临床药物动力学quinupristin / dalfopristin。
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Bearden DT
临床药物动力学quinupristin / dalfopristin。
43 Pharmacokinet。2004; (4): 239 - 52。
- PubMed ID
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15005638 (在PubMed]
- 文摘
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Quinupristin / dalfopristin streptogramin各种革兰氏阳性抗菌活性的抗菌。静脉注射药物有最小的口服吸收和管理固定30:70 quinupristin dalfopristin比。之间的线性关系已经观察到剂量和最大血浆浓度。单剂7.5毫克/公斤生产管理最大血浆浓度的2.3 - -2.7 mg / L quinupristin dalfopristin -8.2和6.1 mg / L。曲线下的面积(AUC)获得相同的剂量是2.7 - -3.3,6.5 - -7.7毫克。分别h / L quinupristin和dalfopristin。重复管理导致13 - 21%最大血浆浓度的增加和21 - 26%增加AUC quinupristin和dalfopristin。Quinupristin和dalfopristin稳态量分布的0.46 - -0.54和0.24 - -0.30 L /公斤,分别。Quinupristin展品蛋白质绑定(55 - 78%)高于dalfopristin(11 - 26%),虽然这两个实体分配到组织。血液中浓度超过已报告的肾脏,肝脏,脾脏,唾液腺和灵长类动物的白细胞。 Extravascular penetration, as measured in blister fluid, is 40-80%. Both quinupristin and dalfopristin are extensively metabolised via nonenzymatic reactions. Quinupristin is conjugated to form two active compounds, a cysteine moiety and a glutathione moiety. Dalfopristin is hydrolysed to the active metabolite pristinamycin IIA. The metabolites exert antibacterial activity similar to that of the parent compounds. Quinupristin/dalfopristin is excreted primarily in the faeces (75-77%), with lesser renal excretion (15-19%). The elimination half-lives of quinupristin and dalfopristin are similar, and are 0.7-1.3 hours after single doses. The metabolites have slightly longer half-lives, ranging from 1.2 to 1.8 hours. With repeated doses, plasma clearance of quinupristin and dalfopristin is reduced by approximately 20% compared with single doses, resulting in clearances of 0.7-0.8 L/h/kg. Saturable protein binding has been hypothesised as a causative mechanism. Quinupristin/dalfopristin is an inhibitor of cytochrome P450 3A4, resulting in multiple drug interactions. Ciclosporin AUC increased by 5-222% when coadministered with quinupristin/dalfopristin. Careful monitoring of patients receiving drugs that are substrates of cytochrome P450 3A4 is suggested.Quinupristin/dalfopristin is administered at 7.5 mg/kg every 8-12 hours, depending upon the severity of infection. The pharmacodynamic parameter linked with antibacterial activity for quinupristin/dalfopristin appears to be the ratio of AUC to the minimal inhibitory concentration. The additional activity of a prolonged post-antibiotic effect may also be important for efficacy.
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- 药物酶
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药物 酶 类 生物 药理作用 行动 Dalfopristin 细胞色素P450 3 a4 蛋白质 人类 未知的抑制剂细节 Quinupristin 细胞色素P450 3 a4 蛋白质 人类 未知的抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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药物 交互 整合药物之间
在您的软件的交互环孢霉素 Quinupristin 环孢霉素的血清浓度时可以增加与Quinupristin相结合。
