Journal of Antimicrobial Chemotherapy (1999) 43, Suppl. B, 83-90
© 1999 The British Society for Antimicrobial Chemotherapy
Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man
Pharma Research Center, Institute of Clinical Pharmacology, Bayer AG, 42096 Wuppertal, Germany
The pharmacokinetics of moxifloxacin and its metabolites M1 (sulpho-compound) and M2 (acyl-glucuronide) were characterized in 12 healthy male volunteers in an open, randomized, crossover study. After an overnight fast the volunteers were given a single 400 mg dosage of moxifloxacin either as a tablet or a 1 h infusion with a washout phase of at least 1 week between the two treatments. Multiple plasma, faeces and urine samples were collected for the analysis of moxifloxacin and metabolites using validated HPLC with fluorescence detection. The AUC for both formulations was comparable with bioequivalence criteria fulfilled, with C max after oral treatment approximately 31% lower. Following oral administration, absorption was fast with low to medium variability (mean dissolution and absorption time 2.4 h). The absolute bioavailability was 86%. The excretion of moxifloxacin and its metabolites was quantified in a subset of eight subjects. More than 96% of the dose was recovered from urine and faeces after oral dosing, and >98% following iv administration of the drug. M1, which is strongly bound to plasma proteins (90%), was mainly eliminated into faeces (approximately 37–38% of the administered dose) and to a minor extent into urine (2.5% of the administered dose) by active tubular secretion. M2 (only 5% bound to plasma protein) was only found in urine, where it amounted to approximately 14% of the dose. Plasma concentrations of the metabolites were much lower than those of the parent compound. Moxifloxacin was well tolerated with few adverse events and no clinically relevant changes in laboratory values.
* Tel: +49-202-364289; Fax: +49-202-368998; E-mail: heino.stass.hs{at}bayer.ag.de
CiteULike 
Connotea 
Del.icio.us What's this?
This article has been cited by other articles:
|
|
 |
|
  C. Skalioti, T. Tsaganos, D. Stamatiadis, E. J. Giamarellos-Bourboulis, J. Boletis, and K. Kanellakopoulou PHARMACOKINETICS OF MOXIFLOXACIN IN PATIENTS UNDERGOING CONTINUOUS AMBULATORY PERITONEAL DIALYSIS Perit. Dial. Int., September 1, 2009; 29(5): 575 - 579. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Malik, K. Hnatkova, A. Schmidt, and P. Smetana Electrocardiographic QTc Changes Due to Moxifloxacin Infusion J. Clin. Pharmacol., June 1, 2009; 49(6): 674 - 683. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. B. Landersdorfer, M. Kinzig, F. F. Hennig, J. B. Bulitta, U. Holzgrabe, G. L. Drusano, F. Sorgel, and J. Gusinde Penetration of Moxifloxacin into Bone Evaluated by Monte Carlo Simulation Antimicrob. Agents Chemother., May 1, 2009; 53(5): 2074 - 2081. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. van den Boogaard, G. S. Kibiki, E. R. Kisanga, M. J. Boeree, and R. E. Aarnoutse New Drugs against Tuberculosis: Problems, Progress, and Evaluation of Agents in Clinical Development Antimicrob. Agents Chemother., March 1, 2009; 53(3): 849 - 862. [Full Text] [PDF]
|
|
|
|
 |
|
 J. Barth, D. Jager, R. Mundkowski, B. Drewelow, T. Welte, and O. Burkhardt Single- and multiple-dose pharmacokinetics of intravenous moxifloxacin in patients with severe hepatic impairment J. Antimicrob. Chemother., September 1, 2008; 62(3): 575 - 578. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. Ayalasomayajula, C.-M. Yeh, S. Vaidyanathan, B. Flannery, H. A. Dieterich, D. Howard, M. P. Bedigian, and W. P. Dole Effects of Aliskiren, a Direct Renin Inhibitor, on Cardiac Repolarization and Conduction in Healthy Subjects J. Clin. Pharmacol., July 1, 2008; 48(7): 799 - 811. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 T. F. Murphy, A. L. Brauer, K. Eschberger, P. Lobbins, L. Grove, X. Cai, and S. Sethi Pseudomonas aeruginosa in Chronic Obstructive Pulmonary Disease Am. J. Respir. Crit. Care Med., April 15, 2008; 177(8): 853 - 860. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. K. Olofsson, L. L. Marcusson, A. Stromback, D. Hughes, and O. Cars Dose-related selection of fluoroquinolone-resistant Escherichia coli J. Antimicrob. Chemother., October 1, 2007; 60(4): 795 - 801. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. Grossi, J. Caillon, C. Arvieux, C. Jacqueline, D. Bugnon, G. Potel, and A. Hamel In Vivo Efficacy of Moxifloxacin Compared with Cloxacillin and Vancomycin in a Staphylococcus aureus Rabbit Arthritis Experimental Model Antimicrob. Agents Chemother., September 1, 2007; 51(9): 3401 - 3403. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Weiner, W. Burman, C.-C. Luo, C. A. Peloquin, M. Engle, S. Goldberg, V. Agarwal, and A. Vernon Effects of Rifampin and Multidrug Resistance Gene Polymorphism on Concentrations of Moxifloxacin Antimicrob. Agents Chemother., August 1, 2007; 51(8): 2861 - 2866. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
I. Odenholt and O. Cars Pharmacodynamics of moxifloxacin and levofloxacin against Streptococcus pneumoniae, Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli: simulation of human plasma concentrations after intravenous dosage in an in vitro kinetic model J. Antimicrob. Chemother., November 1, 2006; 58(5): 960 - 965. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. Wacke, S. Forster, U. Adam, R. G. Mundkowski, E. Klar, U. T. Hopt, and B. Drewelow Penetration of moxifloxacin into the human pancreas following a single intravenous or oral dose J. Antimicrob. Chemother., November 1, 2006; 58(5): 994 - 999. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. Alou, M.-J. Gimenez, D. Sevillano, L. Aguilar, F. Cafini, O. Echeverria, E. Perez-Trallero, and J. Prieto A pharmacodynamic approach to antimicrobial activity in serum and epithelial lining fluid against in vivo-selected Streptococcus pneumoniae mutants and association with clinical failure in pneumonia J. Antimicrob. Chemother., August 1, 2006; 58(2): 349 - 358. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Wirtz, J. Kleeff, S. Swoboda, I. Halaceli, H. K. Geiss, T. Hoppe-Tichy, M. W. Buchler, and H. Friess Moxifloxacin penetration into human gastrointestinal tissues J. Antimicrob. Chemother., May 1, 2004; 53(5): 875 - 877. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. J. M. Lenaerts, V. Gruppo, J. V. Brooks, and I. M. Orme Rapid In Vivo Screening of Experimental Drugs for Tuberculosis Using Gamma Interferon Gene-Disrupted Mice Antimicrob. Agents Chemother., February 1, 2003; 47(2): 783 - 785. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. J. Giamarellos-Bourboulis, L. Karnesis, I. Galani, and H. Giamarellou In Vitro Killing Effect of Moxifloxacin on Clinical Isolates of Stenotrophomonas maltophilia Resistant to Trimethoprim-Sulfamethoxazole Antimicrob. Agents Chemother., December 1, 2002; 46(12): 3997 - 3999. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Yoshimatsu, E. Nuermberger, S. Tyagi, R. Chaisson, W. Bishai, and J. Grosset Bactericidal Activity of Increasing Daily and Weekly Doses of Moxifloxacin in Murine Tuberculosis Antimicrob. Agents Chemother., June 1, 2002; 46(6): 1875 - 1879. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
I. Odenholt, E. Lowdin, I. Gustafsson, and O. Cars Pharmacodynamics of Moxifloxacin against Streptococcus pyogenes in an In Vitro Kinetic Model Antimicrob. Agents Chemother., June 1, 2002; 46(6): 2046 - 2048. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
B. Lindner, A. Wiese, K. Brandenburg, U. Seydel, and A. Dalhoff Lack of Interaction of Fluoroquinolones with Lipopolysaccharides Antimicrob. Agents Chemother., May 1, 2002; 46(5): 1568 - 1570. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
N. Lounis, A. Bentoucha, C. Truffot-Pernot, B. Ji, R. J. O'Brien, A. Vernon, G. Roscigno, and J. Grosset Effectiveness of Once-Weekly Rifapentine and Moxifloxacin Regimens against Mycobacterium tuberculosis in Mice Antimicrob. Agents Chemother., December 1, 2001; 45(12): 3482 - 3486. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. H. Williams Jr Fluoroquinolones for Respiratory Infections : Too Valuable To Overuse Chest, December 1, 2001; 120(6): 1771 - 1775. [Full Text] [PDF]
|
|
|
|
 |
|
 S. Sethi and T. F. Murphy Bacterial Infection in Chronic Obstructive Pulmonary Disease in 2000: a State-of-the-Art Review Clin. Microbiol. Rev., April 1, 2001; 14(2): 336 - 363. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
G. L. Mandell and E. J. Coleman Activities of Antimicrobial Agents against Intracellular Pneumococci Antimicrob. Agents Chemother., September 1, 2000; 44(9): 2561 - 2563. [Abstract] [Full Text]
|
|