使用bivalirudin患者的肾功能损害。

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使用bivalirudin患者的肾功能损害。

J侵入性心功能杂志。2000;12月12 5 F: 33 f-6。

PubMed ID
11156732 (在PubMed
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文摘

绝大多数急性冠状动脉综合征患者的肾功能损害从衰老过程或潜在疾病,如肾硬化或糖尿病。例如,在第三阶段的研究bivalirudin PTCA使用,只有25%的病人肾功能正常:46%有轻度肾功能障碍,28%有中度肾功能损害,约1%有严重肾功能损害。beplayapp在肾功能正常的患者,静脉注射药物动力学的bivalirudin剂量比例(线性),特点是快速等离子体间隙(4.58毫升/分钟/公斤),体积小的分布(0.2 L /公斤),和一个消除半衰期约为30分钟。beplayapp肾清除率是消除bivalirudin的主要路线。至于其他小的多肽,bivalirudin肾小球过滤,在近曲小管分泌,远曲小管的重吸收和降解细胞内溶酶体组成氨基酸。有直接bivalirudin剂量之间的积极关系,血浆浓度和局部血栓形成质激活时间(aPTT)或活化凝血时间(ACT)。比较研究的药物动力学和药效学bivalirudin正常肾功能(肾小球滤过率(GFR)大于或等于90毫升/分钟;肾小球滤过率(GFR) n = 8)、轻度(60 - 89毫升/分钟;肾小球滤过率(GFR) n = 8)、中度(30-59毫升/分钟;n = 7),或严重(肾小球滤过率(GFR) < 30毫升/分钟; n = 10) renal impairment showed that while clearance was similar in the normal (4.58 ml/minute/kg) and mildly impaired (4.94 ml/minute/kg) groups, the clearance rate was reduced 45% in the moderate impairment (2.50 ml/minute/kg) group and about 68% in the severe impairment (1.46 ml/minute/kg) group. Clearance was further reduced (77%) in a group of 12 dialysis dependent patients (1.04 ml/minute/kg). There was a strong positive correlation between plasma bivalirudin concentrations and aPTT. The derived maximal effect (Emax) was similar for the normal (58.3 seconds), mildly impaired (44.7 seconds) and moderately impaired (56.8 seconds) groups, but prolonged in the severely renally impaired (79.4 seconds) and dialysis dependent (84.4 seconds) patients. These kinetic and dynamic results have recently been substantially confirmed in patients undergoing percutaneous transluminal coronary angioplasty (PTCA), where reduced plasma clearance (20%) and elevated ACTs were observed in patients with moderate renal impairment. The bleeding results of the phase 3 PTCA clinical trial (involving 4,312 patients) in which patients were classified as having normal renal function, or mild, moderate or severe renal impairment (using the above criteria), is consistent with the pharmacokinetic data. The incidence of major bleeding was directly correlated with renal function for both bivalirudin (normal, 1.2%; mild, 1.9%; moderate, 6%; severe, 0%) and heparin (normal, 3.1%; mild, 8.5%; moderate, 12.7%; severe, 26.7%). Importantly, the incidence of major bleeding was significantly less on bivalirudin than heparin in patients with any degree of renal impairment. The mean 45-minute ACT values were similar (350-400 seconds) in the normal, mild and moderately impaired groups, but elevated in the severely impaired group (450 seconds). A multivariate analysis of bleeding covariates in this database indicated that GFR is an important risk factor for bleeding (r(2) = 0.054), and accounted for twice the variability in bleeding as either sex or age.

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