Probenecid, an old β-lactams pharmacokinetic enhancer for a renewed use: A retrospective study

Infect Dis Now. 2022 Aug;52(5):273-279. doi: 10.1016/j.idnow.2022.05.006. Epub 2022 May 27.

Abstract

Background: Optimized antibiotic plasma predictor efficacy is essential in systemic infections. The uricosuric agent probenecid inhibits tubular excretion of antibiotics and may be used as β-lactam pharmacokinetic enhancer (BLPKE), even though few data are currently available for this purpose.

Methods: We conducted a monocentric and retrospective observational study including all patients who received probenecid in combination with parenteral β-lactam antibiotics for systemic infections from Jan 1, 2014 to Dec 31, 2019. Demographics, infection characteristics, treatment and ATC (antibiotics trough concentration) were investigated.

Results: All in all, 38 patients were included. Eight patients had a history of sickle cell disease. Hyperfiltration (defined as eGFR>130mL/min/1.73m2) was detected in twenty-one patients including six with sickle cell disease. Probenecid (500mg q6h orally) was added to antibiotics for a median (IQR) of 13 days (6.75-21.75), after a median (IQR) time lapse of 7 days (4-16) following the initiation of antibiotics. Probenecid was administered for low antibiotic trough concentration in 29 patients, for increased renal clearance in 5 patients and for persisting fever despite antibiotic therapy in 4 patients (including 1 infective relapse). A second plasma trough concentration, following probenecid administration, was available in 19 patients within a median (IQR) 3 days (2-5). Probenecid induced increased ATC in 18/19 patients (94.7%), with a median (IQR) change of +228.4% (IQR 38.7-633). No major adverse effects were reported.

Conclusion: Probenecid could be a BLPKE. Our data suggest this drug should be used more often to optimize β-lactam pharmacokinetics in clinical practice.

Keywords: Antibiotic; Pharmacokinetics; Probenecid; Renal hyperfiltration.

Publication types

  • Observational Study

MeSH terms

  • Anemia, Sickle Cell*
  • Anti-Bacterial Agents / therapeutic use
  • Humans
  • Probenecid* / pharmacokinetics
  • Probenecid* / therapeutic use
  • Retrospective Studies
  • beta-Lactams / therapeutic use

Substances

  • Anti-Bacterial Agents
  • beta-Lactams
  • Probenecid