Garraffo R, Bernard E, Leclercq-Boscherel B, Garret C, Bidault R, Etesse H, Dellamonica P; Interscience Conference on Antimicrobial Agents and Chemotherapy.
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 1999 Sep 26-29; 39: 47 (abstract no. 1926).
Univ. Hosp., Nice
GFX is a new fluoroquinolone with a high tissue and intracellular distribution. An in vitro study has previously shown an intra/extracellular concentration ratio of 66.2 at 37 degrees C after an incubation time of 30 minutes. The objective of this study was to assess the in vivo intracellular penetration of GFX and to compare its plasma PK at steady-state with its PK in human polymorphonuclear leukocytes (PMN[s]). Twelve healthy volunteers (6 males and 6 females) received 600 mg of GFX once daily for 7 days. Blood samples were collected on day 7 at different times over 48 h. Plasma and PMN[s] concentrations of GFX were assayed by HPLC with fluorescence detection. The limit of quantification was 0.01 mg/L. PK parameters of GFX in plasma and PMNs were compared with ANOVA and Wilcoxon test. [table: see text] As with in vitro results, these data show that GFX highly concentrates into human neutrophils. The large uptake of GFX by PMNs combined with a prolonged intracellular half-life support the once daily dosing and its interest in the treatment of infections caused by susceptible intracellular pathogens such as Chlamydia, Mycoplasma and Legionella species.
Publication Types:
Keywords:
- Animals
- Chromatography, High Pressure Liquid
- Female
- Fluoroquinolones
- Half-Life
- Humans
- In Vitro
- Male
- Neutrophils
- Piperazines
- Plasma
- grepafloxacin
- pharmacokinetics
Other ID:
UI: 102244648
From Meeting Abstracts