Table 1.
Structure | Cyclic lipopeptide |
---|---|
Mechanism of action | Bactericidal, binds cytoplasmic membrane, with resultant depolarization of membrane potential, cellularion effl ux and cell death |
In vitro activity | Gram positive organisms, including MRSA, VRSA, and vancomycin resistant enterococci |
CSLI susceptibility cutoff | ≤1 μg/ml; supplementation to 50 μg/ml Ca2+ required for testing in Muellar-Hinton broth |
Pharmacokinetics | Given intravenously, (half- life 8 hours, volume of distribution 100 ml/kg, protein biding 90%-93%, Cmax94 μg/ml with 6 mg/kg dose at steady state, linear kinetics through 12 mg/kg |
Excretion | 78% renal |
Pharmacodynamics | Concentration dependent killing, post-antibiotic effect of 6 hours against S. aureus |
US FDA approved indications | Treatment of complicated skin and skin structure infections (caused by susceptible strains of Gram-positive microorgansisms, including MSSA and MRSA); S. aureus bacteremia, including those with right-sided endocarditis, caused by MSSA and MRSA |
FDA approved dose | 4 mg/kg q24h for skin and soft tissue infections; 6 mg/kg q24h for bacteremia and endocarditis |
Dose for renal dysfunction | Creatinine clearance ≤30 ml/min: 4 mg/kg q48h for skin and soft tissue infections; 6 mg/kg q48h for bacteremia and endocarditis; for hemodialyis, dose after hemodialysis |
Adverse reactions | CPK elevation with and without myopathy, transient neuropathy |
Drug interactions | HMG-CoA inhibitors |
Cost | $171 for 500 mg |
Pregnancy | Class B |
Abbreviations: CSLI, Clinical and Laboratory Standards Institute; CPK, creative phosphokinase; FDA, Food and Drug Administration; MRSA, methicillin-resistant S.aureus; MSSA, methicillin-sensitive S.aureus; VRSA, vancomycin-resistant S.aureus