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老年患者单次及多次给药后奥拉西坦的药代动力学

Oxiracetam pharmacokinetics following single and multiple dose administration in the elderly.

作者信息

Perucca E, Parini J, Albrici A, Visconti M, Ferrero E

机构信息

Institute of Medical Pharmacology, University of Pavia, Italy.

出版信息

Eur J Drug Metab Pharmacokinet. 1987 Apr-Jun;12(2):145-8. doi: 10.1007/BF03189889.

DOI:10.1007/BF03189889
PMID:3691580
Abstract

The kinetics of the nootropic drug oxiracetam was studied in 6 elderly female patients (age range 69-96 years) in good physical condition. After a single oral dose (800 mg), serum oxiracetam levels reached a peak (25 +/- 6 micrograms/ml) within 1-3 h and declined thereafter with a half-life of 3 to 6 h. Eighty-four percent of the administered dose was recovered in urine as unchanged drug within 24 h. During a maintenance regimen (800 b.i.d. at 8 a.m. and 2 p.m.) for 7 days oxiracetam did not show any accumulation in serum, trough serum levels before the morning and afternoon doses being 4.6 +/- 2.3 and 17.0 +/- 8.2 micrograms/ml respectively on day 4 and 5.7 +/- 3.3 and 17.9 +/- 7.7 micrograms/ml respectively on day 7. Comparison with previous pharmacokinetic data obtained in young subjects suggests that the clearance of the drug is lower in the elderly, probably as a result of the physiological decrease in renal function in old age.

摘要

对6名身体状况良好的老年女性患者(年龄范围69 - 96岁)进行了促智药奥拉西坦的动力学研究。单次口服剂量(800毫克)后,血清奥拉西坦水平在1 - 3小时内达到峰值(25±6微克/毫升),此后下降,半衰期为3至6小时。24小时内,84%的给药剂量以原形药物形式在尿液中回收。在维持治疗方案(每天上午8点和下午2点各800毫克,共7天)期间,奥拉西坦在血清中未显示任何蓄积,第4天上午和下午给药前的谷浓度分别为4.6±2.3和17.0±8.2微克/毫升,第7天分别为5.7±3.3和17.9±7.7微克/毫升。与先前在年轻受试者中获得的药代动力学数据相比,表明老年人中该药物的清除率较低,这可能是由于老年时肾功能生理性下降所致。

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引用本文的文献

1
Pharmacokinetics of oxiracetam in patients with renal impairment after a 800 mg single oral dose.单次口服800毫克后,奥拉西坦在肾功能损害患者中的药代动力学。
Eur J Drug Metab Pharmacokinet. 1990 Jul-Sep;15(3):231-7. doi: 10.1007/BF03190209.
2
Pharmacokinetics of oxiracetam in elderly patients after 800 mg oral doses, comparison with non-geriatric healthy subjects.800毫克口服剂量后老年患者奥拉西坦的药代动力学,与非老年健康受试者的比较。
Eur J Drug Metab Pharmacokinet. 1990 Jul-Sep;15(3):223-30. doi: 10.1007/BF03190208.

本文引用的文献

1
Drug therapy: drug disposition in old age.药物治疗:老年人的药物处置
N Engl J Med. 1982 May 6;306(18):1081-8. doi: 10.1056/NEJM198205063061804.
2
Pharmacokinetics of oxiracetam following intravenous and oral administration in healthy volunteers.奥拉西坦在健康志愿者体内静脉注射和口服给药后的药代动力学
Eur J Drug Metab Pharmacokinet. 1984 Jul-Sep;9(3):267-74. doi: 10.1007/BF03189650.
3
Experimental behavioral studies with oxiracetam on different types of chronic cerebral impairment.奥拉西坦对不同类型慢性脑损伤的实验性行为学研究。
Clin Neuropharmacol. 1986;9 Suppl 3:S19-26.