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慢性阿司匹林治疗期间水杨酸盐的代谢

Metabolism of salicylate during chronic aspirin therapy.

作者信息

Rumble R H, Brooks P M, Roberts M S

出版信息

Br J Clin Pharmacol. 1980 Jan;9(1):41-5. doi: 10.1111/j.1365-2125.1980.tb04794.x.

DOI:10.1111/j.1365-2125.1980.tb04794.x
PMID:7356892
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1429927/
Abstract
  1. The effects of chronic administration of aspirin in therapeutic doses (3.9 g/day) on plasma and salivary salicylate levels were studied in eight subjects. 2. The urinary excretion profile for free salicylic acid and metabolites of salicylate were examined. 3. Plasma and salivary salicylate levels declined significantly after peak levels were achieved between days 3 and 10. 4. The decline in plasma and salivary salicylate levels may be due to an induction of a metabolic pathway such as salicylurate formation (Furst, Gupta & Paulus, 1977). Only the mean fraction of salicylate excreted as salicylurate appears to increase with time during the present study, although the change was not significant statistically. 5. The decline in plasma and salivary salicylate levels during chronic therapy may lead to an apparent 'tolerance' of some rheumatoid patients to aspirin.
摘要
  1. 研究了八名受试者长期服用治疗剂量的阿司匹林(3.9克/天)对血浆和唾液中水杨酸盐水平的影响。2. 检测了游离水杨酸和水杨酸盐代谢产物的尿排泄情况。3. 在第3天至第10天达到峰值水平后,血浆和唾液中的水杨酸盐水平显著下降。4. 血浆和唾液中水杨酸盐水平的下降可能是由于诱导了一种代谢途径,如水杨尿酸的形成(Furst、Gupta和Paulus,1977年)。在本研究中,只有作为水杨尿酸排泄的水杨酸盐平均比例似乎随时间增加,尽管这一变化在统计学上并不显著。5. 长期治疗期间血浆和唾液中水杨酸盐水平的下降可能导致一些类风湿性关节炎患者对阿司匹林产生明显的“耐受性”。

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Metabolism of salicylate during chronic aspirin therapy.慢性阿司匹林治疗期间水杨酸盐的代谢
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本文引用的文献

1
Determination of acetylsalicylic acid and salicylic acid in plasma.血浆中乙酰水杨酸和水杨酸的测定。
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Capacity-limited salicylurate formation during prolonged administration of aspirin to healthy human subjects.
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Drug biotransformation interactions in man. I. Mutual inhibition in glucuronide formation of salicylic acid and salicylamide in man.人体中的药物生物转化相互作用。I. 人体中水杨酸和水杨酰胺葡萄糖醛酸苷形成的相互抑制作用。
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Application of salivary salicylate data to biopharmaceutical studies of salicylates.唾液水杨酸数据在水杨酸盐生物制药研究中的应用。
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Salicylate accumulation kinetics in man.人体中水杨酸盐的蓄积动力学
N Engl J Med. 1972 Aug 31;287(9):430-2. doi: 10.1056/NEJM197208312870903.
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Limited capacity for salicyl phenolic glucuronide formation and its effect on the kinetics of salicylate elimination in man.
Clin Pharmacol Ther. 1972 Mar-Apr;13(2):258-68. doi: 10.1002/cpt1972132258.
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Pharmacokinetics of tolbutamide: prediction by concentration in saliva.甲苯磺丁脲的药代动力学:通过唾液浓度进行预测。
Clin Pharmacol Ther. 1974 Dec;16(6):1052-8. doi: 10.1002/cpt19741661052.
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Relationship between dose and apparent volume of distribution of salicylate in children.儿童水杨酸盐剂量与表观分布容积之间的关系。
Pediatrics. 1974 Dec;54(6):713-7.
10
Patterns of plasma concentrations and urinary excretion of salicylate in rheumatoid arthritis.
Clin Pharmacol Ther. 1977 Oct;22(4):410-20. doi: 10.1002/cpt1977224410.