Antibiotics Flashcards
Vancomycin
MOA: blocks cell wall synthesis
Blocks release of peptidoglycan precursor from bactoprenol & transglycosylation-no glycan chain extension
Target: bactoprenol precursor release & transglycosylation
Resistance: target site modify, innate dif terminal residue of pentapeptide than alanine
B-lactams
MOA: inhibition of cell wall synthesis
Blocks transpeptidation reaction formation of peptidoglycan x-links
Targets: penicillin binding proteins
Resistance: inactivation by B-lactamases-mutations of PCP, access
Ex: penicillin, monobactams, carbapenems, cephalosporins
Bactracin
MOA: Blocks cell wall synthesis by blocking dephosphorylation of bactoprenol pyrophosphate and thus cycling of bactoprenol carrier
Target: phosphorylation site of bactoprenol pyrophosphate
Resistance is not common
Polymixin
MOA: alter permeability of susceptible G- bacteria by interacting with LPS and phospholipids
Target: LPS and phospholipids on G- bacteria
Resistance not common
Daptomycin
MOA: binds to cell membranes of susceptible G+ bacteria depolarizing and disrupting ion gradient
Target: cell membranes of G+ bacteria
Resistance is not common
Isoniazid
MOA: block mycolic acid synthesis
Target: mycolic acid synthesis
Resistance: due to reduced uptake and modification of target sites
Mycobacterium cell wall inhibitor
Collistin
MOA: alter permeability of membranes of susceptible G- bacteria by interacting with LPS and phospholipids
Target: LPS and phospholipids on G - bacteria
Resistance not common
Ethionamide
MOA: block mycolic acid synthesis
Target: mycolic acid synthesis
Resistance: due to reduced uptake and modification of target sites
Mycobacterium cell wall inhibitor
Ethambutol
MOA: interferes with arabinogalactan synthesis
Target: arabinogalactan synthesis
Resistance due to reduced uptake and modification of target sites
Mycobacterium cell wall inhibitor
Cycloserine
MOA: interferes with alanine synthetase and racemase
Target: inhibits alanine synthetase/racemase
Resistance use to reduced uptake and modification of target sites
Mycobacterial cell wall inhibitor
Aminoglycosides
Streptomycin kanamycin amikacin gentamicin tobramyci neomycin
Irreversible inhibition of protein synthesis, inhibit elongation
Actively transported into cells, requires oxidative phosphorylation
Target: ribosomes 30s subunit
Resistance: innate target site mutation, access- mutation in active transport, and permeability
Tetracyclines
Doxycycline, minocycline
Reversible inhibition of protein synthesis-blocks tRNA
Target:ribosomes
Resistance: access decreased uptake or increase effluent pumps
Binding: production of a protein that binds tetracycline and protects
Chloramphenicol
MOA: blocks protein synthesis by inhibiting peptidyl transferase
Target: peptidyl transferase
Resistance: chloramphenicol acetyltransferase
Macrolides
Erythromycin, Azithromycin
MOA: reverse inhibition of protein synthesis-blocks translocations
Target: Ribosomes
Resistance: access decreased permeability, target site modification ribosomal protein mutations, target site modification: methylation of rRNA
Lincosamides
Clindamycin, lincomycin, linezolid
MOA: inhibition of protein synthesis blocks translocation
Target: ribosomes 50s subunit
Used for vancomycin resistant G+ organisms and multidrig resistant staphylococci
Quinolones
Nalidixic, cliproflaxin, levofloaxin, ofloxacin
MOA: inhibition of DNA replication
Target: DNA gyrase and topoisomerase
Resistance: target site modification, mutations in DNA
Access: mutations in cell surface which decrease uptake
Rifampicin aka rifampin
MOA: Inhibition of transcription
Target: DNA dependent RNA polymerase
Resistance: target site mutations in RNA polymerase
Metronidazole
MOA: inhibition of DNA repair, bacterial nitro-reductase produces toxic product inhibits DNA repair mechanisms
Target: bacterial DNA and DNA repair systems
Resistance: mutations in reductases
Trimeoprin
MOA-reversibly blocks steps in frolic acid synthesis
Target: frolic acid synthesis
Access: decreased permeability
Bypass or target site modification
Sulfonamides
MOA: reversibly block steps in folic acid synthesis
Target: folic acid synthesis
Access: decreased permeability, bypass or target site modification