DrugsStreptomycin链霉素andamikacin阿米卡星werefirstusedStreptomycin is still used against tuberculosis 肺结核Gentamicin庆大霉素andtobramycin托普霉素aremoreusedtodayNeomycin新霉素ismainlyusedtopically
Drugs Streptomycin 链霉素 and amikacin 阿米卡星 were first used Streptomycin is still used against tuberculosis 肺结核 Gentamicin 庆大霉素 and tobramycin 托普霉素 are more used today Neomycin 新霉素 is mainly used topically
Mechanism of ActionbindingoftRNAAAat the A siteaccordingtotheAAcodon-anticodonrecognitionAAAAthe P sitecontains theprotein informationantianticodoncodoncodoncodonPAMostmacrolides irreversiblybindto the3oS ribosomesubunit,andinterfere with codon-anticodon recognition. The irreversibility mayexplain the bactericide activity, as well as a post-antibiotic effect
Mechanism of Action Most macrolides irreversibly bind to the 30S ribosome subunit, and interfere with codon-anticodon recognition. The irreversibility may explain the bactericide activity, as well as a post-antibiotic effect
EntryintoBacteriaDiffusionthroughtheToo water-porins of thesoluble toGram +Gram-outercrossthethin cell wallmembranethick cell wallinnercomplexoutermembrane(Nakae&Nakae1982)membranewellporinsPassagethroughtheinnerInhibitorsofcellwallmembranedependingonsynthesisfacilitate entry,andpolarization,andthereforeoxygenpotientiate actionMostlyactiveagainstgram(-)，andneveragainstanaerobes厌氧微生物.Used in combination with cell wall inhibitor against gram(+)
Entry into Bacteria •Mostly active against gram(-), and never against anaerobes 厌氧微生物 •Used in combination with cell wall inhibitor against gram(+) Too watersoluble to cross the inner membrane well Inhibitors of cell wall synthesis facilitate entry, and potientiate action Diffusion through the porins of the outer membrane (Nakae & Nakae 1982) Passage through the inner membrane depending on polarization, and therefore oxygen