dr.

Elly Nurus Sakinah

 Antibakteri
 Antimycobacterial
 Antifungal
 Antiviral
 Antiprotozoa
 Antihelminth
 Antikanker
 Antimikroba: obat pembasmi mikroba

 Antibiotik : zat-zat kimia yang dihasilkan oleh

fungi dan bakteri yang menghambat atau
membunuh mikroba jenis lain.

 Toksisitas selektif

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1. Mengganggu metabolisme sel
• Sulfonamid, Trimetoprim
2. Menghambat sintesis dinding sel
• Penisilin, Sefalosporin
3. Mengganggu permeabilitas membran sel
• Polimiksin
4. Menghambat sintesis protein
• Aminoglikosida, Makrolida, Tetrasiklin,
Kloramfenikol
5. Menghambat sintesis atau merusak asam
nukleat
• Rifampisin, kuinolon
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 Aktivitas kerja:
1. BAKTERIOSTATIK
2. BAKTERISID

 Spektrum:
 Broad spectrum
 Narrow spectrum

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 Menginaktivasi enzim yang merusak obat
 Mengurangi akumulasi obat  membran sel
bakteri impermeabel thd obat
 Perubahan tempat ikatan
 Perkembangan jalur metabolik alternatif

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1. Tepat indikasi
1. Profilaksis
2. Terapeutik
1. Empiris: data epidemiologis bakteri
2. Terarah: >>>efektif, aman, spektrum sempit
2. Tepat penderita
3. Tepat obat
4. Tepat dosis
5. Waspada terhadap “AE”
(kejadian yang tidak diinginkan, efek samping obat)

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PENGHAMBAT
SINTESIS DINDING
SEL
• GOLONGAN BETA
LAKTAM
PENISILIN,
SEFALOSPORIN
Mekanisme
kerjaantibiotika β
laktam  memiliki
cincin β laktam 
mencegah ikatan silang
diantara rantai polimer
peptidoglikan  hambat
sintesis dinding sel
BAKTERISID
 ADME:
 A: di usus terganggu makanan kec. Amoksisilin
 D: bebas ke seluruh tubuh, plasenta tapi tidak
teratogenik
 M: tidak bermakna
 E: ginjal

 EFEK SAMPING: hipersensitivitas, diare,

nefritis, neurotoksisitas, gangguan pembekuan
darah

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 Resistensi :
 Aktivitas β laktamase
 Penurunan permeabilitas terhadp obat
 Perubahan protein pengikat penisilin

 OBAT PENTING : Amoksisilin , Ampisilin

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Natural Anti- Aminopenicill Aminopenicill Anti- Anti-
Penicillins Staphyllococc ins ins plus beta- pseudomonal pseudomonal
al penicillins lactamase penicillins penicillins
inhibitor plus beta
lactamase
inhibitor
Penicillin G Oxacillin, Ampicillin, Amoxi- Piperacillin, Pip-
Penicillin V Dicloxacillin, Amoxicillin Clavulinic Ticarcillin Tazobactam,
Methicillin, acid, Ticar-
Nafcillin Ampicillin- Clavulinic acid
Sulbactam
gram-positive Resist Extended antimicrobial Active against Pseudomonas, E.
bacteria except degradation spectrum. coli, klebsiella, enterobacter,
Gram negatives: E. coli, serratia and B. fragilis.
Staphyllococc by Proteus, Salmonella,
us penicillinase. Lower activity against gram
Haemophilus, M.
catarrhalis, Klebsiella, positives
Useful for Often used with
treating S. Neisseria, Enterobacter,
Bactoroides. aminoglycosides when treating
aureus. Used as first line therapy for pseudomonal infections
No added acute otitis media and sinusitis.
benefit in
treating Strep.
species
Cephalosporins : Spectrum of activity
and clinical use
First Second Third Fourth Fifth
generation generation generation generation generation
Cefazolin, Cefuroxime, Cefotaxime, Cefepime, Ceftibiprole
Cephalexin, Cefaclor Ceftriaxone, Sulperazon
cefadroxil Ceftazidime
Cefixime
Most gram positive Increased activity gram negative > Active against Strep, Staph (mssa), aerobic
cocci (Strep, S. against H. flu, gram positive. gram negatives (enterobacter, e. coli,
aureus), E. coli, enterobacter, Useful for klebsiella, proteus and pseudomonas)
Proteus, Klebsiella. Neisseria, proteus, meningitis.
E. coli, klebsiella, M. Ceftriaxone used
catarrhalis, for highly resistant
anaerobes and B. and multi drug
fragilis. resistant strep
pneumo along with
vancomycin
 Sebagian besar diberikan intravena, krn
absorbsi oral jelek
 Per oral : sefadroksil, sefuroksim, sefiksim.
 Efek samping: alergi, perdarahan (akibat efek
anti vitamin K)
 Resistensi  mirip penisilin

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1. Menghambat sintesis dinding sel
▫ Beta lactam:
 Penicillin
 Cephalosporins
 Monobactam
 Carbapenem
▫ Vancomycin
▫ Bacitracin
▫ Daptomycin (new)
2. Meningkatkan permeabilitas membran
▫ Polymyxin
PENGHAMBAT
METABOLISME SEL
Mek. Kerja:
Kompetisi dg
PABA hambat
enz.dihidroptero
at
sintetaseimper
meabel thd
as.folatsintesis
DNA terganggu
SpektrumBAKTE
RIOSTATIKEnter
obakter, klamidia,
pneumocystis
 ADME
 A: oral cukup baik
 D: ke seluruh tubuh, CSS, Plasenta, ASI berikatan
dengan albumin
 M: di hati
 E :ginjal

 EFEK SAMPING: kristaluria, hipersensitivitas,

gangguan darah, kernicterus,potensiasi obat.
 KI neonatus, bayi<2bl, kehamilan

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 TOPIKAL: sulfasetamid, sulfadiazin perak 
combustio
 Trakoma : sulfasetamid topikal dan sistemik
atau tetrasiklin
 ISK : kotrimoksazol

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 MK inhibitir dihidrofolat reduktase
 Spektrum  mirip sulfametoksazol, tapi 20-50
kali lebih poten
 Resistensi afinitas obat menurun
 ADME mirip sulfametoksazol
 ES  defisiensi folat anemia megaloblastik,
leukopenia, dan granulositopenia.

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 Kombinasi trimetropim dengan
sulfametoksazole, BAKTERISID
 MK  sinergistik
 Spektrum  lebih luas dibanding tunggal
 Resistensi  lebih jarang dibanding tunggal
 ESkulit, GIT, SJS
 Dosis: 2 dd 2 tab (sulf 400mg+trim 80) selama
3-7 hari

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 Adverse effect

• Severe allergic reactions

: Anaphylaxis
• Cutaneous reactions
– Toxic epidermal
necrolysis or Steven-
Johnson syndrome
• Myelosuppression
• Hemolytic anemia, esp
in patients with G-6PD
deficiency
PENGHAMBAT
SINTESIS ASAM
NUKLEAT
 Fluoroquinolones
• Ciprofloxacin (IV ;PO/Topical) Ofloxacin (Floxin; Topical), Levofloxacin
(Levaquin; IV ; Oral).

• Synthetic derivatives of nalidixic acid.

• Inhibits DNA gyrase, causing permanent DNA cleavage.

• Pharmacokinetics
▫ Excellent bioavailability
▫ Excellent tissue penetration : Wide distribution - CSF, saliva, bone,
cartilage

• Resistance:
▫ DNA Gyrase mutations
▫ Cellular membrane efflux mechanisms.
▫ Decreased number of porins in target cells.
 Fluoroquinolones
• Adverse effects.
– Headache, dizziness, nausea, lightheadedness
– Limit use in pregnancy, nursing mothers, and
children < 18.
– Drug interactions: may increase levels of
theophylline, warfarin, caffeine and cyclosporine.
(karena dapat lebih menginvasi GIT)
– Absorption decreased when taken with cations.
– Arthralgias - 1%.
 Target the bacterial ribosome.
 Bacterial – 70S (50S/30S)
 Mammalian – 80S (60S/40S)
 High levels may interact with mammalian ribosomes.
 50S binders - Macrolides, Clindamycin,
Chloramphenicol, Streptogramins.
 30S binders - Aminoglycosides, Tetracyclines
 Mupirocin
 First generation
 Erythromycin
 Second generation
 Azithromycin, Clarithromycin
 Ketolide : Telithromycin
 Neomycin , Gentamicin ,Tobramycin, Amikacin
 Binds the 30S subunit.
 Only active against anaerobes because an oxygen
dependent system is required to transport the
molecules into the cell.
 Synergism with cell wall inhibitors is seen because they
increase the permeability of the cell.
 Post antibiotic effect
 Persistent suppression of bacterial growth that occurs after the drug has
been removed
 Gram negative bacilli and Staphyllococcus aureus
INTERAKSI OBAT
EFEK SAMPING
TETRASIKLI N : GIGI COKLAT
AMINOGLIKOSIDA :
OTOTOKSIK
NEFROTOKSIK