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2008
ANTIBIOTIKAEvi Umayah Ulfa
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Antimicrobial Drugs
Chemotherapy The use of drugs to treat adisease
Antimicrobial drugs Interfere with the growth ofmicrobes within a host
Antibiotic Substance produced by amicrobe that, in small amounts,inhibits another microbe
Selective toxicity A drug that kills harmful microbes
without damaging the host
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Table 20.1
MicrobialSources of
Antibiotics
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Table 20.2
Antibiotic Spectrum of Activity
No antibiotic is effective against all microbes
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Mode of Antimicrobial Action
Bacteria have their own enzymes for
Cell wall formation
Protein synthesis
DNA replication
RNA synthesis
Synthesis of essential metabolites
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Mode of Antimicrobial Action
Figure 20.2
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Inhibition of Cell Wall Synthesis
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Beta Lactam Antibiotics (Penicillins)
B-lactams inhibittranspeptidase.
Only effective againstrapidly growing organismsthat synthesizepeptidoglycan. (Ineffectiveagainst mycobacteria.)
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Penicillin
Penicilinase-resistant penicillins
Extended-spectrum penicillins
Penicillins + -lactamase inhibitors
Carbapenems
Monobactam
Inhibitors of Cell Wall Synthesis
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Inhibitors of Cell Wall Synthesis
Figure 20.8
Cincin beta laktam AB penisilin dirusak oleh enzim penisilinase
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Cephalosporins
2nd, 3rd, and 4th
generations moreeffective against
gram-negatives
Antibacterial AntibioticsInhibitors of Cell Wall Synthesis
Figure 20.9
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Polypeptide antibiotics
Bacitracin
Topical application
Against gram-positives
Inhibits regeneration of phospholipids receptorsinvolved in peptidoglycan synthesis.
Vancomycin Glycopeptide
Important "last line" against antibiotic resistant S.aureus
Inhibitors of Cell Wall Synthesis
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Antimycobacterium antibiotics
Isoniazid (INH)
Inhibits mycolic acid synthesis Ethambutol
Inhibits incorporation of mycolic acid
Inhibitors of Cell Wall Synthesis
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Inhibition of Protein Synthesis (Translation)
Figure 20.4
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Chloramphenicol Broad spectrum
Binds 50S subunit, inhibits peptide bondformation
Aminoglycosides
Streptomycin, neomycin, gentamycin
Broad spectrum
Changes shape of 30S subunit
Inhibitors of Protein Synthesis
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Tetracyclines Broad spectrum
Interferes with tRNA attachment
Macrolides Gram-positives
Binds 50S, prevents translocation
Erythromycin
Gram-positives
Binds 50S, prevents translocation
Inhibitors of Protein Synthesis
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Polymyxin B
Bacillus polymyxa(PolimixinA,B,C, and D)
Decapeptide that disrupts the phospholipidlayer incell membrane
Topical
Combined with bacitracin and neomycin in over-
the-counter preparation
Injury to the Plasma Membrane
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Rifamycin Inhibits RNA synthesis
Antituberculosis
Quinolones and fluoroquinolones (DNA Synthesis) Ciprofloxacin
Inhibits DNA gyrase
Urinary tract infections
Inhibitors of Nucleic Acid Synthesis
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Sulfonamides (Sulfa drugs)
Inhibit folic acid synthesis
Broad spectrum
Inhibitions of Sythesis os Essential Metabolites
Figure 5.7
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Figure 20.13
Inhibitions of Sythesis os Essential Metabolites
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Classes of Antibiotics
Lactam AB
Macrolide AB
Tetracyclines
Aminoglycoside AB
Polypeptide AB
Lyncosamide
Chloramphenicol
Rifamycins
Minor AB
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Polyenes
Amphotericin B Azoles
Miconazole
Triazoles Allylamines
Antifungal DrugsInhibition of Ergosterol Synthesis
Figure 20.15
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Echinocandins
Inhibit synthesis of -glucan
Cancidas is used against Candida andPneumocystis
Antifungal DrugsInhibition of Cell Wall Synthesis
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Flucytocine
Cytosine analog interferes with RNA synthesis
Pentamidine isethionate
Anti-Pneumocystis; may bind DNA
Antifungal DrugsInhibition of Nucleic Acids
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Griseofulvin
Used for superficial mycoses
Tolnaftate
Used for athlete's foot; action unknown
Antifungal DrugsInhibition of Microtubules (Mitosis)
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Antiviral DrugsNucleoside and Nucleotide Analogs
Figure 20.16a
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Antiviral DrugsNucleoside and Nucleotide Analogs
Figure 20.16b, c
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Protease inhibitors Indinavir
HIV
Inhibit attachment
Zanamivir
Influenza
Inhibit uncoating
Amantadine Influenza
Interferons prevent spread of viruses to new cells
Viral hepatitis
Antiviral DrugsEnzyme Inhibitors
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Chloroquine Inhibits DNA synthesis
Malaria
Metronidazole Damages DNA
Entamoeba, Trichomonas
Antiprotozoan Drugs
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A ih l i hi
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Mebendazole
Inhibits nutrient absorption
Intestinal roundworms
Ivermectin
Paralyzes worm
Intestinal roundworms
Antihelminthic Drugs
Di k Diff i T
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Disk-Diffusion Test
Figure 20.17
Metode untukmenguji kepekaan
AB
E TMetode untuk
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E Test
Figure 20.18
Metode untuk
menguji kepekaan
AB
B h Dil i TMetode untuk
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Broth Dilution Test
Figure 20.19
Metode untuk
menguji kepekaan
AB
Hasil Uji Kepekaan Antibiotik
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Diameter Hambat
MIC Minimal inhibitory concentration
Kadar minimal AB yang mampu menghambatMO
MBC Minimal bactericidal concentration
Kadar Minimal AB yang mampu membunuhMO
Hasil Uji Kepekaan Antibiotik
A tibi ti R i t
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A variety of mutations can lead to antibiotic resistance.
Mechanisms of antibiotic resistance
1. Enzymatic destruction of drug
2. Prevention of penetration of drug
3. Alteration of drug's target site
4. Rapid ejection of the drug
Resistance genes are often on plasmids or
transposons that can be transferred between bacteria.
Antibiotic Resistance
A tibi ti R i t
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Misuse of antibiotics selects for resistance mutants.
Misuse includes:
Using outdated, weakened antibiotics
Using antibiotics for the common cold and other
inappropriate conditions
Use of antibiotics in animal feed
Failure to complete the prescribed regimen
Using someone else's leftover prescription
Antibiotic Resistance
Eff t f C bi ti f D
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Synergism occurs when the effect of two drugs
together is greater than the effect of either alone.
Antagonism occurs when the effect of two drugs
together is less than the effect of either alone.
Effects of Combinations of Drugs
Eff t f C bi ti f D
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Effects of Combinations of Drugs
Figure 20.22
Th F t f Ch th ti A t
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Antimicrobial peptides
Broad spectrum antibiotics from plants and animals
Squalamine (sharks)
Protegrin (pigs)
Magainin (frogs)
Antisense agents
Complementary DNA or peptide nucleic acids thatbinds to a pathogen's virulence gene(s) and
prevents transcription
The Future of Chemotherapeutic Agents