• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

肾功能受损患者口服丁螺环酮的临床药代动力学

Clinical pharmacokinetics of oral buspirone in patients with impaired renal function.

作者信息

Caccia S, Vigano G L, Mingardi G, Garattini S, Gammans R E, Placchi M, Mayol R F, Pfeffer M

机构信息

Istituto di Ricerche Farmacologiche Mario Negri Via Eritrea, Milano.

出版信息

Clin Pharmacokinet. 1988 Mar;14(3):171-7. doi: 10.2165/00003088-198814030-00005.

DOI:10.2165/00003088-198814030-00005
PMID:3370902
Abstract

12 patients with mild to moderate impairment of renal function and 12 healthy subjects each received 20mg buspirone as a single dose in this acute study. Six anuric patients with chronic renal failure were given two 20mg doses of buspirone, the first 2 days before haemodialysis (between dialyses) and the second during hemodialysis (2 hours before dialysis began). The differences between the median pharmacokinetic values of buspirone for healthy subjects, patients with mild to moderate renal impairment, and anuric patients were not statistically significant. Similarly, there were no significant differences between values in mild to moderate renal failure vs healthy subjects. Some of the median pharmacokinetic values for the active buspirone metabolite 1-(2-pyrimidinyl)-piperazine (1-PP), however, differed significantly for anuric patients, compared with healthy subjects or patients with mild to moderate renal impairment. When assessed between and during haemodialysis, the anuric patients had significantly (p less than 0.05) greater pharmacokinetic median values: half-life (t 1/2) = 15.2 vs 9.8 hours; area under the concentration-time curve (AUC) = 604 vs 404 nmol/L.h; and mean residence time (MRT) = 9.28 vs 6.96 hours. No firm recommendation for specific dosage can be made based on the present data. However, it does appear that in patients with mild to moderate renal impairment, the pharmacokinetics of buspirone and its active metabolite 1-PP are similar to those in individuals with normal renal function. For anuric patients higher concentrations of the 1-PP metabolite are attained while they are not undergoing haemodialysis. A dosage reduction of 25 to 50% might be necessary when buspirone is given to anuric patients.

摘要

在这项急性研究中,12例肾功能轻度至中度受损的患者和12名健康受试者均接受了20mg丁螺环酮单次给药。6例慢性肾衰竭的无尿患者接受了两剂20mg的丁螺环酮,第一剂在血液透析前2天(透析间期)服用,第二剂在血液透析期间(透析开始前2小时)服用。丁螺环酮在健康受试者、轻度至中度肾功能受损患者和无尿患者中的中位药代动力学值差异无统计学意义。同样,轻度至中度肾衰竭患者与健康受试者的值之间也无显著差异。然而,活性丁螺环酮代谢物1-(2-嘧啶基)-哌嗪(1-PP)的一些中位药代动力学值,无尿患者与健康受试者或轻度至中度肾功能受损患者相比有显著差异。在血液透析期间及透析后评估时,无尿患者的药代动力学中位值显著更高(p小于0.05):半衰期(t 1/2)=15.2小时对9.8小时;浓度-时间曲线下面积(AUC)=604对404nmol/L·h;平均驻留时间(MRT)=9.28对6.96小时。基于目前的数据无法给出具体剂量的明确建议。然而,轻度至中度肾功能受损患者中,丁螺环酮及其活性代谢物1-PP的药代动力学似乎与肾功能正常的个体相似。对于无尿患者,在未进行血液透析时1-PP代谢物会达到更高浓度。给无尿患者服用丁螺环酮时可能需要减少25%至50%的剂量。

相似文献

1
Clinical pharmacokinetics of oral buspirone in patients with impaired renal function.肾功能受损患者口服丁螺环酮的临床药代动力学
Clin Pharmacokinet. 1988 Mar;14(3):171-7. doi: 10.2165/00003088-198814030-00005.
2
Disposition kinetics of buspirone in patients with renal or hepatic impairment after administration of single and multiple doses.单次和多次给药后,肾或肝功能损害患者中丁螺环酮的处置动力学。
Eur J Clin Pharmacol. 1994;46(1):41-7. doi: 10.1007/BF00195914.
3
Pharmacokinetics of buspirone following oral administration to rhesus monkeys.
J Pharm Pharmacol. 1999 May;51(5):601-7. doi: 10.1211/0022357991772709.
4
Pharmacokinetics and CNS pharmacodynamics of the 5-HT1A agonist buspirone in humans following acute L-tryptophan depletion challenge.急性L-色氨酸耗竭激发后,5-羟色胺1A受体激动剂丁螺环酮在人体中的药代动力学和中枢神经系统药效学。
Methods Find Exp Clin Pharmacol. 1997 Jun;19(5):351-62.
5
Clinical pharmacokinetics of gabapentin after administration of gabapentin enacarbil extended-release tablets in patients with varying degrees of renal function using data from an open-label, single-dose pharmacokinetic study.一项开放标签、单剂量药代动力学研究的数据显示,在肾功能不同的患者中,使用加巴喷丁恩卡他伯尔缓释片后,加巴喷丁的临床药代动力学。
Clin Ther. 2012 Jan;34(1):201-13. doi: 10.1016/j.clinthera.2011.12.004. Epub 2011 Dec 28.
6
Interactions of buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone.
Pharmacol Toxicol. 1999 Feb;84(2):94-7. doi: 10.1111/j.1600-0773.1999.tb00880.x.
7
Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug.抗焦虑药物丁螺环酮的临床药代动力学与药效学
Clin Pharmacokinet. 1999 Apr;36(4):277-87. doi: 10.2165/00003088-199936040-00003.
8
Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats.丁螺环酮及其代谢物1-(2-嘧啶基)-哌嗪在大鼠体内的药代动力学-药效学建模
J Pharmacol Exp Ther. 2002 Dec;303(3):1130-7. doi: 10.1124/jpet.102.036798.
9
Effect of the novel anxiolytic drug deramciclane on the pharmacokinetics and pharmacodynamics of the CYP3A4 probe drug buspirone.新型抗焦虑药物地拉环烷对细胞色素P450 3A4探针药物丁螺环酮药代动力学和药效学的影响。
Eur J Clin Pharmacol. 2003 Dec;59(10):761-6. doi: 10.1007/s00228-003-0674-3. Epub 2003 Oct 18.
10
Pharmacokinetics of buspirone extended-release tablets: a single-dose study.丁螺环酮缓释片的药代动力学:一项单剂量研究。
J Clin Pharmacol. 2001 Jul;41(7):783-9. doi: 10.1177/00912700122010582.

引用本文的文献

1
Preparation, Swelling, and Drug Release Studies of Chitosan-based Hydrogels for Controlled Delivery of Buspirone Hydrochloride.壳聚糖基水凝胶的制备、溶胀及盐酸丁螺环酮控释性能研究。
Curr Pharm Biotechnol. 2024;25(14):1867-1874. doi: 10.2174/0113892010267638231206164415.
2
Evaluation of Renal Impairment Influence on Metabolic Drug Clearance using a Modelling Approach.运用建模方法评估肾功能损害对药物代谢清除率的影响。
Clin Pharmacokinet. 2023 Feb;62(2):307-319. doi: 10.1007/s40262-022-01205-3. Epub 2023 Jan 11.
3
Treatment of anxiety and depression in transplant patients: pharmacokinetic considerations.

本文引用的文献

1
The application of statistical moment theory to the evaluation of in vivo dissolution time and absorption time.统计矩理论在体内溶出时间和吸收时间评估中的应用。
J Pharmacokinet Biopharm. 1980 Oct;8(5):509-34. doi: 10.1007/BF01059549.
2
Buspirone: chemical profile of a new class of anxioselective agents.丁螺环酮:一类新型抗焦虑药的化学特性
J Clin Psychiatry. 1982 Dec;43(12 Pt 2):4-10.
3
Anxiolytic profiles.抗焦虑特性。
移植患者焦虑和抑郁的治疗:药代动力学考量
Clin Pharmacokinet. 2004;43(6):361-94. doi: 10.2165/00003088-200443060-00002.
4
Clinical pharmacokinetics and pharmacodynamics of buspirone, an anxiolytic drug.抗焦虑药物丁螺环酮的临床药代动力学与药效学
Clin Pharmacokinet. 1999 Apr;36(4):277-87. doi: 10.2165/00003088-199936040-00003.
5
Metabolism of the newer antidepressants. An overview of the pharmacological and pharmacokinetic implications.新型抗抑郁药的代谢。药理学与药代动力学影响概述。
Clin Pharmacokinet. 1998 Apr;34(4):281-302. doi: 10.2165/00003088-199834040-00002.
6
Disposition kinetics of buspirone in patients with renal or hepatic impairment after administration of single and multiple doses.单次和多次给药后,肾或肝功能损害患者中丁螺环酮的处置动力学。
Eur J Clin Pharmacol. 1994;46(1):41-7. doi: 10.1007/BF00195914.
7
Formation of active metabolites of psychotropic drugs. An updated review of their significance.精神药物活性代谢产物的形成。对其重要性的最新综述。
Clin Pharmacokinet. 1990 Jun;18(6):434-59. doi: 10.2165/00003088-199018060-00002.
J Clin Psychiatry. 1983 Nov;44(11 Pt 2):45-57.
4
Buspirone: multicenter efficacy study.丁螺环酮:多中心疗效研究。
J Clin Psychiatry. 1982 Dec;43(12 Pt 2):92-4.
5
Buspirone and diazepam in anxiety: a controlled study.丁螺环酮与地西泮治疗焦虑症的对照研究。
J Clin Psychiatry. 1982 Dec;43(12 Pt 2):81-6.
6
Metabolism and disposition of buspirone.丁螺环酮的代谢与处置
Am J Med. 1986 Mar 31;80(3B):41-51. doi: 10.1016/0002-9343(86)90331-1.
7
Disposition of the psychotropic drugs buspirone, MJ-13805 and piribedil, and of their common active metabolite 1-(2-pyrimidinyl)-piperazine in the rat.精神药物丁螺环酮、MJ - 13805和匹莫齐特及其共同活性代谢物1 - (2 - 嘧啶基) - 哌嗪在大鼠体内的处置情况。
Xenobiotica. 1985 Oct;15(10):835-44. doi: 10.3109/00498258509045035.
8
The comparative efficacy of buspirone and diazepam in the treatment of anxiety.丁螺环酮与地西泮治疗焦虑症的疗效比较
Am J Psychiatry. 1979 Sep;136(9):1184-7. doi: 10.1176/ajp.136.9.1184.