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茶碱的代谢产物3-甲基黄嘌呤对呼吸和心血管系统的影响。

Respiratory and cardiovascular effects of 3-methylxanthine, a metabolite of theophylline.

作者信息

Persson C G, Andersson K E

出版信息

Acta Pharmacol Toxicol (Copenh). 1977 Apr;40(4):529-36.

PMID:577111
Abstract

The effects of 3-methylxanthine (3-MX), a major metabolite of theophylline in man, were studied and compared with those of theophylline in isolated preparations of human and guinea-pig airways, isolated guinea-pig hearts, and in anaesthetized cats. 3-MX was pharmacologically active, producing effects similar to those of theophylline. The guinea-pig and human airways preparations were relaxed; the rate and force of contraction of guinea-pig hearts were increased. In anaesthetized cats, 3-MX decreased the respiratory overflow and arterial blood pressure, and increased the heart rate. Theophylline was always more potent (between 1 and 5 times) than 3-MX. It is suggested that 3-MX may contribute to the effects of theophylline during long-term treatment.

摘要

研究了氨茶碱在人体内的主要代谢产物3-甲基黄嘌呤(3-MX)的作用,并将其与氨茶碱在人及豚鼠气道离体标本、豚鼠离体心脏以及麻醉猫体内的作用进行了比较。3-MX具有药理活性,产生的作用与氨茶碱相似。豚鼠和人的气道标本舒张;豚鼠心脏的收缩速率和力量增加。在麻醉猫中,3-MX降低了呼吸溢出量和动脉血压,并增加了心率。氨茶碱的效力总是比3-MX强(1至5倍)。有人提出,在长期治疗期间,3-MX可能对氨茶碱的作用有贡献。

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引用本文的文献

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Nonlinear renal excretion of theophylline and its metabolites, 1-methyluric acid and 1,3-dimethyluric acid, in rats.大鼠体内茶碱及其代谢产物1-甲基尿酸和1,3-二甲基尿酸的非线性肾排泄
Arch Pharm Res. 1994 Apr;17(2):124-30. doi: 10.1007/BF02974236.
2
Hypoxia, arterial pH and theophylline disposition.缺氧、动脉血pH值与茶碱的处置
Clin Pharmacokinet. 1993 Oct;25(4):283-99. doi: 10.2165/00003088-199325040-00004.
3
Pharmacokinetics of enprofylline in patients with impaired renal function after a single intravenous dose.单次静脉给药后恩丙茶碱在肾功能受损患者中的药代动力学。
Eur J Clin Pharmacol. 1984;26(1):87-93. doi: 10.1007/BF00546714.
4
Pharmacokinetics of theophylline and its metabolites during acute renal failure. A case report.急性肾衰竭时茶碱及其代谢产物的药代动力学。病例报告。
Clin Pharmacokinet. 1991 Nov;21(5):400-8. doi: 10.2165/00003088-199121050-00007.
5
Clinical pharmacokinetics of theophylline.茶碱的临床药代动力学
Clin Pharmacokinet. 1978 Jul-Aug;3(4):267-93. doi: 10.2165/00003088-197803040-00002.