In vitro activity of Ro 15-8074, a new oral cephalosporin, against Neisseria gonorrhoeae

Ng, W. S.; Chau, Pui Hing; Leung, Y. K.; Wong, Pak-Kin

doi:10.1128/aac.28.3.461

Cited by 19 publications

(8 citation statements)

References 9 publications

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“…The compounds were much more active than cefaclor or cephalexin against H. influenzae and N. gonorrhoeae and inhibited beta-lactamase-producing isolates of these species. Our results are similar to those of Ng et al (5) against N. gonorrhoeae.…”

Section: Resultssupporting

confidence: 82%

In vitro activity and beta-lactamase stability of two oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074)

Neu¹,

Chin²,

Labthavikul³

1986

Antimicrob Agents Chemother

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Ceftetrame and cefetamet (Ro 15-8074), two new orally administered aminothiazolyl imimomethoxy cephalosporins, inhibited hemolytic streptococci and Streptococcus pneumoniae at .0.5 ,ug/ml but were less active against staphylococci than were cephalexin and cefaclor. They did not inhibit S. faecalis, S. faecium, Listeria monocytogenes, Corynebacterium JK species, or Pseudomonas aeruginosa. Haemophilus influenzae, Branhamella catarrhalis, and Neisseria gonorrhoeae, including ampicillin-resistant isolates, were inhibited at <0.25 ,ug/ml. Both agents inhibited Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Proteus mirabilis, Salmonella species, Shigella species, Citrobacter diversus, and Aeromonas hydrophila resistant to ampicillin, cephalexin, and cefaclor at .2 ,ug/ml, although many isolates of Enterobacter cloacae, Citrobacter freundii, and Serratia marcescens resistant to cefotaxime were not inhibited by these agents. A marked inoculum effect was noted for Enterobacteriaceae carrying the Richmond-Sykes type 1A chromosomally mediated beta-lactamases, but plasmid-mediated beta-lactamases did not hydrolyze the compounds. Both drugs inhibited the chromosomally mediated beta-lactamase of E. cloacae, P99. Although there has been great progress in the development of parenteral cephalosporins stable to attack by betalactamases and active against a wide spectrum of grampositive and -negative bacteria, this goal has not been achieved for oral cephalosporins (2). The early oral cephalosporins, cephalexin and cephradine, although moderately stable to attack by beta-lactamases, have had relatively poor activity against important respiratory pathogens such as Haemophilus influenzae and Br-anhacmellai catarrhalis (1, 7). Furthermore, their activity against Streptococcus pneiumoniae is significantly lower than that of the parenteral cephalosporins, and these compounds do not inhibit many beta-

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Section: Resultssupporting

confidence: 82%

In vitro activity and beta-lactamase stability of two oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074)

Neu¹,

Chin²,

Labthavikul³

1986

Antimicrob Agents Chemother

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“…Studies reported elsewhere showed Ro 15-8074 to be very active against H. influenzae and Neisseria gonorrhoeae, including P-lactanmase-producing strains (7,9,10,13 …”

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confidence: 99%

“…The 7'-substitutions provide for an increased Ro 15-8074 antimicrobial activity against the Enterobacteriaceae, Haemophilus influenzae, and Neisseria spp. compared with currently available orally administered cephalosporins (2,7,(9)(10)(11)). An additional feature of Ro 15-8074 is its P-lactamase stability (9).…”

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confidence: 99%

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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

Jones¹,

Fuchs²,

Barry³

et al. 1986

Antimicrob Agents Chemother

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“…Other workers have found that Ro 15-8074/001 is more active than cefaclor, cefadroxil, ampicillin, and TMP-SMX against the Enterobacteriaceae (2) and more active than amoxicillin-clavulanic acid and cefaclor against pencillinase-producing and nonpenicillinaseproducing Neisseria gonorrhoeae (1). Further studies are indicated to determine the clinical efficacy of this new oral cephalosporin.…”

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confidence: 99%

Antimicrobial spectrum of Ro 15-8074/001, a new oral cephalosporin

Thomas¹,

Lang²

1986

Antimicrob Agents Chemother

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The activity of Ro 15-8074/001 was compared with that of cefaclor, amoxicillin-clavulanic acid, trimethoprim-sulfamethoxazole, norfloxacin, and ceftriaxone against 225 clinical isolates. It was more active than cefaclor, amoxicillin-clavulanic acid, and trimethoprim-sulfamethoxazole against members of the family Enterobacteriaceae and Haemophilus influenzae and had activity similar to that of cefaclor against nonenterococcal streptococci. It was not usefully active against Pseudomonas aeruginosa, Streptococcusfaecalis, or most isolates of staphylococci.Ro 15-8075 (Fig. 1A) is the pivaloylomethoxyester of an aminothiazolyl cephalosporin. After oral administration and absorption the ester group is enzymatically split to produce the free acid Ro 15-8074 (Fig. 1B). Peak levels in serum of 5 ,ug of Ro 15-8074 per ml are achieved following oral administration of 1 g of Ro 15-8075, and 80 to 100% of the free acid is excreted in the urine over the first 24 h. When administered to mice with experimental infections due to a range of gram-positive or -negative organisms, curative doses for 50% (of mice) of Ro 15-8075 were 5 to 100 times lower than those of cephalexin (data on file, F. Hoffmann-La Roche and Co. Ltd., Basel, Switzerland). We used the sodium salt (Ro 15-8074/001) of the free acid to compare the activity of this compound with that of four other oral antibiotics and ceftriaxone against a variety of bacteria.Ro 15-8074/001 was a gift from F. Hoffman-La Roche. All other antibiotics were donated by their respective manufacturers. Antimicrobial activity was determined by an agar dilution method with fresh serial dilutions of compounds prepared according to the instructions of the manufacturer. The inoculum was prepared from a fresl overnight broth culture adjusted to a McFarland 0.5 standard and then diluted to deliver 105 CFU with a replicating spot device. Haemophilus influenzae and nonenterococcal streptococci were tested on Mueller-Hinton agar supplemented with 5% chocolatized horse blood and 1% IsoVitaleX (BBL Microbiology Systems, Cockeysville, Md.) incubated in 8% C02 at 37°C for 18 h. All other isolates were tested on MuellerHinton agar incubated in air at 37°C for 18 h. Serial dilutions of trimethoprim-sulfamethoxazole (TMP-SMX) were supplemented with 5% lysed horse blood. Susceptibility to amoxicillin-clavulanic acid was determined by using a constant ratio of amoxicillin to clavulanic acid of 2:1.The

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In vitro activity of Ro 15-8074, a new oral cephalosporin, against Neisseria gonorrhoeae

Cited by 19 publications

References 9 publications

In vitro activity and beta-lactamase stability of two oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074)

In vitro activity and beta-lactamase stability of two oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074)

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

Antimicrobial spectrum of Ro 15-8074/001, a new oral cephalosporin

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