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Cloxacillin is a semisynthetic β-lactamase inhibitor. It binds to and inactivates penicillin-binding proteins that cross-link peptidoglycans, which are structural components of bacterial cell walls. In vitro, addition of cloxacillin (0.50 μg/ml) almost completely inhibits B. megaterium growth. Cloxacillin inhibits recombinant type Ib penicillinase, P. vulgaris cephalosporinase, and C. freundii cephalosporinase (Kis = 15, 0.27, and 0.027 μM, respectively) as well as S. aureus and S. epidermidis growth (MICs = 0.2 and 0.2 μg/ml, respectively). In vitro, addition of cloxacillin (0.50 μg/ml) almost completely inhibits B. megaterium growth. Formulations containing cloxacillin have been used to treat infections caused by methicillin-sensitive staphylococci.

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