Table 1.
Putative biofilm-active antibiotics
Antibiotic | Class | MOA | Spectrum of activity | Important side effects b |
Rifampicin at1/2: 4 h | Rifamycin | BactericidalInhibition of bacterial RNA synthesis | Gram-positive and -negative bacteria | Nausea, gastrointestinal disturbances, hepatotoxicity, thrombocytopenia, rash, red discoloration of urine, flu-like symptoms |
Daptomycint1/2: 9 h | Lipopetide | BactericidalInsertion of hydrophobic tail into cell membrane, resulting in membrane depolarization and cell death | Gram-positive bacteria including MRSA, VRSA, VRE, and PRSP. Log- and stationary-phase of bacteria | Nausea, vomiting, diarrhea, hypertension and hypotension, myopathy, neuropathy, urethritis, anemia, hypokalemia, arthralgia |
Linezolidt1/2: 6 h | Oxazolidinones | BacteriostaticBinds to the bacterial 23S ribosomal RNA of the 50S subunit, thus preventing the formation of a functional 70S complex. Production by MSSA and MRSA | Gram-positive bacteria including MRSA, MSSA, CoNS, and enterococci including VRE.Good tissue distribution and bioavailability | Nausea, vomiting, diarrhea, thrombocytopenia, myelosuppression, reversible optic neuritis, irreversible peripheral neuropathy, serotonin syndrome |
Tigecyclinet1/2: 42 h | Glycylcylines (synthetic derivative of tetracyclines) | BacteriostaticBinds 30S bacterial ribosomal subunit and prevents binding of tRNA to the mRNA ribosome complex | Active against Gram-positive bacteria (including VRE and MRSA), Gram-negative bacilli, and anaerobes | Nausea, vomiting, diarrhea, sore mouth and throat, dysphagia, vitamin B complex deficiency, dental abnormalities, hepatotoxicity |
Minocyclinet1/2: 15 h | Tetracyclines | Same as tigecycline | Similar to tigecycline and also active against Neisseria meningitidis | Similar to tigecycline and in addition, vestibular disturbances with dizziness, tinnitus, and impaired balance—especially in women |
Vancomycint1/2: 8 h | Glycopeptides | BactericidalInhibits bacterial cell wall formationInterferes with peptidoglycan synthesis | Gram-positive bacteria. MRSA | Tinnitus, deafness (reversible on cessation of drug), nephrotoxicity, maculopapular rash (with rapid i.v. infusion) |
Should ideally be used as combination therapy to avoid rapid emergence of resistance.
MOA: mechanism of action; MRSA: methicillin-resistent Staphylococcus aureus; MSSA: methicillin-sensitive Staphylococcus aureus;
VRE: vancomycin-resistent enterococcus; PRSP: penicillin-resistant Streptococcus pneumoniae; CoNS: coagulase-negative staphylococci; t1/2: serum half-life of drug.
These side effects are generally attributed to systemic administration.