临床药物动力学linezolid,小说oxazolidinone抗菌。
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跟踪狂DJ, Jungbluth GL
临床药物动力学linezolid,小说oxazolidinone抗菌。
Pharmacokinet。2003; 42 (13): 1129 - 40。doi: 10.2165 / 00003088-200342130-00004。
- PubMed ID
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14531724 (在PubMed]
- 文摘
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Linezolid是第一个从oxazolidinone类抗菌批准。药物对革兰氏阳性微生物大量的抗菌活性如链球菌、葡萄球菌和enterococci,包括物种对传统的抗菌治疗。Linezolid完全可利用相比口服和静脉注射后管理。最大血浆浓度linezolid通常实现口服后1到2个小时之间。食物稍微降低了速度,但程度上的吸收。的分布linezolid大约相当于全身水,还有低蛋白结合血清白蛋白(31%)。linezolid的消除半衰期是5 - 7小时,400 - 600毫克每天政府提供稳态浓度在治疗范围内。Linezolid主要通过non-renal间隙两种代谢物和肾清除率的母体化合物。大约50%的服用剂量尿液中出现的两个主要代谢产物,和大约35%表现为父药物。小程度的非线性已经观察到,30%剂量的5倍增加后减少间隙。 The nonlinearity is not relevant over the therapeutic dosage range. Plasma linezolid concentrations in elderly patients, patients with mild to moderate hepatic impairment or mild to severe renal impairment are similar to those achieved in young or healthy volunteers. Higher concentrations are observed in women as compared with men, but the difference is not sufficient to warrant an adjustment in dosage. In patients with severe renal impairment requiring haemodialysis, the exposure to the two primary metabolites was 7 to 8-fold higher than in patients with normal renal function. Therefore, linezolid should be used with caution in patients with severe renal insufficiency. A higher clearance of linezolid was found in children as compared with adults, and therefore higher daily dosages per kg bodyweight are required in children. There is no pharmacokinetic interaction when linezolid is coadministered with aztreonam, gentamicin or warfarin. Linezolid is a mild, reversible, inhibitor of monoamine oxidases A and B. Coadministration of linezolid with the adrenergic agents pseudoephedrine and phenylpropanolamine resulted in increases in blood pressure relative to these agents alone or to placebo. The degree of the change in blood pressure was within that associated with normal daily activities. No interaction was observed when linezolid was coadministered with the serotonergic agent dextromethorphan.