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色甘酸钠对地塞米松代谢的影响。

The effects of disodium cromoglycate on dexamethasome metabolism.

作者信息

Brooks S M, Sholiton L J, Altenau P

出版信息

Am Rev Respir Dis. 1976 Dec;114(6):1191-4. doi: 10.1164/arrd.1976.114.6.1191.

Abstract

The effect of disodium cromoglycate on dexamethasone metabolism was studied in 4 patients with bronchial asthma before and after 3 weeks of treatment. Labeled dexamethasome was injected intravenously and serial blood samples were collected during the next 6 hours. Transport kinetics of labeled dexamethasone were determined using a 2-compartment model. Baseline plasma equilibrated half-life values ranged from 133 to 258 min, and metabolic clearance rate ranged from 134 to 912 liter per day. After disodium cromoglycate therapy a small decrease in labeled dexamethasone clearance occurred. There was a mean increase in half-life of 20 min (9 per cent), being 201+/-51 (mean +/- SD) before therapy and 220+/-57 min after therapy. This was not significant. Metabolic clearance rate decreased 13 per cent (59 liter per day), being 441+/-334 liter per day before and 382+/-304 liter per day after treatment (P less than 0.05). Other transport kinetics of labeled dexamethasone were not significantly different with therapy. The results of this investigation demonstrate that disodium cromoglycate produces small but probably not significant changes in dexamethasone metabolism. The investigation supports the thesis that the steroid-sparing effect of disodium cromoglycate is not the result of depression of corticosteroid plasma clearance with longer duration of steroid action but most likely is the result of the effect of disodium cromoglycate on cellular mechanisms and inhibition of mediator release.

摘要

在4例支气管哮喘患者中,研究了色甘酸钠对其地塞米松代谢的影响,观察了治疗3周前后的变化。静脉注射标记地塞米松,并在随后6小时内采集系列血样。采用二室模型测定标记地塞米松的转运动力学。基线血浆平衡半衰期为133~258分钟,代谢清除率为每天134~912升。色甘酸钠治疗后,标记地塞米松清除率略有下降。半衰期平均增加20分钟(9%),治疗前为201±51(均值±标准差)分钟,治疗后为220±57分钟。此差异无统计学意义。代谢清除率下降13%(59升/天),治疗前为441±334升/天,治疗后为382±304升/天(P<0.05)。标记地塞米松的其他转运动力学参数在治疗前后无显著差异。本研究结果表明,色甘酸钠对皮质激素代谢有微小但可能无显著意义的改变。该研究支持以下论点:色甘酸钠的激素节省效应并非由于皮质激素血浆清除率降低及激素作用时间延长,而很可能是色甘酸钠对细胞机制及介质释放抑制作用的结果。

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