INVITRO ACTIVITY AND HUMAN PHARMACOKINETICS OF TEICOPLANIN
INVITRO ACTIVITY AND HUMAN PHARMACOKINETICS OF TEICOPLANIN
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DOI：
10.1128/aac.26.6.881
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发表时间：
1984-01-01
影响因子：
4.9
通讯作者：
DESCHEPPER, PJ
中科院分区：
文献类型：
--
作者：
VERBIST, L;TJANDRAMAGA, B;DESCHEPPER, PJ
替考拉宁是一种与万古霉素相关的新抗生素，测定了其对456株革兰氏阳性球菌的体外活性。与万古霉素相比，替考拉宁对葡萄球菌的活性相似，但对肠球菌和β-葡萄球菌的活性高4-40倍。溶血性和草绿色链球菌。在6名健康志愿者中研究了替考拉宁3和6 mg/kg i. v.以及3 mg/kg i.m.单次给药后的药代动力学。两次静脉给药后的动力学参数非常相似。3和6 mg/kg静脉给药的血浆浓度曲线显示三指数下降，消除半衰期分别为47.3和44.1 h。尿液（0-102 h）中回收的剂量百分比分别为43.2%和44.1%。血浆曲线下面积与剂量相关：分别为256.5和520.9 μ g/h/ml。替考拉宁3 mg/kg i.m.注射后的生物利用度90%，峰值水平为7.1 μ g/ml。3-mg/kg剂量后24小时血浆中的平均水平分别为2.1和2.3 μ g/ml，6-mg/kg静脉内剂量后24小时血浆中的平均水平为4.2 μ g/ml。
The in vitro activity of teicoplanin, a new antibiotic related to vancomycin, was determined against 456 gram-positive cocci. The activity of teicoplanin in comparison with that of vancomycin was similar against staphylococci, but 4-40 times higher against enterococci and .beta.-hemolytic and viridans streptococci. The single-dose pharmacokinetics of teicoplanin were studied in 6 healthy volunteers after administration of 3 and 6 mg/kg i.v. and of 3 mg/kg i.m. The kinetic parameters after both i.v. doses were very similar. The curves for concentration in plasma for the 3- and 6-mg/kg intravenous doses showed a triexponential decline with elimination half-lives of 47.3 and 44.1 h, respectively. The percentages of the doses recovered in urine (0-102 h) were 43.2 and 44.1%, respectively. The areas under the plasma curves were dose related: 256.5 and 520.9 .mu.g/h per ml, respectively. The bioavailability of teicoplanin after injection of 3 mg/kg i.m. was 90% and the peak level was 7.1 .mu.g/ml. The mean levels in plasma 24 h after the 3-mg/kg doses were 2.1 and 2.3 .mu.g/ml, respectively, and the mean level in plasma 24 h after the 6-mg/kg i.v. dose was 4.2 .mu.g/ml.