Single oral dose pharmacokinetics of the two main components of pristinamycin in humans

A preliminary study of the pharmacokinetics of the two main components of pristinamycin, PIA and PIIA is reported. A single oral dose of 2 g of pristinamycin was administered to six patients with normal renal and hepatic function. The samples were withdrawn during 9·5 h and assayed by HPLC. PIA and...

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Bibliographic Details
Published in:Journal of antimicrobial chemotherapy 1990-04, Vol.25 (4), p.651-656
Main Authors: Koechlin, Christophe, Kempf, Jean-François, Jehl, François, Monteil, Henri
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Aged
Aged, 80 and over
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Chromatography, High Pressure Liquid
Female
Half-Life
Humans
Male
Medical sciences
Middle Aged
Pharmacology. Drug treatments
Virginiamycin - administration & dosage
Virginiamycin - blood
Virginiamycin - pharmacokinetics
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Summary:A preliminary study of the pharmacokinetics of the two main components of pristinamycin, PIA and PIIA is reported. A single oral dose of 2 g of pristinamycin was administered to six patients with normal renal and hepatic function. The samples were withdrawn during 9·5 h and assayed by HPLC. PIA and PIIA plasma levels evolved in parallel in each subject and their kinetic parameters were comparable: Tmax of 3·25± 1·80 h and 3·08± 1·98 h, Cmax of 0·760±0·427 mg/l and 0·581±0·285mg/l, elimination half-life of 4·03±2·77 h−1 and 2·83±0·75 h−1 respectively. The relative proportions of PIA and PIIA, which govern the antibacterial activity of the mixture, were maintained during the study in the range of values leading to 90–100% of optimal activity against Staphylococcus aureus. The sum of the plasma concentrations of PIA and PIIA, which can be considered to be equivalent to the concentration of total pristinamycin, was superior to the MICs for the most susceptible staphylococal strains during the entire period of study. On the other hand, the sum of PIA and PIIA concentrations exceeded the MICs for the less susceptible strains for only 4 h. These results differ from the scanty pharmacokinetic data presently available, which were obtained by microbiological methods.
ISSN:0305-7453
1460-2091
DOI:10.1093/jac/25.4.651