药物动力学conivaptan盐酸盐,抗利尿激素V(1) /(2)受体拮抗剂,euvolemic或hypervolemic低钠血症患者有或没有从潜在的充血性心力衰竭,为期4天开放研究。

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毛泽东ZL,跟踪狂D, Keirns J

药物动力学conivaptan盐酸盐,抗利尿激素V(1) /(2)受体拮抗剂,euvolemic或hypervolemic低钠血症患者有或没有从潜在的充血性心力衰竭,为期4天开放研究。

其他。2009年7月,31 (7):1542 - 50。doi: 10.1016 / j.clinthera.2009.07.011。

PubMed ID
19695403 (在PubMed
]
文摘

背景:Conivaptan nonpeptide抗利尿激素V(1) /(2)受体拮抗剂,产生一个控制血清钠浓度增加euvolemic或hyper-volemic低钠血症患者住院。目的:本研究评估的药物动力学conivaptan euvolemic或hypervolemic低钠血症患者有或没有潜在的充血性心力衰竭的人参与一个疗效和耐受性的临床试验。方法:数据来自一个非盲、多中心的研究被用来评估conivaptan在血症患者的药物动力学。病人接受了20毫克负荷剂量静脉注射超过30分钟,其次是一个连续为期4天注入20或40毫克/天。在整个人群中,血浆conivaptan浓度测定在基线,结束时负荷剂量(0.5小时),在24小时内,在天3和4,后续在11天的访问。一个子集的病人在研究2网站(“pharmacokineticrich”子集)药代动力学分析提供了额外的样品在1天,4日和24小时;第二天24小时;和第五天在1、2、7、12、24小时。结果:等离子conivaptan浓度进行评估在31个病人conivaptan 20毫克/天(平均(SD)的年龄,73.1(14.3)年;体重68.1公斤(17.2); 71.0% female; 87.1% white, 9.7% black, 3.2% other) and 172 patients who received co-nivaptan 40 mg/d (mean [SD] age, 71.5 [14.4] years; weight, 65.6 [15.9] kg; 64.0% female; 90.1% white, 6.4% black, 3.5% other). The pharmacokinetic-rich subset included 8 patients who received conivap-tan 20 mg/d (mean [SD] age, 76.3 [12.4] years; weight, 71.5 [14.7] kg; 87.5% female; 100% white) and 8 who received conivaptan 40 mg/d (mean [SD] age, 78.3 [7.9] years; weight, 71.3 [15.6] kg; 37.5% female; 100% white). In the overall patient group, plasma conivaptan concentrations were the highest after the 30-minute (C(0.5h)) loading dose (mean [SD] C(0.5h) = 733 [323] and 701 [343] ng/mL with conivap-tan 20 and 40 mg/d, respectively) and then declined during day 1 to concentrations (C(24h)) (mean [SD] C(24h) = 84 [78] and 215 [129] ng/mL with conivaptan 20 and 40 mg/d, respectively) that were maintained by the continuous infusion of 20 or 40 mg/d. At the end of infusion (96 hours), the mean (SD) plasma conivaptan concentrations were 176 (196) and 308 (321) ng/mL for conivaptan 20 and 40 mg/d, respectively. A ratio of 1.75 indicated near dose proportionality; however, interpatient variability was evident. No apparent differences in plasma conivaptan concentrations measured at 0.5 or 96 hours were observed between patients with euvolemic or hypervolemic hypona-tremia or between patients with or without congestive heart failure. In the pharmacokinetic-rich subset, for conivaptan 20 and 40 mg/d, respectively, conivaptan clearance was 18.7 and 9.5 L/h, the elimination t1/2 was 5.3 and 10.2 hours, and exposure to conivaptan in terms of AUC(infinity) was 6996 and 30,771 ng . h/mL. CONCLUSION: The results of this study suggest that the pharmacokinetics of conivaptan 20 and 40 mg/d do not differ by volume status or the presence or absence of congestive heart failure.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
Conivaptan 后叶加压素V1a受体 蛋白质 人类
是的
拮抗剂
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Conivaptan 后叶加压素V2受体 蛋白质 人类
是的
拮抗剂
 细节