metoclopramide combined 8ith deF1amethasone7 randomised double blind multicentre trial# #M*. %&&9 u '%3 @@@->
[email protected]@%6# KPubMed KCrossRe/ %# !a0ana , =arshili0a U# Com1parative !tud0 o/ Metoclopramide, Ondansetron, and Tranisetron in Proph0laFis o/ Postoperative Nausea and Gomitin in Patient "nderoin Laparoscopic Cholec0stectom0 "nder Teneral naesthesia# Asian *ournal of !%ar'acy + ife Science# %&'% San1 Mar3%-'.7:>1@# @# !chriever S, =Vhlen M, =roich +# KCurrent state o/ kno8lede and devel1opments in the proph0laFis and acute treatment o/ miraine# Kin Terman #un(esgesun(%eits-lattGesun(%eitsforsc%ung Gesun(%eitssc%ut. %&'6 u3B>-:.7 >61:%# KPubMed KCrossRe/ 6# Mad(unkova !, Maltepe C, Warine D, +oren T# Patterns o/ antiemetic use amon american 8omen 8ith nausea and vomitin o/ prenanc0# /-stet Gynecol. %&'6
Ma03'%@ !uppl '7'BB!# KPubMed KCrossRe/ B# $onini M, Cardura !M, Messoni 4, Rizzi C# $herapeutic Potential o/ Drus 8ith MiFed B)$6 receptor o1nist5B)$@ receptor ntaonist ction in Control o/ 4mesis# !%ar'acological 0esearc%. 'B Ma03@'-B.7%B>1 %9&# KPubMed KCrossRe/ 9# Oermanns !, Rosenthal J# -4ds#. 4nc0clopedia o/ Molecular Pharmacolo0# S&ringer Science + #usiness Me(ia, %nd ed# %&&:, pp# 69'# ># !mith !), CoF LR, !mith =R# Dopamine receptor antaonists# Annals of &alliati"e 'e(icine# %&'% Sul 3'-%.#
:# 4uropean medical aenc0# 4u1ropean Medicines enc0 recom1mends chanes to the use o/ meto1clopramide# %& December %&'@# 4M5 '@%@5%&'6 Corr# ' KPDW # So UU, +im U=, Uan MR, Chan US# 4Ftrap0ramidal side eects a/ter metoclopramide administration in a post1anesthesia care unit ? case re1port# orean * Anest%esiol# %&'% !ep3 9@
[email protected]%>619# KPubMed KCrossRe/ '&# Moos DD, )ansen DS# Metoclopramide and eFtrap0ramidal s0mptoms7 a case report# * !erianest% Nurs. %&&: Oct3%@-B.7%%1# KPubMed KCrossRe/ ''# de Ronde MJ, +inma )S, Munts T# K!evere parkinsonism due to metoclopramide7 the importance o/ earl0 reconition# Krticle in Dutch Ne( Ti2(sc%r Geneesk(. %&'@3 'B>-%9.79&@># KPubMed '%# Rao !, Camilleri M# Revie8 article7 metoclopramide and tardive d0skinesia# Ali'ent !%ar'acol T%er # %&'& San3@'-'.7''1# KPubMed KCrossRe/ '@# !haer D, =utter;eld M, Pamer C, Macke0 C# $ardive D0skinesia and Metoclopramide "se7 4ects o/ Cisapride Market Jithdra8al# * A' !%ar' Assoc 3$445). %&&6 Nov1Dec3 66-9.799'199B# KPubmed '6# Me0er $, =elson $4, Mcllister R# $ardive D0skinesia7 Distressin Dru1Induced Movement Disorder# US !%ar'. %&'6 San3@-'.7 )!'@1)!'9# 'B# rumuam S, Gi(a0alakshmi M# Metoclopramide 1 induced ocu1lo0ric crises presentin as encepha1litis in a 0oun irl# 6n(ian * !%ar'acol. %&'% Mar366-%.7%99?%9># KPubMed KCrossRe/ '9# Jalker M, !amii # Chronic se1vere d0stonia a/ter sinle eFposure to antiemetics# A' * 7'erg Me(# %&&9 San3%6-'.7'%B1># KPubMed KCrossRe/ '># Gan Cool R, Doordui(n S+, !e0naeve C# !evere akathisia as a side eect o/ metoclopramide# !%ar' 8orl( Sci. %&'& Dec3@%-9.7>&619# KPubMed KCrossRe/ ':# Chauhan T, Na0ar P, +ash0ap !# Metoclopramide1induced akathisia# S naesthesiol Clin Pharmacol# %&'% Oct3%:-6.7B6:?B6# KPubMed KCrossRe/
