Anda di halaman 1dari 64

FARMAKOLOGI

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

4
Penggolongan Atas Dasar
Mekanisme Kerjanya

Zat bakterisida, pada dosis biasa berkhasiat mematikan


kuman
1. Zat yang bekerja terhadap fase tumbuh, ex: penisilin dan
sefalosporin, polopeptida (polimiksin, basitrasin),
rifampisin, asam nalidiksat dan kuinolon.
2. Zat yang bekerja trhadap fase istirahat, ex:
aminoglikosida, nitrofurantoin, INH, kotrimoksazol.

Zat bakteriostatik, pada dosis biasa terutama berkhasiat


menghentikan pertumbuhan dan perbanyakan kuman.
Ex: sulfonamida, kloramfenikol, tetrasiklin, makrolida,
linkomisin.

Farmakologi_RINA YUNIARTI, S.Farm, Apt.


What Manner Can We Kill?
Time-dependent
Drug concentration must remain constantly above the
minimum inhibitory concentration (MIC)
-lactams, vancomycin
Concentration-dependent
Drug concentration must reach a certain concentration, many
times based on the area under the curve (AUC)
Fluoroquinolones
Tergantung waktu
konsentrasi obat harus tetap terus di atas konsentrasi hambat minimum
(MIC)
-laktam, vankomisin
Tergantung konsentrasi
konsentrasi obat harus mencapai konsentrasi tertentu, berkali-kali
didasarkan pada daerah di bawah kurva (AUC)
fluoroquinolones
7
What Can We Disrupt?
Cell Wall
Folic Acid Synthesis
Nucleic Acid Synthesis
Ribosome
Cell Membrane

8
CELL WALL
INHIBITORS

9
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

12
-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

13
Penicillin Classifications
Narrow-spectrum penicillins
Penicillinase-resistant penicillins
Extended-spectrum penicillins

14
Narrow-Spectrum Penicillins
PENICILLIN G
More active against Neiserra and anaerobes
PENICILLIN V
Keep it straight:V is not IV

Good activity against Gram {+} cocci


Anaerobic activity (except Bacteroides)

15
Extended-spectrum PCNs
Aminopenicillins
Carboxypenicillins
Ureidopenicillins

16
Aminopenicillins
Agents
AMPICILLIN
AMOXICILLIN
BACAMPICILLIN
Broader spectrum over penicillin
Gram {-} aerobes

17
Carboxypenicillins
Agents
CARBENICILLIN
TICARCILLIN
More coverage than the aminopenicillins
Increased Gram {-} coverage
Peudeomonas aeruginosa
Ticarcillin 2-4 > Carbenicillin
Enterobacter
Carbenicillin concentrates rapidly in urine

18
-Lactamase Inhibitors
Chemicals with no antibacterial activity
that irreversibly inactivate -lactamase
SULBACTAM
With ampicillin
TAZOBACTAM
With pipercillin
CLAVULANATE/CLAVULANIC ACID
With amoxicillin
With ticarcillin

19
CEPHALOSPORINS
1st Generation Agents

CEFAZOLIN
CEFADROXIL
Cephalosporin analog of amoxicillin
CEPHALEXIN
Cephalosporin analog of ampicillin
CEPHALOTHIN

Great Gram {+} activity

20
2nd Generation Agents
CEFOXITIN
CEFOTETAN
CEFONICID
CEFPROZIL
CEFUROXIME

More Gram {-} activity than 1st


generation agents
Often used for UTIs and URIs
21
3rd Generation Agents
CEFIXIME
CEFOPERAZONE
CEFOTAXIME
CEFTAZIDIME
CEFTRIAXONE

Have even better Gram {-} coverage than


second generation agents
Loses more Gram {+} coverage

22
4th Generation Cephalosporins
CEFEPIME

Has most of the Gram {-} coverage with


Gram {+} coverage
Anti-pseudomonal activity
No anaerobic activity

23
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

24
MONOBACTAMS
AZTREONAM
Resistant to most Gram {-} -lactamases

25
CARBAPENEM
Agents
ERTAPENEM
IMIPENEM
MEROPENEM

Ertapenem lacks coverage against


Pseudomonas acinetobacter, two common
nosocomial agents

26
GLYCOPEPTIDES
VANCOMYCIN
TEICOPLANIN

Gram {+} aerobes


MRSA
Penicillin-resistant pneumococcus

27
Folic Acid Synthesis
Inhibitors

30
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
31
Kombinasi
Kombinasi Sulfa + Trimetoprim

TRIMETOPRIM + SULFAMETOXAZOLE =
COTRIMOXAZOLE
Nucleic Acid
Synthesis Inhibitors

33
FLUOROQUINOLONES

Inhibit DNA topoisomerase II (DNA


gyrase)
Bacteriostatic

34
1st Generation Fluoroquinolones
NALIDIXIC ACID
Gram {-} coverage only
Enterobacteraceae
E. Coli
Klebsiella
Proteus

35
2nd Generation Fluoroquinolones

Agents
CINOXACIN
LOMEFLOXACIN
NORFLOXACIN
Increased Gram {-} spectrum

36
Advanced 2nd Generation
Fluoroquinolones

Agents
CIPROFLOXACIN
OFLOXACIN
Has increased Gram {-} coverage along
with atypicals
Cipro has good Pseudomonas coverage

37
3rd Generation Fluoroquinolones
Agents
GATIFLOXACIN
LEVOFLOXACIN
L-isomer of Ofloxacin
Same coverage as 2nd generation with moderate
Gram {+} activity
Used in community acuquired pneumonia

38
Fluoroquinolones Side Effects
Complexes with cations
Photosensitivity
Renal elimination
Tendon rupture
Do not give if <18yo

39
RIBOSOMAL
INHIBITORS

41
Inhibitors of Protein Synthesis
TETRACYCLINES
DOXYCYCLINE
TETRACYCLINE

Tetracycline Spectrum
Gram {+} Bacilli
Gram {-} Rods
Gram {-} Bacilli

44
Tetracycline SE
Chelates with cations
Decreased absorption with dairy, calcium
Deposition on calcified tissues
GI upset
Phototoxicity

45
AMINOGLYCOCIDES
AMIKACIN
GENTAMICIN
NETILMYCIN
NEOMYCIN
KANAMYCIN
STREPTOMYCIN
TOBRAMYCIN

47
Aminoglycocide Spectrum
Gram {-} Bacteria
Pseudomonas aeruginosa
Vibrio cholerae
Yersinia pestis (PLAGUE! )
Enterobacter aerogenes
E. coli
Klebsiella pneumoneae
Proteus
Serratia
48
Aminoglycocide SE
Renally eliminated
Ototoxicity
Nephrotoxicity
Neomycin-used topically, orally for hepatic
failure
Streptomycin-used in TB

49
MACROLIDES
AZALIDES:
AZITHROMYCIN
KETOLIDES:
TELITHROMYCIN
MACROLIDES:
CLARITHROMYCIN
DIRITHROMYCIN
ERYTHROMYCIN

51
Macrolide Spectrum
Gram (+) cocci
Gram (+) bacilli

52
LINCOMYCINS
CLINDAMYCIN
LINCOMYCIN

Lincomycin Spectrum
Gram {+} aerobes
Gram {+} anaerobes
Gram {-} anaerobes
NO gram {-} aerobic coverage
Think of these as 2nd-line penicillins

55
Lincomycin SE
Rash
Neutropenia
Thrombocytopenia
Erythema multiforme (rare)
Pseudomembranous colitis

56
CHLORAMPHENICOL
TIAMPHENICOL
CHLORAMPHENICOL

Broad spectrum against Gram {+}, Gram


{-}, and anaerobes.

57
Cell Membrane
Inhibitors

58
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

59
PUSAT INFORMASI OBAT (PIO)
PC. IKATAN APOTEKER INDONESIA (IAI)
PONOROGO
Sekertariat : Apotek Kimia Farma
jl. Jend. Sudirman no.09 Ponorogo
Email: iaiponorogo@gmail.com

NASRUHAN ARIFIANTO, S.Farm., M.Farm.Klin., Apt.


WA : 081331443337
BBM : 233D670E
Selamat belajar.

Anda mungkin juga menyukai