ANTIBIOTIK
NASRUHAN ARIFIANTO
Antibiotik
Berasal dari bahasa yunani: Anti
(lawan),Bios (hidup )
Antibiotik adalah Suatu zat kimia yang
dihasilkan oleh bakteri yang berkhasiat
obat apabila digunakan dalam dosis
tertentu dan berkhasiat mematikan atau
menghambat pertumbuhan kuman dan
toksisitasnya tidak berbahaya bagi
manusia.
Farmakologi_RINA YUNIARTI, S.Farm, Apt.
Principles of antibacterial therapy
How Can We Inhibit Bacteria?
Bacteristatic
Inhibits a vital pathway used in the growth of the
bacteria, but does not directly cause death
Bactericidal
Disrupts bacterial function so much that death will
occur
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Penggolongan Atas Dasar
Mekanisme Kerjanya
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CELL WALL
INHIBITORS
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Inhibitors of Cell Wall Synthesis
Fig. 1.1 Simplified scheme of bacterial cell wall synthesis showing site of action of cell
wall-active antibiotics. (Reproduced from Medical Microbiology, 16th Edition by David
Greenwood (2003), with permission from Elsevier
CELL WALL AGENTS
-Lactams
Penicillins
Cephalosporins
Monbactams
Carbapenems
Glycopeptides
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-LACTAM SUBTYPES
All share a -lactam ring, thereby having the
same mechansim of action (and explaining the
cross-sensitivity between classes)
Penicillins
Cephalosporins
Monobactams
Carbapenems
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Penicillin Classifications
Narrow-spectrum penicillins
Penicillinase-resistant penicillins
Extended-spectrum penicillins
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Narrow-Spectrum Penicillins
PENICILLIN G
More active against Neiserra and anaerobes
PENICILLIN V
Keep it straight:V is not IV
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Extended-spectrum PCNs
Aminopenicillins
Carboxypenicillins
Ureidopenicillins
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Aminopenicillins
Agents
AMPICILLIN
AMOXICILLIN
BACAMPICILLIN
Broader spectrum over penicillin
Gram {-} aerobes
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Carboxypenicillins
Agents
CARBENICILLIN
TICARCILLIN
More coverage than the aminopenicillins
Increased Gram {-} coverage
Peudeomonas aeruginosa
Ticarcillin 2-4 > Carbenicillin
Enterobacter
Carbenicillin concentrates rapidly in urine
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-Lactamase Inhibitors
Chemicals with no antibacterial activity
that irreversibly inactivate -lactamase
SULBACTAM
With ampicillin
TAZOBACTAM
With pipercillin
CLAVULANATE/CLAVULANIC ACID
With amoxicillin
With ticarcillin
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CEPHALOSPORINS
1st Generation Agents
CEFAZOLIN
CEFADROXIL
Cephalosporin analog of amoxicillin
CEPHALEXIN
Cephalosporin analog of ampicillin
CEPHALOTHIN
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2nd Generation Agents
CEFOXITIN
CEFOTETAN
CEFONICID
CEFPROZIL
CEFUROXIME
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4th Generation Cephalosporins
CEFEPIME
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CSF penetrance
2nd Generation
Cefuroxime
Generally not used due to decreased efficacy
3rd Generation
Cefotaxime
Q6-8 dosing
Agent of choice in neonatal meningitis (along with
ampicillin)
Ceftriaxone
Q12-24 dosing
Agent of choice for adult meningitis
Causes kernicterus in neonates
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MONOBACTAMS
AZTREONAM
Resistant to most Gram {-} -lactamases
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CARBAPENEM
Agents
ERTAPENEM
IMIPENEM
MEROPENEM
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GLYCOPEPTIDES
VANCOMYCIN
TEICOPLANIN
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Folic Acid Synthesis
Inhibitors
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Folic Acid Inhibitors
SULFAS
SULFAMETOXAZOL
SULFDIAZIN
SULFASALAZIN
Inhibit dihydropteroate synthetase, an enzyme
involved in the synthesis of bacterial folic acid
TRIMETHOPRIM
Inhibit dihydrofolate reductase, an enzyme
necessary for thymidine synthesis
Both are bacteriostatic
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Kombinasi
Kombinasi Sulfa + Trimetoprim
TRIMETOPRIM + SULFAMETOXAZOLE =
COTRIMOXAZOLE
Nucleic Acid
Synthesis Inhibitors
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FLUOROQUINOLONES
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1st Generation Fluoroquinolones
NALIDIXIC ACID
Gram {-} coverage only
Enterobacteraceae
E. Coli
Klebsiella
Proteus
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2nd Generation Fluoroquinolones
Agents
CINOXACIN
LOMEFLOXACIN
NORFLOXACIN
Increased Gram {-} spectrum
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Advanced 2nd Generation
Fluoroquinolones
Agents
CIPROFLOXACIN
OFLOXACIN
Has increased Gram {-} coverage along
with atypicals
Cipro has good Pseudomonas coverage
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3rd Generation Fluoroquinolones
Agents
GATIFLOXACIN
LEVOFLOXACIN
L-isomer of Ofloxacin
Same coverage as 2nd generation with moderate
Gram {+} activity
Used in community acuquired pneumonia
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Fluoroquinolones Side Effects
Complexes with cations
Photosensitivity
Renal elimination
Tendon rupture
Do not give if <18yo
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RIBOSOMAL
INHIBITORS
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Inhibitors of Protein Synthesis
TETRACYCLINES
DOXYCYCLINE
TETRACYCLINE
Tetracycline Spectrum
Gram {+} Bacilli
Gram {-} Rods
Gram {-} Bacilli
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Tetracycline SE
Chelates with cations
Decreased absorption with dairy, calcium
Deposition on calcified tissues
GI upset
Phototoxicity
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AMINOGLYCOCIDES
AMIKACIN
GENTAMICIN
NETILMYCIN
NEOMYCIN
KANAMYCIN
STREPTOMYCIN
TOBRAMYCIN
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Aminoglycocide Spectrum
Gram {-} Bacteria
Pseudomonas aeruginosa
Vibrio cholerae
Yersinia pestis (PLAGUE! )
Enterobacter aerogenes
E. coli
Klebsiella pneumoneae
Proteus
Serratia
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Aminoglycocide SE
Renally eliminated
Ototoxicity
Nephrotoxicity
Neomycin-used topically, orally for hepatic
failure
Streptomycin-used in TB
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MACROLIDES
AZALIDES:
AZITHROMYCIN
KETOLIDES:
TELITHROMYCIN
MACROLIDES:
CLARITHROMYCIN
DIRITHROMYCIN
ERYTHROMYCIN
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Macrolide Spectrum
Gram (+) cocci
Gram (+) bacilli
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LINCOMYCINS
CLINDAMYCIN
LINCOMYCIN
Lincomycin Spectrum
Gram {+} aerobes
Gram {+} anaerobes
Gram {-} anaerobes
NO gram {-} aerobic coverage
Think of these as 2nd-line penicillins
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Lincomycin SE
Rash
Neutropenia
Thrombocytopenia
Erythema multiforme (rare)
Pseudomembranous colitis
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CHLORAMPHENICOL
TIAMPHENICOL
CHLORAMPHENICOL
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Cell Membrane
Inhibitors
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DAPTOMYCIN
Unique mechanism of action that it binds
to bacterial membranes and causes a rapid
depolarization of membrane potential
which leads to inhibition of protein, DNA,
and RNA synthesis
Used in antibiotic resistant MRSA, VRE, and
linezolid-resistant strains
Can cause myalgias
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PUSAT INFORMASI OBAT (PIO)
PC. IKATAN APOTEKER INDONESIA (IAI)
PONOROGO
Sekertariat : Apotek Kimia Farma
jl. Jend. Sudirman no.09 Ponorogo
Email: iaiponorogo@gmail.com