Single- and multiple-dose pharmacokinetics of oral moxifloxacin and clarithromycin, and concentrations in serum, saliva and faeces

被引:30
作者
Burkhardt, O
Borner, K
Stass, H
Beyer, G
Allewelt, M
Nord, CE
Lode, H
机构
[1] Chest Hosp Heckeshorn, Dept Chest & Infect Dis, DE-14109 Berlin, Germany
[2] Free Univ Berlin, Univ Hosp Benjamin Franklin, Inst Clin Chem & Pathobiochem, D-1000 Berlin, Germany
[3] Bayer AG, Pharma Res Ctr, D-5600 Wuppertal, Germany
[4] Karolinska Inst, Huddinge Univ Hosp, Stockholm, Sweden
关键词
D O I
10.1080/0036554021000026963
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
Moxifloxacin and clarithromycin are important antibacterial drugs in the treatment of community-acquired respiratory tract infections. In a double-blind, randomized, 2-period cross-over study the pharmacokinetics of moxifloxacin versus clarithromycin were determined after single and multiple doses in 12 healthy male volunteers. The concentrations of the antibiotics in serum, saliva and faeces were measured by validated high-performance liquid chromatographic methods. In serum, moxifloxacin exhibited a mean peak concentration of 3.1 +/- 0.6 mg/l after a time to peak concentration of 1.67 +/- 0.96 h on day 1, with a significant increase to 3.98 +/- 1.10 mg/l on day 7 ( p < 0.05). The area under the curve-12 revealed a highly significant increase from 28.2 +/- 4.1 mg*h/l on day 1 to 39.5 +/- 6.6 mg*h/l on day 7 ( p < 0.01). There were also significant differences in terminal half-life between day 1 and day 7 [10.6 h (range 9.0-12.8) vs 14.9 h (range 12.6-28.1); p < 0.01] and in mean residence time (15.1 +/- 1.9 vs 18.2 +/- 2.4 h; p < 0.01). The concentrations of moxifloxacin in saliva were well equilibrated with serum at a relatively constant saliva-serum ratio of about 0.8. Pharmacokinetic parameters of clarithromycin and its metabolite, 14-hydroxy-clarithromycin, were similar to previously published data. Accumulation was found. No serious adverse events were observed with either study drug.
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页码:898 / 903
页数:6
相关论文
共 23 条
[1]   INVITRO ACTIVITY OF A NEW MACROLIDE, A-56268, COMPARED WITH THAT OF ROXITHROMYCIN, ERYTHROMYCIN, AND CLINDAMYCIN [J].
BARRY, AL ;
THORNSBERRY, C ;
JONES, RN .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1987, 31 (02) :343-345
[2]  
BARTLETT JG, 1995, NEW ENGL J MED, V333, P1619
[3]   Impact of moxifloxacin versus clarithromycin on normal oropharyngeal microflora [J].
Beyer, G ;
Hiemer-Bau, M ;
Ziege, S ;
Edlund, C ;
Lode, H ;
Nord, CE .
EUROPEAN JOURNAL OF CLINICAL MICROBIOLOGY & INFECTIOUS DISEASES, 2000, 19 (07) :548-550
[4]  
BORNER K, 1992, METH SURV A, V22, P137
[5]   CORRELATION BETWEEN PHARMACOKINETICS, PHARMACODYNAMICS AND EFFICACY OF ANTIBACTERIAL AGENTS IN ANIMAL-MODELS [J].
DALHOFF, A ;
ULLMANN, U .
EUROPEAN JOURNAL OF CLINICAL MICROBIOLOGY & INFECTIOUS DISEASES, 1990, 9 (07) :479-487
[6]   In vitro activity of BAY 12-8039, a new 8-methoxyquinolone [J].
Dalhoff, A ;
Petersen, U ;
Endermann, R .
CHEMOTHERAPY, 1996, 42 (06) :410-425
[7]  
Edlund C, 2000, SCAND J INFECT DIS, V32, P81, DOI 10.1080/00365540050164272
[8]  
FASSBENDER M, 1995, CLIN MICROBIOL INFEC, V1, P235
[9]   DEVELOPMENT OF A POPULATION PHARMACOKINETIC MODEL AND OPTIMAL SAMPLING STRATEGIES FOR INTRAVENOUS CIPROFLOXACIN [J].
FORREST, A ;
BALLOW, CH ;
NIX, DE ;
BIRMINGHAM, MC ;
SCHENTAG, JJ .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1993, 37 (05) :1065-1072
[10]   PHARMACODYNAMICS OF INTRAVENOUS CIPROFLOXACIN IN SERIOUSLY ILL-PATIENTS [J].
FORREST, A ;
NIX, DE ;
BALLOW, CH ;
GOSS, TF ;
BIRMINGHAM, MC ;
SCHENTAG, JJ .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1993, 37 (05) :1073-1081