Antibacterial agents Flashcards
(45 cards)
List 5 ways bacterial resistance to antibiotics
efflux pump decrease entry altered target site enzymatic degradation Bypass pathways
Selective toxicity
affects microbes > hosts
Examples of selectivity toxicity
Folate metabolisms, protein/nucleic acid synthesis (ribosomes, gyrase), Cell walls, fungal cell membrane (cell wall diff structures)
Antibiotic spectrum (3)
Narrow
Extended
Broad
Narrow antibiotic
Gram + or -
Extended antibiotic
Gram + and -
Broad antibiotic
Gram + and - and atypical
Three categories of resistance
natural/intrinsic
escape
acquired
Natural/intrinisic resistance
lack drug targets
Escape resistance
Precursor still there. Drug stopped synthesis but source is not removed - important to surgically drain/remove precursors
Acquired resistance
Mutational (requires multiple steps/generations)
Plasmid mediated: Conjugation (physical contact), transduction (virus carrying resistance), Transformation (DNA from environment)
Drugs easily enter CSF
chloramphenicol
Sulfonamides - trimethoprim
Cephalosporins (3/4)
Rifampin - Metronidazole
Enter CNS with inflammation
Penicillins
vancomycin
ciprofloxacin
tetracycline
Enter CSF poorly
aminoglycosides
cephalosporins (1/2)
Erythromycin
Lindamycin
Cholesterol is in mammalian membrane as _______ is in fungal cell membran
ergosterol
Inhibition of synthesis of stage 1 cell wall
Alanine racemase: cycloserine; enolpyruvate transferase: fosfomycin
Inhibition of synthesis of stage 2 cell wall
D-ala-D-ala pentapeptide: Vancomycin; bactoprenol lipid carrier: bacitracin
Inhibition of synthesis of stage 3 cell wall
Transpeptidase: penicillins, cephalosporins, monobactams, carbapenems
inhibition of synthesis/damage to cell membrane
daptomycin, polymixin B
Modification of synthesis or metabolism of nucleic acids
DNA gyrase: Fluoroquinolones
RNA pol: rifampin
DNA: metronidazole, nitrofurantonin
Inhibition/modification of protein synthesis
30S: aminoglycosides (irrev), tetracyclines
50S: clindamycin, macrolides, chloramphenicol, treptogramins
Isoleucyl-tRNA synthetase: mupriocin
Modification of intermediary metabolisms (ie. folate)
Dihydropteroate synthase: Sulfonamides
Dihydrofolate reductase: Trimethoprim
bactericidal mechanisms
inhibition of cell wall synthesis
disruption of cell membrane function
interference with DNA function/synthesis
Bacteriostatic mechanism
inhibition of protein synthesis (except aminoglycosides)
inhibitions of intermediary metabolic pathways