Penetration into tissues of various drugs active against gram-positive bacteria.

ABSTRACT

Gram-positive bacteria are the most important pathogens causing hospital- and community-acquired infections. We therefore reviewed the penetration of various antibiotics active against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus into tissues, where staphylococcal infections are common. Rifampicin reaches heart valve concentrations of 65% of the simultaneous serum levels. At 8 h after administration blood and tissues concentrations of rifampicin exceeded the MIC90 values for S. aureus as well as for S. epidermidis. After a 2-g intravenous bolus injection of flucloxacillin heart valve concentrations exceeded MIC values for staphylococci for more than 8 h whereas subcutaneous and muscle concentrations declined within the same time to undetectable levels. The MIC90 values of vancomycin for S. epidermidis and Enterococcus faecalis are 2.0 and 4.0 mg/l respectively and for S. aureus 1.0 mg/l. This concentration is reached in subcutaneous tissue, heart valves and muscle for at least 4-6 h after administration of 15 mg/kg, however the corresponding value for Enterococcus faecalis in heart valve is maintained only for 3-4 h. After two and three dose regimens of teicoplanin serum and bone levels were significantly higher than fat levels, exceeding the MIC90 values for S. aureus, S. epidermidis and E. faecalis. The ratio of tissue concentration of teicoplanin to serum concentrations was 11% for fat and 65% for bone.