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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Ceftobiprole medocaril sodium is the pro-drug of the active moiety ceftobiprole. Conversion from the prodrug ceftobiprole medocaril sodium, to the active moiety ceftobiprole, occurs rapidly and is mediated by non-specific plasma esterases. Ceftobiprole undergoes minimal metabolism to the open-ring metabolite, which is microbiologically inactive.
Ceftobiprole
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Andrew Henderson, Baek-Nam Kim, David L. Paterson
Ceftobiprole, formerly BAL 9141 or RO 63-9141, is a novel pyrrolidinone-3-ylidene-methyl cephalosporin with clinically demonstrable activity against methicillin-resistant Staphylococcus aureus (MRSA). Ceftobiprole medocaril (BAL 5788, JNJ 30982081, JNJ 30982081, RO 65-5788, RO 655788) is a water-soluble prodrug of ceftobiprole. This antibiotic is the first beta-lactam antibiotic to have In vitro activity against MRSA and vancomycin-resistant S. aureus (VRSA). Although not yet available in the USA, ceftobiprole has been approved for use in Canada and a number of European countries.
Ceftobiprole medocaril for the treatment of pneumonia
Published in Expert Review of Anti-infective Therapy, 2023
Wan-Hsuan Hsu, Chi-Kuei Hsu, Chih-Cheng Lai
Ceftobiprole medocaril (prodrug) have been developed for intravenous administration. After administration, the water-soluble ceftobiprole medocaril is converted to ceftobiprole (active form) rapidly within 10–54 seconds in plasma by type A plasma esterase, and the majority of concentrations are free to distribute [30] (Figure 1). Ceftobiprole medocaril achieves its bactericidal activity by inhibiting transpeptidases, especially showing strong affinities to penicillin-binding protein (PBP) 2a, PBP2×, and PBP3. PBP2a, PBP2×, and PBP3 are the membrane-associated enzymes responsible for β-lactam drug resistance in MRSA, PRSP, and MSSA respectively [31]. Ceftobiprole interferes with peptidoglycan biosynthesis of the bacterial cell wall, forming a chemical barricade to defend against β-lactam antibiotics. Hence, ceftobiprole medocaril is able to destruct these defense mechanisms of resistant bacteria strains.
Emergence of coagulase-negative staphylococci
Published in Expert Review of Anti-infective Therapy, 2020
Karsten Becker, Anna Both, Samira Weißelberg, Christine Heilmann, Holger Rohde
Ceftaroline fosamil is a fifth-generation cephalosporin with activity against methicillin-resistant staphylococci, including CoNS. The FDA approved ceftaroline for the treatment of acute bacterial SSSI and community-acquired pneumonia. Several in vitro studies found that almost all CoNS, including S. epidermidis, S. haemolyticus, S. capitis, S. caprae, S. lugdunensis, and S. warneri, are susceptible against ceftaroline. In vitro activity was documented also in methicillin-, linezolid-, or daptomycin resistant isolates [188,189]. Similar to ceftaroline, ceftobiprole medocaril is a fifth-generation cephalosporin with activity against MRSA. FDA approved ceftobiprole for the treatment of hospital-acquired pneumonia (excluding ventilator-associated pneumonia) and community-acquired pneumonia in adults. Early studies [190] were later on confirmed by applying EUCAST non-species-related breakpoints showing that CoNS from clinical specimens were 100% susceptible against ceftobiprole [191–193]. Importantly, this observation was also made in CoNS isolated from prosthetic joint infections [166,194]. Interestingly, in an animal model of biofilm-associated S. aureus infection, ceftaroline exhibited greater activity than vancomycin [181]. It will be of major interest to evaluate the potential activity of fifth-generation cephalosporins against biofilm-forming CoNS in animal models of infection.
Ceftobiprole medocaril for the treatment of community-acquired pneumonia
Published in Expert Opinion on Pharmacotherapy, 2018
Vicenç Falcó, Joaquin Burgos, Benito Almirante
Pharmacokinetics of ceftobiprole medocaril was studied in a double-blind, single-ascending-dose study with 40 healthy male subjects. The subjects were randomized to receive placebo or ceftobiprole medocaril as a 200-mL intravenous infusion over 30 min. The doses used were 125, 250, 500, 750, and 1000 mg [39]. The elimination half-life was about 3 h. More than 70% of the administered dose was excreted as ceftobiprole in the urine, and almost no prodrug was detected. After the infusion of 750 mg, the mean plasma ceftobiprole concentrations exceeded the minimal inhibitory concentration (MIC) at which 100% of MRSA isolates are inhibited for approximately 7 h or 58% of a 12-h dosing interval [5]. Pharmacokinetic data from a multiple-dose study with 16 healthy male volunteers who received 500 or 750 mg (as ceftobiprole equivalents) confirmed the same findings [40].