Drug General Information (ID: DDIO652ZBH)
  Drug Name Probenecid Drug Info Ceftaroline fosamil Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Uricosuric Agents Cephalosporins/Beta-Lactamase Inhibitors
  Structure

 Mechanism of Probenecid-Ceftaroline fosamil Interaction (Severity Level: Moderate)
     Competitive inhibition of renal tubular secretion Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Probenecid Ceftaroline fosamil
      Mechanism Competitive inhibition of renal tubular secretion of some cephalosporins Cephalosporins
      Key Mechanism Factor 1
Factor Name Renal tubular secretion
Factor Description Renal tubular secretion allows selective transfer of substances from the blood around the capillaries into the renal tubules via filtrate. Drug excretion may be reduced when two drugs compete for renal tubular secretion.
      Mechanism Description
  • Decreased elimination of Ceftaroline fosamil caused by Probenecid mediated competitive inhibition of renal tubular secretion

Recommended Action
      Management Although probenecid has been used therapeutically to enhance serum levels of various beta-lactam antibiotics, the potential for increased adverse effects should be considered when probenecid is added to existing cephalosporin therapy, particularly when the latter is given at high dosages or to patients who are elderly or have renal dysfunction. Adjustment of the cephalosporin dosage may be required in accordance with the individual product labeling. For example, cefotaxime dosage should generally not exceed 6 grams/day when administered with probenecid. Probenecid reportedly does not affect the elimination of ceftazidime or ceftriaxone.

References
1 DiPiro JT, Welage LS, Levine BA, et al. Single-dose cefmetazole versus multiple dose cefoxitin for prophylaxis in abdominal surgery.?J Antimicrob Chemother. 1989;23 Suppl D:71-77. [PMID: 2722725]
2 LeBel M, Paone RP, Lewis GP. Effect of probenecid on the pharmacokinetics of ceftizoxime.?J Antimicrob Chemother. 1983;12(2):147-155. [PMID: 6311785]
3 Product Information. Vantin (cefpodoxime proxetil). Pharmacia and Upjohn, Kalamazoo, MI.