Farmakologi

Chloramphenicol Spiramycin
Ciprofloxacin
Garamycin Doxycyclin Amikacin
Streptomycin

Tigecyclin Amoxicillin
Tetracyclin Cephalosporin Thiamphenicol

Cloxacillin Azithromycin Colistin

Rifampicin Clindamycin Ampicillin

Antibiotik

Hamzah.dr Sp.FK
 Antibiotik
Obat/bahan yg dapat
membunuh kuman
Yg dihasilkan oleh
mikroba / jamur

sintetik
 KU
Host

Gejala infeksi
 KU
Host

Ku Antibiotika

Gejala infeksi
 Antibiotik

Sawar darah otak

Kapsul sendi
Mata
Dinding abses

Kuman

Antibiotik : - Absorpsi GI tract <<<

- Konsentrasi >>>>>>> (Tract UG )
 manusia
kinetik
Bayi/dws/tua
Pria/ wanita
utama

Antibiotik Penyakit infeksi efek

Hamil
Gg ren /hpr
samping
dinamik
farmakologi klinik
 berjasa

Obat Sembuh

berdosa
Prinsip pemberian antibiotik :

1. Pastikan diagnosa ok Infeksi ( panas blm tentu ok kuman )

2. Infeksi serius ..... .pemeriksaan culture
3. Bila dilakukan culture,
sambil menunggu hasil , beri  Antibiotik empirical
4. pemilihan Antibiotik yg rasional
- Kuman
- Host
5. Monitoring keberhasilan terapi  culture
6. Kombinasi antibiotik
- infeksi campuran
- Synergis
- Penyebab tidak tahu
- Mencegah resistensi
7. Prophylactic ( Pre/post Op , Endocarditis )
 Klasifikasi :
Struktur Spektrum Titik tangkap
kimia kerja
* Penicillin * Broad * Dinding sel
* Cephalosporin * Narrow
*Tetracyclin
* Membran sel
*Chloramphenicol
* Macrolid
* Aminoglycoside * Sintesa protein
* Quinolon
* Asam nukleat
Titik tangkap kerja :
Dinding Membrane Sintesa Asam
sel sel protein nukeat
Peinicilin Colistin Chloramphenicol Rifampicin
Tetracyclin
Cephalosporin Polimixin-B
Carbapenam Quinolon
Monobactam Macrolide
Fosfomycin Ketolide
Aztreonam Azol
Meropenam
Lincomycin
Ertapenam
Vancomycin
Streptogramin Co-
Bacitracin Oxazoladinone trimoxazol
Cycloserin Aminoglycosid
 Antibiotik penghambat sintesa dinding sel
Penicillin Cephalosporin miscellaneous

Narrow spectrum Broad Extend Narrow Broad Carbapenam

spect ed Spect spectrum spectrum - Imipenam
- Meropenam
Monobactam
Penicilin Penicilina Ampi Carbeni 1st gene 2nd ,
ase se cilin, - Aztreonam
3nd
suscep resistant Amox 4th
tible Pipera Fosfomycin
cilin Gene
* Methi Ertapenam
Penicil G
cillin Vancomycin
Mezlo
Penicil V * Nafcillin cillin, Bacitracin
* Iso Cycloserin
Xazolyl Azlocillin
Pen
 Bacterial protein synthesis inhibitors
( A-B menghambat sintesa protein )
Broad Moderate Narrow
spectrum spectrum spectrum

Chlor Tera Macro Ketolid Linco Strepto Oxazo Amino

amphe cyclin lide samide gramin ladino glycocide
nicol ne

(Line
zolid)
 Hepatotoksik
>>> < t½ >>
Tetracyclin Penicilin Chloramphenicol
Erythromycin Cephalosporin Rifampicin
Lincomycin
As-Nalidixin
Sulfonamid
Nitrofurantoin
 Nefrotoksik
>> <<<< / -
Aminoglycoside Chloramphenicol
Polymixin Chlortetracyclin
Colistin Doxycyclin
Minocyclin
Cephaloridin
Rifampicin
Cephalotin
Lincomycin
As-Nalidixin
Sulfonamide
 Kadar di CSF
Inflamasi
Pen / Ceph - +
Tetracyclin -
Chloramphenicol +
Aminoglycoside << <
Macrolide -
Quinulon <
Clindamycin -
Rifampicin +
 Antibiotik
Hepatotoksik Nephrotoksik CSF ( + )
Tetracyclin Aminoglycoside Chloramphenicol
Erythromycin Polymixin Rifampicin
Colistin
Cephaloridin Itis ( + )
Cephalotin Pen / Ceph
Bacterosid Bacteriostatik

Penicilin Tetracyclin
Dosis >>
Cephalosporin Chloramphenicol
Gentamicin Erythromycin
Rifampicin Lincomycin Bac-sid
Polymycin Sulfonamide
Bacitracin
Streptomycin
Tx Antibiotika kombinasi

Sinergis ………Bac-sid + bac-sid

Aditif ………… bac-statik + bac-statik

Antagonis…… bac-sid + bac-statik

Resistensi

AB

Ku Ku Natural drug resisten

Aquired
Transferred/
Ku resisten “infectious”
*Transformation
*Transduction
*Conjugation
Cross resisten :
Struktur kimia
sama : der Tetracyclin
Polymyxin B ~ Colistin
Neomycin ~ Kanamycin
tak sama : Erythromycin ~ Clindamycin / Lincomycin

Reaksi yg merugikan :
*Superinfeksi ( broad > narrow )
*Hipersensitifitas ( allergi )
Perlu diketahui pengobatan dengan Antibiotik

sama dengan obat lain

……………………………………………………………..

Ada istilah MIC
( Minimum Inhibitory Consentration )
 Contoh-contoh Antibiotika:
Dinding Membrane Sintesa Asam
Sel sel protein nukeat
Peinicilin Colistin Chloramphenicol Rifampicin

Cephalosporin Polimixin-B Tetracyclin F-Quinolon

Macrolide Azol
( Metronidazole )

Clindamycin
Co-
trimoxazol
Aminoglycosid
Titik tangkap kerja Antibiotik :
Dinding Membrane Sintesa Asam
sel sel protein nukeat
Peinicilin
Cephalosporin
Carbapenam
Monobactam
Fosfomycin
Aztreonam
Meropenam
Ertapenam
Vancomycin
Bacitracin
Cycloserin
Penicillin
Penicillin
*Alami : jamur Penicilinum Notatum/ Chrysogenum
*Semi sintetik
*Sintetik : rumus bangun : 6-Aminopenicillanic acid

amidase S

C C C

C N C
-lactamase / penicilinase
Kuman-kuman yg sudah membentuk -lactamase

Staphylococcus

H. Influenzae

N. Gonococcus Beta-lactamase

E. Colli (Penicillinase)

????????
Penicillin

Farmakokinetik :
Abs : Pe cepat / Po bervariasi
Dist : seluruh jar tb ( serum ~ jar )
kadar (<) mata, prostat, CNS
( kec. Inflamasi ….. Meningitis )
Eks : * urine ( >> ) : 90 % sekrs tubulus
10 % filtrasi glomerulus
* sputum / ASI
Penicillin

Farmakokinetik :
Probenicid dapat menghambat sekresi Penicillin
di tubulus

t½ Penicillin >>
Organic acid lain : Aspirin, Phenylbutazone,

sulfonamide Indomethacin, thiazide,

furosemid, etacrynic acid
Penicilin
Generic name spectrum PO Pen-ase Res
1.Pen-G GR+>> - -
2. Pen-V Idem+GR-< + -
3. Methicilin Idem - +
4. Nafcillin idem - +
5. Isoxazolyl –
Penicilin
Oxacillin Idem + +
Cloxacillin Idem + +
Dicloxacillin Idem + +
Flucloxacillin idem + +
Penicillin
Generic name spectrum PO Pen-ase Res
6. Ampicillin GR-/+ (BS) + -
7. Amoxycillin Idem + -
- -
8. Carbenicillin GR- >
Carbenicillin- + -
indanyl Idem - -
9. Ticarcillin Idem - -
10.Piperacillin idem
 Penicillin
Narrow spectum Broad Extended
spectrum Spectrum
Generasi- 1 : Generasi- 2 : Generasi- 3 :
Penicillin G , Ampicillin , Carbenicilin, Piperacillin
Penicillin V
Amoxicillin, Generasi- 4 :
Antistapylococal :
Methicillin, Nafcillin, Bacampicillin Mezlocillin, Azlocillin
Isoxazolyl penicilin:
oxacillin,
cloxacillin,
dicloxacillin
Kuman yg sensitif: Penicillin
Narrow spectum Broad Extended
spectrum Spectrum
Generasi- 1 Genenerasi- 2 : Generasi- 3
- Strptococc,
- bacteria G + / - - inf serius trct resp /
Staphylococc UG
- G + coccos - Bacteremia
- Neisseria, E coli
ok pseudomonas,
- Spirochetes -bacillus proteus
- anaerob anaerobic

Antistaphylococal : - Spirochates
Generasi- 4
-Staphylococc yg - most inf serius

resisten
Kuman-kuman yg sudah membentuk -lactamase

Staphylococcus

H. Influenzae

N. Gonococcus Beta-lactamase

E. Colli (Penicillinase)

????????
Beta-lactamase inhibitor:
Clavulanic acid Sulbactam / Tazobactam
( penicillinic acid sulfon )
Streptomyces semi sintetik
clavigerus ( inti pen )
cara kerja
Mengikat beta-lactamase
( anti bacteria <<< )
+ Amoxycillin + Ampicillin
( Augmentin ) ( Unasyn )
Penicillin

Klinis:
* First choice drug  bac meningitis,
inf bone, joints, skin, soft tisssue,
throat, bronchi, tr UG.
* Gonorrhoea, syphilis
( banyak kuman yg sudah resistens
al : Staphycc )
* Pemberian bersama pil KB....KB ↓
Cephalosporine
Cephalosporin
Jamur Cephalosporium acremonium semi sintetik
Cara kerja / struktur kimia ~ Pen
rumus bangun : 7 aminocephalosporanic acid

amidase S ( relatif tahan pen-ase )

Cross alergy ~ Pen

C C C
( Jarang 10-20 % )
 Kinetik ~ Pen
C N C
-lactamase
C
Kuman Cephalosporin

Genersi
I II III IV
Terutama pd Plus > Kuman >>
Kuman Kuman Gram (- ) Kuman
gram (+) gram ( - ) Gram (- )
< Kuuman
Gram ( + )
Cephalosporin

Genersi
I II III IV
Cefadroxil Cefuroxim Cefotaxime Cefipim

Cefazolin Cefaclor Ceftriaxone

Cefradin Cefoxitin Ceftazidime

Cefalexin Cefotetan
use Cephalosporin

Genersi
I II III IV
-Streptococc = gen I -Streptococc -Inf trct
-Staphylococc Plus / Peumococc urinary
-Inf urinary trct - H.Influenza, ( << ) -inf trct
-Inf bone / joint - N Gonorrhae Resp
-inf upper Resp -Gram ( - )
trct GI / UG ( Infeksi
( >>> ) serius )
Klinis : (cephalosporin)
* Bacteriemia ( + aminolgycosida )
* Surgical prophylaxis ( Pre / post OP )
* Mixed infection ( + anaerobes )
* Pen-ase producing N.gonorrhae
* Bac- gram (- )
Reaksi yg merugukan :
* Pemberian Po.. N / V / D , IM …iritasi/pain
IV… thromboplibitis
*Allergy
* Hipoprothrombinemia
 Antibiotik
penghambat sintesa protein
Titik tangkap kerja Antibiotik :
Dinding Membrane Sintesa Asam
sel sel protein nukeat
Chloramphenicol
Tetracyclin

Macrolide
Ketolide

Lincomycin
Streptogramin
Oxazoladinone
Aminoglycosid
 Bacterial protein synthesis inhibitors
( A-B menghambat sintesa protein )
Broad Moderate Narrow
spectrum spectrum spectrum

Chlor Tera Macro Ketolid Linco Strepto Oxazo Amino

amphe cyclin lide samide gramin ladino glycocide
nicol ne

(Line
zolid)
Subclass Prototype Other agents

Chloramphenicol Chloramphenicol

Tetracyclin Tetracyclin Demeclocyclin, Doxycyclin,

Minocyclin, Tigecyclin

Macrolid Erythromycin Clarithromycin, Azithromycin

Ketolid Telithromycin

Lincosamide Lincomycin Clindamycin

Streptogramin Quinupristin-
Dalfopristin

Oxazoladinone Linezolid

Aminoglycosides
- Systemic Gentamicin Amikacin,Netilmicin,
Tobramycin,Streptomycin
- Local Neomycin Gentamicin,Kanamycin
- Aminocyclitol Spectinomycin
Chloramphenicol
Chloramphenicol
- Sintetik
- Menghambat Sintesa protein
- Broad spct ~ Tetra
( H.influenzae, Neisseria meningitis,
Strptococc pneumonia, Salmonella )
Penggunaan jarang ? ( systemic infection )
Depressi bone marrow

Agranulocytosis
Chloramphenicol
 glucoronyl transferase ( hepar )
Chloramphenicol
glucoronide
new borne (-) ( hepar <<< )
t-tbh < , muntah
Chloramphenicol >>>> Kulit kelabu
( Gray - sindrom ) Circulatory failure
Shock… mati
Klinis :
* Second line utk meningitis/brain abscess (cephalosporine )
* Haemophillus epiglotis anak
* Inf salmonella (typhoid fever, salmonella septicemia )
* salep mata
* Hamil / ASI ?
Drug interaction :
* Chloramphenicol menghambat metb obat lain
( phenytoin, tolbutamid, warfarin )
* Pemberian bersama Phenobarbital, Rifampicin
 memperpendek waktu paruh Chloramphenicol.
Cytochrom 450 ( dihasilkan di microsomal hati )
komponen utama enzym yg berperan pada
proses oksidasi.

Induksi inhibisi
-Rifampisin - Cemitidin
-Carbamazepin - Erythromicin
-Phenobarbital - Ciprofloxacin
-Phenytoin - Chloramphenicol
( > 1 minggu ) ( beberapa hari )
Thiamphenicol
~ Chloramphenicol
( - NO2 diganti –CH2So2 ( sulfomethyl ) )
Anti bac < ( kec :Bordetella pertusis /
Shigella sonnei )
Depresi bone marrow <<
Klinis : - Bronchitis - GO
- inf sal empedu
- salmonella ( Typh – ParaTyph )
Tetracyclin
Tetracyclin :
* Tetracyclin * Doxycyclin
* Oxyteteracyclin * Minocyclin
* Tigecycline (iv)
Basa sukar larut air ( bentuk garam mudah larut )
Stabil pH asam
Cara kerja : - Menghambat Sintesa protein
- Bacteriostatik
Broad spct : G +/- , Ricketsia, protozoa, Chlamydia
F.Kinetik :
Abs : Po tak lengkap
Chelasi dg ion Ca , Mg , Al
membentuk ikatan komplek : - tak larut
- sukar di abs
Makanan mengurangi abs ( kec : Doxy / Mino )
Dist : seluruh jar
Doxy / Mino : lipid sol >>
Oxytetra : lipid sol <<
Disimpan di tulang / gigi ( gigi coklat ) ( < 8-9 th )
Menembus sawar uri … discoloration gigi
Eks : Ren ( >>> )
Bile ( < )
Doxycyclin : eks bile >>>
( renal failure  akumulasi (-) )
 Use:

1. Inf Mycoplasma-pneumoniae , Chlamydia,

Rikettsia, Vibro species
2. Alternative drug Syphilis, inf tract resp,
prophylaxis inf chronis bronchitis, Eptospirosis, Acne.
3. Selective ulcus ok Helibacter pylori (tetracyclin ),
prevensi Malaria (Doxycyclin ), pengobatan amebiasis
4. Hamil / ASI ?

5. Tigecyclin ( der Minocyclin ) → ?

Tigecyclin ( der Minocyclin )
- Bacteriostatik, broad spectrum (iv)
 efektif pd ku yg sudah resisten Tetra, Methicillin,
Vancomycin, ku yg produksi betalactamase,
Efektif :
Kuman : streptococc, staphylococc, coliform (proteus -),
chlamydia , mycobacteria , Anaerob
Pd kelainan hepar dosis < ( tidak pada kel Ren )
Use : skin, soft tissue, intra abdominal infection
Efek samping = Tetra
ES : ( tetracyclin )
* Iritasi lambung ( > Oxytetra )
* Superinfeksi
* Hepatotoksik ( < Oxy / Tetra )
* Discoloration gigi / pertumbuhan tl ( < Oxy / Doxy )
* Antianabolik
* Photosensitif ( Demeclocyclin )
* Vistibular  dizziness/vertigo(reversble): doxy/mono
* waktu perdarahan >>
* Renal tubular acidosis “Fanconi syndrom” ( tetra kadaluarsa )
Macrolide
Macrolide :
* Erythromycin

* Spiramycin
*Roksitromycin
*Claritomycin
*Azithromycin
Erythomycin
( dari streptomyces erythreus)
- menghambat sintesa protein
- Bacteriostatik…side (~ dosis )
Spectrum :
- Gram + cocci - Spirochetes
- Neisseriae - Ent-histolityca
- Coryn- diphteriae - Mycopl-pneumoniae
- H. influenzae - Virus besar
Resistensi antar Macrolide
Klinis :
*inf Upper resp *Diphteri carrier
*G (+) Pen-resisten
*lues Pen allargy *Acne
ES :
Po: N / V/ D /
Glositis / Stomatitis / super infeksi
Spiramycin (Rovamycin )

Cara kerja ~ Erythromycin

Spectrum : gram + / -
clamydia trachomatis
Toxoplasma gondii
Cryptosporidum muris ( AIDS )
F-kinetik :
Abs : po baik
Dist  bronchus/saliva, prostat, muscle.
Eks : - urine
- bile
t ½ : 4 -8 jam
ES : GI tract  N / V / mulut kering
skin rash / asma / colitis
Klinis : Inf staphylococc / streptococc / pneumococc
GO ( resisten )
Toxoplasmosis
Trachoma
Roksitromycin ~ Erythromycin
* iritasi lambung <<
* kadar jar >
* t½ 10 jam ( 2dd )

Azithromycin  t½ >> ( 1dd 500 mg )

Azithromycin
Efektif terhadap gram (-) H influenza,
N gonorrhae , chlamydia
Terhadap G (+) << dp Erythromicin
Const di jaringan >> plasma (t½ =50 h )
( pemberian 1dd )
Use : inf trct Resp, soft tissue ,
trct UG (chlamydia )
Efek samping terhadap GI tract << erythromicin
Ketolid
Telithromycin ( stuktur ketolid ~ Macrolid )
- Cara kerja / specrtum ~ Erythromycin
( sensitif pada kuman yg sudah resisten thdp Macrolid
ok terikat kuat pada ribosome )
- Pemberian oral once daily
- Eliminasi bile dan urine
- Penggunaan terbatas ok efek sampingnya
Hepatotoksik, gangg penglihatan
 Lincosamide
( Lincomycin / Clindamycin )
Lincomycin / Clindamycin

larut air
acid stable
bacterioside
toksisitas : liver damage / CV collaps

Digeser Clindamycin :
- Potensi >, Toksisitas << , cross resistensi +
Clindamycin
Menghambat sintesa protein
Spectrum = - erythromicin ( partial cross resisten Erythromicin )
= benzylpenicillin
- Anaerobes ( bacteroides fragilis )
Abs per os
Metb hepar ....entrohepatic cycle ( bile const 2-5 x plasma )
Use : staphylococc bone / joint infection, dental infection
Second choice Toxoplasmosis
Infecsi kulit ( G + ) , Acne,
Non-sexuallay transmitted inf women
Efek samping: GI tract N,V, D
Streptogramin
Quinopristin-dalfopristin
* Kombinasi dari 2- Streptogramin
* Bacteriocid
* Efektif thdp kuman yg sudah resisten penicillin,
methicillin, vancomycin
* Pemberian iv
* ( menyebabkan arthralgia-myalgia sindrom )
* Streptogramin adalah inhibitor CYP3A4
Menyebabkan kadar bbp obat meningkat
( astemizole, cisaprid, ciclosporin, diazepam, warfarin )
Oxazoladinone
Linezolid ( Zyvox )
- Antibiotik pertama dari oxazolidinone
- Menghambat sintesa protein
- Efektif thdp ku yg sudah resisten (gram +) cocci
( penicillin, vancomycin)
- Pemberian peroral / parentral
- Metabolisme mel hepar
- Eliminasi half life 4 -6 jam
- Efek samping throbositopenia , neutropenia
Aminoglycosida
Subclass Prototype Other agents

Aminoglycosides
- Systemic Gentamicin Amikacin,
Netilmicin,
Tobramycin
Streptomycin

- Local Neomycin Gentamicin,

Kanamycin
Aminocyclitol Spectinomycin

- Spectinomycin ( im,single dose ) GO ( yg allergi betalactam )

Aminoglycosida
Streptomycin
Neomycin Abs : Po <<<
Kanamycin : Ik-protein <
( Amikasin / Dibikasin) Eliminasi di glo
Tobramycin Tox: -Ototoksik
Garamicin -Nephrotoksik
Netilmicin -Curare like
Spectinomycin -Skin reaction
 Farmakokinetik :
* Poorly lipid soluble ( parentral )
* Unable to enter the CNS
* Not metabolised
* Excreted unchanged by the kidney
Clinical uses: ( Aminoglycoside )
* Terutama gram (-) ( garamicin, tobramycin, amikacin )
* Sering dikombinasi dg beta-lactam antibiotik (penicillin )
 untuk inf ku gram (+ )
* Streptomycin + Penicillin  entrococcal carditis
* Mycobac-tbc resisten Streptomycin ( penggantinya Amikacin )
* Neomycin, kanamycin  topical dan oral
* Spectinomycin ( der – Aminocyclitol)
- Single dose ( im ) → Gonorrhea ( alergi beta lactam )
* Hamil / ASI ?
Garamicin ( Gentamicin )
Abs : Po <<
Eks : …glo ( bentuk tak berubah )
renal failure .. Akumulasi obat
ES : gg keseimbangan / pendengaran
* keseimbangan  garamcin, tobramycin
* pendengaran  amikacin, kanamycin
Tak dianjurkan ibu hamil / neonatus ( ? )
Klinis : sistemik ( Gram - )
topikal : kulit ( luka bakar) , salep mata
Resistensi Aminoglycosida
- Terutama pada ku gram negatif
- gram postif streptococc ( s-pneumoniae ), entrococci

* resisten thdp Garamicin dan Aminogylosida lain


Ok membentuk enzym transferases
 Inactivasi Amikacin, garamicin, tobramycin
( tidak pada streptomycin )
Netilmicin kurang sensitif thdp transferase
Titik tangkap kerja Antibiotik :
Dinding Membrane Sintesa Asam
sel sel protein nukeat
Colistin

Polimixin-B
Polymyxin
Polymyxin A / B / C / D / E / M

colistin
Bacterioside  G (-)
Inf trct UG / telinga / kulit
Use  Topikal ( aman ) , ( + neomycin + corticostroid )
sistemik (gg Ren / CNS)
Potensiasi dg obat neuro-muscl paralysis
 kelemahan otot
Lysis mast sel  histamin
Colistin
Spectrum / cara kerja ~ Polymyxin-B
Potensi <
Abs Po : < 5 th (+) , dewasa (-)
Menembus placenta barrier
ES ~ Polymyxin-B
CI : myasthenia gravis
Use : - GI tract ( E.colli yg resisten neomycin )
Titik tangkap kerja Antibiotik :
Dinding Membrane Sintesa Asam
Sel sel protein nukeat
Rifampicin

Quinolon

Azol

Co-
trimoxazol
Rifampicin
Rifampicin
* Semi sintetik
* Broad spct : gram (+) cocci
gram (-) bacilli
Tuberculosa / lepra
* ES : GI  Nausea / vomiting
Hepar ( terutama kel - hepar )
* Enzym inducer
* Use : TBC / Lepra
pseudomembrane colitis
Quinolon
Quinolon / Fluroquinolon
Generasi I Generasi II Generasi III
Nalidixic acid* Norfloxacin . Moxifloxacin .
Gemifloxacin
Pipemidic acid* Ciprofloxacin
Ofloxacin . Getifloxacin
Cinoxin Pefloxacin . (?)
Sparfloxacin.
Levofloxacin .
quinolon

Cara kerja :

Menghambat DNA girase

( enzym supercoiling DNA )
Spektrum :

Quinolons  Gram (-) ( trct UG )

Fluoroquinolons  Gram (-) >>
GO / Chlamydia
Staphylococc
Pseudomonas A
F. Kinetik :
Abs : Po ( 50 – 90 % )

Dist : luas  const Ren / Pulmo > serum

CSF < serum

Sekrs : ren : F-quinolon

non renal : Quinolon + Pefloxacin
Pada Hepatic failure dapat diberi : F-quinolon
( kec. Pefloxacin )
Kinetik per oral

* Nalidixic acid + ( t ½ = 6 jam )

* Norfloxacin ++ ( t ½ = 3 jam )

* Ciprofloxacin ++ ( t ½ = 3 jam )

* Ofloxacin ++ ( t ½ = 4 jam )

* Sparfloxacin ++
* Levofloxacin ++ ( t ½ = 7 jam )

* Pefloxacin +++
* Moxifloxacin ++ / entral ( t ½ = 10 jam )

* Gemifloxacin ++ / entral
* Getifloxacin. ( ? ) ++ / entral
 Quinolon
(Asam Nalidiksat ) Abs per oral ( cepat )
Ekskresi ( cepat ) → ren

( jadi tak manfaat utk infeksi sistemik )

Norfloxacin ~ asam Nalidiksat

- kadar urin tinggi ,
- kadar serum rendah
( tidak berguna utk infeksi diluar sal kemih )
Klinis :( f-quinolon )-
• Infeksi : * saluran kemih ( cipro / nor / of )
* saluran cerna ( cipro / of / pe )
* saluran napas ( ciporo / of / levo / moxi /
gemi / gati ? )

* tulang- sendi ( cipro )

* kulit - jar lunak ( cipro ? )

* ok sexual ( cipro / levo )
Klinis Cipr Of levo Nor Pe Moxi Gemi Gati
( itis )
UG + + +

GI + + + (?) +

Resp + + + + + +

Tl-snd +

Sk- st +
Sexual + +
Klinis :( f-quinolon )

*Complicated urinary tract infection

* Gonorrhae
* Cervisitis
* Prostatitis
* Typhoid fever
* Septicemia ( thdp ku yg sensitive )
* Resp tract infection( bukan ok pneumococci )
Adversed reaction : ( f-quinolon )
- Gangg GI tarct
- Skin rashes
- Joint pains
- Allergy
- Menghambat ikatan GABA dg reseptornya
 convulsi
- Gangg pertumbuhan tulang / cartilage
( ibu hamil / anak masa pertumbuhan (-) )
 Azoles
1.Metronidazole Antibacteria /
Tinidazole Antiprotozoa
2.Fluconazole Anti fungal
Itraconazole
Clotrimazole
Econazole
Ketokonazole
Miconazole
3. Albendazole Anthelminthic
Mebendazole
Thiabendazole
Metronidazole : bacterostatik
- Utk ku anaerob
-Direduksi gug nitronya menjadi bentuk aktif →
berikatan DNA pembentukan nucleic acid <<<

Kinetik : Abs oral / rectal baik

Utk inf liver, usus, jar pelvic
Wkt paroh 8 jam
Clinic
-Sepsis ok ku anaerob ( bacteroides ,anaerob cocci )
-Colitis pseudomembrane
-Trichomoniasis trct UG
-Amebiasis . Giardiasis
-Acute ulcerative gingivitis. Inf dental
-Anaerob vaginosis
Metronidazole

Efek samping : N /V / D
pusing., dizziness,ataxia,
rash, urticaria. Angio-oedema, kejang
Dosis >> carsinogenic (rodent )

Dosis : Anaerobic infection

- Peros 400 mg/ 8 jam

- Rectal 1 g / 8 jam ( utk 3 hari )

dilanjutkan 1 g / 12 jam
Co-trimoxazole
Sulfonamides & Trimethoprim

Sulfadiazine
Sulfisoxazole
Sulfamethoxazole +Trimethoprim Co-trimoxazole
( Bactrim )
Sulfacetamide
 Co-trimoxazole :
( bacterioside )

Trimethoprim ( 1) + Sulfamethoxazole (5)

( bacteriosatik ) ( bacteriostatik)
Pteridine precursor + PABA

Pteridine + PABA
+ glutamic acid
sulfonamid
Folic acid

Dihydrofolic acid

trimethoprim Dihydrofolic acid reductase

Tetrahydrofolic acid 

DNA  Bacterial growth

Klinis : (Co-trimoxazole )
* Inf-systemic
* Inf chronis - trct UG
* Inf-ku gram (-) bacilus
* Inf-trct Resp ( bronchitis ok S.pneumoniae, H.influenzae )
* Otitis media ( S.pneumoniae, H.influenzae )
* Typhoid fever ( resisten Chloramphenicol, Ampicilin )

Drug of choice Tx / Px :
Pneumonia ( ok. Pneumocytsis carinii )
( terutama pend dengan immunosppressed )
Adverse effects ( co-trimoxazole )
Sulfonamide Trimethoprim
Alergy-rash, fever, Macrocytic anemia
Stevens-johnson synd Trombocytopenia
Agranulocytosis
Kristal uria
Haemolysis
Inhibit metab- obat

Aplastic anemia (elderly)

Teratogenic ( folate antagonist)
Faktor kegagalan
tx. Antibiotik
Faktor kegagalan Tx. Antibiotik
01. Indikasi kurang tepat
02. Daya tahan tubuh <
03. Dosis <
04. Resistensi : (optimal dose/ freq ) 5-10 hari
( kec penyakit tertentu :
typhoid, tuberculosa, endocarditis )
Pemberian lama perlu observasi
Adversed reaction >>, mahal

05. Superinfeksi
Faktor kegagalan Tx. Antibiotik

06. Infeksi campuran

07. Tindakan bedah
- Absess diinsisi dulu

08. R. hipersensitif
09. Interaksi obat
Tetra dengan antacida/Mg, AL, Ca

10.Farmakokinetik
Aminoglycosida abs Peros <<
Buku acuhan

* The farmacological basis of therapeutics (Goodman & Gilmans)

* Basic clinical pharmacology ( Bertram G Katzung)
* Pharmacology -Examination & broad review
Katzung & Trevor’s (2008 )
* Medical Pharmacology ( Peter winstanley & Tom Walley (2002 )
• WHO Model Formulary (2002 )
• Pharmacology Principles and applications ( 2009 )
Eugenia M.Fulcher, Robert M.Fulcher,Cathy Dubeansky S
* Farmakologi dan terapi ( UI -2008 )
 Pertanyaan :

1. Gray sindrom ? Mengapa ?

2. Mengapa balita tidak boleh diberi Tetracyclin ?

( Ibu hamil ? Ibu menyusui ? )

3. Mengapa Tetracyclin tak boleh

diberikan bersama antasida ?
4. Apa Clavulanic acid ?
5. Mengapa ibu hamil tak boleh diberi
Aminoglycosida ?
( kalau ibu menyusui )
6. Pend dengan kelainan ginjal bila diberi antibiotika
gol Tetracyclin; Gol Tetracyclin apa yg boleh diberikan
mengapa ?

7. Apa tujuan pemberian Probenicid bersama Penicillin ?

selamat belajar