Dicloxacillin and flucloxacillin: pharmacokinetics, protein binding and serum bactericidal titers in healthy subjects after oral administration.
The pharmacokinetics of dicloxacillin and flucloxacillin were studied in 12 healthy volunteers after oral administration. The participants received a single dose of either dicloxacillin (0.5 g, 0.75 g or 1.0 g) or flucloxacillin (0.75 g) in a cross-over fashion. Antibiotic concentrations were determined in serum and urine by bioassay and followed for 8 and 24 h, respectively. The three dicloxacillin dosages showed no significant differences for the serum elimination half-lives (t1/2 beta, median: 72 min). Comparing 0.75 g flucloxacillin with the same dose of dicloxacillin, no significant differences between the values of Cmax, t1/2 beta and AUC were found. Protein binding as determined by ultrafiltration in pooled serum was 94.7-96.2% for flucloxacillin and 96.4-97.2% for dicloxacillin. The serum bactericidal titers were similar for the two drugs. In conclusion, dicloxacillin and flucloxacillin showed similar pharmacokinetic behavior after 0.75 g doses in human volunteers.
Røder
B L
BL
Div. of Preventive Microbiology, Statens Seruminstitut, Copenhagen, Denmark.
Frimodt-Møller
N
N
Espersen
F
F
Rasmussen
S N
SN
D000284:Administration, Oral; D000328:Adult; D001798:Blood Proteins / Q000378:metabolism; D018592:Cross-Over Studies; D004009:Dicloxacillin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005436:Floxacillin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D011446:Prospective Studies; D011485:Protein Binding; D013211:Staphylococcus aureus / Q000187:drug effects; D014462:Ultrafiltration
D001798:Blood Proteins; D005436:Floxacillin; D004009:Dicloxacillin