The efficacy of cefuroxime for the treatment of acute gonorrhoea in men.

Price, John; Fluker, J. L.

doi:10.1136/sti.54.3.165

Cited by 11 publications

(7 citation statements)

References 16 publications

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“…This regimen had produced only a 2% failure rate in a previous study (Sanchez et al 1983). Intramuscular cefuroxime 1.5g in combination with oral probenecid 19 produced failure rates of 1.5% (Price & Gluker 1978), 2.8% (Morrison et al 1980) and 4.0% (Lossick et al 1982). Similar rates were seen with 750mg and 19 doses of cefuroxime (Fowler et al 1978;Morrison et al 1980;Price & Gluker 1978).…”

Section: Gonorrhoeasupporting

confidence: 78%

“…Intramuscular cefuroxime 1.5g in combination with oral probenecid 19 produced failure rates of 1.5% (Price & Gluker 1978), 2.8% (Morrison et al 1980) and 4.0% (Lossick et al 1982). Similar rates were seen with 750mg and 19 doses of cefuroxime (Fowler et al 1978;Morrison et al 1980;Price & Gluker 1978). The site of infection did not appear to influence the failure rate (Lossick et al 1982), although pharyngeal gonorrhoea was associated with a very high failure rate (46%) in I ,.report (Graudal et al 1985).…”

Section: Gonorrhoeasupporting

confidence: 74%

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Cephalosporin-Probenecid Drug Interactions

Brown

1993

Clinical Pharmacokinetics

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The effect of concurrent probenecid administration on the pharmacokinetics of cephalosporin antibiotics varies with the available cephalosporins. Most cephalosporins are affected to some degree by concurrent probenecid administration, although ceforanide, ceftazidime, ceftriaxone and latamoxef (moxalactam) have no significant changes in pharmacokinetics. For those cephalosporins affected by probenecid, the predominant findings are impairment in renal clearance resulting in increased peak serum concentrations, an increased area under the concentration-time curve (AUC), and both delayed and prolonged recovery of the cephalosporin in the urine. The distribution of the cephalosporins is affected to varying degrees, with reports of increased penetration into ocular, central nervous system and blister fluids noted with some agents. The clinical relevance of the changes in cephalosporin distribution associated with probenecid administration has not been investigated. The dose and timing of probenecid administration appear to be major determinants in any possible interaction. Studies with ceftizoxime and cefoxitin suggest that larger probenecid doses result in greater changes in the pharmacokinetics of cephalosporins. Prolonged probenecid therapy before administration of a cephalosporin did not seem to be as relevant as the probenecid dosage in determining the magnitude of the interaction. Probenecid administration with or immediately before cephalosporin administration appears able to produce these documented changes in cephalosporin pharmacokinetics. The route of administration (oral versus parenteral) of either prolosporin pharmacokinetics. The route of administration (oral versus parenteral) of either probenecid or the cephalosporin does not appear to influence the characteristics of the interactions. The therapeutic efficacy of a combination of a cephalosporin with probenecid has been most thoroughly studied for single-dose treatment of gonorrhoea. The addition of probenecid to cephalosporin therapy results in sustained systemic concentrations adequate for eradication of Neisseria gonorrhoeae. Regimens involving either second or third generation cephalosporins demonstrate good success rates with single-dose therapy. However, the success of ceftriaxone administered alone for treatment of both penicillase-producing and non-penicillase-producing strains of N. gonorrhoeae suggests that the addition of probenecid is unnecessary. The use of probenecid, in combination with cephalosporins, to enhance the treatment of other venereal and systemic infections has preliminary, inconclusive support.

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Section: Gonorrhoeasupporting

confidence: 78%

Section: Gonorrhoeasupporting

confidence: 74%

Cephalosporin-Probenecid Drug Interactions

Brown

1993

Clinical Pharmacokinetics

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“…Although a number of new P-lactam antibiotics have been reported to show promising in vitro and in vivo activities (2,3,6,8,9), few can be administered orally. Of these drugs, cefaclor and amoxicillin-clavulanic acid (Augmentin) have been reported to be active against PPNG strains both in vitro and in vivo (4,10).…”

mentioning

confidence: 99%

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

Ng¹,

Chau²,

Leung³

et al. 1985

Antimicrob Agents Chemother

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Ro 15-8074, a new cephalosporin the pivaloyloxymethylester of which (Ro 15-8015) is orally absorbable, showed greater in vitro activity than cefaclor ngainst 48 Neisseria gonorrhoeae strains, including 25 penicillinase-producing strains. Unlike cefaclor, Ro 15-8074 was unaffected by increase in ihoculum size, and it exhibited a remarkable stability against gonococcal P-lactamase hydrolysis.The emergence of penicillinase-producing Neisseria gonorrhoeae (PPNG) strains showing high resistance to penicillin has prompted the search for effective alternative drugs against these isolates. Although a number of new P-lactam antibiotics have been reported to show promising in vitro and in vivo activities (2,3,6,8,9), few can be administered orally. Of these drugs, cefaclor and amoxicillin-clavulanic acid (Augmentin) have been reported to be active against PPNG strains both in vitro and in vivo (4, 10). In this study, therefore, we evaluated the in vitro activity of Ro 15-8074 in comnparison with those of cefaclor and amoxicillin-clavulanic acid against N. gonorrhoeae strains and also tested their hydrolytic stability to gonococcal P-lactamase. Ro 15-8074 is an aminothiazolyl-2-methoxyiminoacetamido-3-desacetoxy cephalosporanic acid, and its pivaloyloxymethylester, Ro 15-8075, is orally absorbable. After absorptioh, the ester group of Ro 15-8075 is enzymatically split off the cephalosporin ring, giving rise to the active cephalosporanic acid Ro 15-8074 (Fig. 1).The 48 N. gonorrhoeae strains tested were clinical isolates NH2

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“…There is good clinical trial evidence for the efficacy of ceftriaxone 250 mg intramuscular and cefixime 400 mg oral in gonorrhoea, and to show that these regimens are equivalent in efficacy. 17 There are also small, rather old, trials to support the use of cefuroxime 1.5 g intramuscular 18 and cefuroxime axetil 1 g oral. 19 We cannot, however, find formal validation of cefuroxime axetil at 200 mg in gonorrhoea, and one study found cefuroxime 1.0 g oral inferior to ciprofloxacin for gonococcal urethritis in men, though not for cervical infection in women.…”

Section: Discussionmentioning

confidence: 99%

Which cephalosporin for gonorrhoea?

Ison¹

2004

Sexually Transmitted Infections

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The recommended treatment for gonorrhoea in the United Kingdom has, until recently, included the fluoroquinolone, ciprofloxacin, which consequently was used by most genitourinary medicine clinics. In 2002 national surveillance data showed that resistance to ciprofloxacin had risen to a prevalence of 9. 8% (9% in 2003), indicating that the target of .95% efficacy in first line therapy was no longer achievable. The third generation cephalosporins, ceftriaxone (intramuscular) or cefixime (oral), are the recommended alternatives, but recent audit data reveal other cephalosporins are currently being used to treat gonorrhoea, notably including cefuroxime (intramuscular or, often, oral). A pharmacodynamic analysis was undertaken to determine whether all these regimens were equally potent. Ceftriaxone, 250 (or 500) mg intramuscularly, or cefixime, 400 mg orally, were calculated to give free drug concentrations above the MIC 90 for 22-50 hours post dose whereas the cefuroxime regimens being used were pharmacodynamically borderline, achieving this target for only 6.8-11.2 hours and raising the spectre that continued use may select for stepwise increases in resistance, as occurred with penicillin. We therefore underscore that ceftriaxone or cefixime should be the agents of choice to replace ciprofloxacin, as recommended in the new treatment guidelines, and that cefuroxime is a poor substitute.

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The efficacy of cefuroxime for the treatment of acute gonorrhoea in men.

Cited by 11 publications

References 16 publications

Cephalosporin-Probenecid Drug Interactions

Cephalosporin-Probenecid Drug Interactions

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

Which cephalosporin for gonorrhoea?

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