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Dr. IIT FITRIANINGRUM DEPARTEMEN FARMAKOLOGI OBA T ANTIMIK OBAKTERI

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Dr. IIT FITRIANINGRUM

DEPARTEMEN FARMAKOLOGI

OBAT ANTIMIKOBAKTERI

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Infeksi mikobakteri suit !isembu"kan !ari semua #enis bakteri

Mikobakteri ambat berkemban$%reatif resisten t"!

antibiotik%akti&itas ter$antun$ 'e(atn)a se

membea"Da(at men#a!i !ormant *ti!ak aktif+ s"$ m#! san$at

resisten t"! berba$ai #enis obat

Dibunu" san$at ambat oe" bbr( obat )an$ aktif 

Din!in$ se mikobakteri ka)a akan i(i! )an$ suit!itembus% (ro(orsi )an$ bermakna !i intrase%t!(t!m makrofa$susa" !itembus oe" obat !$n(enetrasi ema"

O&er&ie,

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Men)embu"kan

Men'e$a" kematian

Men'e$a" kekambu"an

Memutuskan rantai (enuaranMen'e$a" ter#a!in)a resistensi kuman t"!

OAT

 TU-UAN PENGOBATAN TB

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 obat ini (ertama

/. Isonia0i!

1. Rifam(in

2.  P)ra0inami!

3.  et"ambuto

4.  stre(tom)'in

Antimikroba !aam (en$obatan Tuber'uosis

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Obat ini ke!ua

/. Amika'in

1. Aminosai')i' a'i!

2. 5a(reom)'in

3. 5i(ro6o7a'in

4. 5ofa0imine

8. 5)'oserine

9. Et"ionami!e

:. Le&o6o7a'in

;. Rifabutin

/<. Rifa(entin

Obat antimikroba !aam(en$obatab Tuber'uosis

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Rejimen Lama pengobatan(dalam bulan)

Isonia0i!%rifam(in%()ra0inami!e

8

Isonia0i!% rifam(in ;

Rifam(in% et"ambuto%()ra0inami!e

8

Rifam(in% et"ambuto /1

Isonia0i!% et"ambuto /:

Lama (en$obatan TB )an$!irekomen!asikan

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Mu!a" arut !aam air

=truktur miri( ()ri!o7ine

=e'ara in &itro% men$"ambat besar basi

tuberke (a!a konsentrasi <%1 m(>mLBakterisi! basi tuberke )an$ se!an$ aktif

berkemban$

Kuran$ efektif utk mea,an #enis mikobakteri

ati(ikaAktif mea,an or$anisme ekstrase !an

intrase

I=ONIA?ID

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 Men$"ambat sintesis !ari mycolic acid yangada pada dinding sel mikobakteri

Mutan resisten se$era terseeksi #ika isonia0i!

!iberikan seba$ai obat tun$$a

MEKANI=ME KER-A

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Isoniazid an$sun$ !isera( !ari sa 'erna

Dosis (er ora 2<< m$*4 m$>k$BB utk anak@anak+

Ber!ifusi 'e(at !aam !ara" ke seuru" 'airantubu" !an #arin$an

Metaboit isonia0i! !an seba$ian ke'i obat!aam bentuk teta( !ikeuarkan meaui urin

Pa!a (asien $a$a $in#a !osisn)a />2@/>1 !ari!osis norma

FARMAKOKINETIK 

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Isonia0i! !iin!ikasikan utk (en'e$a"antuberkuosis (a!a in!i&i!u )an$ kontak erat!en$an kasus tuberkuosis (umoner aktif 

In!i&i!u imunokom(ris *(asien I !an AID==eba$ai (en'e$a"an !ari tuber'uosis aktif

(a!a in!i&i!u )an$ terinfeksi M.tuber'uosis!en$an tes tuberkuin (ositif 

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Reaksi aer$i ruam kuit% !emam #aran$ ter#a!i

 Toksisitas "e(atitis *ke"ian$an nafsu

makan%mua%munta"%ikterus%n)eri kua!ran kananatas+sto( obat

Penin$katan aminotransferase *"in$$a 2@37+ tan(a$e#aa ti!ak (eru (en$"entian obat

Neuro(ati (erifer (a!a (asien !$n !osis ebi" !ari

4m$>k$bb>"ari%(a!a (asien !$n

manutrisi%ako"oisme%DM%AID= !an uremia.Anemia akibat !eCsiensi ()ri!o7ine

Menurunkan metaboisme ("en)toin%s"$ ka!arn)amenin$katefek toksik

Efek =am(in$

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Aktif se'ara in &itro mea,an kokkus $ram !an $ram@% bakteri enterik% mikobakteri !anchlamydia

Pemberian Rifam(in seb$ai obat tun$$amen)eeksi or$anisme@or$anisme resistensitin$$i

 Ti!ak ter!a(at resistensi sian$ !$n

antimikroba ain%ke'uai !$n turunann)a%se(erti rifabutin

Bersifat bakterisi! t"! mikobakteri

Rifam(in !a(at membunu" or$anisme )an$

ta"an t"! b)k #enis obat

RIFAMPIN

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 Disera( !en$an baik se'ara (er ora%!iekskresikan meaui "ati menu#u em(e!u

Resirkuasi t#! !i entero"e(atis km!!iekskresikan !aam #uma" besar sb$metaboit (! feses !an se#uma" ke'i (! urin

Di!istribusikan se'ara uas !aam 'airantubu" !an #arin$an

Pen$ikat (rotein )an$ reatiftin$$i%konsentrasin)a (a!a L5= "an)a bia t#!(era!an$an (! sea(ut otak atau ==.tuan$beakan$

FARMAKOKINETIK 

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Dosis Rifam(in 8<<m$>"ari */< m$>k$bb>"ari+ (erora !iberikan bersama isonia0i!%et"ambuto !an OAT)$ ain utk men$"in!ari resistensi obat

=eba$ai (roCaksis isonia0i!%(a!a (asien1 )an$

ti!ak !(t men$konsumsi isonia0i! seba$ai (roCaksis kontak (a!a anak !en$an

.in6uen0a ti(e B

Kombinasi Rifam(in utk (en$obatan infeksi

=taCo'o''us serius *osteomieitis% en!okar!itis+Kombinasi !en$an 5eftria7one atau &an'om)'in utk

menin$itis o.k (neumo'o''us )$ resisten t"!(enisiin

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arna oran)e )$ ti!ak berba"a)a (a!a

urin%kerin$at%air mata !an ensa kontak

Ruam kuit%trombosito(enia%nefritis

Ikterus"e(atitis

Proteinuria rin$an=in!r.miri( 6u bia (emberian kuran$ !ari 17semin$$u

Men$eiminasi obat ain *men$in!uksi en0immikrosom+ met"a!one%antikoa$uasi%bbr(

antikon&usan%(en$"ambat (rotease%kontrase(siMenurunkan ka!ar serum !ari

ketokona0o%')'os(orine%'"oram("eni'o

EFEK =AMPING

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 sen)a,a sintetis )an$ arut !m air !an ta"an(anas

Pen$"ambat !ari arabinosyl transferasemikobakteri

 Arabynosyl transferase teribat !aam(oimerasi arabino$)'an *kom(onenessensia (! !in!in$ se+

Gan$$uan sintesis arabino$)'anmen$$an$$u (erta"anan se% menin$katkanakti&itas obat1 i(oCik *rifam(in !ano6oksasin+

Disera( !en$an baik meaui usus

ETAMBUTOL

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Akumuasi et"ambuto t#! (! $an$.$in#a%!osis!ikuran$i "in$$a se(aru"n)a *#ika kirenskreatinin /< mL>menit+

Menembus sa,ar otak "an)a #ika sea(ut otakterinfeksi

Resistensi et"ambuto t#! 'e(at #ika !iberikansb$ obat tun$$a

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Dosis (er ora /4@14 m$>k$ !iberikan se'aratun$$a !$n !osis "arian kombinasi isonia0i!atau rifam(in

Dosis )an$ tin$$i untuk (en$obatanmenin$itis tuber'uosa

Dosis et"ambuto 4<m$>k$ utk #a!,a(emberian !osis !ua kai !m semin$$u

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Neuritis retrobuber"ian$n)a ta#am(en$i"atan !an buta ,arna mera"@"i#au

Pemberian !osis "in$$a 14m$>k$ terusmenerus seama berbuan1 berefek (a!ata#am (en$i"atan

Kontrain!ikasi (a!a anak1

EFEK =AMPING

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=e#enis ni'otinami!e%stabi%se!ikit arut !aamair% 'uku( mura"

( netra%ti!ak aktif in &itro% (a!a ( 4%4 !(tmen$"ambat basi tuberke !an bbr( #enismikobakteri

Obat !isera( oe" makrofa$ !an akti&itasn)amea,an or$anisme intraseuer )an$ t!(t

(a!a in$k.asam

PHRA?INAMIDE

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Dosis 14 m$>k$>"ari (er ora

Disera( !ari sauran 'erna !an !i!istribusikanse'ara uas ke #arin$an tubu" termasuksea(ut otak )$ terinfeksi

aktu (aru" :@// #am

Re#imen (en$obatan !osis 4<@9<m$>k$ !uakai semin$$u atau ti$a kai semin$$u

Diberikan bersama1 rifam(in !an isonia0i!sb$ a$en sterii0atorJ aktif utk mea,an sisa@sisa or$anisme intraseuer

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Resistensi t#! san$at 'e(at%t( t!k t#! resistensisian$ !$n antimikobakteri )$ ain

Kombinasi ()ra0inami!e !$n 'i(ro6o7a'inatau o6oksasin utk (en'e$a"an aktif (!kontak erat (en!erita Tb%!an (! kasus Tb)an$ resisten t"! berba$ai ma'am obat

Efek sam(in$ "e(atotoksik %mua%munta"

!emam% "i(erurisemia

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=eba$ian basi@basi tuberke !i"ambat oe"stre(tom)'in

=(esies mikobakteri non tuber'uosissemuan)a resisten ke'uai M.a&ium 'om(e7*MA5+ !an M)'oba'terium kansasii

=uit menembus ke !aam se%s"$ "n)a aktifutk mea,an basi tuberke ekstraseuer

Menembus sa,ar otak !an men'a(ai !osistera(eutik (!a ra!an$ sea(ut otak

=TREPTOMH5IN

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Dosis /4m$>k$>"ari s'r i.m atau i.& setia("ari utk !e,asa% anak1 1<@3< m$>k$>"ariti!ak ebi" !ari /@/%4 $ utk bbr( min$$u

Obat@obat ain !iberikan s'r simutan utkmen'e$a" resistensi

Efek sam(in$ ototoksik !annefrotoksik%&erti$o.

Dosis !isesuaikan !$n fun$si $in#aEfek toksik !(t !ikuran$i #ika (en$$unaan

ti!ak ebi" !ari 8 bn

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Ber"ubun$an !en$an isonoa0i! men$"ambat mycolicacid

=uit arut !aam air % !imetaboisme !i "ati

=eba$ian besar basi tuberke !i"ambat se'ara in &itro

Dosis a,a 14< m$ sekai se"ari !$n tia( kenaikan14< m$ !osis )an$ !irekomen!asikan /$>"ari*/4m$>k$>"ari+ #aran$ !(t !itoeransi

Men)ebabkan iritasi )an$ serius (a!a ambun$ !an

$e#aa neuroo$ise(atotoksik

 T#! resistensi sian$ antara isonia0i! !an et"ionami!e

ETIONAMIDE

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Antibiotik (e(ti!a (en$"ambat sintesis(rotein !i"asikan !ari Streptomycescapreolus

=e'ara in &itro men$"ambat ban)akmikobakteri tmasuk M.tuber'uosis

=train M.tuber'uosis )an$ resisten t"!=tre(tom)'in atau amika'in%rentan t"!

5a(reom)'inBersifat nefretoksik !an ototoksik

*tinitus%tui%$an$.&estibuer+

Dosis sama !$n stre(tom)'in

5a(reom)'in

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Pen$"ambat sintesis !in!in$ se

Men$"ambat berba$ai strain M.tuber'uosis

Dosis utk Tb <%4@/ $>"ari !iba$i !m 1 !osis

Diekskresikan !i $in#a% !osis !ikuran$i #ikakirens kreatinin 4< mL>menit

Neuro(ati (erifer !an !isfun$si sistem (usat*!e(resi%$e#aa (sikosis+

Diberikan bersama !$n ()ri!o7ine /4<m$>"ari

5)'oserin

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='r in &itro men$"ambat basi tuberke

Mu!a" !isera( sauran 'erna

Dosis :@/1 $>"ari (.o *!e,asa+% 2<<

m$>k$>"ari *anak1+Di!istribusikan ke #arin$an !an 'airan

tubu"%ke'uai L5=

Diekskresikan !i urin%konsentrasi tin$$i

menimbukam kristauriaEfek sam(in$ (a!a GI

e(atotoksik #ika !iberikan 2@: min$$u

AMINO=ALI5HLI5 A5ID *PA=+

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WHO 1R99?9=9 > 3R99*=9 ATAU E9+ 3R22

9 9E9

99T9DEPKES  1R99E9?9> 3R22

PULMONOLOG 1R99E9?9 > 3R99

3R22

99E9

/=T 5ATEGORH

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WHO  1R99E9?9=9 > /R99?9E9

4R99E9 ATAU

4R22F2 *FULLH =UPERI=ED+

DEPKES 1R99E9?9=9 > /R99E9?9

> 4R22E2

PULMONOLOG 1R99E9?9=9>/R99E9?9>

8R99E9 ATAU

8R22E2

1ND 5ATEGORH

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WHO   @ 1R99?9>1R99@ 1R22?2>1R22

  8929

DEPKES   @ 1R99?9>3R22

PULMONOLOG  @ 1R99?9>3R99

@ 1R22?2>3R22

!HRON"! #$ IN FOR LIFE

2RD 5ATEGORH

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#%an& 'ou