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影响两种苯并噻嗪类非甾体抗炎药(吡罗昔康和异恶酰胺)动力学的因素。

Factors affecting the kinetics of two benzothiazine non-steroidal anti-inflammatory medicines, piroxicam and isoxicam.

作者信息

Edwards I R, Ferry D G, Campbell A J

出版信息

Eur J Clin Pharmacol. 1985;28(6):689-92. doi: 10.1007/BF00607917.

DOI:10.1007/BF00607917
PMID:4065194
Abstract

The pharmacokinetics of isoxicam and piroxicam were compared in 12 young adults (less than 40 years) and 12 elderly subjects (greater than 65 years). After a single oral dose of 200 mg isoxicam or 20 mg piroxicam blood samples were taken for 168 h and the plasma drug concentrations determined by HPLC. The elimination half life of piroxicam for the adults was 57.1 +/- 16.4 h (mean +/- SD; harmonic mean 52.9 h) and for the elderly subjects was 57.8 +/- 22.1 h (harmonic mean 52.1 h). The corresponding values after isoxicam were 34.3 +/- 13.6 h (harmonic mean 31.6) for the adults and 39.1 +/- 22.7 h (harmonic mean 33.5) for the elderly subjects. Similarly no differences were noted in either the AUC0-infinity after piroxicam (adults 154.1 +/- 52.2 micrograms . h/ml, elderly 163.6 +/- 99.1 micrograms . h/ml) and isoxicam (adults 642.7 +/- 241.9 micrograms . h/ml, elderly 787.9 +/- 613.1 micrograms . h/ml) or the apparent oral clearance of piroxicam (adults 2.39 +/- 0.80 ml/min, elderly 2.51 +/- 0.90 ml/min) and isoxicam (adults 5.84 +/- 2.04 ml/min, elderly 5.59 +/- 2.12 ml/min). One adult and two elderly subjects exhibited slower elimination of both medicines than the remainder of each group. However determination of the oxidation phenotype using sparteine metabolism showed that this was not a likely determinant of the reduced clearance.

摘要

对12名年轻成年人(40岁以下)和12名老年受试者(65岁以上)的异恶酰胺和吡罗昔康的药代动力学进行了比较。单次口服200毫克异恶酰胺或20毫克吡罗昔康后,采集血样168小时,并用高效液相色谱法测定血浆药物浓度。吡罗昔康在成年人中的消除半衰期为57.1±16.4小时(均值±标准差;调和均值52.9小时),在老年受试者中为57.8±22.1小时(调和均值52.1小时)。异恶酰胺后的相应值在成年人中为34.3±13.6小时(调和均值31.6),在老年受试者中为39.1±22.7小时(调和均值33.5)。同样,吡罗昔康(成年人154.1±52.2微克·小时/毫升,老年人163.6±99.1微克·小时/毫升)和异恶酰胺(成年人642.7±241.9微克·小时/毫升,老年人787.9±613.1微克·小时/毫升)的AUC0-无穷大,以及吡罗昔康(成年人2.39±0.80毫升/分钟,老年人2.51±0.90毫升/分钟)和异恶酰胺(成年人5.84±2.04毫升/分钟,老年人5.59±2.12毫升/分钟)的表观口服清除率均未发现差异。一名成年人和两名老年受试者对两种药物的消除速度比每组的其余受试者慢。然而用司巴丁代谢法测定氧化表型表明,这不太可能是清除率降低的决定因素。

相似文献

1
Factors affecting the kinetics of two benzothiazine non-steroidal anti-inflammatory medicines, piroxicam and isoxicam.影响两种苯并噻嗪类非甾体抗炎药(吡罗昔康和异恶酰胺)动力学的因素。
Eur J Clin Pharmacol. 1985;28(6):689-92. doi: 10.1007/BF00607917.
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A comparison of isoxicam pharmacokinetics in young and elderly subjects.年轻与老年受试者异恶酰吡唑酮药代动力学的比较。
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Effect of impairment of renal function on the accumulation and disposition of isoxicam.肾功能损害对异恶酰胺蓄积和处置的影响。
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Pharmacokinetics of isoxicam in the elderly.异恶酰胺在老年人中的药代动力学。
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Pharmacokinetics of oxicam nonsteroidal anti-inflammatory agents.昔康类非甾体抗炎药的药代动力学
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Pharmacokinetic projections for isoxicam and piroxicam in old and young subjects.老年和青年受试者中异恶丙嗪和吡罗昔康的药代动力学预测。
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[Onset of effect of isoxicam and piroxicam. A double-blind parallel study].[异恶酰胺和吡罗昔康的起效时间。一项双盲平行研究]
Fortschr Med. 1985 Jan 24;103(4):73-6.
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Pharmacokinetics of piroxicam in man.吡罗昔康在人体中的药代动力学。
Eur J Rheumatol Inflamm. 1983;6(1):46-55.

引用本文的文献

1
Pharmacokinetics of oxicam nonsteroidal anti-inflammatory agents.昔康类非甾体抗炎药的药代动力学
Clin Pharmacokinet. 1994 Feb;26(2):107-20. doi: 10.2165/00003088-199426020-00004.
2
The pharmacokinetics of piroxicam in elderly persons with and without renal impairment.吡罗昔康在有和没有肾功能损害的老年人中的药代动力学。
Br J Clin Pharmacol. 1994 Jan;37(1):1-5. doi: 10.1111/j.1365-2125.1994.tb04230.x.
3
Piroxicam and naproxen plasma concentrations in patients with osteoarthritis: relation to age, sex, efficacy and adverse events.

本文引用的文献

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Piroxicam: a review of its pharmacological properties and therapeutic efficacy.吡罗昔康:其药理特性与治疗效果综述
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Benoxaprofen.苯恶洛芬
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Defective N-oxidation of sparteine in man: a new pharmacogenetic defect.人司巴丁N-氧化缺陷:一种新的药物遗传学缺陷。
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