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Antibiotic and Its Resistance

Eddy Bagus Wasito


Definition
Classification
Desirable properties
Mechanism of bacterial resistance
Definition
Chemical substance
Produced by microorganism
Small concentration inhibit microorganism
Wholly / partially synthesis
A chemical substance derived from or
produced by various species of
microorganisms which is capable in small
concentrations inhibits the growth of other
microorganisms
Wholly / partially synthesis
Mechanism(s) of action
Affect the cell wall synthesis
Affect the cytoplasmic membrane function
Inhibit the protein synthesis
Interfere the DNA function
Metabolic antagonism
Interfere with Cell Wall Synthesis
Beta lactam antibiotic (Penicillin, Cephalosporin,
Monobactam, Carbapenem, Oxacephem, Clavam )
Cycloserin
Fosfomycin
Vancomycin
Bacitracin
Cell Membrane Inhibitor
Polymyxin (A E)
Polyene (Azole)
Inhibitor of Protein Synthesis
Inhibitor of transcription (Actinomycin D,
Rifampin)
Inhibitor of translation
30S ribosomal unit (Aminoglycoside, Tetracyclin,
Nitrofurans)
50S ribosomal subunit (Chloramphenicol,
Erythromycin, Lincomycin, Clindamycin, Puromycin,
Fusidic acid)
Metabolite Analoque
Inhibitor of tetrahydrofolate synthesis
(Sulfonamide, Sulfone, PAS)
Inhibitor of Dihydrofolate Reduktase
(Trimethoprim)
Others (Isoniazid, Flucytosine)
Desirable properties of
an antibiotic
Selective toxicity
Bactericidal
Does not cause resistancy
Should not be allergenic
Should not cause adverse side effects
Remain active in plasma, body fluids,
exudates
Continued .
Water soluble and stable
Bactericidal level in the body be rapidly
reach and maintain for prolonged period
Broad spectrum
Resistance may be attributed
Inactivation of the drug
Alteration of the target site
Blocking transport of the drug into the cell
Resistance of cycloserine :
Loss of the alanine transport
Elevated of alanine racemase & D-alanyl-
D-alanyl synthetase
Resistance of fosfomycin :
Altered transport system
Altered target enzym - decrease affinity
Resistane of aminoglycoside :
Acetylation of amino group (3 enzym)
Phosphorylation of hydroxyl group (5 enzym)
Adenylation of hydroxyl group (4 enzym)
Resistance of chloramphenicol :
Chloramphenicol acetyl transferase
Resistance of erythromycin :
Altered L4 & L12 of 50S subunit ribosome
(E.coli)
Resistance of sulfonamid :
Altered dihydropteroate synthetase

Resistane of trimethoprim :
Dihydrofolate reductase

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