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Antimicrobial Agents and Chemotherapy, March 2001, p. 917-921, Vol. 45, No. 3
Department of Pharmacology, Gifu University School of
Medicine, Gifu 500-8705,1 Shitoro
Clinic, Hamamatsu 432-8066,2 and R & D Division, Clinical Development Department, Schering-Plough KK, Osaka
541-0046,3 Japan
Received 13 April 2000/Returned for modification 8 October
2000/Accepted 26 December 2000
The pharmacokinetic properties of an everninomicin antibiotic
(SCH27899; Ziracin) were studied with healthy Japanese male volunteers
by single (1, 3, 6, and 9 mg/kg of body weight) and multiple 60-min
intravenous infusions (3, 6, and 9 mg/kg once daily for 10 consecutive
days following a 2-day interval after the initial dose). At single
doses the peak serum concentration and the area under the serum
concentration-time curve linearly increased with the dose. While total
body clearance (CL; 31.2 to 45.6 ml/kg/h) and percent cumulative
urinary recovery as unchanged drug (4.9 to 7.1%) were rather constant
irrespective of doses, the terminal half-life of
0066-4804/01/$04.00+0 DOI: 10.1128/AAC.45.3.917-921.2001
Copyright © 2001, American Society for Microbiology. All rights reserved.
Pharmacokinetics of a New Parenteral Oligosaccharide Antibiotic,
SCH27899 (Ziracin), in Healthy Subjects
phase
(t1/2
; 14.2 to 19.6 h) were slightly
prolonged at the higher two doses compared with the lower two doses.
With repeated doses of SCH27899, a statistically significant decrease
and increase were found in CL and t1/2
of
about 36 and 21%, respectively, although these changes may be
clinically irrelevant. The most commonly reported adverse events were
local reactions such as erythema, pain, and palpable venous cord
of mild to moderate degree around the injection site, which could be
managed by changing the injection sites.
*
Corresponding author. Mailing address: Department of
Pharmacology, Gifu University School of Medicine, 40 Tsukasa-machi,
Gifu 500, Japan. Phone: 81-58-267-2231. Fax: 81-58-267-2959. E-mail: uematsu{at}cc.gifu-u.ac.jp.
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