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