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老年肾功能不全患者与年轻成年人相比多西环素的药代动力学

[The pharmacokinetics of doxycycline in kidney insufficiency in geriatric patients compared to younger adults].

作者信息

Simon C, Malerczyk V, Engelke H, Preuss I, Grahmann H, Schmidt K

出版信息

Schweiz Med Wochenschr. 1975 Nov 29;105(48):1615-20.

PMID:1215947
Abstract

In young adults i.v. injection of 200 mg doxycycline was followed by a rapid fall in serum levels in the first 30 minutes and than a slow decrease (serum concentration after 24 h on average 1.0 mug/ml). Biological half-life was 11.9 h, final distribution volume 50.0 litres and urine recovery 70%. After oral administration of 200 mg doxycycline the serum peaks measured were 3.4 mug/ml (2 1/2 h later). With repeated doses of 100 mg every 24 h serum peaks were 2.8 mug/ml and serum concentrations after 24 h 0.8-0.9 mug/ml (urine recovery 43%). The area under the curve was 25.5% less than after i.v. injection. In 7 adults with chronic renal failure the half-life of doxycycline varied between 10 and 24 h. With repeated oral administration of doxycycline (100 mg every 24 h) there was no accumulation of the drug in blood. During hemodialysis (Stuttgart kidneys, Rhône-Poulenc plates) doxycycline injected i.v. was eliminated as rapidly as before. In renal failure doxycycline may be given in the same dosage as where renal function is normal. In 12 geriatric patients without renal disease, serum levels of doxycycline after i.v. injection of 200 mg were not significantly different from those of young adults (distribution volume 46.2 +/- 16.2 litres). It can therefore be assumed that tissue penetration of the drug is similar in the elderly and in young adults.

摘要

在年轻成年人中,静脉注射200毫克多西环素后,血清水平在最初30分钟内迅速下降,随后缓慢降低(24小时后血清浓度平均为1.0微克/毫升)。生物半衰期为11.9小时,终末分布容积为50.0升,尿回收率为70%。口服200毫克多西环素后测得的血清峰值为3.4微克/毫升(2个半小时后)。每24小时重复给药100毫克时,血清峰值为2.8微克/毫升,24小时后血清浓度为0.8 - 0.9微克/毫升(尿回收率43%)。曲线下面积比静脉注射后小25.5%。在7名慢性肾功能衰竭的成年人中,多西环素的半衰期在10至24小时之间变化。重复口服多西环素(每24小时100毫克)后,药物在血液中无蓄积。在血液透析期间(斯图加特肾,罗纳 - 普朗克平板),静脉注射的多西环素消除速度与之前一样快。在肾功能衰竭时,多西环素的给药剂量可与肾功能正常时相同。在12名无肾脏疾病的老年患者中,静脉注射200毫克多西环素后的血清水平与年轻成年人无显著差异(分布容积为46.2±16.2升)。因此可以假设,该药物在老年人和年轻成年人中的组织穿透情况相似。

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