Stein Gary E, Schooley Sharon
Department of Medicine, Michigan State University, East Lansing 48824, USA.
Pharmacotherapy. 2002 May;22(5):593-6. doi: 10.1592/phco.22.8.593.33214.
To investigate the serum bactericidal activity (SBA) over time of extended-release clarithromycin against moderately resistant strains of Streptococcus pneumoniae.
Prospective, single-dose pharmacodynamic study.
University-affiliated research center.
Eleven healthy male volunteers.
All volunteers received a single dose of extended-release clarithromycin as two 500-mg tablets, and blood samples were obtained at 0, 2, 6, 12, and 24 hours after administration of the dose.
For each blood sample, a serum bactericidal titer (SBT) was determined against S. pneumoniae strains with minimum inhibitory concentrations (MICs) of 0.5, 1.0, 2.0, 4.0, and 8.0 microg/ml to clarithromycin. The median SBT was determined for each time period. The extended-release formulation of clarithromycin exhibited SBA for 24 hours against pneumococcal strains with MICs of 0.5, 1.0, and 2.0 microg/ml. No SBA was observed against isolates with MICs of 4.0 or 8.0 microg/ml.
The extended-release formulation of clarithromycin, taken once/day, will provide SBA for 24 hours against strains of S. pneumoniae with MICs of 2.0 microg/ml or less.
研究缓释克拉霉素对中度耐药肺炎链球菌菌株随时间变化的血清杀菌活性（SBA）。
前瞻性单剂量药效学研究。
大学附属研究中心。
11名健康男性志愿者。
所有志愿者均服用单剂量缓释克拉霉素，为两片500毫克片剂，并在给药后0、2、6、12和24小时采集血样。
对每份血样测定针对克拉霉素最低抑菌浓度（MIC）分别为0.5、1.0、2.0、4.0和8.0微克/毫升的肺炎链球菌菌株的血清杀菌效价（SBT）。确定每个时间段的SBT中位数。克拉霉素缓释制剂对MIC为0.5、1.0和2.0微克/毫升的肺炎球菌菌株表现出24小时的SBA。对MIC为4.0或8.0微克/毫升的分离株未观察到SBA。
每日服用一次的克拉霉素缓释制剂对MIC为2.0微克/毫升或更低的肺炎链球菌菌株可提供24小时的SBA。
