Vol.59 No.S-1 May 2011
Evaluation of regimens reducing injection site reaction by intravenous levofloxacin in healthy subjects
1)Jikei University School of Medicine, 3-25-8 Nishi-Shinbashi, Minato-ku, Tokyo, Japan
2)R&D Division, Daiichi Sankyo Company, Limited
3)Development Division, Inforward Incorporated
4)CPC Clinic, Medipolis Medical Research Institute
Abstract
With transient injection site reactions frequently reported in the phase I study of intravenous levofloxacin(LVFX), our purpose was to minimize the injection site reactions by determining effects of diluent (5% glucose and saline), post dilution drug concentration (5 and 2.5 mg/mL), and infusion time (60 and 120 minutes), dripped by four methods of administration.
When subjects received with a drug concentration of 5 mg/mL used 5% glucose as a diluent and with an infusion time of 60 minutes, injection site reactions were observed in 88.9% (8/9). Saline was used as a diluent at a drug concentration of 5 mg/mL with an infusion time of 60 minutes, at 100% (9/9), at a drug concentration of 2.5 mg/mL with an infusion time of 60 minutes, at 77.8% (7/9), and at a drug concentration of 2.5 mg/mL with an infusion time of 120 minutes, at 66.7% (6/9). In each method, the injection site reactions reported were transient, most of them occurred within the first 30 minutes after the start of infusion and all were resolved by 1 hour after the end of infusion. None of the events required treatment or led to treatment discontinuation.
Because the injection site reaction with the LVFX injection was admitted in high frequency as for each method of administration, we were not able to find a clear reduction method to appear in the injection site reaction. The decrease in total number of events was observed when drug concentration was 2.5 mg/mL or the drug was infused in 120 minutes with LVFX in saline. All injection site reactions admitted were transitory, mild, and local responses, and did not lead to administering discontinuance. It was thought that the injection site reaction should be cautiously evaluated clinically, though it has no critical influence to safe use of this medicine. Nonetheless, as with existing injectable antimicrobials, administration of intravenous LVFX may potentially cause shock and anaphylactoid reactions, and thus should follow Guidelines for Prevention of Anaphylactic Reactions with Antimicrobials 2004.
Key word
levofloxacin injection, injection site reaction
Received
November 10, 2010
Accepted
April 4, 2011
Jpn. J. Chemother. 59 (S-1): 10-17, 2011
