3 Aminoglycosides Macromolecule … Polycations +++ Major effective on gram negativeStreptomycinAmikacinGentamicinTobramycinSisomicinNetilmicinNeomycinKanamycin
4 Mechanism of action Bacterial protein synthesis inhibitors Passive diffusion through outer membraneActive O2 dependent transport through cell membraneBind at 30s subunit ribosomeInhibit initiation complex formationMiscoding of mRNA … non-function/ toxic peptideBlock of ribosome translocation … Breakdown of polysome into monosomeIrreversible … Bactericidal**
6 Synergism & antagonism Synergism with beta-lactam antibioticsbeta-lactam act on cell wallincrease AGs penetrationAntagonism with beta-lactam antibioticsform complex with beta-lactam ringloss of activityShould not mix together in drug preparation
7 Once daily Aminoglycosides Concentration dependent killingHigher peak … Higher effectProlong Post Antibiotic Effects (PAEs)Can be given ODLess toxicity >>> nephrotoxicity***Concentration dependent … SaturationTime dependentSaturation of tubular uptake
10 Spectinomycin Aminoglycosides like No amino sugar & glycosidic bonds Alternative for gonorrhea in penicillin hypersensitivity in pregnancy***IM inj.No cross resistance with other drugs used in gonorrheaADRs … pain at injection site, fever, nausea, nephrotoxic, anemia
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