左氧氟沙星的临床药物动力学。
文章的细节
-
引用
复制到剪贴板 -
鱼DN,周润发
左氧氟沙星的临床药物动力学。
Pharmacokinet。1997年2月,32(2):101 - 19所示。doi: 10.2165 / 00003088-199732020-00002。
- PubMed ID
-
9068926 (在PubMed]
- 文摘
-
左氧氟沙星是氟喹诺酮类抗生素和光学S -(-)异构体的外消旋药物氧氟沙星的物质。它有一个广泛的体外活性对革兰氏阳性和革兰氏阴性细菌,以及某些其他病原体如支原体、衣原体、军团菌、分枝杆菌spp。左氧氟沙星更活跃的反对比R -(+)氧氟沙星细菌病原体。左氧氟沙星半水化合物,制定的商业产品,左氧氟沙星97.6%的体重。左氧氟沙星药物动力学被消灭一阶线性2-compartment开放模型。在健康志愿者血浆浓度达到平均药物血浆浓度峰值(Cmax)约2.8和5.2 mg / L后1 - 2小时内口服左氧氟沙星的250和500毫克片剂,分别。口服左氧氟沙星的生物利用度接近100%,很少受到政府与食物的影响。口服吸收是非常快速和完整的,不同血清浓度时间配置文件后500毫克口服或静脉注射剂量(注入超过60分钟)。单剂量口服左氧氟沙星50到1000毫克产生意味着Cmax和曲线下的面积(AUC)从大约0.6到9.4 mg / L和4.7至108毫克。h / L,分别增加线性dose-proportional的方式。左氧氟沙星的药物代谢动力学情况是类似在multiple-dose方案后单剂量。左氧氟沙星广泛分布到全身,平均体积分布的1.1 L /公斤,并渗透到大多数身体组织和体液。 Drug concentrations in tissues and fluids are generally greater than those observed in plasma, but penetration into the cerebrospinal fluid is relatively poor (concentrations approximately 16% of simultaneous plasma values). Levofloxacin is approximately 24 to 38% bound to serum plasma proteins (primarily albumin); serum protein binding is independent of serum drug concentrations. The plasma elimination half-life (t1/2 beta) ranges from 6 to 8 hours in individuals with normal renal function. Approximately 80% of levofloxacin is eliminated as unchanged drug in the urine through glomerular filtration and tubular secretion; minimal metabolism occurs with the formation of no metabolites possessing relevant pharmacological activity. Renal clearance and total body clearance are highly correlated with creatinine clearance (CLCR), and dosage adjustments are required in patients with significant renal dysfunction. Levofloxacin pharmacokinetics are not appreciably affected by age, gender or race when differences in renal function, and body mass and composition are taken into account. Important drug interactions exist with aluminium- and magnesium-containing antacids and ferrous sulfate, as with other fluoroquinolones, resulting in significantly decreased levofloxacin absorption when administered concurrently. These agents should be administered at least 2 hours before or after levofloxacin administration. Cimetidine and probenecid decrease levofloxacin renal clearance and increase t1/2 beta; the magnitudes of these interactions are not clinically significant. Levofloxacin appears to have only minor potential for significantly altering the pharmacokinetics of theophylline, warfarin, zidovudine, ranitidine, digoxin or cyclosporin; however, patients receiving these drugs concurrently should be monitored closely for signs of enhanced pharmacological effect or toxicity. Levofloxacin pharmacokinetics are not significantly altered by sucralfate when administration of these drugs is separated by at least 2 hours.
DrugBank数据引用了这篇文章
- 药物
- 药物反应
-
反应 细节 细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
