Pharmacokinetic-pharmacodynamic target attainment and clinical outcomes
in patients treated with oral flucloxacillin plus probenecid
Abstract
Aim Oral flucloxacillin may be co-administered with probenecid to
increase flucloxacillin concentrations and increase attainment of
pharmacokinetic-pharmacodynamic (PK-PD) targets. The aims of this study
were to describe outcomes of patients treated with oral flucloxacillin
plus probenecid as follow-on therapy from initial intravenous treatment,
and to identify optimal dosing regimens when treating infections caused
by susceptible Gram-positive organisms. Methods We performed a
prospective observational study of adults treated with oral
flucloxacillin 1000 mg and probenecid 500 mg 8-hourly (with food) for
proven or probable staphylococcal infections. We developed a population
pharmacokinetic model of free flucloxacillin concentrations within
Monolix, in order to estimate probability of PK-PD target attainment
(fT>MIC), and used Monte Carlo simulation to explore
optimal dosing regimens. Results The 45 patients (73% male) had a
median (range) age of 49 years (20 – 74), weight of 90 kg (59 – 167),
fat free mass (Janmahasatian) of 65 kg (38 – 89) and eGFR (CKD-EPI) of
89 mL/min/1.73m2 (41 – 124). The most common infections were
osteomyelitis (n=18, 40%) and septic arthritis (n=12, 27%). Forty
patients (89%) were cured 30 days after completion of therapy. 10
(22%) experienced nausea which did not require treatment alternation.
Free flucloxacillin clearance depended on allometrically-scaled fat free
mass, and increased by 1% for each unit increase in eGFR. Conclusion
Oral flucloxacillin and probenecid was well-tolerated and efficacious.
Patients with higher fat free mass and eGFR may require four times daily
dosing and/or therapeutic drug monitoring to ensure PK-PD target
attainment.