Antimicrobial activity of Ro 15-8074, active metabolite of a new oral cephalosporin (Ro 15-8075), against 7,775 recent clinical isolates

Jones, Ronald N.; Fuchs, Peter; Barry, Arthur L.; Ayers, Leona W.; Gerlach, E.; Gavan, Thomas L.

doi:10.1128/aac.30.6.961

Cited by 20 publications

(2 citation statements)

References 10 publications

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“…These studies confirm the antimicrobial activities of these new cephalosporins (1,4,(9)(10)(11)13). However, their clinical usefulness will ultimately be determined by the pharmacokinetics of orally administered formulations.…”

supporting

confidence: 77%

Preliminary antimicrobial susceptibility interpretive criteria for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) disk tests

Jones¹,

Barry²

1987

J Clin Microbiol

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Preliminary interpretive zone criteria were calculated for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) by using 10and 30-,ig disks and three possible MIC susceptibility breakpoints. Absolute interpretive agreement between MICs and zone size criteria ranged from 91.8 to 97.2%. Very major errors (false susceptibility) were s1.2% for both cephalosporin disk tests. Morganella morganii strains appeared to produce the highest rates of very major interpretive errors with cefetamet disks. Cefetamet (formerly Ro 15-8075) and cefteram (formerly Ro 19-5248 and T-2588) are orally administered cephalosporin pivoxyl esters which, as free acids, possess an antimicrobial activity most similar to that of céfixime (1, 4, 5, 9-11, 13). Each free acid (Ro 15-8074 and Ro 19-5247 or T-2525) has been linked to form the pivaloyloxymethylester that allows gastrointestinal tract absorption but produces a somewhat lower concentration in serum than do currently available cephalosporins (12; data on file at Hoffmann-La Roche, Inc., Nutley, N.J.). Even with these lower drug levels in blood, cefetamet and cefteram have sufficient potency to cover members of the family Enterobacteriaceae, Haemophilus influenzae, pathogenic neisseriae, Branhamella catarrhalis, and most streptococci (1, 4, 9-11, 13). In this brief report, we compare the antimicrobial activities of the free acids of these two new orally administered cephalosporins. We additionally present the preliminary determinations of disk diffusion test interpretive criteria with 10and 30-pLg cefetamet and cefteram disks. Cefetamet and cefteram were provided by Hoffmann-La Roche, Inc. (R. Cleeland). Both drugs were tested in cationsupplemented Mueller-Hinton broth by dilution methods described by the National Committee for Clinical Laboratory Standards (8). Additional medium supplementation for fastidious organisms was prepared according to the National Committee for Clinical Laboratory Standards M7-A recommendations (8). The disk diffusion tests were also performed by National Committee for Clinical Laboratory Standards procedures (7) by using 10-and 30-,ug disks prepared by the investigators to 110% of the stated potency. Regression analyses were calculated by the least-squares method as adapted to a computer by using the zone diameter as the independent variable. The error rates were calculated for three possible susceptibility MIC breakpoints to try to minimize the false-susceptibility error rate to s1.0% (6).

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supporting

confidence: 77%

Preliminary antimicrobial susceptibility interpretive criteria for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) disk tests

Jones¹,

Barry²

1987

J Clin Microbiol

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“…The pivoxit ester bond is cleaved on the first passage of the orally administered compound through the intestinal mucosa and/or the liver, liberating the respective microbiologically active carboxylic acid (10). In view of the plasma concentrations achievable with cefetamet pivoxil in humans (10) and the MICs obtained with cefetamet in this and other studies (11,12,(18)(19)(20), cefetamet pivoxil may prove useful in treatment of infections with streptococci other than enterococci, Enterobacteriaceae, Haemophilus spp., Branhamella catarrhalis, Neisseria spp. and Vibrio spp.…”

Section: Discussionmentioning

confidence: 95%

In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil

Angehrn

Hohl

Then

1989

Eur. J. Clin. Microbiol. Infect. Dis.

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The in vitro activity of cefetamet, the microbiologically active metabolite of the orally administered prodrug cefetamet pivoxil, was compared with that of cephalexin, cefaclor, cefuroxime and amoxicillin. Cefetamet was highly active against Enterobacteriaceae, Neisseria spp., Vibrio spp., Haemophilus influenzae and streptococci other than enterococci. Cefetamet inhibited cefaclor-resistant species such as Proteus vulgaris, Providencia stuartii, Providencia rettgeri and Serratia marcescens. Staphylococci, Pseudomonas aeruginosa and cephalosporinase-overproducing strains of Enterobacter cloacae were resistant to cefetamet. The superior activity of cefetamet compared with older oral beta-lactam antibiotics against a large number of gram-negative pathogens correlated with enhanced stability towards beta-lactamases. In accordance with the in vitro findings, cefetamet pivoxil showed good activity in experimental infections in the mouse and rat, suggesting satisfactory bioavailability in these animals after oral administration.

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The bacterium Xanthomonas

1993

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Antimicrobial activity of Ro 15-8074, active metabolite of a new oral cephalosporin (Ro 15-8075), against 7,775 recent clinical isolates

Cited by 20 publications

References 10 publications

Preliminary antimicrobial susceptibility interpretive criteria for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) disk tests

Preliminary antimicrobial susceptibility interpretive criteria for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) disk tests

In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil

The bacterium Xanthomonas

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