Antibiotic Action Flashcards
beta-lactams (penicillin, cepalosporin)
inhibit the final transpeptidation reaction in cross-linking of peptidoglycan
Vancomycin
inhibit the polymerization of NAM and NAG onto peptidoglycan
Cycloserine
inhibits the isomerization from L to D aa
Cell-wall active antimicrobials?
beta lactams (penicillin, cepalosporin…), vancomycin, cycloserine
Outer and cytoplasmic membrane-active antimicrobials?
Polymyxin
Polymyxin
cationic surfactants disrupting bacterial outer and cytoplasmic membrane
Which one inhibits protein synthesis at the ribosomal level?
Aminoglycoside, tetracylines, chloramphenicol, macrolides
How aminoglycosides and tetracylcines, etc… prevent from harming human protein synthesis?
Selective toxicity is due to difference between bacterial and mammalian ribosomes.
Aminoglycoside representative drugs?
streptomycin kanamycin gentamicin neomycin tobramycin amikacin
Aminoglycoside action?
bind to specific target proteins in the 30S ribosomal subunit and inhibit protein synthesis
Tetracycline
reversibly bind 30S ribosomal subunit and inhibit binding of aminoacyl tRNA
Chloramphenicol
bind reversibly 50S ribosomal subunit
inhibit peptidyl transferase and peptide bond formation
Macrolides and lincomycins representative drug?
Macrolides: erythromycin
Lincomycins: lincomycin and clindamycin
Macrolides and lincomycins action?
bind 23S ribosomal RNA of the 50S subunit
inhibit peptidyl transferase
Which drugs inhibit nucleic acid synthesis?
Quinolones
Rifampicin
Quinolones
inhibit DNA gyrase & topoisomerase
interfere DNA replication
Rifampicin
inhibits RNA polymerase
interfere with transcription initiation
Which drugs are metabolic inhibitory antimicrobials?
Sulfonamide
Trimethroprim
Isoniazid
Metroniadazole
Sulfonamide
(structural analog of p-aminobenzoic acid) competitively inhibit formation of folic acid, preventing nucleic acid synthesis
How sulfonamide selective for bacteria?
only bacteria, NOT human, possess enzymes for making folic acid
Trimethoprim
inhibiting enzyme dihydrofolate reductase
interfere with folate metabolism
How trimethoprim selective for bacteria?
Both bacterial and human cells have dihydrofolate reductase. However, bacterial enzyme is 50000-fold greater sensitivity to the drug –> selective toxicity.
Isoniazid
inhibit lipid synthesis
Metronidazole
interfere with anaerobic metabolism