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法莫替丁在肾衰竭患者中的药代动力学和药效学。

Pharmacokinetics and dynamics of famotidine in patients with renal failure.

作者信息

Gladziwa U, Klotz U, Krishna D R, Schmitt H, Glöckner W M, Mann H

机构信息

Department of Internal Medicine, Technical University of Aachen, F.R.G.

出版信息

Br J Clin Pharmacol. 1988 Sep;26(3):315-21. doi: 10.1111/j.1365-2125.1988.tb05282.x.

Abstract
  1. Famotidine, a new histamine H2-receptor antagonist was administered intravenously (20 mg) to 22 patients with end stage renal disease during a dialysis free interval (n = 6) and during different blood purification processes including haemodialysis (HD; n = 4), intermittent haemofiltration (HF; n = 4), continuous haemofiltration (CHF; n = 4) and continuous ambulatory peritoneal dialysis (CAPD; n = 4). The plasma, the dialysate/filtrate and the urine concentrations of famotidine were analysed by h.p.l.c. 2. In addition, intra-gastric pH was measured by a long-term-pH probe in seven patients with renal failure and in six patients with normal renal function (control group) following 20 mg famotidine. 3. A 7 to 10 fold prolongation of famotidine's elimination half-life (27.2 +/- 8.5 h; mean +/- s.d.) was observed in patients with renal failure as compared with the half-life (2.6-3.6 h) in subjects with normal renal function. 4. Total body clearance (CL) and volume of distribution (V) were found to be 33.5 +/- 10.1 ml min-1 and 1.3 +/- 0.7 l kg-1, respectively in patients with end-stage renal failure. 5. Blood purification processes have shown considerable variation in clearing famotidine from the body: 16.4 +/- 8.9 and 6.0 +/- 2.9% of the administered dose in HD with polysulphone and cuprophan membranes respectively, 7.7 +/- 5.2% in HF with a polyacrylonitrile membrane (each for 5 h), 4.5 +/- 1.1% in CAPD and 16.2 +/- 4.9% in CHF with a polysulphone membrane within 24 h.(ABSTRACT TRUNCATED AT 250 WORDS)
摘要
  1. 法莫替丁是一种新型组胺H2受体拮抗剂,在无透析间期(n = 6)以及包括血液透析(HD;n = 4)、间歇性血液滤过(HF;n = 4)、连续性血液滤过(CHF;n = 4)和持续性非卧床腹膜透析(CAPD;n = 4)等不同血液净化过程中,对22例终末期肾病患者静脉注射(20毫克)。通过高效液相色谱法分析法莫替丁的血浆、透析液/滤液及尿液浓度。2. 此外,对7例肾衰竭患者和6例肾功能正常患者(对照组)在给予20毫克法莫替丁后,用长期pH探头测量胃内pH值。3. 与肾功能正常受试者的半衰期(2.6 - 3.6小时)相比,观察到肾衰竭患者中法莫替丁的消除半衰期延长了7至10倍(27.2 +/- 8.5小时;平均值 +/- 标准差)。4. 终末期肾衰竭患者的总体清除率(CL)和分布容积(V)分别为33.5 +/- 10.1毫升/分钟和1.3 +/- 0.7升/千克。5. 血液净化过程在清除体内法莫替丁方面显示出相当大的差异:在使用聚砜膜和铜仿膜进行血液透析时,分别为给药剂量的16.4 +/- 8.9%和6.0 +/- 2.9%;在使用聚丙烯腈膜进行血液滤过5小时时为7.7 +/- 5.2%;在持续性非卧床腹膜透析中为4.5 +/- 1.1%;在使用聚砜膜进行连续性血液滤过24小时内为16.2 +/- 4.9%。(摘要截取自250字)

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