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Clinical Pharmacology
CLINICAL PHARMACOLOGY
BACTROBAN CREAM ® brand of mupirocin calcium cream, 2%
For Dermatologic Use Pharmacokinetics Text Continues Below
Systemic absorption of mupirocin through intact human skin is minimal. The systemic absorption of mupirocin was studied following application of Bactroban Cream three times a day for 5 days to various skin lesions (greater than 10 cm in length or 100 cm 2 in area) in 16 adults (aged 29 to 60 years) and 10 children (aged 3 to 12 years). Some systemic absorption was observed as evidenced by the detection of the metabolite, monic acid, in urine. Data from this study indicated more frequent occurrence of percutaneous absorption in children (90% of patients) compared to adults (44% of patients). However, the observed urinary concentrations in children (0.07 -1.3 µg/ mL [1 pediatric patient had no detectable level]) are within the observed range (0.08 -10.03 µg/ mL [9 adults had no detectable level]) in the adult population. In general, the degree of percutaneous absorption following multiple dosing appears to be minimal in adults and children. Any mupirocin reaching the systemic circulation is rapidly metabolized, predominantly to inactive monic acid, which is eliminated by renal excretion. Microbiology Mupirocin is an antibacterial agent produced by fermentation using the organism Pseudomonas fluorescens. It is active against a wide range of gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). It is also active against certain gram-negative bacteria. Mupirocin inhibits bacterial protein synthesis by reversibly and specifically binding to bacterial isoleucyl transfer-RNA synthetase. Due to this unique mode of action, mupirocin demonstrates no in vitro cross-resistance with other classes of antimicrobial agents. Resistance occurs rarely. However, when mupirocin resistance does occur, it appears to result from the production of a modified isoleucyl-tRNA synthetase. High-level plasmid-mediated resistance (MIC >1024 mcg/ mL) has been reported in some strains of S. aureus and coagulase-negative staphylococci. Page: 1 | 2 | Next >>
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