Cefoxitin Levels in Human Aqueous Humor

Axelrod, Judith L.; Kochman, Richard S.

doi:10.1016/s0002-9394(14)74923-2

Cited by 20 publications

(2 citation statements)

References 18 publications

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“…However, the resulting CSF concentrations were not sufficient for clinical benefit (Liu et al 1979). The concentration of cefoxitin remained elevated in serum and aqueous humour when a single oral dose of probenecid 500mg was given 30 min before administration of intravenous cefoxitin 2000mg (Axelrod & Kochman 1980). These investigators suggested that probenecid also inhibited the organic anion pump that removes anions from the aqueous humour of the eye (Axelrod & Kochman 1980).…”

Section: Cefoxitinmentioning

confidence: 99%

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: Cefoxitinmentioning

confidence: 99%

Cephalosporin-Probenecid Drug Interactions

Brown

1993

Clinical Pharmacokinetics

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“…In a further 110 patients, the interval before sampling was varied in order to permit an emination of the kinetics of penetration. In another 10 patients, cefuroxime was given topically at the completion of surgery to assess the effect of a corneal wound on aqueous penetration. Cefuroxime concentrations were measured by high performance liquid chromatography on 0.2 ml samples of aqueous aspirated from the anterior chamber.…”

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confidence: 99%